鹽酸白屈菜紅堿作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetChelerythrine chlorideCat. No.: HY-12048CAS No.: 3895-92-9分式: CHClNO分量: 383.82作靶點(diǎn): PKC; Bcl-2 Family; Apoptosis; Autophagy作通路: Epigenetics; TGF-beta/Smad; Apoptosis; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 4.35 mg/mL (11.33 mM

2、; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 2.6054 mL 13.0269 mL 26.0539 mL5 mM 0.5211 mL 2.6054 mL 5.2108 mL10 mM 0.2605 mL 1.3027 mL 2.6054 mL請(qǐng)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(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)

3、實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.43 mg/mL (1.12 mM); Clear solution此案可獲得 0.43 mg/mL (1.12

4、 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 4.3 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.44 mg/mL (1.15 mM); Clear solution此案可獲得 0.44 mg/mL (1.15 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例

5、，取 100 L 4.4 mg/mL 的澄均勻。DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 0.44 mg/mL (1.15 mM); Clear solution此案可獲得 0.44 mg/mL (1.15 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 4.4 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Chelerythrine ch

6、loride 種有效，可滲透細(xì)胞的蛋酶 C (protein kinase C) 抑制劑，能夠抑制 PKC 活性，IC50 值為 660 nM。Chelerythrine chloride 抑制 Bcl-XL-Bak BH3 肽結(jié)合，IC50 為 1.5 M，并從 Bcl-XL 取代了 Bax。 Chelerythrine chloride 誘導(dǎo)細(xì)胞凋亡 (apoptosis) 和噬 (autophagy)。IC & Target PKC PKA TPK660 nM (IC50) 0.17 mM (IC50) 0.1 mM (IC50)體外研究 Chelerythrine inhibits t

7、he BclXL-Bak BH3 peptide binding with IC50 of 1.5 M and displaces Bax, a BH3-containingprotein, from BclXL. Mammalian cells treated with Chelerythrine undergoes apoptosis with characteristic features thatsuggest involvement of the mitochondrial pathway1. Chelerythrine treatment inhibits LPS-induced

8、TNF- level andNO production in LPS-induced murine peritoneal macrophages through selective inhibition of p38 mitogen-activatedprotein kinase (MAPK) and extracellular signal-regulated protein kinases 1 and 2 (ERK1/2) activation. Moreover, theeffects of chelerythrine on NO and cytokine TNF- production

9、 can possibly be explained by the role of p38 MAPKand ERK1/2 in the regulation of inflammatory mediators expression2. Chelerythrine shows cytotoxic effect on thehuman monocytic leukaemia cells with LD50 value of 3.46 M. Two hours after LPS stimulation, cells influenced bysanguinarine and Chelerythri

10、ne significantly decline the CCL-2 expression by a factors of 3.5 and 1.93. Chelerythrinechloride significantly enhances the phosphorylation of ERK1/2 in a dose-dependent manner. In addition, chelerythrinechloride inhibits the phosphorylation of p384.體內(nèi)研究 Chelerythrine displays significant anti-infl

11、ammatory effects in experimentally induced mice endotoxic shock model invivo through inhibition of LPS-induced tumor necrosis factor-alpha (TNF-) level and nitric oxide (NO) production inserum2. Chelerythrine chloride (5 mg/kg/day, i.p.) induces apoptosis of RCC cells without significant toxicity to

12、 mice.Chelerythrine Chloride treatment leads to a dose-dependent accumulation of p534.PROTOCOLCell Assay 1 Cell viability is evaluated via MTT assay. Cells (2103 HEK-293 cells/well and 3103 SW-839 cells/well) in 100 Lmedium are seeded into 96-well plates, and incubated for 12 h. Next, the medium in

13、each well is replaced withmedium containing various concentrations of Chelerythrine Chloride, and the cells are incubated at 37C for anadditional 24 and 48 h. Subsequently, 20 L MTT (5 mg/mL) is added to each well. Following an additional incubationat 37C for 4 h, the supernatant is removed, and 100

14、 L DMSO is added to each well. The absorbance values (read at540 nm) are determined using the iMark Microplate Absorbance Reader. The data are analyzed using MicroplateManager software (ver. 6.3; 1689520).MCE has not independently confirmed the accuracy of these methods. They are for reference only.

15、Animal A total of 5106 SW-839 cells are mixed with Matrigel, and injected subcutaneously into the flanks of 14 5-week-Administration 1 old male BALB/c nude mice. The mice are maintained in 1830-cm cages containing three mice each, at atemperature of 22C using a 12 h light/dark cycle. Food and water

16、is available ad libitum. The mice are randomLyPage 2 of 3 www.MedChemEdivided into two groups (n=7). As previously described, the mice are administrated with chelerythrine chloride at adose of 5 mg/kg/day via intraperitoneal injection for 5 weeks, with the first injection of chelerythrine chlorideur

17、ring24 h after injection with the SW-839 cells. The control mice are administered with the same volume of PBS containing1% DMSO. The volume and weight of the mouse tumors are measured once a week. All the mice are sacrificed 36days subsequent to inoculation of the cancer cells, when the tumors are r

18、esected.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) FASEB J. 2019 Oct. Sci Rep. 2017 Aug 23;7(1):9201. Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Li W, et al. Effe

19、ct of Chelerythrine Against Endotoxic Shock in Mice and Its Modulation of Inflammatory Mediators in Peritoneal Macrophages Throughthe Modulation of Mitogen-Activated Protein Kinase (MAPK) Pathway. Inflammation. 2012 Jul 24.2. Pencikova K, et al. Investigation of sanguinarine and chelerythrine effects on LPS-induced inflammatory gene expression in THP-1 cell line.Phytomedicine. 2012 Jul 15;19(10):890-5. Epub 2012 May 14.3. Chen XM, et al. Chelerythrine chloride induces apoptosis in renal cancer HEK-293 and SW-839 cell lines. Oncol Lett. 2016 Jun;11(6):3917-39244. Herbert