In vitro activities of crude extracts and triterpenoid constituents of Dichapetalum crassifolium Chodat against clinical isolates of Schistosoma haematobium

被引:6
|
作者
Chama, Mary Anti [1 ]
Onyame, Henry Akwaffo [1 ]
Fleischer, Claudine [1 ]
Osei-Safo, Dorcas [1 ]
Waibel, Reiner [2 ]
Otchere, Joseph [3 ]
Addae-Mensah, Ivan [1 ]
Wilson, Michael [3 ]
机构
[1] Univ Ghana, Sch Phys & Math Sci, Dept Chem, POB LG 56, Legon, Ghana
[2] Friedrich Alexander Univ Erlangen Nurnberg, Dept Chem & Pharm, Schuhstr 19, D-91052 Erlangen, Germany
[3] Univ Ghana, Noguchi Mem Inst Med Res, Coll Hlth Sci, Parasitol Dept, Legon, Ghana
关键词
Natural product chemistry; Organic chemistry; Pharmaceutical chemistry; Dichapetalum crassifolium; Schistosoma haematobiwn; Dichapetalin A; Dichapetalin M; Maslinic acid; Pomolic acid; TROPICAL MEDICINAL-PLANTS; CHEMICAL-CONSTITUENTS; ACID; DERIVATIVES;
D O I
10.1016/j.heliyon.2020.e04460
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
Dichapetalum crassifolium Chodat (Dichapetalaceae) is widely distributed in Africa, Tropical Asia and Latin America. As part of our quest for potential bioactive lead compounds for various neglected tropical diseases, were port the anti-schistosomal potential of the crude extracts and chemical constituents of the stems and roots of Dichapetalum crassifolium. Column chromatography of extracts of the stems and roots led to the isolation and identification of three oleanane-type triterpenoids, friedelan-3 beta-ol (1), friedelan-3-one (2), and maslinic acid (3);the ursane-type tritepenoid, pomolic acid (4) and the dammarane-type tetracyclic triterpenoids, dichapetalin A(5) and dichapetalin M (6). Dichapetalin A was isolated from only the roots. Isolated compounds were identified by comparison of their physico-chemical and spectral data with published data. The highest in vitro anti-schistosomalactivity (IC50) of the crude extracts against clinical isolates of Schistosoma haematobium (Bilharz 1852) was 248.6 mu g/ml for the ethyl acetate extract of the root while dichapetalin A gave the highest activity at 151.1 mu g/ml among the compounds compared with the 15.5 mu g/ml for the standard drug, praziquantel. The rest of the compounds showed activities in the order 177.9, 191.0, and 378.1 mu g/ml respectively for mixture of beta-sitosterol/stigmasterol, dichapetalin M and friedelan-3-one. The least active extract was the methanol extract of the stem (893.7 mu g/ml). The constituents of D. crassifolium showed activity against the S. haematobium that are below praziquantel. It is envisaged that the presence of multiple layers and the minute sizes of pores in the eggshells, may preclude penetration of eggs by the compounds.
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页数:10
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