Momordica charantia (Bitter Melon)

Momordica charantia (Bitter Melon)

Product Name: Момордика белая, Momordica charantia, Balsambirne, melón amargo, margose, كَرْلا, มะระขี้นก, achchi qovun, аччы бадыран, acı qovun, харбузаи талх, kartusis, rūgčioji melona, гірка диня, מרה חריפה

Synonyms: горькая дыня, горький огурец, индийская дыня, бальзамическая груша, bitter melon, bitter gourd, balsam pear, karela, balsambirne, bittergurke, melón amargo, calabaza amarga, margose, concombre amer, كَرلا بلسمي, มะระ, ฟักขม

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

Main indications for use of Momordica charantia: type 2 diabetes mellitus, dyslipidemia, obesity, metabolic syndrome, hyperglycemia, chronic hepatitis, fatty liver disease, viral hepatitis B, viral hepatitis C, herpetic infection, candidiasis, inflammatory bowel diseases, ulcerative colitis, atherosclerosis, polycystic ovary syndrome, acne vulgaris, psoriasis, eczema, chronic fatigue syndrome, iron deficiency anemia.

Use of Momordica charantia in mixtures and complexes: pulmonary tuberculosis, bronchial asthma, chronic bronchitis, influenza A and B virus, osteoarthritis, rheumatoid arthritis, gout, chronic renal failure, nephrolithiasis, human papillomavirus, immunodeficient conditions, burns, trophic ulcers, stage II hypertension, dementia, Alzheimer's disease.

Pharmacological properties of Momordica charantia

Antihyperglycemic, hypolipidemic, antioxidant, hepatoprotective, anti-inflammatory, antimicrobial, antiviral, antifungal, immunomodulatory, anticarcinogenic, analgesic, wound healing, anthelmintic, angioprotective, cardioprotective, neuroprotective, adaptogenic, spasmolytic.

Dosage of pharmaceutical forms — Momordica charantia

Powder — Momordica charantia

Indications (Powder): type 2 diabetes mellitus, dyslipidemia, obesity, metabolic syndrome, hyperglycemia, chronic hepatitis, fatty liver disease, viral hepatitis B, viral hepatitis C, inflammatory bowel diseases, ulcerative colitis, atherosclerosis, polycystic ovary syndrome, acne vulgaris, psoriasis, eczema, chronic fatigue syndrome, iron deficiency anemia.

Standard Dosage (Powder): 3–5 grams of powder per day, divided into 2–3 doses, with warm water.

Enhanced Dosage (Powder): 6–8 grams of powder per day for type 2 diabetes mellitus with pronounced hyperglycemia, pronounced dyslipidemia, grade III obesity.

Maximum Dosage (Powder): 10 grams of powder per day for resistance to type 2 diabetes mellitus therapy, pronounced steatohepatosis, severe forms of metabolic syndrome.

Preventive Dosage (Powder): 2 grams of powder 1 time a day in courses of 30 days 2 times a year for chronic hepatitis in remission, atherosclerosis, overweight, patients with a hereditary predisposition to type 2 diabetes mellitus.

Pediatric Dosage (Powder): for children from 12 years of age and body weight from 35 kg — 1–2 grams of powder per day, divided into 2 doses.

Contraindications (Powder): contraindicated in case of individual intolerance, severe hypoglycemia, acute ulcerative lesions of the stomach and duodenum; no scientifically documented contraindications during pregnancy, lactation, and in children under 12 years of age.

Side Effects (Powder): in case of overdose, may cause nausea, diarrhea, abdominal cramps, pronounced hypoglycemia.

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 20%.

Preparation method (Powder): To prepare 100 g of powder, use 120 g of dried fruits of Momordica charantia. Cut the fruits into thin slices, dry in a drying oven at a temperature not exceeding 45 °C to a residual moisture of 8–10%. Grind the dried raw material in a mill to a powder state with a particle size of not more than 0.3 mm. Sieve through a No. 60 sieve. Store in airtight containers.

Storage Conditions and Shelf Life (Powder): store in a dry, light-protected place at a temperature not exceeding 25 °C, in tightly closed containers shielded from electromagnetic radiation; shelf life is 24 months, after opening — use within 60 days.

Dry Extract — Momordica charantia

Indications (Dry Extract): type 2 diabetes mellitus, hyperglycemia, dyslipidemia, obesity, metabolic syndrome, chronic hepatitis, viral hepatitis B, viral hepatitis C, atherosclerosis, psoriasis, acne vulgaris, eczema, polycystic ovary syndrome, iron deficiency anemia.

Standard Dosage (Dry Extract): 300–500 mg of dry extract per day, divided into 2–3 doses.

Enhanced Dosage (Dry Extract): 800–1000 mg of dry extract per day for pronounced hyperglycemia, grade III obesity, severe forms of dyslipidemia.

Maximum Dosage (Dry Extract): 1500 mg of dry extract per day for resistance to type 2 diabetes mellitus therapy and severe metabolic syndrome.

Preventive Dosage (Dry Extract): 200 mg 1 time a day in courses of 30 days 2 times a year for atherosclerosis, overweight, chronic hepatitis in remission.

Pediatric Dosage (Dry Extract): for children from 12 years of age and body weight from 35 kg — 100 mg of dry extract per day.

Contraindications (Dry Extract): contraindicated in case of individual intolerance, severe hypoglycemia, acute inflammatory diseases of the gastrointestinal tract; no scientifically documented contraindications during pregnancy, lactation, and in children under 12 years of age.

Side Effects (Dry Extract): in case of overdose of dry extract, may cause nausea, vomiting, diarrhea, abdominal pain, hypoglycemia.

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 15%.

Preparation method (Dry Extract): To prepare 100 g of dry extract, take 500 g of dried fruits of Momordica charantia, grind to a fraction of 2–3 mm, perform maceration in 70% ethanol (the organic solvent is used for extraction only and is not a component of the finished product) in a raw material:solvent ratio of 1:10, keep for 72 hours at a temperature of 25 °C with daily stirring. Filter, evaporate in a water bath at a temperature not exceeding 50 °C to a thick extract, then dry completely in a vacuum drying oven to a powder state. Control of solvent removal — complete disappearance of ethanol odor. Permissible residual ethanol content — not more than 500 ppm.

Storage Conditions and Shelf Life (Dry Extract): store in airtight containers, in a dry dark place at a temperature not exceeding 25 °C, shielded from electromagnetic radiation; shelf life is 24 months, after opening use within 90 days.

Tincture — Momordica charantia

Indications (Tincture): type 2 diabetes mellitus, hyperglycemia, dyslipidemia, obesity, metabolic syndrome, chronic hepatitis, viral hepatitis B, viral hepatitis C, atherosclerosis, polycystic ovary syndrome, acne vulgaris, psoriasis, eczema, iron deficiency anemia.

Standard Dosage (Tincture): 5 ml of tincture 2 times a day, diluted in 50 ml of warm water.

Enhanced Dosage (Tincture): 7 ml of tincture 2 times a day for pronounced hyperglycemia, grade III obesity, severe dyslipidemia.

Maximum Dosage (Tincture): 10 ml of tincture 2 times a day for resistance to type 2 diabetes mellitus therapy and severe metabolic syndrome.

Preventive Dosage (Tincture): 3 ml of tincture 1 time a day for a course of 30 days 2 times a year for atherosclerosis, chronic hepatitis in remission, predisposition to type 2 diabetes mellitus.

Pediatric Dosage (Tincture): not recommended for children under 14 years of age due to ethanol content.

Contraindications (Tincture): contraindicated in case of individual intolerance, severe hypoglycemia, liver diseases in the stage of decompensation, alcoholism, pregnancy and lactation; data on contraindications for children under 14 years of age are scientifically documented due to ethanol content.

Side Effects (Tincture): in case of overdose of Tincture, may cause nausea, vomiting, diarrhea, abdominal cramps, hypoglycemia, dizziness.

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): To prepare 100 ml of tincture, take 20 g of dried ground fruits of Momordica charantia, place in a glass container, pour 100 ml of 70% ethanol (the organic solvent is used for extraction only and is not a component of the finished product), infuse for 14 days in a dark place at a temperature of 20–25 °C, shaking daily. Filter, store in airtight containers. If complete removal of ethanol is necessary (for example, for external use) — evaporate in a water bath at a temperature not exceeding 50 °C until the odor completely disappears, permissible residual ethanol content — not more than 500 ppm.

Storage Conditions and Shelf Life (Tincture): store in dark glass containers at a temperature of 5–20 °C, protecting from light and EMI; shelf life is 24 months, after opening — 6 months.

Oil Infusion — Momordica charantia

Indications (Oil Infusion): psoriasis, eczema, acne vulgaris, burns, trophic ulcers, inflammatory skin diseases, atherosclerosis (external use as applications), arthritis, osteoarthritis.

Standard Dosage (Oil Infusion): external use 2 times a day on affected areas of skin in a thin layer with light rubbing.

Enhanced Dosage (Oil Infusion): 3 times a day for acute inflammatory skin processes, severe forms of psoriasis, trophic ulcers.

Maximum Dosage (Oil Infusion): up to 4 times a day for resistant forms of dermatoses and chronic joint inflammation (externally).

Preventive Dosage (Oil Infusion): 1 time a day in courses of 14 days 3 times a year for the prevention of exacerbations of chronic dermatoses in patients with psoriasis and eczema.

Pediatric Dosage (Oil Infusion):) allowed in children from 6 years of age for external use — 1 time a day on small areas of skin.

Contraindications (Oil Infusion): contraindicated in case of individual intolerance to components, purulent skin infections, deep wounds; no scientifically documented contraindications during pregnancy and lactation.

Side Effects (Oil Infusion): in case of overdose of oil infusion, may cause local skin irritation, allergic reaction, itching.

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

Preparation method (Oil Infusion): To prepare 100 g of infusion, take 20 g of dry fruits of Momordica charantia, grind to a fraction of 3–5 mm, pour 100 g of coconut oil, heat in a water bath to a temperature of 40–45 °C and keep for 4 hours, stirring periodically. Strain through cheesecloth, squeeze the raw material, filter the oil and pour into dark glass vials.

Storage Conditions and Shelf Life (Oil Infusion): store in a dark cool place at a temperature of 5–20 °C, in tightly closed containers shielded from EMI; shelf life is 12 months, after opening — 60 days.

Vaginal Suppository — Momordica charantia

Indications (Vaginal Suppository): vulvovaginal candidiasis, bacterial vaginosis, urogenital trichomoniasis, inflammatory diseases of the vagina, atrophic vaginitis, chronic cervicitis.

Standard Dosage (Vaginal Suppository): 1 suppository (2.5 g) vaginally 1 time a day at night for a course of 7–10 days.

Enhanced Dosage (Vaginal Suppository): 1 suppository (2.5 g) vaginally 2 times a day for pronounced bacterial vaginosis, recurrent candidiasis.

Maximum Dosage (Vaginal Suppository): 1 suppository (2.5 g) 3 times a day for severe forms of candidiasis resistant to therapy and for mixed vaginal infections.

Preventive Dosage (Vaginal Suppository): 1 suppository (2.5 g) 1 time a week for a course of 1 month for chronic recurrent candidiasis, atrophic vaginitis, for postmenopausal patients to maintain normal microflora.

Pediatric Dosage (Vaginal Suppository): not used in children under 18 years of age.

Contraindications (Vaginal Suppository): contraindicated in case of individual intolerance to components, acute vaginal injuries, uterine bleeding of unknown etiology; no scientifically documented contraindications during pregnancy and lactation.

Side Effects (Vaginal Suppository): in case of overdose of suppositories, may cause local burning, itching, allergic reaction of the mucous membrane.

Adjustment for Patient Body Weight (Vaginal Suppository): not required.

Preparation method (Vaginal Suppository): To prepare 100 g of the product, take 10 g of Momordica charantia fruit powder, mix with 90 g of cocoa butter melted in a water bath at a temperature not exceeding 40 °C. Mix the mass until homogeneous, pour into suppository molds with a volume of 2.5 g. Cool at a temperature of 8–10 °C until solidified, remove from the molds.

Storage Conditions and Shelf Life (Vaginal Suppository): store at a temperature of 5–8 °C, in a dark place, in tightly closed containers, shelf life is 12 months, after opening the package — use within 14 days.

Rectal Suppository — Momordica charantia

Indications (Rectal Suppository): hemorrhoids, chronic proctitis, anal fissure, non-specific ulcerative colitis in the acute stage, chronic paraproctitis.

Standard Dosage (Rectal Suppository): 1 suppository (2 g) rectally 1 time a day at night for a course of 7–14 days.

Enhanced Dosage (Rectal Suppository): 1 suppository (2 g) rectally 2 times a day for pronounced pain syndrome, inflammation, exacerbation of stage II–III hemorrhoids.

Maximum Dosage (Rectal Suppository): 1 suppository (2 g) 3 times a day for severe forms of proctitis, thrombosed hemorrhoids, resistant forms of ulcerative colitis.

Preventive Dosage (Rectal Suppository): 1 suppository (2 g) 1 time a week for a course of 1 month in patients with chronic hemorrhoids in remission, with a tendency to constipation.

Pediatric Dosage (Rectal Suppository): used in children from 12 years of age with body weight from 35 kg — 1 suppository (1 g) 1 time a day for a course of up to 7 days.

Contraindications (Rectal Suppository): contraindicated in case of individual intolerance to components, acute bleeding from the rectum, malignant tumors of the rectum; no scientifically documented contraindications during pregnancy and lactation.

Side Effects (Rectal Suppository): in case of overdose of suppositories, may cause burning, itching, increased pain syndrome, diarrhea.

Adjustment for Patient Body Weight (Rectal Suppository): for body weight below 60 kg, reduce the dose of the suppository by 50%; for body weight above 90 kg, increase by 20%.

Preparation method (Rectal Suppository): To prepare 100 g of the product, take 10 g of Momordica charantia fruit powder, mix with 90 g of cocoa butter melted in a water bath at a temperature not exceeding 40 °C. Mix the resulting mass until homogeneous, pour into rectal suppository molds with a volume of 2 g, cool at 8–10 °C, remove from the molds.

Storage Conditions and Shelf Life (Rectal Suppository): store in a refrigerator at a temperature of 5–8 °C, in a light-protected place, shelf life is 12 months, after opening — use within 14 days.

Nasal Drops — Momordica charantia

Indications (Nasal Drops): allergic rhinitis, chronic catarrhal rhinitis, chronic sinusitis, rhinosinusitis, nasopharyngitis, nasal polyposis (as part of complex therapy).

Standard Dosage (Nasal Drops): 2 drops into each nostril 2 times a day for a course of 7–10 days.

Enhanced Dosage (Nasal Drops): 3 drops into each nostril 3 times a day for chronic sinusitis, rhinitis with pronounced mucosal edema.

Maximum Dosage (Nasal Drops): 4 drops into each nostril 3 times a day for resistant forms of chronic rhinosinusitis.

Preventive Dosage (Nasal Drops): 2 drops into each nostril 1 time a day for a course of 14 days for seasonal allergic rhinitis, chronic rhinosinusitis outside exacerbation.

Pediatric Dosage (Nasal Drops): allowed for children from 6 years of age — 1 drop into each nostril 1–2 times a day for a course of up to 7 days.

Contraindications (Nasal Drops): contraindicated in case of individual intolerance to components, nosebleeds, atrophic rhinitis; no scientifically documented contraindications during pregnancy and lactation.

Side Effects (Nasal Drops): in case of overdose of nasal drops, may cause burning in the nose, sneezing, rhinorrhea, nasal congestion.

Adjustment for Patient Body Weight (Nasal Drops): not required, as the dosage depends on the volume of the nasal passage, not on body weight.

Preparation method (Nasal Drops): To prepare 100 ml of drops, take 10 g of dry Momordica charantia fruit powder, pour 100 ml of 40% ethanol (the organic solvent is used for extraction only), keep for 5 days at a temperature of 20–25 °C, shaking daily. Filter, evaporate in a water bath at a temperature not exceeding 50 °C until the alcohol smell completely disappears, residual ethanol content not more than 500 ppm, then bring to a volume of 100 ml with sterile saline solution. Pour into sterile dropper bottles.

Storage Conditions and Shelf Life (Nasal Drops): store in a refrigerator at a temperature of 5–8 °C, in a light-protected place, shelf life is 6 months, after opening — use within 14 days.

Ear Drops — Momordica charantia

Indications (Ear Drops): external otitis, chronic otitis media, earwax plug, furunculosis of the external auditory canal, itching of the external auditory canal.

Standard Dosage (Ear Drops): 3 drops into the affected ear 2 times a day for a course of 7 days.

Enhanced Dosage (Ear Drops): 4 drops 3 times a day for chronic otitis media and furunculosis of the external auditory canal.

Maximum Dosage (Ear Drops): 5 drops 3 times a day for severe purulent forms of external otitis (only as part of complex therapy).

Preventive Dosage (Ear Drops): 2 drops 1 time a day for a course of 5 days after water procedures in patients with recurrent external otitis.

Pediatric Dosage (Ear Drops): allowed for children from 6 years of age — 1–2 drops 1–2 times a day for a course of 5–7 days.

Contraindications (Ear Drops): contraindicated in case of individual intolerance to components, perforation of the eardrum, purulent discharge with an unpleasant odor; no scientifically documented contraindications during pregnancy and lactation.

Side Effects (Ear Drops): in case of overdose of ear drops, may cause burning, itching, swelling of the ear canal, short-term hearing loss.

Adjustment for Patient Body Weight (Ear Drops): not required.

Preparation method (Ear Drops): To prepare 100 ml of drops, take 10 g of dry Momordica charantia fruits, grind to a fraction of 2–3 mm, pour 100 ml of coconut oil, heat in a water bath to a temperature of 40–45 °C and keep for 4 hours, stirring periodically. Strain, filter, pour into dark dropper bottles.

Storage Conditions and Shelf Life (Ear Drops): store in a dark cool place at a temperature of 5–20 °C, in tightly closed containers, shelf life is 12 months, after opening — 30 days.

Ointment — Momordica charantia

Indications (Ointment): psoriasis, eczema, acne vulgaris, trophic ulcers, burns, allergic dermatitis, atopic dermatitis, arthritis, osteoarthritis (local application to the joint area).

Standard Dosage (Ointment): apply a thin layer to the affected area of skin 2 times a day, with light massaging movements.

Enhanced Dosage (Ointment): apply 3 times a day for pronounced skin inflammation, active phase of psoriasis, infected trophic ulcers.

Maximum Dosage (Ointment): apply up to 4 times a day for severe inflammatory lesions of the skin and joints as part of complex therapy.

Preventive Dosage (Ointment): apply 1 time a day for a course of 14 days every 3 months for chronic dermatoses, predisposition to exacerbations of psoriasis, eczema.

Pediatric Dosage (Ointment): allowed in children from 6 years of age — 1 time a day on a small area of skin for atopic dermatitis and eczema.

Contraindications (Ointment): contraindicated in case of individual intolerance to components, purulent skin processes, deep wounds; no scientifically documented contraindications during pregnancy and lactation.

Side Effects (Ointment): in case of overdose of ointment, may cause local irritation, allergic reaction, itching.

Adjustment for Patient Body Weight (Ointment): not required.

Preparation method (Ointment): To prepare 100 g of ointment, take 15 g of Momordica charantia fruit powder, 50 g of coconut oil, 30 g of beeswax, 5 g of shea butter. Melt the coconut oil and shea butter in a water bath at a temperature of 40–45 °C, add the Momordica charantia powder, keep for 30 minutes with stirring, then add the beeswax, stir until homogeneous, pour into sterile jars and cool.

Storage Conditions and Shelf Life (Ointment): store in a cool dark place at a temperature of 5–20 °C, in airtight containers shielded from EMI; shelf life is 12 months, after opening — 60 days.

Cream-Emulsion — Momordica charantia

Indications (Cream-Emulsion): psoriasis, eczema, acne vulgaris, seborrheic dermatitis, burns, dry skin, inflammatory skin diseases in the subacute stage.

Standard Dosage (Cream-Emulsion): apply a thin layer 2 times a day to clean dry skin.

Enhanced Dosage (Cream-Emulsion): apply 3 times a day for pronounced peeling, dryness, skin irritation.

Maximum Dosage (Cream-Emulsion): apply up to 4 times a day for severe forms of dermatosis (only as part of complex therapy).

Preventive Dosage (Cream-Emulsion): 1 time a day at night in courses of 14 days every 3 months in patients with chronic dermatoses.

Pediatric Dosage (Cream-Emulsion): allowed in children from 3 years of age — 1 time a day on a small area of skin.

Contraindications (Cream-Emulsion): contraindicated in case of individual intolerance to components, weeping forms of dermatitis, purulent skin lesions; no scientifically documented contraindications during pregnancy and lactation.

Side Effects (Cream-Emulsion): in case of overdose of cream-emulsion, may cause burning, itching, skin erythema.

Adjustment for Patient Body Weight (Cream-Emulsion): not required.

Preparation method (Cream-Emulsion): To prepare 100 g of cream, take 10 g of Momordica charantia fruit powder, 50 g of coconut oil, 30 g of distilled water, 8 g of beeswax, 2 g of emulsifier (natural lecithin). Melt the coconut oil and wax in a water bath at 45 °C, add the Momordica charantia powder, stir, separately heat the water to 45 °C, slowly pour into the oil phase, adding lecithin, whisk until a homogeneous emulsion is obtained, pour into sterile jars.

Storage Conditions and Shelf Life (Cream-Emulsion): store in a refrigerator at a temperature of 5–8 °C, in tightly closed containers, protected from light and EMI; shelf life is 6 months, after opening — 30 days.

Serum — Momordica charantia

Indications (Serum): acne vulgaris, post-inflammatory hyperpigmentation, rosacea, seborrheic dermatitis, melasma, skin photoaging, dry skin, decreased skin elasticity, expression and age wrinkles.

Standard Dosage (Serum): apply 2–3 drops of serum to cleansed facial and neck skin 1 time a day in the evening.

Enhanced Dosage (Serum): apply 2–3 drops of serum 2 times a day (morning and evening) for pronounced signs of photoaging, hyperpigmentation, dry skin.

Maximum Dosage (Serum): apply 4–5 drops 2 times a day for severe forms of post-inflammatory hyperpigmentation, deep wrinkles, pronounced loss of skin elasticity.

Preventive Dosage (Serum): apply 2–3 drops of serum 1 time a day in the evening for a course of 30 days every 6 months in patients with photosensitive skin prone to early aging.

Pediatric Dosage (Serum): not used in children under 16 years of age.

Contraindications (Serum): contraindicated in case of individual intolerance to components, active inflammatory skin processes, purulent eruptions, open wounds; no scientifically documented contraindications during pregnancy and lactation.

Side Effects (Serum): in case of overdose of serum, may cause burning, redness, itching, skin peeling.

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

Preparation method (Serum): To prepare 100 g of serum, take 5 g of dry Momordica charantia extract, 70 g of distilled water, 20 g of aloe vera gel, 5 g of coconut oil. Dissolve the dry extract in distilled water at a temperature of 35–40 °C, add the aloe vera gel, mix thoroughly, then add the coconut oil in the form of a fine emulsion using a hand blender. Filter the finished mixture through a sterile 0.45 µm filter, pour into dropper bottles.

Storage Conditions and Shelf Life (Serum): store in a refrigerator at a temperature of 5–8 °C, in dark containers shielded from EMI; shelf life is 3 months, after opening — use within 30 days.

Toxicity and biosafety — Momordica charantia

Toxicity studies of Momordica charantia show that with oral administration of fruit extract to mice, the LD₅₀ value is more than 4000 mg/kg body weight, which indicates low acute toxicity with oral use. With intravenous administration of seed extract, the LD₅₀ in mice was noted at about 50 mg/kg, which is associated with the presence of toxic protein compounds such as ribosome-inactivating proteins (e.g., momordicin and α-momorcharin). Long-term use in high doses may cause hypoglycemia, diarrhea, and abdominal cramps. Based on available data, when therapeutic dosages are observed, Momordica charantia is considered relatively safe for oral use, but parenteral forms require strict control and limitation due to high toxicity when administered directly into the blood.

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

Pharmacodynamics — Momordica charantia

The pharmacodynamic properties of Momordica charantia are determined by a complex of biologically active compounds, including triterpene saponins, flavonoids, plant-derived peptides, ribosome-inactivating proteins, phenolic acids, alkaloids, and sterols. These compounds act on various physiological systems of the body, exerting both local and systemic effects. At the level of the digestive system, they are able to modulate the activity of enzyme complexes, affecting the hydrolysis and absorption of carbohydrates and lipids, as well as alter the secretion of digestive juices. At the endocrine level, an effect on insulin secretion and sensitivity is observed, as well as the regulation of a number of hormonal signals involved in energy metabolism. On the part of the immune system, Momordica charantia exhibits a modulating effect, altering the balance of pro-inflammatory and anti-inflammatory mediators, including cytokines, which helps regulate the immune response. The anti-inflammatory effect is realized through the inhibition of the activity of enzymes involved in the synthesis of inflammatory mediators, as well as through the stabilization of cell membranes. Antioxidant activity is associated with the presence of phenolic compounds and flavonoids capable of neutralizing free radicals and reducing oxidative stress. On the nervous system, Momordica charantia has a predominantly indirect effect, associated with improved microcirculation and modulation of the level of certain neurotransmitters, as well as a possible effect on central and peripheral mechanisms of metabolic regulation. With respect to the skin and mucous membranes, a local wound healing, keratolytic, and antimicrobial effect is noted, due to both direct damage to the cell walls of microorganisms and modulation of the local immune response. The effect on the cardiovascular system is manifested through an effect on vascular tone and modulation of the vascular endothelium, mediated by both antioxidant and anti-inflammatory mechanisms. With systemic exposure, the pharmacological effects of Momordica charantia can combine to form a complex profile including antioxidant, anti-inflammatory, immunomodulatory, hypolipidemic, metabolically active, and regenerative effects, confirmed by the results of pharmacological and biochemical studies on cell models and in vivo.

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

Pharmacokinetics — Momordica charantia

Absorption of active compounds of Momordica charantia following oral administration occurs mainly in the small intestine, where saponins and flavonoids undergo partial transformation under the action of microflora, which contributes to the formation of metabolites with altered biological activity. Peptide compounds undergo partial hydrolysis by proteases, but some of them may be absorbed in an incompletely broken down form, realizing a systemic effect. With transdermal administration (ointment, cream, serum), the penetration of active components occurs through the stratum corneum of the skin, followed by diffusion into the dermis, while lipophilic components (terpenoids, sterins) can be deposited in the adipose tissue of the skin, providing a prolonged effect. When applied through mucous membranes (suppositories, drops), faster entry of hydrophilic components into the systemic circulation is observed, bypassing a significant part of first-pass metabolism through the liver. The distribution of active substances in the body depends on their lipophilicity: polar compounds circulate in the plasma mainly in free form or in complex with proteins, while lipophilic ones are deposited in adipose tissue and cell membranes. The metabolism of most compounds of Momordica charantia occurs in the liver with the participation of phase I and II enzymes, including hydroxylation, methylation, conjugation with glucuronic and sulfuric acids. The resulting metabolites, as a rule, have altered biological activity and greater hydrophilicity, which facilitates their excretion. Excretion is carried out primarily with bile and feces for lipophilic metabolites, and with urine for hydrophilic compounds and their conjugates. A small amount of volatile components may be excreted through the lungs, as well as through the sweat glands during intense sweating. With long-term use, moderate accumulation of lipophilic components in tissues is possible, which requires compliance with recommended courses of use and breaks between them.

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

Mechanisms of Action and Scientific Rationale — Momordica charantia

The biological activity of Momordica charantia is associated with a complex of secondary metabolites, including triterpene saponins (e.g., momordicides), plant-derived polypeptides, phenolic compounds, flavonoids, and ribosome-inactivating proteins. These substances affect enzyme systems and signaling cascades involved in the regulation of metabolism, inflammatory processes, and cell proliferation. In vitro studies show that saponins of Momordica charantia are able to inhibit the activity of the enzymes α-glucosidase and α-amylase, altering the dynamics of polysaccharide hydrolysis. Peptide compounds and proteins such as α-momorcharin have the ability to interact with ribosomes, inhibiting protein synthesis in target cells, as confirmed in cell culture experiments. Flavonoids and phenolic acids exhibit antioxidant activity, binding free radicals and suppressing lipid peroxidation, which reduces the activation of pro-inflammatory signaling pathways, including NF-κB and MAPK. Additionally, it has been established that extracts of Momordica charantia can modulate cytokine production (TNF-α, IL-6, IL-10) and affect the activity of macrophages and neutrophils, which indicates a multi-level immunomodulatory effect. Some compounds affect the expression of genes regulating apoptosis and the functioning of glucocorticoid receptors, which may be associated with anti-inflammatory and adaptogenic effects.

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

Synergy — Momordica charantia

Scientific research demonstrates that Momordica charantia exhibits pharmacological synergy with a number of medicinal plants and natural compounds, with the nature of the interaction being both additive and potentiating. In vitro and in vivo experiments have shown that the combination of Momordica charantia with Trigonella foenum-graecum enhances the modulation of the activity of carbohydrate metabolism enzymes and increases antioxidant activity due to the cumulative content of saponins and flavonoids. Co-administration with Gymnema sylvestre demonstrates potentiation of the regulatory effect on the secretion of insulin-like peptides, which is associated with the synergistic action of triterpene saponins of both taxa. The combination with Curcuma longa enhances the anti-inflammatory effect due to the simultaneous inhibition of COX and LOX enzymes, as well as the suppression of NF-κB activation, which was confirmed on cellular models of inflammation. In combination with Camellia sinensis, an additive increase in antioxidant potential is observed, due to the total content of polyphenols and catechins. Studies also indicate a modulating interaction with Allium sativum, in which the regulation of endothelial function and the activity of antioxidant enzymes are enhanced, which is explained by the combination of organosulfur compounds of garlic and phenolic components of Momordica charantia. These interactions confirm that the use of Momordica charantia as part of phytocomplexes with taxa having similar or complementary pharmacological properties can provide a broader spectrum of action due to the multi-target effect on signaling cascades and cellular targets.

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

Geography of use and traditional medicine — Momordica charantia

Momordica charantia is known in the traditional medical and cultural practices of tropical and subtropical Asia, Africa, and a number of Latin American countries. In Southeast Asia, the plant occupies an important place in the folk medicine of Thailand, Vietnam, Cambodia, and Laos, where it is used in the form of decoctions, fresh juice, Tinctures, and oil macerates. In the Indian Ayurvedic tradition, known for more than two thousand years, bitter melon was mentioned in ancient Sanskrit herbal guides, including classical collections attributed to the schools of Charaka and Sushruta, where it was used fresh and as part of complex mixtures. In China, references to its use are found in medical chronicles of the Ming era, where the fruits and leaves were described as an important component of phytotherapeutic preparations. In African ethnomedical practices, especially in East and West Africa, the fruits and seeds were used in the form of decoctions and powders, as well as an element of purification rituals. In the Caribbean region and Central American countries, the plant is known as culturally significant, including in Creole traditions, where it was used in home tinctures and oil infusions. In Thai folk medicine, fresh and dried fruits were sometimes used as part of steam procedures and wraps. In the ritual practice of some peoples of Southeast Asia, the fruits and seeds were used as amulets and in symbolic actions associated with cleansing the home. Archaeoethnobotanical studies indicate the use of wild forms of bitter melon in southern China and India more than 2000 years ago, which is confirmed by finds of seeds in layers of ancient settlements. In the folklore of a number of peoples of Southeast Asia, bitter melon was considered a plant capable of protecting against evil spirits and "purifying the blood," which reflects a synthesis of medical and symbolic ideas.