2021
DOI: 10.3389/fonc.2021.745584
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Ursolic Acid Inhibits Breast Cancer Metastasis by Suppressing Glycolytic Metabolism via Activating SP1/Caveolin-1 Signaling

Abstract: Breast cancer remains the most common malignancy and the leading causality of cancer-associated mortality among women worldwide. With proven efficacy, Oldenlandia diffusa has been extensively applied in breast cancer treatment in Traditional Chinese Medicine (TCM) for thousands of years. However, the bioactive compounds of Oldenlandia diffusa accounting for its anti-breast cancer activity and the underlying biological mechanisms remain to be uncovered. Herein, bioactivity-guided fractionation suggested ursolic… Show more

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Cited by 23 publications
(23 citation statements)
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“…Treatment with ursolic acid increased SP1 expression and promoted SP1 binding to the Caveolin-1 ( CAV1 ) promoter to increase CAV1 transcription. Activation of CAV1 by SP1 downregulates glycolytic metabolism and damages mitochondrial function in breast cancer cells [ 95 ].…”
Section: Breast Cancermentioning
confidence: 99%
“…Treatment with ursolic acid increased SP1 expression and promoted SP1 binding to the Caveolin-1 ( CAV1 ) promoter to increase CAV1 transcription. Activation of CAV1 by SP1 downregulates glycolytic metabolism and damages mitochondrial function in breast cancer cells [ 95 ].…”
Section: Breast Cancermentioning
confidence: 99%
“…It has also been shown that ursolic acid suppressed proliferation and induced apoptosis in breast cancer cells, but not in non-malignant cells. Ursolic acid also repressed metastasis in both zebrafish and mouse models via the suppression of glycolysis through the activation of SP1/caveolin-1 signaling [ 159 ]. Another research group has demonstrated that ursolic acid inhibited energy metabolism.…”
Section: Plants From Different Continents Used In Ethnomedicine For T...mentioning
confidence: 99%
“…Ursolic acid is a pentacyclic triterpenoid found in apple peels (Malus domestica) [100,101]. Ursolic acid protects against breast cancer by activating SFRP4 (Wnt agonist), inhibiting miRNA-499A-5p in MCF7, MDA-MB-231, and CSC cells [102], and also activates SP1/Caveoli-1 signaling, thereby inhibiting breast cancer metastasis [103]. Ursolic acid also protects against intestinal cancer progression, where it dose-dependently attenuates the number and growth of cells while down-regulating FN1, CDH2, CTNNB1, and TWSIT gene expression.…”
Section: Ursolic Acidmentioning
confidence: 99%
“…Ursolic acid Apple peels ↑ sFRP4, sp1, Caveolin-1, Bax, p21, p53, Cyclin B1, Caspase-3, Caspase-8, Caspase-9, fibronectin-1, E-Cad, and LC3-II Gliolastoma [104], breast [100,101], intestinal [102], lung [103], colorectal [105], esophageal [106], and pancreatic [107] [111], breast [112,113], prostate [115], ovarian [114], colorectal [116,117], lung [118], gastric [56], and endometrial [119] cancer ↓ MMP-2, FAK, CDK1, PSA, TMPRSS2, TMEPA1, PI3K, Akt, Bcl-2, TS, RhoA, Rac1, JAK/STAT3, MAPK, and NFκB Quercetin Apple, chili pepper, blueberry, cherry, cranberry, black tea, and red wine ↑ p53 Liver [120,121], prostate [122,123], colon [123], leukemia [123], lymphoma [123], breast [123,124], pancreatic [125], lung [126],…”
mentioning
confidence: 99%