Ursolic acid: benefits, dosage, contraindications

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Ursolic acid is an organic compound found in a wide variety of plants and fruits, such as the skins of apples and grapes, rosemary, sage, peppermint, and holy basil (also called Tulsi). It is a pentacyclic terpenoid, an important class of organic compounds. Pentacyclic triterpenoids are intermediates in the biosynthesis of steroid hormones in plants. They exhibit several biological activities, including anticancer, antidiabetic, hepatoprotective, and anti-inflammatory effects. Research on ursolic acid remains preliminary, but it may prevent muscle weakness and dystrophy. It stimulates the development and growth of skeletal muscle cells, hence its anabolic effect. Under these conditions, ursolic acid may help counteract age-related declines in muscle function and promote gains in muscle strength among athletes. Ursolic acid has also shown promising anti-inflammatory and anticancer properties, observed in vitro and in vivo. Ursolic acid demonstrated in vivo (in mice) effects on glioma tumors, liver cancer cells, bladder cancer cells, melanoma, and prostate cancer cells. However, ursolic acid has very low oral bioavailability in humans. Indeed, ursolic acid is poorly soluble in water. These properties currently limit its use, despite its significant pharmacological potential.

Scientific name(s)

UA

Family or group: 

Phytochemicals


Indications

Scoring methodology

EFSA approval.

Several randomized, double-blind, controlled clinical trials (> 2), including a significant number of patients (>100), with consistently positive conclusions for the indication.
Several randomized, double-blind, controlled clinical trials (> 2), including a significant number of patients (>100), with positive conclusions for the indication.
One or more randomized studies, or several cohorts or epidemiological studies, with positive conclusions for the indication.
Clinical studies exist but are uncontrolled, with conclusions that may be positive or conflicting.
No clinical studies to date that can demonstrate the indication.


Sports performance
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An increase in IRSINE levels, which is thought to be involved in the physiology of skeletal muscles, was observed in a clinical study conducted in athletes to measure muscle strength following ursolic acid supplementation. In a clinical trial, the combination of ursolic acid supplementation (450 mg/day) with resistance training for a period of 8 weeks increased muscle strength and levels of IGF-1 (insulin-like growth factor) compared with training alone, although the authors did not observe significant gains in lean body mass, i.e., body mass without fat.

Posologie

posologieOral

posologie450 mg

populationAdults

formulationdry extract


Muscular dystrophy
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Research has shown that ursolic acid could serve as a therapeutic intervention against age-related muscle atrophy and dysfunction. Studies have also demonstrated that it substantially improved skeletal muscle mass and grip strength in rodents. rnrnA similar study found that ursolic acid increased the number of satellite cells and activated myoglobin expression in aged mice, suggesting that it positively altered skeletal muscle renewal by stimulating protein synthesis and suppressing atrophy factors. rnrnOther studies have reported that ursolic acid ameliorated skeletal muscle atrophy by inhibiting pathways associated with muscle wasting. These include the MuRF-1 and atrogin-1 pathways, two key mediators of protein degradation in skeletal muscles.rnrnIt has also been shown that ursolic acid increased skeletal muscle hypertrophy by enhancing secretion of insulin-like growth factor 1 (IGF-1).rnrnFinally, it was shown that a 12-week treatment with ursolic acid improved skeletal muscle strength and mass in a dose-dependent manner via upregulation of Akt/mammalian target of rapamycin (mTOR) signaling and downregulation of skeletal muscle atrophy markers such as Atrogin-1 and MuRF-1.rnrn

Posologie

posologieOrally

posologie400 mg

duration7 - days

populationSeniors

formulationdry extract


Weight control
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According to a study, ursolic acid at 100 mg/kg in rats appears to attenuate the increase in triglycerides in response to a fatty meal, which is thought to occur through inhibition of pancreatic lipase. An equivalent human dose is estimated at 160 mg/kg.

Posologie

posologieOral

posologie160 mg

duration12 weeks

populationAdults

formulationdry extract


Properties


Metabolic

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In an in vivo study, it was reported that ursolic acid reduces adipocyte growth while stimulating fat burning. In fact, researchers showed that ursolic acid increases energy expenditure (thermogenesis) by stimulating the growth of brown adipose tissue while inhibiting the growth of white adipose tissue. Thus, researchers found that dietary supplementation with ursolic acid was able to inhibit body weight gain in the mice studied. However, further research is still needed to confirm this hypothesis.

Usages associés

Muscular dystrophy, Weight control

Anticancer

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Ursolic acid exerts most of its anticancer effects by regulating apoptosis-related factors, which leads to reduced proliferation and angiogenesis, thereby preventing the formation of cancerous tumors and metastases.


Anti-inflammatory

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Ursolic acid has an anti-inflammatory effect by inhibiting 5-lipoxygenase and COX-2.


Safe dosage

Adults aged 18 or older: 150 mg - 450 mg