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Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice
文献类型：期刊论文
| 作者 | Yang, HJ; Chen, D; Cui, QZC; Yuan, X; Dou, QP |
| 刊名 | CANCER RESEARCH
 |
| 出版日期 | 2006-05-01 |
| 卷号 | 66期号:9页码:4758-4765 |
| ISSN号 | 0008-5472 |
| DOI | 10.1158/0008-5472.CAN-05-4529 |
| 英文摘要 | Interest in the use of traditional medicines for cancer prevention and treatment is increasing. In vitro, in vivo, and clinical studies suggest the potential use of proteasome inhibitors as novel anticancer drugs. Celastrol, an active compound extracted from the root bark of the Chinese medicine "Thunder of God Vine" (Tripterygium wilfordii Hook F.), was used for years as a natural remedy for inflammatory conditions. Although Celastrol has been shown to induce leukemia cell apoptosis, the molecular target involved has not been identified. Furthermore, whether Celastrol has antitumor activity in vivo has never been conclusively shown. Here, we report, for the first time, that Celastrol potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome (IC50 = 2.5 mu mol/L) and human Prostate cancer cellular 26S proteasome (at 1-5 mu mol/L). Inhibition of the proteasome activity by Celastrol in PC-3 (androgen receptor- or AR-negative) or LNCaP (AR-positive) cells results in the accumulation of ubiquitinated proteins and three natural proteasome substrates (I kappa B-alpha, Bax, and p27), accompanied by suppression of AR protein expression (in LNCaP cells) and induction of apoptosis. Treatment of PC-3 tumor-bearing nude mice with Celastrol (1-3 mg/kg/d, i.p., 1-31 days) resulted in significant inhibition (65-93%) of the tumor growth. Multiple assays using the animal tumor tissue samples from both early and end time points showed in vivo inhibition of the proteasomal activity and induction of apoptosis after Celastrol treatment. Our results show that Celastrol is a natural proteasome inhibitor that has a great potential for cancer prevention and treatment. |
| WOS研究方向 | Oncology |
| 语种 | 英语 |
| WOS记录号 | WOS:000237496900028 |
| 出版者 | AMER ASSOC CANCER RESEARCH |
| 源URL | [http://202.127.146.157/handle/2RYDP1HH/1177]  |
| 专题 | 中国科学院武汉植物园 |
| 通讯作者 | Dou, QP |
| 作者单位 | 1.Wayne State Univ, Sch Med, Barbara Ann Karmanos Canc Inst, Prevent Program, Detroit, MI 48201 USA 2.Wayne State Univ, Sch Med, Dept Pathol, Detroit, MI 48201 USA 3.Chinese Acad Sci, Wuhan Bot Garden, Wuhan, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, HJ,Chen, D,Cui, QZC,et al. Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice[J]. CANCER RESEARCH,2006,66(9):4758-4765. |
| APA | Yang, HJ,Chen, D,Cui, QZC,Yuan, X,&Dou, QP.(2006).Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice.CANCER RESEARCH,66(9),4758-4765. |
| MLA | Yang, HJ,et al."Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice".CANCER RESEARCH 66.9(2006):4758-4765. |
入库方式： OAI收割
来源：武汉植物园
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