Effect of the Derivatives of Andrographolide on the Morphology of Bacillus subtilis

다국어 초록 (Multilingual Abstract)

Andrographis paniculata has been reported to have antiviral, antipyretic and anticancer activities. Andrographolide, an ent-labdane diterpene, is an active constituent in this plant. In this study, andrographolide (1) and its natural derivative 14-deoxy-11,12-didehydroandrographolide (2) and 5 other semisynthetic derivatives were tested for their activity against Grampositive and Gram-negative bacteria and Candida albicans. Only derivatives bearing a 14-acetyl group showed activity, and this activity was only against Gram-positive bacteria. 14-Acetylandrographolide showed the highest potency against Bacillus subtilis; the other 14-acetylandrographolides with additional substitution at the 3- and 19-hydroxyl groups showed lower activity against Gram-positive bacteria. The morphology of B. subtilis after being treated with 14-acetylandrographolide was investigated with TEM. This is the first report on 14-acetylandrographolide’s quantified antibacterial activity, and the crucial functional group of this ent-labdane that plays an important role in perturbing the morphogenesis of B. subtilis leading to cell death.

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