silibinin

Silibinin (Silybin) is the major active constituent of silymarin, a standardized extract of the milk thistle seeds, containing a mixture of flavonolignans consisting of silibinin, isosilibinin, silicristin, silidianin and others. Silibinin itself is a mixture of two diastereomers, silybin A and silybin B, in approximately equimolar ratio. Both in vitro and animal research suggest that silibinin has hepatoprotective (antihepatotoxic) properties that protect liver cells against toxins. Silibinin has also demonstrated in vitro anti-cancer effects against human prostate adenocarcinoma cells, estrogen-dependent and -independent human breast carcinoma cells, human ectocervical carcinoma cells, human colon cancer cells, and both small and nonsmall human lung carcinoma cells.

Silybin is a flavonoid from Silybum that inhibits P-glycoprotein-assisted extracellular efflux, inhibits cytochrome P450 enzymes, has the advantage of being well-tolerated, can be used as an adjunctive treatment for hepatotoxicity and chronic hepatitis and cirrhosis, and has antioxidant and anti-inflammatory activity in cosmetic applications, as well as being capable of blocking the MCT8 transporter protein.

Silybin B (Silibinin B) is an effective inhibitor of raloxifene 4 '- and 6-glucosalylation, an effective anti-fibrinogenic and anti-oligomeric component of Silymarin, with free radical scavenging activity of 1, 1-diphenyl-2-pyridinyl hydrazine (DPPH), and a protective effect against cisplatin-induced neurotoxicity by alleviating DNA damage and apoptosis. Silybin B can inhibit the growth of human chronic myeloid leukemia K562 cells and induce apoptosis.

(±)-Silybin, a racemate of Silybin, demonstrates a range of biological activities including inducing apoptosis and possessing hepatoprotective, antioxidant, anti-inflammatory, and anti-cancer properties [1] [2].