BicyclolBicyclol
MedChemExpress (MCE)
HY-B0766
118159-48-1
SY801
99.91%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma.
Bicyclol (0.1-1 mmol/L, 3 h) inhibits the release of ALT and AST, as well as the production of MDA, in CCl4-induced hepatotoxic Wistar rat hepatocytes in a dose-dependent manner[1]. Bicyclol (40 and 80 μM
1 h) reduces palmitic acid (HY-N0830)-induced apoptosis in human hepatocyte HL-7702 cells and inhibits palmitic acid (HY-N0830)-induced activation of MAPKs and NF-κB in macrophages[2]. Bicyclol (200 μM
10 h) reduces the level of intracellular oxygen free radicals in HCV-infected Huh7.5 cells and inhibits the phosphorylation of p38, ERK, JNK, and NF-κB[4]. Bicyclol (10 μM
30 min) alleviates serrata-induced hepatocyte inactivation, destruction, and lipid peroxidation. Bicyclol (0-500 μM
0-48 h) effectively inhibits the proliferation of HepG2 cells in a dose-dependent and time-dependent manner[5]. Bicyclol (0-100 μM
24 h) reverses vincristine sulfate (HY-N0488) resistance in VinRKB cells by 2.8, 7.3, and 20.7 times, respectively[6]. Bicyclol (50 and 100 μM
12-72 h) alters the intracellular drug concentrations in vincristine sulfate (HY-N0488)-resistant human epidermoid carcinoma VinRKB and doxorubicin (HY-15142A)-resistant human breast cancer AdrRMCF-7 cells, sensitizing the resistant cells to anticancer drugs[8].
Bicyclol (50, 100 and 200 mg/kg
p.o.
single dose) has a dose-dependent protective effect against liver damage induced by different drugs in mice[1]. Bicyclol (50 and 150 mg/kg
p.o.
once a day for 3 days) has a significant protective effect against Acetaminophen (HY-66005) induced mitochondrial damage in mouse hepatocytes[1]. Bicyclol (150 mg/kg
p.o.
once a day for 3 days) inhibits the expression of Fas/FasL mRNA and the release of TNF-α in mouse hepatocytes induced by ConA and plays an anti-apoptotic role in hepatocytes[1]. Bicyclol (300 mg/kg
p.o.
once daily for 3 days) alleviates ConA- and Acetaminophen (HY-66005) induced liver damage in mice, reducing serum transaminases, liver necrosis, mitochondrial cytochrome C and apoptosis-inducing factor (AIF) release, and liver DNA fragmentation[1]. Bicyclol (75 and 150 mg/kg
p.o.
6 times per week except Sunday for 7 weeks) significantly improves liver damage and fibrosis in rats and mice induces by chronic CCl4 and Dimethylnitosamine hepatotoxicity1]. Bicyclol (25 and 50 mg/kg
p.o.
once every other day for 4 weeks) alleviates hyperlipidemia and liver damage and inhibites inflammatory signaling pathways in HFD-induced NAFLD mice[2]. Bicyclol (200 mg/kg
i.p.
3 times a day for 2 days) inhibits iron-induced apoptosis in the liver of CCl4-induced ALI mice and exerts a hepatoprotective effect[5].
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[1]. Walsh, S.W., Y. Wang, and A. Killian, AA-2414, an antioxidant and thromboxane receptor blocker, completely inhibits peroxide-induced vasoconstriction in the human placenta. J Pharmacol Exp Ther, 1999. 290(1): p. 220-6. [Content Brief]
[2]. Weixin Zhao, et al. "Bicyclol ameliorates nonalcoholic fatty liver disease in mice via inhibiting MAPKs and NF-κB signaling pathways." Biomedicine & Pharmacotherapy 141 (2021): 111874. [Content Brief]
[3]. Hui-Juan Dai, et al. "Induction of heat shock protein 27 by bicyclol attenuates d-galactosamine/lipopolysaccharide-induced liver injury." European Journal of Pharmacology 791 (2016): 482-490. [Content Brief]
[4]. Li Hu, et al. "Bicyclol attenuates liver inflammation induced by infection of hepatitis C virus via repressing ROS-mediated activation of MAPK/NF-κB signaling pathway." Frontiers in Pharmacology 9 (2018): 1438. [Content Brief]
[5]. Tianming Zhao, et al. "Regulating Nrf2-GPx4 axis by bicyclol can prevent ferroptosis in carbon tetrachloride-induced acute liver injury in mice." Cell death discovery 8.1 (2022): 380. [Content Brief]
[6]. Yu Wang, et al. "Bicyclol induces cell cycle arrest and autophagy in HepG2 human hepatocellular carcinoma cells through the PI3K/AKT and Ras/Raf/MEK/ERK pathways." BMC cancer 16 (2016): 1-15. [Content Brief]
[7]. Tianming Zhao, et al. "Therapeutic potential of bicyclol in liver diseases: lessons from a synthetic drug based on herbal derivative in traditional Chinese medicine." International Immunopharmacology 91 (2021): 107308. [Content Brief]
[8]. Bing Zhu, et al. "Chemosensitizing multiple drug resistance of human carcinoma by Bicyclol involves attenuated P-glycoprotein, GST-P and Bcl-2." Cancer biology & therapy 5.5 (2006): 536-543. [Content Brief]
