The major natural bioactive constituent of Andrographis paniculata (AP) (Burm. f.) Nees Andrographolide (1) and its derivatives are well acknowledged in literature for its biological activities such as anti-cancer, anti-diabetic, anti-inflammatory, anti-bacterial, anti-malarial, antihepatitis, anti-HIV, anti-atherosclerosis, hepatoprotective, FXR antagonist, and α-glucosidase inhibition. Many reports are available related to Andrographolide (1) but a consolidated review on the chemical modification of andrographolide with special emphasis on its different functional groups with respect to their biological activities is still missing from the previous literature. Therefore, herein we have collected a literature for the period 2009 onwards in relation to chemistry on andrographolide (1) and its effect on respective biological activity. Also, special attempt on increasing the bioavailability of andrographolide (1) has been given for the designing of various targeted drug delivery systems.
Keywords: Acylation; Andrographolide (1); Bioavailability; Biological activities; Chemical modification; Clinical trial; Epoxidation.
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