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一种来自续随子(大戟科续随子属)的新型P-糖蛋白抑制剂。

A new P-glycoprotein inhibitor from the caper spurge (Euphorbia lathyris).

作者信息

Appendino Giovanni, Della Porta Carla, Conseil Gwenaëlle, Sterner Olov, Mercalli Enrico, Dumontet Charles, Di Pietro Attilio

机构信息

Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche, Viale Ferrucci 33, 28100 Novara, Italy.

出版信息

J Nat Prod. 2003 Jan;66(1):140-2. doi: 10.1021/np0203537.

Abstract

The macrocyclic lathyrane polyester Euphorbia factor L10 (1a) has been obtained from the seeds of the caper spurge (E. lathyris). The interaction of L10 (1a) and its acetyl derivative (1b) with P-glycoprotein, a multidrug transporter overexpressed in cancer cells and responsible for resistance to chemotherapy, was investigated. The results established lathyrane diterpenoids as a novel chemotype for P-glycoprotein inhibitors.

摘要

大环千金二萜聚酯大戟因子L10(1a)已从续随子(E. lathyris)的种子中获得。研究了L10(1a)及其乙酰衍生物(1b)与P-糖蛋白的相互作用,P-糖蛋白是一种在癌细胞中过度表达并导致化疗耐药的多药转运蛋白。结果确定千金二萜类化合物是P-糖蛋白抑制剂的一种新型化学类型。

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