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来自绢毛木兰的抗疟和抗利什曼原虫类黄酮。

Antiplasmodial and antileishmanial flavonoids from Mundulea sericea.

作者信息

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

机构信息

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.

出版信息

Fitoterapia. 2021 Mar;149:104796. doi: 10.1016/j.fitote.2020.104796. Epub 2020 Nov 30.

Abstract

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).

摘要

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)。

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