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研究:达雅克洋葱鳞茎(Merr)乙醇提取物对良性前列腺增生(BPH)的 COX-2 抑制作用作为治疗创新。

and Study: COX-2 Inhibition by Ethanol Extract of Dayak Onion Bulb ( Merr) as Treatment Innovation of Benign Prostatic Hyperplasia (BPH).

机构信息

Doctoral Program of Medical Science, Faculty of Medicine, Brawijaya University, Malang, East Java, Indonesia.

Department of Pharmacology, Faculty of Medicine, Brawijaya University, Malang, East Java, Indonesia.

出版信息

Antiinflamm Antiallergy Agents Med Chem. 2021;20(1):68-74. doi: 10.2174/1871523019666200304121702.

DOI:10.2174/1871523019666200304121702
PMID:32129166
Abstract

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.

摘要

简介

良性前列腺增生症(BPH)是一种男性良性肿瘤,组织病理学上表现为上皮细胞和前列腺基质增多。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 中的慢性炎症表现为 COX-2 的过度表达,这会触发 Bcl-2 抗凋亡蛋白的表达。达雅洋葱(Eleutherine americana Merr)是一种典型的加里曼丹植物,被称为前列腺疾病的治疗方法。这种植物含有黄酮类化合物,可以抑制 COX-2 酶,从而减少前列腺素 E2 的产生。

方法

这项研究是一种计算实验和体外实验室实验研究,旨在确定达雅洋葱乙醇提取物对 COX-2 的抑制活性。

结果与讨论

在计算机模拟中,黄酮类化合物与 TYR371 活性部位的 COX-2 受体强烈相关。因此,它有可能抑制 COX-2。COX-2 抑制剂会导致 BCL-2 失活,从而导致 BPH 细胞凋亡。在使用人全血测定的体外研究中,达雅洋葱鳞茎乙醇提取物对 COX-2 的 IC50 为 40.57ng/ml,对 COX-1 的 IC50 为 364.89ng/ml。因此,IC50 COX-2 与 IC50 COX-1 的比值为 0.11。

结论

达雅洋葱鳞茎的乙醇提取物对 COX-2 具有抑制活性。因此,它有可能成为 BPH 治疗的创新药物。

患者总结

一位健康的男性,年龄 25-35 岁(询问病史、体格检查和实验室检查),过去 2 周内未使用 NSAIDs。

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