Chepkirui Carolyne, Ochieng Purity J, Sarkar Biswajyoti, Hussain Aabid, Pal Chiranjib, Yang Li Jun, Coghi Paolo, Akala Hoseah M, Derese Solomon, Ndakala Albert, Heydenreich Matthias, Wong Vincent K W, Erdélyi Máté, Yenesew Abiy
Department of Chemistry, University of Nairobi, P.O. Box 30197-00100, Nairobi, Kenya.
Department of Zoology, West Bengal State University, Barasat, North 24 Parganas, West Bengal, India.
Fitoterapia. 2021 Mar;149:104796. doi: 10.1016/j.fitote.2020.104796. Epub 2020 Nov 30.
Five known compounds (1-5) were isolated from the extract of Mundulea sericea leaves. Similar investigation of the roots of this plant afforded an additional three known compounds (6-8). The structures were elucidated using NMR spectroscopic and mass spectrometric analyses. The absolute configuration of 1 was established using ECD spectroscopy. In an antiplasmodial activity assay, compound 1 showed good activity with an IC of 2.0 μM against chloroquine-resistant W2, and 6.6 μM against the chloroquine-sensitive 3D7 strains of Plasmodium falciparum. Some of the compounds were also tested for antileishmanial activity. Dehydrolupinifolinol (2) and sericetin (5) were active against drug-sensitive Leishmania donovani (MHOM/IN/83/AG83) with IC values of 9.0 and 5.0 μM, respectively. In a cytotoxicity assay, lupinifolin (3) showed significant activity on BEAS-2B (IC 4.9 μM) and HePG2 (IC 10.8 μM) human cell lines. All the other compounds showed low cytotoxicity (IC > 30 μM) against human lung adenocarcinoma cells (A549), human liver cancer cells (HepG2), lung/bronchus cells (epithelial virus transformed) (BEAS-2B) and immortal human hepatocytes (LO2).
从绢毛相思树叶提取物中分离出5种已知化合物（1 - 5）。对该植物根部进行类似研究又得到另外3种已知化合物（6 - 8）。通过核磁共振光谱分析和质谱分析阐明了这些化合物的结构。利用电子圆二色光谱确定了化合物1的绝对构型。在抗疟活性试验中，化合物1表现出良好的活性，对氯喹耐药的W2株的半数抑制浓度（IC）为2.0 μM，对氯喹敏感的恶性疟原虫3D7株的IC为6.6 μM。还对其中一些化合物进行了抗利什曼原虫活性测试。脱氢羽扇豆醇（2）和绢毛相思黄酮（5）对药物敏感的杜氏利什曼原虫（MHOM/IN/83/AG83）有活性，IC值分别为9.0和5.0 μM。在细胞毒性试验中，羽扇豆醇（3）对BEAS - 2B（IC 4.9 μM）和HePG2（IC 10.8 μM）人细胞系表现出显著活性。所有其他化合物对人肺腺癌细胞（A549）、人肝癌细胞（HepG2）、肺/支气管细胞（上皮病毒转化）（BEAS - 2B）和永生化人肝细胞（LO2）显示出低细胞毒性（IC > 30 μM）。
