Therapeutic Interventions Using Ursolic Acid for Cancer Treatment

Ray, Navin; Kim, Soo Mi

doi:10.4172/2161-0444.1000367

Cited by 11 publications

(7 citation statements)

References 75 publications

(89 reference statements)

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“…Ursolic acid (UA) ( Figure 1 A), a pentacyclic triterpene, is a common chemical constituent existing mainly in the Lamiaceae family [ 12 ]. Studies have indicated that UA can affect multiple molecular signaling pathways related to human carcinogenesis, apoptosis, inflammation, metastasis, autophagy, and proliferation [ 13 , 14 ]. Lewinska et al found UA could mediate changes in the glycolytic pathway to promote cytotoxic autophagy and apoptosis in phenotypically different breast cancer cells [ 15 ].…”

Section: Introductionmentioning

confidence: 99%

Ursolic Acid Enhances the Sensitivity of MCF-7 and MDA-MB-231 Cells to Epirubicin by Modulating the Autophagy Pathway

et al. 2022

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Breast cancer is the leading cause of cancer death among women in the world, and its morbidity and mortality are increasing year by year. Epirubicin (EPI) is a commonly used drug for the treatment of breast cancer but unfortunately can cause cardiac toxicity in patients because of dose accumulation. Therefore, there is an urgent need for new therapies to enhance the sensitivity of breast cancer cells to EPI. In this study, we found ursolic acid (UA) can significantly improve the drug sensitivity of human breast cancer MCF-7/MDA-MB-231 cells to EPI. Next, we observed that the co-treatment of UA and EPI can up-regulate the expression of autophagy-related proteins Beclin-1, LC3-II/LC3-I, Atg5, and Atg7, and decrease the expression levels of PI3K and AKT, which indicates that the potential mechanism should be carried out by the regulating class III PI3K(VPS34)/Beclin-1 pathway and PI3K/AKT/mTOR pathway. Furthermore, we found the autophagy inhibitor 3-methyladenine (3-MA) could significantly reverse the inhibitory effect of co-treatment of UA and EPI on MCF-7 and MDA-MB-231 cells. These findings indicate that UA can dramatically enhance the sensitivity of MCF-7 and MDA-MB-231 cells to EPI by modulating the autophagy pathway. Our study may provide a new therapeutic strategy for combination therapy.

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Section: Introductionmentioning

confidence: 99%

Ursolic Acid Enhances the Sensitivity of MCF-7 and MDA-MB-231 Cells to Epirubicin by Modulating the Autophagy Pathway

et al. 2022

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“…Other research has shown that ursolic acid has anti-obesity properties and can be a potential drug for therapeutic treatment of obesity. Ursolic acid also possesses anti-proliferative activity and can be used to treat cancer (Cargnin and Gnoatto, 2017; Navin and Mi Kim, 2016). LC MS/MS and GC MS of methanol and hexane extracts confirmed the presence of roburic acid at m/z, 441.3779.…”

Section: Discussionmentioning

confidence: 99%

Phytochemical characterization and in vitro antibacterial activity of Xeroderris stuhlmannii (Taub.) Mendonca & E.P. Sousa bark extracts

Selemani

Kazingizi

Manzombe

et al. 2020

Preprint

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The use of herbal medicine is common in many rural communities in Zimbabwe because generic drugs are expensive and not readily available. In this work, we documented the important phytochemicals from Xeroderris stuhlmannii (Taub.) Mendonca & E.P. Sousa (Murumanyama in Shona), bark extracts and tested their antibacterial activity in order to demonstrate its potential as an antimicrobial agent. Qualitative screening of secondary metabolites confirmed the presence of alkaloids, flavonoids, terpenoids, steroids and polyphenols in the crude bark extracts. The MICs values for the crude extracts on six bacterial strains ranged from 0.23 to 0.80 mg/mL. Antimicrobial tests showed higher potency for crude bark extracts on E. Coli (MIC, 0.232 mg/mL) and lower potency on coliform (MIC, 0.798 mg/mL). LC-MS/MS analysis of various fractions confirmed the presence of twenty-eight phytochemicals whereas, twelve phytochemicals were identified using GC-MS. Both techniques confirmed the presence of ursolic acid, roburic acid, reticuline, rotenone and p-coumaric acid glucoside in hexane and methanol extracts. In summary, our findings show that Xeroderris stuhlmannii (Taub.) Mendonca & E.P. Sousa contain many phytochemical compounds that have antimicrobial activity. Moreover, some of the compounds in the bark extract have been shown to possess antioxidant, antiviral, antitumor and anti-inflammatory properties. Thus, Xeroderris stuhlmannii (Taub.) Mendonca & E.P. Sousa barks can act as a useful herbal supplement for treatment of a number of diseases in rural communities where modern drugs are expensive and not readily available.

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“…UA may occur as an aglycone or free acid of saponins [52,53]. UA has a low solubility in water, but high solubility in alcoholic sodium hydroxide (NaOH) and glacial acetic acid [54][55][56][57]. The UA chemical formula is C 30 H 48 O 3 , with a melting point of 283-285 • C. The properties of the UA structure indicate that it has a molecular weight of 456.7g/mol [20,52,53,58].…”

Section: Chemistry Of Uamentioning

confidence: 99%

“…Wu and colleagues (2017) produced several UA derivatives (47)(48)(49)(50)(51)(52)(53)(54)(55)(56)(57)(58)(59)(60)(61) in an effort to study the greater power and bioavailability of the UA by adding an acyl group at position C-3 to make the most of the structure-activity relationship. They further synthesized ester derivatives by a process of esterification with suitable acid chlorides in the presence of a DMAP catalyst.…”

Section: Chemistry Of Uamentioning

confidence: 99%

Ursolic Acid and Its Derivatives as Bioactive Agents

et al. 2019

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Non-communicable diseases (NCDs) such as cancer, diabetes, and chronic respiratory and cardiovascular diseases continue to be threatening and deadly to human kind. Resistance to and side effects of known drugs for treatment further increase the threat, while at the same time leaving scientists to search for alternative sources from nature, especially from plants. Pentacyclic triterpenoids (PT) from medicinal plants have been identified as one class of secondary metabolites that could play a critical role in the treatment and management of several NCDs. One of such PT is ursolic acid (UA, 3 β-hydroxy-urs-12-en-28-oic acid), which possesses important biological effects, including anti-inflammatory, anticancer, antidiabetic, antioxidant and antibacterial effects, but its bioavailability and solubility limits its clinical application. Mimusops caffra, Ilex paraguarieni, and Glechoma hederacea, have been reported as major sources of UA. The chemistry of UA has been studied extensively based on the literature, with modifications mostly having been made at positions C-3 (hydroxyl), C12-C13 (double bonds) and C-28 (carboxylic acid), leading to several UA derivatives (esters, amides, oxadiazole quinolone, etc.) with enhanced potency, bioavailability and water solubility. This article comprehensively reviews the information that has become available over the last decade with respect to the sources, chemistry, biological potency and clinical trials of UA and its derivatives as potential therapeutic agents, with a focus on addressing NCDs.

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Therapeutic Interventions Using Ursolic Acid for Cancer Treatment

Cited by 11 publications

References 75 publications

Ursolic Acid Enhances the Sensitivity of MCF-7 and MDA-MB-231 Cells to Epirubicin by Modulating the Autophagy Pathway

Ursolic Acid Enhances the Sensitivity of MCF-7 and MDA-MB-231 Cells to Epirubicin by Modulating the Autophagy Pathway

Phytochemical characterization and in vitro antibacterial activity of Xeroderris stuhlmannii (Taub.) Mendonca & E.P. Sousa bark extracts

Ursolic Acid and Its Derivatives as Bioactive Agents

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