Vincamine CAS:1617-90-9
Formula C21H26N2O3
Molar mass 354.45 g·mol−1
Trade names Oxybral SR
Vincamine is a monoterpenoid indole alkaloid found in the leaves of Vinca minor (lesser periwinkle), comprising about 25-65% of its indole alkaloids by weight. It can also be synthesized from related alkaloids.
Vincamine is a monoterpenoid indole alkaloid obtained from the leaves of Vinca minor with a vasodilatory property. Studies indicate that vincamine increases the regional cerebral blood flow.
It is sold in Europe as a prescription medicine for improving cerebral blood flow, brain metabolism, and increasing the firing rate of locus coeruleus-noradrenergic system. Vincamine is a peripheral vasodilator that increases blood flow to the brain. Generic drugs containing vincamine exist in specific regions.Most common drug preparations are in the sustained release tablet forms.
Vincamine is a poorly soluble potent neuroprotector and cerebral vasodilator, used for the treatment for CNS disorders. In some cases, the bioavailability of pure compounds is strongly influenced by the co-administration of other constituents, and in some cases, the so called ‘phytocomplex’ may act as enhancer of absorption of selected phytochemicals. In this paper, the oral bioavailability of vincamine when administered as a standardised Vinca minor L. leaf dry extract rather than pure indole alkaloid is demonstrated to be higher.
The chosen alkaloid-enriched and standardised dry extract was widely characterised by means of HPLC–MS, PXRD, DSC, XPS, 13C and 15N solid-state NMR (SSNMR) using pure vincamine as a matter of comparison. Then, the in vitro dissolution performances of the two products and their in vivo bioavailability in rats were evaluated. The sevenfold improvement in oral bioavailability of the dry extract with respect to the pure vincamine was ascribed to interactions between the indole alkaloid and the corollary of ingredients of the dry extract, giving rise to the protonation of the alkaloid vincamine, thus enhancing its dissolution in physiological fluids. Present data demonstrate that alkaloid vincamine administered as a whole plant extract has a higher bioavailability compared to the pure chemical compound.
Graphical abstract
The oral bioavailability of vincamine from an alkaloid-enriched Vinca minor L. leaf dry extract is sevenfold higher compared to pure vincamine, thus suggesting that the administration of standardised extract may be more effective compared with pure compound.
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