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Title

Cytotoxic activity of Pulsatilla chinensis saponins and their structure–activity relationship.

Authors

Xu, Kun; Shu, Zhan; Xu, Qiong-Ming; Liu, Yan-Li; Li, Xiao-Ran; Wang, Yong-Lin; Yang, Shi-Lin

Abstract

The cytotoxic activity of 36 saponins isolated from roots ofPulsatilla chinensis(Bunge) Regel against the human cancer cell lines (A549, SGC-7901) and the human hepatic cell line (HL-7702) was tested by 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium bromide assay. Saponins1–14showed considerable cytotoxic activity, whereas saponins15–36showed no significant activity, which suggested that a free carboxylic group located at C-28 of aglycon is essential for their cytotoxic activity. Moreover, the analysis of structure–activity relationships also suggested that the oleanane-type saponins showed better cytotoxic activity than lupane-type saponins, and the length and linkage of glycolic chain attached to C-3 of aglycon displayed an important effect to the potent cytotoxicity. In conclusion, oleanolic acid 3-O-α-l-rhamnopyranosyl-(1 → 2)-[β-d-glucopyranosyl-(1 → 4)]-α-l-arabinopyranoside (5) exhibited the most significant cytotoxic activity.

Subjects

LIQUID chromatography; CELL lines; DRUG design; GLYCOSIDES; CHINESE medicine; MOLECULAR structure; RESEARCH funding; PLANT roots; DATA analysis software; CYTOTOXINS; DESCRIPTIVE statistics; IN vitro studies

Publication

Journal of Asian Natural Products Research, 2013, Vol 15, Issue 6, p680

ISSN

1028-6020

Publication type

Academic Journal

DOI

10.1080/10286020.2013.790901

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