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Phytochemical study of Piliostigma thonningii, a medicinal plant grown in Nigeria.
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2018-08-25 , DOI: 10.1007/s00044-018-2238-1
Michael Afolayan 1, 2, 3 , Radhakrishnan Srivedavyasasri 1 , Olayinka T Asekun 2 , Oluwole B Familoni 2 , Abayomi Orishadipe 3 , Fazila Zulfiqar 1 , Mohamed A Ibrahim 1, 4 , Samir A Ross 1, 5
Affiliation  

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 (316). 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.

中文翻译:

尼日利亚药用植物 Piliostigma thonningii 的植物化学研究。

Piliostigma thonningii (Schumach.) Milne-Redhead。(豆科)在非洲国家用于各种药用目的。对P. thonningii的植物化学研究产生了两种新从天然来源中分离出来的化合物,2 β -methoxyclovan-9 α -ol ( 1 ) 和methylent -3 β -Hydroxylabd -8(17)-en-15-oate ( 2),以及 14 种已知化合物 ( 316 )。化合物14 (阿普特罗酸)对布氏锥虫具有潜在选择性, IC 50分别为 7.89 和 3.42 μM。化合物2对布氏锥虫杜氏利什曼原虫无鞭毛体具有活性, IC 50分别为 3.84 和 7.82 μM。分离代谢物的结构活性关系(SAR)表明,C-2 处的羟基化增强了倍半萜13中对布氏锥虫的抗原虫活性。类似地,拉丹烷二萜中 C-3 的羟基化提高了对布氏锥虫的抗原虫活性。
更新日期:2018-08-25
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