Identification, biological activity, and mechanism of the anti-ischemic quinolone analog.
The quinolone analog SQ-4004 has been identified as a potentially excellent anti-ischemic agent, which exhibited highly potent efficacy in reducing infarct volume size in vivo rat MCAO model (32.1% at 0.01mg/kg) and potent cardioprotective effect at myocardial infarction in vivo model (26.6% at 0.01mg/kg) while it exhibited highly reduced anti-bacterial activity. The mechanistic study revealed that the anti-ischemic activity might exert via an anti-apoptotic pathway, which implies its therapeutic uses against the ischemic cell injuries including ischemic stroke and ischemic heart disease.
Park
Chan-Hee
CH
College of Pharmacy, Seoul National University, San 56-1 Shinrim-Dong, Kwanak-Gu, Seoul 151-742, Republic of Korea.
Lee
Jongwon
J
Jung
Hwi Young
HY
Kim
Min Ji
MJ
Lim
Sun Ha
SH
Yeo
Hyung Tae
HT
Choi
Eung Chil
EC
Yoon
Eun Jeong
EJ
Kim
Kyu Won
KW
Cha
Jong Ho
JH
Kim
Seok-Ho
SH
Chang
Dong-Jo
DJ
Kwon
Do-Yeon
DY
Li
Funan
F
Suh
Young-Ger
YG
D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D002545:Brain Ischemia / Q000188:drug therapy / Q000473:pathology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004195:Disease Models, Animal; D006801:Humans; D008954:Models, Biological; D015394:Molecular Structure; D009203:Myocardial Infarction / Q000188:drug therapy / Q000473:pathology; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D011804:Quinolines; C037219:quinoline