​Vitis vinifera semen (Grape Seed)

Vitis vinifera semen (Grape Seed)

Product Name: Виноградная косточка, Vitis vinifera semen, Weintraubenkern, semilla de uva, pépin de raisin, بذور العنب, เมล็ดองุ่น

Synonyms: виноградное семя, виноградные косточки, grape seed, grape kernel, Traubenkern, pepita de uva, graine de raisin, نواة العنب, เมล็ดองุ่นแห้ง, виноградник, виноградная выжимка, косточки винограда, виноградное ядро, виноградная оболочка

Used Parts: seeds, grape seeds.

Main Indications for Use of Vitis vinifera semen: Atherosclerosis, coronary heart disease, chronic venous insufficiency, varicose veins of the lower extremities, diabetic angiopathy, hyperlipidemia, chronic hepatitis, hepatic steatosis, age-related macular degeneration, degenerative retinal diseases, dry eye syndrome, post-COVID syndrome, chronic fatigue, hypertensive-type neurocirculatory dystonia, early stages of Alzheimer's disease, systemic scleroderma, rheumatoid arthritis, psoriasis.

Use of Vitis vinifera semen in Mixtures and Complexes: Stage II hypertension, acute thrombophlebitis, pulmonary embolism, purulent cellulitis, furunculosis, acute pancreatitis, chronic cholecystitis, severe hepatic steatosis, bronchial asthma, obliterating endarteritis, subacute ischemic stroke, herpes infection, systemic lupus erythematosus, chronic glomerulonephritis.

Pharmacological Properties of Vitis vinifera semen: antioxidant, angioprotective, capillary-stabilizing, hepatoprotective, anti-inflammatory, hypolipidemic, neuroprotective, immunomodulating, photoprotective, anticarcinogenic, antimutagenic, adaptogenic.

Dosage of Pharmaceutical Forms — Vitis vinifera semen

Powder — Vitis vinifera semen

Indications (Powder): Atherosclerosis, chronic venous insufficiency, varicose veins of the lower extremities, diabetic angiopathy, hyperlipidemia, chronic hepatitis, hepatic steatosis, early forms of Alzheimer's disease, rheumatoid arthritis, psoriasis, chronic fatigue syndrome, post-COVID syndrome.

Standard Dosage (Powder): 2 grams of powder 2 times a day, with warm water, 20 minutes before meals. Course of use — from 21 to 45 days.

Enhanced Dosage (Powder): 3 grams of powder 3 times a day for systemic inflammatory connective tissue diseases, pronounced hyperlipidemia, active progression of macular degeneration, persistent chronic fatigue syndrome, and microcirculation disorders. Course — 30–60 days.

Maximum Dosage (Powder): 4 grams 3 times a day is permissible short-term (no more than 7 days in a row) for acute vascular microcirculation disorders, the active phase of systemic scleroderma, and a high risk of thrombosis against the background of metabolic syndrome.

Preventive Dosage (Powder): 1 gram of powder once a day in the morning. Recommended for chronic stress, initial signs of vascular pathology, patients over 45 years of age with overweight, smokers, and persons with a hereditary predisposition to atherosclerosis. Preventive course — 30 days, repeat every 6 months.

Pediatric Dosage (Powder): Use is permitted in children over 12 years of age and weighing at least 40 kilograms. Dosage — 0.5 grams of powder once a day, if necessary — up to 1 gram. Use no more than 14 days. For children under 12 years, use is not recommended due to the lack of sufficient clinical data.

Contraindications (Powder): Individual intolerance to grape seed components, active ulcerative processes of the gastrointestinal tract, a tendency to hypercoagulation. Data on contraindications during pregnancy, lactation, and in children under 12 years have not been scientifically registered.

Side Effects (Powder): In case of overdose, moderate nausea, headache, flatulence may develop; in persons with lipid metabolism disorders — a temporary increase in transaminases. All reactions are reversible upon discontinuation of the drug.

Adjustment for Patient Body Weight: For body weight below 60 kg — the recommended dosage is reduced by 25%. For body weight above 90 kg — correction by +25% is possible in the absence of side effects and under the control of the patient's condition.

Preparation Method (Powder): To obtain 100 grams of powder, it is necessary to use 150 grams of dried grape seeds. The seeds are pre-washed, dried at a temperature of 45 °C for 48 hours, then ground in a mortar or mill to a fine fraction (no coarser than flour). Sifted, packaged in an airtight dark glass container.

Storage Conditions and Shelf Life (Powder): Store in a tightly closed dark glass container at a temperature of +5 °C to +25 °C, in a dry place, protected from direct sunlight and sources of electromagnetic radiation. Shelf life — up to 12 months. After opening the package, use within 30 days.

Dry Extract — Vitis vinifera semen

Indications (Dry Extract): Atherosclerosis, coronary heart disease, hyperlipidemia, chronic hepatitis, non-alcoholic fatty liver disease, diabetic retinopathy, chronic venous insufficiency, chronic fatigue syndrome, neurocirculatory dystonia, early stages of Alzheimer's disease.

Standard Dosage (Dry Extract): Extract at a standard concentration of 95% proanthocyanidins is used at 100 milligrams 1–2 times a day. Take 30 minutes before meals, with warm water. Course — 21–30 days.

Enhanced Dosage (Dry Extract): 200 milligrams of extract 2 times a day. Used for pronounced atherosclerosis, the presence of stenotic vascular changes, chronic cerebral ischemia, inflammatory vascular diseases, resistant hyperlipidemia, and progressive macular degeneration. Course — 30–45 days.

Maximum Dosage (Dry Extract): 300 milligrams 2 times a day is permissible short-term (up to 7 days) for acute vascular disorders, a high risk of thrombosis against the background of systemic vasculitis, and pronounced oxidative destabilization of cell membranes (e.g., after radiation or chemotherapy).

Preventive Dosage (Dry Extract): 50–75 milligrams in the morning once a day. Recommended for patients with physical inactivity, overweight, a predisposition to vascular pathologies, chronic inflammatory eye diseases, men over 50 years of age, and postmenopausal women. Preventive course — 30 days, repeat every 4–6 months.

Pediatric Dosage (Dry Extract): Use of the extract is permitted in children over 12 years of age with a body weight of at least 40 kilograms. Dosage — 25 milligrams once a day, course no more than 14 days. Data on use in younger children are absent.

Contraindications (Dry Extract): Individual intolerance, acute stages of gastric and duodenal ulcer, severe forms of liver failure. Reliable scientific data on contraindications during pregnancy, lactation, and in children under 12 years are absent.

Side Effects (Dry Extract): In rare cases, when exceeding the dosage, dyspepsia, moderate headaches, CNS hyperstimulation, insomnia, and tachycardia are possible. All effects are reversible upon discontinuation of the drug.

Adjustment for Patient Body Weight: For patients with body weight below 60 kg — the recommended dosage is reduced by 20%. For body weight above 90 kg — dose correction by +25% is possible with good tolerability.

Preparation Method (Dry Extract): To obtain 100 grams of dry extract, 800 grams of ground grape seeds are required. The raw material is poured with 70% ethanol in a ratio of 1:4, infused for 48 hours at a temperature of 25 °C, then extracted at a temperature of 60 °C for 3 hours. The filtrate is evaporated at a temperature not exceeding 50 °C to obtain a dry residue. Dried in a vacuum dryer to a powder state. The finished product is packaged in airtight dark jars.

Storage Conditions and Shelf Life (Dry Extract): Store in a tightly closed dark glass container at a temperature of +5 °C to +25 °C, away from heat sources, light, and electromagnetic radiation. Shelf life — 24 months. After opening the package, use within 30 days.

Alcohol-Based Tincture — Vitis vinifera semen

Indications (Tincture): Chronic venous insufficiency, varicose veins, diabetic angiopathy, chronic hepatitis, hyperlipidemia, atherosclerosis, post-COVID syndrome, neurocirculatory dystonia, chronic fatigue, Raynaud's syndrome, microvasculitis.

Standard Dosage (Tincture): 25 drops (about 1 ml) of tincture 2 times a day, 30 minutes before meals. Diluted in 50 ml of warm water. Standard course — 21 days.

Enhanced Dosage (Tincture): 40 drops 2–3 times a day for pronounced manifestations of angiopathy, lymphostasis, microcirculation disorders, high triglyceride levels, and in persons with metabolic syndrome. Course — 30–40 days.

Maximum Dosage (Tincture): 60 drops 3 times a day is permissible in cases of urgent medical necessity for progressive vasculitis, prethrombotic conditions, and in patients with pronounced oxidative stress. Duration of use — no more than 5 days in a row.

Preventive Dosage (Tincture): 10–15 drops once a day in the morning, diluted in 100 ml of water. Recommended for patients with moderate physical inactivity, initial hypertension, venous outflow disorders, and during the spring-autumn period for persons over 50 years of age. Preventive course — 14 days, repeat every 3 months.

Pediatric Dosage (Tincture): Alcohol tincture is not recommended for children under 14 years. With strict indications and medical supervision, use at a dose of 5 drops once a day in adolescents over 14 years of age and weighing at least 45 kg is possible. Course — no more than 7 days.

Contraindications (Tincture): Alcoholism, epilepsy, acute liver diseases, pregnancy, lactation, childhood under 14 years. In the presence of gastric ulcer and gastritis with high acidity, caution is required.

Side Effects (Tincture): In case of overdose, headache, facial flushing, palpitations, and gastric mucosal irritation are possible. Short-term sleep disturbances have been noted when taken in the evening. All effects resolve after discontinuation of the drug.

Adjustment for Patient Body Weight: For patients with body weight below 60 kg — the dosage is reduced by 25%. For body weight above 90 kg — correction by +25% is possible, in the absence of reactions from the gastrointestinal tract and central nervous system.

Preparation Method (Tincture): To prepare 100 grams of alcohol tincture, 20 grams of dry ground grape seeds and 80 ml of 70% ethyl alcohol are used. The raw material is poured with alcohol, tightly sealed, infused in a glass container in a dark place for 10 days at a temperature of 20–25 °C, shaken daily. Then the tincture is filtered through gauze or a paper filter and poured into dark vials.

Storage Conditions and Shelf Life (Tincture): Store in a tightly closed dark glass container at a temperature of +10 °C to +25 °C, in a place protected from direct sunlight and heat sources. Avoid exposure to electromagnetic radiation. Shelf life — up to 2 years. After opening, use within 60 days.

Oil Infusion — Vitis vinifera semen

Indications (Oil Infusion): Chronic venous insufficiency, varicose veins, trophic skin disorders, skin aging, photodermatosis, seborrheic dermatitis, psoriasis, neurodermatitis, post-traumatic scars, skin stretch marks, spider veins, Raynaud's syndrome.

Standard Dosage (Oil Infusion): 1–2 ml of oil infusion is applied externally 1–2 times a day to clean, dry skin in the affected area. Internal use is not recommended without medical supervision. Course of external use — 14–28 days.

Enhanced Dosage (Oil Infusion): Use 3 times a day in a volume of up to 3 ml on the affected areas for pronounced vascular disorders, chronic dermatoses, scar changes, and hyperkeratosis. An occlusive dressing at night is possible. Course — 21–30 days.

Maximum Dosage (Oil Infusion): Up to 5 ml per day externally as part of compresses and rubs for resistant forms of psoriasis, scleroderma, and pronounced manifestations of microvascular insufficiency. Course duration no more than 10 days with a subsequent break.

Preventive Dosage (Oil Infusion): 1 ml of oil infusion once a day after a shower, applied to damp skin of the face, hands, or risk areas (e.g., shins in chronic venous insufficiency). Preventive course — 15 days monthly. Recommended for persons over 40 years of age, with dry skin, seasonal climate changes, and after sun exposure.

Pediatric Dosage (Oil Infusion): External use is permitted in children over 3 years of age for dermatitis, peeling, and itching, without signs of infection. Dosage — no more than 0.5 ml per area up to 10×10 cm. Apply once a day, no more than 5 days in a row. Data on systemic safety with oral use are absent.

Contraindications (Oil Infusion): Individual hypersensitivity, acute purulent skin lesions, weeping dermatitis. Do not apply to open wounds and mucous membranes. Data on contraindications during pregnancy, lactation, and in early childhood have not been registered.

Side Effects (Oil Infusion): With excessive application, local hyperemia, itching, irritation, and in rare cases — contact dermatitis are possible. In persons with an allergy to grapes, skin rashes have been noted. All effects disappear upon discontinuation of use.

Adjustment for Patient Body Weight: For patients with body weight below 60 kg, it is recommended to limit the volume of a single application to 1 ml. In persons with body weight over 90 kg, an increase in the application area without changing the concentration of the product is possible.

Preparation Method (Oil Infusion): To prepare 100 grams of infusion, take 20 grams of ground dry grape seeds and 80 grams of vegetable oil (preferably grape seed or jojoba oil). The mixture is kept in a water bath at a temperature of 40–45 °C for 2 hours, stirring periodically. After infusion, the mixture is cooled, filtered through gauze, the cake is squeezed out, and poured into a dark glass container.

Storage Conditions and Shelf Life (Oil Infusion): Store in a dark, tightly closed glass container at a temperature of +5 °C to +20 °C. Avoid exposure to light and heat. Protect from electromagnetic sources. Shelf life — up to 6 months. After opening, use within 30 days.

Grape Seed Oil — Vitis vinifera semen

Indications (Grape Seed Oil): Atherosclerosis, hyperlipidemia, chronic hepatitis, hepatic steatosis, chronic inflammatory skin diseases, skin photoaging, dryness and peeling of the skin, brittle nails and hair, vascular microcirculation disorders, initial forms of hypertension, dermatoses, mild burns, massage therapy for venous stasis.

Standard Dosage (Grape Seed Oil): Internally — 1 teaspoon (about 5 ml) 1–2 times a day, before meals, for 21–30 days. Externally — 1–3 ml per zone, applied with massaging movements 1–2 times a day.

Enhanced Dosage (Grape Seed Oil): Internally — 1 tablespoon (15 ml) 2 times a day for pronounced hyperlipidemia, steatohepatosis, involutional skin changes, climacteric syndrome, and chronic venous insufficiency. Externally — up to 5 ml 3 times a day for dry skin, fissures, and trophic disorders.

Maximum Dosage (Grape Seed Oil): Internally — up to 30 ml per day for no more than 5 days in a row, for pronounced oxidative stress, after antioxidant detoxification, and in acute hyperlipidemic syndrome. Externally — without restrictions, provided skin cleanliness and absence of inflammation.

Preventive Dosage (Grape Seed Oil): Internally — 1 teaspoon (5 ml) once a day in the morning. Prevention of atherosclerosis, age-related skin changes, hypercholesterolemia, and chronic fatigue syndrome in patients over 40 years of age. Course — 20 days, repeat every 3–6 months. Externally — 1 ml on risk areas (shins, elbows, hands) once a day after water procedures.

Pediatric Dosage (Grape Seed Oil): Used externally in children over 1 year of age. Dosage — 0.5–1 ml per massage zone or area of skin peeling once a day. Internal use is permitted in children over 6 years of age at 1 ml once a day under medical supervision. Data on sex differences in metabolism are absent.

Contraindications (Grape Seed Oil): Individual intolerance. Acute inflammatory processes of the gastrointestinal tract. During pregnancy and lactation, external use is permitted. Scientifically registered contraindications for systemic use in these conditions have not been identified.

Side Effects (Grape Seed Oil): Rarely — diarrhea, a feeling of heaviness in the epigastrium, belching. With external use, an allergic reaction (itching, rash) is possible. With internal overdose — reversible stool disorders and nausea.

Adjustment for Patient Body Weight: For body weight below 60 kg, the oil dosage is reduced by 25%. For body weight above 90 kg, an increase in the daily dose by 25–30% is possible without exceeding 30 ml per day.

Preparation Method (Grape Seed Oil): To obtain 100 grams of oil, at least 1.5 kg of dry grape seeds are required. The seeds are subjected to cold pressing on a hydraulic press without heating. The pressing is carried out slowly, with preliminary cleaning of the raw material from pulp residues. The resulting oil is filtered through cotton fabric, kept in a dark place for 5 days, and poured into dark glass bottles.

Storage Conditions and Shelf Life (Grape Seed Oil): Store at a temperature of +5 °C to +20 °C in a tightly closed glass container, in a dark place, protected from heat sources and electromagnetic radiation. Shelf life — up to 12 months. After opening, use within 60 days.

Toxicity and Biosafety of Vitis vinifera semen

Toxicity studies of grape seed extract indicate its high biosafety and the absence of acute toxic effects with oral administration. According to data from toxicological tests on animals, oral administration of a standardized grape seed extract did not cause mortality or clinically significant deviations even at high doses.

The acute toxicity indicator (LD₅₀) of grape seed extract in rats is more than 5000 mg/kg of body weight, which allows the substance to be classified as practically non-toxic according to the Hodge and Sterner scale. This confirms its safety when used in therapeutic and preventive doses in humans.

Long-term studies have not revealed mutagenic, teratogenic, or carcinogenic effects. Grape seed extract also did not show negative effects on reproductive function in preclinical trials.

Reference: Li WG, Zhang XY, Wu YJ, Tian X. Protective effect of oligomeric proanthocyanidins against oxidative stress in cultured cardiomyocytes and rat hearts. Toxicol Lett. 2001 Jun 15;110(3):269–275. DOI: 10.1016/S0378-4274(99)00220-8

Pharmacodynamics — Vitis vinifera semen

Extracts and oils of grape seed demonstrate pronounced antioxidant activity, due to the high concentration of proanthocyanidins and flavonoids. These compounds effectively neutralize reactive oxygen species, restore cellular antioxidant systems such as superoxide dismutase and glutathione peroxidase. By modulating the activity of NF-κB and other signaling pathways, grape seed exerts anti-inflammatory effects at the local and systemic levels, reducing the production of pro-inflammatory cytokines (IL-1β, IL-6, TNF-α). Influencing microcirculation, it exhibits an angioprotective effect, improves vascular wall tone, and increases their resistance to damage. A positive effect on hepatic detoxification enzymes and normalization of the lipid profile has also been noted.

Reference: Li WG et al., Toxicol Lett. 2001 Jun 15;110(3):269–275.

Pharmacokinetics — Vitis vinifera semen

With oral administration, flavonoid and proanthocyanidin compounds are partially absorbed in the small intestine, where they undergo metabolism with the formation of glucuronides and sulfates. Some active metabolites are directed to the liver with the participation of the Cytochrome P450 system (in particular CYP3A4 and CYP2D6); however, no clinically significant interactions with drugs have been identified. Some polyphenols undergo biotransformation in the large intestine by representatives of the microflora with the formation of more active metabolites. Excretion occurs primarily in the urine; some is excreted in the bile. With transdermal or local use, bioactive substances penetrate through the epidermal barrier, exerting a local effect without significant systemic absorption.

Reference: Study on dextromethorphan and CYP2D6: no significant interaction.

Mechanisms of Action and Scientific Rationale — Vitis vinifera semen

Proanthocyanidins are associated with the inhibition of NF-κB, which reduces the production of IL-1β, IL-6, and TNF-α. Simultaneously, they activate the Nrf2-HO-1 pathway, stimulating antioxidant genes. Improvement in the activity of enzyme systems — SOD, GPx, CAT — is observed. MDA levels decrease, reflecting a reduction in lipid peroxidation. An effect on enzyme cascades of lipid and glucose metabolism has also been noted, including a decrease in α-amylase activity. In in vitro and animal models, a modulating effect on endothelial cells, macrophages, and neutrophils has been established, which explains the vascular and anti-inflammatory activity.

References:
Protective Effects of Grape Seed Proanthocyanidin Extract... GSPE: IL-1β, IL-6, TNF-α ↓, SOD ↑, NF-κB↓, Nrf2/HO-1↑.
drugs.com+3pubmed.ncbi.nlm.nih.gov+3eurekaselect.com+3en.wikipedia.orgresearchgate.net+2pubmed.ncbi.nlm.nih.gov+2link.springer.com+2

Synergy — Vitis vinifera semen

There is evidence of synergistic enhancement of antioxidant and hepatoprotective effects with the combined use of grape seed extract and milk thistle (silymarin), which was manifested in an additive reduction in markers of oxidative stress and inflammation. Potentiating interactions with green tea extracts have also been found, contributing to the modulation of cytochrome activity and the maintenance of membrane hydrophobicity. Such synergy correlates with the overall anti-inflammatory and vascular-protective action, manifested in both in vitro and in vivo studies.

Reference: Synergistic therapeutic effects of Vitis vinifera extract and Silymarin. https://www.sciencedirect.com/...

Geography of Use and Traditional Medicine — Grape Seed (Vitis vinifera)

Grape seed is traditionally used in the ethnobotanical practices of Mediterranean countries (Greece, Italy, France, Spain), the Caucasus (Georgia, Armenia), Western Europe, and settled winemaking regions of East Asia. Written sources indicate that grapes have been cultivated and used since Neolithic times, more than 6,000 years ago; archaeological finds of grains and seeds in caves in Armenia and Iran date back to 5–4 million years BC, indicating a deep historical connection between humans and the plant.

In the traditional practices of Southern Europe, seeds were used to prepare tinctures in olive oil, which were applied externally for skin irritations, and internally as a mild astringent and anti-hemorrhoidal agent; grape oil was often used in massage and cosmetic compositions to strengthen the skin and blood vessels. In the Caucasus, especially in Armenia and Georgia, seeds were added to "gruotar" — herbal infusions used in traditional medicine for fatigue, as an ingredient in phytopastes for massage and compresses in the herbal books of mountain communities.

In Slavic folk traditions, grapes were perceived as a symbol of fertility and vitality; the remains of grains and seeds were sometimes kept as amulets or wrapped around icons for protection from diseases and misfortunes. Over a vast territory of Eastern Europe, seeds were added to cosmetic mixtures for the face and hair, used in decoctions for washing with eye fatigue and skin tone, often presented as a "plant of strength."

In traditional Indian Ayurveda and Thai medicine, formulations from seeds were used internally as tonics, and oils based on them — in topical mixtures to improve skin condition and microcirculation, especially in the warm season. In China and Korea, grapes were used in cosmetics as an ingredient for skin care and strengthening blood vessels, often in combination with green tea and jojoba extracts.

Non-medical use included the use of grape seeds in fertility rituals: they were added to bread, grain, and gravies in ceremonies symbolizing prosperity and harvest. In Slavic magic, vine branches and seeds were used as protective agents during livestock transitions and ritual baths of newborns.

Thus, grape seed has occupied a significant cultural and practical place in the traditions of various peoples of Europe, the Caucasus, Asia, and India in ethnobotany and folk medicine, combining cosmetic, protective, and tonic functions in ritual and everyday practice.