Formulated Phytosterols - A New Treatment For Benign Prostatic Hyperplasia

配方植物甾醇——良性前列腺增生的新疗法

• 批准号: 7109864
• 负责人: Curtis A Spilburg
• 金额: $ 12.87万
• 依托单位: LIFELINE TECHNOLOGIES, INC.
• 依托单位国家: 美国
• 财政年份: 2006
• 资助国家: 美国
• 起止时间: 2006-09-15 至 2008-02-29
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7109864
• 关键词: benign prostate hyperplasia; clinical research; clinical trials; dihydrotestosterone; drug design /synthesis /production; drug screening /evaluation; human subject; intermolecular interaction; male; oxidoreductase inhibitor; patient oriented research; pharmacokinetics; phosphatidylcholines; plant extracts; reproductive system disorder chemotherapy; sitosterols; steroid hormone metabolism; testosterone 5 alpha reductase

DESCRIPTION (provided by applicant): Benign prostatic hyperplasia (BPH) refers to the enlargement of the prostate gland, which occurs in 50% of 60-year old men with increasing incidence with age. This unchecked growth is most likely caused by dihydrotestosterone (DHT), and it produces a decreasing quality of life because of deterioration of urinary flow rate, nocturia and acute urinary retention. While drugs are currently used to treat this condition, many men would prefer to use plant sterol-containing products because they have fewer side effects. Unfortunately, the sterols contained in many of these products are of questionable efficacy, most likely because they are insoluble in water and have variable bioavailability. By mixing plant sterols with lecithin, Lifeline Technologies, Inc. has shown that this combination renders lipid sterols dispersible in water, which enhances their biological activity. Importantly, this patented technology was used in preliminary studies to show that properly formulated plant sterols inhibit steroid 5 alpha reductase to lower DHT. Moreover, when delivered to men as a single dose in a breakfast drink, formulated sterols also lowered circulating DHT 4 hours after administration. Results from the clinical and biochemical experiments outlined herein will extend these studies. First, they will provide a quantitative description of the mechanism of inhibition between plant sterols and 5 alpha reductase. Second in a clinical trial, a complete time course of DHT suppression will be determined after sterol administration, providing the basis for a dose response curve. The work inititated here and pursued in a Phase II application will lead to a new, non-pharmaceutical approach for the treatment of BPH. Because of the acknowledged safety of plant sterols, the proposed product will be cost effective, free of side effects and available over the counter. Benign prostatic hyperplasia is a chronic condition that lowers the quality of life in older men by causing nocturia and deterioration of urinary flow rate. This proposal explores a formulation method for plant sterols that lowers blood levels of dihyrotestosterone, the presumed causative agent of the disease. Because of the acknowledged safety of plant sterols, the proposed product will be cost effective, free of side effects and available over the counter.

描述（申请人提供）：良性前列腺增生（BPH）是指前列腺肿大，发生于50%的60岁男性，且发病率随着年龄的增长而增加。这种不受控制的生长很可能是由二氢睾酮 (DHT) 引起的，并且由于尿流率恶化、夜尿和急性尿潴留，它会导致生活质量下降。虽然目前使用药物来治疗这种情况，但许多男性更喜欢使用含有植物甾醇的产品，因为它们的副作用较少。不幸的是，许多这些产品中所含的甾醇的功效值得怀疑，很可能是因为它们不溶于水并且具有可变的生物利用度。 Lifeline Technologies, Inc. 已证明，通过将植物甾醇与卵磷脂混合，这种组合使脂质甾醇可分散在水中，从而增强其生物活性。重要的是，这项专利技术在初步研究中的应用表明，正确配制的植物甾醇可以抑制类固醇5α还原酶，从而降低DHT。此外，当以早餐饮料中的单剂量形式提供给男性时，配制的甾醇还可在给药后 4 小时降低循环 DHT。本文概述的临床和生化实验的结果将扩展这些研究。首先，他们将定量描述植物甾醇和 5α 还原酶之间的抑制机制。其次，在临床试验中，将在施用甾醇后确定 DHT 抑制的完整时程，为剂量反应曲线提供基础。这里启动并在二期应用中进行的工作将带来一种治疗 BPH 的新的非药物方法。由于植物甾醇的安全性得到公认，因此所提议的产品将具有成本效益、无副作用且可在柜台购买。良性前列腺增生是一种慢性疾病，会导致夜尿和尿流量下降，从而降低老年男性的生活质量。该提案探索了一种植物甾醇的配制方法，该方法可以降低血液中二氢睾酮的水平，二氢睾酮是该疾病的假定致病因子。由于植物甾醇的安全性得到公认，因此所提议的产品将具有成本效益、无副作用且可在柜台购买。