Department of Pharmaceutical Sciences, Ritsumeikan University, Kusatsu 525-8577, Japan.
Hayashikane Sangyo Co., Ltd., Yamaguchi 750-8608, Japan.
Int J Mol Sci. 2023 Jul 21;24(14):11765. doi: 10.3390/ijms241411765.
Roxb. pericarp extract (TBE) has a polyphenol-rich composition and exhibits potent antioxidant and anti-glycation activities in vitro. In the present study, we investigated the inhibitory effects of TBE on 5α-reductase in vitro using LNCaP cells and in vivo using a mouse model of castrated benign prostatic hyperplasia. TBE showed concentration-dependent inhibitory effects in the 5α-reductase (5αR) activity assay. In a reporter assay using AR-Luc/LNCaP cells, TBE inhibited the activity induced by testosterone, but not that induced by dihydrotestosterone. TBE also suppressed prostate cell proliferation, prostate-specific antigens, and transmembrane protease serine 2 expression in a castrated benign prostatic hyperplasia mouse model. In addition, ellagic acid, but not gallic acid, decreased 5αR and AR-Luc activities. Together, these results suggest a potential role for TBE in benign prostatic hyperplasia through inhibition of 5αR.
罗辛比果皮提取物（TBE）含有丰富的多酚类化合物，具有很强的抗氧化和抗糖化活性。在本研究中，我们使用 LNCaP 细胞在体外和去势良性前列腺增生小鼠模型中体内研究了 TBE 对 5α-还原酶的抑制作用。TBE 在 5α-还原酶（5αR）活性测定中表现出浓度依赖性抑制作用。在使用 AR-Luc/LNCaP 细胞的报告基因测定中，TBE 抑制了由睾丸酮诱导的活性，但不抑制由二氢睾丸酮诱导的活性。TBE 还抑制了去势良性前列腺增生小鼠模型中前列腺细胞增殖、前列腺特异性抗原和跨膜蛋白酶丝氨酸 2 的表达。此外，鞣花酸而非没食子酸降低了 5αR 和 AR-Luc 的活性。综上所述，这些结果表明 TBE 通过抑制 5αR 在良性前列腺增生中具有潜在作用。
