Cardioprotective effect of novel sulphonamides-1,3,5-triazine conjugates against ischaemic-reperfusion injury via selective inhibition of MMP-9.
Diseases affecting cardiovascular system are ranked as a top most cause of morbidity and mortality. Herein, a novel class sulphonamides-1,3,5-triazine conjugates have been synthesized and tested for inhibitory activity against MMP-2 and MMP-9. The results of the study showed that these molecules efficiently inhibit MMP-9 than MMP-2, revealing compound 8e as the most potent inhibitor (IC50= 2.34 ± 0.56 nm). Due to involvement of MMP-9 in many cardiovascular diseases, particularly in myocardial ischaemia (MI), compound 8e was further subjected for the determination of the protective effect on isoproterenol (ISO)-induced myocardial injury in rats.
Department of Anesthesiology, Zhejiang Hospital, Hangzhou, Zhejiang, China.|Department of Anesthesiology, Nanfang Hospital of Southern Medical University, Guangzhou, Guangdong, China.
Xiao-Zhu
XZ
Zheng
Department of Anesthesiology, Zhejiang Hospital, Hangzhou, Zhejiang, China.
Jia-Li
JL
Zhou
Department of Anesthesiology, Nanfang Hospital of Southern Medical University, Guangzhou, Guangdong, China.
Jing
J
Ye
Department of Anesthesiology, Nanfang Hospital of Southern Medical University, Guangzhou, Guangdong, China.
Pei-Pei
PP
Guo
Department of Anesthesiology, Nanfang Hospital of Southern Medical University, Guangzhou, Guangdong, China. linchunshui@hotmail.com.
Chun-Shui
CS
Lin
D000818:Animals; D000975:Antioxidants / Q000378:metabolism; D002316:Cardiotonic Agents / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D006321:Heart / Q000187:drug effects; D020128:Inhibitory Concentration 50; D007545:Isoproterenol / Q000633:toxicity; D008297:Male; D020778:Matrix Metalloproteinase 2 / Q000737:chemistry / Q000378:metabolism; D020780:Matrix Metalloproteinase 9 / Q000737:chemistry / Q000378:metabolism*; D061965:Matrix Metalloproteinase Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D009206:Myocardium / Q000378:metabolism / Q000473:pathology; D011485:Protein Binding; D051381:Rats; D017208:Rats, Wistar; D015427:Reperfusion Injury / Q000139:chemically induced / Q000188:drug therapy; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry; D014227:Triazines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use
D000975:Antioxidants; D002316:Cardiotonic Agents; D061965:Matrix Metalloproteinase Inhibitors; D013449:Sulfonamides; D014227:Triazines; D020778:Matrix Metalloproteinase 2; D020780:Matrix Metalloproteinase 9; D007545:Isoproterenol
1,3,5-triazine; MMP inhibition; biochemical assay; myocardial ischaemia; sulphonamide