title: Photo biological activation of NSO donor mixed-ligand complexes: in vivo and preclinical perspectives.
abstract: Pyrazolone incorporating N-acetylcysteine (NAC) mixed-ligand complexes are described as promising anti-inflammatory, anticonvulsant, SODs mimetic and cytotoxic compounds possibly due to its antioxidant profile. In this study, we have evaluated the pharmacologic activity, antioxidant and toxicological profiles of compounds (1-6). Among them, compounds 1 and 4 were haemobiocompatible than the others. Both complexes 1 and 4 display efficient photo-nuclease activity upon irradiation with UV-A light of 365 nm and red light of 647 nm as compared with others. Mechanistic studies reveal that the DNA cleavage oxidative pathway involves H2O2 and singlet oxygen as the reactive oxygen species. Interestingly, both compounds 1 and 4, show non-toxic effects in vitro to human normal lymphocyte cells, revealing that they are selective in killing only the cancer cells as expected for a better drug. In addition, considering the safety profile, these compounds are promising as preventive and/or therapeutic agents against oxidative damage.
authors.affiliation: Research Department of Chemistry, VHNSN College, Virudhunagar 626 001, Tamil Nadu, India.
authors.forename: Muthusamy
authors.initials: M
authors.lastname: Selvaganapathy
authors.affiliation: Research Department of Chemistry, VHNSN College, Virudhunagar 626 001, Tamil Nadu, India.
authors.forename: Narayanaperumal
authors.initials: N
authors.lastname: Pravin
authors.affiliation: Research Department of Chemistry, VHNSN College, Virudhunagar 626 001, Tamil Nadu, India.
authors.forename: Krishnan
authors.initials: K
authors.lastname: Pothiraj
authors.affiliation: Research Department of Chemistry, VHNSN College, Virudhunagar 626 001, Tamil Nadu, India. Electronic address: drn_raman@yahoo.co.in.
authors.forename: Natarajan
authors.initials: N
authors.lastname: Raman
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology; D000927:Anticonvulsants / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D001522:Behavior, Animal / Q000187:drug effects; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D056831:Coordination Complexes / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D053837:DNA Cleavage / Q000187:drug effects / Q000528:radiation effects; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D005658:Fungi / Q000187:drug effects; D006801:Humans; D008024:Ligands; D008027:Light; D008214:Lymphocytes / Q000187:drug effects / Q000528:radiation effects; D008826:Microbial Sensitivity Tests; D051381:Rats; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy; D014466:Ultraviolet Rays
chemical_list: D000890:Anti-Infective Agents; D000927:Anticonvulsants; D000970:Antineoplastic Agents; D056831:Coordination Complexes; D008024:Ligands
keywords: N-acetylcysteine; Non-toxic effects; Photo-nuclease activity; Therapeutic agents