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Betulinic Acid — Structure, Health Benefits, Supplements, & Food Sources

Article author photo Ani Harutyunyan by Ani Harutyunyan | Last updated on June 19, 2024
Medically reviewed by Elen Khachatrian Article author photo Elen Khachatrian

Betulinic Acid — Structure, Health Benefits, Supplements, & Food Sources


Betulinic acid, a naturally occurring pentacyclic triterpenoid phytochemical, is present in the bark of many different species of plants, especially those in the Betulaceae family, which includes birch trees. This bioactive compound has various therapeutic qualities, such as its anti-inflammatoryanti-malarialanti-HIV, and anticancer effects.

 Betulinic acid has shown promise as a cancer treatment since it may cause apoptosis in various cancer cell lines without damaging healthy cells. This has piqued the curiosity of researchers. Because of its selectivity, betulinic acid is a good target for creating new pharmacological medicines due to its natural abundance and comparatively low toxicity.

Betulinic Acid Structure

Betulinic acid is distinguished by its complex molecular structure, consisting of multiple functional groups and five fused rings, all supporting the compound's biological activity. Its chemical formula is C30H48O3: its C-3 and C-28 positions are occupied by hydroxyl and carboxyl groups, respectively (1). The solubility and interaction of the substance with different biological targets rely heavily on these functional groups. Because of its big, non-polar structure, betulinic acid is relatively hydrophobic, which affects its distribution and absorption within the body. Its normal form is a white powder with crystals with a melting point between 307 and 310°C. Because of its structure, the chemical can interact with lipid bilayers and integrate into cell membranes.Betulinic Acid Structure

Absorption and Metabolism

Betulinic acid is metabolized by hepatic enzymes in the liver, passing through several metabolic changes in the human body. After it is consumed or given, it is absorbed into the bloodstream and delivered to the liver, where Phase I and Phase II metabolic processes occur (2).

During Phase I metabolism, betulinic acid undergoes oxidation, reduction, and hydrolysis reactions, which are aided by cytochrome P450 enzymes. These processes increase the compound's polarity and introduce or reveal functional groups like hydroxyl groups. One typical alteration that improves betulinic acid's solubility is hydroxylation.

Following phase I, betulinic acid metabolites undergo phase II metabolism, conjugating with endogenous molecules such as glucuronic acid, sulfate, or glycine. This conjugation process, catalyzed by enzymes like UDP-glucuronosyltransferases, results in the formation of more water-soluble derivatives, which are easier to excrete.

The resultant metabolites are excreted from the body primarily through urine and, to a lesser extent, bile. This metabolic pathway ensures that betulinic acid and its metabolites do not accumulate to toxic levels in the body. 

Betulinic Acid Food Sources

The bark of the white birch tree (106mg) is by far the most notable source of betulinic acid among meals (3). 

Some fruits and vegetables, including pears (2.59mg), apples (4.4mg), and plums, contain lesser levels of betulinic acid (4) (5). These fruits are beneficial to health since they contain this bioactive component in addition to necessary minerals. 

Betulinic acid is another compound found in some medicinal herbs, such as thyme and rosemary (1 mg), which increases their potential for therapeutic use (6).

Betulinic Acid Supplements

Currently, betulinic acid consumption is not governed by formal guidelines or dietary recommendations. 

Since this molecule is uncommon in the diet, it is investigated more in the context of medicinal research than nutrition. Rather than coming from dietary sources, betulinic acid is used in concentrated forms like extracts or isolated compounds in most studies on the topic (7).

If betulinic acid is being evaluated as a supplement or therapeutic agent, it is essential to consult medical specialists to establish a safe dosage based on a patient's specific medical condition and the most recent data from scientific studies. It is not advised to self-medicate or take large amounts of betulinic acid unsupervised because there are no established rules, and there could be side effects.

Betulinic Acid Health Benefits 


Significant anti-inflammatory effects of betulinic acid are demonstrated in a number of ways. Its principal mechanism of action involves inhibiting nuclear factor-kappa B (NF-κB), a protein complex that is essential for controlling the immune system's reaction to inflammation. Tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6) are two examples of pro-inflammatory mediators and cytokines that are produced less when betulinic acid inhibits NF-κB (8). Moreover, betulinic acid prevents the signaling pathways that cause inflammation by blocking the activation of mitogen-activated protein kinases (MAPKs). Moreover, it lowers the expression of the enzyme cyclooxygenase-2 (COX-2), which is in charge of producing prostaglandins that promote inflammation. Moreover, betulinic acid's antioxidant qualities lower oxidative stress, which frequently plays a role in the development of chronic inflammation.


One of the main ways that betulinic acid works is by activating apoptosis, which is a type of controlled cell death that kills cancer cells without damaging the healthy tissue around them. By altering the mitochondrial membrane potential, betulinic acid triggers intrinsic apoptotic pathways. This results in the release of cytochrome C and the activation of caspases, two essential proteins in the apoptosis cascade. Furthermore, betulinic acid inhibits the growth and multiplication of cancer cells, exhibiting anti-proliferative effects. It interferes with multiple signaling pathways, such as the MAPK and NF-κB pathways, which are important for inflammation, cell survival, and proliferation. Additionally, betulinic acid possesses anti-angiogenic qualities. It may stop new blood vessels from growing, which is necessary for tumors to grow and metastasize. It deprives cancers of vital nutrition and oxygen by inhibiting angiogenesis (9). 

It has been discovered that betulinic acid is very effective in the treatment of melanoma because it selectively promotes apoptosis in cancer cells while keeping healthy cells (10). Furthermore, inducing pathways leading to cell death has demonstrated promise in treating neuroblastoma, a kind of cancer originating from nerve tissues (11). 

Betulinic acid has shown promise in preventing cell division and metastasis in prostate cancer. Research has also shown that it can prevent breast cancer by causing apoptosis and inhibiting the cancer cell cycle (12). 

Moreover, betulinic acid is a broad-spectrum anticancer drug since it acts against lung and colon tumors (13) (14). 


Betulinic acid has drawn interest due to its possible antimalarial effects. These qualities work through a variety of mechanisms. Betulinic acid exhibits potential as a versatile antimalarial drug due to its ability to impact several stages of the parasite life cycle, such as the liver and blood stages (15). The parasite's ability to produce energy and survive depends on the potential of its mitochondrial membrane, which is disrupted by one of its main mechanisms. The depolarization of this membrane brought on by betulinic acid causes a drop in ATP synthesiscellular stress, and the Plasmodium parasite's programmed cell death, or apoptosis. Its selective toxicity further enhances the compound's therapeutic potential, which targets the parasite while sparing the host cells.

Anti-HIV Properties

Betulinic acid, a compound found in nature, and its modified versions are showing a lot of promise in fighting HIV. These derivatives block critical steps in the virus's life cycle: they inhibit the virus's protease enzyme, prevent it from entering host cells, and stop it from replicating (16). One standout derivative, Bevirimat (PA-457), prevents the virus from maturing properly, making it non-infectious, and has shown good results in clinical trials (17). Other derivatives, like RPR103611 and IC9564, also demonstrate strong anti-HIV activity through various mechanisms. These modified versions of betulinic acid are designed to be more effectiveeasier for the body to absorb, and less toxic (18). However, there's always a risk of the virus developing resistance, and researchers need to fine-tune how these drugs work in the body. Despite these challenges, betulinic acid derivatives are a promising area of research in the quest to treat HIV effectively.


terpenoid found in plants, betulinic acid is distinguished by a complicated molecular structure with five fused rings and numerous functional groups, all supporting the compound's biological activity. White birch bark contains the highest concentration of betulinic acid, with smaller amounts also present in pears, apples, and rosemary, among other fruits and herbs. Its anti-inflammatory and anti-cancer qualities, as well as its ability to suppress tumor angiogenesis and induce apoptosis in cancer cells, make it a noteworthy health benefit. Furthermore, by preventing the growth of the virus and the activity of protease enzymes, betulinic acid derivatives have demonstrated promise in the fight against HIV

Although betulinic acid has therapeutic promise, acceptable dosage guidelines have not yet been developed, emphasizing the necessity of physician supervision when using this medication.

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