Anti-Proliferative Activities of Terpenoids Isolated from Alisma orientalis and their Structure-Activity Relationships

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 16, 12 Issues, 2016

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex

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Anti-Proliferative Activities of Terpenoids Isolated from Alisma orientalis and their Structure-Activity Relationships

Anti-Cancer Agents in Medicinal Chemistry, 15(2): 228-235.

Author(s): Wen Xu, Ting Li, Jian-Fang Qiu, Shui-Sheng Wu, Ming-Qing Huang, Li-Gen Lin, Qing-Wen Zhang, Xiu-Ping Chen and Jin-Jian Lu.

Affiliation: College of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, China.


This study aimed to isolate terpenoids from Alisma orientalis (Sam.) Juzep. and elucidate their antiproliferative activities, as well as structure-activity relationships. Fourteen protostane-type triterpenoids were isolated from the rhizome of A. orientalis. Among these triterpenoids, alisol A (1), alisol A 24-acetate (2), alisol B (3), alisol B 23-acetate (4), and alisol G (8) presented inhibitory effects on cancer cell lines tested. Compounds 3 and 4 showed the highest potential; IC50 values for HepG2, MDA-MB-231, and MCF-7 cells were 16.28, 14.47, and 6.66 μM for 3 and 18.01, 15.97, and 13.56 μM for 4, respectively. Based on these results, we concluded that the degree of C-16 oxidation and the double bond between C-13 and C-17 may be significant in anti-proliferative activities. Further study showed that 3 and 4 effectively induced apoptosis, as confirmed by flow cytometry. Increased intracellular calcium concentration and endoplasmic reticulum stress were detected after treatment with 4 in HepG2 cells. Although compounds 1 and 2 induced minimal apoptosis, they evidently delayed the G2/M phase in HepG2 cells. Further study showed that 1–4 also enhanced LC3II expression, indicating autophagy is occured.


Alisma orientalis, alisol B, anti-proliferative, protostane, structure-activity relationships, triterpenoid.

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Article Details

Volume: 15
Issue Number: 2
First Page: 228
Last Page: 235
Page Count: 8
DOI: 10.2174/1871520614666140601213514
Price: $58

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