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- W2740608623 abstract "This study was designed to determine the in vitro mechanisms by which the novel silybin derivative, (E)-3-(3-(benzyloxy) phenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one (HM015k or 15k), produces its anticancer efficacy in ovarian cancer cells. Compound 15k induced apoptosis in ovarian cancer cells in a time-dependent manner by significantly upregulating the expression of Bax and Bak and downregulating the expression of the Bcl2. Interestingly, 15k induced the cleavage of Bax p21 into its more efficacious cleaved form, Bax p18. In addition, caspase 3 and caspase 9 were cleaved to their active forms, inducing the cleavage of poly ADP ribose polymerase (PARP) and β-catenin. Furthermore, in OV2008 cells, 15k induced significant cleavage in nuclear β-catenin to primarily inactive fragments of lower molecular weight. Furthermore, 15k reversed the metastatic potential of OV2008 cells by inhibiting their migration and invasiveness. The mesenchymal phenotype in OV2008 was reversed by 15k, causing cells to be rounder with epithelial - like phenotypes. The 15k-induced reversal was further confirmed by significant upregulation of the E-cadherin expression, an epithelial marker, while N-cadherin, a mesenchymal marker, was downregulated in OV2008 cells. Compound 15k inhibited the expression of the oncogenic c-Myc protein, downregulated proteins DVL3 and DVL2 and significantly upregulated cyclin B1. Also, 15k significantly downregulated the expression levels of ABCG2 and ABCB1 transporters in resistant ABCG2 overexpressing H460/MX20 and resistant ABCB1 overexpressing MDCK/MDR1 cells, respectively. Finally, 15k was safe in zebrafish in vivo model at concentrations up to 10 µM and induced no major toxicities in cardiac, morphology and swimming position parameters. Overall, 15k is a multi-targeted inhibitor with an efficacy against metastatic and resistant ovarian cancer. Future in vivo studies will be conducted to determine the efficacy of 15k in tumor-bearing animals." @default.
- W2740608623 created "2017-08-08" @default.
- W2740608623 creator A5000133026 @default.
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- W2740608623 creator A5074080090 @default.
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- W2740608623 creator A5088367170 @default.
- W2740608623 date "2017-08-02" @default.
- W2740608623 modified "2023-10-01" @default.
- W2740608623 title "HM015k, a Novel Silybin Derivative, Multi-Targets Metastatic Ovarian Cancer Cells and Is Safe in Zebrafish Toxicity Studies" @default.
- W2740608623 cites W1489084607 @default.
- W2740608623 cites W1553345136 @default.
- W2740608623 cites W1592729189 @default.
- W2740608623 cites W1922025862 @default.
- W2740608623 cites W1964064617 @default.
- W2740608623 cites W1964617786 @default.
- W2740608623 cites W1965025928 @default.
- W2740608623 cites W1966369019 @default.
- W2740608623 cites W1968532316 @default.
- W2740608623 cites W1968967017 @default.
- W2740608623 cites W1969867759 @default.
- W2740608623 cites W1977178308 @default.
- W2740608623 cites W1978878974 @default.
- W2740608623 cites W1987473368 @default.
- W2740608623 cites W1991242976 @default.
- W2740608623 cites W1991953785 @default.
- W2740608623 cites W1992499848 @default.
- W2740608623 cites W1995074959 @default.
- W2740608623 cites W2001151803 @default.
- W2740608623 cites W2004594957 @default.
- W2740608623 cites W2006424018 @default.
- W2740608623 cites W2007792721 @default.
- W2740608623 cites W2008757142 @default.
- W2740608623 cites W2016133409 @default.
- W2740608623 cites W2019580313 @default.
- W2740608623 cites W2025636716 @default.
- W2740608623 cites W2029086576 @default.
- W2740608623 cites W2031171659 @default.
- W2740608623 cites W2036805643 @default.
- W2740608623 cites W2038271205 @default.
- W2740608623 cites W2038784909 @default.
- W2740608623 cites W2039888539 @default.
- W2740608623 cites W2045269572 @default.
- W2740608623 cites W2047172303 @default.
- W2740608623 cites W2051294566 @default.
- W2740608623 cites W2051446073 @default.
- W2740608623 cites W2054359817 @default.
- W2740608623 cites W2055325954 @default.
- W2740608623 cites W2057505281 @default.
- W2740608623 cites W2060184827 @default.
- W2740608623 cites W2063168427 @default.
- W2740608623 cites W2064980235 @default.
- W2740608623 cites W2069031289 @default.
- W2740608623 cites W2070755882 @default.
- W2740608623 cites W2075711878 @default.
- W2740608623 cites W2080835467 @default.
- W2740608623 cites W2081145901 @default.
- W2740608623 cites W2082905439 @default.
- W2740608623 cites W2084421367 @default.
- W2740608623 cites W2088244733 @default.
- W2740608623 cites W2090137644 @default.
- W2740608623 cites W2090153150 @default.
- W2740608623 cites W2095202492 @default.
- W2740608623 cites W2096638312 @default.
- W2740608623 cites W2097777938 @default.
- W2740608623 cites W2108026241 @default.
- W2740608623 cites W2108459871 @default.
- W2740608623 cites W2111251544 @default.
- W2740608623 cites W2111757377 @default.
- W2740608623 cites W2112420045 @default.
- W2740608623 cites W2116508133 @default.
- W2740608623 cites W2122624385 @default.
- W2740608623 cites W2124465755 @default.
- W2740608623 cites W2124741080 @default.
- W2740608623 cites W2130941707 @default.
- W2740608623 cites W2131080175 @default.
- W2740608623 cites W2131532199 @default.
- W2740608623 cites W2133554162 @default.
- W2740608623 cites W2135387903 @default.
- W2740608623 cites W2135956341 @default.
- W2740608623 cites W2137005750 @default.
- W2740608623 cites W2140804732 @default.
- W2740608623 cites W2141037581 @default.
- W2740608623 cites W2141400767 @default.
- W2740608623 cites W2145642308 @default.
- W2740608623 cites W2149598894 @default.
- W2740608623 cites W2149837109 @default.
- W2740608623 cites W2151213561 @default.
- W2740608623 cites W2153770286 @default.
- W2740608623 cites W2154473845 @default.
- W2740608623 cites W2158021558 @default.
- W2740608623 cites W2162665020 @default.
- W2740608623 cites W2170556339 @default.
- W2740608623 cites W2171140538 @default.
- W2740608623 cites W2286081257 @default.