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从选定的尼日利亚药用植物中体外筛选蛋白酪氨酸磷酸酶1B和二肽基肽酶IV抑制剂。

In vitro screening for protein tyrosine phosphatase 1B and dipeptidyl peptidase IV inhibitors from selected Nigerian medicinal plants.

作者信息

Saidu Yusuf, Muhammad Suleiman Alhaji, Abbas Abdullahi Yahaya, Onu Andrew, Tsado Ibrahim Mohammed, Muhammad Luba

机构信息

Department of Biochemistry, Usmanu Danfodiyo University, Sokoto.

出版信息

J Intercult Ethnopharmacol. 2016 Dec 22;6(2):154-157. doi: 10.5455/jice.20161219011346. eCollection 2017 Apr-Jun.

Abstract

BACKGROUND/AIM: Protein tyrosine phosphatase 1B (PTP 1B) and dipeptidyl peptidase IV (DPP IV) have been identified as one of the drug targets for the treatment of Type-2 diabetes. This study was designed to screen for PTP 1B and DPP-IV inhibitors from some Nigerian medicinal plants.

MATERIALS AND METHODS

PTP 1B and DPP-IV drug discovery kits from Enzo Life Sciences were used to investigate in vitro inhibitory effect of crude methanolic extract of 10 plants; , , , , , , , , , and .

RESULTS

The results indicated PTP IB inhibition by (68.2 ± 2.29%), (67.4 ± 2.80%), (57.2 ± 2.50%), (55.1 ± 2.19%), and (41.2 ± 1.87%) were significantly ( < 0.05) higher as compared with standard inhibitor, sumarin while that of (18.1 ± 2.00%) was significantly lower as compared with sumarin. The PTB 1B inhibition by (31.5 ± 1.90%) was not significantly ( > 0.05) different from that of sumarin. The DPP-IV inhibition by (68.1 ± 2.71%) was significantly higher as compared with a known inhibitor, P32/98. (57.0±1.91%), (56.6±2.01%), (51.0±1.30%), (44.6 ± 2.40%), (36.2 ± 2.00%), (35.4 ± 2.10%), and (33.6 ± 1.50%) show significantly ( < 0.05) lower inhibitions toward DPP-IV.

CONCLUSION

The work demonstrated that these plant materials could serve as sources of lead compounds in the development of anti-diabetic agent(s) targeting PTP 1B and/or DPP-IV.

摘要

背景/目的:蛋白酪氨酸磷酸酶1B(PTP 1B)和二肽基肽酶IV(DPP IV)已被确定为治疗2型糖尿病的药物靶点之一。本研究旨在从一些尼日利亚药用植物中筛选PTP 1B和DPP-IV抑制剂。

材料与方法

使用来自安捷伦生命科学公司的PTP 1B和DPP-IV药物发现试剂盒,研究10种植物的甲醇粗提物的体外抑制作用; , , , , , , , , 以及 。

结果

结果表明, (68.2±2.29%)、 (67.4±2.80%)、 (57.2±2.50%)、 (55.1±2.19%)和 (41.2±1.87%)对PTP IB的抑制作用与标准抑制剂苏木精相比显著更高(P<0.05),而 (18.1±2.00%)与苏木精相比显著更低。 (31.5±1.90%)对PTB 1B的抑制作用与苏木精相比无显著差异(P>0.05)。 (68.1±2.71%)对DPP-IV的抑制作用与已知抑制剂P32/98相比显著更高。 (57.0±1.91%)、 (56.6±2.01%)、 (51.0±1.30%)、 (44.6±2.40%)、 (36.2±2.00%)、 (35.4±2.10%)和 (33.6±1.50%)对DPP-IV的抑制作用显著更低(P<0.05)。

结论

该研究表明,这些植物材料可作为开发靶向PTP 1B和/或DPP-IV的抗糖尿病药物的先导化合物来源。

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