PDR for Herbal Medicines

HERBAL MONOGRAPHS GRAPE/363

Flower and Fruit: The flowers are in compound compact

panicles. The petals are about 5 mm long and droop like the

sepals. The fruit is oblong to globular. 6 to 22 mm long, dark

blue-violet, red, green or yellow, juicy, sweet or sour. The

seeds are pear-shaped, with hard skin and two long dimples

on the side.

ACTIONS AND PHARMACOLOGY

COMPOUNDS

Flavonoids (4 to 5%): including. kaempferol-3-O-gluco-

4p" sides, quercetin-3-O-glucosides

Tannins: procyanidolic oligomers (proanthocyanidins), in-

cluding constituent monomers of catechin epicatechin

Non-flavonoids (Stilbenes): resveratrol and viniferins

Fruit acids: including, tartaric acid, malic acid, succinic

acid, citric acid, oxalic acid

Phenylacrylic acid derivatives: p-cumaroyl acid, caffeoyl

acid, feruloylsuccinic acid

EFFECTS

Antiatherosclerotic Effects: The oxidation of low-density

lipoproteins (LDL) by free radicals is associated with the

initiation of atherosclerosis. Proanthocyanidin decreases the

number of LDL-positive macrophage-derived foam cells in

atherosclerotic lesions. The compound also inhibits the

oxidation of cholesteryl linoleate in LDL to exert a reduction

in atherosclerosis of the aorta (Nuttall, 1998, Yamakoshi,

1999).

^ Anticarcinogenic/Antitumor: Chemoprotective properties of
proanthocyanidins include activity against free radicals and
oxidative stress (Ye, 1999). The anti-tumor-promoting acitv-
ity due to strong antioxidant effects of the compound has
been demonstrated in animal models (Zhao, 1999).
Antioxidant Effects: Proanthocyanidin from the Grape Seed
extract exerts a concentration-dependent inhibition of oxy-
gen free radicals. In one study, the antioxidant effect of
proanthocyanidin was more potent compared to vitamin C

and vitamin E succinate (Bagchi, 1997). The compound also

inhibits peroxidation of phosphatidylcholine liposomes

(Plumb, 1998).

Hair Growth: Proanthocyanidins extracted from Grape

Seeds promote proliferation of hair follicle cells, and possess

remarkable hair-cycle converting activity from the telogen

phase to the anagen phase. Epicatechin and catechin are the

constitutive monomers inducing the degree of polymeriza-

tion inducing hair growth (Takahashi, 1998).

Hepatoprotective Effects: Proanthocyanidin has been shown

to significantly attenuate acetaminophen induced hepatic

DNA damage, apoptosic and necrotic cell death of liver

cells. The component also antagonizes acetaminophen in-

duced changes in bcl-Xl expression (Ray, 1999).

Ischemia Prevention: Maintenance of microvascular injury

by procyanidins occurs through the scavenger effect of

reactive oxygen species (Maffei Facino, 1994). Procyanidins

also reduce ventricular contraction in a dose-dependent

fashion. Procyandins decrease coronary perfusion pressure

and improve cardiac mechanical performance. (Maffei Faci-

no R, 1996).

Vascular Effects: Procyanidins isolated from Grape Seed

stabilizes capillary walls and prevents increases in perme-

ability which inhibits edema (Robert, 1990; Zafirov, 1990).

Overproduction of hyaluronan content associated with patho-

logic venous walls, in particular vein-lymphatic edema, is

decreased by procyanidolic oligomers (Drubaix, 1997).

Procyanidolic oligomers cross-link collagen fibers, resulting

in reinforcement of the natural cross-linking of collagen that

forms the collagen matrix of vascular connective tissue

(Tixier et al, 1984). The vascular activity of procyanidin has

positive effects on diabetic retinopathy, night vision and

ocular stress (Boissin, 1988; Corbe, 1988; Soyeux, 1987).

CLINICAL TRIALS

Peripheral Venous Insufficiency

The efficacy of Grape Seed extract was evaluated for the

treatment of venous insufficiency and symptoms due to

hormonal supplementation. Grape Seed extract (150 mg

twice daily) was administered to 4,729 patients in an open-

label study. Peripheral venous insufficiency was evaluated

45 and 90 days after treatment. The efficacy score was based

on symptoms of nocturnal cramps, paresthesias, sensation of

warmth, cyanosis and edema. The sensation of heaviness in

the legs decreased in 57% of cases by day 45 and 89.4% by

day 90. In addition, the improvement of symptoms occurred

in 66% of cases by day 45 and 79-83% of cases by day 90

(Henriet, 1993).

Leaves, Stem and Root: The vine is a 30 cm high climber

with deep, heavily-branched roots and a woody trunk. The

trunk has striped, loose bark. The brown-red to brown-

yellow branches are glabrous or slightly downy and finely

grooved. The leaves are orbicular, generally in 3 to 5 lobes

or blades. They are deeply notched at the stem. The upper

surface of the leaves is glabrous, the under surface is lanate.

Habitat: The plant is indigenous to southern Europe and

western Asia and is cultivated today in all temperate regions

of the world.

Production: Vine leaves are the foliage leaves of Vitis

vinifera.