From times immemorial, natural products have played an important role in the management of human health. Andrographis paniculata, belonging to the family Acanthaceae and its constituents are reported to possess a wide range of biological properties such as anti-cancer, anti-diabetic, anti-inflammatory, anti-bacterial, anti-malarial, anti-hepatitis, anti-HIV, anti-atherosclerosis, hepatoprotective, FXR antagonist, and α-glucosidase inhibitory activities. Andrographolide (1), 14-deoxy andrographolide (2), 14-deoxy 11,12-didehydro andrographolide (3) and other related labdane diterpenes are identified as the bioactive constituents of the plant. Promising biological properties of the major constituent Andrographolide (1) along with structural amenability for facile semi-synthetic modifications have led to the generation of structurally diverse bioactive labdane diterpenes. Structure Activity Relationship (SAR) studies on the new analogues synthesized by our group by modifying the 3,14,19- hydroxyl groups, double bond across C-8,17 and the lactone moiety of Andrographolide will be discussed.

Andrographolide: A versatile natural product for the generation of structurally diverse bioactive diterpenes

254th National Meeting (2017)

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