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抗癌西波烷型三萜类化合物的生物催化作用。

Biocatalysis of the anticancer sipholane triterpenoids.

作者信息

Jain Sandeep, Shirode Amit, Yacoub Shenouda, Barbo Ashley, Sylvester Paul W, Huntimer Eric, Halaweish Fathi, El Sayed Khalid A

机构信息

College of Pharmacy, University of Louisiana at Monroe, Monroe, Louisiana, USA.

出版信息

Planta Med. 2007 Jun;73(6):591-6. doi: 10.1055/s-2007-967188. Epub 2007 May 7.

DOI:10.1055/s-2007-967188
PMID:17486535
Abstract

The Red Sea sponge Callyspongia (= Siphonochalina) siphonella is a rich source of sipholane triterpenoids. Biocatalysis of the major sipholanes, sipholenol A (1) and sipholenone A (2), respectively, by Mucor ramannianus ATCC 9628 and Cunninghamella elegans ATCC 7929 afforded four new metabolites 3 - 6 along with sipholenol G and 28-hydroxysipholenol A. Major sipholanes along with their biocatalytic products were investigated for their antiproliferative activity against the highly malignant +SA mouse mammary epithelial cell line. Sipholenone A (2) was the most active sipholane inhibiting +SA cell proliferation with an IC(50) value of 20 - 30 microM. Sipholenone A, also, showed cytotoxicity against MCF-7 at a dose of 0.9 microM and antiangiogenic activity in the CAM (chorio-allantoic membrane) assay. This is the first report on anticancer activity of these triterpenoids.

摘要

红海海绵Callyspongia(= Siphonochalina)siphonella是西波烷三萜类化合物的丰富来源。分别用拉曼毛霉ATCC 9628和雅致小克银汉霉ATCC 7929对主要的西波烷类化合物西波醇A(1)和西波烯酮A(2)进行生物催化,得到了四种新的代谢产物3 - 6以及西波醇G和28 - 羟基西波醇A。研究了主要的西波烷类化合物及其生物催化产物对高度恶性的+SA小鼠乳腺上皮细胞系的抗增殖活性。西波烯酮A(2)是最具活性的西波烷类化合物,抑制+SA细胞增殖的IC(50)值为20 - 30 microM。西波烯酮A在剂量为0.9 microM时对MCF - 7也表现出细胞毒性,并在鸡胚绒毛尿囊膜(CAM)试验中具有抗血管生成活性。这是关于这些三萜类化合物抗癌活性的首次报道。

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