• Voacanga africana
    Voacanga africana
  • Voacanga africana
    Voacanga africana

Vinpocetine

VINPOCETINE (EP)

EP
DMF

Linnea extracts and manufactures Vinpocetine as a botanical ingredient for psychic and neurological pharmaceutical purposes.

Cognitive function loss has become a major health concern due to the large number of individuals experiencing dementia, memory loss and other such difficulties, and also due to the lack of effective medical treatment. It is often passed off as a natural part of aging, but the use of nutritional supplements and botanical substances has been found to enhance cognitive function and, very importantly, to help reverse and prevent cognitive dysfunction. Vinpocetine is a peripheral vasolidator that increases cerebral blood flow [1], activates cerebral metabolism [2] with neuroprotective effects and supports brain functions such as concentration and memory. Furthermore it has been identified as a strong anti-inflammatory agent, more recently it has been considered for its potential role in the treatment of Parkinson’s disease [3,4,5].

Source

Vinpocetine (ethyl ester of Apovincamine) is a semisynthetic alkaloid derived of Vincamine that is found in the aerial part of the Vinca minor plant. Linnea Vincamine production process is based on synthesis from the Tabersonine, an indole alkaloid obtained from Voacanga africana seeds.

Voacanga africana is a tropical, evergreen tree belonging to the Apocynaceae family, with yellow or white flowers, that grows up to a height of around 6 m. Native to the West African rainforests, it prefers well composted rich soils in a protected sunny to partly shaded position, and is sensitive to drought and frost. Voacanga africana is well known to African magic healers although little is known about the actual use of the seeds and bark of the various Voacanga species other than the fact that the plant is held in high esteem for ritual purposes. The Voacanga seeds are carefully harvested through a selected network of suppliers. Each shipment leaving West Africa is inspected previously by a Linnea representative in situ so as to ensure raw materials of the highest quality all over the world.

Activity

Vinpocetine attenuates disorders caused by hypoxia or deficient cerebral metabolism improving oxygen and glucose utilisation by brain cells.

In patients with cerebral haemorrhage, cerebral infarction and cerebrosclerosis, Vinpocetine gives improvements in both mental and neurological symptoms by promoting the redistribution of the blood flow towards ischemic areas. The general effect on the cerebral metabolism is attributable to the combination of several activities resulting in a general neuroprotective effect and memory improvement. Its calcium-channel blocking activity and inhibitory effect on voltage-gated sodium channel attenuate reperfusion injury and may help to reduce the toxic effects of oxidative stress [6].

The inhibition of Acetylcholine release evoked by excitatory amino acids protects neurons against excitotoxicity [7]. In addition, Vinpocetine has been shown to inhibit c-GMP phosphodiesterase, which enhances c-GMP levels in the vascular smooth muscle, thus reducing the resistance of the blood vessels of the brain and increasing cerebral blood flow [8]. In some studies, Vinpocetine has demonstrated an antioxidant activity equivalent to that of Vitamin E [9].

Common Applications and Evidence

Common Applications and Evidence

Vinpocetine is widely used in the management of psychic and neurological symptoms (memory disorders, aphasia, apraxia, motor disorders, dizziness and headache) and acute and chronic cerebral circulatory disorders of various origins (post-apoplectic, post-traumatic or sclerotic). Vinpocetine improves collateral circulation (in ischemic brain damage, advanced brain damage and advanced cerebral arteriosclerosis) in the treatment of cerebral vascular insufficiency in patients with coronary heart disease and arterial hypertension (stroke). Vinpocetine is also used to treat acute and chronic ophthalmological diseases of various origins, providing an improvement in visual acuity in 70% of the patients treated. In otology, Vinpocetine can be used in vascular presbycusis, some toxic (iatrogenic) hearing impairments and vertigo of labyrinth origin.

Clinical evidence

There is strong evidence to support the use of Vinpocetine in the treatment of chronic ischemic cerebrovascular disorders and growing evidence suggests that it may also be beneficial in the treatment or prevention of acute ischemic stroke and various forms of dementia. Many clinical studies have indicated positive results in neurological symptoms and improvements in memory and other cognitive functions. Such results seem primarily attributable to the increase of capillary blood flow and cellular metabolism. This data has also been confirmed by neuropsychological tests, carried out to measure cerebral perfusion and parenchymal oxygen extraction, using Near Infrared Spectroscopy (NIRS), Transcranial Doppler (TCD) and Positron Emission Tomography (PET) methods [10,11,12].

Acute and chronic cerebrovascular disorders

Vinpocetine has been used successfully in the treatment of cerebrovascular disease, after intravenous and oral administration. The infusion of Vinpocetine was evaluated in a multicenter clinical epidemiology program including 4’865 patients suffering from chronic cerebrovascular insufficiency and arterial hypertension.

The data analysis revealed a significant decrease in patients’ complaints (p<0.001) and the severity of neurological symptoms (p<0.05) and an improvement in scores on the Tinnetti scale (p<0.001) and in the MMSE (p<0.001) [13]. In a recent clinical and instrumental study, the group of patients affected by Discirculatory Encephalopathy (DE), treated with Vinpocetine, reported improvements in all neurological syndromes. After 12 months, the use of Vinpocetine led to a significant decrease in the risk of DE progression, the development of transitory ischemic attacks and stroke in treated patients in comparison with the control group (the relative risks were 0.01 and 0.14 respectively) [14].

Cognitive functions and degenerative senile cerebral dysfunction

The clinical features of chronic cerebral hypoperfusion are the symptoms of cognitive impairment and organic psychiatric disorders of various origins (subcortical arteriosclerotic leucoencephalopathy, vascular dementia, Alzheimer’s disease, etc.). The mechanism of action of Vinpocetine interferes in many different ways with the biochemical and pathophysiological processes attributable to chronic cerebral hypoperfusion, irrespective of the cause of hypoperfusion [15].

A meta-analysis of six randomized, placed-controlled trials involving 731 patients with degenerative senile cerebral dysfunction showed that Vinpocetine was highly effective in the treatment of senile cerebral dysfunction, improving the patients’ cognitive performance and their ability to do daily activities. Using several psychometric testing scales, the researchers demonstrated that Vinpocetine has a highly significant effect on cognitive and motor functions as well as on physical symptoms (speech and movement capabilities, muscular coordination and strength, sensory-perceptual skills) [16,17].

Technical Description
Name of the plant Voacanga africana
Part of the plant used Seeds
Formula C22H20N2O2
IUPAC Name (3α,16α)-eburnamenine-14-carboxylic acid ethyl ester.
Synonyms Ethyl-apovincaminate; (3, 16) - Eburnamenine-14-carboxylic acid ethyl ester.
Molecular Weight 350.46 g/mol
CAS N. 42971-09-5

Structural Formula
Vinpocetine

Bibliografic References
  1. “Effects of vinpocetine on the redistribution of cerebral blood flow and glucose metabolism in chronic ischemic stroke patients: a PET study”. Journal of the Neurological Sciences 229-230: 275–84. (2005). Szilágyi G, Nagy Z, Balkay L, et al.
  2. “Neuroprotective effects of vinpocetine in vivo and in vitro. Apovincaminic acid derivatives as potential therapeutic tools in ischemic stroke” (in Hungarian). Acta Pharmaceutica Hungarica 72 (2): 84–91 (2002). Dézsi L, Kis-Varga I, Nagy J, Komlódi Z, Kárpáti E.
  3. “Vinpocetine. Monograph”. Alternative Medicine Review 7 (3): 240–3. (2002).
  4. “Vinpocetine inhibits NF-kappaB-dependent inflammation via an IKK-dependent but PDE-independent mechanism.”. Proceedings of the National Academy of Sciences of the United States of America 107 (21): 9795–800 (2010). Jeon, KI; Xu, X; Aizawa, T; Lim, JH; Jono, H; Kwon, DS; Abe, J; Berk, BC et al.
  5. “Vinpocetine as a potent antiinflammatory agent.” Proceedings of the National Academy of Sciences of the United States of America 107 (22): 9921–2 (2010). Medina, AE.
  6. Role of sodium channel inhibition in neuroprotection: effect of Vinpocetine. Brain Res Bull; 53:245-254 (2000). Bonoczk P, Gulyas B, Adam-Vizi V, et al.
  7. Antioxidants protect against glutamateinduced cytotoxicity in a neuronal cell line. J Pharmacol Exp Ther;250:1132-1140 (1989). Miyamoto M, Murphy TH, Schnaar RL, Coyle JT.
  8. Cyclic nucleotide phosphodiesterases: functional implications of multiple isoforms. Physiol Rev. 75:725-748 (1995). Beavo JA.
  9. Indole derivatives as neuroprotectants. Life Sci;65:1943- 1950 (1999). Stolc S.
  10. Cerebral effects of a single dose of intravenous vinpocetine in chronic stroke patients: a PET study. J Neuroimaging; 8:197- 204 (1998). Szakall S, Boros I, Balkay L, et al.
  11. Clinical and non-clinical investigations using positron emission tomography, near infrared spectroscopy and transcranial Doppler methods on the neuroprotective drug vinpocetine: a summary of evidences. J Neurol Sci.;203- 204:259-62 (2002). Vas A, Gulyás B, Szabó Z, Bönöczk P, Csiba L, Kiss B, Kárpáti E, Pánczél G, Nagy Z.
  12. Effect of parenteral or oral vinpocetine on the hemorheological parameters of patients with chronic cerebrovascular diseases. Phytomedicine 16, 111–117 (2009). Gergely Fehera,b, Katalin, Koltaib, GaborKesmarkyb, BeataHorvathb, KalmanTothb, Samuel Komolya, Laszlo Szaparya
  13. Efficacy of cavinton in the treatment of patients with chronic blood flow insufficiency. Russian multicenter clinicalepidemiological program “CALIPSO”. - Zh Nevrol Psikhiatr Im S S Korsakova.110(12):49-52 (2010). Chukanova E.
  14. Cavinton in the complex treatment of patients with chronic cerebrovascular insufficiency. Zh Nevrol Psikhiatr Im S S Korsakova.109(9):35-9 (2009). Chukanova EI
  15. The use of vinpocetine in chronic disorders caused by cerebral hypoperfusion. Orv Hetil.;142(8):383-9. (2001) Horváth S
  16. Investigation of the effect of vinpocetine on cerebral blood flow and cognitive functions. Ideggyogy Sz. Jul 30;60(7-8):301- 10 (2007). Valikovics
  17. Meta-analysis of Cavinton. Praxis. September 15;7(9):63-8. (1988) Nagy Z, Vargha P, Kovacs L, Bonoczk P.
  18. Summary of safety tests of ethyl apovincaminate. Arzneimittel-Forschung /Drug Research 26 (I), Nr. 10a (1976). E. Cholnoky and L. l. Dömök
  19. The safety and lack of efficacy of vinpocetine in Alzheimer’s disease. J Am Geriatr Soc;37:515-520. (1989) Thal LJ, Salmon DP, Lasker B, et al.

 

Vinpocetina

Linnea extracts and manufactures Vinpocetine as a botanical ingredient for psychic and neurological pharmaceutical purposes.