{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,9]],"date-time":"2026-03-09T05:26:13Z","timestamp":1773033973350,"version":"3.50.1"},"reference-count":30,"publisher":"MDPI AG","issue":"8","license":[{"start":{"date-parts":[[2022,8,15]],"date-time":"2022-08-15T00:00:00Z","timestamp":1660521600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"University of Fribourg in Switzerland","award":["No 13-174 RG\/CHE\/AF\/AC_G"],"award-info":[{"award-number":["No 13-174 RG\/CHE\/AF\/AC_G"]}]},{"name":"University of Fribourg in Switzerland","award":["UNESCO FR: 3240277733"],"award-info":[{"award-number":["UNESCO FR: 3240277733"]}]},{"name":"TWAS (The World Academic of Science)","award":["No 13-174 RG\/CHE\/AF\/AC_G"],"award-info":[{"award-number":["No 13-174 RG\/CHE\/AF\/AC_G"]}]},{"name":"TWAS (The World Academic of Science)","award":["UNESCO FR: 3240277733"],"award-info":[{"award-number":["UNESCO FR: 3240277733"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceutics"],"abstract":"<jats:p>The aim of this study was to identify bioactive secondary metabolites from Ochna rhizomatosa with potential inhibitory effects against HIV and Plasmodium falciparum. A phytochemical study of O. rhizomatosa root barks resulted in the identification of three new biflavonoids (1\u20133), along with four known ones (4\u20137). Compound 7 (Gerontoisoflavone A) was a single flavonoid present in the rootbark of the plant and was used as a reference. Compound 1 (IC50 = 0.047 \u00b5M) was the only one with a noteworthy inhibitory effect against HIV-1 integrase in vitro. Chicoric acid (IC50 = 0.006 \u00b5M), a pure competitive inhibitor of HIV-1 integrase, was used as control. Compound 2 exhibited the highest antiplasmodial activity (IC50 = 4.60 \u00b5M) against the chloroquine-sensitive strain of Plasmodium falciparum NF54. Computational molecular docking revealed that compounds 1 and 2 had the highest binding score (\u2212121.8 and \u2212131.88 Kcal\/mol, respectively) in comparison to chicoric acid and Dolutegravir (\u2212116 and \u2212100 Kcal\/mol, respectively), towards integrase receptor (PDB:3LPT). As far as Plasmodium-6 cysteine s48\/45 domain inhibition is concerned, compounds 1 and 2 showed the highest binding scores in comparison to chloroquine, urging the analysis of these compounds in vivo for disease treatment. These results confirm the potential inhibitory effect of compounds 1 and 2 for HIV and malaria treatment. Therefore, our future investigation to find inhibitors of these receptors in vivo could be an effective strategy for developing new drugs.<\/jats:p>","DOI":"10.3390\/pharmaceutics14081701","type":"journal-article","created":{"date-parts":[[2022,8,15]],"date-time":"2022-08-15T23:44:03Z","timestamp":1660607043000},"page":"1701","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":9,"title":["In Vitro and In Silico Potential Inhibitory Effects of New Biflavonoids from Ochna rhizomatosa on HIV-1 Integrase and Plasmodium falciparum"],"prefix":"10.3390","volume":"14","author":[{"given":"Ang\u00e9lique Nicolas","family":"Messi","sequence":"first","affiliation":[{"name":"Department of Organic Chemistry, Faculty of Science, University of Yaounde I, Yaounde P.O. Box 812, Cameroon"},{"name":"Department of Chemistry, University of the Free State, 205 Nelson Mandela Avenue, Bloemfontein 9301, South Africa"},{"name":"Department of Chemistry, University of Fribourg, Chemin du Mus\u00e9e 9, CH-1700 Fribourg, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Susan Lucia","family":"Bonnet","sequence":"additional","affiliation":[{"name":"Department of Chemistry, University of the Free State, 205 Nelson Mandela Avenue, Bloemfontein 9301, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Brice Ayissi","family":"Owona","sequence":"additional","affiliation":[{"name":"Department of Biochemistry, Faculty of Science, University of Yaounde I, Yaounde P.O. Box 812, Cameroon"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4561-5589","authenticated-orcid":false,"given":"Anke","family":"Wilhelm","sequence":"additional","affiliation":[{"name":"Department of Chemistry, University of the Free State, 205 Nelson Mandela Avenue, Bloemfontein 9301, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Eutrophe Le Doux","family":"Kamto","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Faculty of Science, University of Yaounde I, Yaounde P.O. Box 812, Cameroon"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0222-7949","authenticated-orcid":false,"given":"Joseph Thierry","family":"Ndongo","sequence":"additional","affiliation":[{"name":"Department of Chemistry, Higher Teacher Training College, University of Yaounde 1, Yaounde P.O. Box 47, Cameroon"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8667-8351","authenticated-orcid":false,"given":"Xavier","family":"Siwe-Noundou","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Sciences, School of Pharmacy, Sefako Makgatho Health Sciences University, Pretoria 0204, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7289-3408","authenticated-orcid":false,"given":"Madan","family":"Poka","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Sciences, School of Pharmacy, Sefako Makgatho Health Sciences University, Pretoria 0204, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Patrick H.","family":"Demana","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Sciences, School of Pharmacy, Sefako Makgatho Health Sciences University, Pretoria 0204, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6788-6449","authenticated-orcid":false,"given":"Rui W. M.","family":"Krause","sequence":"additional","affiliation":[{"name":"Nanomaterials and Medicinal Organic Chemistry Laboratory, Department of Chemistry, Rhodes University, Grahamstown 6140, South Africa"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jos\u00e9phine","family":"Ngo Mbing","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Faculty of Science, University of Yaounde I, Yaounde P.O. Box 812, Cameroon"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Dieudonn\u00e9 Emmanuel","family":"Pegnyemb","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Faculty of Science, University of Yaounde I, Yaounde P.O. Box 812, Cameroon"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Christian G.","family":"Bochet","sequence":"additional","affiliation":[{"name":"Department of Chemistry, University of Fribourg, Chemin du Mus\u00e9e 9, CH-1700 Fribourg, Switzerland"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2022,8,15]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"9","DOI":"10.1086\/498577","article-title":"Effect of HIV-1 Infection on Antimalarial Treatment Outcomes in Uganda: A Population-Based Study","volume":"193","author":"Kamya","year":"2006","journal-title":"J. Infect Dis."},{"key":"ref_2","unstructured":"United States Agency for International Development (2021, June 27). U.S. President\u2019s Malaria Initiative, Available online: https:\/\/www.cdc.gov\/malaria\/malaria_worldwide\/cdc_activities\/pmi.html."},{"key":"ref_3","unstructured":"World Health Organization (2022, July 20). 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