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Constituents of West African medicinal plants. II. The isolation of alkaloids from selected Triclisia species.西非药用植物的成分。II. 从选定的三棱子属植物中分离生物碱。
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[Active antihelminitic alkaloids: active in vitro against Leishmanic Tropica the protozoa involved in leishmaniasis].[活性抗蠕虫生物碱：体外对参与利什曼病的热带利什曼原虫具有活性]
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Lack of mixed agonist-antagonist properties of [Gln8-Gly31]-beta h-EP-Gly-Gly-NH2 and [Arg9,19,24,28,29]-beta h-EP in the rat vas deferens neuroeffector junction: studies with naloxone, beta-funaltrexamine and ICI 174,864.[谷氨酰胺8-甘氨酸31]-β人促肾上腺皮质激素释放因子-甘氨酸-甘氨酸-氨基在大鼠输精管神经效应器连接处缺乏混合激动剂-拮抗剂特性以及[精氨酸9,19,24,28,29]-β人促肾上腺皮质激素释放因子：用纳洛酮、β-氟纳曲胺和ICI 174,864进行的研究
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一系列双苄基异喹啉生物碱的体外抗疟原虫、抗阿米巴和细胞毒性活性。

In vitro antiplasmodial, antiamoebic, and cytotoxic activities of a series of bisbenzylisoquinoline alkaloids.

作者信息

Marshall S J, Russell P F, Wright C W, Anderson M M, Phillipson J D, Kirby G C, Warhurst D C, Schiff P L

机构信息

Department of Pharmacy, University of Brighton, United Kingdom.

出版信息

Antimicrob Agents Chemother. 1994 Jan;38(1):96-103. doi: 10.1128/AAC.38.1.96.

DOI:10.1128/AAC.38.1.96
PMID:8141587
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC284403/
Abstract

Twenty-four bisbenzylisoquinoline alkaloids were screened for antiplasmoidal, antiamoebic, and cytotoxic activities by use of in vitro microtests. Eight of the alkaloids had antiplasmodial activity, with a 50% inhibitory concentration (IC50) of less than 1 microM against a multidrug-resistant strain of Plasmodium falciparum (chloroquine had an IC50 of 0.2 microM). The three alkaloids most active against Entamoeba histolytica, aromoline, isotrilobine, and insularine, had IC50s of 5 to 11.1 microM (metronidazole had an IC50 of 1.87 microM). None of the 24 bisbenzylisoquinoline alkaloids exhibited significant cytotoxicity against the KB cell line, the most toxic being berbamine, with an IC50 of 17.8 microM (the IC50 of podophyllotoxin was 0.008 microM). Bisbenzylisoquinoline alkaloids merit further investigation as potential novel antimalarial agents.

摘要

通过体外微量试验对24种双苄基异喹啉生物碱进行了抗疟原虫、抗阿米巴和细胞毒性活性筛选。其中8种生物碱具有抗疟原虫活性，对一株耐多药恶性疟原虫的半数抑制浓度（IC50）小于1微摩尔/升（氯喹的IC50为0.2微摩尔/升）。对溶组织内阿米巴最具活性的3种生物碱，即芳啉、异三叶豆碱和海岛藤碱，其IC50为5至11.1微摩尔/升（甲硝唑的IC50为1.87微摩尔/升）。24种双苄基异喹啉生物碱中无一对KB细胞系表现出显著的细胞毒性，毒性最大的是小檗胺，其IC50为17.8微摩尔/升（鬼臼毒素的IC50为0.008微摩尔/升）。双苄基异喹啉生物碱作为潜在的新型抗疟药物值得进一步研究。