沙茴香中伞形花内酯A对白血病细胞系的活性

Activity of elaeochytrin A from Ferula elaeochytris on leukemia cell lines.

作者信息

Alkhatib Racha, Hennebelle Thierry, Joha Sami, Idziorek Thierry, Preudhomme Claude, Quesnel Bruno, Sahpaz Sevser, Bailleul François

机构信息

Laboratoire de Pharmacognosie, E.A., Faculté des Sciences Pharmaceutiques et Biologiques, Université de Lille 2, Lille, France.

出版信息

Phytochemistry. 2008 Dec;69(17):2979-83. doi: 10.1016/j.phytochem.2008.09.019. Epub 2008 Nov 5.

DOI:10.1016/j.phytochem.2008.09.019

PMID:18992904

Abstract

Phytochemical investigation of the roots of Ferula elaeochytris made it possible to isolate two sesquiterpene esters, 6-anthraniloyljaeschkeanadiol (elaeochytrin A) and 4beta-hydroxy-6alpha-(p-hydroxybenzoyloxy)dauc-9-ene (elaeochytrin B), as well as eight known compounds: 6-angeloyljaeschkeanadiol, teferidin, ferutinin, 6-(p-hydroxybenzoyl)epoxyjaeschkeanadiol, 6-(p-hydroxybenzoyl)lancerotriol, 5-caffeoylquinic acid, 1,5-dicaffeoylquinic acid and sandrosaponin IX. The cytotoxic activities of all compounds were investigated on K562R (imatinib-resistant) human chronic myeloid leukaemia and DA1-3b/M2(BCR-ABL) (dasatinib-resistant) mouse leukemia cell line. Elaeochytrin A was the most active compound on both cell lines (IC(50)=12.4 and 7.8microM, respectively). It was also tested on non-resistant human promyelocytic leukemia cells (HL60, IC(50)=13.1microM) and was not toxic to normal peripheral blood mononuclear cells up to 100microM.

摘要

对油蒿根进行植物化学研究，得以分离出两种倍半萜酯，即6-邻氨基苯甲酰基雅氏二醇（油蒿素A）和4β-羟基-6α-（对羟基苯甲酰氧基）-9-烯胡萝卜素（油蒿素B），以及8种已知化合物：6-当归酰基雅氏二醇、铁费里定、费鲁亭、6-（对羟基苯甲酰基）环氧雅氏二醇、6-（对羟基苯甲酰基）兰氏三醇、5-咖啡酰奎宁酸、1,5-二咖啡酰奎宁酸和桑德罗皂苷IX。研究了所有化合物对K562R（伊马替尼耐药）人慢性髓性白血病细胞和DA1-3b/M2(BCR-ABL)（达沙替尼耐药）小鼠白血病细胞系的细胞毒性活性。油蒿素A是对这两种细胞系活性最高的化合物（IC(50)分别为12.4和7.8μM）。还对非耐药人早幼粒细胞白血病细胞（HL60，IC(50)=13.1μM）进行了测试，在浓度高达100μM时对正常外周血单个核细胞无毒。