Abstract
Protein tyrosine phosphatase (PTP) 1B and dipeptidyl peptidase (DPP) IV are important in down regulation and secretion of insulin, respectively. While PTP 1B regulates insulin binding to its receptor, DPP IV hydrolyses incretin, which is an important regulator of postprandial insulin secretion. The study evaluated the in vitro inhibitory effect of different fractions of Senna nigricans against PTP IB and DPP IV and the results were compared with standard inhibitors, sumarin and P32/98. The methanolic extract was further fractionated using Soxhlet apparatus and then the most potent fraction eluted through column on silica gel. The result indicated that the methanolic fraction had the highest inhibition percentage of 56.43±3.98 against PTP 1B. The inhibition of PTP 1B by methanolic fraction was significantly (P 0.05) different from that of sumarin, while hexane fraction had the inhibition of 19.03±4.24% which was significantly (P<0.05) decreased as compared with sumarin. The result of DPP IV inhibition indicated that the methanolic, hexane and ethyl acetate fractions were not significantly different, but all the fractions were significantly less active than the standard inhibitor, P32/98 which recorded 63.1±4.67% inhibition of DPP IV. Because of S. nigricans as sources of PTP 1B inhibitors most especially and to some extent DPP IV inhibitors, the plant may be a potential source for the discovery of lead compounds as PTP 1B and DPP IV inhibitors to treat type 2 diabetes mellitus. Key words: Protein tyrosine phosphatase, dipeptidyl peptidase, inhibitors, Senna nigricans.
Highlights
Diabetes mellitus is a metabolic disorder which is due to a defect in insulin secretion, insulin action, or both
The percentage Protein tyrosine phosphatase (PTP) 1B and dipeptidyl peptidase (DPP) IV inhibitions of Soxhlet fractions of S. nigricans are presented in Figures 1 and 2, respectively
The results show that methanolic fraction had the highest percent inhibition of 56.43±3.98% for PTP 1B (Figure 1) as against the standard inhibitor, sumarin (30.12±3.46%)
Summary
Diabetes mellitus is a metabolic disorder which is due to a defect in insulin secretion, insulin action, or both. Insulin deficiency or resistance led to various metabolic alterations in diabetic subjects or animals which increased blood glucose and caused dyslipidaemia (Himma et al, 2014). The prevalence of type 2 diabetes mellitus is rapidly increasing worldwide, and it is estimated that more than 430 million people will be affected by 2030 (Shaw et al, 2010). Natural products have been shown to play a significant role in the development of novel drugs for the treatment and prevention of diseases (Gilani and Rahman, 2005)
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