ArticleAnti-cancer agents in medicinal chemistry2025
Discovery of a Novel Co-crystal of Chrysin and Oroxylin A with Anticancer Properties from Leaves of
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Abstract
backgroundAs the number of new cancer cases increases every year, there is a necessity to develop new drugs for the treatment of different types of cancers. Plants' resources are considered to be huge reservoirs for therapeutic agents in nature. Among all the medicinal plants,
aimThis study was conducted with the aim of identifying new anticancer compounds from the leaves of
objectiveIn this study, we elucidated the structure of a new co-crystal compound, which was isolated from the leaf extract of
methodsA crystal compound from the chloroform extract of leaves of
resultsThe novel co-crystal consists of two active pharmaceutical ingredients (APIs) in a 1:1 ratio, i.e., oroxylin A and chrysin. The isolated new co-crystal induced death in HeLa cells with a very low IC50 value of 8.49 μM. It induced caspase-dependent apoptosis in HeLa cells by activation of Caspase-3 through inhibition of ERKs and activation of p38 of MAPK cell signalling pathway.
conclusionThis study presents the first report on the discovery of a naturally occurring co-crystal of chrysin and oroxylin A and the involvement of ERKs and p38 of MAPK pathways in the induction of apoptosis in HeLa cells by the co-crystal. Our study sheds light on the development of a co-crystal of chrysin and oroxylin A in a specific ratio of 1:1 for combination therapy of the two APIs. The purified co-crystal was found to be more efficient compared to the compounds present individually. Further analysis of the physiochemical properties and molecular mechanisms of the isolated co-crystal in different cancer cells is warranted for its application in therapeutics.
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