title: Novel lysosome targeted molecular transporter built on a guanidinium-poly-(propylene imine) hybrid dendron for efficient delivery of doxorubicin into cancer cells.
abstract: An efficient synthetic approach has been adopted to construct a new dendron-based octa-guanidine appended molecular transporter with a lysosomal targeted peptide-doxorubicin conjugate. The transporter alone (G8-PPI-FL) is found to be non-toxic, showed higher cellular uptake compared to Arg-8-mer and exhibited excellent selectivity towards lysosomes in cathepsin B expressing HeLa cells, while the Dox-conjugate showed significant cytotoxicity to cancer cells without affecting the non-cancerous cells.
authors.affiliation: Chemical Sciences & Technology Division, CSIR-National Institute for Interdisciplinary Science & Technology (CSIR-NIIST), Industrial Estate, Pappanamcode, Thiruvananthapuram-695019, Kerala, India. kkmaiti@niist.res.in kkmaiti29@gmail.com.
authors.forename: Jyothi B
authors.initials: JB
authors.lastname: Nair
authors.forename: Saswat
authors.initials: S
authors.lastname: Mohapatra
authors.forename: Surajit
authors.initials: S
authors.lastname: Ghosh
authors.forename: Kaustabh K
authors.initials: KK
authors.lastname: Maiti
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000737:chemistry* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D001120:Arginine / Q000737:chemistry; D002401:Cathepsin B / Q000378:metabolism; D050091:Dendrimers / Q000737:chemistry*; D004317:Doxorubicin / Q000737:chemistry* / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry*; D019791:Guanidine / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D008247:Lysosomes; D010455:Peptides / Q000737:chemistry; D011126:Polypropylenes / Q000737:chemistry*
chemical_list: D000903:Antibiotics, Antineoplastic; D050091:Dendrimers; D004337:Drug Carriers; D010455:Peptides; D011126:Polypropylenes; C443641:poly(propyleneimine); D004317:Doxorubicin; D001120:Arginine; D002401:Cathepsin B; D019791:Guanidine