Ursolic acid (UA): A metabolite with promising therapeutic potential

Kashyap, Dharambir; Tuli, Hardeep Singh; Sharma, Anil Kumar

doi:10.1016/j.lfs.2016.01.017

Cited by 250 publications

(156 citation statements)

References 148 publications

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“…For instance, HIF-1α is associated with enhanced apoptosis resistance (Kilic et al, 2007), while UA could promote apoptosis in many conditions and various types of cancer (Kashyap et al, 2016). Moreover, we also detected decreased apoptotic tumor cells by the terminal deoxynucleotidyl transferase dUTP nick end labeling (TUNEL) assay under hypoxia, which could be reversed by UA (data not shown).…”

Section: Discussionmentioning

confidence: 77%

“…and Prunell avulgaris L. (Cheung et al, 2006;Cheung and Zhang, 2008). It exhibits a broad range of pharmacological effects such as anti-inflammatory, antiviral, antioxidant, and hepatoprotective activities (Feuillolay et al, 2016;Kashyap et al, 2016;Siegel et al, 2016), and has proven to be effective in treating various types of cancers including CRC (Pathak et al, 2007;Prasad et al, 2012;Lin et al, 2013;Kadioglu and Efferth, 2015). Several mechanisms by which UA acts as a chemosensitizer have been proposed, such as pro-apoptosis (Meng et al, 2015) and anti-angiogenesis (Lin et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

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Ursolic acid sensitized colon cancer cells to chemotherapy under hypoxia by inhibiting MDR1 through HIF-1α

Shan

Xuan

Zhang

et al. 2016

J. Zhejiang Univ. Sci. B

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Abstract:Objective: To explore the efficacy of ursolic acid in sensitizing colon cancer cells to chemotherapy under hypoxia and its underlying mechanisms. Methods: Three colon cancer cell lines (RKO, LoVo, and SW480) were used as in vitro models. 5-Fluorouracil (5-FU) and oxaliplatin were used as chemotherapeutic drugs. Cell viability and apoptosis were tested to evaluate the sensitivity of colon cancer cells to chemotherapy. The transcription and expression levels of hypoxia-inducible factor-1α (HIF-1α), multidrug resistance gene 1 (MDR1), and vascular endothelial growth factors (VEGF) were assessed by quantitative real-time polymerase chain reaction (qRT-PCR) and immunoblotting. Cycloheximide and MG132 were used to inhibit protein synthesis and degradation, respectively. In vitro tube formation assay was used to evaluate angiogenesis. Results: We demonstrated the chemosensitizing effects of ursolic acid with 5-FU and oxaliplatin in three colon cancer cell lines under hypoxia. This effect was correlated to its inhibition of MDR1 through HIF-1α. Moreover, ursolic acid was capable of inhibiting HIF-1α accumulation with little effects on its constitutional expression in normoxia. In addition, ursolic acid also down-regulated VEGF and inhibited tumor angiogenesis. Conclusions: Ursolic acid exerted chemosensitizing effects in colon cancer cells under hypoxia by inhibiting HIF-1α accumulation and the subsequent expression of the MDR1 and VEGF.

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Section: Discussionmentioning

confidence: 77%

Section: Introductionmentioning

confidence: 99%

Ursolic acid sensitized colon cancer cells to chemotherapy under hypoxia by inhibiting MDR1 through HIF-1α

Shan

Xuan

Zhang

et al. 2016

J. Zhejiang Univ. Sci. B

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“…Molecules with a skeleton of oleanane and ursane seem to be responsible, among others, for anti-inflammatory activity of a variety of medicinal plants through inhibition of enzymes involved in the production of eicosanoids, such as cyclooxygenase and phospholipase A2, which impede the release of cytokines, histamine and serotonin (13). However, they have never been described in the Salix genus.…”

Section: Resultsmentioning

confidence: 99%

The bioguided fractionation and pharmacological activity of an endemic Salix canariensis species

2017

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The present study was designed to confirm the wide traditional use of treating pain with Salix canariensis, an endemic species of the Macaronesian region. The active compounds were identified. Pharmacological activities were explored in experimental animals by acetic acid-induced writhing, formalin and Levy´s tests, and bioactive compounds were identified after a bio-guided fractionation of the most active organic extract. S. canariensis extract, orally administrated at different doses, led to a significant reduction in writhing, caused a moderate decrease of formalin-induced pain and revealed an excellent dose-dependent anti-inflammatory effect. Bioassay-guided fractionation of the ethyl acetate extract suggested the possible presence of pentacyclic triterpenes from oleanane and ursane series. These findings allow the conclusion that S. canariensis exerts analgesic and anti-inflammatory activities, documenting its traditional use in the treatment of pain and inflammatory diseases.

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“…Ursolic acid (27) is an α-amyrin type of triterpene, again with carboxylic function at C-17. Similarly to oleanolic (26) and maslinic (28) acid, it can be isolated from several plant species with potent medicinal properties [142]. Similar to previously mentioned triterpenic acids, it shows activities beneficial in the treatment of civilization diseases like for example cancer, cardiovascular diseases or chronic inflammations [142].…”

Section: Triterpenes and Steroidsmentioning

confidence: 96%

Kazakh Ziziphora Species as Sources of Bioactive Substances

et al. 2016

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Ziziphora species represent the prototypical example of the Lamiaceae family. The phytochemicals present in Ziziphora include monoterpenic essential oils, triterpenes and phenolic substances belonging to the flavonoids. In Kazakh traditional medicine, Ziziphora species possess several medicinal uses. In particular, Z. bungeana Lam. and Z. clinopodioides Lam. are used for the treatment of illnesses related to the cardiovascular system or to combat different infections. Unfortunately, the majority of the information about the complex Ziziphora species is only available in Russian and Chinese language, therefore, we decided gather all available information on Kazakhstan Ziziphora, namely its content compounds, medicinal uses and published patents, to draw the attention of scientists to this very interesting plant with high medicinal potential.

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Ursolic acid (UA): A metabolite with promising therapeutic potential

Cited by 250 publications

References 148 publications

Ursolic acid sensitized colon cancer cells to chemotherapy under hypoxia by inhibiting MDR1 through HIF-1α

Ursolic acid sensitized colon cancer cells to chemotherapy under hypoxia by inhibiting MDR1 through HIF-1α

The bioguided fractionation and pharmacological activity of an endemic Salix canariensis species

Kazakh Ziziphora Species as Sources of Bioactive Substances

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