Sołtys Agnieszka, Galanty Agnieszka, Grabowska Karolina, Paśko Paweł, Zagrodzki Paweł, Podolak Irma
Department of Pharmacognosy, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.
Department of Food Chemistry and Nutrition, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.
Pharmaceuticals (Basel). 2023 Jul 5;16(7):965. doi: 10.3390/ph16070965.
Benign prostatic hyperplasia (BPH) is a common urological disease affecting aging men. Its pathogenesis is regarded as complex and multifactorial, with sex hormones and inflammation as key contributory factors. In the current study, we investigated the anti-BPH potential of terpenoids present in the fruits of (EHRH.) PERS. Not only the effects on testosterone-stimulated normal prostate epithelial PNT2 cells, namely suppression of 5--reductase activity, PSA secretion, and cell proliferation, were determined but also the inhibitory activity on heat-induced protein denaturation, hyaluronidase, as well as IL-6, TNF-α, and NO release in LPS-treated macrophages. terpenoids significantly inhibited 5--reductase activity and reduced PSA secretion in PNT2 cells, reversing the stimulatory effect of testosterone. PNT2 cell proliferation was also found to be attenuated. Subsequently, all compounds reduced the release of pro-inflammatory mediators in RAW 264.7 cells. In addition, ursolic acid (UA) and its aldehyde (UAL) were the most potent hyaluronidase inhibitors of all compounds, with IC values of 225.75 µg/mL and 369.77 µg/mL, respectively. For better understanding and interpretation of the overall effect of terpenoids on different aspects of BPH pathogenesis and development, cluster analysis was applied.
良性前列腺增生（BPH）是一种影响老年男性的常见泌尿系统疾病。其发病机制被认为是复杂且多因素的，性激素和炎症是关键的促成因素。在本研究中，我们调查了（EHRH.）PERS.果实中存在的萜类化合物的抗BPH潜力。不仅测定了其对睾酮刺激的正常前列腺上皮PNT2细胞的影响，即对5-α还原酶活性、前列腺特异性抗原（PSA）分泌和细胞增殖的抑制作用，还测定了其对热诱导的蛋白质变性、透明质酸酶以及脂多糖（LPS）处理的巨噬细胞中白细胞介素-6（IL-6）、肿瘤坏死因子-α（TNF-α）和一氧化氮（NO）释放的抑制活性。萜类化合物显著抑制PNT2细胞中的5-α还原酶活性并减少PSA分泌，逆转了睾酮的刺激作用。还发现PNT2细胞增殖减弱。随后，所有化合物均减少了RAW 264.7细胞中促炎介质的释放。此外，熊果酸（UA）及其醛（UAL）是所有化合物中最有效的透明质酸酶抑制剂，IC值分别为225.75μg/mL和369.77μg/mL。为了更好地理解和解释萜类化合物对BPH发病机制和发展不同方面的总体影响，应用了聚类分析。
