| Literature DB >> 30319238 |
Michael Afolayan1,2,3, Radhakrishnan Srivedavyasasri1, Olayinka T Asekun2, Oluwole B Familoni2, Abayomi Orishadipe3, Fazila Zulfiqar1, Mohamed A Ibrahim1,4, Samir A Ross1,5.
Abstract
Piliostigma thonningii (Schumach.) Milne-Redhead. (Leguminosae) is used for various medicinal purposes in African countries. Phytochemical investigation of P. thonningii yielded two compounds newly isolated from natural sources, 2β-methoxyclovan-9α-ol (1), and methyl-ent-3β-hydroxylabd-8(17)-en-15-oate (2), along with 14 known compounds (3-16). Compounds 1 and 4 (alepterolic acid) showed potential selectivity towards Trypanosoma brucei brucei with IC50 7.89 and 3.42 μM, respectively. Compound 2 showed activity towards T. brucei and Leishmania donovani Amastigote with IC50 3.84 and 7.82 μM, respectively. The structure activity relationship (SAR) of the isolated metabolites suggested that hydroxylation at C-2 enhances the antiprotozoal activity towards T. brucei in sesquiterpenes 1 and 3. Similarly hydroxylation at C-3 in labdane diterpenes elevates the antiprotozoal activity towards T. brucei.Entities:
Keywords: Leishmania donovani; Piliostigma thonningii; Sesquiterpene; Trypanosoma brucei; diterpene
Year: 2018 PMID： 30319238 PMCID： PMC6181138 DOI： 10.1007/s00044-018-2238-1
Source DB: PubMed Journal: Med Chem Res ISSN： 1054-2523 Impact factor: 1.965