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IC50: 11.0 ± 0.28 μg/ml for α-glucosidase; 11.3 ± 0.29 μg/ml for α-amylase

Andrographolide is an irreversible antagonist of NF-κB. The nuclear factor NF-κB pathway has been considered as a prototypical proinflammatory signaling pathway, based on the role of NF-κB in the expression of proinflammatory genes including chemokines, cytokines and adhesion molecules.

In vitro: Andrographolide was found to suppress the expression of inducible nitric oxide synthase in a concentration-dependent manner. In the andrographolide-treated group, a reduction of Akt, c-Jun N-terminal kinase and p65 phosphorylation was observed. Andrographolide also caused a decrease in Bcl-2/NF-κb expression and a dose-dependent increase in the expression of Cleaved-Caspase3/Bax protein [1].

In vivo: Rats were dosed with andrographolide intragastrically for 5 consecutive days in a hepatoprotection study. Results indicated that andrographolide could up-regulate glutamate cysteine ligase catalytic and modifier subunits, heme oxygenase-1, superoxide dismutase-1, glutathione S-transferase protein and mRNA expression in the heart, liver, and kidney [2].

Clinical trial: N/A.
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