Antioxidant property of alpha lipoic acid retains after conjugation with SynB3 Peptide

Alpha lipoic acid (ALA), an antioxidant reagent (1) is currently being proposed as a potential therapeutic candidate against central nervous system (CNS) diseases (2, 3). Although it can cross blood brain barrier (BBB), its poor bioavailability due to its heat sensitivity and susceptibility toward enzymes render its pharmacokinetics poor enough to use as a drug (2).  Several strategies including bioconjugation and encapsulation have been used successfully to improve pharmacokinetics of drug like molecules (4, 5, 6, and 8). Despite having success in many cases, bioconjugation often leads to perturb structure of drugs and hence reduce its activity (7). Therefore, it is important to study the efficacy of drug like compounds after necessary modification. Here we report that antioxidant activity of ALA retains intact after conjugating SynB3 peptide, which is also a BBB active peptide (9, 14). So, new ALA-peptide conjugate may serve as a potential anti-oxidant with improved bioavailability.