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:
- 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:
Biological activity of plant extracts and isolated compounds from Alchornea laxiflora: Anti-HIV, antibacterial and cytotoxicity evaluation
- Ndinteh, Derek T, Olivier, D 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, D 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:
- Authors: Ndinteh, Derek T , Olivier, D 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.
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