Momordica charantia extract, a herbal remedy for type 2 diabetes, contains a specific 11β-hydroxysteroid dehydrogenase type 1 inhibitor

摘要

11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) catalyzes the intracellular regeneration of active cortisol from inert cortisone in key metabolic tissues, thus regulating ligand access to glucocorticoid receptors. There is strong evidence that increased adipose 11β-HSD1 activity may be an important aetiological factor in the current obesity and diabetes type 2 epidemics. Hence, inhibition of 11β-HSD1 has emerged as a promising anti-diabetic strategy, a concept that is largely supported by numerous studies in rodent models as well as limited clinical data with prototype inhibitors. Momordica charantia (also known as bitter melon, bitter gourd or karela) is traditionally used for treatment of diabetes in Asia, South America, the Caribbean, and East Africa. In the present study, we show that M. charantia extract capsules contain at least one ingredient with selective 11β-HSD1 inhibitory activity. The finding constitutes an interesting additional explanation for the well-documented anti-diabetic and hypoglycaemic effects of M. charantia.