Ursolic Acid and Its Derivatives as Bioactive Agents
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 se...
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| Format: | Article |
| Language: | English |
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MDPI AG
2019-07-01
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| Series: | Molecules |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1420-3049/24/15/2751 |
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| author | Sithenkosi Mlala Adebola Omowunmi Oyedeji Mavuto Gondwe Opeoluwa Oyehan Oyedeji |
| author_facet | Sithenkosi Mlala Adebola Omowunmi Oyedeji Mavuto Gondwe Opeoluwa Oyehan Oyedeji |
| author_sort | Sithenkosi Mlala |
| collection | DOAJ |
| description | 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. <i>Mimusops caffra</i>, <i>Ilex paraguarieni,</i> and <i>Glechoma hederacea,</i> 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. |
| first_indexed | 2024-12-11T09:24:40Z |
| format | Article |
| id | doaj.art-1978b533084244f5bd354bb926de2c9c |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-11T09:24:40Z |
| publishDate | 2019-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-1978b533084244f5bd354bb926de2c9c2022-12-22T01:13:11ZengMDPI AGMolecules1420-30492019-07-012415275110.3390/molecules24152751molecules24152751Ursolic Acid and Its Derivatives as Bioactive AgentsSithenkosi Mlala0Adebola Omowunmi Oyedeji1Mavuto Gondwe2Opeoluwa Oyehan Oyedeji3Department of Chemistry, Faculty of Science and Agriculture, University of Fort Hare, Private Bag X1314, Alice 5700, South AfricaDepartment of Chemical and Physical Sciences, Faculty of Natural Sciences, Walter Sisulu University, Private Bag X1, Mthatha 5117, South AfricaDepartment of Human Biology, Faculty of Health Sciences, Walter Sisulu University, Private Bag X1, Mthatha 5117, South AfricaDepartment of Chemistry, Faculty of Science and Agriculture, University of Fort Hare, Private Bag X1314, Alice 5700, South AfricaNon-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. <i>Mimusops caffra</i>, <i>Ilex paraguarieni,</i> and <i>Glechoma hederacea,</i> 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.https://www.mdpi.com/1420-3049/24/15/2751non-communicable diseasespentacyclic triterpenoidsursolic acidderivativessourcesbiological studiesclinical trials. |
| spellingShingle | Sithenkosi Mlala Adebola Omowunmi Oyedeji Mavuto Gondwe Opeoluwa Oyehan Oyedeji Ursolic Acid and Its Derivatives as Bioactive Agents Molecules non-communicable diseases pentacyclic triterpenoids ursolic acid derivatives sources biological studies clinical trials. |
| title | Ursolic Acid and Its Derivatives as Bioactive Agents |
| title_full | Ursolic Acid and Its Derivatives as Bioactive Agents |
| title_fullStr | Ursolic Acid and Its Derivatives as Bioactive Agents |
| title_full_unstemmed | Ursolic Acid and Its Derivatives as Bioactive Agents |
| title_short | Ursolic Acid and Its Derivatives as Bioactive Agents |
| title_sort | ursolic acid and its derivatives as bioactive agents |
| topic | non-communicable diseases pentacyclic triterpenoids ursolic acid derivatives sources biological studies clinical trials. |
| url | https://www.mdpi.com/1420-3049/24/15/2751 |
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