SaikosaponinD (SSd) is a major triterpenoid saponin derivative from Radix bupleuri, which has been long used in Chinese traditional medicine for treatment of various inflammation-related diseases; it shows potent anti-inflammatory activity through inhibitory effects on NF-κB activation and thereby on iNOS, COX-2 and pro-inflammatory cytokines.
Saikosaponin D attenuates CCl4-induced hepatic fibrosis in rats, which may be related to its effects of hepato-protective and anti-inflammation properties,the down-regulation of liver TNF-α, IL-6 and NF-κBp65 expression and the increased I-κBα activity in liver.
Saikosaponin D is an agonist of the glucocorticoid receptor (GR), and it possesses neuroprotective effects in corticosterone-treated PC12 cells; SSD exhibits its anti-apoptotic effects via differential regulation of mitochondrial and nuclear GR translocation, partial reversal of mitochondrial dysfunction, inhibition of the mitochondrial apoptotic pathway, and selective activation of the GR-dependent survival pathway.
Saikosaponin D is a novel autophagic inducer, can increase cytosolic calcium level via direct inhibition of sarcoplasmic/endoplasmic reticulum Ca(2+) ATPase pump, leading to autophagy induction through the activation of the Ca(2+)/calmodulin-dependent kinase kinase-AMP-activated protein kinase-mammalian target of rapamycin pathway, which has the potential of being developed into an anti-cancer agent for targeting apoptosis-resistant cancer cells.
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