Screening of Anthocleista djalonesis Fractions and Compounds against HIV-1 Integrase and HIV-1 Protease
Journal Title: Journal of Complementary and Alternative Medical Research - Year 2017, Vol 4, Issue 1
Abstract
Aim: HIV, the virus that causes AIDS, is one of the world’s deadliest diseases today. Drug resistance and narrow spectrum of available therapeutics is a main problem during HIV treatment. Therefore, new drugs effective against drug-resistant HIV strains are needed. The aim of this study was to screen Anthocleista djalonensis extracts, fractions and isolated compounds for in vitro anti-HIV-1 Integrase (HIV-1 IN) and HIV-1 Protease (HIV -1 PR) activities. Place and Duration of Study: The study was carried out in the Department of Organic Chemistry, Rhodes University, Grahamstown, South Africa. The period was between March and July, 2016. Methodology: The ethyl acetate and acetone extracts of the roots of Anthocleista djalonensis and fractions and compounds obtained from column chromatography of acetone extract were screened for their inhibitory activity against HIV -1 Integrase using a non-radioactive ELISA-based HIV-1 integrase assay. The screening was carried out at concentration range of 10-5 -102 μg/ml. The screening for anti-protease activity was performed using a fluorogenic octapeptide substrate, HIV-FRET (1) and a recombinant HIV-1 Protease solution. Results: The ethyl acetate and acetone extracts showed inhibitory effects on HIV -1 Integrase with IC50 of 1.3001 ± 0.217 µg/mL and 0.7216 ± 0.0028 µg/mL respectively. IC50 values of 0.0077 ± 0.009 µg/mL, 5.0001± 0.1719 µg/mL, 3.5113 ± 0.3613 µg/mL and 0.0736 ± 0.0005 µg/ml were obtained for chromatographic fractions F-1, F-2, F-3 and F-4 respectively. The compounds Bauerenone, Bauerenol and a mixture of Stigmasterol and β-Sitosterol isolated from A. djalonensis had IC50 values of 5.6112 ± 0.8767 µg/mL, 4.8075 ± 0.0732 µg/mL and 0.8916 ± 0.0327 respectively. Conclusion: Bauerenone, Bauerenol and a mixture of Stigmasterol and β-Sitosterol isolated from A. djalonensis showed significant (P< 0.05) inhibitory activities against HIV-1 Integrase. However, there was no activity against HIV-1 protease at 50 µg/mL by the extracts, fractions and isolated compounds.
Authors and Affiliations
Ijeoma Solomon Okoro, Terrumun AmomTor-Anyiin, John Ogbaji Igoli, Muluh Emmanuel Khan, Mbeh Ubanga Eteng
Keywords
Related Articles
- EP ID EP337210
- DOI 10.9734/JOCAMR/2017/36908
- Views 72
- Downloads 0
In-vitro DPPH Free Radical Scavenging Activity of the Plant Murraya koenigii Linn (Curry Leaf) in Rajshahi, Bangladesh
Aim: The use of herbal medicine is becoming popular day by day due to toxicity and side effects of allopathic medicines and hence the present study was carried out to assess the in-vitro DPPH free radical scavenging pote...
Chemical Constituents and Nutrient Composition of Carica papaya and Vernonia amygdalina Leaf Extracts
The present study evaluates the chemical constituents and nutrient composition of leaf extracts of Carica papaya and Vernonia amygdalina. The chemical constituents were analysed using gas chromatography mass spectrometry...
Comparing the Antimicrobial Potential of Sahara Honey from Algeria and Manuka Honey against Urogenital Microorganisms
Aims: Various studies have been conducted to investigate the antimicrobial properties of honey from different parts of the world. To date; no extensive studies of the antimicrobial properties of Sahara honey (SH) on urog...
Triterpenoids from Poria cocos and Their Potential In vitro Hepatoprotective Effects
Aims: To isolate triterpenoids from the surface layer of Poria cocos and evaluate their hepatoprotective activities in vitro. Study Design: Triterpenoids were isolated and identified from the surface layer of Poria cocos...
Effects of Moringa oleifera Leaf Powder Suspension on the Pharmacokinetics of Amodiaquine in Rats
Aims: Moringa oleifera Lam (Moringaceae) is commonly used as food plant, food supplement and as medicine in most African countries. With increasing acceptance and use of M. oleifera as food and medicine, the possibility...