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Anti-proliferative activities of terpenoids isolated from alisma orientalis and their structure-activity relationships
Xu,Wen1; Li,Ting2; Qiu,Jian Fang1; Wu,Shui Sheng1; Huang,Ming Qing1; Lin,Li Gen2; Zhang,Qing Wen2; Chen,Xiu Ping2; Lu,Jin Jian2
2015
Source PublicationAnti-Cancer Agents in Medicinal Chemistry
ISSN1871-5206
Volume15Issue:2Pages:228-235
AbstractThis 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.
KeywordAlisma orientalis Alisol B Anti-proliferative Protostane Structure-activity relationships Triterpenoid
DOI10.2174/1871520614666140601213514
URLView the original
Language英语
Scopus ID2-s2.0-84926165984
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Cited Times [WOS]:18   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionUniversity of Macau
Affiliation1.College of Pharmacy,Fujian University of Traditional Chinese Medicine,Fuzhou,China
2.State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,University of Macau,Macao,Macao
Recommended Citation
GB/T 7714
Xu,Wen,Li,Ting,Qiu,Jian Fang,et al. Anti-proliferative activities of terpenoids isolated from alisma orientalis and their structure-activity relationships[J]. Anti-Cancer Agents in Medicinal Chemistry,2015,15(2):228-235.
APA Xu,Wen,Li,Ting,Qiu,Jian Fang,Wu,Shui Sheng,Huang,Ming Qing,Lin,Li Gen,Zhang,Qing Wen,Chen,Xiu Ping,&Lu,Jin Jian.(2015).Anti-proliferative activities of terpenoids isolated from alisma orientalis and their structure-activity relationships.Anti-Cancer Agents in Medicinal Chemistry,15(2),228-235.
MLA Xu,Wen,et al."Anti-proliferative activities of terpenoids isolated from alisma orientalis and their structure-activity relationships".Anti-Cancer Agents in Medicinal Chemistry 15.2(2015):228-235.
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