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3,3＇-Diindolylmethane

CAS No. : 1968-05-4

MCE 站：3,3＇-Diindolylmethane

产品活性：3，3＇-Diindolylmethane 是一种有效的雄激素受体 (AR) 拮抗剂。

研究领域：Others  |  Autophagy

作用靶点：Androgen Receptor  |  Autophagy

In Vitro: 3,3＇-Diindolylmethane (DIM) is a strong antagonist of androgen receptor (AR) function but exhibits less than obvious structural similarity to the endogenous AR ligand, dihydrotestosterone (DHT). 3,3＇-Diindolylmethane is a major digestive product of indole-3-carbinol, a potential anticancer component of cruciferous vegetables. 3,3＇-Diindolylmethane exhibits potent antiproliferative ａnd antiandrogenic properties in androgen-dependent human prostate cancer cells. 3,3＇-Diindolylmethane suppresses cell proliferation of LNCaP cells ａnd inhibits DHT stimulation of DNA synthesis. Moreover, 3,3＇-Diindolylmethane inhibits endogenous PSA transcription ａnd reduced intracellular ａnd secreted PSA protein levels induced by DHT in LNCaP cells. Also, 3,3＇-Diindolylmethane inhibits, in a concentration-dependent manner, the DHT-induced expression of a prostate-specific antigen promoter-regulated reporter gene construct in transiently transfected LNCaP cells. Co-treatment with 50 μM 3,3＇-Diindolylmethane partially inhibits the translocation of AR induced by DHT treatment ａnd showed distribution of the AR to be both cytoplasmic ａnd nuclear. Furthermore, 3,3＇-Diindolylmethane treatment prevents the formation of AR foci in the nucleus. 3,3＇-Diindolylmethane alone produces a predominantly cytoplasmic distribution of fluorescence.

In Vivo: Mice are randomized into two groups ａnd are treated daily s.c. with either vehicle or 3,3＇-Diindolylmethane (10 mg/kg) for 30 days. Tumor volume ａnd the weight of mice are recorded once every 3 days using calipers. 3,3＇-Diindolylmethane (DIM) treatment resulted in a marked inhibition of SNU-484 xenograft tumor growth. Notably, the body weight of mice from both groups did not significantly differ from the vehicle control following 30 days of drug exposure, suggesting that 3,3＇-Diindolylmethane has no severe toxicity to the mice. Taken together, these findings demonstrate that 3,3＇-Diindolylmethane administration significantly inhibited SNU-484 xenograft growthin vivo mediated by the inactivation of YAP.

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