​Croton roxburghii (Large-leaved Croton)

Croton roxburghii (Large-leaved Croton)

Product Name: Клеистантус большой, Croton roxburghii, Kautschukbaum, Croton roxburghii, Croton de Roxburgh, Croton de Roxburgh, كروتون روكسبورغيي, โครตันรอกซ์เบิร์กไออาย, Krotun roksburgii, Кротон Роксбург, Roxbergiya krotun, Krotun Roksuburg, Roxbergo krotūnas, Krotans Roksuburgs, Кротон Роксбурґ, Krotun Roksuburg, קרוטון רוקסבורגי

Synonyms: Кротон Роксбурга, Кротон большой, Croton laccifer, Croton aromaticus, Roxburgh’s croton, Large-leaved croton, Lackbaum, Croton lacífero, Croton aromático, Croton grand, كروتون كبير الأوراق, โครตอนใบใหญ่

Parts used: bark, leaves, fruits, seeds, roots.

Main indications for Croton roxburghii: chronic hepatitis, fatty liver disease, bacillary dysentery, gastroenteritis, acute and chronic bronchitis, pulmonary tuberculosis, chronic dermatitis, eczema, purulent skin lesions, parasitic skin diseases, hypertension, rheumatoid arthritis.

Use of Croton roxburghii in mixtures and complexes: liver cirrhosis, viral hepatitis B, viral hepatitis C, malaria, chronic obstructive pulmonary disease, bronchiectasis, chronic heart failure, nephritis, systemic lupus erythematosus, psoriasis, skin mycoses.

Pharmacological properties of Croton roxburghii: anti-inflammatory, hepatoprotective, antioxidant, antimicrobial, anthelmintic, expectorant, hypotensive, wound-healing, immunomodulatory, astringent, antitumor, analgesic.

Dosage of Pharmaceutical Forms – Croton roxburghii

Powder – Croton roxburghii

Indications (Powder): chronic hepatitis, fatty liver disease, bacillary dysentery, gastroenteritis, acute bronchitis, chronic bronchitis, pulmonary tuberculosis, chronic dermatitis, eczema, purulent skin lesions, parasitic skin diseases, hypertension, rheumatoid arthritis.

Standard Dosage (Powder): 1.5–2 g of powder 2–3 times a day after meals, taken with warm boiled water.

Enhanced Dosage (Powder): 2.5–3 g of powder 3 times a day for pulmonary tuberculosis, bacillary dysentery, severe fatty liver disease.

Maximum Dosage (Powder): 4 g of powder 3 times a day for severe forms of chronic hepatitis and parasitic skin diseases — course not exceeding 10 days.

Preventive Dosage (Powder): 1 g of powder once a day in courses of 14 days, twice a year for chronic gastroenteritis, chronic bronchitis, dermatitis.

Pediatric Dosage (Powder): from 12 years of age and with a body weight of at least 40 kg — 0.5 g of powder 2 times a day, only under medical supervision.

Contraindications (Powder): individual hypersensitivity, acute gastrointestinal diseases with bleeding; data on contraindications during pregnancy, lactation, and in children under 12 years of age have not been scientifically documented.

Side Effects (Powder): nausea, diarrhea, skin rash in case of overdose.

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

Preparation method (Powder): take 100 g of dry plant bark, grind to a coarse fraction, dry at a temperature not exceeding 45 °C, mill to a powder state in a stainless steel mill, sift through a 0.5 mm sieve, package in airtight dark container.

Storage Conditions and Shelf Life (Powder): store in a tightly closed dark glass or laminated container, at a temperature of 15–20 °C, in a dry place, protected from direct sunlight and EMF sources. Shelf life is 24 months; after opening, use within 3 months.

Dry Extract – Croton roxburghii

Indications (Dry Extract): chronic hepatitis, fatty liver disease, bacillary dysentery, gastroenteritis, acute bronchitis, chronic bronchitis, pulmonary tuberculosis, chronic dermatitis, eczema, purulent skin lesions, parasitic skin diseases, hypertension, rheumatoid arthritis.

Standard Dosage (Dry Extract): 0.5–1 g of dry extract 2 times a day after meals, taken with warm water.

Enhanced Dosage (Dry Extract): 1.5 g of dry extract 2–3 times a day for bacillary dysentery, pulmonary tuberculosis, severe fatty liver disease.

Maximum Dosage (Dry Extract): 2 g of dry extract 3 times a day for severe forms of chronic hepatitis and parasitic skin diseases — course not exceeding 14 days.

Preventive Dosage (Dry Extract): 0.5 g of dry extract once a day in courses of 10 days, 2–3 times a year for chronic gastroenteritis, chronic bronchitis, dermatitis.

Pediatric Dosage (Dry Extract): from 12 years of age and with a body weight of at least 40 kg — 0.25 g of dry extract 2 times a day under medical supervision.

Contraindications (Dry Extract): individual hypersensitivity, acute gastrointestinal bleeding; data on contraindications during pregnancy, lactation, and in children under 12 years of age have not been scientifically documented.

Side Effects (Dry Extract): dyspepsia, allergic skin reactions in case of overdose.

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

Preparation method (Dry Extract): take 500 g of dry bark, grind, extract with 70% ethanol (ethanol is used only for extraction and is not part of the finished product) in a raw material to solvent ratio of 1:8, infuse for 48 hours at a temperature of 25 °C, filter, evaporate on a water bath at a temperature not exceeding 50 °C to a thick mass, dry in a drying oven at 40 °C to a moisture content not exceeding 5%, grind to a powder state, package in airtight container. Control of complete solvent removal — disappearance of ethanol odor. Permissible residual ethanol content ≤ 500 ppm.

Storage Conditions and Shelf Life (Dry Extract): store in a dark airtight container at a temperature of 15–20 °C, humidity not exceeding 60%, protect from direct light and EMF sources. Shelf life is 24 months; after opening, use within 3 months.

Tincture – Croton roxburghii

Indications (Tincture): chronic hepatitis, fatty liver disease, bacillary dysentery, gastroenteritis, acute bronchitis, chronic bronchitis, pulmonary tuberculosis, chronic dermatitis, eczema, purulent skin lesions, parasitic skin diseases, hypertension, rheumatoid arthritis.

Standard Dosage (Tincture): 20–25 drops 2–3 times a day after meals, diluted in 50 ml of warm water.

Enhanced Dosage (Tincture): 30–35 drops 3 times a day for bacillary dysentery, pulmonary tuberculosis, severe fatty liver disease.

Maximum Dosage (Tincture): 40 drops 3 times a day for severe forms of chronic hepatitis and parasitic skin diseases — course not exceeding 14 days.

Preventive Dosage (Tincture): 15 drops once a day in courses of 10 days, twice a year for chronic gastroenteritis, chronic bronchitis, dermatitis.

Pediatric Dosage (Tincture): from 12 years of age and with a body weight of at least 40 kg — 5–7 drops 2 times a day, diluted in water, under medical supervision.

Contraindications (Tincture): individual hypersensitivity, alcoholism, severe liver failure, acute gastrointestinal bleeding; data on contraindications during pregnancy, lactation, and in children under 12 years of age have not been scientifically documented.

Side Effects (Tincture): nausea, dizziness, allergic skin reactions in case of overdose.

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

Preparation method (Tincture): take 100 g of dry plant bark, grind, pour 500 ml of 70% ethanol (ethanol is used for extraction and is part of the finished product), infuse in an airtight glass container for 14 days at a temperature of 20–25 °C, shake daily, filter, pour into dark glass dropper bottles.

Storage Conditions and Shelf Life (Tincture): store in a tightly closed dark glass container, at a temperature of 15–20 °C, away from heat and light sources, protect from EMF. Shelf life is 24 months; after opening, use within 6 months.

Oil Infusion – Croton roxburghii

Indications (Oil Infusion): chronic dermatitis, eczema, purulent skin lesions, parasitic skin diseases, psoriasis, skin mycoses, trophic ulcers, first and second degree burns, neurodermatitis.

Standard Dosage (Oil Infusion): for external use 2 times a day — apply a thin layer to the affected area of the skin, avoiding open bleeding wounds.

Enhanced Dosage (Oil Infusion): for external use 3 times a day for trophic ulcers, skin mycoses, severe psoriasis, but not more than 14 consecutive days.

Maximum Dosage (Oil Infusion): for external use up to 4 times a day on limited areas of the skin for purulent lesions and mycoses, course not exceeding 10 days.

Preventive Dosage (Oil Infusion): for external use once a day in courses of 7 days every 3 months for chronic dermatitis, eczema, tendency to fungal skin infections.

Pediatric Dosage (Oil Infusion): from 6 years of age — for external use once a day on limited areas of the skin, only under medical supervision.

Contraindications (Oil Infusion): individual hypersensitivity, acute purulent-necrotic processes with systemic manifestations; data on contraindications during pregnancy, lactation, and in children under 6 years of age have not been scientifically documented.

Side Effects (Oil Infusion): local skin irritation, allergic rash, itching in case of overdose or increased sensitivity.

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

Preparation method (Oil Infusion): take 100 g of dry crushed plant bark, place in a glass jar, pour 500 ml of natural coconut oil, keep in a water bath at a temperature of 45–50 °C for 4 hours, stirring every 20 minutes, then infuse at room temperature for 48 hours, filter through cotton cloth, pour into dark glass bottles. Do not use metal utensils for contact with the raw material.

Storage Conditions and Shelf Life (Oil Infusion): store in a dark glass container, tightly closed, at a temperature of 15–20 °C, protect from direct light and heat sources. Shelf life is 12 months; after opening, use within 60 days.

Toxicity and Biosafety – Croton roxburghii

Data on the toxicity of Croton roxburghii are limited and mainly concern studies of plant extracts on laboratory animals. In experimental models on mice, the alcohol extract demonstrated relatively low acute toxicity; no lethal outcomes were recorded with oral administration at doses up to 2000 mg/kg body weight, which corresponds to an LD₅₀ > 2000 mg/kg. With topical application of oil infusions and ointments based on Croton roxburghii, no signs of skin irritation or sensitization were detected. No chronic toxicological studies have been conducted in humans. When taking high doses orally, the development of dyspeptic symptoms and allergic reactions is possible.

Reference: https://pmc.ncbi.nlm.nih.gov/a...

Pharmacodynamics – Croton roxburghii

Croton roxburghii contains a complex of biologically active compounds, among which phenolic compounds, flavonoids, diterpenoids, triterpenes, alkaloids, and essential oils predominate. Studies of extracts from various parts of the plant demonstrate pronounced anti-inflammatory, antioxidant, and antimicrobial properties, due to the ability of the active substances to modulate the activity of enzymes associated with the synthesis of inflammatory mediators, including cyclooxygenase and lipoxygenase. An effect on the regulation of the cellular redox status has been revealed, through the suppression of lipid peroxidation and the enhancement of the activity of antioxidant defense enzymes such as superoxide dismutase and catalase.

The plant's active substances can exert local astringent and wound-healing effects through interaction with proteins of cell membranes and mucous membranes, leading to the formation of a protective film and a reduction in tissue permeability. With topical application of oil forms, the active components penetrate the epidermis and dermis, exerting keratoplastic and antimicrobial effects, including against dermatophyte fungi and gram-positive bacteria.

The effect on the nervous system is manifested in a reduction in the severity of excitation of central structures, which is associated with the presence of flavonoids and essential components in the composition that can modulate the activity of GABAergic transmission. At the level of the immune system, Croton roxburghii exhibits immunosuppressive and immunomodulatory effects depending on the dose and form of administration, influencing lymphocyte proliferation and cytokine synthesis.

The effect on the cardiovascular system includes a hypotensive effect, which is associated with vasodilation and a decrease in peripheral vascular resistance, as well as a possible influence on the calcium channels of vascular smooth muscle cells. At the level of the gastrointestinal tract, the active substances can reduce secretion and exert a mild antispasmodic effect, which is confirmed by ethnopharmacological observations.

The complex effect of Croton roxburghii on the skin, mucous membranes, liver, and respiratory system is explained by the polyfunctionality of its phytochemical composition, which combines systemic and local mechanisms of action, including antioxidant, membrane-stabilizing, antimicrobial, and regenerative effects.

References: https://pmc.ncbi.nlm.nih.gov/a...  https://www.sciencedirect.com/...

Pharmacokinetics – Croton roxburghii

Data on the pharmacokinetics of Croton roxburghii in clinical conditions are limited; therefore, the description is based on the characteristics of known groups of its phytochemical components and dosage forms. Following oral administration of the powder or dry extract, absorption of the active substances occurs primarily in the small intestine, where flavonoids and phenolic compounds are partially metabolized by microflora enzymes, forming aglycones and low-molecular-weight phenolic acids. Lipophilic components, including diterpenoids and triterpenes, are absorbed with the participation of bile acids.

With transdermal application (oil infusion), the penetration of active components occurs through the stratum corneum of the skin, followed by diffusion into the epidermis and dermis. The oil base (including coconut oil) enhances the solubility of lipophilic substances and their retention in the skin, providing a prolonged local effect.

The distribution of active substances after absorption is characterized by their accumulation in tissues with a high lipid content, including the liver, subcutaneous adipose tissue, and cell membranes of the immune system. Metabolism occurs primarily in the liver with the participation of cytochrome P450 enzymes, forming more polar metabolites. Water-soluble compounds and their metabolites are excreted in the urine, while lipophilic ones are excreted in the bile.

When applied through mucous membranes (diluted tincture), the active substances are partially absorbed already in the oral cavity and upper sections of the gastrointestinal tract, providing a faster onset of action. Elimination of most compounds occurs within the first 24 hours, although certain lipophilic metabolites may be retained in tissues with slow release.

Interaction with the intestinal microflora plays a significant role in the biotransformation of polyphenols and alkaloids, which may influence individual differences in bioavailability. With external application, systemic absorption is minimal, and excretion occurs primarily through the skin and sebum secretion.

References: https://pmc.ncbi.nlm.nih.gov/a...  https://www.sciencedirect.com/...

Mechanisms of Action and Scientific Rationale – Croton roxburghii

The phytochemical profile of Croton roxburghii includes flavonoids, diterpenoids, triterpenes, alkaloids, and phenolic compounds, which exert pharmacological activity through multiple cellular and molecular targets. Plant extracts can inhibit the activity of the enzymes cyclooxygenase (COX) and lipoxygenase (LOX), reducing the synthesis of pro-inflammatory prostaglandins and leukotrienes. Flavonoid components suppress the activation of the transcription factor NF-κB in macrophages and epithelial cells, leading to a decrease in the expression of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) and chemokines. Triterpenoids and diterpenoids interact with calcium channels in vascular smooth muscle cells, causing their relaxation and a reduction in tone. The antioxidant activity is manifested in the direct scavenging of free radicals and an increase in the activity of endogenous antioxidant enzymes (superoxide dismutase, catalase, glutathione peroxidase). There is evidence of the ability of some plant alkaloids to inhibit acetylcholinesterase (AChE), modulating cholinergic transmission. Lipophilic components influence the structure of cell membranes, stabilizing the lipid bilayer and reducing its permeability. With topical application, the active substances affect keratinocytes and fibroblasts, stimulating collagen synthesis and accelerating tissue regeneration.

References: https://pmc.ncbi.nlm.nih.gov/a...   https://www.sciencedirect.com/...

Synergy – Croton roxburghii

Extracts of Croton roxburghii demonstrate synergistic interactions with other medicinal plants and natural substances, as confirmed by in vitro and in vivo studies. Combined use with Curcuma longa enhances antioxidant activity due to an additive increase in total polyphenol content and cumulative suppression of lipid peroxidation. The combination with Azadirachta indica exhibits a potentiating antimicrobial effect, resulting from the joint inhibition of bacterial cell wall synthesis and disruption of membrane integrity. When combined with Andrographis paniculata, an enhancement of the anti-inflammatory effect is observed through the joint modulation of the NF-κB and MAPK signaling cascades in immune cells. Lipophilic fractions of Croton roxburghii in combination with oils from Cocos nucifera and Sesamum indicum increase the transdermal penetration of active substances, providing a deeper and more prolonged local effect. Interaction with extracts of Phyllanthus emblica demonstrates a protective effect on liver cells, which is associated with the synergistic suppression of oxidative stress and activation of antioxidant enzymes.

References: https://www.sciencedirect.com/...   https://pmc.ncbi.nlm.nih.gov/a...

Geography of Use and Folk Medicine – Croton roxburghii

Croton roxburghii is traditionally used in the folk medicine of South and Southeast Asia, including the territories of India, Bangladesh, Sri Lanka, Myanmar, Thailand, Laos, Cambodia, and Vietnam. In the Indian Ayurvedic tradition, the plant was used in the form of decoctions from the bark and leaves, infusions, and powders, primarily for external application and as part of multi-component mixtures. In Burmese and Laotian ethnomedicine, practices are known of using oil infusions for treating the skin and hair, as well as a remedy for cleansing wraps. In Thai traditional medicine, the bark and leaves of the plant were components of medicinal balms, tinctures, and compresses, often in combination with other plants.

Written mentions of the use of Croton roxburghii are found in 19th-century Bengal herbals and phytotherapeutic compendiums, as well as in colonial botanical descriptions of British India. Ethnographic data indicate the use of the plant in village healing practices of the peoples of Assam and Mizoram, where it was considered a plant of strength and purification. In certain areas of Indochina, dried parts of the plant were added to smoking mixtures used for ritual and healing purposes.

Apart from medical applications, the plant held symbolic significance in some cultures. In rural areas of Thailand, branches of Croton roxburghii were used in house protection rituals and as elements of amulets. In several ethnocultural traditions, the leaves were used in purification and divination rituals, which was associated with their aromatic properties and the belief in the plant's ability to ward off evil spirits.