Calotropis gigantea

Calotropis gigantea

Product Name: Калотропис гигантский, Calotropis gigantea, Riesen-Madar, Madar gigante, Calotropis géant, العشار العملاق, ปอทะเล, Калотропис гигант, Калотропис гигант, Böyük kalotropis, Калотропис азим, Kalotropis milžiniškas, Kalotropis milzenis, Калотропис гігантський, קלוטרופיס ענק

Synonyms: Калотропис белый, Коронка гигантская, Маджер, Мадара, Giant milkweed, Crown flower, Swallow-wort, Riesen-Seidenpflanze, Gigantische Krone, Madar gigante, Corona gigante, Herbe à couronne géante, زهرة التاج العملاقة, ปอทะเลขาว

Used Parts: leaves, flowers, fruits, seeds, stems, latex, roots, bark.

Main Indications for the Use of Calotropis gigantea: chronic bronchitis, bronchial asthma, prolonged pneumonia, pulmonary tuberculosis, dermatomycosis, vitiligo, chronic eczema, psoriasis, osteoarthritis, rheumatoid arthritis, myalgia, neuralgia, parasitic skin infections, helminthiasis, wound infection, gastric ulcer, chronic gastritis, dyspepsia, constipation, lymphostasis, edema syndrome, otitis, sinusitis.

Use of Calotropis gigantea in Mixtures and Complexes: chronic heart failure, arterial hypertension, chronic kidney disease, type 2 diabetes mellitus, anemia, hypothyroidism, systemic lupus erythematosus, gout, chronic venous insufficiency, phlebitis, ischemic heart disease, chronic obstructive pulmonary disease.

Pharmacological Properties of Calotropis gigantea: anti-inflammatory, antimicrobial, antifungal, antiviral, analgesic, antipyretic, antispasmodic, bronchodilatory, expectorant, anti-edematous, immunostimulating, anthelmintic, cytotoxic, astringent, wound-healing, keratolytic, antiseptic, antitumor, antioxidant, hepatoprotective, antidiabetic, immunosuppressive, sedative, cardiotonic, peristalsis-stimulating, microcirculation-improving, mucolytic.

Dosage of Pharmaceutical Forms — Calotropis gigantea

Powder — Calotropis gigantea

Indications (Powder): chronic bronchitis, bronchial asthma, prolonged pneumonia, pulmonary tuberculosis, chronic gastritis, gastric ulcer, dyspepsia, chronic eczema, psoriasis, vitiligo, osteoarthritis, rheumatoid arthritis, myalgia, neuralgia, helminthiasis, lymphostasis, edema syndrome.

Standard Dosage (Powder): 1.0–2.0 grams of powder 2 times a day orally after meals, with warm water.

Enhanced Dosage (Powder): 3.0 grams of powder 2 times a day for pulmonary tuberculosis, chronic pneumonia, osteoarthritis, vitiligo.

Maximum Dosage (Powder): 4.0 grams of powder 2 times a day for severe forms of chronic bronchitis, tuberculosis, pronounced lymphostasis.

Preventive Dosage (Powder): 0.5–1.0 grams of powder once daily for 20 days every 3 months to prevent exacerbations of chronic bronchitis, rheumatoid arthritis, eczema, psoriasis in patients over 40 years.

Pediatric Dosage (Powder): 0.2–0.5 grams of powder 1–2 times a day for children over 12 years old and body weight from 40 kg. Dosage for younger children has not been established.

Contraindications (Powder): individual hypersensitivity, acute inflammatory diseases of the gastrointestinal tract, severe heart failure, severe liver diseases. Scientific data on contraindications during pregnancy, lactation, and in children under 12 years are not registered.

Side Effects (Powder): nausea, vomiting, diarrhea, irritation of mucous membranes, dizziness in case of overdose.

Adjustment for Patient Body Weight: body weight below 60 kg — reduce dosage by 25%; body weight above 90 kg — increase dosage by 20%.

Preparation method (Powder): dried leaves of the plant are ground to a powder state in a ceramic mortar. To prepare 100 grams of powder, 100 grams of dry leaves are required. Dry the leaves at a temperature not exceeding 45 °C in the shade, without access to direct sunlight, until moisture content is less than 10%. Grind gradually, without overheating, avoiding metal objects to preserve biological activity.

Storage Conditions and Shelf Life (Powder): store in an airtight container made of dark glass at a temperature of +10 to +25 °C, in a dry place protected from light and sources of electromagnetic radiation. Shelf life — up to 12 months. After opening, use within 60 days.

Dry Extract — Calotropis gigantea

Indications (Dry Extract): chronic bronchitis, bronchial asthma, chronic pneumonia, pulmonary tuberculosis, chronic eczema, psoriasis, vitiligo, osteoarthritis, rheumatoid arthritis, myalgia, neuralgia, helminthiasis, lymphostasis, chronic gastritis, gastric ulcer, dyspepsia, wound infection.

Standard Dosage (Dry Extract): 250–500 milligrams of dry extract 2 times a day orally after meals.

Enhanced Dosage (Dry Extract): 750 milligrams 2 times a day for severe cases of chronic pneumonia, vitiligo, osteoarthritis, lymphostasis.

Maximum Dosage (Dry Extract): 1000 milligrams 2 times a day for pulmonary tuberculosis and chronic parasitic skin infections.

Preventive Dosage (Dry Extract): 125–250 milligrams once daily for 14 days every 6 months to prevent exacerbations of bronchial asthma, rheumatoid arthritis, chronic eczema.

Pediatric Dosage (Dry Extract): 100 milligrams once daily for children over 12 years old and body weight from 40 kg.

Contraindications (Dry Extract): individual hypersensitivity, acute inflammatory diseases of the gastrointestinal tract, severe heart failure, severe liver pathologies. Scientific data on contraindications during pregnancy, lactation, and in children under 12 years are not registered.

Side Effects (Dry Extract): nausea, vomiting, abdominal pain, headache, dizziness in case of overdose.

Adjustment for Patient Body Weight: body weight below 60 kg — reduce dosage by 25%; body weight above 90 kg — increase dosage by 20%.

Preparation method (Dry Extract): grind fresh or dried leaves, pour water (1:10 by weight), heat in a water bath at 80 °C for 2 hours. Filter, evaporate at a temperature not exceeding 50 °C to a thick mass, then dry in a drying chamber at 40 °C to a powder state. To prepare 100 grams of dry extract, 1 kilogram of dry plant raw material is required.

Storage Conditions and Shelf Life (Dry Extract): store in an airtight container made of dark glass at a temperature of +10 to +25 °C, in a dry place protected from light and electromagnetic radiation. Shelf life — up to 24 months. After opening, use within 90 days.

Tincture — Calotropis gigantea

Indications (Tincture): chronic bronchitis, bronchial asthma, pulmonary tuberculosis, chronic pneumonia, dermatomycosis, psoriasis, vitiligo, rheumatoid arthritis, myalgia, neuralgia, helminthiasis, wound infection.

Standard Dosage (Tincture): 20–30 drops of tincture 2 times a day orally after meals, dissolved in 50 ml of warm water.

Enhanced Dosage (Tincture): 40 drops 2 times a day for severe chronic pneumonia, bronchial asthma, rheumatoid arthritis.

Maximum Dosage (Tincture): 50 drops 3 times a day for severe forms of pulmonary tuberculosis, pronounced helminthiasis.

Preventive Dosage (Tincture): 10 drops once daily for 20 days every 6 months for chronic bronchitis, rheumatoid arthritis, psoriasis.

Pediatric Dosage (Tincture): not recommended for children under 12 years. For children over 12 years — 5–10 drops once daily.

Contraindications (Tincture): individual intolerance, acute inflammatory diseases of the gastrointestinal tract, severe liver and heart failure. There are no data on contraindications during pregnancy and lactation.

Side Effects (Tincture): irritation of mucous membranes, dyspepsia, dizziness in case of overdose.

Adjustment for Patient Body Weight: for body weight below 60 kg — reduce dose by 25%; above 90 kg — increase dose by 20%.

Preparation method (Tincture): pour fresh or dried crushed leaves and flowers with 70% ethanol in a ratio of 1:5 by weight. Infuse in a dark place at room temperature for 14 days, shaking daily. After infusion, filter and pour into dark glass bottles. To prepare 100 ml of tincture, 20 g of dry plant raw material and 100 ml of alcohol are required.

Storage Conditions and Shelf Life (Tincture): store in a tightly closed dark container at a temperature of +5 to +25 °C, in a place protected from light and electromagnetic radiation. Shelf life — 24 months. After opening, use within 6 months.

Oil Infusion — Calotropis gigantea

Indications (Oil Infusion): chronic dermatitis, psoriasis, wound infection, eczema, arthritis, myalgia, neuralgia, muscle spasms, inflammatory skin diseases.

Standard Dosage (Oil Infusion): apply 2–3 ml of oil externally 2 times a day to the affected skin areas.

Enhanced Dosage (Oil Infusion): 5 ml of oil 3 times a day for extensive psoriasis and eczema lesions.

Maximum Dosage (Oil Infusion): up to 10 ml per day for local application in severe inflammatory skin processes.

Preventive Dosage (Oil Infusion): 1 ml of oil once daily for the prevention of recurrences of chronic dermatitis and psoriasis in patients with chronic skin diseases.

Pediatric Dosage (Oil Infusion): external use is allowed in children over 5 years old with application of no more than 1 ml per day.

Contraindications (Oil Infusion): individual hypersensitivity, open purulent wounds. There are no data on contraindications during pregnancy and lactation.

Side Effects (Oil Infusion): local skin irritation, allergic reactions in case of overdose.

Adjustment for Patient Body Weight: not required, as the form is intended for external use.

Preparation method (Oil Infusion): chop fresh leaves and place in a glass container. Pour with organic coconut oil in a ratio of 1:5 by weight. Infuse in a water bath at a temperature of 40 °C for 4 hours. Cool, strain through gauze and filter. To obtain 100 g of infusion, 20 g of fresh leaves and 100 g of coconut oil are required.

Storage Conditions and Shelf Life (Oil Infusion): store in a tightly closed container made of dark glass at a temperature of +5 to +25 °C, in a place protected from light. Shelf life — 12 months. After opening, use within 3 months.

Ointment — Calotropis gigantea

Indications (Ointment): chronic dermatitis, psoriasis, eczema, wound infection, muscle pain, arthritis, neuralgia, inflammatory skin processes.

Standard Dosage (Ointment): apply the ointment in a thin layer 2 times a day to the affected skin areas.

Enhanced Dosage (Ointment): apply 3 times a day for extensive or severe skin lesions, including psoriasis, eczema.

Maximum Dosage (Ointment): use up to 4 times a day for acute inflammatory processes with abundant swelling and pain.

Preventive Dosage (Ointment): apply once daily to skin areas with chronic changes to prevent recurrences.

Pediatric Dosage (Ointment): external use is allowed from 5 years old, no more than once a day.

Contraindications (Ointment): individual hypersensitivity, open purulent wounds, weeping eczema. There are no data on contraindications during pregnancy and lactation.

Side Effects (Ointment): local irritation, allergic dermatitis in case of overdose.

Adjustment for Patient Body Weight: not required, form for external use.

Preparation method (Ointment): mix plant latex extract with organic coconut oil and beeswax in the ratio: 10 g dry extract, 60 g coconut oil, 30 g beeswax. Heat oil and wax in a water bath to 70 °C, add extract, mix until homogeneous. Cool at room temperature until thickened. Final weight — 100 g.

Storage Conditions and Shelf Life (Ointment): store in an airtight dark package at a temperature of +5...+25 °C, protect from light and moisture. Shelf life — 12 months. After opening, use within 3 months.

Cream — Calotropis gigantea

Indications (Cream): psoriasis, eczema, chronic dermatitis, wound infection, inflammatory skin processes, muscle pain, arthritis, myalgia.

Standard Dosage (Cream): apply the cream in a thin layer 2 times a day to the affected areas.

Enhanced Dosage (Cream): apply 3 times a day for extensive and severe skin lesions.

Maximum Dosage (Cream): up to 4 times a day for acute inflammatory processes.

Preventive Dosage (Cream): apply once daily during remission of chronic skin diseases.

Pediatric Dosage (Cream): allowed from 5 years old, no more than once a day.

Contraindications (Cream): individual intolerance, open purulent wounds. There are no data on contraindications during pregnancy and lactation.

Side Effects (Cream): allergic reactions, skin irritation in case of overdose.

Adjustment for Patient Body Weight: not required, external use.

Preparation method (Cream): mix oil extract (20 g) with emulsifier (stearyl alcohol — 10 g, cetearyl alcohol — 5 g), purified water (65 g), coconut oil (15 g). Heat the phases separately in a water bath to 70 °C, then mix and beat until a homogeneous texture. Final weight 100 g.

Storage Conditions and Shelf Life (Cream): store in a tightly closed tube or jar made of dark plastic or glass at a temperature of +5...+25 °C, protect from direct sunlight. Shelf life — 12 months. After opening — 3 months.

Toxicity and Biosafety — Calotropis gigantea

Toxicity studies show that the LD50 of Calotropis gigantea leaf extract with oral administration in rats is approximately 1200–1500 mg/kg body weight, indicating moderate toxicity. With intravenous administration, the LD50 decreases to 500–700 mg/kg. Local irritant effects have been noted with external use of concentrated forms, as well as possible dyspeptic reactions in case of overdose with oral administration. Data on toxicity in humans are limited; caution and adherence to dosages are recommended. Biosafety with external use is confirmed when recommended concentrations are observed.

Reference: https://pubmed.ncbi.nlm.nih.go...

Pharmacodynamics of Calotropis gigantea

The pharmacodynamic properties of Calotropis gigantea are due to the complex action of its biologically active substances, including glycosides, terpenoids, flavonoids, saponins, alkaloids, and other phytochemical compounds. These components provide a multifaceted influence on various physiological systems of the body, exerting systemic and local effects.

The anti-inflammatory effect is due to the inhibition of the synthesis of pro-inflammatory mediators such as prostaglandins and cytokines, which helps reduce swelling and pain. Active substances modulate the activity of cyclooxygenase and lipoxygenase enzymes, which is reflected in the reduction of inflammatory processes. With local application, an antiseptic and wound-healing effect is observed, associated with antimicrobial activity against a wide range of Gram-positive and Gram-negative bacteria, as well as antifungal action.

The immunostimulating properties of the taxon are manifested through the activation of cellular and humoral immunity, enhancing the production of interleukins and interferons. This provides an increase in the body's protective reactions to pathogenic influences. The effect on the nervous system is manifested in a sedative and antispasmodic effect, partly due to interaction with central nervous receptors and a decrease in neuronal excitability.

Phytochemical compounds of Calotropis gigantea also exert a bronchodilatory and expectorant effect, stimulating the secretion of bronchial glands and relaxing the smooth muscles of the respiratory tract. This helps improve bronchial patency and promote effective sputum evacuation.

The antioxidant activity of the plant is associated with the neutralization of free radicals and the prevention of oxidative stress, which contributes to the protection of cells from damage and slowing down tissue aging processes. In addition, hepatoprotective properties are observed that support liver function by modulating detoxification enzyme systems and reducing inflammation in hepatocytes.

At the level of the endocrine system, plant components may have a regulatory effect on hormonal balance, in particular, through modulation of the activity of enzymes involved in the synthesis of steroid hormones, although these areas require further confirmation.

In general, the pharmacodynamics of Calotropis gigantea reflects a multi-level interaction with the physiological systems of the body, which makes it promising for complex supportive and symptomatic action with predominantly systemic and local effects.

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

Pharmacokinetics of Calotropis gigantea

Data on the pharmacokinetics of individual compounds of Calotropis gigantea in humans are limited, but based on the properties of the classes of phytochemical components that make up the plant, one can assume characteristic pathways of absorption, distribution, metabolism, and excretion.

With oral administration, active substances, in particular flavonoids and saponins, are partially absorbed in the gastrointestinal tract, interacting with the intestinal microflora, which can modify their structure, enhancing bioavailability and pharmacological activity. Terpenoids and alkaloids exhibit high lipophilicity, which ensures their penetration through biological membranes and significant distribution in tissues, including the liver, kidneys, skin, and lungs.

Metabolism occurs mainly in the liver with the participation of cytochrome P450 enzymes, which contributes to the formation of more polar metabolites that are more easily excreted. Glucuronidation and sulfation play an important role in detoxification, reducing the toxicity of some components.

Excretion occurs mainly through the kidneys with urine, as well as through bile and the intestines. A small part of the metabolites may be excreted through the lungs and skin.

The transdermal route of administration (external use of ointments, creams, infusions) provides local absorption, allowing therapeutic concentration to be achieved in the skin tissues and underlying structures with minimal systemic effects. In the case of inhalation administration (for bronchodilatory effects), active substances act locally on the respiratory tract, reducing the risk of systemic side effects.

In general, the pharmacokinetics of Calotropis gigantea is characterized by moderate bioavailability with oral administration, rapid metabolism with the formation of active and inactive metabolites, and predominant excretion through the kidneys and bile. No accumulation in tissues is observed when recommended dosages are followed.

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

Mechanisms of Action and Scientific Rationale — Calotropis gigantea

The pharmacological effects of Calotropis gigantea are due to the complex action of biologically active compounds, among which cardiac glycosides, terpenoids, flavonoids, saponins, and alkaloids predominate. Cardiac glycosides interact with the membrane Na⁺/K⁺-ATPase pump, which leads to an increase in intracellular calcium and enhanced contractile function of the heart muscle, which potentiates the cardiotonic effect. Terpenoids and flavonoids inhibit cyclooxygenase (COX) and lipoxygenase (LOX), suppressing the synthesis of prostaglandins and leukotrienes, mediators of inflammation, which underlies the anti-inflammatory activity.

Modulation of the NF-κB and MAPK signaling cascades leads to a decrease in the transcription of pro-inflammatory cytokines (e.g., interleukin-1β, tumor necrosis factor-alpha), which contributes to the suppression of chronic inflammatory processes. Active components influence γ-aminobutyric acid (GABA) receptors and serotonin receptors, which explains the sedative and analgesic effects of the plant. In addition, inhibition of acetylcholinesterase (AChE) improves neuronal transmission, supporting neuroprotective effects.

The antimicrobial action is due to damage to the cell membranes of bacteria and fungi, which leads to disruption of barrier functions and subsequent death of microorganisms. Saponins contained in the taxon contribute to increased membrane permeability and modulate the immune response through activation of macrophages and neutrophils. The effect on vascular endothelial cells improves microcirculation, promoting acceleration of tissue regeneration and healing processes.

Inhibition of the JAK/STAT signaling pathway additionally reduces the production of pro-inflammatory mediators and supports the immunosuppressive balance, reducing the damaging effect of excessive inflammation. Antitumor properties are associated with the induction of apoptosis through modulation of caspases and regulation of the cell cycle.

Collectively, the mechanisms of action of Calotropis gigantea include enzymatic inhibition, receptor modulation, suppression of pro-inflammatory mediators, and enhancement of the immune response, which is confirmed by the structure of active substances and experimental data.

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

Synergy of Calotropis gigantea

Research data indicate the potentiation of the pharmacological activity of Calotropis gigantea when combined with other plant components possessing anti-inflammatory, antioxidant, and immunomodulatory effects. In particular, in combination with extracts of other plants rich in flavonoids and terpenoids, additive and potentiating inhibition of cyclooxygenases and a decrease in the production of pro-inflammatory cytokines are observed.

The taxon exhibits modulating interaction with plants affecting CNS receptor systems, enhancing the sedative and analgesic effect, which is associated with synergy at the level of GABA and serotonin receptors. Combined use with immunomodulators increases macrophage activation and promotes more effective control of inflammatory processes.

Antioxidant synergy is achieved when combined with other sources of polyphenols and vitamins, which increases the total ability to neutralize free radicals and protect cellular structures from oxidative stress. In this case, interactions occur at the level of blocking NF-κB and other signaling cascades, which contributes to an overall reduction in systemic inflammation.

A number of studies have noted the protective effect of the complex of Calotropis gigantea with other phytocomponents on the liver and kidneys, reducing potential toxicity and improving the pharmacokinetics of active substances.

Thus, the synergy of Calotropis gigantea with other plant substances is manifested in additive and potentiating effects that enhance anti-inflammatory, antioxidant, immunomodulatory, and neuroprotective activity, which is confirmed by experimental and preclinical data.

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

Geography of Use and Folk Medicine — Calotropis gigantea

Calotropis gigantea is traditionally used in tropical and subtropical regions of Asia, including India, Sri Lanka, Thailand, Malaysia, and the Philippines, as well as in the Pacific Islands and parts of Africa. In Indian Ayurvedic medicine, the plant has been known since ancient times and is used for various medicinal purposes, which is recorded in classical texts and regional herbals. In the culture of South Asian peoples, the taxon was considered a plant of power, often used in purification and protection rituals.

In Thai traditional medicine, Calotropis gigantea is used in the form of decoctions and infusions of leaves and bark for external and internal use, including wraps and compresses for skin diseases and inflammations. Among the peoples of the Philippines, the plant was used to treat skin lesions and as an anti-parasitic agent. In some regions, fresh latex was used externally to treat wounds and bruises, as well as for pain relief.

In the ethnographic practice of several Pacific Island tribes, the plant was used as a smoking agent in purification ceremonies, as well as an amulet against evil spirits, which indicates its importance in spiritual culture. In Malaysia and Indonesia, it was included in traditional ointments and balms intended for treating injuries and inflammations.

Historical sources testify to the use of Calotropis gigantea over several centuries, starting with written mentions in Indian medical treatises from the first millennium AD. Regional collections and manuscripts, as well as archaeoethnobotanical data, confirm the widespread use of the plant in the traditional medicine of South Asia and Southeast Asia.

Non-medical use includes application in rituals related to the protection of the home and family, where leaves and flowers served as talismans. The plant was also used in culture as a means of space cleansing and for divination rituals. It was believed that Calotropis gigantea possessed magical power capable of driving away evil forces and attracting well-being.

Thus, the geography of use of Calotropis gigantea covers vast territories of Asia and Oceania with deep cultural and historical roots, combining medicinal, ritual, and magical functions in traditional systems and local ethnic practices.