Inhibition of Cyclooxygenase Enzyme by Bioflavonoids in Horsegram Seeds Alleviates Pain and Inflammation

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Author(s): Malarvizhi R, Veeresh Kumar Sali, Meenakshi Bhardwaj, Sugumar Mani, Hannah R. Vasanthi*

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

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Background: Inflammation and pain cause distress and its perception is mainly induced by the prostaglandins synthesized by the cyclooxygenase enzymes. To overcome this unpleasant stress in a safer manner, numerous natural molecules are proven for modulating the COX enzymes. Epicatechin and daidzein are two bioactive natural compounds present in horsegram a legume known for its medicinal properties.

Objective: The present study aims to check the ability of horsegram and specifically some bioactive molecules in it for its ability to be used as an anti-inflammatory and analgesic agent mediated by the inhibition of COX enzymes which can be recommended as a substitute for chemically synthesized NSAIDs.

Methods: The COX enzyme inhibitory nature of epicatechin and daidzein was tested using in silico docking analysis with Autodock software and was further confirmed by in vitro COX inhibitory biochemical assays. Further, the anti-inflammatory and analgesic activity of the horsegram seeds were checked in animal experiments.

Results: The present work involved the quantification of epicatechin and daidzein present in horsegram seeds. The docking studies reveal that both the bioactive molecules exhibit better binding efficiency with COX-2 protein as compared to COX-1. Hence, in vitro COX-2 inhibitory assay performed for epicatechin, daidzein and compared with known analgesic agent diclofenac revealed a pronounced dose dependent inhibitory activity. Further, the in vivo studies on analgesic and anti-inflammatory activity of horsegram exhibited a dose dependent effect which might be due to the presence of bioactive compounds such as epicatechin and daidzein.

Conclusion: The results suggest thatepicatechin and daidzeinpresent in horsegram are potent cyclooxygenase inhibitors and thus in turn would be helpful in the management of inflammation and pain.

Keywords: COX-2 inhibitor, Epicatechin, Daidzein, Horsegram, Inflammation, Pain

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(E-pub Ahead of Print)
DOI: 10.2174/1386207323666200127114551
Price: $95

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