Proanthocyanidins (Pine Bark & Grape Seed Extracts)

Plant extract with a proanthocyanidins contentas therapeutic agent having radical scavenger effect and use thereof

Masquelier J. U.S. Patent No. 4,698,360; 1987

The invention provides a method for preventing and fighting the harmful biological effects of free radicals in the organism of warm blooded animals and more especially human beings, namely cerebral involution, hypoxia following atherosclerosis, cardiac or cerebral infarction, tumour promotion, inflammation, ischeamia, alterations of the synovial fluid, collagen degradation, among others. The method consists in administering to said animals and especially human beings an amount efficient against said effects, of a plant extract with a proanthocyanidins content which has a radical scavenger effect, the extract being in the form of a medicament and coming more especially from the bark of conifers.
 

Evaluation of venotropic drugs by venous gas plethysmography. A study of procyanidolic oligomers

Royer R.J., Schmidt C.L. Sem Hop Paris 1981;57:2009-2013

Venous tone in the lower limbs can be measured be venous occlusion gas plethysmography before and after giving venotropic drugs. Four groups, each of which included ten patients with widespread varicose veins, were given different medications. Each patient was studied by plethysmography during the first five hours following drug ingestion. In untreated controls, venous tone decreased during rest. A reference drug was uneffective. Increase in venous tone induced by 150 mg of procyanidolic oligomers was comparable to that which followed ingestion of a high dose of hamamelis-hydrastis mixture.
 

Antiinflammatory and superoxide radical scavenging activities of a procyanidins containing extract from the bark of Pinus pinaster Sol. and its fractions

Blazsó G., Gábor M., Sibbel R., Rohdewald P. Pharm Pharmacol Lett 1994;3:217-220

The antiinflammatory and free radical scavenging activities of a procyanidins containing extract from the bark of Pinus pinaster Sol. and its fractions were studied. The extract and each of its fractions showed remarkable activity in scavenging superoxide anion radicals. The i.p. administered extract and its fractions were found to decrease the mouse ear edema induced with croton oil statistically significantly in a dose-dependent manner. The extract and the fraction of oligomeric procyanidins decreased inflammation in the mouse ear to a stat. significant degree after oral application. The antiinflammatory and free radical scavenging activities of the fractions were closely correlated (r=0,992).
 

Dietary grape seed tannins affect lipoproteins, lipoprotein lipases and tissue lipids in rats fed hypercholesterolemic diets.

Tebib K., Besançon P., Rouanet J.-M. J Nutr 1994;124:2451-2457

The effects of monomeric and polymeric grape seed tannins on rat plasma lipoproteins, lipoprotein lipase, hepatic lipase and aortic and hepatic lipid concentration were studied. Male Sprague-Dawley rats received either a normal diet (with no added cholesterol and no tannins), a control diet (hypercholesterolemic diet) or hypercholesterolemic diets supplemented with 2% tannin monomers or 2% polymers 3 or 9 wk. Plasma total cholesterol, triacylglycerol, LDL cholesterol and VLDL concentrations were significantly higher and the HDL cholesterol concentration lower in controls and in rats fed the diet supplemented with monomers compared with rats fed polymeric tannins at both time points. Lipoprotein lipase and hepatic lipase activities were significantly higher in control and in monomer-fed groups than in the polymer-fed group. Hepatic and aortic cholesterol and triacylglycerol concentrations were significantly higher in control rats and those fed monomers than in the polymer-fed group. Moreover, plasma HDL cholesterol and hepatic lipase activity were closely associated with low aortic cholesterol and triacylglycerol in rats fed polymeric tannins. These rats also exhibited greater fecal excretion of cholesterol and especially bile acids than the control or monomer-fed groups. Thus dietary grape seed tannins have a pronounced anti-hypercholesterolemic effect by enhancing reverse cholesterol transport and also by reducing intestinal cholesterol absorption and increasing bile acid excretion Article.
 

Action of procyanidolic oligomers on vascular permeability. A study by quantitative morphology

Robert L., Godeau G., Gavignet-Jeannin C., Groult N., Six C., Robert A.M. Path Biol 1990;38:608-616

In normal conditions, vascular permeability is precisely regulated by mechanisms which involve among others the macromolecules of extracellular matrix of the vascular wall. Permeability for a given substance will vary according to the anatomical localisation of the vessel determining also its structure and composition. In some pathological conditions, such as inflammation or diabetes, permeability can be abnormally increased. Increased permeability can be reproduced by i.v. collagenase injection. This permeability increase can be quantified by image analysis using appropriate tracers such as FITC-dextrans of horse-radish peroxidase, on histological sections from control and collagenase treated rats, pretreated or not with procyanidolic oligomers (PCO). We studied cerebral capillaries, aorta and cardiac muscle capillaries. It could be shown that previous treatment of animals with procyanidolic oligomers prevented the permeability increase produced by collagenase injection.
 

Effect of Endotelon (Procyanidolic oligomers) on experimental acute lymphedema of the rat hindlimb

Doutremepuich J.D., Barbier A., Lacheretz F. Lymphology 1991;24:135-139

Endotelon (Procyanidolic Oligomers, Sanofi-Labaz Laboratories) are recognized "angioprotectors" for human venous insufficiency. Using an operative experimental model of lymphedema, we sought pharmacological evidence for potential lymphagogue activity of Endotelon. After surgical interruption of hindlimb lymphatics, rats developed for 7 days, peripheral edema that represented a mean 24% increase in volume compared to the nonoperated hindlimb (control). In this experimental counterpart of lymphedema, Endotelon (400 mg/kg/day p.o.) administered "prophylactically" (i.e., before, during, and 7 days after development of lymphedema) decreased rat hindlimb lymphedema by ~47%. When administered just before lymphedema became established (i.e., curatively), Endotelon and Coumarin (another "angioprotector") failed to affect hindlimb edema.
 

Evidence by in vivo and in vitro studies that binding of pycnogenols to elastin affects its rate of degradation by elastases

Tixier J.M., Godeau G., Robert A.M., Hornebeck W. Biochem Pharmacol 1984;33:3933-3939

Procyanidol oligomers and (+)catechin bound to insoluble elastin markedly affects its rate of degradation by elastases. Insoluble elastin pretreated with procyanidol oligomers (PCO) was resistant to the hydrolysis induced by both porcine pancreatic and human leukocyte elastases. The quantitative adsorption of pancreatic elastase was similar on either untreated or PCO-treated elastin suggesting that the binding of this compound to elastin increases the non-productive catalytic sites of elastase molecules. (+)Catechin-insoluble elastin complexes were partially resistant to the degradation induced by human leukocyte elastase but were hydrolysed at the same rate as untreated samples by a constant amout of pancreatic elastase. In addition, the coacervation profile of kappa-elastin peptides as a function of temperature is greatly modified in presence of these flavonoids. We conclusively evidenced that PCO's bind to skin elastic fibers when injected intradermally into young rabits. As a result, these elastic fibres were found more resistant to the hydrolytic action of porcine pancreatic elastase when injected into the same site. These in vivo studies further emphasized the potential effect of these compounds in preventing elastin degradation by elastase(s) as occurred in inflammatory processes.