| Diterpenoids from Euphorbia royleana reverse P-glycoprotein-mediated multidrug resistance in cancer cells | |
Shaker, Sharpkate; Sang, Jun; Yan, Xue-Long; Fan, Run-Zhu; Tang, Gui-Hua; Xu, You-Kai ; Yin, Sheng5
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| 2020 | |
| Source Publication | PHYTOCHEMISTRY
 |
| ISSN | 0031-9422 |
| Volume | 176Pages:- |
| Abstract | Eight previously undescribed diterpenoids, euphoroyleans A - H, including two cembranes, three ingenanes, two ent-atisanes, and one ent-kaurane, along with 22 known analogues were isolated from the whole plants of Euphorbia royleana. The structures of euphoroyleans A - H, including the absolute configurations, were elucidated by extensive spectroscopic analyses, chemical transformation, and single crystal X-ray diffractions. All the isolates were screened for their chemoreversal abilities on P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) cancer cell line HepG2/DOX, and eight compounds exhibited significant activities. Among them, ingol-3,7,12-triacetate-8-benzoate, the most active MDR modulator with no obvious cytotoxicity, could enhance the efficacy of anticancer drug DOX to ca. 105 folds at 10 mu M, being stronger than the positive drug verapamil. Mechanistic study revealed that ingol-3,7,12-triacetate-8-benzoate could inhibit the transport activity of P-gp rather than its expression, and the possible recognition mechanism between compounds and P-gp was predicted by molecular docking. |
| Keyword | INGOL LATEX ESTERS PLANTS |
| Subject Area | Biochemistry & Molecular Biology ; Plant Sciences |
| DOI | 10.1016/j.phytochem.2020.112395 |
| Indexed By | SCI |
| Language | 英语 |
| WOS ID | WOS:000542646300017 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | https://ir.xtbg.ac.cn/handle/353005/11751 |
| Collection | 2012年后新成立研究组 |
| Affiliation | 1.[Shaker, Sharpkate 2.Sang, Jun 3.Yan, Xue-Long 4.Fan, Run-Zhu 5.Tang, Gui-Hua 6.Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China 7.Chinese Acad Sci, Key Lab Trop Plant Resources & Sustainable Use, Xishuangbanna Trop Bot Garden, Menglun 666303, Yunnan, Peoples R China |
| Recommended Citation GB/T 7714 | Shaker, Sharpkate,Sang, Jun,Yan, Xue-Long,et al. Diterpenoids from Euphorbia royleana reverse P-glycoprotein-mediated multidrug resistance in cancer cells[J]. PHYTOCHEMISTRY,2020,176:-. |
| APA | Shaker, Sharpkate.,Sang, Jun.,Yan, Xue-Long.,Fan, Run-Zhu.,Tang, Gui-Hua.,...&Yin, Sheng.(2020).Diterpenoids from Euphorbia royleana reverse P-glycoprotein-mediated multidrug resistance in cancer cells.PHYTOCHEMISTRY,176,-. |
| MLA | Shaker, Sharpkate,et al."Diterpenoids from Euphorbia royleana reverse P-glycoprotein-mediated multidrug resistance in cancer cells".PHYTOCHEMISTRY 176(2020):-. |
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| Diterpenoids from Eu（2334KB） | 期刊论文 | 出版稿 | 开放获取 | CC BY-NC-SA | View Download | |
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