良性前列腺增生(benign prostatic hyperplasia，BPH)在中老年男性中高发，5α-还原酶对其形成起重要作用。为考察油茶蒲提取物中5α-还原酶抑制活性组分对BPH的作用，本研究采用MTT法测定细胞增殖、Annexin V/PI双染色法检测细胞凋亡，通过给予不同的给药浓度和作用时间，比较各活性组分对人前列腺增生BPH-1细胞的作用。试验结果表明，100 μg/mL浓度下阳性对照非那雄胺、组分Fr5及Fr6的细胞增殖抑制率分别为47.20%±1.02%、48.60%±1.56%、55.23%±0.58%；组分Fr6在各作用浓度下抑制率均显著高于非那雄胺，Fr5与非那雄胺活性相当。活性组分对BPH-1细胞增殖的抑制率与对5α-还原酶的抑制率测定结果趋势相近，两种方法相互印证。时效性试验表明活性组分Fr6药效较非那雄胺持久，细胞凋亡试验表明Fr6在低剂量（25 μg/mL) 时诱导细胞凋亡率即可达12.40%±3.78%，与非那雄胺相近(13.68%±1.02%)，极具开发潜力。

Benign prostatic hyperplasia (BPH) is associated with high morbidity in older men and 5α-reductase plays an important role in BPH pathogenesis. To confirm the effect of 5α-reductase inhibitors (Fr5 and Fr6) purified from oil tea Camellia extract (OCE) on BPH (with finasteride as positive control), cell proliferation was measured by the thiazolyl blue tetrazolium blue (MTT) assay and apoptosis was detected by the Annexin V/PI double-staining method using the benign prostate hyperplastic epithelial cell line (BPH-1). The effects of different drug concentrations and action times on BPH-1 cells were compared. Our results showed that at 100 μg/mL, the positive control as well as active components, Fr5 and Fr6 showed cell proliferation inhibition rates of 47.20% ± 1.02%, 48.60% ± 1.56%, and 55.23% ± 0.58%, respectively. Fr6 showed stronger inhibition than the positive control at all the concentrations tested, while Fr5 showed effects similar to those of the control. The rate of cell proliferation inhibition for OCE was similar to that for 5α-reductase; thus, both methods were mutually confirming. The effect shown by the active component Fr6 also lasted longer than that by positive control. Additionally, the apoptosis rate for low-dose Fr6 (25 μg/mL) was 12.40% ± 3.78%, which was close to that for finasteride at 13.68% ± 1.02%. These results indicate a potential for OCE active components to inhibit BPH, especially Fr6, which warrants further study.

国家自然科学基金资助项目（31270722）