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Planta Med 2004; 70(9): 797-802
DOI: 10.1055/s-2004-827225
Original Paper
Pharmacology
© Georg Thieme Verlag KG Stuttgart · New York

Structure-Activity Relationships of Saponins from Gleditsia sinensis in Cytotoxicity and Induction of Apoptosis

Lei Zhong1 , Ping Li1 , Jian Han1 , Guiqin Qu1 , Dean Guo1
  • 1The State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing, P. R. China
Further Information

Publication History

Received: February 20, 2004

Accepted: May 10, 2004

Publication Date:
23 September 2004 (online)

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Abstract

Thirteen compounds were isolated from the anomalous fruits of Gleditsia sinensis on the basis of bioassay-guided fractionation. These saponins together with six analogues or related compounds were tested for their cytotoxicities against six tumor cell lines by the MTT method. The induction of apoptosis in HL-60 cells by these compounds was determined through flow cytometric analysis. Some structure-activity relationships in cytotoxicity and induction of apoptosis were identified. The evaluation of the cytotoxicity and the ability to induce apoptosis revealed that some important structural features are required for activity. A valuable model which enables prediction of their activities was established and may be employed for the drug design of new Gleditsia saponin analogues.

Key words

Gleditsia sinensis - Leguminosae - saponin - cytotoxicity - apoptosis - structure-activity relationship

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Prof. Dr. Dean Guo

The State Key Laboratory of Natural and Biomimetic Drugs

School of Pharmaceutical Sciences

Peking University

Xueyuan Road 38#

Beijing 100083

P. R. China

Fax: +86-10-8280-2700

Phone: +86-10-8280-2700

Email: gda@bjmu.edu.cn