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Int Immunopharmacol. 2011 Mar;11(3):377-83. doi: 10.1016/j.intimp.2011.01.012. Epub 2011 Jan 19.

Triptolide and its expanding multiple pharmacological functions.

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  • 1National Key Laboratory of Medical Immunology and Institute of Immunology, Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, China. lqy1969@yahoo.com.cn

Abstract

Triptolide, a diterpene triepoxide, is a major active component of extracts derived from the medicinal plant Tripterygium wilfordii Hook F (TWHF). Triptolide has multiple pharmacological activities including anti-inflammatory, immune modulation, antiproliferative and proapoptotic activity. So, triptolide has been widely used to treat inflammatory diseases, autoimmune diseases, organ transplantation and even tumors. Triptolide cannot only induce tumor cell apoptosis directly, but can also enhance apoptosis induced by cytotoxic agents such as TNF-α, TRAIL and chemotherapeutic agents regardless of p53 phenotype by inhibiting NFκB activation. Recently, the cellular targets of triptolide, such as MKP-1, HSP, 5-Lox, RNA polymerase and histone methyl-transferases had been demonstrated. However, the clinical use of triptolide is often limited by its severe toxicity and water-insolubility. New water-soluble triptolide derivatives have been designed and synthesized, such as PG490-88 or F60008, which have been shown to be safe and potent antitumor agent. Importantly, PG490-88 has been approved entry into Phase I clinical trial for treatment of prostate cancer in USA. This review will focus on these breakthrough findings of triptolide and its implications.

Copyright © 2011 Elsevier B.V. All rights reserved.

PMID:
21255694
[PubMed - indexed for MEDLINE]
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