synthase inhibitors

Penicillamine (Artamine), possessing antineoplastic properties, induces apoptosis by a p53-mediated mechanism and inhibits angiogenesis by chelating with copper, a cofactor for angiogenesis. Artamine is a beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, Artamine chelates with heavy metals and increases their urinary excretion.

1. Corylifol A (Corylinin) displays cytotoxic activity against HepG2 and Hep3B hepatocellular carcinoma cell lines, with IC50 values of 4.6 and 13.5 ug/ml, respectively. 2. Corylifol A and Biochanin A can be the potential uncouplers of neuronal nitric oxide synthase-postsynaptic density protein-95. 3. Corylifol A and bavachin are strong inhibitors of UDP-glucuronosyltransferase 1A1 (UGT1A1) with the inhibition kinetic parameters (Ki) values lower than 1 uM.4. Corylifol A and bakuchiol are naturally occurring potent inhibitors of hCE2, with low Ki values ranging from 0.62uM to 3.89 uM. 5. Corylifol A shows an inhibitory effect on IL-6-induced STAT3 promoter activity in Hep3B cells with IC50 values of 0.81 ± 0.15 uμ, it also inhibits STAT3 phosphorylation induced by IL-6 in Hep3B cells, suggests that corylifol A has antiinflammatory activity.

1. Desoxyrhaponticin (Deoxyrhaponticin) is an agent that is potentially effective in controlling postprandial hyperglycemia in diabetes, the in vivo antidiabetic action of this compound can be explained, in part at least, by inhibition of glucose transport in the small intestine and inhibition of glucose reabsorption in the kidney. 2. Desoxyrhaponticin and rhaponticin could be considered as promising fatty acid synthase(FAS) inhibitors, they could inhibit intracellular FAS activity and downregulate FAS expression in human breast cancer MCF-7 cells.

Albaspidin-AP, -PP, -PB inhibit Fatty acid synthase (FAS) with IC50 values ranging from 23.1+ -1.4 to 71.7+ -3.9 microM, they could be considered to be a promising class of FAS inhibitors, and FAS is emerging as a potential therapeutic target to treat can