Sinomenine Hydrochloride
(Synonyms: 盐酸青藤碱; Cucoline hydrochloride) 目录号 : GN10213
Sinomenine Hydrochloride是NF-κB活化的抑制剂。
Cas No.:6080-33-7
Sample solution is provided at 25 µL, 10mM.
Sinomenine Hydrochloride is an inhibitor of NF-κB activation [1]. Sinomenine Hydrochloride inhibits the production of inflammatory mediators, blocks sodium channels, and regulates immune cell activity, exerting anti-inflammatory, immunosuppressive, and analgesic effects [2-3]. Sinomenine Hydrochloride is primarily used to treat autoimmune and inflammatory diseases such as rheumatoid arthritis and osteoarthritis [4].
In HepG2 cells, Sinomenine Hydrochloride (0.5-2μM; 24-72h) significantly inhibits cell growth in a concentration- and time-dependent manner [5]. In MDA-MB-231 cells, Sinomenine Hydrochloride (0-5μM; 48h) inhibits the viability of human breast cancer cells [6]. In ACHN and 786-O cells, Sinomenine Hydrochloride (0-100μM; 24-72h) treatment suppresses the proliferation of ccRCC cells in a dose- and time-dependent manner [7].
In dextran sodium sulfate (DSS) induced colitis mice model, Sinomenine Hydrochloride (20mg/kg, 60mg/kg; ig; 7d) can downregulate the expression levels of Notch1, NICD1, Jagged1, and Hes1 proteins in the colon tissues of colitis mice [8]. In Pb-treated mice model, Sinomenine Hydrochloride (100mg/kg; po; 8 weeks) treatment reduced the levels of liver alanine aminotransferase, aspartate aminotransferase (AST), lactate dehydrogenase (LDH), and MDA [9].
References:
[1]. Jiang S, Li S, Pang S, et al. A systematic review: Sinomenine[J]. Heliyon, 2024, 10(9).
[2]. Jiang W, Fan W, Gao T, et al. Analgesic mechanism of sinomenine against chronic pain[J]. Pain Research and Management, 2020, 2020(1): 1876862.
[3]. Hou W, Huang L, Huang H, et al. Bioactivities and mechanisms of action of sinomenine and its derivatives: a comprehensive review[J]. Molecules, 2024, 29(2): 540.
[4]. Li J, Cao J, Chen Q, et al. Investigating the therapeutic potential of sinomenine in rheumatoid arthritis: anti-inflammatory, antioxidant, and immunomodulatory mechanisms[J]. Naunyn-Schmiedeberg's Archives of Pharmacology, 2024, 397(6): 3945-3958.
[5]. Lu X L, Zeng J, Chen Y L, et al. Sinomenine hydrochloride inhibits human hepatocellular carcinoma cell growth in vitro and in vivo: Involvement of cell cycle arrest and apoptosis induction[J]. International journal of oncology, 2013, 42(1): 229-238.
[6]. Li X, Wang K, Ren Y, et al. MAPK signaling mediates sinomenine hydrochloride-induced human breast cancer cell death via both reactive oxygen species-dependent and-independent pathways: an in vitro and in vivo study[J]. Cell death & disease, 2014, 5(7): e1356-e1356.
[7]. Zhao B, Liu L, Mao J, et al. Sinomenine hydrochloride attenuates the proliferation, migration, invasiveness, angiogenesis and epithelial-mesenchymal transition of clear-cell renal cell carcinoma cells via targeting Smad in vitro[J]. Biomedicine & Pharmacotherapy, 2017, 96: 1036-1044.
[8]. Xu L, Liu W, Huang X, et al. Sinomenine hydrochloride improves DSS-induced colitis in mice through inhibition of the Notch signaling pathway[J]. BMC gastroenterology, 2024, 24(1): 451.
[9]. Li Y, Cai W, Ai Z, et al. Protective effects of sinomenine hydrochloride on lead-induced oxidative stress, inflammation, and apoptosis in mouse liver[J]. Environmental Science and Pollution Research, 2023, 30(3): 7510-7521.
Sinomenine Hydrochloride是NF-κB活化的抑制剂 [1]。Sinomenine Hydrochloride能够抑制炎症介质的产生,阻断钠通道,调节免疫细胞活性,发挥抗炎、免疫抑制和镇痛作用 [2-3]。Sinomenine Hydrochloride主要用于治疗自身免疫性疾病和炎症性疾病,例如类风湿性关节炎和骨关节炎 [4]。
在HepG2细胞中,Sinomenine Hydrochloride(0.5-2μM;24-72h)以浓度和时间依赖性方式显著抑制细胞生长 [5]。在MDA-MB-231细胞中,Sinomenine Hydrochloride(0-5μM;48h)可抑制人乳腺癌细胞的活力 [6]。在ACHN和786-O细胞中,Sinomenine Hydrochloride(0-100μM;24-72h)处理以剂量和时间依赖性方式抑制ccRCC细胞的增殖 [7]。
在葡聚糖硫酸钠(DSS)诱导的结肠炎小鼠模型中,Sinomenine Hydrochloride(20mg/kg,60mg/kg;ig;7d)可下调结肠炎小鼠结肠组织中Notch1、NICD1、Jagged1和Hes1蛋白的表达水平 [8]。在铅处理的小鼠模型中,Sinomenine Hydrochloride(100mg/kg;po;8周)治疗可降低肝脏丙氨酸氨基转移酶、天冬氨酸氨基转移酶(AST)、乳酸脱氢酶(LDH)和丙二醛(MDA)的水平 [9]。
Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | Exponentially growing cells were trypsinized, seeded at an initial density of 8×103 per well in 96-well plates and incubated in standard growth medium for 24h prior to being subjected to different treatments for the indicated periods of time. Cells were subsequently incubated in medium containing MTT (0.5mg/mL) for an additional 4h. The supernatant was removed and 150μL DMSO were added to each well to dissolve the intracellular formazan compound. The absorbance was measured with an ELISA reader at 490nm. The relative cell viability (%) was calculated as the percentage between Sinomenine Hydrochloride-treated cells and the untreated controls. |
Reaction Conditions | 0.5-2μM; 24-72h |
Applications | Sinomenine Hydrochloride significantly inhibits cell growth in a concentration- and time-dependent manner. |
Animal experiment [2]: | |
Animal models | Dextran sodium sulfate (DSS) induced colitis mice model |
Preparation Method | Twenty‐four mice (weight, 20–22g) were randomly divided into four groups: the normal control group (treatment with water) (Normal, n = 6), the model group (Model, n = 6), the Sinomenine Hydrochloride low dose treatment group (SH-20, n = 6), and the Sinomenine Hydrochloride high dose treatment group (SH-60, n = 6). In this experiment, by referring to the previous experimental results and the study of GAO T, two concentration gradients of low dose (20mg/kg) and high dose (60mg/kg) were finally selected to study SH treatment of DSS induced colitis in mice. Except for the normal control group, the remaining three groups of mice drank 4% DSS freely every day for 7 days and replaced the 4% DSS solution every two days. At the same time, the normal control group and the model group were administered 0.2mL of water by oral gavage every day, and the SH low dose and high dose groups were administered with 20mg/kg and 60mg/kg of drugs dissolved in 0.2mL of pure water by oral gavage, respectively. The mice were given intragastric administration once a day for 7 consecutive days. After the end of intragastric administration on the 7th day, all mice were killed on the 8th day, and corresponding blood samples and colon samples were collected. |
Dosage form | 20mg/kg, 60mg/kg; ig; 7d |
Applications | Sinomenine Hydrochloride can downregulate the expression levels of Notch1, NICD1, Jagged1, and Hes1 proteins in the colon tissues of colitis mice. |
References: |
Cas No. | 6080-33-7 | SDF | |
别名 | 盐酸青藤碱; Cucoline hydrochloride | ||
Canonical SMILES | CN1CCC23CC(=O)C(=CC2C1CC4=C3C(=C(C=C4)OC)O)OC.Cl | ||
分子式 | C19H24ClNO4 | 分子量 | 365.85 |
溶解度 | ≥ 14.7mg/mL in DMSO | 储存条件 | Store at 2-8°C |
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1 mg | 5 mg | 10 mg |
1 mM | 2.7334 mL | 13.6668 mL | 27.3336 mL |
5 mM | 0.5467 mL | 2.7334 mL | 5.4667 mL |
10 mM | 0.2733 mL | 1.3667 mL | 2.7334 mL |
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