Sarcophine-Diol Inhibits Expression of COX-2, Inhibits Activity of cPLA2, Enhances Degradation of PLA2 and PLCγ1 and Inhibits Cell Membrane Permeability in Mouse Melanoma B16F10 Cells 英文参考文献.docVIP

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Sarcophine-Diol Inhibits Expression of COX-2, Inhibits Activity of cPLA2, Enhances Degradation of PLA2 and PLCγ1 and Inhibits Cell Membrane Permeability in Mouse Melanoma B16F10 Cells 英文参考文献.doc

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Sarcophine-Diol Inhibits Expression of COX-2, Inhibits Activity of cPLA2, Enhances Degradation of PLA2 and PLCγ1 and Inhibits Cell Membrane Permeability in Mouse Melanoma B16F10 Cells 英文参考文献

Mar. Drugs 2012, 10, 2166-2180; doi:10.3390/mOPEN ACCESS Marine Drugs ISSN 1660-3397 /journal/marinedrugs Article Sarcophine-Diol Inhibits Expression of COX-2, Inhibits Activity of cPLA2, Enhances Degradation of PLA2 and PLCγ1 and Inhibits Cell Membrane Permeability in Mouse Melanoma B16F10 Cells Pawel T. Szymanski 1, Pratik Muley 1, Safwat A. Ahmed 2, Sherief Khalifa 3 and Hesham Fahmy 1,* 1 Department of Pharmaceutical Sciences, College of Pharmacy, South Dakota State University, Brookings, SD 57007, USA; E-Mails: pawel.szymanski@ (P.T.S.); Pratik.Muley@ (P.M.) 2 Department of Pharmacognosy, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, Egypt; E-Mail: safwat_aa@ 3 College of Pharmacy, Qatar University, Doha 02713, Qatar; E-Mail: sherief@.qa * Author to whom correspondence should be addressed; E-Mail: Hesham.Fahmy@; Tel.: +1-605-688-4243; Fax: +1-605-688-5993. Received: 14 June 2012; in revised form: 20 July 2012 / Accepted: 21 September 2012 / Published: 28 September 2012 Abstract: Sarcophine-diol (SD) is a semi-synthetic derivative of sarcophine with a significant chemopreventive effect against non-melanoma skin cancer both in vitro and in vivo. Recently, we have studied the effect of SD on melanoma development using the mouse melanoma B16F10 cell line. In this study, our findings show that SD suppresses cell multiplication and diminishes membrane permeability for ethidium bromide (EB), a model marker used to measure cell permeability for Ca2+ ions. SD also decreases protein levels of COX-2, and increases degradation of phospholipases PLA2 and PLCγ1 and diminishes enzymatic activity of the Ca2+-dependent cPLA2. This lower membrane permeability for Ca2+-ions, associated with SD, is most likely due to the diminished content of lysophosphosphatidylcholine (lysoPC) within cell membranes caused by the effect of SD on PLA2. The decrease in diacylglycerol (DAG) and i