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
Biological activity of plant extracts and isolated compounds from Alchornea laxiflora: Anti-HIV, antibacterial and cytotoxicity evaluation
- Ndinteh, Derek T, Olivier, Denise K, Noundou, Xavier S, Krause, Rui W M, Mnkandhla, D, Isaacs, Michelle, Hoppe, Heinrich C, Muganza, F M, Mbafor, J T, Van Vuuren, S F, Patnala, S
- Authors: Ndinteh, Derek T , Olivier, Denise K , Noundou, Xavier S , Krause, Rui W M , Mnkandhla, D , Isaacs, Michelle , Hoppe, Heinrich C , Muganza, F M , Mbafor, J T , Van Vuuren, S F , Patnala, S
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126634 , vital:35907 , https://doi.org/10.1016/j.sajb.2018.08.010
- Description: This study was designed to assess the cytotoxicity, anti-HIV and antibacterial efficacy of various solvent extracts of roots, stem and leaves of Alchornea laxiflora, as well as five compounds isolated from its methanolic stem extract viz.; ellagic acid (1); 3-O-methyl-ellagic acid (2), 3-O-β-d-glucopyranosyl-β-sitosterol (3), 3-O-acetyl-oleanolic acid (4) and 3-O-acetyl-ursolic acid (5). The tested crude extracts were prepared from several solvent polarities including: hexane (Hex), chloroform (CHCl3), ethyl acetate (EtOAc), ethanol (EtOH), methanol (MeOH) and water (H2O). The anti-HIV properties were assessed on HIV-1 subtype C integrase while the cytotoxicity was tested against Hela cells. The antibacterial activity was studied on a panel of pathogens including gastrointestinal, skin, respiratory and urinary-tract infection causing Gram positive bacteria viz.; Bacillus cereus (ATCC 11778), Enterococcus faecalis (ATCC 29212), Staphylococcus aureus (ATCC 25923) and Staphylococcus saprophyticus (ATCC 15305)] and Gram-negative bacteria, i.e., Escherichia coli (ATCC 25922), Klebsiella pneumoniae (ATCC 13883), Moraxella catarrhalis (ATCC 23246). All the tested samples were determined to be non-toxic due to the low inhibitions observed. The most potent anti-HIV activity was observed for the methanolic extract of A. laxiflora root (ALR4) with an IC50 value of 0.21 ng/ml, which was more active than chicoric acid used as reference drug (6.82 nM). Roots, stem and leaves of A. laxiflora extracts exhibited antibacterial activities against most of the Gram-positive bacteria with the minimum inhibitory concentrations (MIC) ranging between 50 and 63 μg/ml. Compounds 1–5 displayed antibacterial activities against S. saprophyticus with MIC values as low as 4 μg/ml. The results inferred from this study demonstrate the potential of A. laxiflora root as a source for new anti-HIV drugs and scientifically validate the traditional use of A. laxiflora in the treatment of gastrointestinal, skin, respiratory and urinary tract related infections. These results reaffirm the ethnopharmacological significance of African traditional medicines.
- Full Text:
- Date Issued: 2018
- Authors: Ndinteh, Derek T , Olivier, Denise K , Noundou, Xavier S , Krause, Rui W M , Mnkandhla, D , Isaacs, Michelle , Hoppe, Heinrich C , Muganza, F M , Mbafor, J T , Van Vuuren, S F , Patnala, S
- Date: 2018
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/126634 , vital:35907 , https://doi.org/10.1016/j.sajb.2018.08.010
- Description: This study was designed to assess the cytotoxicity, anti-HIV and antibacterial efficacy of various solvent extracts of roots, stem and leaves of Alchornea laxiflora, as well as five compounds isolated from its methanolic stem extract viz.; ellagic acid (1); 3-O-methyl-ellagic acid (2), 3-O-β-d-glucopyranosyl-β-sitosterol (3), 3-O-acetyl-oleanolic acid (4) and 3-O-acetyl-ursolic acid (5). The tested crude extracts were prepared from several solvent polarities including: hexane (Hex), chloroform (CHCl3), ethyl acetate (EtOAc), ethanol (EtOH), methanol (MeOH) and water (H2O). The anti-HIV properties were assessed on HIV-1 subtype C integrase while the cytotoxicity was tested against Hela cells. The antibacterial activity was studied on a panel of pathogens including gastrointestinal, skin, respiratory and urinary-tract infection causing Gram positive bacteria viz.; Bacillus cereus (ATCC 11778), Enterococcus faecalis (ATCC 29212), Staphylococcus aureus (ATCC 25923) and Staphylococcus saprophyticus (ATCC 15305)] and Gram-negative bacteria, i.e., Escherichia coli (ATCC 25922), Klebsiella pneumoniae (ATCC 13883), Moraxella catarrhalis (ATCC 23246). All the tested samples were determined to be non-toxic due to the low inhibitions observed. The most potent anti-HIV activity was observed for the methanolic extract of A. laxiflora root (ALR4) with an IC50 value of 0.21 ng/ml, which was more active than chicoric acid used as reference drug (6.82 nM). Roots, stem and leaves of A. laxiflora extracts exhibited antibacterial activities against most of the Gram-positive bacteria with the minimum inhibitory concentrations (MIC) ranging between 50 and 63 μg/ml. Compounds 1–5 displayed antibacterial activities against S. saprophyticus with MIC values as low as 4 μg/ml. The results inferred from this study demonstrate the potential of A. laxiflora root as a source for new anti-HIV drugs and scientifically validate the traditional use of A. laxiflora in the treatment of gastrointestinal, skin, respiratory and urinary tract related infections. These results reaffirm the ethnopharmacological significance of African traditional medicines.
- Full Text:
- Date Issued: 2018
Secondary metabolites from Tetracera potatoria stem bark with anti-mycobacterial activity.
- Fomogne-Fodjo, M C Y, Ndinteh, Derek T, Olivier, Denise K, Krause, Rui W M, Kempgens, Pierre, Van Vuuren, S
- Authors: Fomogne-Fodjo, M C Y , Ndinteh, Derek T , Olivier, Denise K , Krause, Rui W M , Kempgens, Pierre , Van Vuuren, S
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125556 , vital:35795 , https://doi.org/10.1016/j.jep.2016.11.027
- Description: Ethnopharmacological relevance Tetracera potatoria Afzel. Exg. Don (Dilleniaceae) is a medicinal plant used traditionally in Africa for the treatment of tuberculosis related ailments and respiratory infections. The antibacterial activity of the medium polar extracts of T. potatoria leaves and stem bark was recently reported against Mycobacterium smegmatis (MIC 25 µg/mL) and M. aurum (65 µg/mL), two fast-growing Mycobacterium strains used as model micro-organisms for the more pathogenic strain Mycobacterium tuberculosis (Fomogne-Fodjo et al., 2014). The aim of this study was consequently to isolate the compounds possibly contributing to this activity, and which may therefore be promising precursors to be used for the development of novel anti-TB drugs.
- Full Text:
- Date Issued: 2017
- Authors: Fomogne-Fodjo, M C Y , Ndinteh, Derek T , Olivier, Denise K , Krause, Rui W M , Kempgens, Pierre , Van Vuuren, S
- Date: 2017
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125556 , vital:35795 , https://doi.org/10.1016/j.jep.2016.11.027
- Description: Ethnopharmacological relevance Tetracera potatoria Afzel. Exg. Don (Dilleniaceae) is a medicinal plant used traditionally in Africa for the treatment of tuberculosis related ailments and respiratory infections. The antibacterial activity of the medium polar extracts of T. potatoria leaves and stem bark was recently reported against Mycobacterium smegmatis (MIC 25 µg/mL) and M. aurum (65 µg/mL), two fast-growing Mycobacterium strains used as model micro-organisms for the more pathogenic strain Mycobacterium tuberculosis (Fomogne-Fodjo et al., 2014). The aim of this study was consequently to isolate the compounds possibly contributing to this activity, and which may therefore be promising precursors to be used for the development of novel anti-TB drugs.
- Full Text:
- Date Issued: 2017
Synthesis of silver nanoparticles from a Desmodium adscendens extract and its antibacterial evaluation on wound dressing material
- Lakkakula, Jaya R, Ndinteh, Derek T, van Vuuren, Sandy F, Olivier, Denise K, Krause, Rui W M
- Authors: Lakkakula, Jaya R , Ndinteh, Derek T , van Vuuren, Sandy F , Olivier, Denise K , Krause, Rui W M
- Date: 2017
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195025 , vital:45520 , xlink:href="https://doi.org/10.1049/iet-nbt.2017.0084"
- Description: The one-pot synthesis of silver nanoparticles (AgNPs) using the medium-polar extract of Desmodium adscendens (Sw.) DC. is presented here as an alternative synthesis of metal NPs. Characterisation of the formed NPs showed polydispersed AgNPs ranging from 15 to 100 nm where the concentration of metal ions was found to play a role in the size and shape of the prepared NPs. It could be established that the flavonoids, saponins, and alkaloids present in the extract acted as both reducing and stabilising agents during the formation of the capped metal NPs. This means of NP synthesis was also employed during the in situ immobilisation of AgNPs on gauze and plaster. An evaluation of the antibacterial activity of the medium-polar D. adscendens extract, AgNPs suspended in solution, and the immobilised AgNPs against Staphylococcus aureus (ATCC 25923), Bacillus cereus (ATCC 11778), and Escherichia coli (ATCC 25922) showed high efficacy against the latter in particular. This suggests that gauze, dilute silver nitrate solutions, and D. adscendens extract could be used successfully in the simple in situ preparation of effective antibacterial wound dressings.
- Full Text:
- Date Issued: 2017
- Authors: Lakkakula, Jaya R , Ndinteh, Derek T , van Vuuren, Sandy F , Olivier, Denise K , Krause, Rui W M
- Date: 2017
- Subjects: To be catalogued
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/195025 , vital:45520 , xlink:href="https://doi.org/10.1049/iet-nbt.2017.0084"
- Description: The one-pot synthesis of silver nanoparticles (AgNPs) using the medium-polar extract of Desmodium adscendens (Sw.) DC. is presented here as an alternative synthesis of metal NPs. Characterisation of the formed NPs showed polydispersed AgNPs ranging from 15 to 100 nm where the concentration of metal ions was found to play a role in the size and shape of the prepared NPs. It could be established that the flavonoids, saponins, and alkaloids present in the extract acted as both reducing and stabilising agents during the formation of the capped metal NPs. This means of NP synthesis was also employed during the in situ immobilisation of AgNPs on gauze and plaster. An evaluation of the antibacterial activity of the medium-polar D. adscendens extract, AgNPs suspended in solution, and the immobilised AgNPs against Staphylococcus aureus (ATCC 25923), Bacillus cereus (ATCC 11778), and Escherichia coli (ATCC 25922) showed high efficacy against the latter in particular. This suggests that gauze, dilute silver nitrate solutions, and D. adscendens extract could be used successfully in the simple in situ preparation of effective antibacterial wound dressings.
- Full Text:
- Date Issued: 2017
Interactive efficacies of Elephantorrhiza elephantina and Pentanisia prunelloides extracts and isolated compounds against gastrointestinal bacteria
- Mpofu, Smart J, Olivier, Denise K, Krause, Rui W M, Ndinteh, Derek T, Van Vuuren, S
- Authors: Mpofu, Smart J , Olivier, Denise K , Krause, Rui W M , Ndinteh, Derek T , Van Vuuren, S
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/124122 , vital:35552 , https://doi.org/10.1016/j.sajb.2014.07.002
- Description: Elephantorrhiza elephantina (Burch.) Skeels (Fabaceae) and Pentanisia prunelloides (Klotzsch ex Eckl. & Zeyh.) Walp. (Rubiaceae) are two medicinal plants used extensively in southern Africa to treat various ailments. Often, decoctions and infusions from these two plants are used in combination specifically for stomach ailments. The antimicrobial activities of the methanol and aqueous extracts of the rhizomes of the two plants, as well as the two active ingredients from the plants [(−)-epicatechin and palmitic acid] have been determined apart and in combination against Enterococcus faecalis (ATCC 29212), Escherichia coli (ATCC 8739) and Bacillus cereus (ATCC 11778). The minimum inhibitory concentration (MIC) values for the aqueous (0.50–16.00 mg/mL) and methanol (0.20–16.00 mg/mL) extracts independently demonstrated varied efficacies depending on the pathogen of study. When the two plants were combined in 1:1 ratios, synergistic to additive interactions (ΣFIC values 0.19–1.00) were noted. Efficacy for the two major compounds ranged between 0.13–0.63 mg/mL and mainly synergistic interactions were noted against E. faecalis and E. coli. The predominantly synergistic interactions noted between E. elephantina and P. prunelloides and major compounds, when tested in various ratios against these pathogens, provide some validation as to the traditional use of these two plants to treat bacterial gastrointestinal infections.
- Full Text:
- Date Issued: 2014
- Authors: Mpofu, Smart J , Olivier, Denise K , Krause, Rui W M , Ndinteh, Derek T , Van Vuuren, S
- Date: 2014
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/124122 , vital:35552 , https://doi.org/10.1016/j.sajb.2014.07.002
- Description: Elephantorrhiza elephantina (Burch.) Skeels (Fabaceae) and Pentanisia prunelloides (Klotzsch ex Eckl. & Zeyh.) Walp. (Rubiaceae) are two medicinal plants used extensively in southern Africa to treat various ailments. Often, decoctions and infusions from these two plants are used in combination specifically for stomach ailments. The antimicrobial activities of the methanol and aqueous extracts of the rhizomes of the two plants, as well as the two active ingredients from the plants [(−)-epicatechin and palmitic acid] have been determined apart and in combination against Enterococcus faecalis (ATCC 29212), Escherichia coli (ATCC 8739) and Bacillus cereus (ATCC 11778). The minimum inhibitory concentration (MIC) values for the aqueous (0.50–16.00 mg/mL) and methanol (0.20–16.00 mg/mL) extracts independently demonstrated varied efficacies depending on the pathogen of study. When the two plants were combined in 1:1 ratios, synergistic to additive interactions (ΣFIC values 0.19–1.00) were noted. Efficacy for the two major compounds ranged between 0.13–0.63 mg/mL and mainly synergistic interactions were noted against E. faecalis and E. coli. The predominantly synergistic interactions noted between E. elephantina and P. prunelloides and major compounds, when tested in various ratios against these pathogens, provide some validation as to the traditional use of these two plants to treat bacterial gastrointestinal infections.
- Full Text:
- Date Issued: 2014
Synthesis and magnetic properties of a superparamagnetic nanocomposite pectin-magnetite nanocomposite
- Namanga, Jude, Foba, Josepha, Ndinteh, Derek T, Yufanyi, Divine M, Krause, Rui W M
- Authors: Namanga, Jude , Foba, Josepha , Ndinteh, Derek T , Yufanyi, Divine M , Krause, Rui W M
- Date: 2013
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125075 , vital:35726 , https://doi.org/10.1155/2013/137275
- Description: Magnetic nanocomposites composed of superparamagnetic magnetite nanoparticles in a pectin matrix were synthesized by anin situ coprecipitation method. The pectin matrix acted as a stabilizer and size control host for the magnetite nanoparticles(MNPs) ensuring particle size homogeneity. The effects of the different reactant ratios and nanocomposite drying conditions onthe magnetic properties were investigated. The nanocomposites were characterized by X-ray diffraction (XRD), scanning electronmicroscopy (SEM), transmission electron microscopy (TEM), energy dispersive X-ray spectroscopy (EDX), Fourier-transforminfrared (FT-IR) spectroscopy, and superconducting quantum interference device magnetometer (SQUID). Superparamagneticmagnetite nanoparticles with mean diameters of 9 and 13 nm were obtained, and the freeze-dried nanocomposites had a saturationmagnetization of 54 and 53 emu/g, respectivel
- Full Text:
- Date Issued: 2013
- Authors: Namanga, Jude , Foba, Josepha , Ndinteh, Derek T , Yufanyi, Divine M , Krause, Rui W M
- Date: 2013
- Language: English
- Type: text , article
- Identifier: http://hdl.handle.net/10962/125075 , vital:35726 , https://doi.org/10.1155/2013/137275
- Description: Magnetic nanocomposites composed of superparamagnetic magnetite nanoparticles in a pectin matrix were synthesized by anin situ coprecipitation method. The pectin matrix acted as a stabilizer and size control host for the magnetite nanoparticles(MNPs) ensuring particle size homogeneity. The effects of the different reactant ratios and nanocomposite drying conditions onthe magnetic properties were investigated. The nanocomposites were characterized by X-ray diffraction (XRD), scanning electronmicroscopy (SEM), transmission electron microscopy (TEM), energy dispersive X-ray spectroscopy (EDX), Fourier-transforminfrared (FT-IR) spectroscopy, and superconducting quantum interference device magnetometer (SQUID). Superparamagneticmagnetite nanoparticles with mean diameters of 9 and 13 nm were obtained, and the freeze-dried nanocomposites had a saturationmagnetization of 54 and 53 emu/g, respectivel
- Full Text:
- Date Issued: 2013
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