Compound Monograph
Ursolic acid
Ursolic acid is a pentacyclic triterpenoid (ursane-type) concentrated in the waxy cuticle of apple peel and in culinary Lamiaceae herbs like rosemary and sage. Its marquee signal is skeletal-muscle preservation, discovered through a muscle-atrophy gene-signature screen, but it is a poorly water-soluble BCS-IV molecule with very low oral bioavailability and a plasma half-life under an hour, so every finding must be read against how little of it reaches the blood.
Classification
Ursolic acid is a pentacyclic triterpenoid (ursane), part of the terpenoids class. The largest class of plant compounds, built from five-carbon isoprene units — the essential-oil aromatics, resins, bitter principles, saponins, and plant sterols.
Where Does It Come From? (20)
Ursolic acid is a naturally occurring pentacyclic triterpenoid (ursane), found in Rosemary, Bearberry, Hawthorn and 17 other sources. It is well tolerated orally (low toxicity).
Content by Source (6)
Reported concentrations across the plants that contain ursolic acid — the bar marks the typical level, the line shows the reported range. These are literature figures for varying plant parts and preparations, so read them as a comparative guide, not exact assays.
Pharmacology & Research
Ursolic acid is a pentacyclic triterpenoid of the ursane class — the waxy, lipophilic acid that waterproofs the cuticle of apple peel and accumulates in the leaves of rosemary, sage, thyme, bearberry, holy basil, lemon balm, catnip and many other plants in this database. It carries one of the broadest preclinical literatures of any single triterpene: isolated ursolic acid shows skeletal-muscle-preserving, anti-inflammatory, anticancer, metabolic and GABAergic activity across cell and rodent models 7,12Reference 7In vitroPotent anti-inflammatory activity of ursolic acid, a triterpenoid antioxidant, is mediated through suppression of NF-κB, AP-1 and NF-AT — in vitro / ex vivoView study →Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →. Two facts frame all of it. First, almost every result is preclinical or in vitro — the isolated-molecule human data are limited to a few small, mixed muscle pilots. Second, and more decisive, ursolic acid is a poorly water-soluble BCS class IV compound: oral bioavailability is very low, plasma half-life is under an hour, and it is a substrate for efflux and CYP metabolism 11,12Reference 11Clinical trialA phase I pharmacokinetic study of ursolic acid nanoliposomes in healthy volunteers and patients with advanced solid tumors — phase I clinical trialView study →Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →. Concentrations that work in a dish are not trivially reached from an oral dose, so the potency seen in vitro should be read with heavy discount. Within the source herbs it is usually a supporting constituent in a matrix — hawthorn’s own literature notes that isolated triterpene acids show little of the whole extract’s cardiovascular effect 10Reference 10Comparative study of the cardiovascular activity of shoots, leaves and flowers of Crataegus oxyacantha: 2.
- Best-characterised (preclinical): skeletal-muscle preservation — isolated ursolic acid reduced muscle atrophy and drove hypertrophy in mice by enhancing insulin/IGF-I–Akt signalling, the finding that launched the modern literature 1,2Reference 1AnimalmRNA expression signatures of human skeletal muscle atrophy identify a natural compound that increases muscle mass — Connectivity Map screen + mouse in vivoView study →Reference 2AnimalUrsolic acid increases skeletal muscle and brown fat and decreases diet-induced obesity, glucose intolerance and fatty liver disease — mouse in vivo animal modelView study →.
- Human data, mixed and thin: small supplementation pilots — one reduced markers of muscle damage during resistance training 3Reference 3RCTUrsolic acid supplementation decreases markers of skeletal muscle damage during resistance training in resistance-trained men — randomised pilot trial (450 mg/day, 8 weeks)View study →, but a controlled trial found no added strength or mass benefit 4Reference 4RCTUrsolic acid has no additional effect on muscle strength and mass in active men undergoing a high-protein diet and resistance training — double-blind placebo-controlled trialView study → and a ursolic-acid–standardised loquat-leaf trial found none either 5Reference 5RCTEffect of loquat leaf extract on muscle strength, muscle mass, and muscle function in healthy adults — randomised, double-blind, placebo-controlled trial (~51 mg ursolic acid/day)View study →.
- Mechanistically resolved but preclinical: potent anti-inflammatory/immunomodulatory activity via suppression of NF-κB, AP-1 and NF-AT 7Reference 7In vitroPotent anti-inflammatory activity of ursolic acid, a triterpenoid antioxidant, is mediated through suppression of NF-κB, AP-1 and NF-AT — in vitro / ex vivoView study →; broad anticancer activity across cultured tumour lines 12Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →; anti-obesity/metabolic effects in mice 2Reference 2AnimalUrsolic acid increases skeletal muscle and brown fat and decreases diet-induced obesity, glucose intolerance and fatty liver disease — mouse in vivo animal modelView study →.
- The caveat: very low oral bioavailability and a sub-hour half-life; no large isolated-molecule human trial; several source-herb roles are whole-plant, not molecule, results 10,11Reference 10Comparative study of the cardiovascular activity of shoots, leaves and flowers of Crataegus oxyacantha: 2Reference 11Clinical trialA phase I pharmacokinetic study of ursolic acid nanoliposomes in healthy volunteers and patients with advanced solid tumors — phase I clinical trialView study →.
1. Skeletal muscle & atrophy
The signal that made ursolic acid famous. Querying the Connectivity Map with an mRNA signature of human muscle atrophy (from fasting and spinal-cord-injury muscle) singled out isolated ursolic acid as a compound whose transcriptional effect was the opposite of atrophy; in mice it then reduced fasting-induced atrophy and drove hypertrophy, increasing fibre size, grip strength and exercise capacity by enhancing insulin/IGF-I–Akt signalling and suppressing atrophy-associated genes (atrogin-1, MuRF1) 1Reference 1AnimalmRNA expression signatures of human skeletal muscle atrophy identify a natural compound that increases muscle mass — Connectivity Map screen + mouse in vivoView study →. Human translation is much weaker. An 8-week pilot in resistance-trained men (450 mg/day isolated ursolic acid + training) lowered circulating markers of muscle damage (CK, CK-MB, LDH) versus training alone 3Reference 3RCTUrsolic acid supplementation decreases markers of skeletal muscle damage during resistance training in resistance-trained men — randomised pilot trial (450 mg/day, 8 weeks)View study →, but a double-blind controlled trial in active men on a high-protein diet found no additional strength or lean-mass benefit 4Reference 4RCTUrsolic acid has no additional effect on muscle strength and mass in active men undergoing a high-protein diet and resistance training — double-blind placebo-controlled trialView study →, and a randomised trial of a ursolic-acid–standardised loquat-leaf extract (~51 mg UA/day, 12 weeks) found no change in muscle strength, mass or function 5Reference 5RCTEffect of loquat leaf extract on muscle strength, muscle mass, and muscle function in healthy adults — randomised, double-blind, placebo-controlled trial (~51 mg ursolic acid/day)View study →.
Gap: the pivotal mechanism is mouse; the human trials are few, small and net-negative on the hard outcomes (strength, mass), and doses that reproduce the mouse effect are limited by poor oral bioavailability.
2. Anti-inflammatory & immune
One of the better-mechanised signals, and the thread that connects ursolic acid’s roles across the source herbs. Isolated ursolic acid inhibits activation, proliferation and cytokine secretion in T cells, B cells and macrophages, acting through suppression of the immunoregulatory transcription factors NF-κB, AP-1 and NF-AT and of upstream ERK/JNK phosphorylation 7Reference 7In vitroPotent anti-inflammatory activity of ursolic acid, a triterpenoid antioxidant, is mediated through suppression of NF-κB, AP-1 and NF-AT — in vitro / ex vivoView study →. This is the activity credited to ursolic acid within bearberry (NF-κB-linked anti-inflammatory contribution alongside arbutin) and to the triterpene fraction of yerba maté — where maté raised activity of the antioxidant enzyme paraoxonase-2 — and holy basil 6,7Reference 6In vitroYerba maté (Ilex paraguariensis) enhances the gene modulation and activity of paraoxonase-2 — in vitro and in vivo studies (whole-extract, ursolic acid among candidate actives)View study →Reference 7In vitroPotent anti-inflammatory activity of ursolic acid, a triterpenoid antioxidant, is mediated through suppression of NF-κB, AP-1 and NF-AT — in vitro / ex vivoView study →. In motherwort, isolated ursolic acid also reduced Staphylococcus aureus adhesion and superoxide production, an anti-virulence rather than bactericidal effect 15Reference 15In vitroLeonurus cardiaca L. herb — a derived extract and ursolic acid as factors affecting the adhesion capacity of Staphylococcus aureus in the context of infective endocarditis — in vitroView study →.
Gap: the mechanism is resolved but the evidence is in-vitro/ex-vivo; there is no controlled human anti-inflammatory trial of the isolated molecule, and systemic exposure is capped by bioavailability.
3. Anticancer
The broadest but thinnest signal. Isolated ursolic acid induces apoptosis and cell-cycle arrest and suppresses proliferation, angiogenesis and metastasis across many cultured tumour lines, acting on MAPK, PI3K/Akt/mTOR, STAT3, EGFR and NF-κB signalling while upregulating p53 and p21 12Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →. This antiproliferative activity is why apple-peel ursolic acid is repeatedly flagged as a chemopreventive candidate, and it underlies the chemopreventive attribution in rosemary 12Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →.
Gap: almost entirely in vitro at high micromolar concentrations the poor oral bioavailability makes hard to reach systemically; in-vivo tumour work is sparser and there are no efficacy trials in cancer patients — only an early-phase nanoliposome PK/safety study 11Reference 11Clinical trialA phase I pharmacokinetic study of ursolic acid nanoliposomes in healthy volunteers and patients with advanced solid tumors — phase I clinical trialView study →.
4. Metabolic (glucose, obesity, lipids)
Tied to the muscle work. In the same programme, isolated ursolic acid fed to mice on a high-fat diet increased skeletal muscle and brown fat, and decreased diet-induced obesity, glucose intolerance and fatty-liver disease 2Reference 2AnimalUrsolic acid increases skeletal muscle and brown fat and decreases diet-induced obesity, glucose intolerance and fatty liver disease — mouse in vivo animal modelView study →. Mechanistically this overlaps the muscle Akt/IGF-I axis plus increased energy expenditure via brown adipose tissue 2Reference 2AnimalUrsolic acid increases skeletal muscle and brown fat and decreases diet-induced obesity, glucose intolerance and fatty liver disease — mouse in vivo animal modelView study →.
Gap: the metabolic evidence is a single rodent programme; there is no isolated-ursolic-acid human metabolic trial, and the source-herb metabolic effects (e.g. maté’s lipid signals) are whole-plant, not molecule, results.
5. Anxiolytic (GABA-transaminase)
A mechanism-level signal from the lemon balm literature. Isolated ursolic acid — together with its co-occurring isomer oleanolic acid — inhibits GABA-transaminase in vitro, the enzyme that degrades GABA, a plausible route to a calming effect 8Reference 8In vitroBioassay-guided fractionation of lemon balm (Melissa officinalis L.) using an in vitro measure of GABA-transaminase activity — in vitroView study →. In a chronic mouse study a standardised lemon-balm extract reduced anxiety-like behaviour 9Reference 9AnimalEffects of chronic administration of Melissa officinalis L. extract on anxiety-like reactivity and on circadian and exploratory activities in mice — mouse modelView study →.
Gap: the GABA-T inhibition is in vitro and the behavioural data use the whole lemon-balm extract, in which rosmarinic acid is the dominant marker — the anxiolytic human trials on melissa cannot be attributed to ursolic acid, and its brain penetration at dietary intake is unquantified.
6. Cardiovascular
The oldest attribution, and the clearest illustration of the isolate-vs-plant problem. An early study of Crataegus oxyacantha (hawthorn) on the isolated rabbit heart attributed part of the coronary-dilating and positive-inotropic (heart-strengthening) activity to its crataegolic-, ursolic-acid and vitexin-2″-O-rhamnoside content 10Reference 10Comparative study of the cardiovascular activity of shoots, leaves and flowers of Crataegus oxyacantha: 2. Ursolic acid is one of the triterpene acids of hawthorn leaf and flower (total triterpene acids up to ~0.6%).
Gap: hawthorn’s own literature repeatedly finds that single isolated constituents show little of the whole extract’s cardiovascular effect — ursolic acid reads as a supporting member of a constituent matrix, not a stand-alone cardiotonic, and there is no isolated-molecule cardiovascular trial 10Reference 10Comparative study of the cardiovascular activity of shoots, leaves and flowers of Crataegus oxyacantha: 2.
Mechanisms
| Target / pathway | Effect | Relevant to |
|---|---|---|
| Insulin/IGF-I → Akt/mTOR | Activates → ↑protein synthesis, muscle hypertrophy | skeletal muscle, metabolic |
| Atrogin-1 / MuRF1 (atrophy genes) | Suppresses → ↓muscle protein breakdown | skeletal muscle |
| NF-κB, AP-1, NF-AT | Suppresses → ↓cytokines, immune-cell activation | anti-inflammatory, anticancer |
| STAT3, EGFR, MAPK, PI3K/Akt | Modulates → apoptosis, ↓proliferation/angiogenesis | anticancer |
| Brown adipose tissue / energy expenditure | Increases → ↓diet-induced obesity | metabolic |
| GABA-transaminase | Inhibits (in vitro) → ↑GABA | anxiolytic |
Pharmacokinetics
Bioavailability is the load-bearing caveat for the whole ursolic-acid literature. It is a highly lipophilic, poorly water-soluble pentacyclic triterpene — a BCS class IV molecule (low solubility and low permeability) — so its oral bioavailability as the pure compound is very low, the result of poor dissolution, extensive pre-systemic metabolism (including by CYP3A4) and efflux 11,12Reference 11Clinical trialA phase I pharmacokinetic study of ursolic acid nanoliposomes in healthy volunteers and patients with advanced solid tumors — phase I clinical trialView study →Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →. In rodents it is absorbed quickly (Tmax ~30 min) but cleared quickly too, with a plasma half-life under about an hour 12Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →. The one human pharmacokinetic study used a nanoliposome formulation given intravenously to healthy volunteers and cancer patients precisely because plain oral ursolic acid does not achieve useful plasma levels; exposure rose roughly dose-proportionally and the formulation was tolerated up to defined limits 11Reference 11Clinical trialA phase I pharmacokinetic study of ursolic acid nanoliposomes in healthy volunteers and patients with advanced solid tumors — phase I clinical trialView study →. The practical upshot mirrors osthole and berberine: the potent in-vitro concentrations are not reachable from eating apple peel or taking an unformulated capsule, which tempers every downstream claim and is why the applied literature leans on nanoparticles, liposomes, phytosomes and bioenhancers (e.g. piperine) 11,12Reference 11Clinical trialA phase I pharmacokinetic study of ursolic acid nanoliposomes in healthy volunteers and patients with advanced solid tumors — phase I clinical trialView study →Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →.
Clinical trials
There is no large trial of isolated ursolic acid for any indication. The human evidence is three small supplementation studies in the muscle space — a positive pilot on damage markers 3Reference 3RCTUrsolic acid supplementation decreases markers of skeletal muscle damage during resistance training in resistance-trained men — randomised pilot trial (450 mg/day, 8 weeks)View study →, a negative controlled trial on strength/mass 4Reference 4RCTUrsolic acid has no additional effect on muscle strength and mass in active men undergoing a high-protein diet and resistance training — double-blind placebo-controlled trialView study →, and a negative loquat-leaf (UA-standardised) trial 5Reference 5RCTEffect of loquat leaf extract on muscle strength, muscle mass, and muscle function in healthy adults — randomised, double-blind, placebo-controlled trial (~51 mg ursolic acid/day)View study → — plus an early-phase nanoliposome pharmacokinetic/safety study in volunteers and cancer patients 11Reference 11Clinical trialA phase I pharmacokinetic study of ursolic acid nanoliposomes in healthy volunteers and patients with advanced solid tumors — phase I clinical trialView study →. Everything else is preclinical.
| Completed | Planned | Terminated | Preclinical |
|---|---|---|---|
| Few(small muscle pilots; phase-I PK) | Some(e.g. muscle/metabolic in special populations) | — | Extensive |
Last checked: July 2026.
Isolate vs. Plant Studies
Ursolic acid sits at both ends of the isolate-vs-plant spectrum. Its marquee muscle, metabolic, anti-inflammatory and anticancer findings all use the isolated molecule (or defined synthetic/nanoparticle preparations), so those describe the compound rather than a plant standing in for it 1,2,7,12Reference 1AnimalmRNA expression signatures of human skeletal muscle atrophy identify a natural compound that increases muscle mass — Connectivity Map screen + mouse in vivoView study →Reference 2AnimalUrsolic acid increases skeletal muscle and brown fat and decreases diet-induced obesity, glucose intolerance and fatty liver disease — mouse in vivo animal modelView study →Reference 7In vitroPotent anti-inflammatory activity of ursolic acid, a triterpenoid antioxidant, is mediated through suppression of NF-κB, AP-1 and NF-AT — in vitro / ex vivoView study →Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →. But almost all of that is preclinical, and the small human muscle trials are mixed-to-negative 3,4,5Reference 3RCTUrsolic acid supplementation decreases markers of skeletal muscle damage during resistance training in resistance-trained men — randomised pilot trial (450 mg/day, 8 weeks)View study →Reference 4RCTUrsolic acid has no additional effect on muscle strength and mass in active men undergoing a high-protein diet and resistance training — double-blind placebo-controlled trialView study →Reference 5RCTEffect of loquat leaf extract on muscle strength, muscle mass, and muscle function in healthy adults — randomised, double-blind, placebo-controlled trial (~51 mg ursolic acid/day)View study →. The source-herb roles run the other way: within hawthorn, bearberry, lemon balm and yerba maté, ursolic acid is a supporting triterpene in a matrix, and the human clinical effects of those herbs (hawthorn’s cardiotonic action, lemon balm’s anxiolysis) are whole-plant results that cannot be reassigned to ursolic acid — hawthorn’s literature explicitly finds isolated constituents underperform the whole extract 10Reference 10Comparative study of the cardiovascular activity of shoots, leaves and flowers of Crataegus oxyacantha: 2. Read the preclinical work as evidence for the molecule and the herb trials as evidence for the plants.
Prevalence in Nature
Ursolic acid is one of the most widely distributed plant triterpenoids, concentrated in the epicuticular wax of fruit peels and in the leaves and aerial parts of many families — most prominently the mint family (Lamiaceae) and the heath, rose, apple, myrtle and holly families 12,13Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →Reference 13Pentacyclic triterpene distribution in various plants — rich sources for a new group of multi-potent plant extracts — analytical surveyView study →. It occurs chiefly in surface tissue: fruit cuticle, leaf epidermis and flowers, rather than roots. By measured concentration the richest sources are culinary Lamiaceae leaves — rosemary at ~2.95% dry weight, sage ~1.8%, lavender ~1.6% and thyme ~0.9% — with bearberry leaf ~1.2% 13Reference 13Pentacyclic triterpene distribution in various plants — rich sources for a new group of multi-potent plant extracts — analytical surveyView study →. Apple peel, the compound’s iconic dietary source, is actually lower on a concentration basis (~0.33–0.58% of dry weight, i.e. ~3–6 mg/g), though because the peel of one medium apple holds roughly 40–50 mg it is a meaningful everyday exposure 14Reference 14Triterpene content in flesh and peel of apples grown on different rootstocks — analytical studyView study →. It co-occurs almost universally with its regioisomer oleanolic acid (oleanane skeleton) at lower levels, the two differing only in the position of one methyl group.
Biosynthetically it is a triterpenoid built from the universal C30 precursor 2,3-oxidosqualene: an oxidosqualene cyclase (α-amyrin synthase) folds the chain into the pentacyclic ursane skeleton α-amyrin, which cytochrome-P450 enzymes of the CYP716 family then oxidise stepwise at C-28 to the carboxylic acid, yielding ursolic acid (the parallel oleanane route gives oleanolic acid) 16Reference 16Functional characterization of CYP716 family P450 enzymes in triterpenoid biosynthesis in tomato — plant biochemistryView study →. It is essentially a plant product; there is no established endogenous animal source.
Discovery & Synthesis
Ursolic acid was identified in the epicuticular wax of apples in the 1920s, among the first triterpenoids characterised from a fruit cuticle; its name derives from this waxy origin, and it carries the older synonyms urson, prunol and malol (the last two reflecting early isolation from Prunus and Malus fruit) 12Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →. Its molecular formula is C₃₀H₄₈O₃ and its systematic name is 3β-hydroxyurs-12-en-28-oic acid. A practical, scalable total chemical synthesis is not well documented — the pentacyclic ursane skeleton is synthetically demanding, and there is no commercial synthetic route. Consequently ursolic acid is manufactured entirely by extraction from plant material: apple pomace (a cheap by-product of juice and cider pressing), rosemary and sage leaf, and Eriobotrya (loquat) leaf are the usual feedstocks, purified by solvent extraction and chromatography 13,14Reference 13Pentacyclic triterpene distribution in various plants — rich sources for a new group of multi-potent plant extracts — analytical surveyView study →Reference 14Triterpene content in flesh and peel of apples grown on different rootstocks — analytical studyView study →. Most of the medicinal-chemistry effort has gone not into synthesising the parent molecule but into semi-synthetic C-3/C-28 derivatives and into formulation (nanoparticles, liposomes) to overcome its poor bioavailability 11,12Reference 11Clinical trialA phase I pharmacokinetic study of ursolic acid nanoliposomes in healthy volunteers and patients with advanced solid tumors — phase I clinical trialView study →Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →.
Patents: not yet researched (future patent-loop pass).
Toxicity & Safety
Ursolic acid carries a low toxicity flag. It is a normal component of the human diet — present in the skins of apples and many fruits and in common culinary herbs — and reviews describe it as generally well tolerated in animal studies, with no signature acute organ toxicity at the doses used and a wide preclinical safety margin 12Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →. The small human muscle pilots reported no serious adverse events at 450 mg/day for 8–12 weeks 3,4Reference 3RCTUrsolic acid supplementation decreases markers of skeletal muscle damage during resistance training in resistance-trained men — randomised pilot trial (450 mg/day, 8 weeks)View study →Reference 4RCTUrsolic acid has no additional effect on muscle strength and mass in active men undergoing a high-protein diet and resistance training — double-blind placebo-controlled trialView study →. The main theoretical concern is metabolic: ursolic acid is a substrate for and inhibitor of CYP3A4, and formulation work deliberately pairs it with the CYP inhibitor piperine to raise exposure, so at high supplemental intakes an interaction with CYP3A4-cleared medications is plausible though undocumented in humans 11,12Reference 11Clinical trialA phase I pharmacokinetic study of ursolic acid nanoliposomes in healthy volunteers and patients with advanced solid tumors — phase I clinical trialView study →Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →. A formal human safety database and interaction studies do not yet exist because the isolated molecule has not been trialled at scale, so absence of reported harm should not be read as established safety. As with all constituents on this database, the herbs that supply ursolic acid carry their own whole-plant cautions (for example hawthorn’s potential to add to cardiac-glycoside drugs) that are separate from any property of ursolic acid itself.
Dosage
There is no established human dose for isolated ursolic acid. The small muscle pilots used 450 mg per day of the isolated compound over 8 weeks 3,4Reference 3RCTUrsolic acid supplementation decreases markers of skeletal muscle damage during resistance training in resistance-trained men — randomised pilot trial (450 mg/day, 8 weeks)View study →Reference 4RCTUrsolic acid has no additional effect on muscle strength and mass in active men undergoing a high-protein diet and resistance training — double-blind placebo-controlled trialView study →; a loquat-leaf trial delivered ~51 mg/day of ursolic acid over 12 weeks 5Reference 5RCTEffect of loquat leaf extract on muscle strength, muscle mass, and muscle function in healthy adults — randomised, double-blind, placebo-controlled trial (~51 mg ursolic acid/day)View study →; and preclinical rodent work commonly uses tens to a couple of hundred milligrams per kilogram, figures inflated to compensate for poor absorption 1,2Reference 1AnimalmRNA expression signatures of human skeletal muscle atrophy identify a natural compound that increases muscle mass — Connectivity Map screen + mouse in vivoView study →Reference 2AnimalUrsolic acid increases skeletal muscle and brown fat and decreases diet-induced obesity, glucose intolerance and fatty liver disease — mouse in vivo animal modelView study →.
| Application | Form | Dose (studied) | Source |
|---|---|---|---|
| Muscle / resistance training | Isolated ursolic acid | 450 mg/day, 8 wk | 3,4Reference 3RCTUrsolic acid supplementation decreases markers of skeletal muscle damage during resistance training in resistance-trained men — randomised pilot trial (450 mg/day, 8 weeks)View study →Reference 4RCTUrsolic acid has no additional effect on muscle strength and mass in active men undergoing a high-protein diet and resistance training — double-blind placebo-controlled trialView study → |
| Muscle function | Loquat-leaf extract (UA-standardised) | ~51 mg UA/day, 12 wk | 5Reference 5RCTEffect of loquat leaf extract on muscle strength, muscle mass, and muscle function in healthy adults — randomised, double-blind, placebo-controlled trial (~51 mg ursolic acid/day)View study → |
| Cancer (PK/safety only) | IV nanoliposome | dose-escalation, phase I | 11Reference 11Clinical trialA phase I pharmacokinetic study of ursolic acid nanoliposomes in healthy volunteers and patients with advanced solid tumors — phase I clinical trialView study → |
Because oral bioavailability is very low and metabolism rapid, plain oral ursolic acid reaches only low plasma levels, and bioavailability-enhanced forms (nanoparticles, liposomes, piperine-paired) change exposure substantially 11,12Reference 11Clinical trialA phase I pharmacokinetic study of ursolic acid nanoliposomes in healthy volunteers and patients with advanced solid tumors — phase I clinical trialView study →Reference 12Systematic reviewUrsolic acid: a systematic review of its pharmacology, toxicity and rethink on its pharmacokinetics based on PK-PD model — reviewView study →. These are doses studied in research and are not a personal recommendation.
References
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