IMR Press / FBL / Volume 25 / Issue 3 / DOI: 10.2741/4814

Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on imrpress.com as a courtesy and upon agreement with Frontiers in Bioscience.

Article
Hyperoside exerts potent anticancer activity in skin cancer
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1 Department of Dermatology, The Affiliated Huaian No. 1 People's Hospital of Nanjing Medical University, Huai'an, Jiangsu 223300 P.R. China
2 Department of Orthopaedics, The Affiliated Huaian No. 1 People's Hospital of Nanjing Medical University, Huai'an, Jiangsu 223300 P.R. China
Send correspondence to: Pengfei Wu, Department of Orthopaedics, The Affiliated Huaian No. 1 People's Hospital of Nanjing Medical University, Huai'an, Jiangsu 223300 P.R. China, Tel: 86-0517-84922766, Fax: 86-0517-84922766, E-mail: wpfdoctor@yeah.net
Front. Biosci. (Landmark Ed) 2020, 25(3), 463–479; https://doi.org/10.2741/4814
Published: 1 January 2020
(This article belongs to the Special Issue Leader sequences of coronavirus are altered during infection)
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 in vivo. In vitro 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 vivo in DMBA/TPA induced skin tumors. These data suggest that hyperoside might be of therapeutic value in chemoprevention of skin cancer.

Keywords
Hyperoside
Skin Cancer
Apoptosis
Autophagy
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