Co-encapsulation of rifampicin and isoniazid in crude soybean lecithin liposomes
- Nkanga, Christian I, Noundou, Xavier S, Walker, Roderick B, Krause, Rui W M
- Authors: Nkanga, Christian I , Noundou, Xavier S , Walker, Roderick B , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183536 , vital:44005 , xlink:href="https://doi.org/10.17159/0379-4350/2019/v72a11"
- Description: Despite the well-known anti-mycobacterial actions of isoniazid (INH) and rifampicin (RIF), the clinical success of tuberculosis (TB) therapy requires prolonged administration of multiple drugs in high doses, which often result in frequent adverse effects and low patient adherence. Although liposomes are promising candidates for controlled delivery of anti-TB drug, the high cost of synthetic and highly purified natural lipids currently used in liposomal technology might preclude the universal application of therapeutic liposomes. This work aimed at evaluating the potential of a cost-effective lipid material, crude soybean lecithin (CL), to co-encapsulate RIF and INH for liposomal dual delivery. RIF was encapsulated in CL-liposomes with/without cholesterol using film hydration method, after which INH was incorporated using a freeze–thawing technique. Dynamic light scattering, differential scanning calorimetry, X-ray diffraction and dialysis were used for liposome characterization. Liposomes containing CL alone (CLL) exhibited 90%encapsulation efficiency for RIF and 59%for INH. The mean size and surface charge of CLL were 1114nm and –63mV, respectively. In addition, CLL showed a controlled release profile for the co-encapsulated drugs. CLL would be promising vehicles for macrophage-targeting drug delivery. The present findings demonstrate the feasibility of using CL for preparation of combination products for liposomal delivery.
- Full Text:
- Authors: Nkanga, Christian I , Noundou, Xavier S , Walker, Roderick B , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/183536 , vital:44005 , xlink:href="https://doi.org/10.17159/0379-4350/2019/v72a11"
- Description: Despite the well-known anti-mycobacterial actions of isoniazid (INH) and rifampicin (RIF), the clinical success of tuberculosis (TB) therapy requires prolonged administration of multiple drugs in high doses, which often result in frequent adverse effects and low patient adherence. Although liposomes are promising candidates for controlled delivery of anti-TB drug, the high cost of synthetic and highly purified natural lipids currently used in liposomal technology might preclude the universal application of therapeutic liposomes. This work aimed at evaluating the potential of a cost-effective lipid material, crude soybean lecithin (CL), to co-encapsulate RIF and INH for liposomal dual delivery. RIF was encapsulated in CL-liposomes with/without cholesterol using film hydration method, after which INH was incorporated using a freeze–thawing technique. Dynamic light scattering, differential scanning calorimetry, X-ray diffraction and dialysis were used for liposome characterization. Liposomes containing CL alone (CLL) exhibited 90%encapsulation efficiency for RIF and 59%for INH. The mean size and surface charge of CLL were 1114nm and –63mV, respectively. In addition, CLL showed a controlled release profile for the co-encapsulated drugs. CLL would be promising vehicles for macrophage-targeting drug delivery. The present findings demonstrate the feasibility of using CL for preparation of combination products for liposomal delivery.
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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:
- 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.
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Encapsulation of isoniazid-conjugated phthalocyanine-In-cyclodextrin-in-liposomes using heating method
- Nkanga, Christian I, Krause, Rui W M
- Authors: Nkanga, Christian I , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193999 , vital:45414 , xlink:href="https://doi.org/10.1038/s41598-019-47991-y"
- Description: Liposomes are reputed colloidal vehicles that hold the promise for targeted delivery of anti-tubercular drugs (ATBDs) to alveolar macrophages that host Mycobacterium tuberculosis. However, the costly status of liposome technology, particularly due to the use of special manufacture equipment and expensive lipid materials, may preclude wider developments of therapeutic liposomes. In this study, we report efficient encapsulation of a complex system, consisting of isoniazid-hydrazone-phthalocyanine conjugate (Pc-INH) in gamma-cyclodextrin (γ-CD), in liposomes using crude soybean lecithin by means of a simple organic solvent-free method, heating method (HM). Inclusion complexation was performed in solution and solid-state, and evaluated using UV-Vis, magnetic circular dichroism, 1H NMR, diffusion ordered spectroscopy and FT-IR. The HM-liposomes afforded good encapsulation efficiency (71%) for such a large Pc-INH/γ-CD complex (PCD) system. The stability and properties of the PCD-HM-liposomes look encouraging; with particle size 240 nm and Zeta potential −57 mV that remained unchanged upon storage at 4 °C for 5 weeks. The release study performed in different pH media revealed controlled release profiles that went up to 100% at pH 4.4, from about 40% at pH 7.4. This makes PCD-liposomes a promising system for site-specific ATBD delivery, and a good example of simple liposomal encapsulation of large hydrophobic compounds.
- Full Text:
- Authors: Nkanga, Christian I , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/193999 , vital:45414 , xlink:href="https://doi.org/10.1038/s41598-019-47991-y"
- Description: Liposomes are reputed colloidal vehicles that hold the promise for targeted delivery of anti-tubercular drugs (ATBDs) to alveolar macrophages that host Mycobacterium tuberculosis. However, the costly status of liposome technology, particularly due to the use of special manufacture equipment and expensive lipid materials, may preclude wider developments of therapeutic liposomes. In this study, we report efficient encapsulation of a complex system, consisting of isoniazid-hydrazone-phthalocyanine conjugate (Pc-INH) in gamma-cyclodextrin (γ-CD), in liposomes using crude soybean lecithin by means of a simple organic solvent-free method, heating method (HM). Inclusion complexation was performed in solution and solid-state, and evaluated using UV-Vis, magnetic circular dichroism, 1H NMR, diffusion ordered spectroscopy and FT-IR. The HM-liposomes afforded good encapsulation efficiency (71%) for such a large Pc-INH/γ-CD complex (PCD) system. The stability and properties of the PCD-HM-liposomes look encouraging; with particle size 240 nm and Zeta potential −57 mV that remained unchanged upon storage at 4 °C for 5 weeks. The release study performed in different pH media revealed controlled release profiles that went up to 100% at pH 4.4, from about 40% at pH 7.4. This makes PCD-liposomes a promising system for site-specific ATBD delivery, and a good example of simple liposomal encapsulation of large hydrophobic compounds.
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Green synthesis of zinc oxide nanoparticles using Solanum torvum (L) leaf extract and evaluation of the toxicological profile of the ZnO nanoparticles–hydrogel composite in Wistar albino rats
- Ezealisiji, Kenneth E, Siwe-Noundou, Xavier, Maduelosi, Blessing, Nwachukwu, Nkemakolam, Krause, Rui W M
- Authors: Ezealisiji, Kenneth E , Siwe-Noundou, Xavier , Maduelosi, Blessing , Nwachukwu, Nkemakolam , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194015 , vital:45416 , xlink:href="https://doi.org/10.1007/s40089-018-0263-1"
- Description: Current study reports a simple and one-pot synthesis of zinc oxide nanoparticles (ZnONPs) using an aqueous extract of Solanum torvum and evaluation of its toxicological profile (0.5% w/w and 1.0% w/w) in Wistar albino rats with respect to the biochemical index. The nanoparticles were characterized using ultraviolet–visible spectroscopy, transmission electron microscopy, Fourier transform infrared spectroscopy and X-ray diffraction technique. Dynamic light scattering (DLS) and zeta potential of synthesized nanoparticles were analyzed to know the average size and stability of particles. Synthesized nanoparticles were stable, discreet, and mostly spherical, and size of particles was within the nanometre range. Biochemical markers of hepatic and renal functions were measured. Zinc oxide nanoparticles significantly decreased serum uric acid level (p less than 0.001) in a dose-dependent manner, while the serum alkaline phosphatase level was increased at the two test doses. The level of alanine transaminase was increased after exposure for 28 days (p less than 0.05). This study concludes that biogenic zinc oxide nanoparticles-infused hydrogel applied dermatologically could affect hepatic and renal performance in rats, and there was an observed cumulative toxicological effect with time of exposure.
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- Authors: Ezealisiji, Kenneth E , Siwe-Noundou, Xavier , Maduelosi, Blessing , Nwachukwu, Nkemakolam , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194015 , vital:45416 , xlink:href="https://doi.org/10.1007/s40089-018-0263-1"
- Description: Current study reports a simple and one-pot synthesis of zinc oxide nanoparticles (ZnONPs) using an aqueous extract of Solanum torvum and evaluation of its toxicological profile (0.5% w/w and 1.0% w/w) in Wistar albino rats with respect to the biochemical index. The nanoparticles were characterized using ultraviolet–visible spectroscopy, transmission electron microscopy, Fourier transform infrared spectroscopy and X-ray diffraction technique. Dynamic light scattering (DLS) and zeta potential of synthesized nanoparticles were analyzed to know the average size and stability of particles. Synthesized nanoparticles were stable, discreet, and mostly spherical, and size of particles was within the nanometre range. Biochemical markers of hepatic and renal functions were measured. Zinc oxide nanoparticles significantly decreased serum uric acid level (p less than 0.001) in a dose-dependent manner, while the serum alkaline phosphatase level was increased at the two test doses. The level of alanine transaminase was increased after exposure for 28 days (p less than 0.05). This study concludes that biogenic zinc oxide nanoparticles-infused hydrogel applied dermatologically could affect hepatic and renal performance in rats, and there was an observed cumulative toxicological effect with time of exposure.
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In vitro antimalarial, antitrypanosomal and HIV-1 integrase inhibitory activities of two Cameroonian medicinal plants
- Fouokeng, Yannick, Feumo Feusso, H M, Mbosso Teinkela, Jean E, Siwe-Noundou, Xavier, Wintjens, René T, Isaacs, Michelle, Hoppe, Heinrich, Krause, Rui W M, Azébazé, Anatole G B, Vardamides, Juliette C
- Authors: Fouokeng, Yannick , Feumo Feusso, H M , Mbosso Teinkela, Jean E , Siwe-Noundou, Xavier , Wintjens, René T , Isaacs, Michelle , Hoppe, Heinrich , Krause, Rui W M , Azébazé, Anatole G B , Vardamides, Juliette C
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195014 , vital:45519 , xlink:href="https://doi.org/10.1016/j.sajb.2018.10.008"
- Description: Antiplasmodial, antitrypanosomal and anti-HIV-1 activities of crude extracts, fractions and some isolated compounds from two Cameroonian medicinal plants: Antrocaryon klaineanum Pierre (Anacardiaceae) and Diospyros conocarpa Gürke ex K. Schum. (Ebenaceae) were assessed. The phytochemical studies led to the isolation of eight compounds (1–8) from Diospyros conocarpa and six compounds (6, 9–13) from Antrocaryon klaineanum. These compounds were identified as mangiferolic acid (1), 3β, 22(S)-dihydroxycycloart-24E-en-26-oic acid (2), lupeol (3), aridanin (4), betulin (5), betulinic acid (6), bergenin (7), D-quercitol(8), entilin C(9), entilin A(10), antrocarine A(11), 7R,20(S)-dihydroxy-4,24(28)-ergostadien-3-one(12) and stigmasterol glucoside (13). The criteria for activity were set as follows: an IC50 value more than 10 μg/mL for crude extracts and more than 1 μg/mL for pure compounds. The hexane/ethyl acetate (1:1) fraction of A.klaineanum root bark (AKERF1) and the hexane/ethyl acetate (1:1) fraction of A.klaineanum trunk bark (AKETF1) presented the strongest antiplasmodial activities with IC50 values of 0.4 and 4.4 μg/mL, respectively. Aridanin (4) and antrocarine A(11), as well as the crude extract of D.conocarpa roots (EDCR), AKERF1 and AKETF1 showed moderate trypanocidal effects. The crude extract of A.klaineanum root bark (AKER) and AKETF1 exhibited attractive activities on HIV-1 integrase with IC50 values of 1.96 and 24.04 μg/mL, respectively. The results provide baseline information on the use of A.klaineanum and D.conocarpa extracts, as well as certain components, as sources of new antiplasmodial, antitrypanosomal and anti-HIV drugs.
- Full Text:
- Authors: Fouokeng, Yannick , Feumo Feusso, H M , Mbosso Teinkela, Jean E , Siwe-Noundou, Xavier , Wintjens, René T , Isaacs, Michelle , Hoppe, Heinrich , Krause, Rui W M , Azébazé, Anatole G B , Vardamides, Juliette C
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195014 , vital:45519 , xlink:href="https://doi.org/10.1016/j.sajb.2018.10.008"
- Description: Antiplasmodial, antitrypanosomal and anti-HIV-1 activities of crude extracts, fractions and some isolated compounds from two Cameroonian medicinal plants: Antrocaryon klaineanum Pierre (Anacardiaceae) and Diospyros conocarpa Gürke ex K. Schum. (Ebenaceae) were assessed. The phytochemical studies led to the isolation of eight compounds (1–8) from Diospyros conocarpa and six compounds (6, 9–13) from Antrocaryon klaineanum. These compounds were identified as mangiferolic acid (1), 3β, 22(S)-dihydroxycycloart-24E-en-26-oic acid (2), lupeol (3), aridanin (4), betulin (5), betulinic acid (6), bergenin (7), D-quercitol(8), entilin C(9), entilin A(10), antrocarine A(11), 7R,20(S)-dihydroxy-4,24(28)-ergostadien-3-one(12) and stigmasterol glucoside (13). The criteria for activity were set as follows: an IC50 value more than 10 μg/mL for crude extracts and more than 1 μg/mL for pure compounds. The hexane/ethyl acetate (1:1) fraction of A.klaineanum root bark (AKERF1) and the hexane/ethyl acetate (1:1) fraction of A.klaineanum trunk bark (AKETF1) presented the strongest antiplasmodial activities with IC50 values of 0.4 and 4.4 μg/mL, respectively. Aridanin (4) and antrocarine A(11), as well as the crude extract of D.conocarpa roots (EDCR), AKERF1 and AKETF1 showed moderate trypanocidal effects. The crude extract of A.klaineanum root bark (AKER) and AKETF1 exhibited attractive activities on HIV-1 integrase with IC50 values of 1.96 and 24.04 μg/mL, respectively. The results provide baseline information on the use of A.klaineanum and D.conocarpa extracts, as well as certain components, as sources of new antiplasmodial, antitrypanosomal and anti-HIV drugs.
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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:
- 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.
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Phytochemical, anti-inflammatory and anti-trypanosomal properties of Anthocleista vogelii Planch (Loganiaceae) stem bark
- Eze, Fabian I, Siwe-Noundou, Xavier, Osadebe, Patience, Krause, Rui W M
- Authors: Eze, Fabian I , Siwe-Noundou, Xavier , Osadebe, Patience , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194059 , vital:45419 , xlink:href="https://doi.org/10.1016/j.jep.2019.111851"
- Description: Ethnopharmacological relevance: Anthocleista vogelii Planch (Loganiaceae) is used in African Traditional Medicine for the treatment of pain and inflammatory disorders as well as sleeping sickness. Aim of the study: To determine the in vivo anti-inflammatory and in vitro anti-trypanosomal activities of the extracts of A. vogelii stem bark and identify the phytochemical classes of the fractions responsible for the activities. Materials and methods: The in vivo anti-inflammatory activity of the extracts was evaluated using the egg albumin-induced rat paw oedema model while the in vitro anti-trypanosomal activity was assessed on Trypanosoma brucei brucei. The in vitro cytotoxicity was assessed on HeLa (human cervix adenocarcinoma) cell line. Results: The methanolic extract of A. vogelii stem bark, with 11.2% yield, gave LD50 > 5000 mg/kg. The n-hexane fraction of the extract contains steroids, terpenes and fatty acids and yielded non-cytotoxic terpenoidal column fraction with anti-trypanosomal IC50 of 3.0 μg/mL. The ethylacetate fraction at 100 mg/kg dose significantly (p less than 0.05) provoked 37.8, 62.5 and 69.7% inhibition of oedema induced by egg-albumin at the second, fourth and sixth hours respectively. Conclusion: The study demonstrated that the anti-inflammatory and anti-trypanosomal activities of A. vogelii are probably due to non-cytotoxic terpenoids and validated the traditional use of A. vogelii in the treatment of inflammation and sleeping sickness.
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- Authors: Eze, Fabian I , Siwe-Noundou, Xavier , Osadebe, Patience , Krause, Rui W M
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194059 , vital:45419 , xlink:href="https://doi.org/10.1016/j.jep.2019.111851"
- Description: Ethnopharmacological relevance: Anthocleista vogelii Planch (Loganiaceae) is used in African Traditional Medicine for the treatment of pain and inflammatory disorders as well as sleeping sickness. Aim of the study: To determine the in vivo anti-inflammatory and in vitro anti-trypanosomal activities of the extracts of A. vogelii stem bark and identify the phytochemical classes of the fractions responsible for the activities. Materials and methods: The in vivo anti-inflammatory activity of the extracts was evaluated using the egg albumin-induced rat paw oedema model while the in vitro anti-trypanosomal activity was assessed on Trypanosoma brucei brucei. The in vitro cytotoxicity was assessed on HeLa (human cervix adenocarcinoma) cell line. Results: The methanolic extract of A. vogelii stem bark, with 11.2% yield, gave LD50 > 5000 mg/kg. The n-hexane fraction of the extract contains steroids, terpenes and fatty acids and yielded non-cytotoxic terpenoidal column fraction with anti-trypanosomal IC50 of 3.0 μg/mL. The ethylacetate fraction at 100 mg/kg dose significantly (p less than 0.05) provoked 37.8, 62.5 and 69.7% inhibition of oedema induced by egg-albumin at the second, fourth and sixth hours respectively. Conclusion: The study demonstrated that the anti-inflammatory and anti-trypanosomal activities of A. vogelii are probably due to non-cytotoxic terpenoids and validated the traditional use of A. vogelii in the treatment of inflammation and sleeping sickness.
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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:
- 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.
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Un-functionalized gold nanoparticles as a simple colorimetric probe for sensitive and selective detection of dopamine
- Khanyile, Nokuthula, Krause, Rui W M, Vilakazi, Sibulelo, Torto, Nelson
- Authors: Khanyile, Nokuthula , Krause, Rui W M , Vilakazi, Sibulelo , Torto, Nelson
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195048 , vital:45522 , xlink:href="http://dx.doi.org/10.17159/0379-4350/2019/v72a27"
- Description: A dopamine (DA) colorimetric probe based on the growth and aggregation of un-functionalized gold nanoparticles (AuNPs) is reported. Upon addition of AuNPs to dopamine at various concentrations, the shape, size and colour change of the nanoparticles results in spectral shifts to higher wavelengths and hence colour change is the mode of detection. The colour change can be easily observed by the naked eye from as low as 5.0 nM DA, even under sub-optimal conditions. Under optimal pH conditions the calculated limit of detection was 2.5 nM (3σ). The probe was successfully applied to whole blood sample and showed good selectivity and sensitivity towards DA. The simple, sensitive and selective probe could be an excellent alternative for on-site and immediate detection of DA without the use of instrumentation and would thus be useful for rapid diagnostic applications.
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- Authors: Khanyile, Nokuthula , Krause, Rui W M , Vilakazi, Sibulelo , Torto, Nelson
- Date: 2019
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195048 , vital:45522 , xlink:href="http://dx.doi.org/10.17159/0379-4350/2019/v72a27"
- Description: A dopamine (DA) colorimetric probe based on the growth and aggregation of un-functionalized gold nanoparticles (AuNPs) is reported. Upon addition of AuNPs to dopamine at various concentrations, the shape, size and colour change of the nanoparticles results in spectral shifts to higher wavelengths and hence colour change is the mode of detection. The colour change can be easily observed by the naked eye from as low as 5.0 nM DA, even under sub-optimal conditions. Under optimal pH conditions the calculated limit of detection was 2.5 nM (3σ). The probe was successfully applied to whole blood sample and showed good selectivity and sensitivity towards DA. The simple, sensitive and selective probe could be an excellent alternative for on-site and immediate detection of DA without the use of instrumentation and would thus be useful for rapid diagnostic applications.
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Conjugation of isoniazid to a zinc phthalocyanine via hydrazone linkage for pH-dependent liposomal controlled release
- Nkanga, Christian, Krause, Rui W M
- Authors: Nkanga, Christian , Krause, Rui W M
- Date: 2018
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194992 , vital:45517 , xlink:href="https://doi.org/10.1007/s13204-018-0776-y"
- Description: Tuberculosis (TB) remains the leading cause of mortality from infectious diseases. Extended TB treatment and frequent adverse effects, due to poor bioavailability of anti-tubercular drugs (ATBDs), represent the main rationales behind liposomal encapsulation for controlled delivery. Liposomes have been reported as potential vehicles for targeted delivery of ATBDs due to their rapid uptake by macrophages, which are known as the main host cells for TB causative agent (Mycobacterium tuberculosis). Additionally, the need for controlled release of ATBDs arises because leakage is part of the key liposome challenges for hydrophilic compounds like isoniazid (INH). In this study, INH was conjugated to a highly hydrophobic photosensitizer, zinc (II) phthalocyanine (PC), through hydrazone bonding. The obtained conjugate (PC–INH) was encapsulated in liposomes by film hydration method. PC–INH loaded liposomes (PILs) were characterized using dynamic light scattering, transmission electron microscopy, energy-dispersive X-ray spectrometry and UV–Vis absorption spectrometry, which was used also for estimation of encapsulation efficiency (%EE). INH release was evaluated in different pH media using dialysis. Particle size, zeta potential and %EE of PILs were about 506 nm, − 55 mV and 72%, respectively. Over 12 h, PILs exhibited 22, 41, 97 and 100% of INH, respectively, released in pH 7.4, 6.4, 5.4 and 4.4 media. This pH-dependent behavior is attractive for site-specific delivery. These findings suggest the conjugation of chemotherapeutics to phthalocyanines using pH-labile linkages as a potential strategy for liposomal controlled release.
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- Authors: Nkanga, Christian , Krause, Rui W M
- Date: 2018
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/194992 , vital:45517 , xlink:href="https://doi.org/10.1007/s13204-018-0776-y"
- Description: Tuberculosis (TB) remains the leading cause of mortality from infectious diseases. Extended TB treatment and frequent adverse effects, due to poor bioavailability of anti-tubercular drugs (ATBDs), represent the main rationales behind liposomal encapsulation for controlled delivery. Liposomes have been reported as potential vehicles for targeted delivery of ATBDs due to their rapid uptake by macrophages, which are known as the main host cells for TB causative agent (Mycobacterium tuberculosis). Additionally, the need for controlled release of ATBDs arises because leakage is part of the key liposome challenges for hydrophilic compounds like isoniazid (INH). In this study, INH was conjugated to a highly hydrophobic photosensitizer, zinc (II) phthalocyanine (PC), through hydrazone bonding. The obtained conjugate (PC–INH) was encapsulated in liposomes by film hydration method. PC–INH loaded liposomes (PILs) were characterized using dynamic light scattering, transmission electron microscopy, energy-dispersive X-ray spectrometry and UV–Vis absorption spectrometry, which was used also for estimation of encapsulation efficiency (%EE). INH release was evaluated in different pH media using dialysis. Particle size, zeta potential and %EE of PILs were about 506 nm, − 55 mV and 72%, respectively. Over 12 h, PILs exhibited 22, 41, 97 and 100% of INH, respectively, released in pH 7.4, 6.4, 5.4 and 4.4 media. This pH-dependent behavior is attractive for site-specific delivery. These findings suggest the conjugation of chemotherapeutics to phthalocyanines using pH-labile linkages as a potential strategy for liposomal controlled release.
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Facile synthesis of glutathione-l-Cysteine co-capped CdTe core shell system
- Daramola, Olamide A, Siwe-Noundou, Xavier, Krause, Rui W M, Marks, John A
- Authors: Daramola, Olamide A , Siwe-Noundou, Xavier , Krause, Rui W M , Marks, John A
- Date: 2017
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195003 , vital:45518 , xlink:href="https://doi.org/10.1166/jnn.2017.13823"
- Description: Semiconductor nanoparticles also known as quantum dots (QDs) have been used in diverse areas of application due to their good optical and photo-physical properties. The synthesis of core–shell QDs have assisted to improve the stability of most nano-particles but the size and long term stability of such materials have been problematic. However, thiol-capped CdTe QDs have been regarded as some of the most widely synthesized nanoparticles due to their unique optical properties. The use of un-stable tellurium source such as NaHTe or highly toxic H2Te gas makes the reaction condition cumbersome. In this study, we prepared some CdTe QDs and core–shell QDs using K2TeO3 as a stable source of tellurium without inert gas protection. This was done using a co-capped bio-compatible coating such as cysteine and glutathione following a modified standard method to produce QDs in the yields of about 60 to 80%. All the synthesized materials were subsequently characterized using various characterization techniques. The systematic optimization of the reaction parameters such as reaction time, pH and mole ratio results with a drastic red shift in wavelength (546–600 nm) by the CdTe core proved that an extra material has been deposited unto the surface of the CdTe core. The 60 days stability test conducted demonstrated that the core–shell nanoparticles were quite stable. Since this reaction was performed under open air conditions and no special ligand or buffer solution was used, it may suitably be applied on an industrial scale.
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- Authors: Daramola, Olamide A , Siwe-Noundou, Xavier , Krause, Rui W M , Marks, John A
- Date: 2017
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195003 , vital:45518 , xlink:href="https://doi.org/10.1166/jnn.2017.13823"
- Description: Semiconductor nanoparticles also known as quantum dots (QDs) have been used in diverse areas of application due to their good optical and photo-physical properties. The synthesis of core–shell QDs have assisted to improve the stability of most nano-particles but the size and long term stability of such materials have been problematic. However, thiol-capped CdTe QDs have been regarded as some of the most widely synthesized nanoparticles due to their unique optical properties. The use of un-stable tellurium source such as NaHTe or highly toxic H2Te gas makes the reaction condition cumbersome. In this study, we prepared some CdTe QDs and core–shell QDs using K2TeO3 as a stable source of tellurium without inert gas protection. This was done using a co-capped bio-compatible coating such as cysteine and glutathione following a modified standard method to produce QDs in the yields of about 60 to 80%. All the synthesized materials were subsequently characterized using various characterization techniques. The systematic optimization of the reaction parameters such as reaction time, pH and mole ratio results with a drastic red shift in wavelength (546–600 nm) by the CdTe core proved that an extra material has been deposited unto the surface of the CdTe core. The 60 days stability test conducted demonstrated that the core–shell nanoparticles were quite stable. Since this reaction was performed under open air conditions and no special ligand or buffer solution was used, it may suitably be applied on an industrial scale.
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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.
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- 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.
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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.
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- 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.
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A colorimetric probe for dopamine based on gold nanoparticles-electrospun nanofibre composite
- Ngomane, Nokuthula, Torto, Nelson, Krause, Rui W M, Vilakazi, Sibulelo
- Authors: Ngomane, Nokuthula , Torto, Nelson , Krause, Rui W M , Vilakazi, Sibulelo
- Date: 2015
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195407 , vital:45562 , xlink:href="https://doi.org/10.1016/j.matpr.2015.08.036"
- Description: An easily prepared solid state colorimetric probe for detecting the neurotransmitter dopamine (DA) was developed. The probe, in the form of an electrospun Nylon−6 (N6) nanofibre with embedded un−functionalized gold nanoparticles (UF−AuNPs) produces a clear colour change in the presence of a DA that is detectable by the naked eye. Characterisation of the nanofibre using UV/vis spectroscopy and electron microscopy (TEM) confirmed the formation of the AuNPs in the polymer solution, and that the AuNPs were completely encapsulated within the composite nanofibres before exposure to the analytes. The probe exhibited very high sensitivity towards DA resulting in colour change of the composite fibres from purple to navy blue/black even under low concentrations of DA. The probe was also selective to DA since the colour remained unchanged in the presence of commonly encountered interfering species such as ascorbic acid, uric acid, catechol, epinephrine and norepinephrine. Moreover, the colour change was observed rapid, occurring either immediately on contact with higher concentrations (5 x10−4 M) or within about 3−5 min for the lower concentrations (e.g. 5 x10−7 M). Since this probe does not require the use of any instruments, and is both rapid and stable over time, it can be applied in the field by an inexperienced person.
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- Authors: Ngomane, Nokuthula , Torto, Nelson , Krause, Rui W M , Vilakazi, Sibulelo
- Date: 2015
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195407 , vital:45562 , xlink:href="https://doi.org/10.1016/j.matpr.2015.08.036"
- Description: An easily prepared solid state colorimetric probe for detecting the neurotransmitter dopamine (DA) was developed. The probe, in the form of an electrospun Nylon−6 (N6) nanofibre with embedded un−functionalized gold nanoparticles (UF−AuNPs) produces a clear colour change in the presence of a DA that is detectable by the naked eye. Characterisation of the nanofibre using UV/vis spectroscopy and electron microscopy (TEM) confirmed the formation of the AuNPs in the polymer solution, and that the AuNPs were completely encapsulated within the composite nanofibres before exposure to the analytes. The probe exhibited very high sensitivity towards DA resulting in colour change of the composite fibres from purple to navy blue/black even under low concentrations of DA. The probe was also selective to DA since the colour remained unchanged in the presence of commonly encountered interfering species such as ascorbic acid, uric acid, catechol, epinephrine and norepinephrine. Moreover, the colour change was observed rapid, occurring either immediately on contact with higher concentrations (5 x10−4 M) or within about 3−5 min for the lower concentrations (e.g. 5 x10−7 M). Since this probe does not require the use of any instruments, and is both rapid and stable over time, it can be applied in the field by an inexperienced person.
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