A new class of β-carboline alkaloid-peptide conjugates with therapeutic efficacy in acute limb ischemia/reperfusion injury

We describe a novel class of β-carboline alkaloid-peptide conjugates that possess both free radical scavenging and thrombolytic activity. These conjugates demonstrate therapeutic efficacy in a rat arterial thrombosis assay, as well as free radical scavenging capacity as evaluated in a PC12 cell surv...

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Veröffentlicht in:European journal of medicinal chemistry 2011-05, Vol.46 (5), p.1453-1462
Hauptverfasser: Bi, Wei, Bi, Yue, Xue, Ping, Zhang, Yanrong, Gao, Xiang, Wang, Zhibo, Li, Meng, Baudy-Floc’h, Michèle, Ngerebara, Nathaniel, Michael Gibson, K., Bi, Lanrong
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Sprache:eng
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Zusammenfassung:We describe a novel class of β-carboline alkaloid-peptide conjugates that possess both free radical scavenging and thrombolytic activity. These conjugates demonstrate therapeutic efficacy in a rat arterial thrombosis assay, as well as free radical scavenging capacity as evaluated in a PC12 cell survival assay. Our results indicate that β-carboline alkaloid-peptide conjugate 26a exerts a significant protective effect against local and remote organ injury induced by limb I/R injury in the rat. A novel class of β-carboline alkaloid-peptide conjugates that possess both free radical scavenging and thrombolytic activity is described in this manuscript. [Display omitted] ► In this manuscript, we have developed a novel class of β-carboline alkaloid-peptide conjugates. ► These conjugates possess good free radical scavenging and thrombolytic activities. ► Compound 26a exerts a significant protective effect against limb I/R injury in the rat.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2011.01.021