Botanical Source

Asperulosidic acid has been recently used in chinese medicine as a useful drug against some tumors. It has anticlastogenic activity, since the anticlastogenic irridoids have an alpha-unsaturated carbonyl group, this structure is considered to play an important role in the anticlastogenicity. Asperulosidic acid can inhibit the seed germination and growth of seedlings of large crabgrass. Asperulosidic acid, and 6-O-(beta-D-glucopyranosyl)-1-O-octanoyl-beta-D-glucopyranose are effective in suppressing 12-O-tedtradecanoylphorbol-13-acetate (TPA)- or epidermal growth factor (EGF)-induced cell transformation and associated AP-1 activity.

Limonin is a widely used dietary supplement, one of the most prevalent citrus limonoids, which has antioxidant, anti-inflammatory, anticancer and anti-human immunodeficiency virus(HIV)activity. It induced a down regulation of TLR-2 ,TLR-4,TNF-α, TNF-α/IL-10,NF-κB and caspase. It showed the potent inhibition of CYP3A4, with IC50 values of 6.20 μM (CYP3A4/testosterone) and 19.10 μM (CYP3A4/midazolam).

Wogonin is one major constituent of Scutellaria baicalensis, possesses potent anticancer activities , the activities are largely due to their abilities to scavenge oxidative radicals, to attenuate NF-kappaB activity, to inhibit several genes important for regulation of the cell cycle, to suppress COX-2 gene expression and to prevent viral infections.

Farrerol has antioxidative, anti-bacterial, anti-inflammatory, antiangiogenic activities, it is a potential candidate for the intervention of endothelial-injury-associated cardiovascular diseases. Farrerol inactivates KEAP-1 or activates the Akt, p38 and ERK to facilitate the release of Nrf2 from Keap1 and subsequent reduces the intracellular production of reactive oxygen species via the induction of HO-1 expression. Farrerol can inhibit angiogenesis through down regulation of Akt/mTOR, Erk and Jak2/Stat3 signal pathway, and can inhibit IL-1β-induced inflammatory responses in osteoarthritis chondrocytes by blocking PI3K/Akt/NF-κB signaling pathway.