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Ursolic And Oleanolic Acids

Also known as: 3β-Hydroxyurs-12-en-28-oic acid, UA, Oleanolic Acid, 3β-Hydroxyolean-12-en-28-oic acid, OA, Ursolic Acid

Overview

Ursolic and oleanolic acids are naturally occurring pentacyclic triterpenoids found in various plants and medicinal herbs. Commonly recognized for their anti-inflammatory, antioxidant, and potential anticancer properties, these compounds contribute to human diets and promote various health benefits. Predominantly studied through in vitro and animal research, their roles in managing cardiometabolic health and gastrointestinal health are at the forefront of current dietary supplement discourse. Despite a significant amount of literature—over 700 articles published in the last decade on these compounds—the body of clinical evidence in human studies remains limited, confining knowledge primarily to animal models and laboratory settings. Evidence strongly supports their anti-inflammatory and antioxidant efficacy, with ongoing investigations into their efficacy against cancer and metabolic diseases. However, both acids display low oral bioavailability, which may restrict their clinical applicability unless reformulated for better absorption.

Benefits

Ursolic acid exhibits notable benefits including: 1) **Anti-inflammatory Effects**: Robust evidence shows that it significantly reduces pro-inflammatory cytokines such as IL-1β, IL-6, and TNF-α, while enhancing antioxidant enzymes like SOD and GSH. These effects are validated across animal and in vitro studies. 2) **Antioxidant Effects**: Ursolic acid elevates GSH levels and decreases MDA levels, indicating strong antioxidant properties. 3) **Gastrointestinal Health**: It demonstrates anti-proliferative, anti-metastatic, and pro-apoptotic effects in cancer models, although clinical effectiveness is hampered by low bioavailability. Clinical outcomes regarding cardiometabolic risk factors remain inconclusive, as systematic reviews indicate no significant changes after supplementation. Overall, while the anti-inflammatory and antioxidant effects are widely supported, individual benefits can vary, and further human research is necessary.

How it works

Ursolic acid modulates inflammatory responses by inhibiting pro-inflammatory cytokines and upregulating antioxidant enzymes. It operates through critical biological pathways, including interaction with NF-κB signalling, which governs the immune response. Additionally, by altering lipid membrane fluidity and permeability, it influences cellular signaling, which exacerbates inflammation and impacts cardiovascular health. Notably, the compound's low oral bioavailability presents challenges in establishing its therapeutic efficacy, driving research into innovative delivery methods such as nanoformulations.

Side effects

Ursolic acid is generally regarded as safe, with low toxicity levels reported in available studies. There is no significant documentation of common side effects in human research, suggesting minimal adverse effects. Limited animal studies hint at absence of serious side effects in dosing trials, yet the long-term safety of supplementation remains unexplored in human contexts. No specific drug interactions or contraindications have been established; however, there remains a gap in understanding its pharmacodynamics in special populations like pregnant women, children, and the elderly. Considering the current lack of comprehensive data on side effects and interactions, individuals should exercise caution, particularly when considering long-term use or concurrent supplementation.

Dosage

Establishing precise dosage for ursolic acid poses challenges due to variability in study methodologies. General doses ranging from 50.94 to 450 mg/day have been noted as having potential efficacy, particularly concerning anti-inflammatory outcomes. As no optimal dosage ranges are confirmed, it is advised to consider the formulations concerning bioavailability; nanoformulations may enhance absorption and effectiveness. While 450 mg/day was safely administered in studies, defining a maximum safe dose remains uncertain due to insufficient long-term human data. Timing for administration of dosage has not been standardized, allowing flexibility based on individual needs.

FAQs

What is the best way to take ursolic acid?

To optimize effectiveness, consider using nanoformulations due to their improved bioavailability.

Are there any side effects?

Current evidence suggests minimal side effects, but long-term safety has not been thoroughly studied.

Is ursolic acid safe for long-term use?

Long-term safety profiles are not well established; caution is recommended.

Can ursolic acid interact with other medications?

There is no significant evidence of drug interactions, yet caution is advised until more research is available.

What can I expect from taking ursolic acid?

Anti-inflammatory and antioxidant effects are anticipated, though clinical benefits can be variable.

Research Sources

https://pubmed.ncbi.nlm.nih.gov/37841938/ – This systematic review and meta-analysis examines the anti-inflammatory and antioxidant properties of ursolic acid, with results affirming significant reductions in inflammatory cytokines and increased antioxidant levels across various preclinical models. The review emphasizes the high quality of evidence from multiple studies but acknowledges the need for more human clinical trials.
https://pubmed.ncbi.nlm.nih.gov/15994040/ – A meta-analysis focusing on the effects of ursolic acid on cardiometabolic risk factors found no significant changes in parameters such as body weight and lipid profiles. The analysis, while moderate in quality due to limited studies, highlights the need for further investigation into its utility in metabolic health.
https://www.mdpi.com/2079-6382/10/11/1381 – This review summarizes the anticancer effects of ursolic acid, particularly against gastrointestinal cancers. The findings underscore the compound's potential in reducing tumor proliferation and metastasis, although the lack of extensive human data limits definitive conclusions regarding clinical efficacy.
https://pubmed.ncbi.nlm.nih.gov/38923885/ – Investigating the effectiveness of various formulations, this study explores improving ursolic acid bioavailability through nanoformulations. It provides insights into absorption mechanisms and highlights limitations of conventional forms found in current dietary supplements.
https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2024.1405497/full – This comprehensive article presents the pharmacological effects of ursolic acid, detailing its antioxidant and anti-inflammatory mechanisms, and explores future research directions for improved delivery systems. The review offers a critical examination of the existing literature centered on its health benefits.