大葱乙醇提取物抑制COX-2治疗良性前列腺增生(BPH)的实验研究

Hendra Sutapa, Mochammad Aris Widodo, Basuki Bambang Purnomo, Doddy M Soebadi, Edvin Prawira Negara
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引用次数: 3

摘要

简介:良性前列腺增生(Benign Prostatic Hyperplasia, BPH)是男性的一种良性肿瘤,在组织病理学上以上皮细胞和前列腺间质增生为特征。雄激素、雌激素、基质-上皮相互作用、生长因子和慢性炎症在BPH的发生中起关键作用。BPH慢性炎症以COX-2过度表达为特征,COX-2会触发Bcl-2抗凋亡蛋白的表达。大葱(Eleutherine Americana Merr)是一种典型的加里曼丹植物,以治疗前列腺疾病而闻名。这种植物含有类黄酮,可以抑制COX-2酶,从而减少前列腺素E2的产生。方法:采用实验研究和体外实验研究相结合的方法,测定大葱乙醇提取物对COX-2的抑制作用。结果与讨论:硅酸类黄酮与TYR371活性侧COX-2受体密切相关。因此,它具有抑制COX-2的潜力。COX-2抑制剂可使BCL-2失活,使BPH发生细胞凋亡。在体外人全血法研究中,大葱球乙醇提取物的IC50 COX-2为40.57 ng/ml, IC50 COX-1为364.89 ng/ml。因此,IC50 COX-2与IC50 COX-1的比值为0.11。结论:大葱乙醇提取物对COX-2具有抑制作用。因此,它有可能成为前列腺增生症治疗的一项创新。患者简介:健康男性,年龄25-35岁(有病史,体格和实验室检查),过去2周未使用非甾体抗炎药。
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In Silico and In Vitro Study: COX-2 Inhibition by Ethanol Extract of Dayak Onion Bulb (Eleutherine Americana Merr) as Treatment Innovation of Benign Prostatic Hyperplasia (BPH).

Introduction: Benign Prostatic Hyperplasia (BPH) is a benign tumor in males, which is histopathologically known with an increase of epithelial cells and prostatic stroma. Androgens, estrogens, stroma-epithelial interactions, growth factors, and chronic inflammation play a key role in the occurrence of BPH. Chronic inflammation in BPH is characterized by excessive expression of COX-2, which will trigger the expression of Bcl-2 anti-apoptotic protein. Dayak onion (Eleutherine Americana Merr) is a typical Kalimantan plant that is known as the treatment for prostate disease. This plant contains flavonoids which can inhibit the COX-2 enzyme thus causing a reduction in the production of prostaglandin E2.

Methods: This research was experimental research computationally and in vitro laboratory experimental research to determine COX-2 inhibitory activity by ethanol extracts of Dayak onion.

Results and discussion: In in silico flavonoid, it was strongly related to COX-2 receptor on the active side of TYR371. Thus, it had the potential to inhibit COX-2. COX-2 inhibitor would cause BCL-2 to be inactive so that apoptosis occurr in BPH. In the in vitro research using human whole blood assay, the Dayak Onion bulb ethanol extract had IC50 COX-2 of 40.57 ng/ml and IC50 COX-1 of 364.89 ng/ml. Therefore, the ratio of IC50 COX-2 to IC50 COX-1 was 0.11.

Conclusion: Ethanol extract of Dayak onion bulb has an inhibitory activity against COX-2. Thus, it has a potential of being an innovation for BPH treatment. Patient Summary: A healthy male, age 25-35 years old (history taking, physical and laboratory examination), and not using NSAIDs for the past 2 weeks.

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来源期刊
Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry
Anti-Inflammatory and Anti-Allergy Agents in Medicinal Chemistry Pharmacology, Toxicology and Pharmaceutics-Pharmacology
CiteScore
3.30
自引率
0.00%
发文量
11
期刊介绍: Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new anti-inflammatory & anti-allergy agents. Publishing a series of timely in-depth reviews written by leaders in the field covering a range of current topics, Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in the field.
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