Saikosaponin B1

Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the 5-HT_2C receptor with an EC₅₀ of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB)^[1][4]. In Vitro:Saikosaponin B1 (10 nM-10 μM, 36 h) reduces the level of glioma-associated oncogene homolog (GLI)-luciferase activity in transfected Shh Light II cells with an IC₅₀ of 241.8 nM^[1].
Saikosaponin B1 (5 μM, 6-24 h) does not target GLI transcription factor and it downstream molecules, as Saikisaponin B1 shows no inhibition activity against PGE2 (HY-P3502B)-induced TCF/LEF and GLI activity in transfected LS174T cells, or TNF-α-induced NF-κB in HEK293T cell^[1].
Saikosaponin B1 (3 μM, 36 h) fails to inhibit GLI-luciferase activity increased by limiting negative regulation from SUFU in SUFU-knockout Shh Light II cells, indicating Saikosaponin B1 targets Hh pathway via upstream components of SUFU^[1].
Saikosaponin B1 (3 μM, 36 h) significantly prevents the increased of Gli1 mRNA expression induced by SAG (HY-12848) (a synthetic Hh pathway agonist binds to SMO) in Shh Light II cells with an IC₅₀ of 3.64 μM^[1].
Saikosaponin B1 (10 nM-10 μM, 72 h) significantly inhibits the proliferation of DAOY cell line (derived from nodular MB with GLI transcriptional activity)^[1].
Saikisaponin B1 (1-10 μM, 0-24 h) decreases expression of TGF-β1-induced HSC activation biomarkers^[2].
Saikisaponin B1 (0-10 μM) with biotin-label retains the inhibition activity of fibrotic protein expression in the activated HSC-T6 cells and shows the most remarkable binding to STAT3^[2].
Saikisaponin B1 (50 μM) with biotin-label pulls down the STAT3 protein but no obvious interactions with JAK2 or IL-6 in HSC-T6 cells, LX-2 cells, and mouse liver tissues^[2].
Saikisaponin B1 (1-10 μM) inhibits STAT3 phosphorylation in Tyr 705 but does not influence Ser 727 phosphorylation in HSC-t6 and LX-2 cells^[2].
Saikisaponin B1 (5-10 μM, 24 h) disrupts STAT3 dimerization even in the presence of IL-6 (20 ng/mL) at 10 μM in HSC-T6 cells^[2].
In Vivo:Saikosaponin B1 (30 mg/kg, i.p., daily for 18 d) significantly inhibits tumor growth and reduces Gli1 mRNA in tumor tissues in MB mice subcutaneously allografted with primary MB tumor tissues^[1].
Saikosaponin B1 (200 mg/kg, i.p., three times a week from week 4 to week 7) ameliorates the Thioacetamide (TAA) (HY-Y0698)-induced morphological changes and liver damage with decreased collagen deposition in TAA-induced liver fibrosis model^[2].
Saikosaponin B1 (10 mg/kg, s.c., twice a week for 4 weeks) attenuates the fibrosis histopathological characteristics of the liver tissues in CCl₄-induced liver fibrotic mice^[2].
Saikosaponin B1 (20 mg/kg, i.p., for 4 weeks) fails to further reduce liver fibrosis in response to CCl₄ in CCl₄mediated liver fibrosis STAT3 knockout mice model, suggesting STAT3 knockdown abrogated the antifibrosis effect of Saikosaponin B1^[2].
Saikosaponin B1 (2.5-10 mg/kg, i.p., once per day for 7 consecutive days) inhibits pulmonary edema in LPS (HY-D1056)-induced ALI mice^[3].