Screening of Anthocleista djalonesis Fractions and Compounds against HIV-1 Integrase and HIV-1 Protease
by Ijeoma Solomon Okoro(1), Terrumun AmomTor-Anyiin(1), John Ogbaji Igoli(1), Muluh Emmanuel Khan(1) and Mbeh Ubanga Eteng(2)
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, HIVFRET (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 ß-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 ß-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. Keywords: Anthocleista djalonensis, Bauerenol, Bauerenone, HIV-1 integrase, HIV-1 protease,
1 – Department of Chemistry, Federal University of Agriculture, P.M.B. 2373, Makurdi, Benue State,
2 – Department of Biochemistry, Faculty of Sciences, University of Calabar, P.M.B. 1115, Calabar, Cross
This work was carried out in collaboration between all authors. Author ISO designed the study, performed the statistical analysis, wrote the protocol and wrote the first draft of the manuscript. Authors ISO and MUE managed the analyses of the study. Author TATA managed the literature searches. Authors JOI and MEK identified the compounds. All authors read and approved the final manuscript.
Prof Mbeh Eteng
Mbeh Eteng is a Professor of Biochemistry in the Faculty of University of Calabar. He holds a Ph.D from the University of Calabar (2000). He was Dean of Faculty of Basic Medical Science (2012-2016) and Chairman Committee of Deans (2014-2015). Member Governing Board UCTH, Calabar (2018 -till date). Fellow, Institute of Co-operate Administration. His current area of research is on malaria/prostrate hyperplaxia and medicinal plants research and use in management. He has successfully supervised 25 Ph.Ds.
Get to know more about him and access more of his publications through his personal knowledgebase – http://www.mbeheteng.com.ng
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