Novel histidine-conjugated galactosylated cationic liposomes for efficient hepatocyte-selective gene transfer in human hepatoma HepG2 cells
To enhance gene transfection to hepatocytes by cationic liposomes, it is necessary to overcome a number of barriers existing in the process from administration to gene expression. Recently we and other group have demonstrated that the escape of plasmid DNA (pDNA)/cationic liposome complexes (lipople...
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description | To enhance gene transfection to hepatocytes by cationic liposomes, it is necessary to overcome a number of barriers existing in the process from administration to gene expression. Recently we and other group have demonstrated that the escape of plasmid DNA (pDNA)/cationic liposome complexes (lipoplexes) from the endosome to cytoplasm was rate limiting. In this study, to enhance transfection efficiency by promoting the release of lipoplexes from the endosome to cytoplasm, we proposed utilizing the “proton sponge effect”. Here, we synthesized a novel pH-sensitive histidine-modified galactosylated cholesterol derivative (Gal-His-C4-Chol), for a more efficient gene delivery to hepatocytes. Liposomes containing Gal-His-C4-Chol showed much greater transfection activity than conventional Gal-C4-Chol liposomes based on a receptor-mediated mechanism in HepG2 cells. Hence, this finding should contribute to the development of gene therapy using cationic liposomes toward their clinical application. |
doi_str_mv | 10.1016/j.jconrel.2006.12.019 |
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Recently we and other group have demonstrated that the escape of plasmid DNA (pDNA)/cationic liposome complexes (lipoplexes) from the endosome to cytoplasm was rate limiting. In this study, to enhance transfection efficiency by promoting the release of lipoplexes from the endosome to cytoplasm, we proposed utilizing the “proton sponge effect”. Here, we synthesized a novel pH-sensitive histidine-modified galactosylated cholesterol derivative (Gal-His-C4-Chol), for a more efficient gene delivery to hepatocytes. Liposomes containing Gal-His-C4-Chol showed much greater transfection activity than conventional Gal-C4-Chol liposomes based on a receptor-mediated mechanism in HepG2 cells. Hence, this finding should contribute to the development of gene therapy using cationic liposomes toward their clinical application.</description><identifier>ISSN: 0168-3659</identifier><identifier>EISSN: 1873-4995</identifier><identifier>DOI: 10.1016/j.jconrel.2006.12.019</identifier><identifier>PMID: 17267065</identifier><identifier>CODEN: JCREEC</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Active Transport, Cell Nucleus ; Animals ; Asialoglycoprotein Receptor - metabolism ; Biological and medical sciences ; Carcinoma, Hepatocellular - metabolism ; Cations ; Cell Line, Tumor ; Cell Nucleus - metabolism ; Cell Survival - drug effects ; Cholestenes - metabolism ; Cholesterol Esters - chemistry ; Cholesterol Esters - metabolism ; Cholesterol Esters - toxicity ; Cytoplasm - metabolism ; DNA - chemistry ; DNA - metabolism ; Endosomes - metabolism ; Galactosylated liposomes ; Gene therapy ; General pharmacology ; Genes, Reporter ; Glycopeptides - chemistry ; Glycopeptides - metabolism ; Glycopeptides - toxicity ; Hepatocytes ; Histidine ; Humans ; Hydrogen-Ion Concentration ; Liposomes ; Liver Neoplasms - metabolism ; Luciferases ; Mannitol - metabolism ; Medical sciences ; Mice ; NIH 3T3 Cells ; Particle Size ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Proton sponge effect ; Transfection - methods</subject><ispartof>Journal of controlled release, 2007-04, Vol.118 (2), p.262-270</ispartof><rights>2006 Elsevier B.V.</rights><rights>2007 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c490t-928845b6c9cc6081b1042a20c469261395019420afe664ea385685de719e8edd3</citedby><cites>FETCH-LOGICAL-c490t-928845b6c9cc6081b1042a20c469261395019420afe664ea385685de719e8edd3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.jconrel.2006.12.019$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=18603928$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17267065$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Shigeta, Kosuke</creatorcontrib><creatorcontrib>Kawakami, Shigeru</creatorcontrib><creatorcontrib>Higuchi, Yuriko</creatorcontrib><creatorcontrib>Okuda, Tatsuya</creatorcontrib><creatorcontrib>Yagi, Hiroko</creatorcontrib><creatorcontrib>Yamashita, Fumiyoshi</creatorcontrib><creatorcontrib>Hashida, Mitsuru</creatorcontrib><title>Novel histidine-conjugated galactosylated cationic liposomes for efficient hepatocyte-selective gene transfer in human hepatoma HepG2 cells</title><title>Journal of controlled release</title><addtitle>J Control Release</addtitle><description>To enhance gene transfection to hepatocytes by cationic liposomes, it is necessary to overcome a number of barriers existing in the process from administration to gene expression. Recently we and other group have demonstrated that the escape of plasmid DNA (pDNA)/cationic liposome complexes (lipoplexes) from the endosome to cytoplasm was rate limiting. In this study, to enhance transfection efficiency by promoting the release of lipoplexes from the endosome to cytoplasm, we proposed utilizing the “proton sponge effect”. Here, we synthesized a novel pH-sensitive histidine-modified galactosylated cholesterol derivative (Gal-His-C4-Chol), for a more efficient gene delivery to hepatocytes. Liposomes containing Gal-His-C4-Chol showed much greater transfection activity than conventional Gal-C4-Chol liposomes based on a receptor-mediated mechanism in HepG2 cells. Hence, this finding should contribute to the development of gene therapy using cationic liposomes toward their clinical application.</description><subject>Active Transport, Cell Nucleus</subject><subject>Animals</subject><subject>Asialoglycoprotein Receptor - metabolism</subject><subject>Biological and medical sciences</subject><subject>Carcinoma, Hepatocellular - metabolism</subject><subject>Cations</subject><subject>Cell Line, Tumor</subject><subject>Cell Nucleus - metabolism</subject><subject>Cell Survival - drug effects</subject><subject>Cholestenes - metabolism</subject><subject>Cholesterol Esters - chemistry</subject><subject>Cholesterol Esters - metabolism</subject><subject>Cholesterol Esters - toxicity</subject><subject>Cytoplasm - metabolism</subject><subject>DNA - chemistry</subject><subject>DNA - metabolism</subject><subject>Endosomes - metabolism</subject><subject>Galactosylated liposomes</subject><subject>Gene therapy</subject><subject>General pharmacology</subject><subject>Genes, Reporter</subject><subject>Glycopeptides - chemistry</subject><subject>Glycopeptides - metabolism</subject><subject>Glycopeptides - toxicity</subject><subject>Hepatocytes</subject><subject>Histidine</subject><subject>Humans</subject><subject>Hydrogen-Ion Concentration</subject><subject>Liposomes</subject><subject>Liver Neoplasms - metabolism</subject><subject>Luciferases</subject><subject>Mannitol - metabolism</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>NIH 3T3 Cells</subject><subject>Particle Size</subject><subject>Pharmaceutical technology. 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Drug treatments</subject><subject>Proton sponge effect</subject><subject>Transfection - methods</subject><issn>0168-3659</issn><issn>1873-4995</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU-P1CAYh4nRuOPqR9Bw0VsrUErhZMxGd002etEzYejbGRpaKtBJ5jP4pWWcJnv0REie99_zQ-gtJTUlVHwc69GGOYKvGSGipqwmVD1DOyq7puJKtc_RrnCyakSrbtCrlEZCSNvw7iW6oR0THRHtDv35Hk7g8dGl7Ho3Q1WajuvBZOjxwXhjc0hn_-9rTXZhdhZ7t4QUJkh4CBHDMDjrYM74CIvJwZ4zVAk82OxOgA8wA87RzGmAiN2Mj-tk5o2dDH6A5Z5hC96n1-jFYHyCN9t7i359_fLz7qF6_HH_7e7zY2W5IrlSTEre7oVV1goi6Z4SzgwjlgvFBG1UW0xwRswAQnAwjWyFbHvoqAIJfd_cog_XvksMv1dIWU8uXTYwM4Q1aaoElYx3BWyvoI0hpQiDXqKbTDxrSvQlBT3qLQV9SUFTpsvsUvduG7DuJ-ifqjbtBXi_ASZZ44eix7r0xElBmnJm4T5dOSg6Tg6iThfVFnoXi1_dB_efVf4CwjSq8A</recordid><startdate>20070402</startdate><enddate>20070402</enddate><creator>Shigeta, Kosuke</creator><creator>Kawakami, Shigeru</creator><creator>Higuchi, Yuriko</creator><creator>Okuda, Tatsuya</creator><creator>Yagi, Hiroko</creator><creator>Yamashita, Fumiyoshi</creator><creator>Hashida, Mitsuru</creator><general>Elsevier B.V</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>RC3</scope></search><sort><creationdate>20070402</creationdate><title>Novel histidine-conjugated galactosylated cationic liposomes for efficient hepatocyte-selective gene transfer in human hepatoma HepG2 cells</title><author>Shigeta, Kosuke ; Kawakami, Shigeru ; Higuchi, Yuriko ; Okuda, Tatsuya ; Yagi, Hiroko ; Yamashita, Fumiyoshi ; Hashida, Mitsuru</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c490t-928845b6c9cc6081b1042a20c469261395019420afe664ea385685de719e8edd3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>Active Transport, Cell Nucleus</topic><topic>Animals</topic><topic>Asialoglycoprotein Receptor - metabolism</topic><topic>Biological and medical sciences</topic><topic>Carcinoma, Hepatocellular - metabolism</topic><topic>Cations</topic><topic>Cell Line, Tumor</topic><topic>Cell Nucleus - metabolism</topic><topic>Cell Survival - drug effects</topic><topic>Cholestenes - metabolism</topic><topic>Cholesterol Esters - chemistry</topic><topic>Cholesterol Esters - metabolism</topic><topic>Cholesterol Esters - toxicity</topic><topic>Cytoplasm - metabolism</topic><topic>DNA - chemistry</topic><topic>DNA - metabolism</topic><topic>Endosomes - metabolism</topic><topic>Galactosylated liposomes</topic><topic>Gene therapy</topic><topic>General pharmacology</topic><topic>Genes, Reporter</topic><topic>Glycopeptides - chemistry</topic><topic>Glycopeptides - metabolism</topic><topic>Glycopeptides - toxicity</topic><topic>Hepatocytes</topic><topic>Histidine</topic><topic>Humans</topic><topic>Hydrogen-Ion Concentration</topic><topic>Liposomes</topic><topic>Liver Neoplasms - metabolism</topic><topic>Luciferases</topic><topic>Mannitol - metabolism</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>NIH 3T3 Cells</topic><topic>Particle Size</topic><topic>Pharmaceutical technology. 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Drug treatments</topic><topic>Proton sponge effect</topic><topic>Transfection - methods</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Shigeta, Kosuke</creatorcontrib><creatorcontrib>Kawakami, Shigeru</creatorcontrib><creatorcontrib>Higuchi, Yuriko</creatorcontrib><creatorcontrib>Okuda, Tatsuya</creatorcontrib><creatorcontrib>Yagi, Hiroko</creatorcontrib><creatorcontrib>Yamashita, Fumiyoshi</creatorcontrib><creatorcontrib>Hashida, Mitsuru</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Genetics Abstracts</collection><jtitle>Journal of controlled release</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Shigeta, Kosuke</au><au>Kawakami, Shigeru</au><au>Higuchi, Yuriko</au><au>Okuda, Tatsuya</au><au>Yagi, Hiroko</au><au>Yamashita, Fumiyoshi</au><au>Hashida, Mitsuru</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel histidine-conjugated galactosylated cationic liposomes for efficient hepatocyte-selective gene transfer in human hepatoma HepG2 cells</atitle><jtitle>Journal of controlled release</jtitle><addtitle>J Control Release</addtitle><date>2007-04-02</date><risdate>2007</risdate><volume>118</volume><issue>2</issue><spage>262</spage><epage>270</epage><pages>262-270</pages><issn>0168-3659</issn><eissn>1873-4995</eissn><coden>JCREEC</coden><abstract>To enhance gene transfection to hepatocytes by cationic liposomes, it is necessary to overcome a number of barriers existing in the process from administration to gene expression. Recently we and other group have demonstrated that the escape of plasmid DNA (pDNA)/cationic liposome complexes (lipoplexes) from the endosome to cytoplasm was rate limiting. In this study, to enhance transfection efficiency by promoting the release of lipoplexes from the endosome to cytoplasm, we proposed utilizing the “proton sponge effect”. Here, we synthesized a novel pH-sensitive histidine-modified galactosylated cholesterol derivative (Gal-His-C4-Chol), for a more efficient gene delivery to hepatocytes. Liposomes containing Gal-His-C4-Chol showed much greater transfection activity than conventional Gal-C4-Chol liposomes based on a receptor-mediated mechanism in HepG2 cells. Hence, this finding should contribute to the development of gene therapy using cationic liposomes toward their clinical application.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>17267065</pmid><doi>10.1016/j.jconrel.2006.12.019</doi><tpages>9</tpages></addata></record> |
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subjects | Active Transport, Cell Nucleus Animals Asialoglycoprotein Receptor - metabolism Biological and medical sciences Carcinoma, Hepatocellular - metabolism Cations Cell Line, Tumor Cell Nucleus - metabolism Cell Survival - drug effects Cholestenes - metabolism Cholesterol Esters - chemistry Cholesterol Esters - metabolism Cholesterol Esters - toxicity Cytoplasm - metabolism DNA - chemistry DNA - metabolism Endosomes - metabolism Galactosylated liposomes Gene therapy General pharmacology Genes, Reporter Glycopeptides - chemistry Glycopeptides - metabolism Glycopeptides - toxicity Hepatocytes Histidine Humans Hydrogen-Ion Concentration Liposomes Liver Neoplasms - metabolism Luciferases Mannitol - metabolism Medical sciences Mice NIH 3T3 Cells Particle Size Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Proton sponge effect Transfection - methods |
title | Novel histidine-conjugated galactosylated cationic liposomes for efficient hepatocyte-selective gene transfer in human hepatoma HepG2 cells |
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