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 HCV ) by inhibiting the activation of the 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]
體外研究In Vitro )
Bicyclol (0.1-1 mmol/L, 3 h) 以劑量依賴的方式抑制 CCL4 誘導(dǎo)肝中毒的 Wistar 大鼠肝細胞中 ALT 和 AST 的釋放和 MDA 的產(chǎn)生[1] Palmitic acid (HY-N0830 ) 誘導(dǎo)人肝細胞 HL-7702 細胞的凋亡，并抑制 Palmitic acid (HY-N0830 ) 誘導(dǎo)巨噬細胞中 MAPKs 和 NF-κB 的活化[2] HCV 感染的 Huh7.5 細胞內(nèi)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 ) 耐藥性的逆轉(zhuǎn)作用分別為 2.8、7.3 和 20.7 倍[8] Vincristine sulfate (HY-N0488 ) 耐藥的人口表皮樣癌 VinRKB 和 Doxorubicin (HY-15142A )
耐藥的人乳腺癌 AdrRMCF-7 細胞攝取藥物濃度，使耐藥細胞對抗癌藥物增敏[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.
體內(nèi)研究In Vivo )
Bicyclol (50, 100 和 200 mg/kg; p.o.; 單劑量給藥) 對小鼠不同藥物介導(dǎo)的肝損傷有劑量依賴性的肝損傷保護作用[1] Acetaminophen (HY-66005 ) 誘導(dǎo)的小鼠肝細胞線粒體損傷具有明顯的保護作用[1] mRNA 的表達和 TNF-α 的釋放而起到抗肝細胞凋亡的作用[1] Acetaminophen (HY-66005 ) 引起的小鼠肝損傷，減少血清轉(zhuǎn)氨酶、肝壞死、線粒體細胞色素C 和凋亡誘導(dǎo)因子 (AIF) 的釋放和肝 DNA 斷裂[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 號
性狀
顏色
中文名稱
運輸條件
Room temperature in continental US; may vary elsewhere.
儲存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
2 years
-20°C
1 year
溶解性數(shù)據(jù)
細胞實驗：
DMSO 中的溶解度 : 100 mg/mL (256.19 mM ; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO )
配制儲備液
濃度
溶劑體積
質(zhì)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
查看完整儲備液配制表
*
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效 。 儲備液的保存方式和期限： -80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)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
動物實驗：
請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存 ；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用 ；以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比 ；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
方案 一
請依序添加每種溶劑 ： 10% DMSO PEG300 Tween-80
Solubility: ≥ 2.5 mg/mL (6.40 mM); 澄清溶液
此方案可獲得 ≥ 2.5 mg/mL （飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80 ，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL 。
生理鹽水的配制： 將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案 二
請依序添加每種溶劑 ： 10% DMSO SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.40 mM); 懸濁液; 超聲助溶
此方案可獲得 2.5 mg/mL 的均勻懸濁液，懸濁液可用于口服和腹腔注射。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案 三
請依序添加每種溶劑 ： 10% DMSO Corn Oil
Solubility: ≥ 2.5 mg/mL (6.40 mM); 澄清溶液
此方案可獲得 ≥ 2.5 mg/mL （飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 900 μL 玉米油
以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完 。
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；
如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。
方案 一
請依序添加每種溶劑 ： 0.5% CMC-Na /0.5% Tween-80 in Saline water
Solubility: 1 mg/mL (2.56 mM); 懸濁液; 超聲助溶
方案 二
請依序添加每種溶劑 ： 15% Cremophor EL
Solubility: 2 mg/mL (5.12 mM); 澄清溶液; 超聲助溶
動物溶解方案計算器
請輸入您的動物體內(nèi)配方組成：
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需
助溶劑 包括：
DMSO ，
，均可在 MCE 網(wǎng)站選購。
，
Tween 80 ，均可在 MCE 網(wǎng)站選購。
純度 & 產(chǎn)品資料
純度: 99.91%
選擇批次：
HY-B0766-58****
HY-B0766-21***
參考文獻
[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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