{"title":"喹啉酮诱导的口腔伯基特淋巴瘤细胞S期激酶相关蛋白-2和核因子κ","authors":"Supriatno","doi":"10.2174/1574362413666180912113856","DOIUrl":null,"url":null,"abstract":"\n\n3,4-Dihydro-6-[4-3,4-dimethoxybenzoyl-1-piperazinyl]-2(1H)-quinolinone\n(vesnarinone), a novel inotropic drug with unique and complex mechanisms of action, is\nknown to show antitumor activity against several human malignancies. In the present study,\nvesnarinone-induced signal transduction of S-phase kinase-associated protein 2 (Skp2) and\nNuclear Factor-kappa Beta (NF-κB) as molecular targets of oral malignant Burkitt’s lymphoma\n(Raji cells) was evaluated.\n\n\n\nRaji cells were incubated with vesnarinone at concentrations of 0,\n1.25x10-2, 2.50x10-2, or 5.0x10-2 Molar. After 24 h, chemotactic cell migration was examined by\na Boyden chamber kit. Apoptosis induction was observed by caspase-9 colorimetric assay. To\nevaluate levels of Skp2, NF-kB, and α-tubulin, Western blot analysis was performed.\n\n\n\nVesnarinone markedly suppressed chemotactic cell migration and significantly induced\napoptosis by increasing the caspase-9 activity of Raji cells through down regulation of Skp2\nand NF-κB.\n\n\n\n Vesnarinone decreased the expression of Skp2 and NF-κB indicating these molecules\nmay be targeted for the treatment of oral malignant Burkitt’s lymphoma (BL). The results\nof this work offer a promising therapeutic approach for BL tumors.\n","PeriodicalId":10868,"journal":{"name":"Current Signal Transduction Therapy","volume":"15 1","pages":"88-93"},"PeriodicalIF":0.0000,"publicationDate":"2020-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":"{\"title\":\"S-Phase Kinase-Associated Protein-2 and Nuclear Factor-kappa Beta as Molecular Targets of Oral Burkitt’s Lymphoma Cell Induced by Quinolinone Derivate-Vesnarinone\",\"authors\":\"Supriatno\",\"doi\":\"10.2174/1574362413666180912113856\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"\\n\\n3,4-Dihydro-6-[4-3,4-dimethoxybenzoyl-1-piperazinyl]-2(1H)-quinolinone\\n(vesnarinone), a novel inotropic drug with unique and complex mechanisms of action, is\\nknown to show antitumor activity against several human malignancies. In the present study,\\nvesnarinone-induced signal transduction of S-phase kinase-associated protein 2 (Skp2) and\\nNuclear Factor-kappa Beta (NF-κB) as molecular targets of oral malignant Burkitt’s lymphoma\\n(Raji cells) was evaluated.\\n\\n\\n\\nRaji cells were incubated with vesnarinone at concentrations of 0,\\n1.25x10-2, 2.50x10-2, or 5.0x10-2 Molar. After 24 h, chemotactic cell migration was examined by\\na Boyden chamber kit. Apoptosis induction was observed by caspase-9 colorimetric assay. To\\nevaluate levels of Skp2, NF-kB, and α-tubulin, Western blot analysis was performed.\\n\\n\\n\\nVesnarinone markedly suppressed chemotactic cell migration and significantly induced\\napoptosis by increasing the caspase-9 activity of Raji cells through down regulation of Skp2\\nand NF-κB.\\n\\n\\n\\n Vesnarinone decreased the expression of Skp2 and NF-κB indicating these molecules\\nmay be targeted for the treatment of oral malignant Burkitt’s lymphoma (BL). The results\\nof this work offer a promising therapeutic approach for BL tumors.\\n\",\"PeriodicalId\":10868,\"journal\":{\"name\":\"Current Signal Transduction Therapy\",\"volume\":\"15 1\",\"pages\":\"88-93\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2020-06-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"1\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current Signal Transduction Therapy\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/1574362413666180912113856\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Medicine\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Signal Transduction Therapy","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/1574362413666180912113856","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Medicine","Score":null,"Total":0}
S-Phase Kinase-Associated Protein-2 and Nuclear Factor-kappa Beta as Molecular Targets of Oral Burkitt’s Lymphoma Cell Induced by Quinolinone Derivate-Vesnarinone
3,4-Dihydro-6-[4-3,4-dimethoxybenzoyl-1-piperazinyl]-2(1H)-quinolinone
(vesnarinone), a novel inotropic drug with unique and complex mechanisms of action, is
known to show antitumor activity against several human malignancies. In the present study,
vesnarinone-induced signal transduction of S-phase kinase-associated protein 2 (Skp2) and
Nuclear Factor-kappa Beta (NF-κB) as molecular targets of oral malignant Burkitt’s lymphoma
(Raji cells) was evaluated.
Raji cells were incubated with vesnarinone at concentrations of 0,
1.25x10-2, 2.50x10-2, or 5.0x10-2 Molar. After 24 h, chemotactic cell migration was examined by
a Boyden chamber kit. Apoptosis induction was observed by caspase-9 colorimetric assay. To
evaluate levels of Skp2, NF-kB, and α-tubulin, Western blot analysis was performed.
Vesnarinone markedly suppressed chemotactic cell migration and significantly induced
apoptosis by increasing the caspase-9 activity of Raji cells through down regulation of Skp2
and NF-κB.
Vesnarinone decreased the expression of Skp2 and NF-κB indicating these molecules
may be targeted for the treatment of oral malignant Burkitt’s lymphoma (BL). The results
of this work offer a promising therapeutic approach for BL tumors.
期刊介绍:
In recent years a breakthrough has occurred in our understanding of the molecular pathomechanisms of human diseases whereby most of our diseases are related to intra and intercellular communication disorders. The concept of signal transduction therapy has got into the front line of modern drug research, and a multidisciplinary approach is being used to identify and treat signaling disorders.
The journal publishes timely in-depth reviews, research article and drug clinical trial studies in the field of signal transduction therapy. Thematic issues are also published to cover selected areas of signal transduction therapy. Coverage of the field includes genomics, proteomics, medicinal chemistry and the relevant diseases involved in signaling e.g. cancer, neurodegenerative and inflammatory diseases. Current Signal Transduction Therapy is an essential journal for all involved in drug design and discovery.