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Corosolic Acid

Scientific Name(s): 2 alpha-hydroxy ursolic acid
Common Name(s): Corosolic acid, Glucosol

Medically reviewed by Drugs.com. Last updated on Jan 29, 2024.

Clinical Overview

Use

Corosolic acid has numerous biological properties, including antidiabetic, anti-inflammatory, antiproliferative, and protein kinase C inhibition activity. However, there is a lack of clinical evidence to support these uses.

Dosing

Numerous commercial formulations are available, including tablets, capsules, hypoglycemic food products, and cosmetics. Most formulations are available in capsule form, containing 18% corosolic acid and derived from Lagerstroemia speciosa L. Manufacturer suggested dosage is 1 softgel by mouth 30 minutes before morning and evening meals. Softgel products are marketed for noninsulin dependent type 2 diabetic patients.

Contraindications

Avoid use with hypersensitivity to any of the plant sources of corosolic acid.

Pregnancy/Lactation

Avoid use. Information regarding safety and efficacy in pregnancy and lactation is lacking.

Interactions

None well documented.

Adverse Reactions

There is potential for skin rashes because the product may be derived from several plant species. Caution is warranted in patients with renal impairment; acute lactic acidosis has been reported.

Toxicology

Toxicologic information regarding use in humans is lacking.

Source

Corosolic acid is found in numerous plant species, including Lagerstroemia speciosa L., Tiarella polyphylla D. Don, Datisca cannabina L., Eriobotrya japonica (Thunb.) Lindl., and Perilla frutescens (L.) Britton.

History

Corosolic acid has numerous biological properties including antidiabetic, anti-inflammatory, antiproliferative, and protein kinase C inhibition activity.Jung 2006, Wen 2005 It is found in numerous plants species, particularly L. speciosa.Washino 2004 Most medical research focuses on the compound's efficacy in diabetes. Glucosol (or GlucoFit) is a commercially available product primarily marketed in Japan and the United States as a dietary supplement for weight loss and blood sugar balance.Wen 2005 Corosolic acid is found in numerous cosmetic products, including creams, lotions, hair tonics, as well as in hypoglycemic health foods.Nojima 2006, Nojima 2006, Washino 2004

Chemistry

Corosolic acid is a naturally occurring pentacyclic triterpene also known as 2 alpha-hydroxy ursolic acid.Aguirre 2006, Wen 2007 Chemical analyses focus on the study of corosolic acid and its derivatives as inhibitors of glycogen phosphorylases for potential development of antidiabetic agents.Wen 2005, Wen 2007 There is documented commercial interest in improving the chemical production of corosolic acid and its esters.Matsuyama 2004, Takayama 2004

Uses and Pharmacology

Studies in rats indicate a low oral bioavailability of corosolic acid and a large volume of distribution that is concentrated in tissues and organs.(Qian 2021)

Antimicrobial and antiviral

Experimental data

A combination of in silico and in vitro studies documented strong antimicrobial activity of corosolic acid (derived from Callistemon citrinus [Curtis] Skeels.) against vancomycin-resistant Enterococci with IC50 values superior to ciprofloxacin (15.9 vs 30.2 microM, respectively).(Abdelmalek 2021) Corosolic acid enhanced the activity of treatment with tobramycin against Pseudomonas aeruginosa in a biofilm inhibition assay.(Garo 2007)

An in silico molecular docking study identified corosolic acid to have a high binding score to the spike glycoprotein-receptor binding domain of SARS-CoV-2 virus. Combined with reported medicinal properties of corosolic acid, it was determined to be one of 7 phytochemicals that could be combined to formulate an appropriate therapeutic approach to fight against the virus.(Vardhan 2020)

Cancer

In vitro data

Corosolic acid has cytotoxic activity against several human cancer cell lines. The compound antagonized morphological modification of K-562 leukemic cells. The mechanism of action may be associated with suppression of protein kinase C activity.(Ahn 1998) In addition, cytotoxic activity has been documented against human cancer cell lines HL-60 (leukemia carcinoma), MCF-7 (breast carcinoma), and Hep-G2 (hepatic carcinoma).(Akihisa 2006)

Animal data

In a 2-stage Berenblum experiment on mouse skin papillomas, the inhibitory effect of corosolic acid was comparable or equivalent to beta-carotene, rosmarinic acid, and alpha-linolenic acid.(Banno 2004)

Cardiovascular

Animal and experimental data

In a myocardial infarction (MI) mouse model, administration of corsolic acid was observed to significantly increase survival rates, increase the number of cardiocytes, and reduce infarct size 4 weeks after the MI compared to controls. Left ventricular function (LVF) was also improved in the treatment group and cardiac fibrosis was decreased.(Wang 2020) Corosolic acid has also been shown to inhibit pressure-overload cardiac hypertrophy and improved LVF in another mouse model.(Wang 2019) Corosolic acid has demonstrated vasorelaxation properties that appear to be mediated by endothelial factors and potassium channels.(Luna-Vazquez 2018)

Diabetes and metabolic syndrome

Corosolic acid may improve the insulin pathway. The action of insulin is mediated by tyrosine phosphorylation and initiated by the binding of insulin to the insulin receptor. Corosolic acid may act as an insulin sensitizer, enhancing insulin receptor B phosphorylation indirectly by inhibiting certain nonreceptor protein tyrosine phosphatases.(Shi 2008) Corosolic acid may also enhance GLUT4 glucose transporter processing of glucose uptake into muscle cells.(Miura 2004) Another study reported that corosolic acid inhibited gluconeogenesis by increasing the production of the gluconeogenic intermediate fructose-2,6-bisphosphate in isolated hepatocytes. Corosolic acid may promote glycolysis.(Klein 2007, Yamada 2008) Reversible inhibition of alpha-glucosidase activity has also been reported.(Liu 2020, Ni 2019, Qian 2021)

Animal data

Numerous animal experiments document the effect of corosolic acid on blood glucose. One study in rats found that 1% corosolic acid reduced blood glucose levels at 90 minutes after oral administration.(Hamamoto 1999) Treatment with corosolic acid lowered plasma insulin levels and reduced the blood glucose levels in KK-Ay mice 2 weeks after a single oral dose of 2 mg/kg. Blood glucose in KK-Ay mice treated with corosolic acid decreased in an insulin tolerance test.(Miura 2006) Another experiment showed similar inhibitory action against increasing blood glucose levels.(Matsuyama 2005) Increasing the concentration of corosolic acid may lead to enhanced glucose uptake activity.(Zong 2007) Corosolic acid induced muscle GLUT4 translocation from low-density microsomal membrane to plasma membrane in genetically-induced type 2 diabetic mice.(Klein 2007, Miura 2004)

In an animal model on metabolic syndrome, corosolic acid had antihypertensive, lipid-lowering, antioxidant, and anti-inflammatory effects on rats.(Yamaguchi 2006) In a similar study, corosolic acid reduced blood pressure and serum-free fatty acid levels in rats.(Kunitomo 2007)

Clinical data

In a small randomized clinical trial, 10 patients with type 2 diabetes were treated with an extract from the leaves of L. speciosa standardized to 1% corosolic acid (Glucosol ). Patients receiving Glucosol 32 or 48 mg daily for 2 weeks demonstrated a significant reduction in blood glucose levels. The softgel capsule formulation resulted in a 30% decrease, compared with 20% decrease in blood glucose levels in patients receiving the dry-powder, hard-gelatin capsule formulation. The softgel formulation has better bioavailability, and the active lipophilic triterpene ingredient is better absorbed in an oil-based, soft-gelatin capsule formulation.(Judy 2003)

In a study completed in Japan with 31 patients, corosolic acid lowered postchallenge plasma glucose levels.(Fukushima 2006)

Liver disease

Animal data

In a non-alcoholic steatohepatitis (NASH) mouse model, daily oral administration of corosolic acid for 9 weeks improved hepatic histopathology, macrovesicular steatosis, inflammation, and fibrogenic changes in a dose-dependent manner compared to untreated disease controls. Results were comparable to normal controls and better than the silymarin positive control group. Elevated liver enzymes, triglycerides, and total cholesterol seen in untreated controls were also significantly improved with corosolic acid. The mechanism involved regulation of NF-kappaB, hepatic lipid metabolism, and fibrogenic cytokine signaling.(Liu 2021) Similar hepatoprotective results were reported in a hyperlipidemia mouse model.(Zhang 2020)

Obesity

Animal and in vitro data

Corosolic acid inhibits protein tyrosine phosphatase 1B in vitro; inhibition of this phosphatase is proposed as a therapy for obesity.(Na 2006) Corosolic acid is also a pancreatic lipase inhibitor, the main enzyme for lipid absorption.(Jang 2008) In a mouse study, corosolic acid acted as a peroxisome proliferator-activated receptor alpha agonist, regulating lipid metabolism and increasing fatty acid beta-oxidation in the liver.(Yamada 2008)

Other uses

Activity against the classical pathway of the complement system, inflammasome activation, and several inflammation-related signal transduction factors is documented for corosolic acid and its structural analogs.(Abdelmalek 2021, Qian 2021, Thuong 2006)

Antioxidant activity has also been documented for corosolic acid via regulation of autophagy activation and mitogen-activated protein kinase signaling.(Qian 2021)

Corosolic acid has been shown in vitro to inhibit melanin synthesis, Propionibacterium acnes growth, and release of allergic mediators, while also being a potent stimulator of dermal type 1 collagen production and hyaluronic acid.(Tan 2017)

In circadian clock experiments, peak time of the circadian rhythm was found to be significantly delayed by corosolic acid and appears to act as a synchronizer of cell clocks.(Suzuki 2021)

Suppression of osteoclastogenesis via suppression of intracellular oxidative stress (ie, NF-kappaB) and up-regulation of antioxidants was observed for corosolic acid both in vitro and in an osteolysis mouse model.(Peng 2019)

Dosing

Numerous commercial formulations are available, including tablets, capsules, hypoglycemic food products, and cosmetics. Most formulations are available in capsule form containing 18% corosolic acid extracted from L. speciosa. The manufacturer suggested dosage is 1 softgel by mouth 30 minutes before morning and evening meals. Softgel products are marketed for noninsulin dependent type 2 diabetic patients.Giampapa 2006, Matsuyama 2004, Udell 2003

Pregnancy / Lactation

Avoid use. Information regarding safety and efficacy in pregnancy and lactation is lacking.

Interactions

None well documented.

Adverse Reactions

Avoid use with hypersensitivity to any source plants for corosolic acid. Because the product may be derived from several plant species, there is a potential for skin rashes.

A case of severe acute lactic acidosis was attributed to the likely accumulation of corosolic acid in a patient with type 2 diabetes mellitus, gouty arthritis, and stage 3a chronic kidney disease with non-steroidal anti-inflammatory drug (NSAID)-induced acute renal impairment. The patient had been taking corosolic acid daily for 1 month. One week prior to admission, acute NSAID-induced renal hypoperfusion was thought to have occurred after the patient self-medicated with diclofenac for joint pains, which led to a subsequent accumulation of corosolic acid. Corosolic acid has been shown to inhibit gluconeogenesis and enhance glycolysis.Zheng 2010

Toxicology

A single oral dose toxicity study in rats administered Glucosol 5 g/kg showed no marked pathological findings.Hamamoto 1999

Index Terms

References

Disclaimer

This information relates to an herbal, vitamin, mineral or other dietary supplement. This product has not been reviewed by the FDA to determine whether it is safe or effective and is not subject to the quality standards and safety information collection standards that are applicable to most prescription drugs. This information should not be used to decide whether or not to take this product. This information does not endorse this product as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this product. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this product. This information is not specific medical advice and does not replace information you receive from your health care provider. You should talk with your health care provider for complete information about the risks and benefits of using this product.

This product may adversely interact with certain health and medical conditions, other prescription and over-the-counter drugs, foods, or other dietary supplements. This product may be unsafe when used before surgery or other medical procedures. It is important to fully inform your doctor about the herbal, vitamins, mineral or any other supplements you are taking before any kind of surgery or medical procedure. With the exception of certain products that are generally recognized as safe in normal quantities, including use of folic acid and prenatal vitamins during pregnancy, this product has not been sufficiently studied to determine whether it is safe to use during pregnancy or nursing or by persons younger than 2 years of age.

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