毛蕊花糖苷作用机制 - Medchemexpress - MCE中国

1、Product Data SheetVerbascosideCat. No.: HY-N0021CAS No.: 61276-17-3分式: CHO分量: 624.59作靶点: PKC; Apoptosis; Bacterial; HSV作通路: Epigenetics; TGF-beta/Smad; Apoptosis; Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (160.11 mM)* means soluble

2、, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 1.6011 mL 8.0053 mL 16.0105 mL5 mM 0.3202 mL 1.6011 mL 3.2021 mL10 mM 0.1601 mL 0.8005 mL 1.6011 mL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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1

3、个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.33 mM); Clear solution此案可获得 2.08 mg/mL

4、 (3.33 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.33 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.08 mg/mL (3.33 mM，饱和度未知) 的澄清溶液。以 1

5、mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.33 mM); Clear solution此案可获得 2.08 mg/mL (3.33 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Verbas

6、coside是从 Lantana camara 中得到的糖苷类物质，为 ATP 竞争性的 PKC 抑制剂，IC50 值为 25 M，具有抗肿瘤，抗炎，抗神经性疼痛等作。IC & Target PKC25 M (IC50)体外研究 Verbascoside acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 M. Verbascoside shows Kis of 22 and 28M with respect to ATP and histone, respectively. Verbascoside has pote

7、nt antitumor activity against L-1210 cells,with an IC50 of 13 M1. Verbascoside (5, 10 M) suppresses 2,4-dinitrochlorobenzene (DNCB)-induced T cellcostimulatory factors CD86 and CD54, proinflammatory cytokines, and NFB pathway activation in THP-1 cells2.体内研究 Verbascoside (1%) reduces the overall scra

8、tching behavior incidence as well as the severity of the skin lesions in 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis (AD) mice model. Verbascoside also blocks DNCB-induced expression of proinflammatory cytokine TNF-, IL-6, and IL-4 mRNA in skin lesions2. Verbascoside (50, 100 mg/kg,i.p

9、.) does not modify chronic constriction injury (CCI)-induced cold allodynia. Verbascoside (200 mg/kg, i.p.) decreaseshyper-sensitivity to cold stimulus, acetone, on day 3 in rats. Verbascoside also significantly reduces behavioralchanges associated with neuropathy. Moreover, Verbascoside decreases B

10、ax and increases Bcl-2 on day 33.PROTOCOLCell Assay 1 The lymphocytic mouse leukemia L1210 cells (ATCC, CCL 219) are plated sparsely at 104 cells per well in 24-wellcluster plates in Dulbeccos modified Eagle medium containing 10% fetal calf serum, 4 mM glutamine, 100 U/mLpenicillin, 100 g/mL strepto

11、mycin sulfate, and Verbascoside (solubilized in DMSO). After a 2-day incubation periodat 37C in a humidified atmosphere (5% CO2 in air), growth is monitored by counting cell numbers in a Coulter-counter. IC50 values are calculated on the basis of the linear regression lines established for each comp

12、ound tested1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats2Administration 2 To induce atopic dermatitis (AD)-like symptoms, 2,4-dinitrochlorobenzene (DNCB) is used. Briefly, the dorsal hair ofthe mice is removed using an electronic clipper

13、 2 days before DNCB treatment. An application of 200 L of 1% DNCB(in acetone:olive oil = 4:1) is made to the shaved dorsal skin for sensitization. The repeated challenge is performed onthe same site with 0.2% DNCB once every 3 days for about 2 weeks. The mice are divided into 4 groups (n = 6 pergrou

14、p): (1) vehicle-treated controls, (2) DNCB-treated only, (3) 1% Verbascoside (in acetone:olive oil 4:1)-treatedonly, and (4) DNCB + 1% Verbascoside-treated group2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemEREFERENCES1. Herbe

15、rt JM, et al. Verbascoside isolated from Lantana camara, an inhibitor of protein kinase C. J Nat Prod. 1991 Nov-Dec;54(6):1595-600.2. Li Y, et al. Verbascoside Alleviates Atopic Dermatitis-Like Symptoms in Mice via Its Potent Anti-Inflammatory Effect. Int Arch Allergy Immunol.2018;175(4):220-230.3. Amin B, et al. The Effect of Verbascoside in Neuropathic Pain Induced by Chronic Constriction Injury in Rats. Phytother Res. 2016 Jan;30