Ursolic acid: Benefits, Dosage, Contraindications

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Ursolic acid is an organic compound present in a wide variety of plants and fruits, such as apple and grape skins, rosemary, sage, peppermint, and holy basil (also known as 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 possess multiple biological activities, including anticancer, anti-diabetic, hepatoprotective, and anti-inflammatory effects. Research on ursolic acid remains preliminary, but it could prevent muscle weakness and dystrophy. It encourages the development and growth of skeletal muscle cells, thus exhibiting an anabolic effect. Under these conditions, ursolic acid can combat muscle capacity reduction linked to aging or promote muscle strength gains in athletes. Ursolic acid has also demonstrated interesting anti-inflammatory and anticancer properties, observed in vitro and in vivo. Ursolic acid has shown effects on glioma tumors, liver cancer cells, bladder cancer cells, melanoma, and prostate cancer cells in vivo (in mice). However, ursolic acid has very low oral bioavailability in humans. It is poorly soluble in water, which limits its current use despite its significant pharmacological potential.

Other name(s) 

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Scientific name(s)

UA

Family or group: 

Phytosubstances


Indications

Rating methodology

EFSA approval.

Several clinical trials (> 2) randomized controlled with double blind, including a significant number of patients (>100) with consistently positive outcomes for the indication.
Several clinical trials (> 2) randomized controlled with double blind, and including a significant number of patients (>100) with positive outcomes for the indication.
One or more randomized studies or multiple cohorts or epidemiological studies with positive outcomes for the indication.
Clinical studies exist but are uncontrolled, with conclusions that may be positive or contradictory.
Lack of clinical studies to date that can demonstrate the indication.


Sport performance
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An increase in IRSINE levels, thought to be involved in the physiology of skeletal muscles, was observed in a clinical study among athletes to measure muscle strength following ursolic acid supplementation. In a clinical study, combining ursolic acid supplementation (450 mg/day) with resistance training over 8 weeks increased muscle strength and IGF-1 (insulin-like growth factor) levels compared to training alone, although the authors did not observe significant gains in lean body mass, meaning the body's mass without fat.

Posologie

posologieOrally

posologie450 mg

populationAdults

formulationdry extract


Muscle Dystrophy
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Research has proven that ursolic acid could be a therapeutic intervention against muscle atrophy and dysfunction induced by aging. It also significantly improved skeletal muscle mass and grip strength in rodents. A similar study revealed that ursolic acid increased satellite cell numbers and activated myoglobin expression in aged mice, suggesting it positively altered skeletal muscle rejuvenation by stimulating protein synthesis and suppressing atrophy factors. Other studies reported that ursolic acid improved skeletal muscle atrophy by inhibiting pathways associated with muscle atrophy. These include the muscle protein 1 (MuRF-1) and atrogin-1 pathways, two essential mediators of protein degradation in skeletal muscles. It was also shown that ursolic acid increased skeletal muscle hypertrophy by increasing insulin-like growth factor 1 (IGF-1) secretion. Finally, it was demonstrated that a 12-week treatment with ursolic acid improves skeletal muscle strength and mass in a dose-dependent manner via upregulation of the Akt/mammalian target of rapamycin (mTOR) signaling pathway and downregulation of skeletal muscle atrophy parameters, such as Atrogin-1 and MuRF-1.

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 seems to attenuate the increase in triglycerides in response to a fatty meal, presumed to occur by inhibiting pancreatic lipase. An equivalent dosage in humans is estimated at 160 mg/kg.

Posologie

posologieOrally

posologie160 mg

duration12 - weeks

populationAdults

formulationdry extract


Properties


Metabolic

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In an in-vivo study, ursolic acid was reported to reduce adipocyte growth while stimulating fat burning. Researchers observed that it increases energy consumption (thermogenesis) by promoting the growth of brown adipose tissue and inhibiting white adipose tissue growth. Therefore, dietary supplementation with ursolic acid appears capable of inhibiting body weight gain in the mice studied. However, further research is needed to confirm this hypothesis.

Usages associés

Muscle dystrophy, Weight control

Anticancer

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Ursolic acid exerts most of its anticancer effects through apoptosis regulation, leading to reduced proliferation and angiogenesis, thus preventing tumor formation and metastases.


Anti-inflammatory

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


Safety dosage

Adult from 18 years old: 150 mg - 450 mg