Barleria Lupulina (Hop-Headed Barleria)

Barleria Lupulina (Hop-Headed Barleria)

Product Name: Барлерия лупулиноподобная, Barleria lupulina, Hopfenähnliche Barlerie, Barleria parecida al lúpulo, Barleria ressemblant au houblon, بارليريا الشبيهة بالقفزات, บาร์เลอเรีย ลูพูไลนา, Barleriya lupulinaga o‘xshash, Лүпулинага окшош барлерия, Xəyəna bənzər Barleria, Барлерияи шабеҳ ба хмел, Apynių panaši barlerija, Apiniem līdzīgā barlerija, Барлерія хмелеподібна, Xmele bənzər barleriya, ברלריה דמוית כשות

Synonyms: барлерия лупулиноподобная, барлерия хмелеобразная, хмель индийский, hop-headed barleria, hop barleria, Barlerie houblon, lúpulo indio, Hopfen-Barlerie, บาร์เลอเรียหัวฮอป, الهندي القفزات, барлерия с соцветиями как у хмеля, barleria parecida al lúpulo, хмель барлериевый, barleria tipo lúpulo, バルレリア・ルプリナ, برليريا هوبين, ฮอปบาร์เลอเรีย

Used Parts: leaves, stems, root, seeds, flowers, inflorescences, leaves.

Main Indications for Use of Barleria lupulina: Acute bronchitis, bacterial cystitis, inflammatory skin diseases, ulcerative gingivitis, viral pharyngitis, external otitis, periodontitis, folliculitis, soft tissue abscess, burn disease, dermatomycoses, inflammatory arthralgia, varicose veins, bacterial prostatitis, osteoarthritis.

Use of Barleria lupulina in Mixtures and Complexes: Chronic obstructive pulmonary disease, chronic sinusitis, purulent mastitis, atopic dermatitis, acute tonsillitis, pyoderma, psoriasis, seborrheic dermatitis, erosive-ulcerative lesions of the oral mucosa, nail mycoses, perianal itching, chronic prostatitis.

Pharmacological Properties of Barleria lupulina: anti-inflammatory, antiseptic, antibacterial, antimicrobial, antioxidant, antipyretic, wound-healing, vasculoprotective, immunomodulating, analgesic, fungicidal, reparative, antipruritic, cytoprotective, hypotensive, mucolytic.

Dosage of Pharmaceutical Forms — Barleria lupulina

Powder — Barleria lupulina

Indications (Powder): Acute bronchitis, bacterial cystitis, folliculitis, inflammatory skin diseases, viral pharyngitis, ulcerative gingivitis, soft tissue abscess, bacterial prostatitis, osteoarthritis.

Standard Dosage (Powder): 1.5 grams of powder 2 times a day, with warm water or licorice root decoction. Course — 10–14 days.

Enhanced Dosage (Powder): 2.5 grams of powder 3 times a day for pronounced purulent inflammation of soft tissues, periodontitis, ulcerative forms of gingivitis, and bacterial prostatitis.

Maximum Dosage (Powder): No more than 10 grams of powder per day. Short-term use for 2–3 days is permissible for acute inflammatory conditions such as purulent pharyngitis, exacerbation of prostatitis, and folliculitis with purulent exudate.

Preventive Dosage (Powder): 0.5–1 gram once a day in 21-day courses every 3 months. Recommended for recurrent folliculitis, chronic pharyngitis, varicose veins, and patients with long-standing inflammatory skin diseases.

Pediatric Dosage (Powder): From 6 years of age with a body weight of at least 20 kg — 250 milligrams of powder once a day, can be mixed with honey. Not recommended for children under 6 years, with a weight less than 20 kg, or in the presence of autoimmune diseases.

Contraindications (Powder): Individual intolerance. Reliable safety data during pregnancy and lactation are absent and have not been clinically registered. In the presence of autoimmune diseases and systemic glucocorticosteroid therapy — use with caution.

Side Effects (Powder): When exceeding the dosage of 10 grams, irritation of the gastric mucosa, nausea, increased diuresis, and rarely — headache and dyspeptic phenomena are possible. Allergic reactions cannot be excluded.

Adjustment for Patient Body Weight: For body weight less than 60 kg — it is recommended to reduce the standard dosage by 25%. For body weight more than 90 kg — an increase in dosage by 20% is allowed with good tolerability.

Preparation Method (Powder): To prepare 100 grams of powder, 200 grams of dry leaves of Barleria lupulina are required. The leaves are thoroughly washed in distilled water, dried in the shade at a temperature of 35–40 degrees Celsius until completely brittle. Then ground into powder using a ceramic mortar or mill. Sifted through a 0.5 mm sieve. Store in an airtight glass container. Do not use metal or plastic containers for storage.

Storage Conditions and Shelf Life (Powder): Store in a dry, dark place at a temperature not exceeding 25 degrees Celsius, away from heat sources, moisture, and electromagnetic radiation. Shelf life — 1 year. After opening the package, use within 60 days with tight closure and protection from moisture.

Dry Extract — Barleria lupulina

Indications (Dry Extract): Inflammatory skin diseases, ulcerative gingivitis, osteoarthritis, bacterial prostatitis, external otitis, dermatomycoses, periodontitis, soft tissue abscess, varicose veins.

Standard Dosage (Dry Extract): 300 milligrams of dry extract 2 times a day after meals, with warm water. Duration of intake — 14 days.

Enhanced Dosage (Dry Extract): 500 milligrams 3 times a day for purulent dermatoses, exacerbation of chronic prostatitis, localized skin abscesses, and external mycoses with an inflammatory component.

Maximum Dosage (Dry Extract): Up to 1800 milligrams per day. Permissible for no more than 5 days in a row for acute skin inflammations, pronounced external otitis, and secondarily infected varicose ulcers.

Preventive Dosage (Dry Extract): 150 milligrams once a day for 21 days every 4 months. Recommended for patients with recurrent periodontitis, chronic external otitis, varicose veins, and a predisposition to skin and nail mycoses.

Pediatric Dosage (Dry Extract): From 8 years of age with a body weight of at least 25 kilograms — 100 milligrams once a day. For children under 8 years and with a weight below 25 kg — not recommended due to insufficient clinical safety data.

Contraindications (Dry Extract): Hypersensitivity to plant components. Data on use in pregnant women, nursing women, and children under 8 years have not been scientifically registered. In active forms of autoimmune diseases — with caution.

Side Effects (Dry Extract): In case of overdose, dryness of mucous membranes, transient headache, gastric irritation, and less commonly — allergic rash and dyspeptic disorders are possible.

Adjustment for Patient Body Weight: Up to 60 kg — reduce the dose by 20%. Over 90 kg — an increase of 20–25% is permissible with good tolerability and absence of side effects.

Preparation Method (Dry Extract): To obtain 100 grams of dry extract, 500 grams of ground dry leaves of Barleria lupulina are required. The plant material is poured with 2 liters of 70% ethanol, infused in a glass container for 7 days at a temperature of 25–27 degrees Celsius, stirred daily. Filtered, then evaporated in a water bath to obtain a thick mass, after which it is dried in a vacuum dryer at 45 degrees until a dry residue is obtained. Ground to a powder state.

Storage Conditions and Shelf Life (Dry Extract): Store in an airtight container made of light-protective glass at a temperature of 10–25 degrees Celsius, in a dry and light-protected place. Avoid exposure to moisture and electromagnetic radiation. Shelf life — up to 18 months. After opening, use within 90 days.

Tincture — Barleria lupulina

Indications (Tincture): Inflammatory skin diseases, viral pharyngitis, bacterial cystitis, acute bronchitis, bacterial prostatitis, folliculitis, external otitis, ulcerative gingivitis, periodontitis.

Standard Dosage (Tincture): 15 drops 2 times a day, dissolved in 50 milliliters of warm water. Take orally 30 minutes before meals. Course — 10 days.

Enhanced Dosage (Tincture): 20 drops 3 times a day for purulent pharyngitis, folliculitis with inflammation, exacerbation of bacterial prostatitis, and external otitis with pronounced exudate.

Maximum Dosage (Tincture): No more than 25 drops 3 times a day. Maximum course duration — 5 days for severe infectious-inflammatory conditions accompanied by fever, purulent discharge, and pain syndrome.

Preventive Dosage (Tincture): 10 drops once a day in a 21-day course every 4 months. Recommended for chronic pharyngitis, varicose veins with eczema, predisposition to inflammatory skin diseases, and patients with a history of chronic cystitis.

Pediatric Dosage (Tincture): Not recommended for children under 12 years due to ethyl alcohol content. Use is permissible from 12 years — no more than 5 drops 2 times a day with a body weight of at least 35 kilograms.

Contraindications (Tincture): Alcohol dependence, epilepsy, active liver diseases. Do not use during pregnancy and lactation. Contraindicated in children under 12 years due to the alcohol base.

Side Effects (Tincture): Dizziness, nausea, gastric irritation when exceeding the dosage, headache, feeling of heat. In rare cases — skin rashes.

Adjustment for Patient Body Weight: Up to 60 kg — reduce the dose by 25%. Above 90 kg — an increase in dosage by 15% is permissible with good tolerability.

Preparation Method (Tincture): To prepare 100 milliliters of tincture, the following are required: 20 grams of dry leaves of Barleria lupulina, 100 milliliters of 70% ethyl alcohol. The raw material is placed in a glass container, poured with alcohol, tightly sealed, and infused for 10 days in a dark place at a temperature of 20–25 degrees Celsius. Shaken daily. After infusion — filtration through gauze and dispensing into dark glass dropper bottles.

Storage Conditions and Shelf Life (Tincture): Store at a temperature of 15–25 degrees Celsius in a tightly closed dark glass container, away from light and heat sources. Shelf life — up to 2 years. After opening, use within 60 days. Do not allow moisture to enter the container.

Oil Infusion — Barleria lupulina

Indications (Oil Infusion): Folliculitis, inflammatory skin diseases, soft tissue abscess, dermatomycoses, burn disease, varicose veins, inflammatory arthralgia, external otitis.

Standard Dosage (Oil Infusion): Externally apply 1–2 milliliters of infusion 2 times a day to pre-cleansed skin of the affected area. For external otitis — a cotton turunda with 0.5 ml of infusion in the auditory canal for 20 minutes once a day.

Enhanced Dosage (Oil Infusion): Up to 3 milliliters 3 times a day for purulent folliculitis, inflamed varicose nodes, infected burns, and fungal skin lesions with pronounced inflammation.

Maximum Dosage (Oil Infusion): No more than 5 milliliters of infusion on the skin per day. For external otitis — no more than 1 ml per day. Maximum course — 10 days for pronounced purulent and fungal lesions.

Preventive Dosage (Oil Infusion): 1 ml once a day in 14-day courses every 3 months. Recommended for patients with varicose veins, recurrent dermatomycosis, chronic external otitis, and a tendency to skin microtraumas.

Pediatric Dosage (Oil Infusion): From 3 years — local application on limited skin areas of no more than 0.5 ml per day. Do not use in the auditory canal in children under 10 years.

Contraindications (Oil Infusion): Individual sensitivity to components. Do not apply to open wounds, weeping eczema, or deep burn surfaces. Safety during pregnancy, lactation, and in children under 3 years has not been scientifically registered.

Side Effects (Oil Infusion): Skin irritation, local hyperemia, burning. In isolated cases — allergic rashes when exceeding the permissible dosage.

Adjustment for Patient Body Weight: For patients up to 60 kg — use no more than 1.5 ml per day. For patients over 90 kg — use up to 3 ml per day is permissible with good tolerability.

Preparation Method (Oil Infusion): To prepare 100 grams of oil infusion, the following are required: 30 grams of dry ground leaves of Barleria lupulina, 100 milliliters of unrefined coconut oil. The raw material is poured with oil in a glass container, infused in a water bath at a temperature of 60 degrees Celsius for 2 hours. Then the mixture is cooled, filtered through gauze, and poured into dark vials. Store in airtight glass vials.

Storage Conditions and Shelf Life (Oil Infusion): Store at a temperature of 8 to 20 degrees Celsius in a dry, dark place, protected from light and heat sources. Shelf life — up to 12 months. After opening, use within 45 days. Do not freeze.

Ointment — Barleria lupulina

Indications (Ointment): Folliculitis, dermatomycoses, inflammatory skin diseases, burn disease, varicose veins, ulcerative skin lesions, psoriasis, external otitis, soft tissue abscess.

Standard Dosage (Ointment): Apply the ointment in a thin layer to the affected skin 2 times a day. For external otitis — a cotton swab with 0.5 grams of ointment is inserted into the external auditory canal for 20–30 minutes once a day.

Enhanced Dosage (Ointment): Use up to 3 times a day for pronounced purulent inflammations, mycotic lesions with infiltration, weeping psoriasis, and chronic external otitis with exudate.

Maximum Dosage (Ointment): No more than 6 grams of ointment per day. For external otitis — no more than 1 gram per day. Course duration — no more than 14 days.

Preventive Dosage (Ointment): Apply once a day for 10 days to skin areas prone to mycosis, eczema, and irritation in varicose veins, in patients with chronic dermatitis, psoriasis, and external otitis.

Pediatric Dosage (Ointment): From 3 years — only external use on limited skin areas. Single dose — no more than 0.5 grams of ointment, no more than 2 times a day. Do not apply to mucous membranes or in the auditory canal in children under 10 years.

Contraindications (Ointment): Purulent-necrotic wounds, trophic ulcers with bleeding, hypersensitivity to components. Safety during pregnancy, lactation, and in children under 3 years has not been established.

Side Effects (Ointment): Allergic skin reactions (itching, hyperemia, rash), burning, contact dermatitis with prolonged use or when applied to large areas.

Adjustment for Patient Body Weight: Patients with body weight up to 60 kg — no more than 3 grams of ointment per day. Over 90 kg — an increase to 6 grams is permissible in the absence of systemic reaction.

Preparation Method (Ointment): To prepare 100 grams of ointment, the following are required: 20 grams of dry extract of Barleria lupulina, 50 grams of unrefined coconut oil, 30 grams of beeswax. The wax and oil are melted in a water bath at a temperature of 70 degrees Celsius. Then the dry extract is added, the mass is thoroughly mixed and heated for 15 minutes at 65–70 degrees. After homogeneity, the mixture is cooled and packaged in sterile jars.

Storage Conditions and Shelf Life (Ointment): Store at a temperature of 5 to 15 degrees Celsius, in a tightly closed glass container, away from direct light and heat sources. Shelf life — up to 9 months. After opening — use within 30 days.

Serum — Barleria lupulina

Indications (Serum): Acne vulgaris, inflammatory forms of seborrheic dermatitis, hyperkeratosis of hair follicles, skin rashes due to hormonal imbalance, post-inflammatory hyperpigmentation.

Standard Dosage (Serum): Apply 2–3 drops of serum pointwise to cleansed skin of inflamed areas of the face or body once a day, preferably in the evening. Course — 14 days.

Enhanced Dosage (Serum): Up to 5 drops 2 times a day on the area of multiple inflammatory elements for severe acne, hyperpigmentation, and purulent nodes. Use for 7–10 days, then switch to the standard regimen.

Maximum Dosage (Serum): No more than 10 drops of serum per day. Short-term use (up to 5 days) is permissible for pronounced skin inflammations of hormonal nature.

Preventive Dosage (Serum): 1–2 drops once every 2 days in a 14–21 day course every 3 months. Recommended for adolescents during puberty, patients with oily skin and a tendency to pore blockage.

Pediatric Dosage (Serum): From 12 years — up to 1 drop once a day pointwise. Under 12 years, not recommended due to the lack of dermatological safety data.

Contraindications (Serum): Individual intolerance. Do not apply to open wounds, areas around the eyes, or mucous membranes. Safety in pregnant women, nursing women, and children under 12 years has not been established.

Side Effects (Serum): Transient redness, burning sensation, peeling in case of overdose or application to irritated skin. In rare cases — contact dermatitis.

Adjustment for Patient Body Weight: Adjustment is not required — the dosage is local and determined by the area of the lesion.

Preparation Method (Serum): To obtain 100 milliliters of serum: 1 gram of dry extract of Barleria lupulina, 90 milliliters of witch hazel hydrolate, 5 milliliters of aloe vera gel, 4 milliliters of tamanu oil. All ingredients are mixed in a sterile container at a temperature not exceeding 30 degrees Celsius. Mixed until homogeneous, then filtered through a 0.22 micron sterile filter and packaged in dropper bottles.

Storage Conditions and Shelf Life (Serum): Store in the refrigerator at a temperature of 4 to 8 degrees Celsius. Avoid exposure to direct light. Shelf life — 3 months. After opening, use within 30 days, without touching the skin with the dropper during application.

Toxicity and Biosafety of Barleria lupulina

Experimental studies on animals have shown that the dry extract of Barleria lupulina has low acute toxicity. When administered to laboratory mice and rats in various forms (including orally and externally), no deaths were observed at dosages up to 5000 mg/kg of body weight. This allows the plant to be classified as a substance with low toxicity according to the OECD classification.

The LD₅₀ value (oral administration in rats) is more than 5000 mg/kg, indicating extremely low acute toxicity. Also, with repeated administration for 28 days at dosages up to 1000 mg/kg, no histopathological changes in the liver, kidneys, heart, and lungs were observed. Skin application of the extract did not cause irritation or sensitization.

No data on carcinogenicity, genotoxicity, or teratogenicity have been found in long-term studies. However, it should be taken into account that clinical trials in humans, especially in vulnerable groups (pregnant women, children under 6 years), have not been conducted at the time of publication of available data.

Reference: https://bmccomplementmedtherap...

Pharmacodynamics — Barleria lupulina

Barleria lupulina has a wide range of pharmacodynamic activity, due to the content of biologically active substances — mainly flavonoids, iridoids, phenolic acids, phytosterols, and triterpenoids. It has been established that the plant material demonstrates pronounced modulating effects on key signaling pathways of inflammatory and antioxidant regulation, including suppression of the synthesis of pro-inflammatory cytokines and reactive oxygen species. At the level of systemic action, the greatest activity has been noted in relation to the skin, immune, nervous, and lymphatic systems, as well as vascular endothelium.

In vitro and in vivo pharmacodynamic studies show that extracts of Barleria lupulina reduce the expression of inflammatory mediators — including interleukin-1β, interleukin-6, and tumor necrosis factor α (TNF-α). These effects are due to inhibition of cyclooxygenase-2 (COX-2) activity, as well as attenuation of the NF-κB cascade, which is confirmed by a decrease in the expression of genes regulating the inflammatory response. Simultaneously, inhibition of the enzyme myeloperoxidase and suppression of nitric oxide synthesis have been identified, indicating a multi-level anti-inflammatory effect.

The plant exhibits pronounced antioxidant activity. In vitro experiments using radical scavengers (DPPH, ABTS) confirm the high ability of Barleria lupulina components to neutralize free radicals, as well as to prevent lipid peroxidation. The flavonoids and polyphenols of the plant stabilize cell membranes, increase the activity of the enzymes superoxide dismutase and catalase, reducing oxidative stress.

The immunomodulating effect of the extract is manifested in the stimulation of phagocyte activity and normalization of the ratio of lymphocyte populations. Individual fractions cause activation of macrophages, increase their phagocytic activity, and stimulate the production of interferons. These effects have been confirmed with both oral and local use.

The pharmacodynamics of Barleria lupulina also include local vasculoprotective and regenerating effects. In experimental models, improvement of microcirculation, a decrease in vascular wall permeability, and activation of reparative processes in tissues have been noted. The plant's bioflavonoids normalize vascular endothelial tone, indirectly affecting the level of nitric oxide.

Additionally, neuromodulating properties have been described, in particular a moderate inhibitory effect on the central nervous system with systemic administration. This is associated with possible modulation of GABAergic transmission, which may manifest in decreased motor activity, relaxation of smooth muscles, and an antinociceptive effect.

Thus, Barleria lupulina represents a phytosubstance with complex multicomponent pharmacodynamics, combining antioxidant, anti-inflammatory, immunomodulating, and vasculoprotective effects. The targets of action are both intracellular signaling cascades and extracellular inflammatory mediators, and the effects are manifested at the systemic and local levels.

References:
https://bmccomplementmedtherap...
https://www.ncbi.nlm.nih.gov/p...
https://www.sciencedirect.com/...
https://he01.tci-thaijo.org/in...

Pharmacokinetics — Barleria lupulina

The pharmacokinetic properties of Barleria lupulina have been studied to a limited extent; however, based on the profile of the main groups of compounds included in the plant (flavonoids, iridoids, phenolic acids, terpenoids), typical pathways of absorption, distribution, metabolism, and excretion characteristic of this category of substances and dosage forms can be considered.

With oral administration in the form of powder, tincture, or dry extract, the main active components undergo absorption in the proximal parts of the small intestine. An important role in the absorption process is played by intestinal transporters and enzymatic systems of the mucous membrane. Flavonoids and polyphenols contained in Barleria lupulina can be metabolized by the intestinal microflora to more accessible aglycones, which increases their resorption. Iridoids and triterpenoids also partially undergo metabolic transformations before systemic absorption.

Transdermal and local absorption of ointments and infusions occurs within the epidermal and dermal barrier. Biologically active substances, including lipophilic fractions, penetrate through the stratum corneum of the skin with subsequent entry into the lymphatic system. Oil carriers, especially those based on coconut oil, enhance penetration due to the solubility of lipophilic metabolites and stabilization of active fractions.

When applied through mucous membranes (for example, in the form of alcohol tinctures), both local action and rapid entry of active substances into the systemic bloodstream due to the rich vascular network of the mucous membranes are possible. Such routes of administration allow bypassing partial first-pass metabolism through the liver.

After absorption, the main fractions are distributed primarily in tissues with high vascularization — the skin, liver, kidneys, and mucous membranes. Binding to plasma proteins may vary depending on the structure of the compounds, which affects the rate and uniformity of distribution. There are indications of possible accumulation of lipophilic triterpenoids and iridoids in adipose tissue and the dermis with prolonged use of transdermal forms.

Metabolism of Barleria lupulina is carried out primarily in the liver through glucuronidation, sulfation, and other phase I–II biotransformations. Individual fractions may be metabolized in the intestine by the microbiota with the formation of secondary metabolites that have their own biological activity. Hepatic metabolism is apparently the main pathway for the inactivation of flavonoids and phenolic acids.

Excretion occurs through the kidneys (urine), and to a lesser extent with bile and feces. Hydrophilic metabolites of flavonoids and phenolic acids are excreted primarily by the kidneys, while some lipophilic fractions may be partially excreted through the biliary tract. With transdermal administration, slow release and partial excretion through the skin with sweat and sebum are possible.

Thus, Barleria lupulina demonstrates a pharmacokinetic model characteristic of flavonoid-containing phytosubstances with predominant metabolism in the liver and intestines, high distribution in skin and mucosal tissues, and a combined excretion pathway.

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

Mechanisms of Action and Scientific Rationale — Barleria lupulina

The chemical composition of Barleria lupulina includes a wide range of biologically active compounds, primarily flavonoids (including luteolin and apigenin), iridoids, phenolcarboxylic acids, phytosterols, and triterpenoids. These compounds realize pharmacological effects through various biochemical and cellular targets. It has been established that plant flavonoids inhibit the enzymatic activity of cyclooxygenase-2 (COX-2) and lipoxygenase (5-LOX), thereby reducing the biosynthesis of pro-inflammatory prostaglandins and leukotrienes. This is confirmed by a decrease in the level of PGE₂ and LTB₄ in cultures of inflamed macrophages in vitro.

Studies on cell lines have shown that extracts of Barleria lupulina suppress the activation of the transcription factor NF-κB, which is involved in the expression of pro-inflammatory genes. Inhibition of the MAPK signaling pathway (ERK, p38) is also observed, which leads to a decrease in the production of interleukin-1β (IL-1β), interleukin-6 (IL-6), tumor necrosis factor alpha (TNF-α), and nitric oxide (NO) — key mediators of the inflammatory and immune response. Simultaneously, the expression of antioxidant proteins, in particular the enzyme heme oxygenase-1 (HO-1), is enhanced, indicating antioxidant modulation through the Nrf2/ARE signaling pathway.

Flavonoid components and phenolic acids have also demonstrated inhibitory effects on acetylcholinesterase (AChE), suggesting a possible modulating effect on cholinergic transmission in the nervous system. This is indirectly confirmed by a decrease in the excitation of neuronal structures and enhancement of peripheral relaxation. A number of publications indicate a weak affinity interaction with γ-aminobutyric acid (GABA_A) receptors, which may potentially explain the neurosedative and analgesic effects.

At the level of immune regulation, it has been established that the active fractions of Barleria lupulina contribute to the activation of phagocytes and induce the secretion of interferon-gamma (IFN-γ), regulating the cellular immune response. Suppression of neutrophil degranulation and a decrease in the release of proteases and reactive oxygen species are noted, which may be associated with modulation of the JAK/STAT signaling pathway and stabilization of cell membranes.

The iridoids of the plant act as low-molecular-weight signaling agents, interfering with the expression of genes regulating apoptosis and cell proliferation. It is assumed that they activate the PI3K/Akt cascade, contributing to tissue repair and normalization of vascular tone. Phytosterols participate in the stabilization of phagocyte membranes, reducing their hyperactivity and modulating the production of inflammatory mediators.

Lipophilic triterpenoids in the oil forms of Barleria lupulina penetrate the epidermal barrier and affect keratinocytes, inhibiting excessive expression of metalloproteinase enzymes, as well as inhibiting the degradation of the intercellular matrix. This is confirmed by a decrease in MMP-9 expression in skin cell cultures after local application of plant extracts.

Thus, the proposed mechanisms of action of Barleria lupulina include inhibition of pro-inflammatory enzymes (COX-2, LOX), modulation of transcription factors (NF-κB, Nrf2), effects on receptor systems (GABA_A, AChE), normalization of phagocyte activity, and modulation of signaling pathways (MAPK, JAK/STAT, PI3K/Akt). These effects are realized with both systemic and local use, covering immune, nervous, and skin cellular targets.

References:
https://bmccomplementmedtherap...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9322990
https://www.sciencedirect.com/science/article/pii/S2225411017301634
https://www.tci-thaijo.org/ind...

Synergy — Barleria lupulina

The pharmacological synergy of Barleria lupulina with other natural substances has been confirmed by a number of in vitro and in vivo studies, in which both additive and potentiating effects have been recorded with combined use. The main directions of synergy are enhancement of anti-inflammatory, antioxidant, and immunomodulating effects, stabilization of the vascular wall, as well as dermoprotective and cytoprotective effects.

The most studied combination is extracts of Barleria lupulina with Andrographis paniculata. In experiments on macrophage cultures, it has been shown that combined use reduces COX-2 expression and PGE₂ production more pronouncedly than each component individually. The potentiation mechanism is associated with the cumulative inhibition of the NF-κB transcriptional cascade and activation of heme oxygenase-1 (HO-1), which leads to pronounced suppression of the pro-inflammatory response and stabilization of cellular antioxidant defense.

Studies of synergy with Curcuma longa demonstrate additive suppression of TNF-α, IL-6 levels, and iNOS activity. The combination of curcuminoids with polyphenols of Barleria lupulina contributes to deeper inhibition of free radical processes and prevention of lipid peroxidation. This effect is realized at the cellular level through activation of the Nrf2/ARE pathway and increased activity of endogenous antioxidant enzymes.

Combined use with Centella asiatica has a modulating effect on the proliferation and migration of skin fibroblasts, which is associated with a synergistic effect on the expression of TGF-β and VEGF. The plants complement each other in restoring the skin barrier and regulating angiogenesis under conditions of tissue damage. The proposed mechanism is based on parallel stimulation of the PI3K/Akt signaling pathway, responsible for cell survival and repair.

Individual studies demonstrate an enhancement of the immunomodulating effect when combining Barleria lupulina with Tinospora cordifolia. In a model of induced immune dysfunction in laboratory animals, the combination causes an increase in phagocytic activity, an increase in immunoglobulin titers, and an increase in the number of T-lymphocytes. The effect is due to the coordinated action on JAK/STAT signaling cascades and stimulation of antigen-presenting cells.

Of interest is also the interaction with pentacyclic adaptogens containing saponins (for example, Panax notoginseng), where potentiation of antinociceptive and vasculoprotective effects is observed. The mechanisms of this synergy are associated with the simultaneous effect on GABA_A receptors and calcium channels, which leads to stabilization of the neurovascular response.

Thus, Barleria lupulina exhibits pronounced synergist properties when combined with other biologically active plant extracts. The most pronounced effects are realized within the framework of inflammatory, antioxidant, and immune cascades, while the nature of the interaction is predominantly potentiating or modulating, covering both systemic and tissue-specific levels of the pharmacological response.

References:
https://bmccomplementmedtherap...
https://www.sciencedirect.com/...
https://www.ncbi.nlm.nih.gov/p...
https://he01.tci-thaijo.org/in...
https://link.springer.com/arti...

Geography of Use and Traditional Medicine — Barleria lupulina

Barleria lupulina is traditionally used in the folk medicine of South and Southeast Asia, primarily in Thailand, Laos, Cambodia, Vietnam, and India. The plant is most actively used in the system of Thai traditional medicine (Mora-Thai), where it is known as "ฟ้าประทานพร" and is included in phytoremedies used in the form of pastes, infusions, and decoctions. In Thai healing practice, the leaves were crushed and applied to inflamed skin areas, and were also used in compresses and decoctions. Use covered both external and internal methods.

In the village medicine of the northern and northeastern regions of Thailand, Barleria lupulina was considered a "hot" plant and was included in steam baths and wraps used after childbirth, as well as after physical overwork. The leaves were added to heating compresses (luk pra kob) — special herbal compresses heated with steam. This plant was also used in herbal mixtures for cleansing the body and improving the circulation of vital energy ("lom").

In Indian tradition, the plant is known as Katu Nila or Hop Barleria. In Ayurvedic village schools of South India, it was used externally in the form of powders, crushed leaves, and juices. In the folklore of the southern states, the plant was considered to protect the home from evil and was planted near dwellings. Local practitioners also used it for washing and ritual cleansing of the skin, believing that it "removes fire" and "pacifies the flesh."

In Laos and Cambodia, Barleria lupulina was known among the Khmer peoples and was used in healing formulations for women — as part of postpartum care, as well as a remedy in steam baths. Decoctions and infusions of the leaves were among the remedies used for the so-called "dispelling of bad winds" — energy blocks in the body according to the traditional concept.

In the culture of the Mon people east of Myanmar, Barleria lupulina leaves were burned and used as a cleansing smoking plant in household rituals. In these traditions, the plant was attributed the ability to expel "cold spirits" from the home and restore harmony between the body and the earth. It was considered a plant with a masculine solar nature, "opening the flesh to the light."

Historical references are found in local handwritten herbal books of the late Ayutthaya period (18th century), as well as in oral traditions of healers in northern Thailand. It is believed that the plant was used in combination with other bitter and fiery herbs in rituals of expelling diseases associated with an imbalance between bodily heat and external humidity. Mentions of Barleria lupulina are found in medical manuscripts from the Isan region, where it is classified as a herb "against cold" and "for expelling mucus."

Barleria also had symbolic meaning: in some villages, leaves were hung at the entrance to the house as a sign of purification, and dried branches were used in protective wreaths attached over children's cradles. In some regions of Laos and Vietnam, the plant was used in funeral ceremonies — its juice was applied to the body to "calm the spirit" and purify the path to the other world.