​Ruscus aculeatus (Butcher's Broom)

Ruscus aculeatus (Butcher's Broom)

Product Name: Иглица колючая, Ruscus aculeatus, Mäusedorn, Escoba de carnicero, Petit-houx, الجَزْلاَء, หนามหนู, Qassamtikan, Муштукка, Qaraqatkənarı, Сангдор, Dygliuotoji rūta, Krūmainā rūta, Іглиця колюча, Qaratikanqırağı, הדס קוצני

Synonyms: Иглица, Иглица аптечная, Иглица мясная, Butcher’s broom, Knee holm, Box holly, Mouse thorn, Metzgerbesen, Mäusedornstrauch, Escoba de carnicero, Ruscus, Petit-houx, Faux-houx, مكنسة الجزار, หนามเมาส์, หนามหนู

Used Parts: rhizome, root, shoots, leaves, berries.

Main Indications for the Use of Ruscus aculeatus: Chronic venous insufficiency, phlebothrombosis, post-thrombotic syndrome, varicose veins of the lower extremities, hemorrhoids, orthostatic hypotension, lymphatic edema of the lower extremities, vascular dysfunction, capillaropathy, venous trophic ulcer, angiopathy.

Use of Ruscus aculeatus in Mixtures and Complexes: Trophic skin ulcer, peripheral neuropathy, diabetes mellitus with microangiopathy, restless legs syndrome, chronic prostatitis, arterial hypotension, chronic cellulite, postpartum edema of the lower extremities, fibrous-fatty lipodystrophy.

Pharmacological Properties of Ruscus aculeatus: Venotonic, vasoconstrictive, anti-edema, antiexudative, anti-inflammatory, capillary-protective, angioprotective, anti-hemorrhoidal, antioxidant, mild spasmolytic, regulatory (with respect to vascular tone), anti-cellulite.

Dosage of Pharmaceutical Forms — Ruscus aculeatus

Powder — Ruscus aculeatus

Indications (Powder): Chronic venous insufficiency, varicose veins of the lower extremities, hemorrhoids, lymphatic edema of the lower extremities, phlebothrombosis, angiopathy, venous trophic ulcer, orthostatic hypotension.

Standard Dosage (Powder): 1 gram of powder 2 times a day 30 minutes before meals, with warm water. Course — 30 days.

Enhanced Dosage (Powder): 1.5 grams 2–3 times a day for lymphatic edema of the lower extremities, pronounced hemorrhoids, phlebothrombosis, and venous trophic ulcer. Course — 45 days under specialist supervision.

Maximum Dosage (Powder): Up to 2 grams 3 times a day is possible short-term (no more than 10 days) for acute thrombosis, severe angiopathy, or post-thrombotic syndrome.

Preventive Dosage (Powder): 0.5 grams once a day in the morning on an empty stomach. Recommended for chronic venous insufficiency of grade I, varicose predisposition, and also for persons with a sedentary lifestyle. Course — 30 days every 3 months.

Pediatric Dosage (Powder): Use in children under 12 years of age is not recommended. From 12 years — no more than 0.5 grams once a day. Minimum weight of the child — 40 kilograms.

Contraindications (Powder): Stage II–III arterial hypertension, hypersensitivity to the plant, acute kidney diseases. Data on contraindications during pregnancy, lactation, and in children under 12 years of age have not been scientifically registered.

Side Effects (Powder): With overdose, headache, increased blood pressure, and dyspepsia are possible.

Adjustment for Patient Body Weight (Powder): For body weight below 60 kg — reduce the dose by 25%. For body weight over 90 kg — an increase in dose by 20% is possible in the absence of side effects.

Preparation method (Powder): Take dry cleaned rhizomes and roots of the plant in the amount of 100 grams. Grind in a mortar or using an electric mill to a fine powder state (fractions less than 0.25 mm). Sift through a fine sieve. Store in a tightly closed glass jar.

Storage Conditions and Shelf Life (Powder): Store in an airtight dark glass container at a temperature of 5 to 25 degrees Celsius, in a dry place, protected from direct light and electromagnetic radiation. Shelf life — up to 12 months. After opening — use within 3 months.

Dry Extract — Ruscus aculeatus

Indications (Dry Extract): Chronic venous insufficiency, capillaropathy, hemorrhoids, venous trophic ulcer, lymphatic edema, post-thrombotic syndrome, vascular dysfunction.

Standard Dosage (Dry Extract): 100 milligrams of standardized extract (with a content of at least 5% saponins) 2 times a day, 20 minutes before meals. Duration of course — 30 days.

Enhanced Dosage (Dry Extract): 150–200 milligrams 2 times a day for venous ulcers, lymphedema, pronounced hemorrhoids, and varicose veins of grade III.

Maximum Dosage (Dry Extract): Do not exceed 300 milligrams 2 times a day. Used under medical supervision for no more than 7 days for pronounced phlebothrombosis and edema.

Preventive Dosage (Dry Extract): 50 milligrams once a day in the morning. Indicated for persons with a hereditary predisposition to varicose veins, with a sedentary lifestyle, and postmenopausal women. Courses — 30 days with a 2-month break.

Pediatric Dosage (Dry Extract): Not recommended for children under 14 years of age. From 14 years — no more than 50 milligrams per day. Minimum weight — 45 kilograms.

Contraindications (Dry Extract): Severe hypertension, pregnancy, intolerance to saponins. Safety data during lactation and in childhood are insufficient.

Side Effects (Dry Extract): With overdose, headache, gastric irritation, and a feeling of tightness in the chest are possible.

Adjustment for Patient Body Weight (Dry Extract): For body weight up to 60 kg — 70% of the standard dose. For body weight over 90 kg — an increase to 120% of the standard dose is possible.

Preparation method (Dry Extract): Take 500 grams of ground dry rhizomes. Pour 5 liters of 50% alcohol and infuse at 40 degrees Celsius for 10 days with daily stirring. Strain, evaporate in a water bath to obtain a thick mass, then dry in a drying cabinet at 40 degrees. Grind the resulting extract to a powder state.

Storage Conditions and Shelf Life (Dry Extract): Store in an airtight frosted glass container, in a dark, cool place at a temperature of 5 to 20 degrees Celsius. Avoid contact with moisture and light. Shelf life — 24 months. After opening, use within 90 days.

Alcohol-Based Tincture — Ruscus aculeatus

Indications (Tincture): Chronic venous insufficiency, varicose veins of the lower extremities, hemorrhoids, angiopathy, phlebothrombosis, orthostatic hypotension, capillaropathy.

Standard Dosage (Tincture): 25 drops 2 times a day 20 minutes before meals, diluted in 50 milliliters of water. Course — 30 days.

Enhanced Dosage (Tincture): 30–35 drops 3 times a day for pronounced varicose veins, angiopathy, and thrombophlebitis. Take for 45 days, then take a break of at least 2 weeks.

Maximum Dosage (Tincture): No more than 40 drops 3 times a day. Allowed for no more than 10 days for acute phlebitis, venous trophic ulcer, or pronounced edema of the lower extremities.

Preventive Dosage (Tincture): 15 drops once a day in the morning, diluted in water. Recommended for patients with sedentary work, initial manifestations of venous insufficiency, and women after pregnancy. Course — 20 days every 2 months.

Pediatric Dosage (Tincture): Not recommended for children under 14 years of age due to alcohol content. From 14 years — no more than 10 drops once a day, diluted in water.

Contraindications (Tincture): Alcoholism, epilepsy, liver diseases, pregnancy. Safety data during lactation and in children under 14 years of age have not been scientifically registered.

Side Effects (Tincture): When the dose is exceeded, dizziness, nausea, palpitations, and increased blood pressure are possible.

Adjustment for Patient Body Weight (Tincture): Patients with body weight below 60 kg — use 70% of the standard dose. For weight over 90 kg — increase the dose by 20% with good tolerability.

Preparation method (Tincture): Grind 100 grams of dry rhizome. Pour 1 liter of 40% ethanol. Infuse in an airtight glass container for 14 days in a dark place at a temperature of 18–22 degrees Celsius. Shake daily. After the period, strain the tincture through gauze. Store in a dark glass bottle.

Storage Conditions and Shelf Life (Tincture): Store in a tightly closed dark glass container at a temperature of 5 to 20 degrees Celsius. Avoid exposure to direct sunlight. Shelf life — up to 24 months. After opening — use within 90 days.

Oil Infusion — Ruscus aculeatus

Indications (Oil Infusion): Lymphedema, varicose veins, vascular network, chronic cellulite, venous stasis, postpartum edema.

Standard Dosage (Oil Infusion): Externally: apply 3–5 milliliters of oil to the affected area 2 times a day with light massaging movements. Course — at least 21 days.

Enhanced Dosage (Oil Infusion): Externally: apply 5–7 milliliters 3 times a day for pronounced edema, capillaropathy, fibrous lipodystrophy, and lymphedema.

Maximum Dosage (Oil Infusion): Up to 10 milliliters per application area up to 4 times a day is possible short-term for pronounced edema and pain syndrome. Maximum course — 10 days.

Preventive Dosage (Oil Infusion): 2 milliliters once a day in the evening on the shins and thighs. Used for varicose predisposition, in menopausal women, athletes, and workers who stand for long periods. Course — 15 days with a 1-month break.

Pediatric Dosage (Oil Infusion): Not used in children under 10 years of age. From 10 years — no more than 1 milliliter once a day on a limited area (no more than 100 cm²).

Contraindications (Oil Infusion): Presence of open wounds, pustular skin lesions, individual intolerance. Data on contraindications during pregnancy, lactation, and in children under 10 years of age are absent.

Side Effects (Oil Infusion): Rarely — skin irritation, itching, contact dermatitis with hypersensitivity.

Adjustment for Patient Body Weight (Oil Infusion): Not required for external use. In case of pronounced obesity, an increase in the coverage area and volume of the preparation to 120% of the standard dose is possible.

Preparation method (Oil Infusion): Grind 100 grams of dry rhizomes and pour 500 milliliters of organic cold-pressed coconut oil. Simmer in a water bath at a temperature of 45 degrees Celsius for 4 hours. Pour into a glass jar and infuse for another 5 days in a dark place. Strain through a fine sieve or gauze.

Storage Conditions and Shelf Life (Oil Infusion): Store in an airtight dark glass container at a temperature of 5 to 18 degrees Celsius, in a dry place, away from direct light and heat. Shelf life — 6 months. After opening, use within 60 days.

Vaginal Suppository — Ruscus aculeatus

Indications (Vaginal Suppository): Venous stasis of the pelvic organs, chronic hemorrhoids, lymphatic edema of the perineum, varicose disease of the pelvic veins, postpartum edema, trophic changes of the vaginal mucosa of vascular origin.

Standard Dosage (Vaginal Suppository): 1 suppository once a day at night, in a course of 10–15 days. Insert deep into the vagina.

Enhanced Dosage (Vaginal Suppository): 1 suppository 2 times a day (morning and at night) for pronounced pelvic varicose veins, severe edema, grade III hemorrhoids, and post-thrombotic venous outflow disorders.

Maximum Dosage (Vaginal Suppository): 1 suppository 3 times a day for no more than 5 days, only by doctor's prescription, for acute lymphedema and vascular complications after surgical interventions in the pelvic area.

Preventive Dosage (Vaginal Suppository): 1 suppository every other day before bedtime for 10 days. Repeat the course once every 2 months. Indicated for a predisposition to pelvic varicose disease, chronic venous disorders after pregnancy, and a sedentary lifestyle.

Pediatric Dosage (Vaginal Suppository): Not used in pediatric gynecology. Contraindicated before menarche. After 16 years — with caution, no more than 1 suppository per day with a body weight of 50 kg or more.

Contraindications (Vaginal Suppository): Purulent processes of the vagina, active forms of colpitis and cervicitis, allergy to components, first trimester of pregnancy. Data on use during lactation and in adolescents under 16 years of age are absent.

Side Effects (Vaginal Suppository): Rarely — itching, local mucosal irritation, increased vaginal secretion. With overdose — possible contact vaginitis, burning sensation.

Adjustment for Patient Body Weight (Vaginal Suppository): For body weight up to 50 kg — reduce the frequency of use to once every 2 days. For weight over 90 kg — standard or enhanced regimen is allowed.

Preparation method (Vaginal Suppository): For 100 grams of finished mass: dry extract of butcher's broom rhizomes — 2 grams, cocoa butter — 70 grams, coconut oil — 25 grams, beeswax — 3 grams. Melt the oils in a water bath at a temperature of 50–55 °C, add the extract, mix until homogeneous. Pour into molds, cool. Store in the refrigerator.

Storage Conditions and Shelf Life (Vaginal Suppository): Store in the original packaging at a temperature of 2 to 8 °C. Avoid exposure to light and heat. Shelf life — 6 months. After opening the package — use within 10 days.

Rectal Suppository — Ruscus aculeatus

Indications (Rectal Suppository): Internal and external hemorrhoids, anal fissure, rectal varicose veins, venous stasis of the pelvis, proctitis with a venous component.

Standard Dosage (Rectal Suppository): 1 suppository once a day before bedtime. Course of use — from 10 to 14 days.

Enhanced Dosage (Rectal Suppository): 1 suppository 2 times a day (morning and evening) for pronounced pain syndrome, edema, exacerbation of grade II–III hemorrhoids, and anal bleeding.

Maximum Dosage (Rectal Suppository): 1 suppository 3 times a day — no more than 5 days for acute hemorrhoids, thrombosis of hemorrhoidal nodes, pronounced edema and pain. Use only by doctor's prescription.

Preventive Dosage (Rectal Suppository): 1 suppository every 2 days before bedtime. Course — 10 applications. Repeat every 2 months. Indications — chronic hemorrhoids, sedentary work, increased intra-abdominal pressure, physical inactivity.

Pediatric Dosage (Rectal Suppository): Contraindicated for children under 12 years of age. From 12 years — no more than 1 suppository once every 2 days. Body weight not less than 40 kg.

Contraindications (Rectal Suppository): Acute proctitis, anal bleeding of undetermined origin, malignant neoplasms of the rectum, individual intolerance. Data on use during pregnancy and lactation are absent.

Side Effects (Rectal Suppository): Rarely — itching, burning sensation in the anorectal area, increased sensitivity. With overdose — sphincter spasms, increased inflammatory symptoms.

Adjustment for Patient Body Weight (Rectal Suppository): Weight up to 60 kg — standard dose once every 2 days. Weight over 90 kg — an increase in the frequency of use to 2 times a day is allowed with good tolerability.

Preparation method (Rectal Suppository): For 100 grams of base: dry extract of butcher's broom root — 2.5 grams, coconut oil — 70 grams, cocoa butter — 25 grams, lanolin — 2.5 grams. Melt all components at a temperature of 50–55 °C, mix thoroughly, pour into rectal molds, cool until completely solidified.

Storage Conditions and Shelf Life (Rectal Suppository): Store at a temperature of 2 to 8 °C in light-protected packaging. Shelf life — up to 6 months. After opening the package, use within 7 days.

Cream — Ruscus aculeatus

Indications (Cream): Varicose veins of the lower extremities, chronic venous insufficiency, vascular network, phlebopathy, post-thrombotic syndrome, lymphatic edema, venous trophic ulcer in the granulation stage, chronic cellulite.

Standard Dosage (Cream): Apply a thin layer 2 times a day (morning and evening) to clean skin in the affected area. Course — at least 21 days.

Enhanced Dosage (Cream): Apply 3–4 times a day to the area of vascular disorders for pronounced edema, pain syndrome, lymphedema, and postoperative venous dysfunction.

Maximum Dosage (Cream): Up to 5 applications per day, on a limited area (no more than 300 cm²) — for pronounced vascular disorders, in the first days after venous surgery.

Preventive Dosage (Cream): Once a day on the shins in the evening before bedtime, in courses of 14 days with a 2-week break. Indicated for a sedentary lifestyle, standing work, a predisposition to varicose veins, and heavy legs syndrome.

Pediatric Dosage (Cream): Use in children under 10 years of age is not recommended. From 10 years — once a day on a limited area with a body weight of at least 35 kg.

Contraindications (Cream): Presence of open wounds, weeping dermatoses, pustular skin infections, individual intolerance. Scientific data on safety during pregnancy, lactation, and in children under 10 years of age are absent.

Side Effects (Cream): Rarely — skin itching, redness, contact dermatitis, especially with prolonged use and increased sensitivity.

Adjustment for Patient Body Weight (Cream): Not required for external use. For body weight over 100 kg — an increase in the area of application is possible, while maintaining frequency.

Preparation method (Cream): For 100 grams of finished cream: dry extract of butcher's broom root — 2 grams, witch hazel hydrolate — 10 grams, coconut oil — 20 grams, shea butter — 10 grams, natural emulsifier (cetearyl glucoside) — 5 grams, purified water — 52 grams, plant-derived preservative (with rosemary extract) — 1 gram. Heat the aqueous and oil phases separately to 70 °C, combine with stirring, add the extract, cool to 35 °C, add the preservative, whip until a homogeneous texture is obtained.

Storage Conditions and Shelf Life (Cream): Store in a tightly closed package in a dark, cool place at a temperature of 5 to 15 °C. Avoid exposure to sunlight. Shelf life — 3 months. After opening — use within 30 days.

Ointment — Ruscus aculeatus

Indications (Ointment): Thrombophlebitis, varicose eczema, edema syndrome, venous trophic ulcer, angiopathy, vascular pain, chronic hemorrhoids, bruises with a congestive component.

Standard Dosage (Ointment): Externally: apply 1–2 grams of ointment 2 times a day to the affected area, with light rubbing movements. Course — 14–21 days.

Enhanced Dosage (Ointment): Up to 3 applications per day of 2–3 grams for severe forms of varicose eczema, thrombophlebitis, ulcerative changes in the granulation stage, and pain syndrome.

Maximum Dosage (Ointment): Up to 4 times a day of 3 grams on a limited area (up to 200 cm²). Do not use more than 5 days in a row.

Preventive Dosage (Ointment): Once a day in the evening on the area of venous insufficiency (shins, ankles), in 10-day courses once a quarter. Recommended for patients over 50 years of age, with prolonged standing, and a tendency to edema.

Pediatric Dosage (Ointment): From 12 years — once a day on a small area of skin (up to 50 cm²), no more than 1 gram of ointment. Body weight — at least 40 kilograms.

Contraindications (Ointment): Open ulcers with purulent discharge, infectious skin diseases, individual intolerance. Safety during pregnancy and in children under 12 years of age has not been established.

Side Effects (Ointment): Allergic reactions, increased itching, urticaria, erythema with hypersensitivity.

Adjustment for Patient Body Weight (Ointment): Not required for external use; however, it is recommended to take into account the area of application: up to 2 grams per 100 cm².

Preparation method (Ointment): For 100 grams: thick alcohol extract — 3 grams, beeswax — 8 grams, coconut oil — 30 grams, olive oil — 30 grams, vegetable petroleum jelly — 29 grams. Melt all components in a water bath at a temperature of 50–55 °C, mix until a homogeneous mass is obtained, cool and pour into jars.

Storage Conditions and Shelf Life (Ointment): Store in an airtight package at a temperature of 5 to 20 °C, in a dark place. Shelf life — up to 6 months. After opening, use within 45 days.

Serum — Ruscus aculeatus

Indications (Serum): Vascular network on the face and legs, periorbital edema, couperose, chronoaging of the skin with a vascular component, skin capillaropathy, post-traumatic congestion, fatigue and dullness of the skin, chronic cellulite.

Standard Dosage (Serum): Apply 3–5 drops to cleansed skin 2 times a day (morning and evening), with light tapping movements until completely absorbed. Course — 30 days.

Enhanced Dosage (Serum): Apply 2 times a day of 5–7 drops for pronounced couperose, post-acne with a vascular component, postoperative or lymphatic edema of the face and neck, and chronic capillaropathy.

Maximum Dosage (Serum): Up to 10 drops 3 times a day on a limited area (forehead, cheeks, chin) for edema and vascular disorders in the acute period, no more than 7 days in a row.

Preventive Dosage (Serum): 3 drops once a day in the evening on the face and neck, in courses of 14 days with a 2-week break. Indicated for a tendency to vascular network, patients with thin skin, chronic stress, and perimenopausal women.

Pediatric Dosage (Serum): Not used in children under 16 years of age. For weight over 50 kg and according to indications, spot application once a day on limited areas (for example, after injury) is allowed, no more than 1 drop.

Contraindications (Serum): Purulent inflammatory skin diseases, individual intolerance. Scientifically confirmed data on use during pregnancy, lactation, and in children under 16 years of age are absent.

Side Effects (Serum): Rarely — local irritation, redness, flaking, sensation of heat. With overdose, contact dermatitis and short-term increased skin sensitivity are possible.

Adjustment for Patient Body Weight (Serum): Not required for external spot application. For massive treatment of body skin (for example, for cellulite), the dose should be calculated by area: no more than 1 milliliter per 1000 cm² of skin.

Preparation method (Serum): For 100 grams: water-glycerin extract of butcher's broom rhizome — 5 grams, cypress hydrolate — 30 grams, hyaluronic acid (low molecular weight) — 0.2 grams, panthenol — 1 gram, glycerin — 5 grams, plant-derived preservative (rosemary extract) — 1 gram, purified water — up to 100 grams. Combine all components at a temperature of 20–25 °C, mix thoroughly, package in bottles with a dispenser.

Storage Conditions and Shelf Life (Serum): Store in the refrigerator at a temperature of 4 to 8 °C, in a dark container. Avoid exposure to sunlight and heat. Shelf life — up to 3 months. After opening, use within 30 days.

Toxicity and Biosafety of Ruscus aculeatus

Ruscus aculeatus belongs to the category of non-toxic plants upon oral and external use in therapeutic doses. Conducted studies on animals have shown an extremely low level of acute toxicity.

The LD₅₀ value of dry butcher's broom extract upon oral administration in mice is more than 2,000 mg/kg body weight, which indicates a high biosafety of the substance. With prolonged use, no histologically significant changes in the liver, kidneys, and heart of experimental animals are observed. No mutagenic, carcinogenic, or embryotoxic activity has been detected.

Studies also confirm good tolerability of external forms (ointments, creams, serums), including the absence of sensitization with repeated use.

According to pharmacological evaluation data, Ruscus aculeatus extracts are recognized as safe for use in cosmetics and therapeutic preparations, including drugs used for a long period of time.

Reference: https://www.ncbi.nlm.nih.gov/p...

Pharmacodynamics — Ruscus aculeatus

The pharmacodynamic action of Ruscus aculeatus is associated mainly with active saponins (in particular, steroidal saponins of the ruscogenin and neoruscogenin type), as well as flavonoids, organic acids, and phytosterols contained in the rhizomes of the plant. These compounds exhibit pronounced angiotropic activity and affect both the peripheral vascular system and the microcirculatory bed. The main pharmacological effect is a vasoconstrictive action, realized primarily on venous vessels, especially weakly innervated veins of the lower extremities and pelvic organs. The mechanism of action includes activation of α-adrenoceptors of smooth muscle cells of the vascular wall, which leads to an increase in venous tone and a decrease in venous capacitance.

Additionally, an effect on microcirculation and vascular wall permeability has been confirmed. Ruscus aculeatus stabilizes endothelial cells, reduces exudation, and exerts a capillary-protective effect, probably due to inhibition of the release of inflammation mediators and vasoactive prostaglandins. The local effect with external use includes anti-edema activity, reduction of the inflammatory response, and decrease in tissue stasis. In vitro data indicate possible involvement in the regulation of prostaglandin synthesis through modulation of the cyclooxygenase pathway, without systemic inhibition of the COX-1 enzyme.

Additionally, Ruscus aculeatus affects the lymphatic system, increasing the tone of lymphatic vessels and stimulating lymph outflow, which may be associated with an effect on the smooth muscle elements of the lymphatic wall. The ability of plant components to reduce erythrocyte aggregation and increase the plasticity of capillary blood flow, especially under conditions of venous stasis, has been shown. The plant exerts a moderate antioxidant and anti-inflammatory effect at the level of the skin, which is due to the presence of phenolic compounds and flavonoids, such as rutin and quercetin.

At the systemic level, the pharmacological action of Ruscus aculeatus is realized primarily through the vascular and lymphatic systems, indirectly affecting the microcirculation of the skin, mucous membranes, and internal organs. At the same time, there is no pronounced effect on the cardiovascular system as a whole or the central nervous system at standard dosages, which increases the safety profile of the drug. A moderate modulating effect on skin receptors, including TRPV1 and associated sensory pathways, has also been described, which may explain the mild analgesic effect with external use.

Thus, the pharmacodynamic profile of Ruscus aculeatus includes venotonic, vasoconstrictive, anti-edema, capillary-protective, and angiotropic action, mainly realized through local and systemic mechanisms, without a pronounced effect on neurohumoral regulation and without significant sedative activity.

References:
https://www.ncbi.nlm.nih.gov/p...
https://www.sciencedirect.com/...
https://link.springer.com/arti...
https://www.mdpi.com/2227-9032...
https://pubchem.ncbi.nlm.nih.g...

Pharmacokinetics — Ruscus aculeatus

Complete pharmacokinetic data on the active components of Ruscus aculeatus are absent; however, based on the structure of the main substances (steroidal saponins and flavonoids), as well as data on dosage forms (powder, extract, tincture), a generalized kinetic profile can be reconstructed.

Upon oral administration, saponins undergo partial degradation in the gastrointestinal tract with the participation of microbiota. The main absorption occurs in the small intestine, where bioavailability is limited due to weak lipophilicity and the possibility of hydrolysis to aglycones. Entering the systemic circulation, active metabolites bind to plasma proteins and are distributed mainly in the area of the vascular bed and connective tissue. Terpenoids and flavonoids present in extracts undergo conjugation in the liver followed by excretion mainly with bile and urine.

External dosage forms (ointment, cream, infusion, serum) have predominantly local action with minimal systemic absorption. With transdermal application, the penetration of active substances is limited by the stratum corneum of the epidermis, especially when using a lipophilic base (coconut oil, cocoa butter). Active substances reach subcutaneous vessels, capillaries, and lymphatic structures, where their pharmacodynamic effect is realized. Partial accumulation is possible with long-term course use, especially in lipophilic tissues.

Mucosal routes of administration (suppositories) provide higher bioavailability due to bypassing primary hepatic metabolism. Rectal and vaginal administration promotes absorption through the dense vascular network of the rectum and vagina, providing systemic and local action without significant losses. Excretion of metabolic products occurs mainly through the kidneys (urine) and through bile; an insignificant amount may be excreted with sweat and skin epithelium.

Ingredients contained in the alcoholic tincture, upon oral administration, are absorbed rapidly, especially in the presence of alcohol, which enhances the dissolution of lipophilic fractions. However, at high dosages, competition for liver enzyme systems is possible, especially in the case of polypharmacy with herbal preparations.

References:
https://www.sciencedirect.com/science/article/pii/S0378874113001476
https://pubmed.ncbi.nlm.nih.go...
https://www.mdpi.com/2079-7737...
https://www.ncbi.nlm.nih.gov/p...
https://link.springer.com/arti...

Mechanisms of Action and Scientific Rationale — Ruscus aculeatus

The main mechanisms of action of Ruscus aculeatus are associated with the pharmacological activity of steroidal saponins (ruscogenin, neoruscogenin), flavonoids, and phenolic compounds. In vitro and in vivo studies show that these components modulate vascular tone and capillary permeability through activation of α₁-adrenoceptors of smooth muscle cells of the venous wall. This contributes to vasoconstriction mainly in the venous segment of microcirculation, especially in vessels with low basal tone. Such activity is realized in the absence of a direct effect on arterial vessels, which makes the mechanism selectively directed to the venous system.

Saponins and flavonoids of Ruscus aculeatus possess angiotropic activity, affecting vascular endothelial cells. Inhibition of the release of pro-inflammatory mediators, including tumor necrosis factor α (TNF-α), interleukins IL-6 and IL-1β, has been confirmed. This is associated with blockade of the NF-κB signaling cascade, as well as inhibition of the activation of transcription factors involved in the regulation of the inflammatory response. Simultaneously, inhibition of the expression of vascular adhesion molecules (VCAM-1 and ICAM-1) occurs, which reduces leukocyte migration and damage to the vascular wall.

Pharmacologically confirmed is the effect on cyclooxygenase (COX) and lipoxygenase (LOX) enzyme pathways, in particular — a decrease in PGE2 and LTB4 production. This provides anti-edema and antiexudative action. The plant also exhibits a moderate effect on TRPV receptors of the skin and mucous membranes, which is associated with local modulation of sensory signals and regulation of vascular lumen at the level of microcirculation.

Flavonoids and phenolic acids contained in Ruscus aculeatus are hydrogen donors and active antioxidants capable of neutralizing superoxide radicals and hydrogen peroxide. This contributes to the protection of the vascular endothelium from oxidative stress and prevention of oxidative activation of the MAPK cascade. The effect on the lymphatic system is realized through stimulation of the spontaneous contractile activity of smooth muscle cells of lymphatic vessels, which has been proven in studies using lymphatic perfusion.

At the cellular level, targets of action are endothelial cells, pericytes, macrophages, and neutrophils involved in the inflammatory process and remodeling of the vascular wall. An effect on glycosaminoglycan structures of connective tissue has also been confirmed, which may explain partial protection of vessels from degenerative changes. The effects are manifested both at the systemic and local levels, including the skin, mucous membranes, and venous vessels.

References:
https://www.sciencedirect.com/...
https://link.springer.com/arti...
https://pubmed.ncbi.nlm.nih.go...
https://www.ncbi.nlm.nih.gov/p...
https://pubchem.ncbi.nlm.nih.g...

Synergy — Ruscus aculeatus

Pharmacological synergy of Ruscus aculeatus has been studied mainly in combination with plants and compounds possessing venotonic, anti-inflammatory, and antioxidant effects. One of the most studied areas is the combination with flavonoid glycosides (for example, rutin and diosmin), where potentiation of capillary-protective and venoconstrictive action has been identified. This is explained by the similarity of mechanisms of action and mutual support in the modulation of α₁-adrenergic pathways and stabilization of endothelial cells.

The combination of Ruscus aculeatus with hesperidin and vitamin C leads to enhanced antioxidant activity, due to activation of the glutathione peroxidase system and increased cellular resistance to oxidative stress. When triterpenes from Centella asiatica are added, an additive angioprotective effect is observed, including acceleration of angiogenesis and reduction of pericapillary infiltration. These effects have been confirmed in endothelial cell cultures in vitro and in inflammatory model systems in vivo.

A modulating interaction with bioactive polysaccharides from Hamamelis virginiana has also been registered, where the combination with Ruscus aculeatus reduced vascular wall permeability more effectively than each component individually. An addition of lymphotropic action when used in combination with saponin-containing extracts of Aesculus hippocastanum has been mentioned, due to simultaneous stimulation of venous and lymphatic outflow.

The nature of interactions in most cases is potentiating and tissue-specific, mainly in the area of the vascular wall, connective tissue, and capillary bed. At the molecular level, synergism may be realized through combined inhibition of inflammation mediators (TNF-α, IL-6, PGE2), as well as through additional inhibition of COX-2 and NADPH-oxidase enzyme systems. These data are confirmed both experimentally and in pharmacognostic analysis of multicomponent phytoformulas.

References:
https://www.ncbi.nlm.nih.gov/p...
https://pubmed.ncbi.nlm.nih.go...
https://www.sciencedirect.com/...
https://www.mdpi.com/1420-3049...
https://link.springer.com/arti...

Geography of Use and Traditional Medicine — Ruscus aculeatus

Ruscus aculeatus has traditionally been used in the folk medicine of the Mediterranean countries, the Balkans, the Caucasus, Asia Minor, and some regions of Western Europe. Historically, the plant has been known since ancient times: references to it are found in the texts of Theophrastus and Dioscorides, where it is described as a remedy for vein care and against "stagnant bodily fluids." In medieval Europe, butcher's broom was widely used in monastic herbalists as a remedy for "removing dampness" and strengthening the "blood flow," especially in countries where the Latin and Frankish medical tradition prevailed.

In the folklore of Britain and the Iberian Peninsula, butcher's broom was considered a plant that protects against evil spirits, and its branches were hung at the entrance to the house in winter. In the Slavic tradition in Bulgaria and Serbia, the plant was used as a talisman against the "evil eye," and decoctions of rhizomes were used by women in the postpartum period for washing the legs and body. Also in these regions, wraps and baths with the addition of butcher's broom decoction were practiced for fatigue, "heaviness in the legs," and circulatory disorders.

Among the Germanic peoples, the plant is known as Mäusedorn ("mouse thorn"), where it was used as a symbol of cheerfulness and elasticity. In the village medicine of Southern Germany, root infusions were used as a "cleansing agent" after winter holidays — a tradition partially preserved in home phytotherapy until the 20th century. Among the Celtic peoples, butcher's broom was associated with cyclicality and rebirth — it was used to decorate ritual wreaths and brought into the house on the day of the winter solstice.

In the culture of the peoples of Anatolia (the territory of modern Turkey), a decoction of rhizomes was used as a rub for severe leg fatigue, and in some mountain villages, butcher's broom was part of medicinal pastes based on goat fat and honey. In Jewish folk medicine of the medieval period, butcher's broom was used as an external remedy for cleansing the skin and "relieving internal fires." In Sicily, the plant was used in fertility rituals, and its rhizomes were buried in the field during the first sowing.

In ritual practice, butcher's broom was used as a protective plant. In some regions of the Pyrenees and the Alps, it was planted on the border of villages and at crossroads as a barrier against "transitional spirits." In some Latin rituals, the plant was burned as a cleansing agent before a wedding or ablution ceremony. In modern ethnophytotherapy, butcher's broom rhizomes continue to be used as a component of traditional ointments and infusions.