Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Design, Synthesis and Biological Study of Novel NO-Donor-Caffeic Acid Hybrids as Potential Anti-Atherosclerotic Drug Candidates

Author(s): Nian-Guang Li, Rong Wang, Yu-Ping Tang, Zhi-Hao Shi, Bao-Quan Li, Wei Li, Jian-Ping Yang, Zhen-Jiang Wang, Shu-Lin Song, Li-Hua Qian, Li-Juan Yao, Jun-Zuan Xia, Jia Xu, Feng Feng, Da-Wei Qian, Jin-Ao Duan.


Novel NO-donor-caffeic acid hybrids with antioxidant, nitric oxide release and vasodilator properties were designed and synthesized through a symbiotic approach using caffeic acid and three different NO-donating groups such as nitric ester, 4-hydroxyl-3-phenylfuroxan and 4-hydroxymethyl-3-phenylsulfonylfuroxan. The antioxidant activities of these hybrid products were assessed by DPPH assay and by detecting the TBARS produced in the ferrous salt/ascorbate induced autoxidation of lipids which were present in microsomial membranes of rat hepatocytes. The nitric oxide release activities were assessed by indirect evaluation of the produced nitrite. The vasodilator activities were determined through an in vitro vascular relaxation assay (organ bath) using PGF2α-precontracted porcine pulmonary arteries. The results showed that the target phenylsulfonylfuroxan 12, especially 12a while keeping the antioxidant activity, showed more NO release activity and vasodilating activity than isosorbide dinitrate (ISDN). Thus 12a may be considered as a novel potent anti-atherosclerosiss drug candidate.

Keywords: Atherosclerosis, Nitric oxide donor, Caffeic acid, Antioxidant activity, Nitric oxide release, Vasodilator activity, LDL, Acid Hybrids, Anti-Atherosclerotic, Moiety, reactive oxygen species (ROS), vasodilation, isoproterenol (ISO), myocardial infarction, dibromoalkanes, lipid autooxidation

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

Year: 2011
Page: [550 - 557]
Pages: 8
DOI: 10.2174/157018011795906848
Price: $58