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

References:
[1] Wang ZM,Kang YH,Yang X,Wang JF,Zhang Q,Yang BX,Zhao KL,Xu LP,Yang LP,Ma JX,Huang GH,Cai J,Sun XC.  Andrographolide radiosensitizes human esophageal cancer cell line ECA109 to radiation in vitro. Dis Esophagus.2016 Jan;29(1):54-61.
[2] Chen HW,Huang CS,Li CC,Lin AH,Huang YJ,Wang TS,Yao HT,Lii CK.  Bioavailability of andrographolide and protection against carbon tetrachloride-induced oxidative damage in rats. Toxicol Appl Pharmacol.2014 Oct 1;280(1):1-9.