Prophylactic and therapeutic roles of oleanolic acid its derivatives in several diseases

Sen, Alaattin

doi:10.12998/wjcc.v8.i10.1767

Cited by 51 publications

(45 citation statements)

References 196 publications

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“…The main representatives of the ursane and oleanane groups, ursolic ( 1 ) and oleanolic ( 4 ) acids, respectively, have been extensively studied for therapeutic activities, gaining relevance in cancer treatment for their known activity against several cancerous models such as liver, lung, prostate, endometrial, ovarian and gastric cancers, as recently reviewed elsewhere [26,27] . Concerning CML treatment, studies have shown the comparison between the cytotoxic activity of ursolic and oleanolic acids against the human blastic phase Ph+ K562 cell line in vitro , reporting controversial IC 50 values (Table 1).…”

Section: Natural Pentacyclic Triterpenesmentioning

confidence: 99%

Natural and Semisynthetic Pentacyclic Triterpenes for Chronic Myeloid Leukemia Therapy: Reality, Challenges and Perspectives

et al. 2021

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Chronic myeloid leukemia (CML) is a neoplasm characterized by BCR‐ABL1, an oncoprotein with vital role in leukemogenesis. Its inhibition by tyrosine kinase inhibitors represents the main choice of treatment. However, therapeutic failure is worrying given the lack of pharmacological options. Pentacyclic triterpenes are phytochemicals with outstanding antitumoral properties and have also been explored as a basis for the design of potential leads. In this review, we have gathered and discuss data regarding both natural and semisynthetic pentacyclic triterpenes applied to CML cell treatment. We found consistent evidence that the class of pentacyclic triterpenes in general exerts promising pro‐apoptotic and antiproliferative activities in sensitive and resistant CML cells, and thus represents a rich source for drug development. We also analyze the predicted drug‐like properties of the molecules, discuss the structural changes with biological implications and show the great opportunities this class represents, as well as the perspectives they provide on drug discovery for CML treatment.

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Section: Natural Pentacyclic Triterpenesmentioning

confidence: 99%

Natural and Semisynthetic Pentacyclic Triterpenes for Chronic Myeloid Leukemia Therapy: Reality, Challenges and Perspectives

et al. 2021

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“…One oleanane triterpenoid, known as 2-cyano-3-,12dioxoolean-1,9-dien-28-oic acid (CDDO), is an Nrf2 activator found to play a role in cellular control of ROS/RNS levels associated with tumorigenic DNA damage [25]. CDDO was developed to reduce tumor cell proliferation [26]. Some of its derivatives, including CDDO methyl ester (CDDO-Me) and CDDO imidazolide (CDDO-Im), have antitumor effects [27].…”

Section: Discussionmentioning

confidence: 99%

Therapeutic Potential of RTA 404 in Human Brain Malignant Glioma Cell Lines via Cell Cycle Arrest via p21/AKT Signaling

Tsai

Lieu

Wang

et al. 2021

BioMed Research International

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Background. Glioblastoma multiforme (GBM) is the most common malignant brain tumor in the world. Despite advances in surgical resection, radiotherapy, and chemotherapy, GBM continues to have a poor overall survival. CDDO (2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid), a synthetic triterpenoid, is an Nrf2 activator used to inhibit proliferation and induce differentiation and apoptosis in various cancer cells. One new trifluoroethylamide derivative of CDDO, RTA 404, has been found to have increased ability to cross the blood-brain barrier. However, it is not clear what effect it may have on tumorigenesis in GBM. Methods. This in vitro study evaluated the effects of RTA 404 on GBM cells. To do this, we treated GBM840 and U87 MG cell lines with RTA 404 and assessed apoptosis, cell cycle, cell locomotion, and senescence. DNA content and induction of apoptosis were analyzed by flow cytometry and protein expression by Western blot analysis. Results. RTA 404 significantly inhibited the proliferation of tumor cells at concentrations higher than 100 nM ( p < 0.05 ) and reduced their locomotion ability. In addition, treatment with RTA 404 led to an accumulation of RTA 404-treated G 2 / M phase cells and apoptosis. An analysis of the p21/AKT expression suggested that RTA 404 may not only help prevent brain cancer but it may also exert antitumor activities in established GBM cells. Conclusion. RTA404 can inhibit proliferation, cell locomotion, cell cycle progression, and induce apoptosis in GBM cells in vitro, possibly through its inhibition of N-cadherin and E-cadherin expression via its inhibition of the AKT pathway.

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“…Also, the triterpenes are connected to the protein molecule by Vanderwall's interaction. The above mechanism reveals that the natural analog of triterpenes like OA, UA possesses the additional activity for PTP1B inhibitors by modifying the carbon chain and specifying the phosphatases utilized in the insulin reaction (Shah et al, 2016). In addition to it, a group of synthetic derivatives of OA exhibited an inhibitory effect on PTP1B, associated with insulin resistance (Yang et al, 2020).…”

Section: Role Of Oa In Protein Kinasementioning

confidence: 99%

“…Besides, OA is an active constituent of various medicinal plants like ginseng (1%), papaya fruit, and the skin of an apple (Liu et al, 2019a). Based on pharmacological activities, OA has a significant role in the treatment of diabetic disorders (Zhang et al, 2018), neuroprotective effect in acute neurological disorder (Msibi et al, 2019), hypoglycemic, antiinflammatory, cardio-protective (Sanchez-Rodriguez et al, 2018), antioxidant, lipid-lowering effect, antimicrobial (Jesus et al, 2015), hepatoprotective (Rohilla and Bhatt, 2018), and antiatherosclerotic activity along within the management of cancerous growth (Sen, 2020). Reports found that OA can produce hypoglycemic activity by modulating the insulin signaling process, carbohydrate metabolism in the skeletal muscle of streptozotocin (STZ)-induced experimental diabetic rats due to the direct interaction between the single protein molecule along with the β-phenolic -OH group present at C3 position and a -COOH group at C28 of a hydrophobic pentacyclic structure of OA (Figure 1), thus proved the versatility of OA through in vitro and in silico studies (Mukundwa et al, 2016).…”

Section: Introductionmentioning

confidence: 99%

The promising role of oleanolic acid in the management of diabetes mellitus: A review

Dash¹,

Pattnaik²,

Nityananda³

et al. 2021

J Appl Pharm Sci

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Oleanolic acid (OA) is a bioactive constituent and natural triterpenoid with a pentacyclic structure. OA possesses beneficial effects against diabetes and other metabolic disorder by undergoing a more complex and multifactorial pathway. It activates the insulin response, protects the capability and existence of pancreatic β-cells and also gives protection against diabetic difficulties. The molecular mechanism of antidiabetic activities of OA involve modulation of transduction mechanisms includes oxidative stress-induced hepatic insulin resistance, phosphorylation of extracellular signal-related kinase, protective effect on mitochondrial function, regulates NF-kappa B, suppresses polyol mechanism, formation of advanced glycation end products, activation of M3 muscarinic receptors, and activation of G proteincoupled bile acid receptor.. Thus, the utilization of effective drug or food material carrying OA might be an effective way to control diabetes. Till now, limited clinical studies have been performed to explore the use of OA in the management of diabetes mellitus. However, due to their potential therapeutic activities, OA deserves special attention. In this present review article, we have summarized the antidiabetic potential of OA reported mainly from the period of 2015-2020 with a notable emphasis on the molecular mechanisms. We have searched Google Scholar, medical databases, and websites using related keywords like OA, insulin, diabetes mellitus, herbal medicine, or a combination of them. To qualify for inclusion, the herbal plants should have tremendous antidiabetic activities, established with biomarkers with limited adverse effects.

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Prophylactic and therapeutic roles of oleanolic acid its derivatives in several diseases

Cited by 51 publications

References 196 publications

Natural and Semisynthetic Pentacyclic Triterpenes for Chronic Myeloid Leukemia Therapy: Reality, Challenges and Perspectives

Natural and Semisynthetic Pentacyclic Triterpenes for Chronic Myeloid Leukemia Therapy: Reality, Challenges and Perspectives

Therapeutic Potential of RTA 404 in Human Brain Malignant Glioma Cell Lines via Cell Cycle Arrest via p21/AKT Signaling

The promising role of oleanolic acid in the management of diabetes mellitus: A review

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