Saikosaponin D

Description

Saikosaponin D is a triterpene saponin found in Bupleurum that exhibits antioxidative, immunomodulatory, anti-fibrotic, anti-angiogenic, anticancer, and chemopreventive activities. Saikosaponin D increases activity of superoxide dismutase, catalase, and glutathione peroxidase and decreases activity of malondialdehyde in cellular models of oxidative damage. In other in vitro models, saikosaponin D increases secretion of IL-12, maturation of dendritic cells, and proliferation of lymphocytes. Saikosaponin D inhibits SERCA, increasing intracellular Ca2+ and inducing autophagy. In vivo, this compound decreases severity of fibrosis. In embryos, saikosaponin D decreases microvessel formation. Additionally, this compound decreases tumor formation in DEN-treated animal models and suppresses expression of CEBP-β and COX-2. Saikosaponin D also induces apoptosis and activation of caspases 3 and 7 in hepatocellular carcinoma cells. Saikosaponin D is a Glucocorticoid receptor agonist. It is a COX-2 and iNOS inhibitor.

Chemical Properties

Pale yellow crystals, easily soluble in water and dilute alcohol, difficult to dissolve in benzene, ether and chloroform, derived from the aerial parts of Bupleurum chinense.

Uses

Saikosaponin d (SSd) is an important active component of Bupleurum scorzonerifolium Willd., a traditional Chinese medicinal herb. Saikosaponins such as Saikosaponin D are used to help analyse and resolve the activities of herbal medicines such as Sho-saiko-to.

Uses

Saikosaponin D is an inhibitor of proliferation of human prostate cancer cells through arresting the cell cycle.

Biological Activity

Saikosaponin D inhibits cell growth of human cancer cells by inducing apoptosis and blocking cell cycle progression in the G1 phase. Saikosaponin D was found to stimulate corticotropin-releasing factor (CRF) gene expression and CRF release.

in vivo

IC 50

STAT3; NF-κB; ERβ

Clinical claims and research

We have previously identified a small-molecule, saikosaponin-d (Ssd), that exhibits anti-inflammatory effect via the suppression of NF-κB, NF-AT and AP-1 signaling. We recently showed that Ssd potentiated the anti-cancer potency of TNF-α through NF-κB inhibition. Ssd is one of the major triterpenoid saponins derived from Bupleurum falcatum L. (Umbelliferae), which is commonly prescribed for inflammatory and infectious diseases, and its active component Ssd was reported to have immuno-modulatory, anti-inflammatory, anti-bacterial, anti-viral and anti-cancer activities.