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Int. J. Mol. Sci. 2018, 19(2), 620; https://doi.org/10.3390/ijms19020620

3,5,6,7,8,3′,4′-Heptamethoxyflavone, a Citrus Flavonoid, Inhibits Collagenase Activity and Induces Type I Procollagen Synthesis in HDFn Cells

Department of Biomedical Chemistry, Research Institute for Biomedical & Health Science, College of Biomedical and Health Science, Konkuk University, 268 Chungwon-daero, Chungju-si 27478, Korea
These authors contributed equally to this work.
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Received: 12 January 2018 / Revised: 26 January 2018 / Accepted: 21 February 2018 / Published: 22 February 2018
(This article belongs to the Special Issue Bioactive Phenolics and Polyphenols 2018)
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Abstract

Citrus fruits contain various types of flavonoids with powerful anti-aging and photoprotective effects on the skin, and have thus been attracting attention as potential, efficacious skincare agents. Here, we aimed to investigate the chemical composition of Citrus unshiu and its protective effects on photoaging. We isolated and identified a bioactive compound, 3,5,6,7,8,3′,4′-heptamethoxyflavone (HMF), from C. unshiu peels using ethanol extraction and hexane fractionation. HMF inhibited collagenase activity and increased type I procollagen content in UV-induced human dermal fibroblast neonatal (HDFn) cells. HMF also suppressed the expression of matrix metalloproteinases 1 (MMP-1) and induced the expression of type I procollagen protein in UV-induced HDFn cells. Additionally, HMF inhibited ultraviolet B (UVB)-induced phosphorylation of the mitogen-activated protein kinases (MAPK) cascade signaling components—ERK, JNK, and c-Jun—which are involved in the induction of MMP-1 expression. Furthermore, HMF affected the TGF-β/Smad signaling pathway, which is involved in the regulation of type I procollagen expression. In particular, HMF induced Smad3 protein expression and suppressed Smad7 protein expression in UV-induced HDFn cells in a dose-dependent manner. These findings suggest a role for Citrus unshiu in the preparation of skincare products in future. View Full-Text
Keywords: Citrus unshiu; collagenase; HDFn; Heptamethoxyflavone; Type I procollagen Citrus unshiu; collagenase; HDFn; Heptamethoxyflavone; Type I procollagen
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Kim, H.-I.; Jeong, Y.-U.; Kim, J.-H.; Park, Y.-J. 3,5,6,7,8,3′,4′-Heptamethoxyflavone, a Citrus Flavonoid, Inhibits Collagenase Activity and Induces Type I Procollagen Synthesis in HDFn Cells. Int. J. Mol. Sci. 2018, 19, 620.

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