[Neuroprotective effects of vinpocetine in vivo and in vitro. Apovincaminic acid derivatives as potential therapeutic tools in ischemic stroke].

Abstract

The aim of the present study was to review neuroprotective therapy from the preclinical point of view as a potential tool for the treatment of stroke, as well as to discuss neuroprotective effects of the apovincaminic acid derivative vinpocetine (Cavinton). Our own in vivo and in vitro experiments were aimed at further characterizing pharmacological effects involved in the vinpocetine-induced neuroprotection. The effect of vinpocetine on infarct volume (obtained by 2,3,5-triphenyltetrazolium-chloride staining) was studied in permanent middle cerebral artery occlusion (MCAO) in rats (3 mg/kg i.p., 30 min postischemia). Vinpocetine treatment significantly decreased infarct volume (by 42%, p < 0.05) compared to control, which was better than the effect of nimodipine (17%) or MK-801 (18%). Neurotoxicity measurements were made in primary cortical cell culture using LDH release as an indicator. Vinpocetine dose-dependently inhibited prolonged (24 h) or transient (15 min) glutamate, and transient N-metil-D-aspartate (NMDA) or veratridine (0.1-1 mM) induced excitotoxicity (IC50 = 2-7 x 10(-6) M). In these tests the neuroprotective potency of vinpocetine was lower than that of MK-801, but it was similar to those of flunarizine or nimodipine. These results together with former literature data indicate that apovincaminic acid derivatives possessing strong neuroprotective potential may play an important role in the therapy of ischemic stroke.

• Authors: László Dézsi, Istvánné Kis-Varga, József Nagy, Zsolt Komlódi, Egon Kárpáti
• Journal: Acta pharmaceutica Hungarica (Acta Pharm Hung) Vol. 72 Issue 2 Pg. 84-91 ( 2002) ISSN: 0001-6659 [Print] Hungary
• Vernacular Title: A vinpocetin neuroprotektív hatásai in vivo és in vitro. Apovinkaminsav származékok mint az ischemiás stroke lehetséges terápiás eszközei.
• PMID: 12498034 (Publication Type: English Abstract, Journal Article)

Chemical References

• Neuroprotective Agents
• Vinca Alkaloids
• apovincaminic acid
• vinpocetine

Topics

• Animals
• Brain Ischemia (drug therapy)
• Disease Models, Animal
• Humans
• Ischemic Attack, Transient (drug therapy)
• Neuroprotective Agents (therapeutic use)
• Rats
• Stroke (drug therapy)
• Structure-Activity Relationship
• Vinca Alkaloids (pharmacology, therapeutic use)