Sinapine thiocyanate
(Synonyms: 芥子碱硫氰酸盐) 目录号 : GC30033
Sinapine thiocyanate is the thiocyanate salt form of Sinapine, which shows favorable biological activities such as antioxidant and radio-protective activities.
Cas No.:7431-77-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment: |
The Caco-2 cells are seeded into a 96-well plate with 8000 cells/well for 24 h. After incubation with different doses of Sinapine (0-200 μM), doxorubicin, or both for 24 h, the medium is discarded. Cell survival after exposure to Sinapine alone or a combination of Sinapine and the anti-tumor agent doxorubicin is examined by MTT colorimetric assay[1]. |
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Animal experiment: |
Rats[3]Sixty male Sprague-Dawley rats (95 g) are randomly allotted to 6 groups of 10 rats each and reared in individual cages. Six groups of 10 growing rats each are fed ad libitum for 15 days one of six diets: diet A, rapeseed (3.80 g of sinapine/kg DM); diet B, ethanol/water-extracted rapeseed (0.48 g of sinapine); diet C, control diet; diet G, control diet+3.74 g of extracted sinapine; diet H, control diet + 3.72 g of sinapine+other phenolic compounds; or diet I, control diet+the hydrolysis products of sinapine and other phenolic compounds. The rats are weighed at 8 a.m. on days 1, 4, 8, 11 and 15 of the trial. After sacrifice the gut contents are eliminated to permit determination of empty body weight gain (EBWG). The distribution, refusal and intake of each rat are recorded every day[3]. |
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References: [1]. Guo Y, et al. Sinapine as an active compound for inhibiting the proliferation of Caco-2 cells via downregulation of P-glycoprotein. Food Chem Toxicol. 2014 May;67:187-92. |
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Sinapine thiocyanate is the thiocyanate salt form of Sinapine, which shows favorable biological activities such as antioxidant and radio-protective activities.
| Cas No. | 7431-77-8 | SDF | |
| 别名 | 芥子碱硫氰酸盐 | ||
| Canonical SMILES | COC1=C(O)C(OC)=CC(C=CC(OCC[N+](C)(C)C)=O)=C1.N#C[S-] | ||
| 分子式 | C17H24N2O5S | 分子量 | 368.45 |
| 溶解度 | DMSO : ≥ 125 mg/mL (339.26 mM) | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7141 mL | 13.5704 mL | 27.1407 mL |
| 5 mM | 0.5428 mL | 2.7141 mL | 5.4281 mL |
| 10 mM | 0.2714 mL | 1.357 mL | 2.7141 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Sinapine thiocyanate Inhibits the Proliferation and Mobility of Pancreatic Cancer Cells by Up-Regulating GADD45A
J Cancer 2022 Jan 24;13(4):1229-1240.35281859 PMC8899366
Background: Sinapine thiocyanate (ST), an alkaloid isolated from the seeds of cruciferous species, has exhibited anti-inflammatory, anti-malignancy, and anti-angiogenic effects in previous studies. However, the effects and molecular mechanisms of action of ST in pancreatic cancer (PC) are still limited. Materials and methods: PC cells were treated with different concentrations (0, 20, 40, and 80 μM) of ST. The proliferative ability of PC cells in vitro was determined using cell count kit-8 (CCK-8), 5-ethynyl-2' deoxyuridine, colony formation, and flow cytometry assays. The mobility of PC cells in vitro was analyzed using wound healing assay, transwell assay, Western blotting, and immunofluorescence. High-throughput sequencing followed by bioinformatics analysis, reverse-transcriptase quantitative polymerase chain reaction (RT-qPCR), and Western blotting were performed to identify the key targets of ST. Finally, CCK-8 assay, wound healing assay, and xenograft tumor model were used to determine the relationship between ST and growth arrest and DNA damage-inducible alpha (GADD45A; the key target of ST) and malignant biological properties of PC in vitro and in vivo. Results: ST significantly repressed the PC cell proliferation rate and colony formation in vitro and arrested cells in the G2/M phase. ST inhibited PC cell mobility in vitro and increased E-cadherin expression (an epithelial biomarker). GADD45A was considered the key target of ST in PC and was elevated in PC cells treated with ST. The inhibition of GADD45A significantly alleviated the suppressive effects of ST on PC cell proliferation and mobility in vitro. ST suppressed PC cell proliferation in vivo and increased GADD45A expression in tumor tissues. Conclusion: ST exhibited significant anti-tumor effects on PC cells by upregulating GADD45A. ST may be a potential drug for PC treatment.
Transdermal delivery of Sinapine thiocyanate by gelatin microspheres and hyaluronic acid microneedles for allergic asthma in guinea pigs
Int J Pharm 2022 Jul 25;623:121899.35710072 10.1016/j.ijpharm.2022.121899
Dissolving microneedles (MNs) are an efficient, safe, and generally painless method for transdermal distribution of poorly permeable medicines. Here, dissolving composite MNs were prepared from Sinapine thiocyanate (ST)-loaded gelatin microspheres (GMS) and hyaluronic acid (HA). To immobilize ST in MNs, we used a two-step centrifuging and molding method. When ST-GMS/ST-HA MNs were placed on the skin, they showed extraordinary mechanical strength and dissolved slowly. In vitro, skin implantation ability was assessed with fluorescein isothiocyanate staining, which revealed progressive penetration from the puncture site into deeper tissues. The feasibility of transdermal delivery of ST-GMS/ST-HA MNs in allergic asthma guinea pigs was then determined through in vivo pharmacodynamic and pharmacokinetic tests. The results indicated that ST-GMS/ST-HA MNs, in comparison with the traditional subcutaneous application approach, achieved both high efficiency and continuous release of ST. Therefore, this device is promising for the delivery ST for allergic asthma therapy.
Sinapine thiocyanate Ameliorates Vascular Endothelial Dysfunction in Hypertension by Inhibiting Activation of the NLRP3 Inflammasome
Front Pharmacol 2021 Feb 9;11:620159.33633569 PMC7901921
The increase of blood pressure is accompanied by the changes in the morphology and function of vascular endothelial cells. Vascular endothelial injury and hypertension actually interact as both cause and effect. A large number of studies have proved that inflammation plays a significant role in the occurrence and development of hypertension, but the potential mechanism between inflammation and hypertensive endothelial injury is still ambiguous. The purpose of this study was to explore the association between the activation of NLRP3 inflammasome and hypertensive endothelial damage, and to demonstrate the protective effect of Sinapine thiocyanate (ST) on endothelia in hypertension. The expression of NLRP3 gene was silenced by tail vein injection of adeno-associated virus (AAVs) in spontaneously hypertensive rats (SHRs), indicating that activation of NLRP3 inflammasome accelerated hypertensive endothelial injury. ST not only protected vascular endothelial function in SHRs by inhibiting the activation of NLRP3 inflammasome and the expression of related inflammatory mediators, but also improved AngII-induced huvec injury. In summary, our results show that alleviative NLRP3 inflammasome activation attenuates hypertensive endothelial damage and ST ameliorates vascular endothelial dysfunction in hypertension via inhibiting activation of the NLRP3 inflammasome.
Metabolic profiling and pharmacokinetic studies of Sinapine thiocyanate by UHPLC-Q/TOF-MS and UHPLC-MS/MS
J Pharm Biomed Anal 2022 Jan 5;207:114431.34710728 10.1016/j.jpba.2021.114431
Sinapine thiocyanate (ST) is an index component and pharmacological active component of Semen Sinapis and Semen Raphani, and it is widely used to relieving cough and asthma. This study aimed to obtain the metabolic and pharmacokinetic characterization of ST. The metabolic profiles of ST were obtained from rat plasma, urine, and feces via ultra-performance liquid chromatography-quadrupole-time-of-flight mass spectrometry (UHPLC-Q/TOF-MS). Thirteen metabolites were structurally identified, and the proposed metabolic pathways of ST included deamination, demethylation, hydrogenation, dehydration, and extensive conjugation, including glucuronidation and sulfonation. ST was selected as the plasma marker for the pharmacokinetic study. A simple and sensitive ultra-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was developed for the quantitation of ST in rat plasma. The linear range of ST was 0.1-500 ng/mL (R2 = 0.9976), and the lowest limit of quantification was 0.1 ng/mL. The intra-precision and inter-precision of the assay were 1.31-5.12% and 2.72-7.66%, and the accuracy (RE%) ranged from - 4.88% to 3.82% and - 3.47% to 6.18%. The extraction recovery, matrix effect, and stability of ST were within acceptable limits. The established method was validated and successfully applied to the pharmacokinetic study of ST. For pharmacokinetic experiments, the male Sprague-Dawley rats were administrated with ST solution intravenously (2 mg/kg) or orally (100 mg/kg). The oral absolute bioavailability of ST was calculated as 1.84%, and the apparent volume of distribution of intravenous and intragastric administrations were 107.51 ± 21.16 L/kg and 78.60 ± 14.44 L/kg, respectively. The maximum plasma concentration was 47.82 ± 18.77 nM, and the time to maximum peak was 88.74 ± 20.08 min for the intragastric dosing group. According to the pharmacokinetic and metabolic profiling results, metabolites with high abundance of ST in bio-fluids would be the next object in tissue distribution and pharmacodynamic study.
Effect of stimulating the acupoints Feishu (BL 13) and Dazhui (GV 14) on transdermal uptake of Sinapine thiocyanate in asthma gel
J Tradit Chin Med 2017 Aug;37(4):503-509.32188209
Objective: To investigate the effect of stimulating the acupoints Feishu (BL 13) and Dazhui (GV 14) on the transdermal uptake of Sinapine thiocyanate contained in a gel used for the management of asthma. Methods: Thirty Sprague-Dawley rats were randomly divided into three equal groups using a random number table: the Feishu (BL 13) acupoint group, the Dazhui (GV 14) acupoint group, and the nonacupoint group or control group. Using microdialysis technology, preprocessed skin probes were implanted into the rats at Feishu (BL 13), Dazhui (GV 14), and a nonacupoint site. Asthma gel was then placed on the skin at Feishu (BL 13), Dazhui (GV 14) acupoints, and the nonacupoint for all groups. Dialysate was collected every 30 min for 12 h. The normalized concentration of Sinapine thiocyanate in the skin was determined by high-performance liquid chromatography. Results: The rat in vivo transdermal experiment demonstrated that the quantity-time equation showed a good linear correlation with zero-order kinetics (r > 0.99). The transdermal behavior was in accordance with the first-order rate open model in which the transdermal penetration rates and the accumulative amounts of Sinapine thiocyanate in the skin at the acupoint sites were greater than those through the skin of the nonacupoint site. The systemic maximum concentration and the area under the curve of Sinapine thiocyanate in the acupoint groups were significantly greater than in the nonacupoint group. A lag time was observed in both acupoint groups, but not in the nonacupoint group. Conclusion: Stimulating the acupoints promotes the percutaneous absorption of Sinapine thiocyanate and also controls its release, reducing concentration fluctuations in the blood.