当前位置: X-MOL 学术J. Nat. Med. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Phenylpropanoid conjugated iridoids with anti-malarial activity from the leaves of Morinda morindoides
Journal of Natural Medicines ( IF 3.3 ) Pub Date : 2021-06-29 , DOI: 10.1007/s11418-021-01541-x
Yasinjan Hashim 1 , Kazufumi Toume 1 , Shusaku Mizukami 2, 3, 4 , Yue-Wei Ge 1 , Mayumi Taniguchi 2, 4 , Awet Alem Teklemichael 2, 5 , Nguyen Tien Huy 2, 3, 6 , Joseph M Bodi 7 , Kenji Hirayama 2, 5, 6 , Katsuko Komatsu 1
Affiliation  

Two phenylpropanoid-conjugated iridoids, deglucosyl gaertneroside (1) and morindoidin (2), were isolated from the leaves of Morinda morindoides (Rubiaceae) by activity-guided fractionation using an anti-malarial activity assay. The known related iridoids molucidin (3) and prismatomerin (4), two lignans, abscisic acid, two megastigmanes, and two flavonol glycosides were also identified. The structures of isolated compounds were elucidated using spectroscopic analysis. The isolated compounds were evaluated for anti-malarial activity against the chloroquine/mefloquine-sensitive strains of Plasmodium falciparum together with cytotoxicity against adult mouse brain cells. Potent anti-malarial activity of 3 and 4 (IC50 of 0.96 and 0.80 μM, CC50 of 1.02 and 0.88 μM, and SI of 1.06 and 1.10, respectively) was shown, while new iridoids 1 and 2 and pinoresinol (5) displayed moderate activity (IC50 of 40.9, 20.6, and 24.2 μM) without cytotoxicity (CC50 > 50 μM). These results indicate that 15 may be promising lead compounds for anti-malarial drugs. In addition, our results imply the necessity of the quality control of the extract of M. morindoides leaves based on the contents of 15 in terms of the safety and efficacy.



中文翻译:

巴戟天叶子中苯丙烷共轭环烯醚萜类化合物具有抗疟活性

使用抗疟活性测定,通过活性引导分级从巴戟天(茜草科)的叶子中分离出两种与苯丙烷结合的环烯醚萜苷(deglucosyl gaertneroside ( 1 ) 和morindoidin ( 2 ))。还鉴定了已知的相关环烯醚萜烯苷 ( 3 ) 和棱柱形体 ( 4 )、两种木脂素、脱落酸、两种 megastigmanes 和两种黄酮醇苷。使用光谱分析阐明了分离化合物的结构。评估了分离的化合物对恶性疟原虫的氯喹/甲氟喹敏感菌株的抗疟疾活性以及对成年小鼠脑细胞的细胞毒性。显示了34 的强效抗疟疾活性(IC 50为 0.96 和 0.80 μM,CC 50 分别为 1.02 和 0.88 μM,SI 分别为 1.06 和 1.10),同时显示了新的环烯醚萜类化合物12以及松脂醇 ( 5 )中等活性(IC 50为 40.9、20.6 和 24.2 μM),无细胞毒性(CC 50  > 50 μM)。这些结果表明,1 - 5可能是有前途的先导化合物的抗疟疾药物。此外,我们的结果暗示了对M. morindoides提取物进行质量控制的必要性基于内容的叶子1 - 5中的安全性和有效性的条款。

更新日期:2021-06-30
down
wechat
bug