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Cryptotanshinone(35825-57-1)

Overview: Cryptotanshinone (CTS) is the main fat-soluble extract of Salvia miltiorrhiza, which is orange acicular crystal. It belongs to diterpenoid quinone compounds. Most of these components have ternary or quaternary ring o-quinone or p-quinone structure on the skeleton, making most of them have anti-tumor, antioxidant, anti-inflammatory, antibacterial and other activities. In recent years, great progress has been made in the study of the pharmacological mechanism of this compound.

Role: 1) The therapeutic effect of cryptotanshinone on hepatobiliary carcinoma is predicted by screening technology based on reverse drug effect. The results showed that cryptotanshinone could inhibit the proliferation of human hepatoma SMMC-7721 cells in cell experiments, which might be closely related to its reduction of MAP2K1 protein mRNA expression. In the experiment of human hepatoma HepG-2 cells, Xie Fei found that cryptotanshinone can induce HepG-2 apoptosis by inhibiting the expression of Bcl-2, promoting the expression of Bax, regulating the ratio of Bel-2/Bax, and finally activating the downstream effector easpase-3. 2) Treatment of prostate cancer Prostate cancer (PCa) is a common clinical cancer, and androgen receptor (AR) is the main target of treatment of PCa. Reducing androgen substances or preventing AR production is widely used to inhibit the growth of PCa cells mediated by AR. In vivo and in vitro experiments in mice, tanshinone (including cryptotanshinone, tanshinone I, tanshinone IIA) can inhibit the growth of 130PCa cells. The mechanism may be by blocking cell cycle and inducing cell apoptosis. In addition, cryptotanshinone can inhibit PCa by inhibiting lysine-specific demethylase 1 (LSD1), regulating the demethylation function of histone H3 lysine 9 (H3K9), down-regulating AR signal and inhibiting its transcription activity. It not only affects AR function, but also significantly inhibits AR transcriptional activity and AR target gene expression at mRNA and protein levels. It also blocks the interaction between AR and lysine - specific demethylase - 1LSD1), inhibits the promoter of AR target gene, and increases the monomethylation and dimethylation of histone H3 lysine 9 (H3K9).


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