Uromedic® Pumpkin Seed Derived Δ7-Sterols, Extract and Oil Inhibit 5α-Reductases and Bind to Androgen Receptor in Vitro

Stefan Heim, Stephanie Seibt, H. Stier, M. Moré
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引用次数: 12

Abstract

Dihydrotestosterone (DHT) is implicated in the development of benign prostate hyperplasia (BPH). We investigated if Uromedic? pumpkin (variety of Cucurbita pepo L. convar. citrullinina GREB. var. styriaca GREB) seed soft extract (active ingredients of GRANUFINK? Prosta forte 500 mg), seed oil and isolated Δ7-sterols could inhibit the conversion of [1,2,6,7-3H(N)]-testosterone to DHT by 5α-reductases. Also, we tested competition with [3H]-DHT for binding to the androgen receptor (AR). Pumpkin seed oil and pumpkin seed soft extract were identified as moderately active inhibitors of 5α-R1 and 5α-R2, with almost similar inhibitory capacities (IC50 < 5 mg/ml for 5α-R1 and about IC50 = 6 mg/ml for 5α-R2). The isolated Δ7-sterols were more active inhibitors (IC50 = 0.3 mg/ml for 5α-R1, IC50 = 1.0 mg/ml for 5α-R2). All three test compounds bound to the AR dose-dependently, with strong binding by Δ7-sterols (IC50 = 0.2 mg/ml) and weaker binding by pumpkin seed oil (IC50 = 0.4 mg/ml) and pumpkin seed soft extract (IC50 = 1.1 mg/ml). We propose that inhibition of 5α-reductases and competitive binding to the AR are mechanisms of action, by which the Uromedic? pumpkin seed derived test compounds, most specifically Δ7-sterols, counteract DHT and thereby exert clinically positive effects on the prostate, as well as bladder-strengthening effects.
Uromedic®南瓜籽衍生Δ7-Sterols,提取物和油在体外抑制5α-还原酶并结合雄激素受体
双氢睾酮(DHT)与良性前列腺增生(BPH)的发展有关。我们调查了Uromedic?南瓜(葫芦属南瓜的变种)citrullinina GREB。种. styriaca GREB种子软提取物(GRANUFINK有效成分?Prosta forte 500 mg)、种子油和分离的Δ7-sterols均能抑制5α-还原酶将[1,2,6,7- 3h (N)]-睾酮转化为DHT。此外,我们还测试了与[3H]-DHT结合雄激素受体(AR)的竞争。南瓜籽油和南瓜籽软提取物是5α- r1和5α- r2的中等活性抑制剂,其抑制能力几乎相同(5α- r1的IC50 < 5 mg/ml, 5α- r2的IC50约= 6 mg/ml)。分离得到的Δ7-sterols对5α-R1的IC50为0.3 mg/ml,对5α-R2的IC50为1.0 mg/ml。三种化合物均与AR呈剂量依赖性结合,Δ7-sterols的结合强度较强(IC50 = 0.2 mg/ml),南瓜籽油的结合强度较弱(IC50 = 0.4 mg/ml),南瓜籽软提取物的结合强度较小(IC50 = 1.1 mg/ml)。我们认为5α-还原酶的抑制和与AR的竞争性结合是其作用机制,通过这种机制,Uromedic?南瓜籽衍生的测试化合物,最具体的是Δ7-sterols,抵消DHT,从而在临床上对前列腺和膀胱增强作用发挥积极作用。
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