紫草素作用機制 - Medchemexpress - MCE中國

1、Product Data SheetShikoninCat. No.: HY-N0822CAS No.: 517-89-5分式: CHO分量: 288.3作靶點: Chloride Channel; Pyruvate Kinase; NF-B; TNF Receptor; HIV作通路: Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; NF-B;Apoptosis; Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1

2、 month溶解性數(shù)據(jù)體外實驗 DMSO : 31 mg/mL (107.53 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 3.4686 mL 17.3430 mL 34.6861 mL5 mM 0.6937 mL 3.4686 mL 6.9372 mL10 mM 0.3469 mL 1.7343 mL 3.4686 mL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；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。儲備液的保存式和期限：-80

3、C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 0.5% CMC-Na/saline water2.Solubility: 30 mg/mL

4、(104.06 mM); Suspended solution; Need ultrasonic請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (7.21 mM); Clear solution此案可獲得 2.08 mg/mL (7.21 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲備液加到 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

5、。Page 1 of 2 www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (7.21 mM); Clear solution此案可獲得 2.08 mg/mL (7.21 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Shikonin中草藥紫草的主 成分。Shikonin 種有效的 TMEM16A 氯化物通道 (chlo

6、ride channel) 抑制劑，IC50 為6.5 M。Shikonin 種特異的丙酮酸激酶 M2 (PKM2) 抑制劑，還可以抑制 TNF- 和 NF-B途徑。IC & Target NF-B TNF- TMEM16A chloride PKM2channel6.5 M (IC50)體外研究 Shikonin is an inhibitor of TMEM16A chloride channel with an IC50 of 6.5 M1. Shikonin is also a specific inhibitor ofPKM22 and can also inhibit tumor

7、necrosis factor- (TNF-) and prevent activation of nuclear factor-B (NF-B)pathway. Shikonin at concentrations higher than 50 M significantly inhibits ormal human keratinocytes (NHKs)viability, compare with that of control (P0.05). Pretreatment with Shikonin for 2 h attenuates TNF-induced NF-Bp65 nucl

8、ear translocation3. Treatments of Shikonin at 5 and 7.5 M significantly inhibit the cell viability starting from12 h and the inhibitory effects are presented in time-dependent patterns compare with the 0 h group in both celllines. It is found that 5 M Shikonin displays greater inhibition compare to

9、2.5 M at the time points from 24 to 48 h.The invasiveness of U87 and U251 cells is significantly attenuated when treated with Shikonin at 2.5, 5, and 7.5 Mcompare with the control group at 24 and 48 h (p0.01)4.體內(nèi)研究 Shikonin significantly inhibits the increase in IL-1 and TNF- expression levels in th

10、e rat model of osteoarthritis,compare with those in the osteoarthritis group (P0.01). The NF-B protein expression level is significantlysuppressed by Shikonin in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P0.01). Theinduction of the iNOS level is suppressed by tr

11、eatment with Shikonin in the rat model of osteoarthritis, compare withthat in the osteoarthritis group (P0.01). The administration of Shikonin markedly weakens the up-regulation of COX-2 protein expression in the rat model of osteoarthritis, as compare with that in the osteoarthritis group (P0.01).

12、Theelevation of caspase-3 activity is significantly reduced by Shikonin treatment in the rat model of osteoarthritis,compare with that in the osteoarthritis group (P0.01). The downregulation of Akt phosphorylation is alsosignificantly recovered by treatment with Shikonin in the rat model of osteoart

13、hritis, compare with that in theosteoarthritis group (P0.01)5.PROTOCOLCell Assay 4 U87 and U251 cells are seeded into 96-well plates at a density of 1104 cells per well in standard DMEM andincubated for 24 h under standard conditions (37C and 5% CO2). Then the medium is replaced with either blank,se

14、rum-free DMEM or DMEM containing Shikonin at concentrations of 2.5, 5, and 7.5 M. The total volume in eachwell is 200 L. Finally, the plates are shaken softly and the optical density is recorded at 570 nm (OD570) using a platereader. At least three independent experiments are performed4.MCE has not

15、independently confirmed the accuracy of these methods. They are for reference only.Animal Healthy male Sprague-Dawley rats (n=30; 8 to 10-weeks old, 250 to 300 g) are used in this study. Rats are randomlyAdministration 5 assigned to three groups: Sham-operated group (n=10), osteoarthritis model grou

16、p (n=10) and Shikonin-treatedgroup (n=10). In the sham-operated group, the right knee joint of the anesthetized rat is only exposed under sterilePage 2 of 3 www.MedChemEconditions, and the rats are treated with 0.1 ml/100 g physiological saline (i.p.). In the osteoarthritis model group,osteoarthriti

17、s model rats were treated with 0.1 ml/100 g physiological saline (i.p.). In the Shikonin-treated group,osteoarthritis model rats are treated with 10 mg/kg Shikonin (i.p.) once daily for 4 days after osteoarthritis modeling5.MCE has not independently confirmed the accuracy of these methods. They are

18、for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Int J Biochem Cell Biol. 2018 Mar;96:9-19. J Chemother. 2019 Jul;31(4):214-226.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Jiang Y et al. Shikonin Inhibits Intestinal Calcium-Activated Chloride Channels and Prevents Rotaviral Diarrh

19、ea. Front Pharmacol. 2016 Aug 23;7:270.2. Li W, et al. Shikonin Suppresses Skin Carcinogenesis via Inhibiting Cell Proliferation. PLoS One. 2015 May 11;10(5):e0126459.3. Yan Y, et al. Shikonin Promotes Skin Cell Proliferation and Inhibits Nuclear Factor-B Translocation via Proteasome Inhibition In Vitro. Chin Med J (Engl).2015 Aug 20;128(16):2228-33.4. Zhang FY, et al. Shikonin Inhibits the Migration and Invasion of Huma