alpha-Glucosidase and alpha-Amylase Inhibitory Compounds from three African Medicinal Plants: An Enzyme Inhibition Kinetics Approach

作者：Ibrahim Mohammed Auwal; Habila James Dama; Koorb****ly Neil Anthony; Islam Md Shahidul^*

来源：Natural Product Communications, 2017, 12(7): 1125-1128.

DOI：10.1177/1934578x1701200731

• Bicyclo[2.2.0]hexane-2,3,5-triol
• 3 beta-O-Acetyl betulinic acid
• 2,7-Dihydroxy-4H-1-benzopyran-4-one
• Cassia singueana
• Khaya senegalensis
• Ziziphus mucronata

The quest to find new lead compounds with anti-diabetic effects via the inhibition of alpha-glucosidase and a-amylase had led us to conduct bioassay guided isolation of three African medicinal plants which resulted in the identification of bicyclo[2.2.0]hexane-2,3,5-triol (1),3 beta-O-acetyl betulinic acid (2) and 2,7dihydroxy-4H-1-benzopyran-4-one (3), as the bioactive compounds. The compounds demonstrated a significant (P < 0.05) inhibitory effect on alpha-glucosidase and alpha-amylase activities than acarbose. Steady state kinetic analysis revealed that compounds 1 and 2 inhibited both alpha-amylase and alpha-glucosidase in noncompetitive patterns whilst compound 3 was an uncompetitive inhibitor of alpha-glucosidase and a non-competitive inhibitor of alpha-amylase. In conclusion, the study has identified three new active alpha-glucosidase and alpha-amylase inhibitory compounds that could have the potential to retard postprandial hyperglycemia.

• 出版日期2017-7