生物活性
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 NF-κB ROS-MAPK-NF-κB pathway, and prevents ferroptosis Mdr-1 , GSH/GST and Bcl-2 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[1] [2] [3] [4] [5] [6] [7] [8]
体外研究In Vitro )
Bicyclol (0.1-1 mmol/L, 3 h) 以剂量依赖的方式抑制 CCL4 诱导肝中毒的 Wistar 大鼠肝细胞中 ALT 和 AST 的释放和 MDA 的产生[1] Palmitic acid (HY-N0830 ) 诱导人肝细胞 HL-7702 细胞的凋亡，并抑制 Palmitic acid (HY-N0830 ) 诱导巨噬细胞中 MAPKs 和 NF-κB 的活化[2] HCV 感染的 Huh7.5 细胞内氧自由基水平，抑制了 p38、ERK、JNK 和 NF-κB 的磷酸化[4] [5] [6] Vincristine sulfate (HY-N0488 ) 耐药性的逆转作用分别为 2.8、7.3 和 20.7 倍[8] Vincristine sulfate (HY-N0488 ) 耐药的人口表皮样癌 VinRKB 和 Doxorubicin (HY-15142A )
耐药的人乳腺癌 AdrRMCF-7 细胞摄取药物浓度，使耐药细胞对抗癌药物增敏[8]
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
CCL4-induced intoxication of Wistar rat hepatocytes
Concentration:
10-4 -10-3 mol/L
Incubation Time:
3 h
Result:
Improved rat liver cell viability and reduced cell surface damage such as microvilli aggregation and shedding.
Cell Proliferation Assay[6]
Cell Line:
HepG2 cells
Concentration:
50, 100, 200 and 500 μM
Incubation Time:
24 and 48 h
Result:
Inhibited the phosphorylation of Akt and ERK, and downregulates the expression of cyclin D1, cyclin E2, CDK2, CDK4, p-Rb, and p-mTOR.
Apoptosis Analysis[2]
Cell Line:
Palmitic acid induces human hepatocyte HL-7702 cells
Concentration:
40 and 80 μM
Incubation Time:
1 h
Result:
Inhibited the expression of IL-6 and TNF-α induced by PA.
Western Blot Analysis[8]
Cell Line:
Vincristine-resistant human epidermoid carcinoma VinRKB and doxorubicin-resistant human breast cancer AdrRMCF-7
Concentration:
50 and 100 μM
Incubation Time:
24-72 h
Result:
Reduced the level of p-glycoprotein encoded by the MDR-1 gene in VinRKB and AdrRMCF-7 cells to the level of drug-sensitive cells. The increase of GSH content in virrkb and AdrRMCF-7 cells increased the GST activity of AdrRMCF-7 cells, and the overexpression of Bcl-2 protein.
体内研究In Vivo )
Bicyclol (50, 100 和 200 mg/kg; p.o.; 单剂量给药) 对小鼠不同药物介导的肝损伤有剂量依赖性的肝损伤保护作用[1] Acetaminophen (HY-66005 ) 诱导的小鼠肝细胞线粒体损伤具有明显的保护作用[1] mRNA 的表达和 TNF-α 的释放而起到抗肝细胞凋亡的作用[1] Acetaminophen (HY-66005 ) 引起的小鼠肝损伤，减少血清转氨酶、肝坏死、线粒体细胞色素C 和凋亡诱导因子 (AIF) 的释放和肝 DNA 断裂[1] [1] [2] [5]
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
CCl4, D-Galactosamine, Acetaminophen-Induced Liver Injury in Mice [1]
Dosage:
50, 100 and 200 mg/kg
Administration:
Oral gavage (p.o.) Single dose administration
Result:
Reduced the elevated serum ALT and AST levels in a dose-dependent manner, and also ameliorated the liver lesions.
Animal Model:
Acetaminophen-Induced Liver Injury in Mice [1]
Dosage:
50 and 150 mg/kg
Administration:
Oral gavage (p.o.); Once a day for 3 days
Result:
Reduced mitochondrial ultrastructural damage, mitochondrial AST release, mitochondrial fluidity and mitochondrial swelling, and mitochondrial cytochrome C release.
Animal Model:
ConA and acetaminophen-Induced Liver Injury in Mice [1]
Dosage:
300 mg/kg
Administration:
Oral gavage (p.o.); Once a day for 3 days
Result:
Induced the expression of HSP70/27 mRNA and protein in mouse liver and activated heat shock factor-1 (HSF1) in mouse liver.
Animal Model:
HFD-induced liver inflammation in mice[2]
Dosage:
25 and 50 mg/kg
Administration:
Oral gavage (p.o.); once every other day for the last four weeks of the 16-week HFD induction
Result:
Inhibited the expression levels of pro-inflammatory genes IL-6, TNF-α, IL-1β, COX-2, ICAM-1, VCAM-1, and MCP-1.
Animal Model:
CCl4-induced ALI mice[6]
Dosage:
200 mg/kg
Administration:
Intraperitoneal injection (i.p.); 3 times a day for 2 days
Result:
Inhibited iron accumulation, excessive production of reactive oxygen species, enhanced lipid peroxidation, altered mitochondrial morphology, and decreased GPx4 and xCT protein levels in mouse liver.
Clinical Trial
分子量
Formula
CAS 号
性状
颜色
中文名称
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
2 years
-20°C
1 year
溶解性数据
细胞实验：
DMSO 中的溶解度 : 100 mg/mL (256.19 mM ; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO )
配制储备液
浓度
溶剂体积
质量
1 mg 5 mg 10 mg
1 mM
2.5619 mL
12.8093 mL
25.6187 mL
5 mM
0.5124 mL
2.5619 mL
5.1237 mL
10 mM
0.2562 mL
1.2809 mL
2.5619 mL
查看完整储备液配制表
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效 。 储备液的保存方式和期限： -80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
动物实验：
请根据您的 实验动物和给药方式 选择适当的溶解方案。
以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液澄清的储备液可以根据储存条件，适当保存 ；体内实验的工作液，建议您现用现配，当天使用 ；以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比 ；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
请依序添加每种溶剂 ： 10% DMSO PEG300 Tween-80
Solubility: ≥ 2.5 mg/mL (6.40 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL （饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80 ，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL 。
生理盐水的配制： 将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案 二
请依序添加每种溶剂 ： 10% DMSO SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.40 mM); 悬浊液; 超声助溶
此方案可获得 2.5 mg/mL 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。
20% SBE-β-CD in Saline 的配制（4°C，储存一周）： 2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案 三
请依序添加每种溶剂 ： 10% DMSO Corn Oil
Solubility: ≥ 2.5 mg/mL (6.40 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL （饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 900 μL 玉米油
以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完 。
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；
如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一
请依序添加每种溶剂 ： 0.5% CMC-Na /0.5% Tween-80 in Saline water
Solubility: 1 mg/mL (2.56 mM); 悬浊液; 超声助溶
方案 二
请依序添加每种溶剂 ： 15% Cremophor EL
Solubility: 2 mg/mL (5.12 mM); 澄清溶液; 超声助溶
动物溶解方案计算器
请输入您的动物体内配方组成：
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
纯度 & 产品资料
纯度: 99.91%
选择批次：
HY-B0766-58****
HY-B0766-21***
参考文献
[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]
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