Cordidepsine is A Potential New Anti-HIV Depsidone from Cordia millenii
- Zeukang, Rostanie D, Siwe-Noundou, Xavier, Fotsing, Maurice T, Mbafor, Joseph T, Krause, Rui W M, Choudhary, Muhammad I, Atchade, Alex de Theodore
- Authors: Zeukang, Rostanie D , Siwe-Noundou, Xavier , Fotsing, Maurice T , Mbafor, Joseph T , Krause, Rui W M , Choudhary, Muhammad I , Atchade, Alex de Theodore
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193988 , vital:45413 , xlink:href="https://doi.org/10.3390/molecules24173202"
- Description: Chemical investigation of Cordia millenii, Baker resulted in the isolation of a new depsidone, cordidepsine (1), along with twelve known compounds including cyclooctasulfur (2), lup-20(29)-en-3-triacontanoate (3), 1-(26-hydroxyhexacosanoyl)glycerol (4), glyceryl-1-hexacosanoate (5) betulinic acid (6), lupenone (7), β-amyrone (8), lupeol (9), β-amyrin (10), allantoin (11), 2′-(4-hydroxyphenyl)ethylpropanoate (12) and stigmasterol glycoside (13). Hemi-synthetic reactions were carried out on two isolated compounds (5 and 6) to afford two new derivatives, that is, cordicerol A (14) and cordicerol B (15), respectively. The chemical structures of all the compounds were established based on analysis and interpretation of spectroscopic data such as electron ionization mass spectrometry (EI–MS), high resolution electrospray ionization mass spectrometry (HR-ESI–MS), fast atom bombardment mass spectrometry (FAB–MS), one dimension and two dimension nuclear magnetic resonance (1D and 2D-NMR) spectral data as well as X-ray crystallography (XRC). Lupeol ester derivatives [Lup-20(29)-en-3-triacontanoate (3)], monoglycerol derivatives [1-(26-hydroxyhexacosanoyl)glycerol (4) and glyceryl-1 hexacosanoate (5)] were isolated for the first time from Cordia genus while sulfur allotrope [cyclooctasulfur (2)] was isolated for the first time from plant origin. Biological assays cordidepsine (1) exhibited significant anti-HIV integrase activity with IC50 = 4.65 μM; EtOAc extract of stem barks, EtOAc fraction of roots and leaves were not toxic against 3T3 cells.
- Full Text:
- Date Issued: 2019
- Authors: Zeukang, Rostanie D , Siwe-Noundou, Xavier , Fotsing, Maurice T , Mbafor, Joseph T , Krause, Rui W M , Choudhary, Muhammad I , Atchade, Alex de Theodore
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193988 , vital:45413 , xlink:href="https://doi.org/10.3390/molecules24173202"
- Description: Chemical investigation of Cordia millenii, Baker resulted in the isolation of a new depsidone, cordidepsine (1), along with twelve known compounds including cyclooctasulfur (2), lup-20(29)-en-3-triacontanoate (3), 1-(26-hydroxyhexacosanoyl)glycerol (4), glyceryl-1-hexacosanoate (5) betulinic acid (6), lupenone (7), β-amyrone (8), lupeol (9), β-amyrin (10), allantoin (11), 2′-(4-hydroxyphenyl)ethylpropanoate (12) and stigmasterol glycoside (13). Hemi-synthetic reactions were carried out on two isolated compounds (5 and 6) to afford two new derivatives, that is, cordicerol A (14) and cordicerol B (15), respectively. The chemical structures of all the compounds were established based on analysis and interpretation of spectroscopic data such as electron ionization mass spectrometry (EI–MS), high resolution electrospray ionization mass spectrometry (HR-ESI–MS), fast atom bombardment mass spectrometry (FAB–MS), one dimension and two dimension nuclear magnetic resonance (1D and 2D-NMR) spectral data as well as X-ray crystallography (XRC). Lupeol ester derivatives [Lup-20(29)-en-3-triacontanoate (3)], monoglycerol derivatives [1-(26-hydroxyhexacosanoyl)glycerol (4) and glyceryl-1 hexacosanoate (5)] were isolated for the first time from Cordia genus while sulfur allotrope [cyclooctasulfur (2)] was isolated for the first time from plant origin. Biological assays cordidepsine (1) exhibited significant anti-HIV integrase activity with IC50 = 4.65 μM; EtOAc extract of stem barks, EtOAc fraction of roots and leaves were not toxic against 3T3 cells.
- 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
Purification and biochemical characterisation of a putative sodium channel agonist secreted from the South African Knobbly sea anemone Bunodosoma capense
- van Losenoord, Wynand, Krause, Jason, Parker-Nance, Shirley, Krause, Rui W M, Stoychey, Stoyan, Frost, Carminita L
- Authors: van Losenoord, Wynand , Krause, Jason , Parker-Nance, Shirley , Krause, Rui W M , Stoychey, Stoyan , Frost, Carminita L
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194082 , vital:45421 , xlink:href="https://doi.org/10.1016/j.toxicon.2019.06.222"
- Description: Voltage gated ion channels have become a subject of investigation as possible pharmaceutical targets. Research has linked the activity of ion channels directly to anti-inflammatory pathways, energy homeostasis, cancer proliferation and painful diabetic neuropathy. Sea anemones secrete a diverse array of bioactive compounds including potassium and sodium channel toxins. A putative novel sodium channel agonist (molecular mass of 4619.7 Da) with a predicted sequence: CLCNSDGPSV RGNTLSGILW LAGCPSGWHN CKKHKPTIGW CCK was isolated from Bunodosoma capense using a modified stimulation technique to induce the secretion of the neurotoxin rich mucus confirmed by an Artemia nauplii bio-assay. The peptide purification combined size-exclusion and reverse-phase high performance liquid chromatography. A thallium-based ion flux assay confirmed the presence of a sodium channel agonist/inhibitor and purity was determined using a modified tricine SDS-PAGE system. The peptide isolated indicated the presence of multiple disulfide bonds in a tight β-defensin cystine conformation. An IC50 value of 26 nM was determined for total channel inhibition on MCF-7 cells. The unique putative sodium channel agonist initiating with a cystine bond indicates a divergent evolution to those previously isolated from Bunodosoma species.
- Full Text:
- Date Issued: 2019
- Authors: van Losenoord, Wynand , Krause, Jason , Parker-Nance, Shirley , Krause, Rui W M , Stoychey, Stoyan , Frost, Carminita L
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194082 , vital:45421 , xlink:href="https://doi.org/10.1016/j.toxicon.2019.06.222"
- Description: Voltage gated ion channels have become a subject of investigation as possible pharmaceutical targets. Research has linked the activity of ion channels directly to anti-inflammatory pathways, energy homeostasis, cancer proliferation and painful diabetic neuropathy. Sea anemones secrete a diverse array of bioactive compounds including potassium and sodium channel toxins. A putative novel sodium channel agonist (molecular mass of 4619.7 Da) with a predicted sequence: CLCNSDGPSV RGNTLSGILW LAGCPSGWHN CKKHKPTIGW CCK was isolated from Bunodosoma capense using a modified stimulation technique to induce the secretion of the neurotoxin rich mucus confirmed by an Artemia nauplii bio-assay. The peptide purification combined size-exclusion and reverse-phase high performance liquid chromatography. A thallium-based ion flux assay confirmed the presence of a sodium channel agonist/inhibitor and purity was determined using a modified tricine SDS-PAGE system. The peptide isolated indicated the presence of multiple disulfide bonds in a tight β-defensin cystine conformation. An IC50 value of 26 nM was determined for total channel inhibition on MCF-7 cells. The unique putative sodium channel agonist initiating with a cystine bond indicates a divergent evolution to those previously isolated from Bunodosoma species.
- Full Text:
- Date Issued: 2019
Compounds isolation and biological activities of Piptadeniastrum africanum (hook. f.) Brennan (Fabaceae) roots:
- Teinkela, Jean E M, Noundou, Xavier S, Mimba, Jeanne E Z, Meyer, Franck, Tabouguia, Octavie M, Nguedia, Jules C A, Hoppe, Heinrich C, Krause, Rui W M, Wintjens, René, Azebaze, Anatole G B
- Authors: Teinkela, Jean E M , Noundou, Xavier S , Mimba, Jeanne E Z , Meyer, Franck , Tabouguia, Octavie M , Nguedia, Jules C A , Hoppe, Heinrich C , Krause, Rui W M , Wintjens, René , Azebaze, Anatole G B
- Date: 2020
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/150084 , vital:38938 , https://doi.org/10.1016/j.jep.2020.112716
- Description: The dicotyledonous plant Piptadeniastrum africanum (hook.f.) Brennan (Fabaceae) is used in traditional medicine to treat various human complaints including bronchitis, coughing, urino-genital ailments, meningitis, abdominal pain, treatment of wounds, malaria and gastrointestinal ailments, and is used as a purgative and worm expeller. The present study describes the phytochemical investigation and the determination of the antimicrobial, antiplasmodial and antitrypanosomal activities of crude extract, fractions and compounds extracted from Piptadeniastrum africanum roots.
- Full Text:
- Date Issued: 2020
- Authors: Teinkela, Jean E M , Noundou, Xavier S , Mimba, Jeanne E Z , Meyer, Franck , Tabouguia, Octavie M , Nguedia, Jules C A , Hoppe, Heinrich C , Krause, Rui W M , Wintjens, René , Azebaze, Anatole G B
- Date: 2020
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/150084 , vital:38938 , https://doi.org/10.1016/j.jep.2020.112716
- Description: The dicotyledonous plant Piptadeniastrum africanum (hook.f.) Brennan (Fabaceae) is used in traditional medicine to treat various human complaints including bronchitis, coughing, urino-genital ailments, meningitis, abdominal pain, treatment of wounds, malaria and gastrointestinal ailments, and is used as a purgative and worm expeller. The present study describes the phytochemical investigation and the determination of the antimicrobial, antiplasmodial and antitrypanosomal activities of crude extract, fractions and compounds extracted from Piptadeniastrum africanum roots.
- Full Text:
- Date Issued: 2020
Beneficial effects of medicinal plants in fish diseases
- Stratev, Deyan, Zhelyazkov, Georgi, Noundou, Xavier S, Krause, Rui W M
- Authors: Stratev, Deyan , Zhelyazkov, Georgi , Noundou, Xavier S , Krause, Rui W M
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126177 , vital:35856 , https://doi.org/10.1007/s10499-017-0219-x
- Description: Fish are constantly in contact with pathogens inhabiting water. High populationdensity as well as poor hydrodynamic conditions and feeding lead to an increased sensitivitytowards infections. In order to prevent major economic losses due to diseases, variousmedications are used for treatment and prevention of infections. The use of antimicrobialdrugs in aquacultures could lead to emergence of resistance in pathogenic microorganisms.Alternatives are being sought over the last few years to replace antibiotics, and medicinalplants are one of available options for this purpose. These plants are rich in secondarymetabolites and phytochemical compounds, which have an effect against viral, bacterial, andparasitic diseases in fish. Their main advantage is their natural origin and most of these plantsdo not represent threat for human health, the fish, and the environment. The goal of this reviewis to present information on the treatment of viral, bacterial, and parasitic diseases in fishthrough medicinal plants, with focus on the mechanisms of action of the identified secondarymetabolites, fractions, or plant extracts.
- Full Text:
- Date Issued: 2018
- Authors: Stratev, Deyan , Zhelyazkov, Georgi , Noundou, Xavier S , Krause, Rui W M
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126177 , vital:35856 , https://doi.org/10.1007/s10499-017-0219-x
- Description: Fish are constantly in contact with pathogens inhabiting water. High populationdensity as well as poor hydrodynamic conditions and feeding lead to an increased sensitivitytowards infections. In order to prevent major economic losses due to diseases, variousmedications are used for treatment and prevention of infections. The use of antimicrobialdrugs in aquacultures could lead to emergence of resistance in pathogenic microorganisms.Alternatives are being sought over the last few years to replace antibiotics, and medicinalplants are one of available options for this purpose. These plants are rich in secondarymetabolites and phytochemical compounds, which have an effect against viral, bacterial, andparasitic diseases in fish. Their main advantage is their natural origin and most of these plantsdo not represent threat for human health, the fish, and the environment. The goal of this reviewis to present information on the treatment of viral, bacterial, and parasitic diseases in fishthrough medicinal plants, with focus on the mechanisms of action of the identified secondarymetabolites, fractions, or plant extracts.
- Full Text:
- Date Issued: 2018
Beneficial effects of medicinal plants in fish diseases
- Stratev, Deyan, Zhelyazkov, Georgi, Noundou, Xavier Siwe, Krause, Rui W M
- Authors: Stratev, Deyan , Zhelyazkov, Georgi , Noundou, Xavier Siwe , Krause, Rui W M
- Date: 2008
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123487 , vital:35447 , https://doi.org/10.1007/s10499-017-0219-x
- Description: Fish are constantly in contact with pathogens inhabiting water. High population density as well as poor hydrodynamic conditions and feeding lead to an increased sensitivity towards infections. In order to prevent major economic losses due to diseases, various medications are used for treatment and prevention of infections. The use of antimicrobial drugs in aquacultures could lead to emergence of resistance in pathogenic microorganisms. Alternatives are being sought over the last few years to replace antibiotics, and medicinal plants are one of available options for this purpose. These plants are rich in secondary metabolites and phytochemical compounds, which have an effect against viral, bacterial, and parasitic diseases in fish. Their main advantage is their natural origin and most of these plants do not represent threat for human health, the fish, and the environment. The goal of this review is to present information on the treatment of viral, bacterial, and parasitic diseases in fish through medicinal plants, with focus on the mechanisms of action of the identified secondary metabolites, fractions, or plant extracts.
- Full Text:
- Date Issued: 2008
- Authors: Stratev, Deyan , Zhelyazkov, Georgi , Noundou, Xavier Siwe , Krause, Rui W M
- Date: 2008
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123487 , vital:35447 , https://doi.org/10.1007/s10499-017-0219-x
- Description: Fish are constantly in contact with pathogens inhabiting water. High population density as well as poor hydrodynamic conditions and feeding lead to an increased sensitivity towards infections. In order to prevent major economic losses due to diseases, various medications are used for treatment and prevention of infections. The use of antimicrobial drugs in aquacultures could lead to emergence of resistance in pathogenic microorganisms. Alternatives are being sought over the last few years to replace antibiotics, and medicinal plants are one of available options for this purpose. These plants are rich in secondary metabolites and phytochemical compounds, which have an effect against viral, bacterial, and parasitic diseases in fish. Their main advantage is their natural origin and most of these plants do not represent threat for human health, the fish, and the environment. The goal of this review is to present information on the treatment of viral, bacterial, and parasitic diseases in fish through medicinal plants, with focus on the mechanisms of action of the identified secondary metabolites, fractions, or plant extracts.
- Full Text:
- Date Issued: 2008
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
Blending problem-based learning and peer-led team learning, in an open ended ‘home-grown’pharmaceutical chemistry case study
- Sewry, Joyce D, Veale, Clinton G L, Krause, Rui W M
- Authors: Sewry, Joyce D , Veale, Clinton G L , Krause, Rui W M
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125691 , vital:35809 , https://doi.org/10.1039/C7RP00180K
- Description: Pharmaceutical chemistry, medicinal chemistry and the drug discovery process require experienced practitioners to employ reasoned speculation in generating creative ideas, which can be used to evolve promising molecules into drugs. The ever-evolving world of pharmaceutical chemistry requires university curricula that prepare graduates for their role as designers with the capability of applying complex concepts in pharmaceutical chemistry, thereby improving the decision-making process. Common methods of teaching drug discovery, including the linear nature of the traditional case study model, do not provide a realistic picture of the underlying complexity of the process, nor do they equip students with the appropriate tools for personal sense making and abstraction. In this work, we discuss the creation of an open-ended, nonlinear case study for 3rd year pharmaceutical chemistry students, developed from drug discovery research conducted at Rhodes University. Furthermore, we discuss blending problem based learning (PBL) with peer-led team learning (PLTL) in the context of curriculum transformation, underpinned by the theory of semantic waves, to assist students in the early attainment of abstract concepts and answer questions of contextualisation, personal sense making, relatability, relevance and ultimately the skills for lifelong learning.
- Full Text:
- Date Issued: 2018
- Authors: Sewry, Joyce D , Veale, Clinton G L , Krause, Rui W M
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125691 , vital:35809 , https://doi.org/10.1039/C7RP00180K
- Description: Pharmaceutical chemistry, medicinal chemistry and the drug discovery process require experienced practitioners to employ reasoned speculation in generating creative ideas, which can be used to evolve promising molecules into drugs. The ever-evolving world of pharmaceutical chemistry requires university curricula that prepare graduates for their role as designers with the capability of applying complex concepts in pharmaceutical chemistry, thereby improving the decision-making process. Common methods of teaching drug discovery, including the linear nature of the traditional case study model, do not provide a realistic picture of the underlying complexity of the process, nor do they equip students with the appropriate tools for personal sense making and abstraction. In this work, we discuss the creation of an open-ended, nonlinear case study for 3rd year pharmaceutical chemistry students, developed from drug discovery research conducted at Rhodes University. Furthermore, we discuss blending problem based learning (PBL) with peer-led team learning (PLTL) in the context of curriculum transformation, underpinned by the theory of semantic waves, to assist students in the early attainment of abstract concepts and answer questions of contextualisation, personal sense making, relatability, relevance and ultimately the skills for lifelong learning.
- Full Text:
- Date Issued: 2018
Mg/Triethylammonium Formate: A Useful System for Reductive Dimerization of Araldehydes into Pinacols;Nitroarenes into Azoarenes and Azoarenes into Hydrazoarenes
- Pamar, M Geeter, Govender, P, Muthusamy, K, Krause, Rui W M
- Authors: Pamar, M Geeter , Govender, P , Muthusamy, K , Krause, Rui W M
- Date: 2013
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125107 , vital:35729 , https://doi.org/10.13005/ojc/290316
- Description: Studies are reported which describes the effectiveness of triethylammonium formate in the presence of magnesium for the efficient intermolecular pinacol coupling using MeOH as solvent. Various aromatic carbonyls underwent smooth reductive coupling to give the corresponding 1,2-diols. A series of azo compounds were obtained by the reductive coupling of nitroaromatics while azo compounds were reduced to the corresponding hydrazoarenes by this system. There was no adverse effect on the other reducible and hydrogenolysable groups such as ether linkage, hydroxy and halogens. The reactions are clean, high yielding and inexpensive. All the reactions proceeded smoothly at ambient temperature.
- Full Text:
- Date Issued: 2013
- Authors: Pamar, M Geeter , Govender, P , Muthusamy, K , Krause, Rui W M
- Date: 2013
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125107 , vital:35729 , https://doi.org/10.13005/ojc/290316
- Description: Studies are reported which describes the effectiveness of triethylammonium formate in the presence of magnesium for the efficient intermolecular pinacol coupling using MeOH as solvent. Various aromatic carbonyls underwent smooth reductive coupling to give the corresponding 1,2-diols. A series of azo compounds were obtained by the reductive coupling of nitroaromatics while azo compounds were reduced to the corresponding hydrazoarenes by this system. There was no adverse effect on the other reducible and hydrogenolysable groups such as ether linkage, hydroxy and halogens. The reactions are clean, high yielding and inexpensive. All the reactions proceeded smoothly at ambient temperature.
- Full Text:
- Date Issued: 2013
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
Preparation and use of maize tassels’ activated carbon for the adsorption of phenolic compounds in environmental waste water samples
- 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/10962/125331 , vital:35773 , https://doi.org/10.1007/s11356-014-3742-6
- Description: The determination and remediation of three phenolic compounds bisphenol A (BPA), ortho-nitrophenol (o-NTP), parachlorophenol (PCP) in wastewater is reported. The analysis of these molecules in wastewater was done using gas chromatography (GC) × GC time-of-flight mass spectrometry while activated carbon derived from maize tassel was used as an adsorbent. During the experimental procedures, the effect of various parameters such as initial concentration, pH of sample solution, eluent volume, and sample volume on the removal efficiency with respect to the three phenolic compounds was studied. The results showed that maize tassel produced activated carbon (MTAC) cartridge packed solid-phase extraction (SPE) system was able to remove the phenolic compounds effectively (90.84–98.49 %, 80.75–97.11 %, and 78.27–97.08 % for BPA, o-NTP, and PCP, respectively) . The MTAC cartridge packed SPE sorbent performance was compared to commercially produced C18 SPE cartridges and found to be comparable. All the parameters investigated were found to have a notable influence on the adsorption efficiency of the phenolic compounds from wastewaters at different magnitudes.
- 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/10962/125331 , vital:35773 , https://doi.org/10.1007/s11356-014-3742-6
- Description: The determination and remediation of three phenolic compounds bisphenol A (BPA), ortho-nitrophenol (o-NTP), parachlorophenol (PCP) in wastewater is reported. The analysis of these molecules in wastewater was done using gas chromatography (GC) × GC time-of-flight mass spectrometry while activated carbon derived from maize tassel was used as an adsorbent. During the experimental procedures, the effect of various parameters such as initial concentration, pH of sample solution, eluent volume, and sample volume on the removal efficiency with respect to the three phenolic compounds was studied. The results showed that maize tassel produced activated carbon (MTAC) cartridge packed solid-phase extraction (SPE) system was able to remove the phenolic compounds effectively (90.84–98.49 %, 80.75–97.11 %, and 78.27–97.08 % for BPA, o-NTP, and PCP, respectively) . The MTAC cartridge packed SPE sorbent performance was compared to commercially produced C18 SPE cartridges and found to be comparable. All the parameters investigated were found to have a notable influence on the adsorption efficiency of the phenolic compounds from wastewaters at different magnitudes.
- Full Text:
- Date Issued: 2015
Steam activation, characterisation and adsorption studies of activated carbon from maize tassels.
- Olorundare, O F, Msagati, Titus A, Krause, Rui W M, Okonkwo, J O, Mamba, Bhekie B
- Authors: Olorundare, O F , Msagati, Titus A , Krause, Rui W M , Okonkwo, J O , Mamba, Bhekie B
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123847 , vital:35507 , https://doi.org/10.1080/02757540.2013.877001
- Description: In this paper, steam-produced activated carbon (STAC) from maize tassel (MT) was evaluated for its ability to remove basic dye (methylene blue MB) from aqueous solution in a batch adsorption process. The equilibrium experiments were conducted in the range of 50–300 mg/L initial MB concentrations at 30°C, for effect of pH, adsorbent dosage and contact time. The experimental data were analysed by Langmuir, Freundlich and Temkin isotherm models of adsorption. Freundlich adsorption isotherm was found to have highest value of R2(R2=0.97) compared to other models of Langmuir and Temkin having (0.96 and 0.95 respectively). STAC has a high adsorptive capacity for MB dye (200 mg/g) and also showed favourable adsorption for the dye with the separation factor for the dye-activated carbon system. The kinetic data obtained were analysed using pseudo first-order kinetic equation and pseudo second-order kinetic equation. The experimental data fitted well into pseudo second-order kinetic equation, as demonstrated by the high value of R2.
- Full Text:
- Date Issued: 2014
- Authors: Olorundare, O F , Msagati, Titus A , Krause, Rui W M , Okonkwo, J O , Mamba, Bhekie B
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/123847 , vital:35507 , https://doi.org/10.1080/02757540.2013.877001
- Description: In this paper, steam-produced activated carbon (STAC) from maize tassel (MT) was evaluated for its ability to remove basic dye (methylene blue MB) from aqueous solution in a batch adsorption process. The equilibrium experiments were conducted in the range of 50–300 mg/L initial MB concentrations at 30°C, for effect of pH, adsorbent dosage and contact time. The experimental data were analysed by Langmuir, Freundlich and Temkin isotherm models of adsorption. Freundlich adsorption isotherm was found to have highest value of R2(R2=0.97) compared to other models of Langmuir and Temkin having (0.96 and 0.95 respectively). STAC has a high adsorptive capacity for MB dye (200 mg/g) and also showed favourable adsorption for the dye with the separation factor for the dye-activated carbon system. The kinetic data obtained were analysed using pseudo first-order kinetic equation and pseudo second-order kinetic equation. The experimental data fitted well into pseudo second-order kinetic equation, as demonstrated by the high value of R2.
- Full Text:
- Date Issued: 2014
Activated carbon from lignocellulosic waste residues: effect of activating agent on porosity characteristics and use as adsorbents for organic species
- Olorundare, O F, Okonkwo, J O, Msagati, T A M, Mamba, Bhekie B, Krause, Rui W M
- Authors: Olorundare, O F , Okonkwo, J O , Msagati, T A M , Mamba, Bhekie B , Krause, Rui W M
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125233 , vital:35748 , https://doi.org/10.1007/s11270-014-1876-2
- Description: This paper reports on the effect of activating agents such as the impregnation ratio of phosphoric acid (1:1–1:5) at constant activation temperature on the performance of porous activated carbon from waste residues (maize tassel). The variation in the impregnation ratio of the produced activated carbon (AC) from 1:1 to 1:5 enabled the preparation of a high surface area (1,263 m2/g) and a large pore volume (1.592 cm3/g) of AC produced from maize tassel (MT) using a convectional chemical activating agent (phosphoric acid). Impregnation ratios (IR) of the precursors were varied between 1:1 and 1:5 in which it was found that the ratio of 1:4 was optimal based on the high surface area, while 1:5 has the optimal pore volume value for the produced activated carbon.
- Full Text:
- Date Issued: 2014
- Authors: Olorundare, O F , Okonkwo, J O , Msagati, T A M , Mamba, Bhekie B , Krause, Rui W M
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125233 , vital:35748 , https://doi.org/10.1007/s11270-014-1876-2
- Description: This paper reports on the effect of activating agents such as the impregnation ratio of phosphoric acid (1:1–1:5) at constant activation temperature on the performance of porous activated carbon from waste residues (maize tassel). The variation in the impregnation ratio of the produced activated carbon (AC) from 1:1 to 1:5 enabled the preparation of a high surface area (1,263 m2/g) and a large pore volume (1.592 cm3/g) of AC produced from maize tassel (MT) using a convectional chemical activating agent (phosphoric acid). Impregnation ratios (IR) of the precursors were varied between 1:1 and 1:5 in which it was found that the ratio of 1:4 was optimal based on the high surface area, while 1:5 has the optimal pore volume value for the produced activated carbon.
- Full Text:
- Date Issued: 2014
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
Encapsulation and physicochemical evaluation of efavirenz in liposomes
- Okafor, Nnamdi Ikemefuna, Nkanga, Christian I, Walker, Roderick B, Noundou, Xavier S, Krause, Rui W M
- Authors: Okafor, Nnamdi Ikemefuna , Nkanga, Christian I , Walker, Roderick B , Noundou, Xavier S , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183414 , vital:43988 , xlink:href="https://doi.org/10.1007/s40005-019-00458-8"
- Description: Antiretroviral therapy remains the most efective means of managing the human immune defciency virus/acquired immune defciency syndrome (HIV/AIDS). Application of therapeutics has been hampered by factors including poor bioavailability of most anti-retroviral compounds (ARV), side efects and an alarming emergence of drug resistant strains of the virus. Recent developments and use of drug delivery systems (DDS) has shown potential for improving the pharmacological profle of ARV. Amongst these complex DDS, liposomes have been explored for delivery of ARV. In this study, we have aimed at exploring efcient encapsulation of efavirenz (EFV), a potent ARV using diferent mass ratios of crude soybean lecithin and cholesterol. The EFV-loaded liposomes (EFL) were prepared using thin flm hydration and evaluated for particle size, zeta potential (ZP), encapsulation efciency (EE%), morphology and drug release studies. Diferential scanning calorimetry (DSC), X-ray difraction (XRD), energy dispersity spectroscopy (EDS) and Fourier transform infrared (FTIR) spectroscopy were used for comprehensive physicochemical characterization of EFL. EFL exhibited high encapsulation (99%) in 1:1 crude lecithin to cholesterol mass ratio. The average particle size and Zeta Potential of EFL were found to be 411.10±7.40 nm and −53.5.3±0.06 mV, respectively. EFL showed a relatively controlled EFV release behaviour that was similar to the dissolution profle of un-encapsulated EFV. This suggests that EFL represents a promising vehicle for efective EFV delivery while providing the advantages of a nano-scaled delivery system
- Full Text:
- Date Issued: 2020
- Authors: Okafor, Nnamdi Ikemefuna , Nkanga, Christian I , Walker, Roderick B , Noundou, Xavier S , Krause, Rui W M
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183414 , vital:43988 , xlink:href="https://doi.org/10.1007/s40005-019-00458-8"
- Description: Antiretroviral therapy remains the most efective means of managing the human immune defciency virus/acquired immune defciency syndrome (HIV/AIDS). Application of therapeutics has been hampered by factors including poor bioavailability of most anti-retroviral compounds (ARV), side efects and an alarming emergence of drug resistant strains of the virus. Recent developments and use of drug delivery systems (DDS) has shown potential for improving the pharmacological profle of ARV. Amongst these complex DDS, liposomes have been explored for delivery of ARV. In this study, we have aimed at exploring efcient encapsulation of efavirenz (EFV), a potent ARV using diferent mass ratios of crude soybean lecithin and cholesterol. The EFV-loaded liposomes (EFL) were prepared using thin flm hydration and evaluated for particle size, zeta potential (ZP), encapsulation efciency (EE%), morphology and drug release studies. Diferential scanning calorimetry (DSC), X-ray difraction (XRD), energy dispersity spectroscopy (EDS) and Fourier transform infrared (FTIR) spectroscopy were used for comprehensive physicochemical characterization of EFL. EFL exhibited high encapsulation (99%) in 1:1 crude lecithin to cholesterol mass ratio. The average particle size and Zeta Potential of EFL were found to be 411.10±7.40 nm and −53.5.3±0.06 mV, respectively. EFL showed a relatively controlled EFV release behaviour that was similar to the dissolution profle of un-encapsulated EFV. This suggests that EFL represents a promising vehicle for efective EFV delivery while providing the advantages of a nano-scaled delivery system
- Full Text:
- Date Issued: 2020
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
Electronic and nonlinear optical properties of 2-(((5-aminonaphthalen-1-yl) imino) methyl) phenol
- Ojo, Nathanael D, Krause, Rui W M, Obi-Egbedi, Nelson O
- Authors: Ojo, Nathanael D , Krause, Rui W M , Obi-Egbedi, Nelson O
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193397 , vital:45328 , xlink:href="https://doi.org/10.1016/j.molliq.2020.114157"
- Description: In this study, solvent dependence of electronic and nonlinear optical properties of a new Schiff base, 2-(((5-aminonaphthalen-1-yl)imino)methyl) phenol (DANOHB), has been investigated. Electronic and optical properties of the Schiff base studied using Uv-visible absorption and fluorescence spectroscopic techniques in solution show that the Schiff base exhibits fluorescence with a quantum yield of 0.21 and a Stokes shift of 39 nm. Quantum chemical calculations were performed on the Schiff base at time-dependent density functional level of theory using Becke-3-Lee-Yang-Parr method with 6-311++G(d,p) basis set. Solvent dependence of the excited state energies (EE), energy gap (ΔE), first-order (β) and second-order (γ) hyperpolarizabilities were studied in gas, cyclohexane and ethanol. The medium perturbed the energy levels which implies that the reactivity, activity and stability of the system are solvent sensitive. The γ is more than thirty times higher than urea (standard NLO material) and this property is further enhanced in less polar medium. Small ΔE and large hyperpolarizabilities obtained for this system suggest its good potential in photonics and nonlinear optical devices.
- Full Text:
- Date Issued: 2020
- Authors: Ojo, Nathanael D , Krause, Rui W M , Obi-Egbedi, Nelson O
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193397 , vital:45328 , xlink:href="https://doi.org/10.1016/j.molliq.2020.114157"
- Description: In this study, solvent dependence of electronic and nonlinear optical properties of a new Schiff base, 2-(((5-aminonaphthalen-1-yl)imino)methyl) phenol (DANOHB), has been investigated. Electronic and optical properties of the Schiff base studied using Uv-visible absorption and fluorescence spectroscopic techniques in solution show that the Schiff base exhibits fluorescence with a quantum yield of 0.21 and a Stokes shift of 39 nm. Quantum chemical calculations were performed on the Schiff base at time-dependent density functional level of theory using Becke-3-Lee-Yang-Parr method with 6-311++G(d,p) basis set. Solvent dependence of the excited state energies (EE), energy gap (ΔE), first-order (β) and second-order (γ) hyperpolarizabilities were studied in gas, cyclohexane and ethanol. The medium perturbed the energy levels which implies that the reactivity, activity and stability of the system are solvent sensitive. The γ is more than thirty times higher than urea (standard NLO material) and this property is further enhanced in less polar medium. Small ΔE and large hyperpolarizabilities obtained for this system suggest its good potential in photonics and nonlinear optical devices.
- Full Text:
- Date Issued: 2020
Electronic and nonlinear optical properties of 3-(((2-substituted-4-nitrophenyl) imino) methyl) phenol
- Ojo, Nathanael D, Krause, Rui W M, Obi-Egbedi, Nelson O
- Authors: Ojo, Nathanael D , Krause, Rui W M , Obi-Egbedi, Nelson O
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193408 , vital:45329 , xlink:href="https://doi.org/10.1016/j.comptc.2020.113050"
- Description: This work entails the study of electronic and nonlinear optical (NLO) properties of two synthesized Schiff bases namely 3-(((2-methyl-4-nitrophenyl)imino)methyl)phenol (MMP) and 3-(((2,4-dinitrophenyl)imino)methyl)phenol (DMP). Electronic absorption properties studied using UV–Visible spectrophotometry in ethanol reveal low-energy absorption indicating a low band gap. Time-dependent density functional calculations on their excited state properties with ωB97X-D/6-311++G(d,p) method show comparable transition energies and intensities with the experimental results. Energy gaps (ΔE) and NLO properties were evaluated from the frontier orbitals and hyperpolarizabilities (βtot and γ) in gas, cyclohexane and ethanol. Low ΔE obtained shows the potentials of the systems as organic semiconductor with remarkable band gap stabilization in ethanol. Higher βtot and γ than urea imply that the Schiff bases possess potentials for NLO applications. The solvatochromic shift in transition energies and perturbation of electronic properties reveal the solvent dependence of the electronic and optical properties of MMP and DMP due to solute-solvent interactions.
- Full Text:
- Date Issued: 2020
- Authors: Ojo, Nathanael D , Krause, Rui W M , Obi-Egbedi, Nelson O
- Date: 2020
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193408 , vital:45329 , xlink:href="https://doi.org/10.1016/j.comptc.2020.113050"
- Description: This work entails the study of electronic and nonlinear optical (NLO) properties of two synthesized Schiff bases namely 3-(((2-methyl-4-nitrophenyl)imino)methyl)phenol (MMP) and 3-(((2,4-dinitrophenyl)imino)methyl)phenol (DMP). Electronic absorption properties studied using UV–Visible spectrophotometry in ethanol reveal low-energy absorption indicating a low band gap. Time-dependent density functional calculations on their excited state properties with ωB97X-D/6-311++G(d,p) method show comparable transition energies and intensities with the experimental results. Energy gaps (ΔE) and NLO properties were evaluated from the frontier orbitals and hyperpolarizabilities (βtot and γ) in gas, cyclohexane and ethanol. Low ΔE obtained shows the potentials of the systems as organic semiconductor with remarkable band gap stabilization in ethanol. Higher βtot and γ than urea imply that the Schiff bases possess potentials for NLO applications. The solvatochromic shift in transition energies and perturbation of electronic properties reveal the solvent dependence of the electronic and optical properties of MMP and DMP due to solute-solvent interactions.
- Full Text:
- Date Issued: 2020
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
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