Background: Inflammation and pain, mainly induced by the prostaglandins synthesized
by the cyclooxygenase enzymes, may cause distress. 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
Objective: The present study aims at evaluating the potential of horsegram, and some of its
bioactive molecules, 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
Methods: The present work involved the quantification of epicatechin and daidzein present in
horsegram seeds. 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. Furthermore, the anti-inflammatory and analgesic activities of the
horsegram seeds were evaluated in animal experiments.
Results: Horsegram seeds contain 158.1 microgram/g and 6.51 microgram/g of epicatechin and
daidzein respectively. 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 was performed for epicatechin, daidzein and compared with known analgesic agent
diclofenac which revealed a pronounced dose dependent inhibitory activity. Furthermore, the
analgesic and anti-inflammatory activity of horsegram in experimental animals exhibited a dose
dependent effect which might be due to the presence of the bioactive compounds such as
epicatechin and daidzein.
Conclusion: The results suggest that epicatechin and daidzein present in horsegram are potent
cyclooxygenase inhibitors and thus would be helpful in the management of inflammation and pain.