大戟属植物中重排麻风树型二萜。其对多药耐药逆转作用的评估。

Rearranged jatrophane-type diterpenes from euphorbia species. Evaluation of their effects on the reversal of multidrug resistance.

作者信息

Madureira Ana M, Ferreira Maria-José U, Gyémánt Nora, Ugocsai Katalin, Ascenso José R, Abreu Pedro M, Hohmann Judit, Molnár Joseph

机构信息

Centro de Estudos de Ciências Farmacêuticas, Faculdade de Farmácia da Universidade de Lisboa, Lisboa, Portugal.

出版信息

Planta Med. 2004 Jan;70(1):45-9. doi: 10.1055/s-2004-815454.

DOI:10.1055/s-2004-815454

PMID:14765292

Abstract

The rearranged jatrophane-type diterpenes ( 1 - 3), isolated from the Me (2)CO extracts of Euphorbia portlandica and Euphorbia segetalis, were examined for their effects on multidrug resistance (MDR) in mouse lymphoma cells. Compounds 2 and 3 revealed to be active with the latter being more active than the positive control verapamil, a known resistance modifier. The new compound 1, named portlandicine, was isolated from Euphorbia portlandica and its structure characterised by high-field NMR spectroscopic methods including 2D NMR techniques: COSY, HMQC, HMBC and NOESY. The known diterpene 2, together with aleuritolic acid ( 4), oleanolic acid ( 5), and betulin diacetate ( 6), were also isolated from the same species.

摘要

从大戟属植物波特兰大戟（Euphorbia portlandica）和麦田大戟（Euphorbia segetalis）的甲醇（2）提取物中分离得到的重排麻风树型二萜（1 - 3），对其在小鼠淋巴瘤细胞中的多药耐药性（MDR）作用进行了研究。化合物2和3显示具有活性，后者比已知的耐药性调节剂阳性对照维拉帕米更具活性。新化合物1，命名为波特兰大戟素，从波特兰大戟中分离得到，其结构通过包括二维核磁共振技术（COSY、HMQC、HMBC和NOESY）在内的高场核磁共振光谱方法进行了表征。已知的二萜2，连同桐酸（4）、齐墩果酸（5）和桦木二乙酸酯（6），也从同一物种中分离得到。