Verbascoside是一种从Lantana camara中分离得到的蛋白激酶C（PKC）抑制剂，IC50值为25µM。
Cas No.:61276-17-3
Sample solution is provided at 25 µL, 10mM.
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Verbascoside is an inhibitor of protein kinase C (PKC) isolated from Lantana camara, with an IC50 value of 25µM [1]. Verbascoside can down-regulate the expression of TRPV3 Ca2+-dependent temperature-sensitive channel and inhibit the TAK-1/JNK/AP-1 pathway by phosphorylating SHP-1, thereby exerting anti-inflammatory effects [2]. Verbascoside has been widely used to improve the histological morphology and clinical symptoms of animal colitis and to prevent skin damage caused by ultraviolet radiation[3].
In vitro, Verbascoside treatment for 24 hours significantly inhibited the cell viability of MCF-7 cells and MDA-MB 231 cells, with IC50 values of 0.1270µM and 0.1597µM, respectively[4]. 100µM of Verbascoside pretreatment for 3 hours protected C6 cells from LPS/IFN-γ-induced cell death and inhibited the increase in lipid peroxidation levels[5]. Treatment with 16µM Verbascoside for 5 days significantly enhanced the cell viability of human β cells under endoplasmic reticulum stress conditions, regulated redox homeostasis and improved mitochondrial function[6].
In vivo, Verbascoside treatment via oral administration at a dose of 10mg/kg/day for 42 days improved the memory and spatial cognition abilities of APP/PS1 mice, and reduced the Aβ deposition and tau protein accumulation in the brain tissues[7]. Oral administration of a 60mg/kg dose of Verbascoside daily for 12 weeks significantly inhibited the atherosclerotic pathological progression in ApoE−/− mice fed with a high-fat diet, and improved liver lipid metabolism[8].
References:
[1] Herbert J M, Maffrand J P, Taoubi K, et al. Verbascoside isolated from Lantana camara, an inhibitor of protein kinase C[J]. Journal of Natural Products, 1991, 54(6): 1595-1600.
[2] Saha R, Majie A, Baidya R, et al. Verbascoside: comprehensive review of a phenylethanoid macromolecule and its journey from nature to bench[J]. Inflammopharmacology, 2024, 32(5): 2729-2751.
[3] Alipieva K, Korkina L, Orhan I E, et al. Verbascoside—A review of its occurrence,(bio) synthesis and pharmacological significance[J]. Biotechnology advances, 2014, 32(6): 1065-1076.
[4] Şenol H, Tulay P, Ergören M C, et al. Cytotoxic Effects of Verbascoside on MCF-7 and MDA-MB-231[J]. Turkish Journal of Pharmaceutical Sciences, 2021, 18(5): 637.
[5] Esposito E, Dal Toso R, Pressi G, et al. Protective effect of verbascoside in activated C6 glioma cells: possible molecular mechanisms[J]. Naunyn-Schmiedeberg's archives of pharmacology, 2010, 381(1): 93-105.
[6] Galli A, Marciani P, Marku A, et al. Verbascoside protects pancreatic β-cells against ER-stress[J]. Biomedicines, 2020, 8(12): 582.
[7] Wang C, Cai X, Wang R, et al. Neuroprotective effects of verbascoside against Alzheimer’s disease via the relief of endoplasmic reticulum stress in Aβ-exposed U251 cells and APP/PS1 mice[J]. Journal of Neuroinflammation, 2020, 17(1): 309.
[8] Lei P, Lü J, Yao T, et al. Verbascoside exerts an anti-atherosclerotic effect by regulating liver glycerophospholipid metabolism[J]. Food Science and Human Wellness, 2023, 12(6): 2314-2323.
Verbascoside是一种从Lantana camara中分离得到的蛋白激酶C（PKC）抑制剂，IC50值为25µM[1]。Verbascoside可下调TRPV3钙离子依赖性温度敏感通道的表达，并通过磷酸化SHP-1来抑制TAK-1/JNK/AP-1通路，从而发挥抗炎作用[2]。Verbascoside已被广泛用于改善动物结肠炎的组织形态和临床症状，并预防紫外线辐射引起的皮肤损伤[3]。
在体外，Verbascoside处理MCF-7细胞和MDA-MB 231细胞24小时，显著抑制了细胞活力，IC50值分别为0.1270µM和0.1597µM[4]。100µM的Verbascoside预处理C6细胞3小时，可保护细胞免受LPS/IFN-γ诱导的细胞死亡，并抑制脂质过氧化水平的升高[5]。16µM的Verbascoside处理人类β细胞5天，在内质网应激条件下显著增强了细胞活力，调节了氧化还原稳态并改善了线粒体功能[6]。
在体内，每日口服10mg/kg剂量的Verbascoside，连续42天，改善了APP/PS1小鼠的记忆和空间认知能力，并减少了脑组织中Aβ沉积和tau蛋白积累[7]。每日口服60mg/kg剂量的Verbascoside，连续12周，显著抑制了高脂饮食喂养的ApoE−/−小鼠的动脉粥样硬化病理进展，并改善了肝脏脂质代谢[8]。
| Cell experiment [1]: | |
Cell lines | MCF-7 cells |
Preparation Method | MCF-7 cells were seeded onto 96-well flat-bottomed microculture plates at a density of 5×103 cells/well in DMEM/F-12 medium supplemented with 10% fetal bovine serum, insulin at 4mg/ml, penicillin, and streptomycin (1%) at 37°C, in a 5% CO2 containing humidified chamber. The cells were allowed to adhere to the plates and were treated with various concentrations of Verbascoside (0.1, 0.5, 1, 10, 25, 50, and 100μM) for 24h, and the cell viability was measured. |
Reaction Conditions | 0.1, 0.5, 1, 10, 25, 50, and 100μM; 24h |
Applications | Verbascoside treatment significantly enhanced the cell viability of MCF-7 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | APP/PS1 mice |
Preparation Method | APP/PS1 mice (8 weeks old; 40.7-52.9g) were housed in a room with controlled temperature (21-23°C), humidity (40-60%), and lighting (12h light/dark cycle) and were supplied with water. Mice were randomly divided into two groups and given 0.4ml of normal saline (n=12) or 10mg/kg/day of Verbascoside (n=12) orally for 42 days. After the entire 42-day treatment period, all of the mice were euthanized via intraperitoneal injection of sodium pentobarbital (150mg/kg). Collect the brain tissues of mice for analysis. |
Dosage form | 10mg/kg/day for 42 days; p.o. |
Applications | Verbascoside treatment reduced the Aβ deposition and tau protein accumulation within the brain in APP/PS1 mice. |
References: | |
| Cas No. | 61276-17-3 | SDF | |
| 别名 | 麦角甾苷; Acteoside; Kusaginin; TJC160 | ||
| 化学名 | [(2R,3R,4R,5R,6R)-6-[2-(3,4-dihydroxyphenyl)ethoxy]-5-hydroxy-2-(hydroxymethyl)-4-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxyoxan-3-yl] (E)-3-(3,4-dihydroxyphenyl)prop-2-enoate | ||
| Canonical SMILES | CC1C(C(C(C(O1)OC2C(C(OC(C2OC(=O)C=CC3=CC(=C(C=C3)O)O)CO)OCCC4=CC(=C(C=C4)O)O)O)O)O)O | ||
| 分子式 | C29H36O15 | 分子量 | 624.59 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6011 mL | 8.0053 mL | 16.0105 mL |
| 5 mM | 320.2 μL | 1.6011 mL | 3.2021 mL |
| 10 mM | 160.1 μL | 800.5 μL | 1.6011 mL |
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动物数量 | 只 |
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