Synthesis of silver nanoparticles from a Desmodium adscendens extract and its antibacterial evaluation on wound dressing material
- Lakkakula, Jaya R, Ndinteh, Derek T, van Vuuren, Sandy F, Olivier, Denise K, Krause, Rui W M
- Authors: Lakkakula, Jaya R , Ndinteh, Derek T , van Vuuren, Sandy F , Olivier, Denise K , Krause, Rui W M
- Date: 2017
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195025 , vital:45520 , xlink:href="https://doi.org/10.1049/iet-nbt.2017.0084"
- Description: The one-pot synthesis of silver nanoparticles (AgNPs) using the medium-polar extract of Desmodium adscendens (Sw.) DC. is presented here as an alternative synthesis of metal NPs. Characterisation of the formed NPs showed polydispersed AgNPs ranging from 15 to 100 nm where the concentration of metal ions was found to play a role in the size and shape of the prepared NPs. It could be established that the flavonoids, saponins, and alkaloids present in the extract acted as both reducing and stabilising agents during the formation of the capped metal NPs. This means of NP synthesis was also employed during the in situ immobilisation of AgNPs on gauze and plaster. An evaluation of the antibacterial activity of the medium-polar D. adscendens extract, AgNPs suspended in solution, and the immobilised AgNPs against Staphylococcus aureus (ATCC 25923), Bacillus cereus (ATCC 11778), and Escherichia coli (ATCC 25922) showed high efficacy against the latter in particular. This suggests that gauze, dilute silver nitrate solutions, and D. adscendens extract could be used successfully in the simple in situ preparation of effective antibacterial wound dressings.
- Full Text:
- Date Issued: 2017
- Authors: Lakkakula, Jaya R , Ndinteh, Derek T , van Vuuren, Sandy F , Olivier, Denise K , Krause, Rui W M
- Date: 2017
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195025 , vital:45520 , xlink:href="https://doi.org/10.1049/iet-nbt.2017.0084"
- Description: The one-pot synthesis of silver nanoparticles (AgNPs) using the medium-polar extract of Desmodium adscendens (Sw.) DC. is presented here as an alternative synthesis of metal NPs. Characterisation of the formed NPs showed polydispersed AgNPs ranging from 15 to 100 nm where the concentration of metal ions was found to play a role in the size and shape of the prepared NPs. It could be established that the flavonoids, saponins, and alkaloids present in the extract acted as both reducing and stabilising agents during the formation of the capped metal NPs. This means of NP synthesis was also employed during the in situ immobilisation of AgNPs on gauze and plaster. An evaluation of the antibacterial activity of the medium-polar D. adscendens extract, AgNPs suspended in solution, and the immobilised AgNPs against Staphylococcus aureus (ATCC 25923), Bacillus cereus (ATCC 11778), and Escherichia coli (ATCC 25922) showed high efficacy against the latter in particular. This suggests that gauze, dilute silver nitrate solutions, and D. adscendens extract could be used successfully in the simple in situ preparation of effective antibacterial wound dressings.
- Full Text:
- Date Issued: 2017
Composite polyester membranes with embedded dendrimer hosts and bimetallic Fe/Ni nanoparticles: synthesis, characterisation and application to water treatment
- Malinga, S P, Arotiba, O A, Mapolie, S F, Krause, Rui W M, Diallo, M S, Mamba, Bhekie B
- Authors: Malinga, S P , Arotiba, O A , Mapolie, S F , Krause, Rui W M , Diallo, M S , Mamba, Bhekie B
- Date: 1968
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123619 , vital:35465 , https://doi.org/10.1007/s11051-013-1698-y
- Description: This study describes the preparation, characterization and evaluation of new composite membranes with embedded dendrimer hosts and Fe/Ni nanoparticles. These new reactive membranes consist of films of cyclodextrin–poly(propyleneimine) dendrimers (β-CD–PPI) that are deposited onto commercial polysulfone microporous supports and crosslinked with trimesoyl chloride (TMC). The membranes were subsequently loaded with Fe/Ni nanoparticles and evaluated as separation/reactive media in aqueous solutions using 2,4,6-trichlorophenol as model pollutant. The morphology and physicochemical properties of the composite membranes were characterised using high-resolution transmission electron microscopy (HR-TEM), atomic force microscopy and measurements of contact angle, water intake, porosity and water permeability. The sorption capacity and catalytic activity of the membranes were evaluated using ion chromatography, atmospheric pressure chemical ionisation-mass spectrometry and UV–Vis spectroscopy (UV–Vis). The sizes of the embedded Fe/Ni nanoparticles in the membranes ranged from 40 to 66 nm as confirmed by HR-TEM. The reaction rates for the dechlorination of 2,4,6-trichlorophenol ranged from 0.00148 to 0.00250 min−1. In all cases, we found that the reaction by-products consisted of chloride ions and mixtures of compounds including phenol (m/z = 93), 2,4-dichlorophenol (m/z = 163) and 4-chlorophenol (m/z = 128). The overall results of this study suggest that β-CD–PPI dendrimers are promising building blocks for the synthesis of composite and reactive membranes for the efficient removal of chlorinated organic pollutants from water.
- Full Text:
- Date Issued: 1968
- Authors: Malinga, S P , Arotiba, O A , Mapolie, S F , Krause, Rui W M , Diallo, M S , Mamba, Bhekie B
- Date: 1968
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123619 , vital:35465 , https://doi.org/10.1007/s11051-013-1698-y
- Description: This study describes the preparation, characterization and evaluation of new composite membranes with embedded dendrimer hosts and Fe/Ni nanoparticles. These new reactive membranes consist of films of cyclodextrin–poly(propyleneimine) dendrimers (β-CD–PPI) that are deposited onto commercial polysulfone microporous supports and crosslinked with trimesoyl chloride (TMC). The membranes were subsequently loaded with Fe/Ni nanoparticles and evaluated as separation/reactive media in aqueous solutions using 2,4,6-trichlorophenol as model pollutant. The morphology and physicochemical properties of the composite membranes were characterised using high-resolution transmission electron microscopy (HR-TEM), atomic force microscopy and measurements of contact angle, water intake, porosity and water permeability. The sorption capacity and catalytic activity of the membranes were evaluated using ion chromatography, atmospheric pressure chemical ionisation-mass spectrometry and UV–Vis spectroscopy (UV–Vis). The sizes of the embedded Fe/Ni nanoparticles in the membranes ranged from 40 to 66 nm as confirmed by HR-TEM. The reaction rates for the dechlorination of 2,4,6-trichlorophenol ranged from 0.00148 to 0.00250 min−1. In all cases, we found that the reaction by-products consisted of chloride ions and mixtures of compounds including phenol (m/z = 93), 2,4-dichlorophenol (m/z = 163) and 4-chlorophenol (m/z = 128). The overall results of this study suggest that β-CD–PPI dendrimers are promising building blocks for the synthesis of composite and reactive membranes for the efficient removal of chlorinated organic pollutants from water.
- Full Text:
- Date Issued: 1968
Anti-cancer and anti-trypanosomal properties of alkaloids from the root bark of Zanthoxylum leprieurii Guill and Perr
- Eze, Fabian I, Siwe-Noundou, Xavier, Isaacs, Michelle, Patala, Srivinas, Osadebe, Patience O, Krause, Rui W M
- Authors: Eze, Fabian I , Siwe-Noundou, Xavier , Isaacs, Michelle , Patala, Srivinas , Osadebe, Patience O , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193352 , vital:45324 , xlink:href="http://dx.doi.org/10.4314/tjpr.v19i11.19"
- Description: Purpose: To isolate the anti-cancer and anti-trypanosomal principles of Zanthoxylum leprieurii, a medicinally versatile wild tropical plant used for managing tumours, African trypanosomiasis, and inflammation in southeastern Nigeria. Methods: The pure compounds were isolated using chromatographic methods. The structural elucidation of the pure compounds was based on their NMR (1D and 2D) and mass spectral data as well as chemical test results. Structure-activity relationships were based on the structural differences among the compounds. The cytotoxicity of the extracts and compounds (1, 2, 3, and 4) was evaluated in HeLa (human cervix adenocarcinoma) cell line while the trypanocidal activities were evaluated on Trypanosoma brucei brucei. Results: Two acridone alkaloids, 1-hydroxy-3-methoxy-10-methylacridin-9 (10H)-one, named fabiocinine (1), and 1-hydroxy-2,3-dimethoxy-10-methylacridin-9 (10H)-one (arborinine, 2), together with a furoquinoline alkaloid, skimmianine (3), and a chelerythrine derivative, 6-acetonyl-5,6-dihydrochelerythrine (4) were isolated from the root bark of Zanthoxylum leprieurii. Skimmianine (3) exhibited cytotoxicity and anti-trypanosomal IC50 of 12.8 and 13.2 µg/mL respectively (p less than 0.05). Compound (1) and arborinine (2) were selectively cytotoxic to HeLa cells with cytotoxicity IC50 of 28.49 and 62.71 µg/mL, respectively, while (4) did not show significant activity (p less than 0.05). Conclusion: Zanthoxylum leprieurii root bark contains cytotoxic and trypanocidal compounds, and is thus a potential source of anti-cancer and anti-trypanosomal leads.
- Full Text:
- Date Issued: 2020
- Authors: Eze, Fabian I , Siwe-Noundou, Xavier , Isaacs, Michelle , Patala, Srivinas , Osadebe, Patience O , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193352 , vital:45324 , xlink:href="http://dx.doi.org/10.4314/tjpr.v19i11.19"
- Description: Purpose: To isolate the anti-cancer and anti-trypanosomal principles of Zanthoxylum leprieurii, a medicinally versatile wild tropical plant used for managing tumours, African trypanosomiasis, and inflammation in southeastern Nigeria. Methods: The pure compounds were isolated using chromatographic methods. The structural elucidation of the pure compounds was based on their NMR (1D and 2D) and mass spectral data as well as chemical test results. Structure-activity relationships were based on the structural differences among the compounds. The cytotoxicity of the extracts and compounds (1, 2, 3, and 4) was evaluated in HeLa (human cervix adenocarcinoma) cell line while the trypanocidal activities were evaluated on Trypanosoma brucei brucei. Results: Two acridone alkaloids, 1-hydroxy-3-methoxy-10-methylacridin-9 (10H)-one, named fabiocinine (1), and 1-hydroxy-2,3-dimethoxy-10-methylacridin-9 (10H)-one (arborinine, 2), together with a furoquinoline alkaloid, skimmianine (3), and a chelerythrine derivative, 6-acetonyl-5,6-dihydrochelerythrine (4) were isolated from the root bark of Zanthoxylum leprieurii. Skimmianine (3) exhibited cytotoxicity and anti-trypanosomal IC50 of 12.8 and 13.2 µg/mL respectively (p less than 0.05). Compound (1) and arborinine (2) were selectively cytotoxic to HeLa cells with cytotoxicity IC50 of 28.49 and 62.71 µg/mL, respectively, while (4) did not show significant activity (p less than 0.05). Conclusion: Zanthoxylum leprieurii root bark contains cytotoxic and trypanocidal compounds, and is thus a potential source of anti-cancer and anti-trypanosomal leads.
- Full Text:
- Date Issued: 2020
Secondary metabolites from Tetracera potatoria stem bark with anti-mycobacterial activity.
- Fomogne-Fodjo, M C Y, Ndinteh, Derek T, Olivier, D K, Krause, Rui W M, Kempgens, Pierre, Van Vuuren, S
- Authors: Fomogne-Fodjo, M C Y , Ndinteh, Derek T , Olivier, D K , Krause, Rui W M , Kempgens, Pierre , Van Vuuren, S
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125556 , vital:35795 , https://doi.org/10.1016/j.jep.2016.11.027
- Description: Ethnopharmacological relevance Tetracera potatoria Afzel. Exg. Don (Dilleniaceae) is a medicinal plant used traditionally in Africa for the treatment of tuberculosis related ailments and respiratory infections. The antibacterial activity of the medium polar extracts of T. potatoria leaves and stem bark was recently reported against Mycobacterium smegmatis (MIC 25 µg/mL) and M. aurum (65 µg/mL), two fast-growing Mycobacterium strains used as model micro-organisms for the more pathogenic strain Mycobacterium tuberculosis (Fomogne-Fodjo et al., 2014). The aim of this study was consequently to isolate the compounds possibly contributing to this activity, and which may therefore be promising precursors to be used for the development of novel anti-TB drugs.
- Full Text:
- Date Issued: 2017
- Authors: Fomogne-Fodjo, M C Y , Ndinteh, Derek T , Olivier, D K , Krause, Rui W M , Kempgens, Pierre , Van Vuuren, S
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125556 , vital:35795 , https://doi.org/10.1016/j.jep.2016.11.027
- Description: Ethnopharmacological relevance Tetracera potatoria Afzel. Exg. Don (Dilleniaceae) is a medicinal plant used traditionally in Africa for the treatment of tuberculosis related ailments and respiratory infections. The antibacterial activity of the medium polar extracts of T. potatoria leaves and stem bark was recently reported against Mycobacterium smegmatis (MIC 25 µg/mL) and M. aurum (65 µg/mL), two fast-growing Mycobacterium strains used as model micro-organisms for the more pathogenic strain Mycobacterium tuberculosis (Fomogne-Fodjo et al., 2014). The aim of this study was consequently to isolate the compounds possibly contributing to this activity, and which may therefore be promising precursors to be used for the development of novel anti-TB drugs.
- Full Text:
- Date Issued: 2017
Flavonoids from the Genus Euphorbia
- Magozwi, Douglas K, Dinala, Mmabatho, Mokwana, Nthabiseng, Siwe-Noundou, Xavier, Krause, Rui W M, Sonopo, Molahleli, McGaw, Lyndy J, Augustyn, Wilma A, Tembu, Vuyelwa J
- Authors: Magozwi, Douglas K , Dinala, Mmabatho , Mokwana, Nthabiseng , Siwe-Noundou, Xavier , Krause, Rui W M , Sonopo, Molahleli , McGaw, Lyndy J , Augustyn, Wilma A , Tembu, Vuyelwa J
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/191736 , vital:45159 , xlink:href="https://doi.org/10.3390/ph14050428"
- Description: Plants of the genus Euphorbia are widely distributed across temperate, tropical and subtropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure–activity relationship of Euphorbia flavonoids for the period covering 2000–2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells. Of the investigated species, over 80 different types of flavonoids have been isolated to date. Most of the isolated flavonoids were flavonols and comprised simple O-substitution patterns, C-methylation and prenylation. Others had a glycoside, glycosidic linkages and a carbohydrate attached at either C-3 or C-7, and were designated as d-glucose, l-rhamnose or glucorhamnose. The structure–activity relationship studies showed that methylation of the hydroxyl groups on C-3 or C-7 reduces the activities while glycosylation loses the activity and that the parent skeletal structure is essential in retaining the activity. These constituents can therefore offer potential alternative scaffolds towards development of new Euphorbia-based therapeutic agents.
- Full Text:
- Date Issued: 2021
- Authors: Magozwi, Douglas K , Dinala, Mmabatho , Mokwana, Nthabiseng , Siwe-Noundou, Xavier , Krause, Rui W M , Sonopo, Molahleli , McGaw, Lyndy J , Augustyn, Wilma A , Tembu, Vuyelwa J
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/191736 , vital:45159 , xlink:href="https://doi.org/10.3390/ph14050428"
- Description: Plants of the genus Euphorbia are widely distributed across temperate, tropical and subtropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure–activity relationship of Euphorbia flavonoids for the period covering 2000–2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells. Of the investigated species, over 80 different types of flavonoids have been isolated to date. Most of the isolated flavonoids were flavonols and comprised simple O-substitution patterns, C-methylation and prenylation. Others had a glycoside, glycosidic linkages and a carbohydrate attached at either C-3 or C-7, and were designated as d-glucose, l-rhamnose or glucorhamnose. The structure–activity relationship studies showed that methylation of the hydroxyl groups on C-3 or C-7 reduces the activities while glycosylation loses the activity and that the parent skeletal structure is essential in retaining the activity. These constituents can therefore offer potential alternative scaffolds towards development of new Euphorbia-based therapeutic agents.
- Full Text:
- Date Issued: 2021
Synthesis of pH sensitive dual capped CdTe QDs: their optical properties and structural morphology
- Daramola, Olamide A, Noundou, Xavier S, Nkanga, Christian I, Tseki, Potlaki F, Krause, Rui W M
- Authors: Daramola, Olamide A , Noundou, Xavier S , Nkanga, Christian I , Tseki, Potlaki F , Krause, Rui W M
- Date: 2020
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/156364 , vital:39983 , https://doi.org/10.1007/s10895-020-02526-x
- Description: We herein report five different types of thiol dual capped cadmium tellurite quantum dots (CdTe QDs) namely glutathionemercapto-propanoic acid (QD 1), glutathione-thiolglycolic acid (QD 2), L-cysteine-mercapto-propanoic acid (QD 3), L-cysteinethiol-glycolic acid (QD 4) and mercapto-propanoic acid-thiol-glycolic (QD 5). Dual-capped CdTe QDs were prepared using a one pot synthetic method. Cadmium acetate and sodium tellurite were respectively used as cadmium and tellurium precursors. Photo-physical properties of the synthesized QDs were examined using UV-Vis and photoluminescence spectroscopy while structural characterization was performed by means of transmission electron microscopy (TEM) and Fourier transform infrared (FTIR) spectroscopy.
- Full Text:
- Date Issued: 2020
- Authors: Daramola, Olamide A , Noundou, Xavier S , Nkanga, Christian I , Tseki, Potlaki F , Krause, Rui W M
- Date: 2020
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/156364 , vital:39983 , https://doi.org/10.1007/s10895-020-02526-x
- Description: We herein report five different types of thiol dual capped cadmium tellurite quantum dots (CdTe QDs) namely glutathionemercapto-propanoic acid (QD 1), glutathione-thiolglycolic acid (QD 2), L-cysteine-mercapto-propanoic acid (QD 3), L-cysteinethiol-glycolic acid (QD 4) and mercapto-propanoic acid-thiol-glycolic (QD 5). Dual-capped CdTe QDs were prepared using a one pot synthetic method. Cadmium acetate and sodium tellurite were respectively used as cadmium and tellurium precursors. Photo-physical properties of the synthesized QDs were examined using UV-Vis and photoluminescence spectroscopy while structural characterization was performed by means of transmission electron microscopy (TEM) and Fourier transform infrared (FTIR) spectroscopy.
- Full Text:
- Date Issued: 2020
Simultaneous liposomal encapsulation of antibiotics and proteins: co-loading and characterization of rifampicin and Human Serum Albumin in soy-liposomes
- Bapolisi, Alain M, Nkanga, Christian I, Walker, Roderick B, Krause, Rui W M
- Authors: Bapolisi, Alain M , Nkanga, Christian I , Walker, Roderick B , Krause, Rui W M
- Date: 2020
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/148617 , vital:38755 , https://doi.org/10.1016/j.jddst.2020.101751
- Description: The recurrent development of resistance to antimicrobial agents threatens the ability for successful treatment of infectious diseases. Hydrophobic antibiotics such as rifampicin (Rif) are particularly affected due to poor bioavailability. On the other hand, proteins play important roles in drug delivery and release. Further, the combination of antimicrobials with therapeutic proteins and their encapsulation in liposomes seems a promising approach for improvement of antimicrobial efficacy. This study aimed to encapsulate Rif simultaneously with a large protein, Human Serum Albumin (HSA) in liposomes made from an inexpensive crude soy lecithin (CSL).
- Full Text:
- Date Issued: 2020
- Authors: Bapolisi, Alain M , Nkanga, Christian I , Walker, Roderick B , Krause, Rui W M
- Date: 2020
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/148617 , vital:38755 , https://doi.org/10.1016/j.jddst.2020.101751
- Description: The recurrent development of resistance to antimicrobial agents threatens the ability for successful treatment of infectious diseases. Hydrophobic antibiotics such as rifampicin (Rif) are particularly affected due to poor bioavailability. On the other hand, proteins play important roles in drug delivery and release. Further, the combination of antimicrobials with therapeutic proteins and their encapsulation in liposomes seems a promising approach for improvement of antimicrobial efficacy. This study aimed to encapsulate Rif simultaneously with a large protein, Human Serum Albumin (HSA) in liposomes made from an inexpensive crude soy lecithin (CSL).
- Full Text:
- Date Issued: 2020
Polyurethane composite adsorbent using solid phase extraction method for preconcentration of metal ion from aqueous solution
- Olorundare, O F, Msagati, T A M, Okonkwo, J O, Krause, Rui W M, Mamba, Bhekie B
- Authors: Olorundare, O F , Msagati, T A M , Okonkwo, J O , Krause, Rui W M , Mamba, Bhekie B
- Date: 2015
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125386 , vital:35778 , https://doi.org/10.1007/s13762-014-0645-5
- Description: Polyurethane composite adsorbent polymeric material was prepared and investigated for selected solid-phase extraction for metal ions, prior to its determination by inductively coupled plasma optical emission spectrometry. The surface characterisation was done using Fourier transform infrared spectroscopy. The separation and preconcentration conditions of the analytes investigated includes influence of pH, sample loading flow rate, elution flow rate, type and concentration of eluents. The optimum pH for the highest efficient recoveries for all metal ions, which ranged from 70 to 85 %, is pH 7. The metal ions were quantitatively eluted with 5 mL of 2 mol/L HNO3. Common coexisting ions did not interfere with the separation. The percentage recovery of the metal ions ranged between 70 and 89 %, while the results for the limit of detection and limit of quantification ranged from 0.249 to 0.256 and 0.831 to 0.855, respectively. The experimental tests showed good preconcentration results of trace levels of metal ions using synthesised polyurethane polymer adsorbent composite.
- Full Text:
- Date Issued: 2015
- Authors: Olorundare, O F , Msagati, T A M , Okonkwo, J O , Krause, Rui W M , Mamba, Bhekie B
- Date: 2015
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125386 , vital:35778 , https://doi.org/10.1007/s13762-014-0645-5
- Description: Polyurethane composite adsorbent polymeric material was prepared and investigated for selected solid-phase extraction for metal ions, prior to its determination by inductively coupled plasma optical emission spectrometry. The surface characterisation was done using Fourier transform infrared spectroscopy. The separation and preconcentration conditions of the analytes investigated includes influence of pH, sample loading flow rate, elution flow rate, type and concentration of eluents. The optimum pH for the highest efficient recoveries for all metal ions, which ranged from 70 to 85 %, is pH 7. The metal ions were quantitatively eluted with 5 mL of 2 mol/L HNO3. Common coexisting ions did not interfere with the separation. The percentage recovery of the metal ions ranged between 70 and 89 %, while the results for the limit of detection and limit of quantification ranged from 0.249 to 0.256 and 0.831 to 0.855, respectively. The experimental tests showed good preconcentration results of trace levels of metal ions using synthesised polyurethane polymer adsorbent composite.
- Full Text:
- Date Issued: 2015
pH-Dependent release of isoniazid from isonicotinic acid (4-hydroxy-benzylidene)-hydrazide loaded liposomes
- Nkanga, Christian I, Tor-Anyiin, Terrumun A, Igoli, John O, Noundou, Xavier S, Krause, Rui W M
- Authors: Nkanga, Christian I , Tor-Anyiin, Terrumun A , Igoli, John O , Noundou, Xavier S , Krause, Rui W M
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126427 , vital:35884 , https://doi.org/10.9734/AJOCS/2017/37147
- Description: Liposomes are considered as potential vehicles for the delivery of anti-tuberculosis drugs (ATBD) due to their rapid uptake by alveolar macrophages, where the mycobacterium often resides. This may provide macrophage-targeting effects that would be key to site specific ATBD delivery using pH-sensitive liposomes, considering the pH-gradient found in the phagocytotic pathway. In this study, isoniazid (INH) was conjugated to 4-hydroxy-benzaldehyde via a hydrazone bond to yield isonicotinic acid (4-hydroxy-benzylidene)-hydrazide (INH-HB). This conjugate was encapsulated in crude soybean lecithin liposomes using film hydration method. INH-HB loaded liposomes (IHL) were characterized by means of dynamic light scattering, transmission electron microscopy, differential scanning calorimetry and X-ray diffraction. The release of INH from IHL was evaluated in media of different pH using a dialysis method. The particle size, Zeta Potential and encapsulation efficiency of IHL were about 945 nm, −62 mV and 89% respectively. In media of pH 7.4, 6.4, 5.4 and 4.4; the IHL exhibited respectively 22, 69, 83 and 100% of release over 12 h. In addition to possible targeted delivery, this pH-dependent release behavior may be suitable for minimizing the loss of INH by leakage from liposomes. The characteristics of IHL are promising for potential site-specific delivery of ATBD.
- Full Text:
- Date Issued: 2018
- Authors: Nkanga, Christian I , Tor-Anyiin, Terrumun A , Igoli, John O , Noundou, Xavier S , Krause, Rui W M
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126427 , vital:35884 , https://doi.org/10.9734/AJOCS/2017/37147
- Description: Liposomes are considered as potential vehicles for the delivery of anti-tuberculosis drugs (ATBD) due to their rapid uptake by alveolar macrophages, where the mycobacterium often resides. This may provide macrophage-targeting effects that would be key to site specific ATBD delivery using pH-sensitive liposomes, considering the pH-gradient found in the phagocytotic pathway. In this study, isoniazid (INH) was conjugated to 4-hydroxy-benzaldehyde via a hydrazone bond to yield isonicotinic acid (4-hydroxy-benzylidene)-hydrazide (INH-HB). This conjugate was encapsulated in crude soybean lecithin liposomes using film hydration method. INH-HB loaded liposomes (IHL) were characterized by means of dynamic light scattering, transmission electron microscopy, differential scanning calorimetry and X-ray diffraction. The release of INH from IHL was evaluated in media of different pH using a dialysis method. The particle size, Zeta Potential and encapsulation efficiency of IHL were about 945 nm, −62 mV and 89% respectively. In media of pH 7.4, 6.4, 5.4 and 4.4; the IHL exhibited respectively 22, 69, 83 and 100% of release over 12 h. In addition to possible targeted delivery, this pH-dependent release behavior may be suitable for minimizing the loss of INH by leakage from liposomes. The characteristics of IHL are promising for potential site-specific delivery of ATBD.
- Full Text:
- Date Issued: 2018
Rapid Synthesis of Thiol-Co-Capped-CdTe/CdSe/ZnSe Core Shell-Shell Nanoparticles
- Daramola, Olamide, Siwe-Noundou, Xavier, Tseki, Potlaki, Krause, Rui W M
- Authors: Daramola, Olamide , Siwe-Noundou, Xavier , Tseki, Potlaki , Krause, Rui W M
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/191758 , vital:45161 , xlink:href="https://doi.org/10.3390/nano11051193"
- Description: CdTe QDs has been demonstrated in many studies to possess good outstanding optical and photo-physical properties. However, it has been established from literature that the toxic Cd2+ that tends to leak out into nearby solutions can be protected by less toxic ZnS or ZnSe shells leading to the synthesis of core-shells and multi-core-shells. Hence, this has allowed the synthesis of CdTe multi-core-shells to have gained much interest. The preparation of most CdTe multi-core-shells reported from various studies usually has a longer reaction time (6–24 h) in reaching their highest emission maxima. The synthesis of CdTe multi-core-shells in this study only took 35 min to obtain a highest emission maximum compared to what has been reported from the literature. CdTe multi-core-shells were synthesized by injecting 7, 14, and 21 mL each of Zn complex solution and Se ions into the reacting mixture containing CdTe core-shells (3 h) at 5 min intervals over a 35 min reaction time. The emission maxima of the MPA-TGA-CdTe multi-core-shells at 21 mL injection was recorded around 625 nm. Therefore, we are reporting the rapid synthesis of five different thiol co-capped CdTe/CdSe/ZnSe multi-core-shell QDs with the highest emission maxima obtained at 35 min reaction time.
- Full Text:
- Date Issued: 2021
- Authors: Daramola, Olamide , Siwe-Noundou, Xavier , Tseki, Potlaki , Krause, Rui W M
- Date: 2021
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/191758 , vital:45161 , xlink:href="https://doi.org/10.3390/nano11051193"
- Description: CdTe QDs has been demonstrated in many studies to possess good outstanding optical and photo-physical properties. However, it has been established from literature that the toxic Cd2+ that tends to leak out into nearby solutions can be protected by less toxic ZnS or ZnSe shells leading to the synthesis of core-shells and multi-core-shells. Hence, this has allowed the synthesis of CdTe multi-core-shells to have gained much interest. The preparation of most CdTe multi-core-shells reported from various studies usually has a longer reaction time (6–24 h) in reaching their highest emission maxima. The synthesis of CdTe multi-core-shells in this study only took 35 min to obtain a highest emission maximum compared to what has been reported from the literature. CdTe multi-core-shells were synthesized by injecting 7, 14, and 21 mL each of Zn complex solution and Se ions into the reacting mixture containing CdTe core-shells (3 h) at 5 min intervals over a 35 min reaction time. The emission maxima of the MPA-TGA-CdTe multi-core-shells at 21 mL injection was recorded around 625 nm. Therefore, we are reporting the rapid synthesis of five different thiol co-capped CdTe/CdSe/ZnSe multi-core-shell QDs with the highest emission maxima obtained at 35 min reaction time.
- Full Text:
- Date Issued: 2021
Cyclodextrin grafted calcium carbonate vaterite particles: efficient system for tailored release of hydrophobic anticancer or hormone drugs
- Lakkakula, Jaya R, Kurapati, Rajendra, Tynga, Ivan, Krause, Rui W M, Abrahamse, Heidi, Raichur, Ashok M
- Authors: Lakkakula, Jaya R , Kurapati, Rajendra , Tynga, Ivan , Krause, Rui W M , Abrahamse, Heidi , Raichur, Ashok M
- Date: 2016
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125435 , vital:35783 , https://doi.org/10.1039/C6RA12951J
- Description: Porous CaCO3 microparticles have been used earlier for sustained drug release of hydrophilic drugs but have certain drawbacks for use with hydrophobic drugs. Hence, to overcome these drawbacks, a novel composite of CaCO3 along with cyclodextrin (CD–CaCO3) for the delivery of hydrophobic drugs was developed. Cyclodextrins (CDs), when incorporated within CaCO3, increased the porosity and surface area of microparticles thereby enhancing the encapsulation efficiency of hydrophobic drugs (5-Fluorouracil or Na-L-thyroxine) by forming inclusion complexes with cyclodextrin. Thermogravimetric and FTIR studies confirmed the interaction between the cyclodextrin and CaCO3 microparticles. Raman spectra confirmed the peak of vaterite crystals before and after loading of hydrophobic drugs within the composite. In vitro release studies when performed at pH 4.8 (5-Fu) and pH 1.2 (Na-L-thy) showed release at low pH as CaCO3 is soluble at acidic pH unlike slower release at basic pH. Release kinetics followed a Higuchi kinetic model at pH 4.8 (5-Fu) and pH 1.2 (Na-L-thy) respectively.
- Full Text:
- Date Issued: 2016
- Authors: Lakkakula, Jaya R , Kurapati, Rajendra , Tynga, Ivan , Krause, Rui W M , Abrahamse, Heidi , Raichur, Ashok M
- Date: 2016
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125435 , vital:35783 , https://doi.org/10.1039/C6RA12951J
- Description: Porous CaCO3 microparticles have been used earlier for sustained drug release of hydrophilic drugs but have certain drawbacks for use with hydrophobic drugs. Hence, to overcome these drawbacks, a novel composite of CaCO3 along with cyclodextrin (CD–CaCO3) for the delivery of hydrophobic drugs was developed. Cyclodextrins (CDs), when incorporated within CaCO3, increased the porosity and surface area of microparticles thereby enhancing the encapsulation efficiency of hydrophobic drugs (5-Fluorouracil or Na-L-thyroxine) by forming inclusion complexes with cyclodextrin. Thermogravimetric and FTIR studies confirmed the interaction between the cyclodextrin and CaCO3 microparticles. Raman spectra confirmed the peak of vaterite crystals before and after loading of hydrophobic drugs within the composite. In vitro release studies when performed at pH 4.8 (5-Fu) and pH 1.2 (Na-L-thy) showed release at low pH as CaCO3 is soluble at acidic pH unlike slower release at basic pH. Release kinetics followed a Higuchi kinetic model at pH 4.8 (5-Fu) and pH 1.2 (Na-L-thy) respectively.
- Full Text:
- Date Issued: 2016
Synthesis and characterization of novel zinc phthalocyanines as potential photosensitizers for photodynamic therapy of cancers
- Moeno, Sharon, Ermilov, E A, Kuzyniak, W, Höpfner, M, Krause, Rui W M
- Authors: Moeno, Sharon , Ermilov, E A , Kuzyniak, W , Höpfner, M , Krause, Rui W M
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123673 , vital:35471 , https://doi.org/10.1039/C3PP50393C
- Description: Two novel zinc phthalocyanines (Pcs): tetramethyl tetrakis-2,(3)-[(4-methyl-2-pyridyloxy)phthalocyaninato] zinc(II) (4) and (the negatively charged form) tetrakis-2,(3)-[(3-carboxylicacid-6-sulfanylpyridine)phthalocyaninato] zinc(II) (5), water soluble by virtue of their ionic substituent groups were synthesized. The spectroscopic properties of both compounds were determined and their photodynamic activities were investigated in a human tumor cell model. In aqueous media the two peripherally substituted water soluble Pcs are highly aggregated. The phototoxic activity of the two novel Pcs (Pc 4 and Pc 5; 0–20 μM) was shown to be time- and dose-dependent in human pancreatic carcinoid BON cells, leading to a reduction of tumor cells of >80% compared to the controls. The effectiveness of the treatment appeared to be attenuated by the aggregation of Pcs under aqueous conditions. Interestingly, even those cells that were not immediately killed by the photoactivated photosensitizer seemed to be affected by the Pc photodynamic activity, as a single PDT induced long-lasting effects on cell survival. Even 4 days after PDT, the number of surviving cells did not re-increase or still dropped, as compared to control cells. The underlying mechanism of this observation has to be deciphered in future investigations.
- Full Text:
- Date Issued: 2014
- Authors: Moeno, Sharon , Ermilov, E A , Kuzyniak, W , Höpfner, M , Krause, Rui W M
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123673 , vital:35471 , https://doi.org/10.1039/C3PP50393C
- Description: Two novel zinc phthalocyanines (Pcs): tetramethyl tetrakis-2,(3)-[(4-methyl-2-pyridyloxy)phthalocyaninato] zinc(II) (4) and (the negatively charged form) tetrakis-2,(3)-[(3-carboxylicacid-6-sulfanylpyridine)phthalocyaninato] zinc(II) (5), water soluble by virtue of their ionic substituent groups were synthesized. The spectroscopic properties of both compounds were determined and their photodynamic activities were investigated in a human tumor cell model. In aqueous media the two peripherally substituted water soluble Pcs are highly aggregated. The phototoxic activity of the two novel Pcs (Pc 4 and Pc 5; 0–20 μM) was shown to be time- and dose-dependent in human pancreatic carcinoid BON cells, leading to a reduction of tumor cells of >80% compared to the controls. The effectiveness of the treatment appeared to be attenuated by the aggregation of Pcs under aqueous conditions. Interestingly, even those cells that were not immediately killed by the photoactivated photosensitizer seemed to be affected by the Pc photodynamic activity, as a single PDT induced long-lasting effects on cell survival. Even 4 days after PDT, the number of surviving cells did not re-increase or still dropped, as compared to control cells. The underlying mechanism of this observation has to be deciphered in future investigations.
- Full Text:
- Date Issued: 2014
Antibacterial effects of Alchornea cordifolia (Schumach. and Thonn.) Müll. Arg extracts and compounds on gastrointestinal, skin, respiratory and urinary tract pathogens
- Siwe-Noundou, Xavier, Krause, Rui W M, van Vuuren, Sandy, Tantoh Ndinteh, Derek, Olivier, D K
- Authors: Siwe-Noundou, Xavier , Krause, Rui W M , van Vuuren, Sandy , Tantoh Ndinteh, Derek , Olivier, D K
- Date: 2016
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195418 , vital:45563 , xlink:href="https://doi.org/10.1016/j.jep.2015.12.043"
- Description: Ethnopharmacological relevance:The leaves, stems and roots ofAlchornea cordifolia(Schumach. andThonn.) Müll. Arg. are used as traditional medicine in many African countries for the management ofgastrointestinal, respiratory and urinary tract infections as well as for the treatment of wounds.Aim of the study:To determine the in vitro antibacterial activity of the crude extracts of leaves and stemsofA. cordifoliaon gastrointestinal, skin, respiratory and urinary tract pathogens and to identify thecompounds in the extracts that may be responsible for this activity.Materials and methods:The antibacterial activities of crude extracts [hexane, chloroform (CHCl3), ethylacetate (EtOAc), ethanol (EtOH), methanol (MeOH) and water (H2O)] as well as pure compounds isolatedfrom these extracts were evaluated by means of the micro-dilution assay against four Gram-positivebacteria, i.e.Bacillus cereusATCC 11778,Enterococcus faecalisATCC 29212, Staphylococcus aureusATCC25923 andS. saprophyticusATCC 15305,as well as four Gram-negative bacterial strains, i.e.EscherichiacoliATCC 25922, Klebsiella pneumoniaeATCC 13883, Moraxella catarrhalisATCC 23246 andProteus mir-abilisATCC 43071. The isolation of the active constituents was undertaken by bio-autographic assays inconjunction with chromatographic techniques. The identification and characterisation of the isolatedcompounds were done using mass spectrometry (MS) and Fourier transformed infrared spectrometry(FTIR) as well as 1D- and 2D- nuclear magnetic resonance (NMR) analyses.Results:The leaves and stems ofA. cordifoliaexhibited varied antibacterial activity against all eight pa-thogens. Most of the MIC values ranged between 63 and 2000mg/ml. The highest activities for the crudeextracts (63mg/ml) were observed againstS. saprophyticus[stem (EtOAc, CHCl3and hexane), leaves(MeOH, EtOH, EtOAc and CHCl3)],E. coli[stem (MeOH and EtOH), leaves (MeOH, EtOH, EtOAc andCHCl3)],M. catarrhalis[leaves (EtOAc and CHCl3)],K. pneumoniae[stem (CHCl3), leaves (CHCl3)] andS.aureus[leaves (CHCl3)]. Seven constituents [stigmasterol (1), stigmasta-4,22-dien-3-one (2), friedelin (3),friedelane-3-one-28-al (4), 3-O-acetyl-aleuritolic acid (5), 3-O-acetyl-erythrodiol (6) and methyl-3,4,5-trihydroxybenzoate (methyl gallate) (7)] were isolated from the stem MeOH extract. All these com-pounds displayed some antibacterial activity against the eight pathogens with highest activity againstS.saprophyticus(2mg/ml). Furthermore, this is thefirst report of compounds1,2,3,4,6and7isolated fromA. cordifoliaand where a complete set of 2D-NMR data for fridelane-3-one-28-al (4) is presented.Conclusion:The study demonstrated that the antibacterial activities ofA. cordifoliaextracts may be dueto the presence of the seven isolated compounds, where compounds3–6showed the best activity. Theobserved activity against gastrointestinal, skin, respiratory and urinary tract pathogens supports thetraditional use for the treatment of such ailments.
- Full Text:
- Date Issued: 2016
- Authors: Siwe-Noundou, Xavier , Krause, Rui W M , van Vuuren, Sandy , Tantoh Ndinteh, Derek , Olivier, D K
- Date: 2016
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195418 , vital:45563 , xlink:href="https://doi.org/10.1016/j.jep.2015.12.043"
- Description: Ethnopharmacological relevance:The leaves, stems and roots ofAlchornea cordifolia(Schumach. andThonn.) Müll. Arg. are used as traditional medicine in many African countries for the management ofgastrointestinal, respiratory and urinary tract infections as well as for the treatment of wounds.Aim of the study:To determine the in vitro antibacterial activity of the crude extracts of leaves and stemsofA. cordifoliaon gastrointestinal, skin, respiratory and urinary tract pathogens and to identify thecompounds in the extracts that may be responsible for this activity.Materials and methods:The antibacterial activities of crude extracts [hexane, chloroform (CHCl3), ethylacetate (EtOAc), ethanol (EtOH), methanol (MeOH) and water (H2O)] as well as pure compounds isolatedfrom these extracts were evaluated by means of the micro-dilution assay against four Gram-positivebacteria, i.e.Bacillus cereusATCC 11778,Enterococcus faecalisATCC 29212, Staphylococcus aureusATCC25923 andS. saprophyticusATCC 15305,as well as four Gram-negative bacterial strains, i.e.EscherichiacoliATCC 25922, Klebsiella pneumoniaeATCC 13883, Moraxella catarrhalisATCC 23246 andProteus mir-abilisATCC 43071. The isolation of the active constituents was undertaken by bio-autographic assays inconjunction with chromatographic techniques. The identification and characterisation of the isolatedcompounds were done using mass spectrometry (MS) and Fourier transformed infrared spectrometry(FTIR) as well as 1D- and 2D- nuclear magnetic resonance (NMR) analyses.Results:The leaves and stems ofA. cordifoliaexhibited varied antibacterial activity against all eight pa-thogens. Most of the MIC values ranged between 63 and 2000mg/ml. The highest activities for the crudeextracts (63mg/ml) were observed againstS. saprophyticus[stem (EtOAc, CHCl3and hexane), leaves(MeOH, EtOH, EtOAc and CHCl3)],E. coli[stem (MeOH and EtOH), leaves (MeOH, EtOH, EtOAc andCHCl3)],M. catarrhalis[leaves (EtOAc and CHCl3)],K. pneumoniae[stem (CHCl3), leaves (CHCl3)] andS.aureus[leaves (CHCl3)]. Seven constituents [stigmasterol (1), stigmasta-4,22-dien-3-one (2), friedelin (3),friedelane-3-one-28-al (4), 3-O-acetyl-aleuritolic acid (5), 3-O-acetyl-erythrodiol (6) and methyl-3,4,5-trihydroxybenzoate (methyl gallate) (7)] were isolated from the stem MeOH extract. All these com-pounds displayed some antibacterial activity against the eight pathogens with highest activity againstS.saprophyticus(2mg/ml). Furthermore, this is thefirst report of compounds1,2,3,4,6and7isolated fromA. cordifoliaand where a complete set of 2D-NMR data for fridelane-3-one-28-al (4) is presented.Conclusion:The study demonstrated that the antibacterial activities ofA. cordifoliaextracts may be dueto the presence of the seven isolated compounds, where compounds3–6showed the best activity. Theobserved activity against gastrointestinal, skin, respiratory and urinary tract pathogens supports thetraditional use for the treatment of such ailments.
- Full Text:
- Date Issued: 2016
Nano-enabled liposomal mucoadhesive films for enhanced efavirenz buccal drug delivery
- Okafor, Nnamadi I, Ngoepe, Mpho, Siwe-Noundou, Xavier, Krause, Rui W M
- Authors: Okafor, Nnamadi I , Ngoepe, Mpho , Siwe-Noundou, Xavier , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194032 , vital:45417 , xlink:href="https://doi.org/10.1016/j.jddst.2019.101312"
- Description: Buccal films (BFs) were prepared using a solvent casting method using the liposomal suspension as the dispersing medium. Optimization of some physical properties of the films containing different amounts of polymers was done using digital Vernier calliper and digital weighing balance. The physiochemical properties of the best optimized properties were characterized using Differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier transfer infrared spectroscopy (FTIR), Transmission Electron Microscopy (TEM), Energy dispersive X-ray spectroscopy (EDS), and Scanning Electron Microscopy (SEM). Permeation study of the BFs composed of Carbopol (CP) alone and CP to Pluronic 127 (PF127) demonstrated better bio-adhesive properties than the films made of other polymers such as HPMC (hydroxyl propyl methyl cellulose) and HPMC-PF127. These CP based BFs (without and with PF127) exhibited good film thickness 0.88 ± 0.10 and 0.76 ± 0.14 mm, with weight uniformity 68.22 ± 1.04 and 86.28 ± 2.16 mg, satisfactory flexibility values 258 and 321, and slightly acidic pH 6.43 ± 0.76 and 6.32 ± 0.01. The swelling percentage was found to be 50% for CP and 78% for CP-PF127. The cumulative amount of drug that permeated through the buccal epithelium after 24 h was about 66% from CP and 75% from CP-PF127.
- Full Text:
- Date Issued: 2019
- Authors: Okafor, Nnamadi I , Ngoepe, Mpho , Siwe-Noundou, Xavier , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194032 , vital:45417 , xlink:href="https://doi.org/10.1016/j.jddst.2019.101312"
- Description: Buccal films (BFs) were prepared using a solvent casting method using the liposomal suspension as the dispersing medium. Optimization of some physical properties of the films containing different amounts of polymers was done using digital Vernier calliper and digital weighing balance. The physiochemical properties of the best optimized properties were characterized using Differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier transfer infrared spectroscopy (FTIR), Transmission Electron Microscopy (TEM), Energy dispersive X-ray spectroscopy (EDS), and Scanning Electron Microscopy (SEM). Permeation study of the BFs composed of Carbopol (CP) alone and CP to Pluronic 127 (PF127) demonstrated better bio-adhesive properties than the films made of other polymers such as HPMC (hydroxyl propyl methyl cellulose) and HPMC-PF127. These CP based BFs (without and with PF127) exhibited good film thickness 0.88 ± 0.10 and 0.76 ± 0.14 mm, with weight uniformity 68.22 ± 1.04 and 86.28 ± 2.16 mg, satisfactory flexibility values 258 and 321, and slightly acidic pH 6.43 ± 0.76 and 6.32 ± 0.01. The swelling percentage was found to be 50% for CP and 78% for CP-PF127. The cumulative amount of drug that permeated through the buccal epithelium after 24 h was about 66% from CP and 75% from CP-PF127.
- Full Text:
- Date Issued: 2019
Antiparasitic Constituents of Beilschmiedia louisii and Beilschmiedia obscura and Some Semisynthetic Derivatives
- Waleguele, Christine C, Mba'ning, Brice M, Awantu, Angelbert F, Bankeu, Jean J, Fongang, Yannick S F, Ngouela, Augustin S, Tsamo, Etienne, Sewald, Norbert, Lenta, Bruno N, Krause, Rui W M
- Authors: Waleguele, Christine C , Mba'ning, Brice M , Awantu, Angelbert F , Bankeu, Jean J , Fongang, Yannick S F , Ngouela, Augustin S , Tsamo, Etienne , Sewald, Norbert , Lenta, Bruno N , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193364 , vital:45325 , xlink:href="https://doi.org/10.3390/molecules25122862"
- Description: The MeOH/CH2Cl2 (1:1) extracts of the roots and leaves of Beilschmiedia louisii and B. obscura showed potent antitrypanosomal activity during preliminary screening on Trypanosoma brucei brucei. Phytochemical investigation of these extracts led to the isolation of a mixture of two new endiandric acid derivatives beilschmiedol B (1) and beilschmiedol C (2), and one new phenylalkene obscurene A (3) together with twelve known compounds (4–15). In addition, four new derivatives (11a–11d) were synthesized from compound 11. Their structures were elucidated based on their NMR and MS data. Compounds 5, 6, and 7 were isolated for the first time from the Beilschmiedia genus. Additionally, the NMR data of compound 4 are given here for the first time. The isolates were evaluated for their antitrypanosomal and antimalarial activities against Tb brucei and the Plasmodium falciparum chloroquine-resistant strain Pf3D7 in vitro, respectively. From the tested compounds, the mixture of new compounds 1 and 2 exhibited the most potent antitrypanosomal activity in vitro with IC50 value of 4.91 μM.
- Full Text:
- Date Issued: 2020
- Authors: Waleguele, Christine C , Mba'ning, Brice M , Awantu, Angelbert F , Bankeu, Jean J , Fongang, Yannick S F , Ngouela, Augustin S , Tsamo, Etienne , Sewald, Norbert , Lenta, Bruno N , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193364 , vital:45325 , xlink:href="https://doi.org/10.3390/molecules25122862"
- Description: The MeOH/CH2Cl2 (1:1) extracts of the roots and leaves of Beilschmiedia louisii and B. obscura showed potent antitrypanosomal activity during preliminary screening on Trypanosoma brucei brucei. Phytochemical investigation of these extracts led to the isolation of a mixture of two new endiandric acid derivatives beilschmiedol B (1) and beilschmiedol C (2), and one new phenylalkene obscurene A (3) together with twelve known compounds (4–15). In addition, four new derivatives (11a–11d) were synthesized from compound 11. Their structures were elucidated based on their NMR and MS data. Compounds 5, 6, and 7 were isolated for the first time from the Beilschmiedia genus. Additionally, the NMR data of compound 4 are given here for the first time. The isolates were evaluated for their antitrypanosomal and antimalarial activities against Tb brucei and the Plasmodium falciparum chloroquine-resistant strain Pf3D7 in vitro, respectively. From the tested compounds, the mixture of new compounds 1 and 2 exhibited the most potent antitrypanosomal activity in vitro with IC50 value of 4.91 μM.
- Full Text:
- Date Issued: 2020
Isolation and Characterisation of Stigmasterol and β–Sitosterol from Anthocleista djalonensis A. Chev.
- Okoro, Ijeoma S, Tor-Anyiin, Terrumun A, Igoli, John O, Noundou, Xavier S, Krause, Rui W M
- Authors: Okoro, Ijeoma S , Tor-Anyiin, Terrumun A , Igoli, John O , Noundou, Xavier S , Krause, Rui W M
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126191 , vital:35857 , https://doi.org/10.9734/AJOCS/2017/37147
- Description: Aim: Anthocleista djalonensis A. Chev. is a plant with several chemical constituents whichaccounts for its ethno-pharmacological uses. The present study is aimed at identifying and characterizing the active principles from the roots of the plant. Place and Duration of Study: The study was carried out at the Department of Organic Chemistry,Rhodes University, Grahamstown, South Africa between March and July 2016. Methodology: The root powder was subjected to maceration with methanol to obtain the crude extract. The methanol extract was fractionated using hexane, ethyl acetate and acetone successively. The acetone extract was thereafter subjected to column chromatography to isolate any pure components. Results: White needle-like crystals were obtained which on spectral analysis(IR, 1H NMR, 13C NMR, 2D- NMR, and ESI-MS ) were identified as a mixture of stigmasterol and β-sitosterol. Conclusion: The compounds isolated were identified as stigmasterol and β-sitosterol.
- Full Text:
- Date Issued: 2018
- Authors: Okoro, Ijeoma S , Tor-Anyiin, Terrumun A , Igoli, John O , Noundou, Xavier S , Krause, Rui W M
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126191 , vital:35857 , https://doi.org/10.9734/AJOCS/2017/37147
- Description: Aim: Anthocleista djalonensis A. Chev. is a plant with several chemical constituents whichaccounts for its ethno-pharmacological uses. The present study is aimed at identifying and characterizing the active principles from the roots of the plant. Place and Duration of Study: The study was carried out at the Department of Organic Chemistry,Rhodes University, Grahamstown, South Africa between March and July 2016. Methodology: The root powder was subjected to maceration with methanol to obtain the crude extract. The methanol extract was fractionated using hexane, ethyl acetate and acetone successively. The acetone extract was thereafter subjected to column chromatography to isolate any pure components. Results: White needle-like crystals were obtained which on spectral analysis(IR, 1H NMR, 13C NMR, 2D- NMR, and ESI-MS ) were identified as a mixture of stigmasterol and β-sitosterol. Conclusion: The compounds isolated were identified as stigmasterol and β-sitosterol.
- Full Text:
- Date Issued: 2018
Anti-HIV-1 integrase potency of methylgallate from Alchornea cordifolia using in vitro and in silico approaches:
- Noundou, Xavier S, Musyoka, Thommas M, Moses, Vuyani, Ndinteh, Derek T, Mnkandhla, Dumisani, Hoppe, Heinrich C, Tastan Bishop, Özlem, Krause, Rui W M
- Authors: Noundou, Xavier S , Musyoka, Thommas M , Moses, Vuyani , Ndinteh, Derek T , Mnkandhla, Dumisani , Hoppe, Heinrich C , Tastan Bishop, Özlem , Krause, Rui W M
- Date: 2019
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/162975 , vital:41001 , https://0-doi.org.wam.seals.ac.za/10.1038/s41598-019-41403-x
- Description: According to the 2018 report of the United Nations Programme on HIV/AIDS (UNAIDS), acquired immune deficiency syndrome (AIDS), a disease caused by the human immunodeficiency virus (HIV), remains a significant public health problem. The non-existence of a cure or effective vaccine for the disease and the associated emergence of resistant viral strains imply an urgent need for the discovery of novel anti-HIV drug candidates. The current study aimed to identify potential anti-retroviral compounds from Alchornea cordifolia.
- Full Text:
- Date Issued: 2019
- Authors: Noundou, Xavier S , Musyoka, Thommas M , Moses, Vuyani , Ndinteh, Derek T , Mnkandhla, Dumisani , Hoppe, Heinrich C , Tastan Bishop, Özlem , Krause, Rui W M
- Date: 2019
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/162975 , vital:41001 , https://0-doi.org.wam.seals.ac.za/10.1038/s41598-019-41403-x
- Description: According to the 2018 report of the United Nations Programme on HIV/AIDS (UNAIDS), acquired immune deficiency syndrome (AIDS), a disease caused by the human immunodeficiency virus (HIV), remains a significant public health problem. The non-existence of a cure or effective vaccine for the disease and the associated emergence of resistant viral strains imply an urgent need for the discovery of novel anti-HIV drug candidates. The current study aimed to identify potential anti-retroviral compounds from Alchornea cordifolia.
- Full Text:
- Date Issued: 2019
Cytotoxicity, phytochemical analysis and antioxidant activity of crude extracts from Rhizomes of Elephantorrhiza Elephantina and Pentanisia Prunelloides
- Mpofu, Smart J, Msagati, Titus A M, Krause, Rui W M
- Authors: Mpofu, Smart J , Msagati, Titus A M , Krause, Rui W M
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125097 , vital:35728 , https://doi.org/10.4314/ajtcam.v11i1.6
- Description: Background: Elephantorrhiza elephantina (Ee) and Pentanisia prunelloides (Pp) are two medicinal plants which are widely used to remedy various ailments including diarrhoea, dysentery, inflammation, fever, rheumatism, heartburn, tuberculosis, haemorrhoids, skin diseases, perforated peptic ulcers and sore joints in southern Africa (South Africa, Swaziland, Botswana and Zimbabwe). The following study was conducted to explore the in vitro cytotoxicity, antioxidant properties and phytochemical profile of the two medicinal plants. Materials and Methods: The cytotoxicity of the aqueous and methanol extracts and fractions of both species was studied using the brine shrimp lethality tests (BST) for the first time. Results: The results demonstrated that the lethality (LC50) for crude extracts for both plants ranged between 1.8 and 5.8 ppm and was relatively greater than that for the methanol, ethyl acetate and chloroform fractions of the extracts which ranged between 2.1 ppm and 27 ppm. This suggested that crude extracts were more potent than their respective fractions, further explaining that the different fractions of phytochemicals in these plant species work jointly (in synergy) to exert their therapeutic efficacy. Both aqueous and methanol extracts of the two medicinal plants demonstrated a high degree of antioxidant capacity against the DPPH radical with the Duh and Yen inhibition percentage ranging between 4.5% and 72%. Phytochemical studies of the rhizome extracts showed that the major compounds present include flavonoids, tannins, anthocyanidins, anthraquinones, triterpenoids (oleanolic acid), the steroidal saponin Diosgenin, the sugars, rhamnose, glucuronic acid, Arabinose and hexoses. Conclusion: This is the first report of the detection and isolation of diosgenin and oleanolic acid from the rhizome extracts of Ee and Pp. All structures were determined using spectroscopic/spectrometric techniques (1H NMR and 13C and LC-ESI-MS) and by comparison with literature data.
- Full Text:
- Date Issued: 2014
- Authors: Mpofu, Smart J , Msagati, Titus A M , Krause, Rui W M
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125097 , vital:35728 , https://doi.org/10.4314/ajtcam.v11i1.6
- Description: Background: Elephantorrhiza elephantina (Ee) and Pentanisia prunelloides (Pp) are two medicinal plants which are widely used to remedy various ailments including diarrhoea, dysentery, inflammation, fever, rheumatism, heartburn, tuberculosis, haemorrhoids, skin diseases, perforated peptic ulcers and sore joints in southern Africa (South Africa, Swaziland, Botswana and Zimbabwe). The following study was conducted to explore the in vitro cytotoxicity, antioxidant properties and phytochemical profile of the two medicinal plants. Materials and Methods: The cytotoxicity of the aqueous and methanol extracts and fractions of both species was studied using the brine shrimp lethality tests (BST) for the first time. Results: The results demonstrated that the lethality (LC50) for crude extracts for both plants ranged between 1.8 and 5.8 ppm and was relatively greater than that for the methanol, ethyl acetate and chloroform fractions of the extracts which ranged between 2.1 ppm and 27 ppm. This suggested that crude extracts were more potent than their respective fractions, further explaining that the different fractions of phytochemicals in these plant species work jointly (in synergy) to exert their therapeutic efficacy. Both aqueous and methanol extracts of the two medicinal plants demonstrated a high degree of antioxidant capacity against the DPPH radical with the Duh and Yen inhibition percentage ranging between 4.5% and 72%. Phytochemical studies of the rhizome extracts showed that the major compounds present include flavonoids, tannins, anthocyanidins, anthraquinones, triterpenoids (oleanolic acid), the steroidal saponin Diosgenin, the sugars, rhamnose, glucuronic acid, Arabinose and hexoses. Conclusion: This is the first report of the detection and isolation of diosgenin and oleanolic acid from the rhizome extracts of Ee and Pp. All structures were determined using spectroscopic/spectrometric techniques (1H NMR and 13C and LC-ESI-MS) and by comparison with literature data.
- Full Text:
- Date Issued: 2014
Synthesis, antiplasmodial and antitrypanosomal evaluation of a series of novel 2-oxoquinoline-based thiosemicarbazone derivatives
- Darrell, Oliver T, Hulushe, Siyabonga T, Mtshare, Thanduxolo Elihle, Beteck, Richard M, Isaacs, Michelle, Laming, Dustin, Khanye, Setshaba D, Hoppe, Heinrich C, Krause, Rui W M
- Authors: Darrell, Oliver T , Hulushe, Siyabonga T , Mtshare, Thanduxolo Elihle , Beteck, Richard M , Isaacs, Michelle , Laming, Dustin , Khanye, Setshaba D , Hoppe, Heinrich C , Krause, Rui W M
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123117 , vital:35407 , https://doi.org/10.17159/0379-4350/2018/v71a25
- Description: Herein a series of novel thiosemicarbazones (TSCs) derived from 2-oxoquinoline scaffold is reported, and the target compounds have been successfully synthesized and characterized using standard spectroscopic techniques. The in vitro biological activities of synthesized molecules were evaluated against Plasmodium falciparum malaria parasites (strain 3D7), Trypanosoma brucei brucei parasites (strain 427) and HeLa cells. All the compounds displayed modest or no activity at a concentration of 20 μM and percentage viability of >50 % was often observed. Except for compound 9o, none of the final compounds exhibited cytotoxic effects against HeLa cells at 20 μM.
- Full Text:
- Date Issued: 2018
- Authors: Darrell, Oliver T , Hulushe, Siyabonga T , Mtshare, Thanduxolo Elihle , Beteck, Richard M , Isaacs, Michelle , Laming, Dustin , Khanye, Setshaba D , Hoppe, Heinrich C , Krause, Rui W M
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123117 , vital:35407 , https://doi.org/10.17159/0379-4350/2018/v71a25
- Description: Herein a series of novel thiosemicarbazones (TSCs) derived from 2-oxoquinoline scaffold is reported, and the target compounds have been successfully synthesized and characterized using standard spectroscopic techniques. The in vitro biological activities of synthesized molecules were evaluated against Plasmodium falciparum malaria parasites (strain 3D7), Trypanosoma brucei brucei parasites (strain 427) and HeLa cells. All the compounds displayed modest or no activity at a concentration of 20 μM and percentage viability of >50 % was often observed. Except for compound 9o, none of the final compounds exhibited cytotoxic effects against HeLa cells at 20 μM.
- Full Text:
- Date Issued: 2018
Synthesis and biological evaluation of bis-N2, N2′-(4-hydroxycoumarin-3-yl) ethylidene]-2, 3-dihydroxysuccinodihydrazides
- Manyeruke, Meloddy H, Tshiwawa, Thendamudzimu, Hoppe, Heinrich, Isaacs, Michelle, Seldon, Ronnett, Warner, Digby F, Krause, Rui W M, Kaye, Perry T
- Authors: Manyeruke, Meloddy H , Tshiwawa, Thendamudzimu , Hoppe, Heinrich , Isaacs, Michelle , Seldon, Ronnett , Warner, Digby F , Krause, Rui W M , Kaye, Perry T
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193430 , vital:45331 , xlink:href="https://doi.org/10.1016/j.bmcl.2019.126911"
- Description: A series of N2,N2′-bis[4-hydroxycoumarin-3-yl)ethylidene]-2,3-dihydroxysuccino-hydrazides, containing 4-hydroxycoumarin, hydrazine and tartaric acid moieties, have been prepared and examined for possible biological activity. Several of these compounds exhibit promising HIV-1 integrase inhibition (IC50 = 3.5 μM), and anti-T. brucei (32% viability) and anti-mycobacterial (Visual MIC90 = 15.63 μM) activity.
- Full Text:
- Date Issued: 2020
- Authors: Manyeruke, Meloddy H , Tshiwawa, Thendamudzimu , Hoppe, Heinrich , Isaacs, Michelle , Seldon, Ronnett , Warner, Digby F , Krause, Rui W M , Kaye, Perry T
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193430 , vital:45331 , xlink:href="https://doi.org/10.1016/j.bmcl.2019.126911"
- Description: A series of N2,N2′-bis[4-hydroxycoumarin-3-yl)ethylidene]-2,3-dihydroxysuccino-hydrazides, containing 4-hydroxycoumarin, hydrazine and tartaric acid moieties, have been prepared and examined for possible biological activity. Several of these compounds exhibit promising HIV-1 integrase inhibition (IC50 = 3.5 μM), and anti-T. brucei (32% viability) and anti-mycobacterial (Visual MIC90 = 15.63 μM) activity.
- Full Text:
- Date Issued: 2020