Betulin is a naturally occurring lupin-type pentacyclic triterpenoid compound, primarily derived from the cork layer of the bark of the birch (Betula spp.), where it can comprise up to approximately 22%. In recent years, numerous in vitro, in vivo, and preclinical studies have demonstrated that betulin possesses multiple pharmacological activities, including anti-inflammatory, antioxidant, neuroprotective, cardiovascular protective, metabolic regulating, antibacterial, antiviral, and wound-healing promoting effects.
As a manufacturer of Betulinic acid powder, we are committed to providing high-purity, high-quality betulin raw materials to the global pharmaceutical, health supplement, and cosmetic industries. Please contact our professional team at sales@kintaibio.com.
Betulinic Acid for Potent Anti-inflammatory and Antioxidant Properties
White Birch Bark Extract Betulinic acid enhances the body's antioxidant defense by activating the Nrf2 signaling pathway, significantly upregulating Nrf2-targeted antioxidant and detoxification enzymes (including NQO1, HO-1, GCLC, and GCLM).
In LPS-stimulated macrophages, betulinic acid activates Nrf2 in a pathway-dependent manner (AMPK/AKT/GSK3β), inhibiting the production of inflammatory mediators such as iNOS and COX-2, and blocking the MAPK inflammatory signaling pathway.
Betulinic acid exhibits significant anti-inflammatory activity in in vitro anti-inflammatory evaluations, with IC₅₀ values of 51.27 and 62.10 µg/ml in the protein denaturation inhibition assay and the HRBC membrane stabilization assay, respectively.
This dual anti-inflammatory and antioxidant mechanism is the molecular basis for the multiple health benefits of betulinic acid, making it a promising candidate for intervention in chronic inflammation-related diseases.
Betulinic Acid for Neuroprotection
The pathological mechanisms of central nervous system diseases (such as Alzheimer's disease, Parkinson's disease, and multiple sclerosis) involve oxidative stress, inflammation, and protein misfolding.
Studies have shown that betulinic acid exhibits significant neuroprotective effects in H₂O₂-induced oxidative stress models: it can enhance cell viability, reduce reactive oxygen species (ROS) levels, and decrease apoptosis.
White Birch Bark Extract Betulinic acid can alleviate formaldehyde-induced Tau protein hyperphosphorylation and ROS levels by regulating the PI3K/AKT signaling pathway, thus improving AD-like pathological changes.
In a mouse model of post-stroke cognitive impairment (PSCI), betulinic acid improved cognitive performance, reduced microglia activation, and alleviated neuroinflammation by inhibiting the EGFR/JAK2/STAT3 pathway, significantly decreasing TNF-α, IL-1β, and IL-6 levels.
Betulinic acid can cross the blood-brain barrier and exert neuroprotective effects by regulating dopaminergic signaling, improving cognitive function, and reducing neuroinflammation and oxidative stress.
Betulinic Acid for Cardiovascular Protection
Betulinic acid exhibits potent cardioprotective activity against isoproterenol-induced myocardial injury, reducing infarct size, lowering myocardial enzyme levels, and maintaining hemodynamic function.
Its cardioprotective effect is achieved synergistically through three pathways: anti-inflammatory, anti-apoptotic, and antioxidant.
Betulinic acid also exerts its cardiovascular protective effects through multiple signaling pathways, including NRF2, NF-κB, MAPK, and NFAT, exhibiting antioxidant, anti-inflammatory, anti-apoptotic, and anti-proliferative effects, and enhancing endothelial function through nitric oxide signaling.
Furthermore, betulinic acid reduces lipid accumulation, showing potential interventional value for cardiovascular metabolic diseases such as atherosclerosis.
Betulinic Acid for Metabolic Regulation
In obesity-related studies, betulinic acid demonstrated significant preventive and therapeutic effects in a high-fat diet-induced obese rat model.
Betulinic acid can improve blood lipid and blood glucose profiles, reduce leptin levels, and increase adiponectin levels.
Its mechanism of action involves regulating the expression of genes related to lipid synthesis and degradation, including downregulating lipid synthesis genes such as ACLY, ACC, FAS, SCD1, SREBP-1c, and HMG-CoA reductase, while upregulating PPARγ.
Betulinic acid can also exert energy homeostasis and inflammation regulation by modulating aryl hydrocarbon receptors (AHRs).
In a metabolic syndrome model, betulinic acid (and its derivative betulinic acid) can improve insulin sensitivity, hyperglycemia, inflammation, and oxidative stress.
Betulinic Acid for Promoting wound healing
White Birch Bark Extract Betulinic acid is the first herbal active ingredient approved by the European Medicines Agency for wound treatment-in January 2016, betulinic acid-containing triterpenoid oleogel (Episalvan®) was approved in China and Europe for accelerating the healing of partial dermal wounds.
Clinical studies, using a self-controlled design comparing skin graft donor wounds and burn wounds from the same patient, have demonstrated the clinical efficacy of betulinic acid in accelerating wound healing.
The mechanism of action of betulinic acid covers all three stages of wound healing-the inflammatory phase, the migration phase, and the differentiation phase: after temporary stimulation of the inflammatory phase, keratinocytes migrate to the wound more rapidly, ultimately stimulating epidermal differentiation.
Preclinical and clinical studies have also confirmed the antibacterial and anti-inflammatory effects of betulinic acid, showing positive efficacy in the treatment of wounds from rare diseases such as epidermolysis bullosa.
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