title: N-Acetylcysteine amide: a derivative to fulfill the promises of N-Acetylcysteine.
abstract: In the present human health scenario, implication of oxidative stress in numerous pathologies including neurodegenerative, cardiovascular, liver, renal, pulmonary disorders, and cancer has gained attention. N-Acetylcysteine (NAC), a popular thiol antioxidant, has been clinically used to treat various pathophysiological disorders. However, NAC therapy is routine only in paracetamol intoxication and as a mucolytic agent. Over six decades, numerous studies involving NAC therapy have yielded inconsistent results, and this could be due to low bioavailability. In order to overcome the limitations of NAC, an amide derivative N-Acetylcysteine amide (NACA) has been synthesized to improve the lipophilicity, membrane permeability, and antioxidant property. Recent studies have demonstrated the blood-brain barrier permeability and therapeutic potentials of NACA in neurological disorders including Parkinson's disease, Alzheimer's disease, Multiple sclerosis, Tardive dyskinesia, and HIV-associated neurological disorders. In addition, NACA displays protective effect against pulmonary inflammation and antibiotic-induced apoptosis. Forthcoming research on the possible therapeutic properties of NACA and its generics in the management of pathologies associated with extracellular matrix degradation and oxidative stress-related inflammation is highly exiting. Superior bioavailability of NACA is likely to fulfill the promises of NAC as well as a molecule to improve the endurance and resident time of bioscaffolds and biomaterials. Till date, more than 800 reviews on NAC have been published. However, no comprehensive review is available on the therapeutic applications of NACA. Therefore, the current review would be the first to emphasize the therapeutic potentials of NACA and its derivatives.
authors.affiliation: DOS in Biochemistry, University of Mysore, Manasagangothri, Mysore, India.
authors.forename: K
authors.initials: K
authors.lastname: Sunitha
authors.forename: M
authors.initials: M
authors.lastname: Hemshekhar
authors.forename: R M
authors.initials: RM
authors.lastname: Thushara
authors.forename: M Sebastin
authors.initials: MS
authors.lastname: Santhosh
authors.forename: M
authors.initials: M
authors.lastname: Yariswamy
authors.forename: K
authors.initials: K
authors.lastname: Kemparaju
authors.forename: K S
authors.initials: KS
authors.lastname: Girish
mesh_terms: D000111:Acetylcysteine / Q000008:administration & dosage / Q000031:analogs & derivatives*; D000975:Antioxidants / Q000008:administration & dosage*; D017209:Apoptosis / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004358:Drug Therapy / Q000379:methods*; D005978:Glutathione / Q000378:metabolism; D006801:Humans; D018384:Oxidative Stress / Q000187:drug effects*; D017382:Reactive Oxygen Species / Q000378:metabolism
chemical_list: D000975:Antioxidants; D017382:Reactive Oxygen Species; C487056:N-Acetylcysteinamide; D005978:Glutathione; D000111:Acetylcysteine