| 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 Publication | Anti-Cancer Agents in Medicinal Chemistry
 |
| ISSN | 1871-5206 |
| Volume | 15Issue: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. |
| Keyword | Alisma orientalis Alisol B Anti-proliferative Protostane Structure-activity relationships Triterpenoid |
| DOI | 10.2174/1871520614666140601213514 |
| URL | View the original |
| Language | 英语 |
| Fulltext Access | |
| Citation statistics | |
| Document Type | Journal article |
| Collection | University of Macau |
| Affiliation | 1.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.,...&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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