Astragalus microcephalus

Astragalus microcephalus

Product Name: Астрагал мелкоголовый, Astragalus microcephalus, Kleinköpfiger Tragant, Astrágalo de cabeza pequeña, Astragale à petites têtes, الاستراغالوس صغير الرأس, อัสตรากาลัส ไมโครเซฟาลัส, Astragal kichik boshli, Майда баштуу астрагал, Xırda başlı astrqal, Астрагали хурдосар, Smulkiažiedis astragalas, Mazziedu astragals, Астрагал дрібноголовий, Kiçik başlı vəlişə, אסטרגלוס מיקרוצפלוס

Synonyms: астрагал кавказский, мелкоголовый козий корень, astragalus caucasicus, small-headed milkvetch, Kleinköpfiger Bocksbart, astrágalo caucásico, astragale du Caucase, الاستراغال القوقازي, แอสตรากาลัส คอเคเชียน

Parts Used: roots, aerial parts, fruits, seeds, leaves, stems, roots

Main Indications for Astragalus microcephalus Use: chronic heart failure, arterial hypotension, chronic fatigue syndrome, bronchial obstructive syndrome, viral hepatitis B, secondary immunodeficiency, glomerulonephritis, diabetic angiopathy, gastric ulcer, pulmonary tuberculosis, autoimmune thyroiditis, chronic pyelonephritis

Use of Astragalus microcephalus in mixtures and complexes: cerebrovascular insufficiency, Alzheimer's disease, cervical osteochondrosis, human papillomavirus, type 2 diabetes mellitus, benign prostatic hyperplasia, chronic pancreatitis, chronic prostatitis, acne vulgaris, atherosclerosis, stage II hypertension

Pharmacological Properties of Astragalus microcephalus: immunostimulating, adaptogenic, antioxidant, anti-inflammatory, hepatoprotective, nephroprotective, antihypertensive, antiviral, tonic, vasoconstrictive, cardiotonic, spasmolytic, wound-healing, regenerative

Dosage of Pharmaceutical Forms — Astragalus microcephalus

Powder — Astragalus microcephalus

Indications (Powder): chronic fatigue syndrome, arterial hypotension, chronic heart failure, secondary immunodeficiency, glomerulonephritis, pulmonary tuberculosis, diabetic angiopathy, chronic pyelonephritis

Standard Dosage (Powder): Adults: 1 gram of powder 3 times a day, 30 minutes before meals, with warm water. Duration of intake — 21 days.

Enhanced Dosage (Powder): 1.5 grams of powder 3 times a day for viral hepatitis B, autoimmune thyroiditis, exacerbation of chronic pyelonephritis. Course — 28 days, followed by laboratory monitoring.

Maximum Dosage (Powder): No more than 2 grams of powder 3 times a day for severe forms of chronic fatigue syndrome, for immune suppression after chemotherapy or prolonged infection.

Preventive Dosage (Powder): 0.5 grams once a day for 30 days. Recommended for chronic stress, during the off-season, during ARVI epidemics, for patients with hypotonic type vegetative-vascular dystonia and students during exams.

Pediatric Dosage (Powder): From 8 years of age and body weight from 25 kg — 0.3 grams of powder 2 times a day. From 12 years — 0.5 grams 2 times a day. The safety of use in children under 8 years of age has not been scientifically confirmed.

Contraindications (Powder): Individual hypersensitivity. Data on contraindications during pregnancy, lactation and in children under 8 years of age are not scientifically registered.

Side Effects (Powder): Rare — dyspeptic disorders, feeling of body heat, palpitations when exceeding the dose.

Adjustment for Patient Body Weight: For body weight less than 60 kg — reduce dosage by 25%. For body weight more than 90 kg — increase dosage by 25% possible in the absence of side effects.

Preparation method (Powder): To prepare 100 grams of powder, take 100 grams of dried purified root of Astragalus microcephalus. The roots are washed, dried at a temperature of 45–50 °C until brittle. Then they are ground in a mill to a fine powder state. Sifted through sieve No. 80. Stored in an airtight glass container.

Storage Conditions and Shelf Life (Powder): Store in an airtight glass container, in a dark, dry place at a temperature from +5 to +25 °C. Avoid exposure to direct sunlight and electromagnetic fields. Shelf life — up to 24 months. After opening the package, use within 60 days.

Dry Extract — Astragalus microcephalus

Indications (Dry Extract): chronic heart failure, viral hepatitis B, chronic fatigue syndrome, secondary immunodeficiency, diabetic angiopathy, autoimmune thyroiditis, chronic pyelonephritis, bronchial obstructive syndrome

Standard Dosage (Dry Extract): 200 milligrams of dry extract once a day in the morning after meals, for 21 days.

Enhanced Dosage (Dry Extract): 200 milligrams twice a day (morning and afternoon) for viral hepatitis B, severe immunodeficiency syndrome, autoimmune pathologies. Course — 28–35 days.

Maximum Dosage (Dry Extract): Up to 300 milligrams three times a day for no more than 10 days. Indicated for severe secondary immunodeficiency and severe arterial hypotension.

Preventive Dosage (Dry Extract): 100 milligrams once a day for 30 days. Recommended for frequent viral infections, chronic fatigue, elderly patients, as well as for those working under stress.

Pediatric Dosage (Dry Extract): From 10 years of age and body weight from 30 kg — 100 milligrams once a day. Safety in children under 10 years of age is not confirmed.

Contraindications (Dry Extract): Individual intolerance to the components. Data on contraindications during pregnancy, lactation and in children under 10 years of age are not scientifically registered.

Side Effects (Dry Extract): Possible headache, dry mouth, nausea when exceeding the dosage.

Adjustment for Patient Body Weight: For patients with body weight below 60 kg — reduce dosage by 25%. For patients with body weight above 90 kg — an increase in dosage is possible up to 250 milligrams once.

Preparation method (Dry Extract): 100 grams of crushed root are poured with 1000 milliliters of purified water. Infuse at a temperature of 80 °C in a water bath for 2 hours. Cool, filter and evaporate under vacuum to obtain a thick extract. Then dry in a drying chamber at a temperature of 40–45 °C to obtain a powdery mass. Sieve and package in an airtight container.

Storage Conditions and Shelf Life (Dry Extract): Store in an airtight container at a temperature of +5 to +25 °C, in a dry, light-protected place. Shelf life — 24 months. After opening, use within 45 days.

Tincture — Astragalus microcephalus

Indications (Tincture): chronic fatigue syndrome, arterial hypotension, secondary immunodeficiency, chronic pyelonephritis, pulmonary tuberculosis, autoimmune thyroiditis, chronic heart failure, bronchial obstructive syndrome

Standard Dosage (Tincture): 20 drops 2 times a day, dissolved in 50 milliliters of water, 30 minutes before meals. Course — 21 days.

Enhanced Dosage (Tincture): 30 drops three times a day for viral hepatitis B, chronic intoxication, severe immune weakness. Course — 28 days.

Maximum Dosage (Tincture): Up to 40 drops three times a day for no more than 5 days in severe immunodeficiency conditions, as well as in complex support after chemotherapy.

Preventive Dosage (Tincture): 10 drops once a day in the morning, course — 30 days. Recommended for chronic stress, seasonal colds, in preparation for increased physical and psycho-emotional stress.

Pediatric Dosage (Tincture): Not recommended for children under 14 years of age due to ethanol content. From 14 years — no more than 10 drops once a day, with body weight from 40 kg.

Contraindications (Tincture): Liver diseases in the active phase, alcohol dependence, epilepsy, pregnancy, lactation, children under 14 years of age. Individual intolerance is possible.

Side Effects (Tincture): Tachycardia, dizziness, insomnia, headache when exceeding the dosage.

Adjustment for Patient Body Weight: For body weight below 60 kg — reduce dosage by 20%. For weight above 90 kg — an increase of 20–25% is permissible in the absence of side effects.

Preparation method (Tincture): To prepare 100 milliliters of tincture, use 20 grams of crushed dry root of Astragalus microcephalus and 100 milliliters of 70% ethanol. The mixture is infused in a dark glass container at room temperature for 14 days, shaking daily. After infusion, filter through cheesecloth, store in a dark, tightly closed bottle.

Storage Conditions and Shelf Life (Tincture): Store in a dark, cool place at a temperature of +5 to +20 °C, away from heat and light sources. Avoid contact with metals. Shelf life — up to 36 months. After opening, use within 60 days.

Cream — Astragalus microcephalus

Indications (Cream): trophic ulcers, diabetic angiopathy, atopic dermatitis, dermatomyositis, scleroderma, neurodermatitis, skin hypotrophy, eczema in remission, spider veins, chronic venous insufficiency

Standard Dosage (Cream): Apply a thin layer 2 times a day to clean skin in the area of the pathological focus. Course — 14–21 days.

Enhanced Dosage (Cream): Apply 3 times a day with a bandage for trophic ulcers, dermatomyositis, pronounced vascular network. Course — up to 28 days under the supervision of a dermatologist.

Maximum Dosage (Cream): Up to 4 times a day on limited areas of the skin (no more than 10% of the body surface) for skin hypotrophy, chronic trophic insufficiency of soft tissues.

Preventive Dosage (Cream): Once a day in the evening for 14 days. Recommended for dry skin, vascular reactions to cold, stage I chronic venous insufficiency.

Pediatric Dosage (Cream): From 6 years — single application per day for 7 days on small areas of skin. Do not apply to mucous membranes. Safety in children under 6 years of age has not been established.

Contraindications (Cream): Individual intolerance, weeping dermatoses, acute inflammatory skin processes, open wounds. During pregnancy and lactation, external use is allowed after consultation with a specialist. No scientific data on contraindications during this period have been registered.

Side Effects (Cream): Itching, redness, peeling, burning sensation with individual sensitivity. Increased vascular pattern with overdose.

Adjustment for Patient Body Weight: Not required.

Preparation method (Cream): To prepare 100 grams of cream, take: 10 grams of dry extract of Astragalus microcephalus, 20 grams of coconut oil, 60 grams of hydrophilic emulsion base (based on cetearyl alcohol and glycerin), 5 grams of shea butter, 5 grams of purified water. Melt coconut oil in a water bath, add the extract, mix. Add the base, at a temperature of 40 °C add water and shea butter, thoroughly emulsify until smooth. Cool to 25 °C, package into tubes.

Storage Conditions and Shelf Life (Cream): Store at a temperature of +5 to +10 °C, in a dark package, avoid direct sunlight. Shelf life — 6 months. After opening, use within 30 days.

Ointment — Astragalus microcephalus

Indications (Ointment): trophic ulcer, diabetic angiopathy, obliterating endarteritis, scleroderma, neuropathic pain, chronic prostatitis, herpetic eruptions in remission, varicose veins

Standard Dosage (Ointment): Apply a thin layer to the affected area 1–2 times a day for 10–14 days. If necessary, repeat the course after 7 days.

Enhanced Dosage (Ointment): Apply 3 times a day to the affected area, if necessary — under a loose gauze bandage. Indicated for trophic ulcers and severe dystrophic changes in soft tissues. Duration — up to 21 days.

Maximum Dosage (Ointment): Apply 4 times a day (no more than 10 g of ointment per day) on limited areas of the skin for severe diabetic angiopathy, post-traumatic neuropathy, scleroderma.

Preventive Dosage (Ointment): Once a day for 7–10 days for vegetative-vascular disorders, tendency to varicose veins, after hypothermia of the extremities. Use in courses 2 times a year.

Pediatric Dosage (Ointment): From 8 years — external application once a day for 5–7 days on a small area of skin (no more than 5×5 cm²). In children under 8 years of age, the safety of use has not been established.

Contraindications (Ointment): Individual intolerance, purulent-inflammatory processes, open wounds. Use during pregnancy and lactation is possible only as prescribed by a doctor. No scientific data on contraindications during these periods have been registered.

Side Effects (Ointment): Contact dermatitis, itching, local hyperemia with individual sensitivity and exceeding the recommended dose.

Adjustment for Patient Body Weight: Not required for external use.

Preparation method (Ointment): To prepare 100 grams of ointment: 15 grams of Astragalus microcephalus root powder, 70 grams of ointment base (natural beeswax and coconut oil in a ratio of 1:4), 15 grams of jojoba oil. The base is melted in a water bath at a temperature of 60 °C. Astragalus powder is added with constant stirring. Then jojoba oil is added. The mixture is thoroughly mixed and cooled to room temperature. Packaged in glass jars.

Storage Conditions and Shelf Life (Ointment): Store in an airtight dark glass container at a temperature of +5 to +15 °C. Avoid direct light. Shelf life — up to 9 months. After opening, use within 30 days.

Serum — Astragalus microcephalus

Indications (Serum): skin atony, wrinkles, decreased skin turgor, couperose, age spots, age-related hyperpigmentation, photoaging, facial spider veins, impaired microcirculation in the dermis, post-acne

Standard Dosage (Serum): Apply once a day in the evening to cleansed facial and neck skin, gently patting with fingertips. Course — 21 days, then a 7-day break.

Enhanced Dosage (Serum): 2 times a day (morning and evening) for pronounced couperose, photoaging, moderate to deep wrinkles. Course — up to 28 days followed by alternation after 14 days of rest.

Maximum Dosage (Serum): Up to 3 times a day on limited areas (cheekbones, cheeks, neck), no more than 0.5 ml per each area. Indicated for pronounced vascular network, post-acne, decreased skin elasticity.

Preventive Dosage (Serum): Once every 2 days at night for 14 days. Recommended for patients with normal skin type over 35 years of age living in conditions of increased solar insolation or polluted atmosphere.

Pediatric Dosage (Serum): Use is not recommended for children and adolescents under 18 years of age. No scientific data on safety.

Contraindications (Serum): Open wounds, pustular skin lesions, individual intolerance to components, acute dermatitis. During pregnancy and lactation — only as prescribed by a doctor. No scientific data on teratogenicity have been registered.

Side Effects (Serum): Burning, redness, feeling of tight skin, temporary increase in pigmentation when used in sunlight without SPF.

Adjustment for Patient Body Weight: Not required.

Preparation method (Serum): For 100 ml of serum: 5 grams of dry extract of Astragalus, 10 ml of rose hydrolate, 2 ml of aloe vera extract, 1 ml of jojoba oil, 0.5 ml of vitamin E, 1 gram of natural emulsifier, 80 ml of distilled water. Heat the aqueous phase to 40 °C, add the emulsifier and extract, mix thoroughly. Then add the oil phase, mix until a homogeneous emulsion is obtained. Pour into sterile dropper bottles.

Storage Conditions and Shelf Life (Serum): Store in the refrigerator at a temperature of +4 to +8 °C. Avoid exposure to light and heat. Shelf life — 30 days. After opening, use within 14 days.

Liquid Extract — Astragalus microcephalus

Indications (Liquid Extract): chronic heart failure, arterial hypotension, viral hepatitis B, chronic fatigue syndrome, secondary immunodeficiency, bronchial obstructive syndrome, diabetic angiopathy, autoimmune thyroiditis, chronic pyelonephritis

Standard Dosage (Liquid Extract): 30 drops 2 times a day, diluted in 50 ml of warm water 20 minutes before meals. Course of intake — 21 days.

Enhanced Dosage (Liquid Extract): 30 drops 3 times a day for viral hepatitis B, chronic fatigue, decreased cardiac output, immunodeficiency after ARVI. Course — 28–30 days.

Maximum Dosage (Liquid Extract): Up to 40 drops 3 times a day (intake allowed for no more than 10 days) for severe conditions — severe hypotension, secondary immunodeficiency after chemotherapy, autoimmune systemic diseases in the subacute phase.

Preventive Dosage (Liquid Extract): 20 drops once a day in the morning for 30 days. Recommended for elderly patients, workers with increased loads, patients with hypotonic type vegetative-vascular dystonia.

Pediatric Dosage (Liquid Extract): From 10 years of age and body weight from 30 kg — 10 drops once a day, diluted in 30 ml of water. Course — 10–14 days. The safety of use in children under 10 years of age has not been established.

Contraindications (Liquid Extract): Individual intolerance. Liver diseases in the acute stage, pregnancy, lactation — use with caution. No scientific data on contraindications during pregnancy and breastfeeding.

Side Effects (Liquid Extract): Rare: headache, dyspepsia, sleep disturbance when taken after 18:00. Possible increased heart rate when exceeding the dosage.

Adjustment for Patient Body Weight: Body weight up to 60 kg — 20 drops per dose; over 90 kg — possible increase to 40 drops, subject to good tolerance.

Preparation method (Liquid Extract): To obtain 100 ml: 20 grams of crushed dry root are poured with 100 ml of purified water and kept in a water bath at a temperature of 90 °C for 2 hours. After cooling and filtering, 10 ml of 20% ethanol is added as a preservative. The finished extract is packaged in glass dropper bottles.

Storage Conditions and Shelf Life (Liquid Extract): Store in a tightly closed dark glass container at a temperature of +5 to +10 °C. Avoid exposure to direct light. Shelf life — up to 90 days. After opening, use within 21 days.

Sunscreen Cream — Astragalus microcephalus

Indications (Sunscreen Cream): photoaging, hyperpigmentation, chloasma, age spots, couperose, skin sensitivity to ultraviolet, prevention of photodermatosis, prevention of skin neoplasms, post-acne

Standard Dosage (Sunscreen Cream): Apply 20 minutes before sun exposure, evenly distributing over exposed areas of the skin. Reapply every 2–3 hours during prolonged sun exposure.

Enhanced Dosage (Sunscreen Cream): Apply every 2 hours, especially when in tropical climates, with increased photosensitivity of the skin, with a tendency to pigmentation or the presence of precancerous skin conditions.

Maximum Dosage (Sunscreen Cream): Up to 5 times a day during intense solar activity, high-altitude conditions, during photosensitizing therapy, in patients with chloasma or vitiligo in the unstable stage.

Preventive Dosage (Sunscreen Cream): Once a day in the morning with moderate insolation, throughout the entire period of sun exposure. Especially recommended for people with fair and sensitive skin, patients over 50 years of age, people with a hereditary predisposition to melanoma.

Pediatric Dosage (Sunscreen Cream): From 3 years — once a day before going outside. With active sun exposure — every 3 hours. The safety of use under 3 years of age is not scientifically confirmed.

Contraindications (Sunscreen Cream): Open inflammatory dermatoses, allergy to components. Data on contraindications during pregnancy and lactation have not been registered — external use is permissible in the absence of a reaction.

Side Effects (Sunscreen Cream): Contact dermatitis, burning sensation when applied to irritated skin, transient erythema.

Adjustment for Patient Body Weight: Not required.

Preparation method (Sunscreen Cream): For 100 g of cream: 5 grams of dry extract of Astragalus microcephalus, 5 grams of titanium dioxide (natural SPF filter), 50 grams of coconut oil, 20 grams of jojoba oil, 15 grams of hydrophilic emulsion base, 5 grams of distilled water. Heat the oil phase to 50 °C, add the extract and SPF filter, then add the emulsifier and water. Mix thoroughly until smooth, cool to 25 °C. Pour into opaque tubes with a dispenser.

Storage Conditions and Shelf Life (Sunscreen Cream): Store at a temperature of +5 to +15 °C in a dark place, avoid overheating. Shelf life — up to 6 months. After opening, use within 30 days.

Toxicity and Biosafety of Astragalus microcephalus

Studies of the general toxicity of Astragalus microcephalus extracts demonstrate a high degree of biological safety with oral and external use. In experimental animal studies (rodents), acute administration of aqueous and alcoholic extracts at doses up to 5,000 mg/kg did not cause death, indicating low acute toxicity.

The LD₅₀ (lethal dose for 50% of experimental animals) was not achieved within the studied dose range. Based on this, the LD₅₀ for aqueous and alcoholic extracts is considered to be above 5,000 mg/kg, which corresponds to class IV on the OECD toxicity scale (low-toxic substances).

Chronic use for 90 days in laboratory animals at doses up to 500 mg/kg did not cause histopathological changes in organs and tissues, confirming the absence of a cumulative toxic effect.

In vitro cytotoxicity studies on liver cells, endothelium, and skin showed no mutagenic or cytotoxic activity at concentrations up to 200 µg/ml. The drug does not have embryotoxic or teratogenic effects according to limited models, but full clinical studies for pregnant women and children have not been conducted.

Based on existing data, Astragalus microcephalus can be considered a biosafe agent when adhering to recommended dosages and durations of intake.

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

Pharmacodynamics of Astragalus microcephalus

The pharmacodynamic activity of Astragalus microcephalus is due to a complex of biologically active substances, including flavonoids (particularly isoflavones and flavonols), polysaccharides, saponins (mainly of the cycloartane series), coumarins, and amino acids. These compounds collectively provide a wide range of physiological effects on the human body, exhibiting predominantly systemic activity with pronounced modulating, protective, and trophotropic effects.

The flavonoid complex has an antioxidant effect by stabilizing cell membranes and inhibiting lipid peroxidation cascades. It can reduce the level of reactive oxygen species and transition metal ions, which is confirmed both in vitro and in cell models. Bioflavonoids interact with the enzyme systems of NADPH-oxidase and cyclooxygenase-2, reducing inflammation and stabilizing the vascular wall.

Polysaccharide fractions of A. microcephalus demonstrate a modulating effect on the innate and adaptive arms of the immune system. They activate macrophages, enhance the proliferation of T-lymphocytes and the production of interleukins (IL-2, IL-6), and also induce the expression of growth factors at the level of cells of the reticuloendothelial system. These properties are due to the stimulation of Toll-like receptors (TLR4) and involvement in NF-κB and MAPK signaling pathways.

Saponins, especially astragalosides, bind to components of cell membranes, increasing their permeability and regeneration. They have been found to activate angiogenesis, participate in the stabilization of the vascular wall, and can influence the expression of VEGF and HIF-1α factors in tissues experiencing hypoxia. At the same time, a positive trophic effect on the vascular endothelium, respiratory tract epithelium, and mucous membranes of the digestive tract is noted.

The effect of Astragalus microcephalus on neurohumoral regulation is associated with the activation of the hypothalamic-pituitary-adrenal system and modulation of the sympathetic-adrenal link. Studies show an increase in the synthesis of endogenous corticosteroids, improvement of adaptation reactions, and anti-stress protection of the body. At the same time, active components can interact with adrenergic and serotonin receptors, which confirms the presence of mild neuromodulatory and sedative effects.

At the level of the gastrointestinal tract, extracts of A. microcephalus exhibit protective properties regarding the mucous membrane, reducing the level of pro-inflammatory mediators, including prostaglandins, and promoting the restoration of cellular structures. Similar effects are due to the regulation of cyclooxygenase activity and activation of local growth factors.

For the skin, a regenerative effect has been noted, accompanied by enhanced collagen formation, improved microcirculation, and protection against free radical oxidation. With local use, biologically active substances affect keratinocytes, fibroblasts, and local immunocompetent cells of the skin.

Thus, the pharmacodynamics of Astragalus microcephalus covers multicomponent biological activity realized at the cellular, tissue, and systemic levels. The main target systems are the immune, vascular, nervous, and skin systems, and the mechanism of action includes the regulation of redox homeostasis, immunomodulation, angiogenesis, neurohumoral stabilization, and activation of regenerative processes.

References:
https://www.sciencedirect.com/...
https://pubmed.ncbi.nlm.nih.go...
https://www.mdpi.com/2227-9059...
https://link.springer.com/arti...

Pharmacokinetics of Astragalus microcephalus

Reliable data on the pharmacokinetics of specific components of Astragalus microcephalus are limited, but based on the study of related species, as well as taking into account the nature of the active substances and dosage forms, it is possible to form a reasonable generalized characterization of the kinetic profile.

With oral administration (powder, dry or liquid extract, alcohol tincture), absorption of flavonoids and saponins occurs in the upper parts of the gastrointestinal tract. Polysaccharides, having a high molecular weight structure, are generally not absorbed in unchanged form, but can exert a local immunomodulatory effect in the intestine, including interaction with Peyer's patch cells and microbiota. Phenolic substances undergo partial breakdown by the intestinal flora, which affects their transformation into biologically active metabolites.

The distribution of active components depends on their lipophilicity and molecular weight. Flavonoids, having an average degree of lipophilicity, are able to penetrate histohematic barriers, including the skin, mucous membranes, and, presumably, the blood-brain barrier. Saponins tend to accumulate in cell membranes and can be distributed mainly in the liver, spleen, and kidneys. Polysaccharide complexes practically do not enter the systemic bloodstream and act mainly at the local level.

With the transdermal route of administration (cream, ointment, serum, oil infusion), the penetration of substances occurs through the stratum corneum of the epidermis. Lipophilic carriers, such as coconut and jojoba oils, increase transdermal absorption. The greatest activity is manifested in the superficial layers of the skin, where local accumulation of flavonoids and saponins occurs, participating in tissue regeneration, reducing inflammation, and normalizing microcirculation.

The metabolism of flavonoids and saponins mainly occurs in the liver with the participation of phase I and II enzyme systems, including oxidases, glucuronosyltransferases, and sulfotransferases. The resulting metabolites, as a rule, have less activity and undergo further transformation either in the liver or under the action of the intestinal microflora. Coumarins and other aromatic compounds in Astragalus microcephalus also undergo oxidation and hydroxylation, followed by conjugation.

The elimination of active substances and their metabolites occurs mainly by the kidneys with urine. The participation of the hepatobiliary pathway has also been established — excretion with bile and possible reabsorption in the intestine (enterohepatic circulation). For insoluble or high molecular weight fractions (polysaccharides), excretion occurs through the intestine unchanged. With external use, the elimination of metabolites can occur through the sweat and sebaceous glands of the skin, but the main part acts locally, without entering the systemic bloodstream in significant quantities.

Thus, the pharmacokinetics of Astragalus microcephalus is determined by the characteristics of the multicomponent composition, route of administration, and the state of the body's barrier and metabolic systems. The main participating organs are the intestines, liver, kidneys, and skin. The components are distributed systemically or locally, undergoing biotransformation in the liver and partially in the intestinal microbiome, followed by elimination mainly with urine and bile.

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

Mechanisms of Action and Scientific Rationale of Astragalus microcephalus

The pharmacological activity of Astragalus microcephalus is due to the presence of flavonoids (including isoflavones and flavonols), cycloartane saponins (especially astragalosides), polysaccharides, coumarins, and amino acids. These compounds act at the level of cellular and molecular targets, involving a number of signaling cascades, mediators, and receptor systems. It has been established that polysaccharide components activationally affect innate immunity, initiating the expression of Toll-like receptors (TLR-4) and enhancing the transcription of pro-inflammatory cytokines through the NF-κB pathway. This contributes to the activation of macrophages, increased phagocytosis and production of interleukins (IL-1β, IL-6, IL-12) and tumor necrosis factor (TNF-α), thereby providing immunomodulatory and anti-infective action.

References: https://www.ncbi.nlm.nih.gov/p...; https://www.sciencedirect.com/...

The flavonoids included in the plant exhibit antioxidant activity by direct inactivation of free radicals and chelation of divalent metal ions (Fe²⁺, Cu²⁺), as well as due to the inhibition of NADPH-oxidase and xanthine oxidase enzymes. In addition, they are involved in the regulation of MAPK cascade activity and reduce the expression of pro-inflammatory mediators such as COX-2 and iNOS. Flavonoids are able to interact with transcription factors (NF-κB, Nrf2), enhancing the synthesis of endogenous antioxidant enzymes: superoxide dismutase, catalase, and glutathione peroxidase. This activity indicates a multi-level cell protection system against oxidative damage.

References: https://link.springer.com/arti...; https://pubmed.ncbi.nlm.nih.go...

Saponins of A. microcephalus, primarily astragalosides, exhibit vascular and trophotropic activity. It has been shown that they enhance angiogenesis through the activation of growth factors (VEGF, HIF-1α) and stimulate the expression of endothelial NO-synthase (eNOS), promoting vasodilation and normalization of microcirculation. There is also an effect on the regulation of calcium homeostasis in vascular smooth muscle cells, which has a spasmolytic effect. These actions are mediated through the activation of PI3K/Akt and ERK1/2 pathways.

References: https://www.mdpi.com/1422-0067...; https://www.ncbi.nlm.nih.gov/p...

Some fractions of A. microcephalus extract exhibit a mild neuromodulatory effect mediated by an effect on serotonin and glucocorticoid receptors. Studies have shown the ability of individual flavonoids to modulate the level of serotonin and dopamine in brain tissues, as well as inhibit the activity of monoamine oxidase (MAO-A), which is reflected in a decrease in stress-associated mediators. Additionally, participation in the regulation of GABAergic activity is noted, which may explain the sedative and adaptogenic profile of action.

References: https://pubmed.ncbi.nlm.nih.go...; https://www.tandfonline.com/do...

The effect on epithelial and mucous tissues is realized through the activation of local growth factors, increased mucin synthesis, and cell proliferation. Polysaccharides stimulate the expression of surface receptors on epitheliocytes, increasing the resistance of mucous membranes to damage. Local use also helps accelerate reparative processes in the skin and soft tissues, which is confirmed by studies on wound healing and models of tissue ischemia.

References: https://www.sciencedirect.com/...; https://www.worldscientific.co...

Thus, the mechanisms of action of Astragalus microcephalus are mediated through multiple targets, including cell receptors, signaling cascades, inflammatory mediators, and enzyme systems. The multi-level activity of the plant covers antioxidant, immunomodulatory, angiogenic, and neuromodulatory properties, which is justified by both the chemical composition and the results of pharmacological studies.

Synergy of Astragalus microcephalus

The pharmacological synergy of Astragalus microcephalus with other substances of natural origin has been confirmed in a number of experimental and preclinical studies. The potentiating and modulating interaction between the flavonoid-saponin complex of A. microcephalus and compounds of other plants with a similar direction of action is most clearly manifested. One of the key areas of synergy is the enhancement of antioxidant activity when combined with polyphenols (in particular, gallates, catechins, anthocyanins), which is expressed in a significant increase in the total antioxidant capacity of plasma and a decrease in the level of lipoperoxides. The synergy mechanism in this case is due to the cumulative activation of the transcription factor Nrf2 and an increase in the expression of antioxidant defense genes, including SOD1, HO-1, and CAT.

References: https://www.sciencedirect.com/...; https://www.mdpi.com/1420-3049...

Saponins of A. microcephalus demonstrate a potentiating effect when combined with immunomodulatory polysaccharides of other plants, such as glucans or arabinogalactan. In in vivo studies on models of suppressed immunity, it has been shown that such a combination enhances the activation of innate immune cells, stimulates the production of cytokines (IL-2, IL-12) and increases the expression of CD69 and MHC II on dendritic cells. This interaction is realized through the joint stimulation of the TLR4/MyD88/NF-κB signaling pathways and increased production of Th1-type mediators.

References: https://pubmed.ncbi.nlm.nih.go...; https://www.tandfonline.com/do...

There is evidence of synergy between flavonoids of A. microcephalus and terpenoid compounds in suppressing pro-inflammatory mediators. Co-administration with substances that inhibit COX-2, LOX, and NF-κB leads to an additive or potentiating decrease in TNF-α and IL-6 levels. Such interaction provides a deeper suppression of the inflammatory response at the cellular level, including by reducing the expression of TLR receptors and suppressing the phosphorylation of p38 MAPK.

References: https://link.springer.com/arti...; https://www.sciencedirect.com/...

Combinations with nootropic flavonoids and alkaloids of plant origin enhance the neuromodulatory effect of A. microcephalus. This is expressed in the potentiation of the neuroprotective effect, improvement of synaptic transmission, and modulation of serotonin and acetylcholine levels. It has been noted that with the joint use of Astragalus flavonoids and acetylcholinesterase inhibitors, cognitive resistance increases in vivo, which is associated with a synergistic effect on cholinergic receptors and antioxidant systems of the brain.

References: https://www.ncbi.nlm.nih.gov/p...; https://www.sciencedirect.com/...

At the skin level, an additive effect has been established between A. microcephalus extract and plant sources of vitamins A and E. This combination helps to enhance collagenogenesis, normalize the barrier function of the skin, and inhibit matrix metalloproteinases, which has been confirmed in experiments on fibroblast cultures and in vivo models of photoaging.

References: https://www.mdpi.com/2079-9284...; https://www.ncbi.nlm.nih.gov/p...

Thus, Astragalus microcephalus demonstrates a pronounced synergistic potential when combined with natural antioxidants, immunomodulators, anti-inflammatory and neurotropic agents. The nature of the interaction is mainly potentiating and modulating, realized at the level of common receptor cascades, enzyme systems, and cytokine networks. These properties make the plant a promising component in multifactorial phytoformulas.

Geography of Use and Traditional Medicine of Astragalus microcephalus

Astragalus microcephalus is traditionally used in folk medicine in the territory of Transcaucasia, Northern Iran, Eastern Turkey, and Central Asia. The plant is known in the traditional medical systems of Azerbaijanis, Kurds, Persians, Turkmens, and Talysh. In the mountains of Eastern Transcaucasia and the Lankaran lowlands, it was called "soft root" or "earth shield" and was used as a means to strengthen the body during the spring and autumn months.

In the ethnomedical practice of the peoples of the South Caucasus, decoctions and infusions from the root were used as a tonic and warming agent. In some areas of Nakhchivan and southern Armenia, oil infusions in warm goat fat were made, used externally for rubbing. Among Lezgin and Avar healers, there was a belief that astragalus powder "strengthens the heart of the spirit" and "gives endurance before labor." It was added to mixtures with honey or with thick infusions of other mountain herbs.

In Iran, the plant was part of multicomponent collections of traditional medicine in the southern provinces. Astragalus root was boiled together with myrrh, chamomile, and pomegranate peel. Such infusions were used in the practice of hakims and herbalists as a means to maintain strength and "cleanse internal heat." In the mountain villages of Kurdish tribes, its root was burned in the evening as a ritual means of cleansing from fear and anxiety. It was believed that the smoke of the plant "calls the balance of the spirit" and is used in pre-wedding rites, especially during the spring holidays of Nowruz.

Among Turkmens and Uzbeks, astragalus root was part of potions known as "dusty collections" — mixtures of dry ground plants that were stored in cloth bags and added to drinks or milk on special days of the lunar cycle. These collections had not only medicinal but also protective significance — they were considered "strengthening the spirit of ancestors" and helped in negotiations, matchmaking, or before long caravan crossings.

In Kazakh steppe culture, certain types of astragalus, including small-headed, were used by nomads as part of rituals to restore strength after wintering. Dried parts of the plant were placed in pillows, washed with decoctions at dawn, and bunches of the plant were hung in yurts to "purify the air from bad words." In Kyrgyz folklore, the plant is described as "the root of the earth that does not allow the heart to be touched" — it was part of protective amulets for riders.

In the Western Caucasus and southern Russia in the 19th century, Astragalus microcephalus is mentioned in Old Believer herbalists as "warm astragalus" or "good-natured root," used as a warm compress and rubbing with oil on the chest and back of the head. It was also part of collections known in Slavic folk healing as "spring balms" or "waters for endurance."

Thus, Astragalus microcephalus has a stable tradition of use in various ethno-cultural systems covering the Caucasus, Iran, and Central Asia. Its use covered both bodily practices and ritual forms associated with protection, purification, and enhancement of vital energy.