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标准化刺毛黧豆种子提取物的血管紧张素转换酶(ACE)抑制潜力。

Angiotensin-converting enzyme (ACE) inhibitory potential of standardized Mucuna pruriens seed extract.

作者信息

Chaudhary Sushil Kumar, De Apurba, Bhadra Santanu, Mukherjee Pulok K

机构信息

Department of Pharmaceutical Technology, School of Natural Product Studies, Jadavpur University , Kolkata , India.

出版信息

Pharm Biol. 2015;53(11):1614-20. doi: 10.3109/13880209.2014.996820. Epub 2015 Apr 14.

Abstract

CONTEXT

Mucuna pruriens Linn. (Fabaceae) is a tropical legume, traditionally used for controlling blood pressure. Inhibition of angiotensin-converting enzyme (ACE) is one of the successful strategies for controlling hypertension.

OBJECTIVE

The present study evaluated the ACE inhibition potential of the standardized extract of M. pruriens seeds.

MATERIALS AND METHODS

Standardization of the extract and its fractions were carried out by RP-HPLC method [methanol and 1% v/v acetic acid in water (5:95 v/v)] using levodopa as a marker. The ACE inhibition activity of the extract and fractions was evaluated at different concentrations (20, 40, 60, 80, and 100 µg/mL) using the HPLC-DAD and the UV spectrophotometric method. The liberation of hippuric acid (HA) from hippuryl-L-histidyl-L-leucine (HHL) was estimated in the spectrophotometric method and RP-HPLC assay at 228 nm.

RESULTS

Methanol extract and aqueous fraction showed a maximum activity with IC50 values of 38.44 ± 0.90 and 57.07 ± 2.90 µg/mL (RP-HPLC), and 52.68 ± 2.02 and 67.65 ± 2.40 µg/mL (spectrophotometry), respectively.

DISCUSSION

The study revealed that the aqueous extract contains the highest amount of levodopa. Eventually the methanol extract showed highest ACE inhibition activity except levodopa alone. It was further observed that the inhibition was altered with respect to the change in the content of levodopa in the extract. Thus, it can be assumed that levodopa may be responsible for the ACE inhibition activity of M. pruriens seeds.

CONCLUSION

It can be concluded that M. pruriens seed is a potential ACE inhibitor can be explored further as an effective antihypertensive agent.

摘要

背景

刺毛黧豆(豆科)是一种热带豆科植物,传统上用于控制血压。抑制血管紧张素转换酶(ACE)是控制高血压的成功策略之一。

目的

本研究评估了刺毛黧豆种子标准化提取物的ACE抑制潜力。

材料与方法

采用RP-HPLC法[甲醇和1%(v/v)乙酸水溶液(5:95,v/v)],以左旋多巴为标记物,对提取物及其馏分进行标准化。使用HPLC-DAD和紫外分光光度法,在不同浓度(20、40、60、80和100μg/mL)下评估提取物及其馏分的ACE抑制活性。在分光光度法和RP-HPLC测定中,于228nm处估计马尿酸(HA)从马尿酰-L-组氨酰-L-亮氨酸(HHL)中的释放量。

结果

甲醇提取物和水相馏分表现出最大活性,RP-HPLC法测得的IC50值分别为38.44±0.90和57.07±2.90μg/mL,分光光度法测得的IC50值分别为52.68±2.02和67.65±2.40μg/mL。

讨论

研究表明,水提取物中左旋多巴含量最高。最终,甲醇提取物表现出最高的ACE抑制活性,除了单独的左旋多巴。进一步观察到,抑制作用随提取物中左旋多巴含量的变化而改变。因此,可以假设左旋多巴可能是刺毛黧豆种子ACE抑制活性的原因。

结论

可以得出结论,刺毛黧豆种子是一种潜在的ACE抑制剂,可作为一种有效的抗高血压药物进一步探索。

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