17β hydroxysteroid dehydrogenase type 3 (17β-HSD3) is the key enzyme in the biosynthesis of testosterone, which is an attractive therapeutic target for Prostate cancer (PCa). H10, a novel curcumin analogue, was identified as a potential 17β-HSD3 inhibitor. The pharmacokinetic study of H10 in rats were performed by intraperitoneal (i.p.), intravenous (i.v.) and oral (p.o.) administration. In addition, the inhibitory effects of H10 against liver CYP3A4 were investigated in vitro using human liver microsomes (HLMs). The acute and chronic toxicological characteristics were characterized using single-dose and 30 days administration. All the mice were alive after i.p. H10 with dose of no more than 100 mg/kg which are nearly the maximum solubility in acute toxicity test. The pharmacokinetic characteristics of H10 fitted with linear dynamics model after single dose. Furthermore, H10 could bioaccumulate in testis, which was the target organ of 17β-HSD3 inhibitor. H10 distributed highest in spleen, and then in liver both after single and multiple i.p. administration. Moreover, H10 showed weak inhibition towards liver CYP3A4, and did not cause significant changes in AST and ALT levels after treated with H10 for continuously 30 days. Taken together, these preclinical characteristics laid the foundation for further clinical studies of H10.

17β羟类固醇脱氢酶3型（17β-HSD3）是睾丸激素生物合成中的关键酶，它是前列腺癌（PCa）的有吸引力的治疗靶标。新型姜黄素类似物H10被鉴定为潜在的17β-HSD3抑制剂。H10在大鼠中的药代动力学研究是通过腹膜内（ip），静脉内（iv）和口服（po）进行的。此外，在体外研究了H10对肝脏CYP3A4的抑制作用使用人肝微粒体（HLM）。使用单剂量和30天给药来表征急性和慢性毒理学特征。ip H10后所有小鼠均存活，剂量不超过100 mg / kg，几乎是急性毒性试验中的最大溶解度。H10的药代动力学特征与单次剂量后的线性动力学模型拟合。此外，H10可能在睾丸中生物积累，而睾丸是17β-HSD3抑制剂的靶器官。单次和多次腹膜内给药后，H10在脾脏中分布最高，然后在肝脏中分布。此外，H10对肝脏CYP3A4的抑制作用较弱，并且在连续治疗30天后未引起AST和ALT水平的显着变化。在一起