Saidu Yusuf, Muhammad Suleiman Alhaji, Abbas Abdullahi Yahaya, Onu Andrew, Tsado Ibrahim Mohammed, Muhammad Luba
Department of Biochemistry, Usmanu Danfodiyo University, Sokoto.
J Intercult Ethnopharmacol. 2016 Dec 22;6(2):154-157. doi: 10.5455/jice.20161219011346. eCollection 2017 Apr-Jun.
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.
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 .
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.
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.
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。
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)。
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。