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金丝桃苷在皮肤癌中具有强大的抗癌活性。

Hyperoside exerts potent anticancer activity in skin cancer.

机构信息

Department of Dermatology, The Affiliated Huaian No. 1 People\'s Hospital of Nanjing Medical University, Huai\'an, Jiangsu 223300 P.R. China.

Department of Orthopaedics, The Affiliated Huaian No. 1 People's Hospital of Nanjing Medical University, Huai'an, Jiangsu 223300 P.R. China,

出版信息

Front Biosci (Landmark Ed). 2020 Jan 1;25(3):463-479. doi: 10.2741/4814.

Abstract

Quercetin-3-O-β-D-galactopyranoside, is a hyperoside flavonol glycoside with anti-cancer, anti-inflammatory, and anti-oxidant activities that is derived from Hypericum and Crataegus plants. To this end, we examined the effect of this hyperoside in skin cancer cells lines and in DMBA/TPA induced skin tumors . treatment of cancer cells with hyperoside significantly inhibited phosphoinositide 3-kinase (PI3K)/protein kinase B (Akt)/mammalian target of rapamycin (mTOR)/p38 MAPK axis, concomitantly activated the 5'AMP-activated protein kinase (AMPK) signaling, inhibited proliferation, and induced apoptosis and autophagy. Hyperoside markedly inhibited diffuse epidermal hyperplasia and significantly reduced the changes in phosphorylated levels of PI3K, AKT, mTOR and AMPK while reducing p38 phosphorylation as well as of tumor burden in DMBA/TPA induced skin tumors. These data suggest that hyperoside might be of therapeutic value in chemoprevention of skin cancer.

摘要

槲皮素-3-O-β-D-半乳糖苷是一种具有抗癌、抗炎和抗氧化活性的金丝桃苷类黄酮糖苷,来源于贯叶连翘和山楂属植物。为此,我们研究了这种金丝桃苷在皮肤癌细胞系和 DMBA/TPA 诱导的皮肤肿瘤中的作用。金丝桃苷处理癌细胞显著抑制了磷脂酰肌醇 3-激酶 (PI3K)/蛋白激酶 B (Akt)/哺乳动物雷帕霉素靶蛋白 (mTOR)/p38 MAPK 轴,同时激活了 5'AMP 激活的蛋白激酶 (AMPK)信号通路,抑制了增殖,并诱导了细胞凋亡和自噬。金丝桃苷显著抑制了弥漫性表皮增生,并显著降低了 DMBA/TPA 诱导的皮肤肿瘤中磷酸化 PI3K、AKT、mTOR 和 AMPK 水平的变化,同时降低了 p38 磷酸化和肿瘤负担。这些数据表明,金丝桃苷在皮肤癌的化学预防中可能具有治疗价值。

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