Drug Discovery Opinion

DDO Limited – Consultancy for Biotech and Pharma

May 06 2010

Another Activity for Vinpocetine

Posted by WH in News, tags: drug discovery, inflammation

The Lesser Periwinkle (Vinca minor) Photo: Flickr – Phil Sellens

Vinpocetine is the semi-synthetic derivative (ethyl ester) of the alkaloid, apovincamine, found in the Lesser Periwinle (Vinca minor). It has previously been reported to have neuroprotective properties and to increase cerebral blood flow. Although it is used in Eastern Europe to treat cerebrovascular disorders and age-related memory loss, clinical studies have not conclusively demonstrated efficacy. Nevertheless, the compound is also widely used as a dietary supplement.

Vinpocetine is known to inhibit sodium-gated ion channels and has also been identified as a weak inhibitor (IC₅₀ ~ 10µM) of phosphodiesterase-1 (PDE-1). These activities have been used to explain the neuroprotective and vasorelaxant properties of the molecule.

Vinpocetine

Researchers at University of Rochester Medical Center have now reported potent activity of vinpocetine in a mouse model of lung inflammation, showing promise for the treatment of chronic inflammatory diseases such as COPD, rheumatoid arthritis and psoriasis. The scientists have demonstrated that the mechanism of action is via inhibition of IκB kinase (IKK) resulting in suppression of the proinflammatory transcription factor, NFκB.

Since the compound has a long history of human use, the researchers hope that development of vinpocetine as an antiinflammatory therapy will be easier than for a novel molecule. The university has applied for a patent for vinpocetine for use as an IKK-inhibitor for the treatment of COPD and Yan and Berk, lead scientists of the study, have formed a start-up company, Rock Pharmaceuticals, with the hope of licensing the intellectual property rights.

Full details of the study are currently in press at PNAS, entitled “Vinpocetine inhibits inflammation via an IKK-dependent but PDE-independent mechanism”.

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