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Anti-proliferative activities of terpenoids isolated from alisma orientalis and their structure-activity relationships
Xu W.1; Li T.2; Qiu J.-F.1; Wu S.-S.1; Huang M.-Q.1; Lin L.-G.2; Zhang Q.-W.2; Chen X.-P.2; Lu J.-J.2
2015
Source PublicationAnti-Cancer Agents in Medicinal Chemistry
ISSN18755992 18715206
Volume15Issue:2Pages:228-235
Abstract

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.

KeywordAlisma Orientalis Alisol b Anti-proliferative Protostane Structure-activity Relationships Triterpenoid
DOI10.2174/1871520614666140601213514
URLView the original
Indexed BySCI
Language英语
WOS Research AreaOncology ; Pharmacology & Pharmacy
WOS SubjectOncology ; Chemistry, Medicinal
WOS IDWOS:000351213600010
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Cited Times [WOS]:14   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorHuang M.-Q.; Lu J.-J.
Affiliation1.Fujian University of Traditional Chinese Medicine
2.Universidade de Macau
Recommended Citation
GB/T 7714
Xu W.,Li T.,Qiu J.-F.,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 W..,Li T..,Qiu J.-F..,Wu S.-S..,Huang M.-Q..,...&Lu J.-J..(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 W.,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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