Artocarpus lakoocha Roxb

Artocarpus lakoocha Roxb

Product Name: Артокарпус лакуча, Artocarpus lacucha Roxb. ex Buch.-Ham., Lakucha (de), lakucha / jack del mono (es), artocarpus lacucha (fr), أرتوكاربوس لاكوتشا (ar), มะหาด (th), artokarpus lakucha (uz), арто карпус лакуча (ky), artokarpus lakucha (az), артокарпус лакуча (tg), artokarpusas lakucha (lt), artokarpuss lakucha (lv), артокарпус лакуча (uk), אַרְטוֹקַרְפּוּס לַקוּצ׳ה (he)

Synonyms: Artocarpus lakoocha Roxb.;common English: monkey jack, lakoocha; German: Lakucha-Baum; Spanish: jack del mono; French: artocarpus lacucha; Arabic: شجرة اللاكوتشا؛

Parts Used: bark, wood, leaves, fruits, seeds, roots, latex.

Main Indications for Artocarpus lacucha: dermatomalanosis (melasma), post-inflammatory hyperpigmentation, intestinal cestodiasis (taeniasis, hymenolepiasis), bacterial skin infections (impetigo, folliculitis), inflammatory dermatoses (contact dermatitis, atopic dermatitis in the subacute inflammation phase), skin photodamage (solar erythematous dermatitis).

Use of Artocarpus lacucha in Mixtures and Complexes: acne vulgaris, seborrheic dermatitis, chronic pyodermas, skin and nail mycoses, type 2 diabetes (insulin resistance of skin manifestations), chronic viral dermatoses (recurrent herpes simplex), chronic gastritis with dyspeptic syndrome.

Pharmacological Properties of Artocarpus lacucha: antioxidant, anti-inflammatory, antimicrobial, anthelmintic, tyrosinase inhibitory (depigmenting), photoprotective, cytoprotective, wound-healing, antiglycation, anticolonization (antibiofilm).

Dosage of Pharmaceutical Forms — Artocarpus lacucha

Powder — Artocarpus lacucha

Indications (Powder): dermatomalanosis (melasma), post-inflammatory hyperpigmentation, intestinal cestodiasis (taeniasis, hymenolepiasis), bacterial skin infections (impetigo, folliculitis), inflammatory dermatoses of subacute course (contact dermatitis, atopic dermatitis), skin photodamage (solar erythematous dermatitis).

Standard Dosage (Powder): Orally, 1.5—2.0 grams of powder twice daily, course 14—21 days.

Enhanced Dosage (Powder): Orally, 2.5 grams of powder 2—3 times daily for intestinal cestodiasis and pronounced skin hyperpigmentation, course 10—14 days.

Maximum Dosage (Powder): Orally, 3.0 grams of powder three times daily for severe and resistant cestodiasis, course no more than 7 days.

Preventive Dosage (Powder): Orally, 1.0 gram of powder once daily, in courses of 10 days once every 2 months for patients with chronic contact dermatitis, tendency to skin hyperpigmentation, and during prolonged sun exposure.

Pediatric Dosage (Powder): Orally for children from 6 years old and weighing at least 20 kg — 0.5 grams of powder 1—2 times daily, course 5—7 days.

Contraindications (Powder): Individual intolerance, acute inflammatory diseases of the gastrointestinal tract; scientific data on contraindications during pregnancy, lactation, and for children under 6 years of age are not recorded.

Side Effects (Powder): Overdose may cause diarrhea, abdominal pain, nausea.

Adjustment for Patient Body Weight (Powder): For body weight below 60 kg, reduce the dose by 20%; for body weight above 90 kg, increase the dose by 15%.

Preparation method (Powder): Ingredients for 100 grams: dried bark — 100 grams. Grind the bark into 2—3 cm segments, dry at a temperature not exceeding 50°C to a residual moisture content of no more than 10%. Grind into powder in a stainless steel mill to a particle size of no more than 0.25 mm. Sieve through sieve No. 60. Package in an airtight container made of dark glass.

Storage Conditions and Shelf Life (Powder): Store in a dry, cool, light-protected place, at a temperature from +5 to +25°C, in a tightly closed container, away from sources of electromagnetic radiation; shelf life — 24 months; after opening the package, use within 60 days.

Dry Extract — Artocarpus lacucha

Indications (Dry Extract): dermatomalanosis (melasma), post-inflammatory hyperpigmentation, bacterial skin infections (impetigo, folliculitis), inflammatory dermatoses of subacute course (contact dermatitis, atopic dermatitis), skin photodamage (solar erythematous dermatitis).

Standard Dosage (Dry Extract): Orally, 0.4—0.5 grams of dry extract twice daily, course 14 days.

Enhanced Dosage (Dry Extract): Orally, 0.6—0.8 grams of dry extract 2—3 times daily for pronounced hyperpigmentation and chronic bacterial dermatoses, course up to 10 days.

Maximum Dosage (Dry Extract): Orally, 1.0 gram of dry extract three times daily for severe forms of melasma and pronounced skin photodamage, course no more than 7 days.

Preventive Dosage (Dry Extract): Orally, 0.25 grams of dry extract once daily in courses of 7 days every 3 months for a tendency to hyperpigmentation and skin photodamage.

Pediatric Dosage (Dry Extract): Orally for children from 6 years old and weighing at least 20 kg — 0.15—0.2 grams of dry extract once daily, course 5 days.

Contraindications (Dry Extract): Individual intolerance; scientific data on contraindications during pregnancy, lactation, and for children under 6 years of age are not recorded.

Side Effects (Dry Extract): Overdose may cause dyspepsia, short-term nausea, weakness.

Adjustment for Patient Body Weight (Dry Extract): For body weight below 60 kg, reduce the dose by 15%; for body weight above 90 kg, increase the dose by 10%.

Preparation method (Dry Extract): Ingredients for 100 grams: dried bark — 500 grams, 70% ethanol — 2.5 liters. Pour the ground dry bark with ethanol, infuse at a temperature of +25°C for 72 hours, stirring periodically. Filter, evaporate the solvent in a water bath at a temperature not exceeding 50°C to a thick mass, perform vacuum evaporation to completely remove the solvent to a residual content of <10 ppm (according to pharmacopoeial standards). Dry under vacuum to a powdery state. Package in an airtight container made of dark glass.

Storage Conditions and Shelf Life (Dry Extract): Store in a dry, light-protected place at a temperature of +5...+20°C, in a tightly closed container, away from sources of electromagnetic radiation; shelf life — 24 months; after opening the package, use within 45 days.

Tincture — Artocarpus lacucha

Indications (Tincture): dermatomalanosis (melasma), post-inflammatory hyperpigmentation, bacterial skin infections (impetigo, folliculitis), inflammatory dermatoses of subacute course (contact dermatitis, atopic dermatitis), skin photodamage (solar erythematous dermatitis).

Standard Dosage (Tincture): Orally, 20 drops of tincture diluted in 50 ml of boiled water, twice daily 30 minutes before meals, course 10—14 days.

Enhanced Dosage (Tincture): Orally, 25 drops three times daily for pronounced skin hyperpigmentation and chronic bacterial skin infections, course up to 10 days.

Maximum Dosage (Tincture): Orally, 30 drops three times daily for resistant forms of melasma, course no more than 7 days.

Preventive Dosage (Tincture): Orally, 10 drops once daily in courses of 7 days every 3 months for chronic contact dermatitis and a tendency to skin photodamage.

Pediatric Dosage (Tincture): Orally for children from 12 years old and weighing at least 40 kg — 5—7 drops of tincture diluted in 50 ml of water, 1—2 times daily, course 5 days.

Contraindications (Tincture): Individual intolerance, alcoholism, decompensated liver disease; scientific data on contraindications during pregnancy, lactation, and for children under 12 years of age are not recorded.

Side Effects (Tincture): Overdose may cause dizziness, nausea, drowsiness.

Adjustment for Patient Body Weight (Tincture): For body weight below 60 kg, reduce the dose by 20%; for body weight above 90 kg, increase the dose by 15%.

Preparation method (Tincture): Ingredients for 100 grams of finished product: dried bark — 30 grams, 70% ethanol — 100 ml. Grind the dry bark into pieces of 0.5—1 cm, place in a glass jar, pour ethanol, close the lid. Infuse at a temperature of +20...+25°C in a dark place for 14 days, shaking daily. Filter, press the raw material, pour the filtrate into dark glass bottles. Ethanol is used only as an extractant and is part of the finished preparation in the permissible concentration for tinctures (according to pharmacopoeia).

Storage Conditions and Shelf Life (Tincture): Store in a tightly closed container made of dark glass at a temperature of +5...+25°C, away from sources of light and heat; shelf life — 24 months; after opening, use within 90 days.

Lotion — Artocarpus lacucha

Indications (Lotion): dermatomalanosis (melasma), post-inflammatory hyperpigmentation, skin photodamage (solar erythematous dermatitis), inflammatory dermatoses of subacute course (contact dermatitis, atopic dermatitis), bacterial skin infections (impetigo, folliculitis).

Standard Dosage (Lotion): Apply topically to the affected skin areas 1—2 times daily, course 14—21 days.

Enhanced Dosage (Lotion): Apply topically to the affected areas 3 times daily for pronounced hyperpigmentation and post-inflammatory skin changes, course up to 14 days.

Maximum Dosage (Lotion): Apply topically up to 4 times daily for resistant hyperpigmentation, course no more than 10 days.

Preventive Dosage (Lotion): Apply topically to the skin once daily for 7 days every 2 months for chronic contact dermatitis, skin photodamage, and a tendency to hyperpigmentation.

Pediatric Dosage (Lotion): Topical use for children from 6 years old, apply once daily to limited skin areas, course up to 7 days.

Contraindications (Lotion): Individual intolerance; scientific data on contraindications during pregnancy, lactation, and for children under 6 years of age are not recorded.

Side Effects (Lotion): Overdose may cause skin irritation, erythema.

Adjustment for Patient Body Weight (Lotion): Not required, as the form is for topical application.

Preparation method (Lotion): Ingredients for 100 grams of finished product: dry bark extract — 2 grams, distilled water — 60 grams, coconut oil — 10 grams, vegetable glycerin — 5 grams, emulsifier (glycerin stearate) — 2 grams, 20% ethanol — 20 grams, citric acid — 0.2 grams. Heat the aqueous phase (water, glycerin) to +40°C; in a separate container, combine coconut oil and emulsifier, heat to +40°C. Mix the aqueous and oil phases, add the dry extract dissolved in ethanol. Stir until homogeneous, cool to +25°C, add citric acid. Package in opaque bottles with a dispenser.

Storage Conditions and Shelf Life (Lotion): Store at a temperature of +5...+20°C, away from direct sunlight, in a tightly closed package; shelf life — 12 months; after opening, use within 60 days.

Toxicity and Biosafety — Artocarpus lacucha

Studies of the acute toxic effects of Artocarpus lacucha extracts on laboratory animals have shown low toxicity. Oral administration of the ethanolic bark extract to mice at doses up to 2000 mg/kg body weight showed no lethal outcomes or clinical signs of intoxication, allowing the preparation to be classified as practically non-toxic according to the OECD classification. The oral LD₅₀ exceeds 2000 mg/kg. Topical application of the extract showed no irritant or sensitizing effects in standard dermatological tests.

Reference: https://wjpsonline.com/index.p...

Pharmacodynamics — Artocarpus lacucha

Artocarpus lacucha contains a wide range of biologically active compounds, including polyphenols, flavonoids (especially oxyresveratrol), triterpenoids, and other phenolic derivatives, which determine its pharmacodynamic profile. These substances exhibit pronounced antioxidant activity by binding and inactivating free radicals, leading to a reduction of oxidative stress at the cellular and tissue levels. This results in a membrane-stabilizing effect and the maintenance of cellular structure integrity under conditions of damaging factors.

Extracts of A. lacucha have an anti-inflammatory effect, realized through inhibition of the activity of enzymes involved in the synthesis of inflammatory mediators, as well as by reducing the production of pro-inflammatory cytokines. With topical application, these effects manifest as a reduction in erythema, edema, and subjective sensations of skin irritation.

Antimicrobial activity covers a range of gram-positive and gram-negative bacteria, as well as some dermatophytes. The mechanism of antibacterial action is associated with disruption of the integrity of the bacterial cell wall, changes in cytoplasmic membrane permeability, and inhibition of microbial cell enzymes.

A characteristic pharmacodynamic property of A. lacucha is the inhibition of tyrosinase, the key enzyme in melanin biosynthesis. This action is primarily due to the content of oxyresveratrol, which blocks the catalytic center of the enzyme, slowing pigment formation. This effect is particularly pronounced with topical application and underlies the depigmenting and skin tone-evening properties.

A modulating influence on protein glycation processes is also observed, which helps maintain tissue elasticity and slow structural changes in collagen. Photoprotective properties have been noted, associated with the absorption and scattering of ultraviolet radiation, as well as the activation of endogenous skin antioxidant enzymes.

The pharmacodynamic effects of A. lacucha are realized both locally and systemically, depending on the route of administration. With oral intake, active components may have a general modulating effect on the immune system, reducing the excessive activity of inflammatory cascades.

Reference: https://www.sciencedirect.com/... https://www.academia.edu/14622...

Pharmacokinetics — Artocarpus lacucha

With oral administration of the powder or dry extract of A. lacucha, absorption of polyphenols and flavonoids occurs mainly in the small intestine, where they may undergo partial metabolism with the formation of glucuronides and sulfates. Biotransformation begins at the level of the intestinal mucosa and continues in the liver, where conjugation occurs with an increase in water solubility. Triterpenoids and other lipophilic components are absorbed more slowly and depend more on the presence of dietary fats.

With transdermal application, as in the form of lotions or tinctures, penetration of active substances occurs through the stratum corneum of the epidermis, with subsequent distribution in epidermal and dermal structures. Lipophilic components (e.g., triterpenoids) accumulate more actively in the lipid layers of the skin, while polyphenols and oxyresveratrol penetrate into the aqueous phases of tissues, exhibiting local biochemical effects.

The distribution of active substances in the body depends on their polarity: hydrophilic metabolites circulate predominantly in blood plasma, lipophilic ones can be deposited in adipose tissue and cell membranes.

Metabolism occurs through oxidative, reductive, and hydrolytic reactions, followed by conjugation. The main role in inactivation belongs to hepatic enzymes, including uridine diphosphate-glucuronosyltransferases and sulfotransferases.

Excretion of polar metabolites occurs primarily in urine, and to a lesser extent in bile. Lipophilic compounds may be excreted more slowly, partially with the participation of the skin (through sebaceous and sweat glands). Interaction with intestinal microflora plays an important role in the biotransformation of some phenolic compounds, which can affect their final activity profile.

Reference: https://www.sciencedirect.com/... https://pubmed.ncbi.nlm.nih.go...

Mechanisms of Action and Scientific Rationale — Artocarpus lacucha

The pharmacological activity of Artocarpus lacucha is due to the presence of phenolic compounds, flavonoids (including oxyresveratrol), triterpenoids, and other polyphenolic metabolites, which exhibit multiple mechanisms of action. The antioxidant effect is associated with direct electron and hydrogen donation to neutralize reactive oxygen and nitrogen species, as well as with the activation of endogenous antioxidant systems via the Nrf2/ARE signaling pathways. The anti-inflammatory action is realized through suppression of the activation of the transcription factor NF-κB, leading to a reduction in the expression of pro-inflammatory cytokines (IL-1β, IL-6, TNF-α) and mediators such as prostaglandins and leukotrienes by inhibiting COX-2 and 5-LOX enzymes.

The inhibitory influence on tyrosinase is associated with the competitive binding of the enzyme's active site by phenolic compounds, which prevents the oxidation of L-tyrosine and L-DOPA in the melanogenesis process. Additionally, oxyresveratrol can interfere with the MAPK cascade, which regulates the expression of genes involved in melanin synthesis. The antimicrobial effect is partly explained by disruption of the integrity of the microbial cell membrane and inhibition of bacterial hydrolases.

Modulation of protein glycation is achieved by binding reactive carbonyl intermediates, which prevents the formation of advanced glycation end products (AGEs) and supports the structural integrity of collagen. Photoprotective properties are realized through the absorption of ultraviolet radiation and reduction of UV-induced oxidative stress, mediated by a decrease in the levels of activated metalloproteinases (MMPs) in the skin.

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

Synergy — Artocarpus lacucha

Research shows that Artocarpus lacucha exhibits pronounced pharmacological synergy when combined with other plant taxa possessing similar or complementary effects. Combined use with Camellia sinensis (green tea) leads to potentiation of antioxidant action due to the summation of the activity of polyphenols and catechins, which enhances the suppression of oxidative stress at the cellular level. The combination with Curcuma longa (turmeric) demonstrates additive and partially potentiating anti-inflammatory action due to synchronous inhibition of NF-κB and COX-2, as well as modulation of cytokine production.

In combination with Glycyrrhiza glabra (licorice), enhanced antibacterial activity is observed, which is attributed to the joint disruption of bacterial membrane integrity and blockade of pathogen enzyme systems. Combination with Aloe vera enhances tissue-specific regenerative and photoprotective effects due to synchronous activation of fibroblasts and reduction of metalloproteinase levels in the skin.

Furthermore, the combination of A. lacucha with natural sources of vitamin C, such as Citrus limon (lemon), contributes to modulation of collagen synthesis and enhancement of the depigmenting effect due to synergistic inhibition of tyrosinase and stabilization of collagen fibers.

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

Geography of Use and Folk Medicine — Artocarpus lacucha

Artocarpus lacucha is traditionally used in Southeast Asia, primarily in Thailand, Laos, Myanmar, Cambodia, Vietnam, as well as in the northeastern regions of India and Bangladesh. In Thai traditional medicine, the bark of the tree is known as "mahad" and is used in the form of powder and decoctions for external and internal use. In the ethnomedical practices of the peoples of northern Thailand and Lanna, the bark and heartwood of the tree were used to prepare infusions and macerates, which were applied to the skin or used in baths. In some Thai villages, bark powder was added to ritual cleansing mixtures used in ablution ceremonies at the beginning of the Buddhist New Year (Songkran).

In folk medicine, the fruits were consumed as a source of nutrients, and the latex from the trunk was used for household needs. Ancient Burmese herbal texts mention the use of A. lacucha wood for preparing decoctions used in bathing procedures for general strengthening of the body. In the Indian Ayurvedic tradition, the bark of the plant is known as a component of cleansing mixtures used for maintaining skin health.

Historical mentions of the use of A. lacucha are recorded in Thai written sources starting from the Ayutthaya period (14th—18th centuries), where the plant appeared in royal herbals. In some ethnocultural practices, it was considered a plant that brings purification and protection, and could be part of amulets or charm bags worn on the person. In the ritual practice of certain ethnic groups in northern Laos and Thailand, it was used in combination with aromatic plants for fumigating rooms during ceremonies for exorcising evil spirits.