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Licochalcone A, a Polyphenol Present in Licorice, Suppresses UV-Induced COX-2 Expression by Targeting PI3K, MEK1, and B-Raf

التفاصيل البيبلوغرافية
العنوان: Licochalcone A, a Polyphenol Present in Licorice, Suppresses UV-Induced COX-2 Expression by Targeting PI3K, MEK1, and B-Raf
المؤلفون: Nu Ry Song, Jong-Eun Kim, Jun Seong Park, Jong Rhan Kim, Heerim Kang, Eunjung Lee, Young-Gyu Kang, Joe Eun Son, Sang Gwon Seo, Yong Seok Heo, Ki Won Lee
المصدر: International Journal of Molecular Sciences, Vol 16, Iss 3, Pp 4453-4470 (2015)
بيانات النشر: MDPI AG, 2015.
سنة النشر: 2015
المجموعة: LCC:Biology (General)
LCC:Chemistry
مصطلحات موضوعية: Licochalcone A, Solar ultraviolet, Cyclooxygenase-2, PI3K, MEK1, B-Raf, Biology (General), QH301-705.5, Chemistry, QD1-999
الوصف: Licorice is a traditional botanical medicine, and has historically been commonly prescribed in Asia to treat various diseases. Glycyrrhizin (Gc), a triterpene compound, is the most abundant phytochemical constituent of licorice. However, high intake or long-term consumption of Gc has been associated with a number of side effects, including hypertension. However, the presence of alternative bioactive compounds in licorice with anti-carcinogenic effects has long been suspected. Licochalcone A (LicoA) is a prominent member of the chalcone family and can be isolated from licorice root. To date, there have been no reported studies on the suppressive effect of LicoA against solar ultraviolet (sUV)-induced cyclooxygenase (COX)-2 expression and the potential molecular mechanisms involved. Here, we show that LicoA, a major chalcone compound of licorice, effectively inhibits sUV-induced COX-2 expression and prostaglandin E2 PGE2 generation through the inhibition of activator protein 1 AP-1 transcriptional activity, with an effect that is notably more potent than Gc. Western blotting analysis shows that LicoA suppresses sUV-induced phosphorylation of Akt/ mammalian target of rapamycin (mTOR) and extracellular signal-regulated kinases (ERK)1/2/p90 ribosomal protein S6 kinase (RSK) in HaCaT cells. Moreover, LicoA directly suppresses the activity of phosphoinositide 3-kinase (PI3K), mitogen-activated protein kinase kinase (MEK)1, and B-Raf, but not Raf-1 in cell-free assays, indicating that PI3K, MEK1, and B-Raf are direct molecular targets of LicoA. We also found that LicoA binds to PI3K and B-Raf in an ATP-competitive manner, although LicoA does not appear to compete with ATP for binding with MEK1. Collectively, these results provide insight into the biological action of LicoA, which may have potential for development as a skin cancer chemopreventive agent.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 1422-0067
Relation: http://www.mdpi.com/1422-0067/16/3/4453; https://doaj.org/toc/1422-0067
DOI: 10.3390/ijms16034453
URL الوصول: https://doaj.org/article/06b4b93aaad84906a4351f6c5ccee33a
رقم الأكسشن: edsdoj.06b4b93aaad84906a4351f6c5ccee33a
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:14220067
DOI:10.3390/ijms16034453