Momordica charantia L (Cucurbitaceae) is commonly known as bitter melon and thrives in tropical areas such as Amazon, East Africa, Asia, South America, and the Caribbean. Indigenous populations have been using bitter melons to treat diabetes and related health conditions. Cucurbitane-type triterpenes and their glycosides from this plant have received the most attention due to their wide range of biological activities. More than 240 cucurbitane triterpenoids have been reported from different bitter melon plants. However, the constituents responsible for the hypoglycemic/antihyperglycemic activities have not been determined. Therefore, to understand active constituents responsible for anti-diabetic activity, present research was conducted to isolate potential compounds from bitter melon. Ten compounds were isolated from bitter melon and structures were unambiguously elucidated by spectrscopic studies. Purified compounds displayed potential inhibition of carbolytic enzymes. Momordicoside G and 2-hydroxy-5-O-β-D-xylopyranosyl benzoic acid exhibited the highest α-amylase and α-glucosidase inhibition respectively. Furthermore, molecular docking studies substantiated in vitro findings in which isolated compounds were able to bind to the active sites of both enzymes. Additionally, the isolated compounds significantly attenuated lipopolysaccharide-induced inflammation, downregulating the expression of pro-inflammatory markers NF-κB, iNOS, IL-6, IL-1β, TNF-α, and Cox-2 in murine macrophage RAW264.7. Moreover, 2-hydroxy-5-O-β-D-xylopyranosyl benzoic acid was isolated for the first time, and significantly suppressed the expression of Cox-2 and IL-6 compared to the LPS-treated group. Our findings suggest that selected compounds purified from bitter melon may have potential to reduce risk from diabetes as functional food ingredients based on their inhibition potential α-amylase and α-glucosidase.

Antidiabetic and anti-inflammatory potential of isolated compounds from bitter melon: In vitro and in silico approaches

2019 Fall National Meeting

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