Abstract
Strategy, Management and Health Policy Enabling Technology, Genomics, Proteomics Preclinical Research Preclinical Development Toxicology, Formulation Drug Delivery, Pharmacokinetics Clinical Development Phases I-III Regulatory, Quality, Manufacturing Postmarketing Phase IV Triptolide is the principal active ingredient in extracts from the Chinese herb, Tripterygium wilfordii Hook.F (TwHF) and has various biological functions including immunosuppression, anti-inflammatory, antiviral, and antitumor properties. Triptolide has antitumor activity in a variety of tumors, and numerous studies have attempted to elucidate the potential antitumor mechanism. Triptolide can modulate histone methylation, suggesting that epigenetic mechanisms may play an important role in its antitumor activity. The present study assessed the association between the antitumor effects of triptolide in androgen-independent prostatic cancer and the regulation of histone methylation. Triptolide inhibited the proliferation of the androgen-independent prostatic cancer cell line, Du145 and induced apoptosis in a time- and dose-dependent manner. Triptolide decreased histone H3K27me3 methylation via downregulation of histone methyltransferase enhancer of zeste 2, which may represent the antitumor mechanism of triptolide.
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