Abstracts
Cancer (Proanthocyanidins)
Cancer
The effect of dietary supplementation of flavonoidal compounds such as quercetin, rutin, luteolin and (+)-catechin on the incidence of fibrosarcoma induced by 20-methylcholanthrene (20-MC) in male Swiss albino mice was observed. Subcutaneous injection of 20-MC produced 100% tumor incidence and the onset of tumor appeared within 7 weeks. The compounds rutin and (+)-catechin did not influence tumor.
Elangovan-V; Sekar-N; Govindasamy-S: Chemopreventive potential of dietary bioflavonoids against 20-methylcholanthrene-induced tumorigenesis. Cancer-Lett. 1994 Nov 25; 87(1): 107-13.
Edema
Edema
An experimental investigation was made of the influence of 0-(beta-hydroxyethyl)-rutin (HR) on the effect of indomethacin (1, 2 or 4 mg/kg i.p.) in inhibiting rat paw edema. HR was given once daily during a 6-day pretreatment, with the final dose 90 minutes before the inflammatory reaction was induced. In the group of HR-pretreated rats which also received indomethacin in a dose of 2 or 4 mg/kg, the extent of the carrageenin-edema was diminished significantly in comparison to that in experimental animals treated merely with indomethacin.
Blazso-G; Gabor-M.: Influence of 0-(beta-hydroxyethyl)-rutin on the edema-inhibiting effect of indomethacin. Acta-Pharm-Hung. 1994 Jul; 64(4): 123-4.
Electrochemistry
Electrochemistry
The electrochemical properties of four structurally related flavonoids, quercetin, quercetin-3-O-rhamnose (quercitrin), quercetin-3-O-rutinose (rutin) and luteolin were investigated.
Hendrickson-HP; Kaufman-AD; Lunte-CE.: Electrochemistry of catechol-containing flavonoids. J-Pharm-Biomed-Anal. 1994 Mar; 12(3): 325-34.
Free Radicals (Proanthocyanidins)
Free Radicals
The abilities of 15 flavonoids as a scavenger of active oxygens (hydroxyl radical and superoxide anion) were studied. Hydroxyl radical (.OH) was generated by the Fenton system, and assayed by the determination of methanesulfonic acid (MSA) formed from the reaction of dimethyl sulfoxide (DMSO) with .OH. (+)-Catechin, (-)-epicatechin, 7,8-dihydroxy flavone, and rutin showed the .OH scavenging effect 100-300 times superior to that of mannitol, a typical .OH scavenger.
Hanasaki-Y; Ogawa-S; Fukui-S.: The correlation between active oxygens scavenging and antioxidative effects of flavonoids. Free-Radic-Biol-Med. 1994 Jun; 16(6): 845-50.
Toxicology (Proanthocyanidins)
Toxicology
Proanthocyanidins (PA) (condensed tannins) and hydrolyzable tannins (HT) are the two major classes of tannins. Proanthocyanidins are flavonoid polymers. Hydrolyzable tannins are polymers of gallic or ellagic acid esterified to a core molecule, commonly glucose or a polyphenol such as catechin. Proanthocyanidins are the most common type of tannin found in forage legumes.
Proanthocyanidins are considered to be non-toxic because they are not absorbed, but they are associated with lesions of the gut mucosa.
Nutritional toxicology of tannins and related polyphenols in forage legumes. Reed-JD J-Anim-Sci. 1995 May; 73(5): 1516-28.
Cardioprotective Effect
Cardioprotective effect
According to this study, grape seed-proanthocyanidins may have a cardioprotective effect against ischemia reperfusion injury. This substance was ingested orally by a group of rats. Another group served as a control during the trial. Proanthocyanidin-fed animals were resistant to myocardial ischemia reperfusion injury, and exhibited a reduced extent of myocardial infarction, as compared to the control group. As a result, proanthocyanidins may have cardioprotective activities and be beneficial to the human heart.
Sato M, Maulik G, Ray PS, Bagchi D, Das DK: Cardioprotective Effects of Grape Seed Proanthocyanidin Against Ischemic Reperfusion Injury, J Mol Cell Cardiol 1999 Jun; 31(6): 1289-1297
Chronic Venous Insufficiency
Chronic venous insufficiency
Treatment of oligomeric proanthocyanidins (Pycnogenols-OPC) may reveal a positive effect among patients with chronic venous insufficiency. In a clinical trial, patients with non-complicated chronic venous insufficiency were administered orally with Pycnogenols-OPC. Over 80% of the patients had experienced significant improvements with no itching and pain. Only minor swelling of the lower limbs occurred. No adverse side effects were reported. This supplement may alleviate patients' symptoms due to chronic venous insufficiency.
Costantini A, De Bernardi T, Gotti A: Clinical and capillaroscopic evaluation of chronic uncomplicated venous insufficiency with procyanidins extracted from vitis vinifera, Minerva Cardioangiol 1999 Jan-Feb; 47(1-2): 39-46
Oxidative Stress & Grape Seed Extract
Oxidative stress
Proanthocyanidins found in grape seed extract may reduce oxidative stress and protect heart cells from injury, according to this study. Researchers exposed chick heart cells to antimycin A, a drug known to stimulate oxidative stress in the mitochondria of the cell, with or without grape seed extract. The degree of oxidation could be determined by the florescence of an attached marker - higher oxidation results in more florescence. After two hours of antimycin A exposure, cells that were treated with grape seed extract exhibited less oxidative stress and cell death than non-treated heart cells.
Shao ZH, et al: Grape seed proanthocyanidins reduce oxidant stress in cardiomyocytes, Acad Emerg Med 2001 May;8(5):562
Organ Toxicity
Organ Toxicity
Grape seed extract may protect organ-specific cells against chemical-induced damage, according to this study conducted in mice. Half of the test animals received oral grape seed proanthocyanidin extract for 7-10 days prior to chemical exposure. All mice then received chemicals known to damage certain organs: acetaminophen (liver), amiodarone (lungs), doxorubicin (heart), cadmium chloride (kidneys) or dimethylnitrosamine (brain), and were then tested for chemical-induced biological changes to the specific organ involved. Grape seed extract preexposure dramatically decreased chemical signs of organ toxicity, and organ analysis revealed inhibition of cell death and DNA damage. However, grape seed extract only partially protected brain tissue.
Bagchi D, Ray SD, Patel D, Bagchi M: Protection against drug- and chemical-induced multiorgan toxicity by a novel IH636 grape seed proanthocyanidin extract, Drugs Exp Clin Res 2001;27(1):3-15
Anti-Apoptotic Mechanism
Anti-Apoptotic mechanism
Grape seed proanthocyanidins (GSPE) may prevent chemotherapy-induced damage of cells by affecting the regulation of several genes associated with apoptosis, according to this study. Cells treated with chemotherapeutic agents were exposed to GSPE in order to elucidate its protective mode of action. RT-PCR analysis revealed a subsequent increase in Bcl-2, an anti-apoptotic gene, and decreases in two proapoptotic genes, c-myc and p53. The authors suggest that GSPE may protect normal cells by preventing the apoptosis that ensues after exposure to chemotherapeutic toxins.
Joshi SS, Kuszynski CA, Bagchi D: The cellular and molecular basis of health benefits of grape seed proanthocyanidin extract, Curr Pharm Biotechnol 2001 June;2(2):187-200
Cardiomyocyte Protection
Cardiomyocyte protection
Grape seed proanthocyanidin extract (GSPE) may protect cardiomyocytes from ischemic injury by acting as an in vivo antioxidant, according to this animal study. Rats were given either a regular diet or a diet supplemented with oral doses of GSPE for three weeks. The rats were then sacrificed and their hearts were perfused. Ischemic injury was then inflicted on the hearts for 30 minutes, followed by 2 hours of reperfusion.
It was found that GSPE inhibited the induction of proapoptotic genes and therefore reduced the number of apoptotic cells in the myocardium. It also decreased the production of reactive oxygen species in the heart and improved postischemic contractile function.
Sato M, Bagchi D, Tosaki A, Das DK: Grape seed proanthocyanidin reduces cardiomyocyte apoptosis by inhibiting ischemia/reperfusion-induced activation of JNK-1 and C-JUN, Free Radic Biol Med 2001 Sep 5;31(6):729-37
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