Anyam John V, Daikwo Priscilla E, Ungogo Marzuq A, Nweze Nwakaego E, Igoli Ngozichukwuka P, Gray Alexander I, De Koning Harry P, Igoli John O
Phytochemistry Research Group, Department of Chemistry, University of Agriculture, Makurdi, Nigeria.
Institute of Infection, Immunity and Inflammation, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, United Kingdom.
Front Chem. 2021 Apr 21;9:624741. doi: 10.3389/fchem.2021.624741. eCollection 2021.
The powdered roots of the medicinal plant were extracted with hexane and ethyl acetate, and the extracts were subjected to column chromatography for the isolation of potentially bioactive compounds and their screening against kinetoplastid pathogens. NMR and HREI mass spectrometric analyses identified two new diterpenes, characterized as 16, 19-dihydroxycassa-12-en-15-one (Sandynone, ) and (5S, 7R, 8R, 9R, 10S, 13Z, 17S)-7,8:7,17:16,17-triepoxy-7,8-seco-cassa-13-ene (niloticane B, ). The previously reported (5S,7R,8R,9R,10S) -(-)-7,8-seco-7, 8-oxacassa-13,15-diene-7,17-diol (), (5S,7R,8R,9R,10S) -(-)-7,8-seco-7, 8-oxacassa-13,15-dien-7-ol-17-al (), and (5S,7R,8R,9R,10S) -(-)-7,8-seco-7, 8-oxacassa-13,15-dien-7-ol () a, mixture of stigmasterol () and sitosterol (), and lupeol () were also isolated. Several column fractions displayed significant activity against a panel of and spp., and from the most active fraction, compound was isolated with high purity. The compound displayed high activity, particularly against , , and (0.88-11.7 µM) but only a modest effect against human embryonic kidney cells and no cross-resistance with the commonly used melaminophenyl arsenical and diamidine classes of trypanocides. The effect of compound against promastigotes was irreversible after a 5-h exposure, leading to the sterilization of the culture between 24 and 48 h.
用己烷和乙酸乙酯提取药用植物的根粉，提取物进行柱色谱分离以分离潜在的生物活性化合物，并对动质体病原体进行筛选。核磁共振（NMR）和高分辨电喷雾电离质谱（HREI）分析鉴定出两种新的二萜类化合物，分别为16,19 - 二羟基卡萨 - 12 - 烯 - 15 - 酮（Sandynone）和(5S, 7R, 8R, 9R, 10S, 13Z, 17S)-7,8:7,17:16,17 - 三环氧 - 7,8 - 裂环 - 卡萨 - 13 - 烯（尼罗烷B）。还分离出先前报道的(5S,7R,8R,9R,10S) - (-)-7,8 - 裂环 - 7,8 - 氧杂卡萨 - 13,15 - 二烯 - 7,17 - 二醇、(5S,7R,8R,9R,10S) - (-)-7,8 - 裂环 - 7,8 - 氧杂卡萨 - 13,15 - 二烯 - 7 - 醇 - 17 - 醛、(5S,7R,8R,9R,10S) - (-)-7,8 - 裂环 - 7,8 - 氧杂卡萨 - 13,15 - 二烯 - 7 - 醇，以及豆甾醇和谷甾醇的混合物和羽扇豆醇。几个柱层析级分对一组布氏锥虫和枯氏锥虫显示出显著活性，从活性最高的级分中以高纯度分离出化合物。该化合物显示出高活性，特别是对布氏锥虫、枯氏锥虫和罗得西亚锥虫（0.88 - 11.7 μM），但对人胚肾细胞只有适度影响，并且与常用的三聚氰胺苯基砷剂和双脒类锥虫杀灭剂无交叉耐药性。化合物对前鞭毛体的作用在暴露5小时后是不可逆的，导致培养物在24至48小时内被灭菌。
