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]。