Abstract
Triple-negative breast cancer (TNBC), an aggressive subtype of breast cancer, shows higher metastases and relapse rates than other subtypes. The metastasis of TNBC is the main reason for the death of TNBC patients. Increasing evidence has shown that inhibiting the metastasis of TNBC is a good method for TNBC treatment. Here, VSP-17 was designed and synthesized as an agonist of PPARγ, evidenced by upregulating the expression of CD36 and increasing the activity of PPARγ reporter gene. VSP-17 obviously inhibited the migration and invasion process of MDA-MB-231 cells but showed little effect on the viability of MDA-MB-231 cells. Notably, VSP-17 could selectively promote the expression of E-cadherin without affecting the expression of BRMS1, CXCL12, MMP9, Orai1, Stim1, TGF-β, and VEGF. In addition, VSP-17 significantly suppressed the metastasis of liver and promoted the expression of E-cadherin in MDA-MB-231 xenograft model. In conclusion, VSP-17 inhibited the metastasis process of TNBC via upregulating the expression of E-cadherin.
Highlights
Triple-negative breast cancer (TNBC), an aggressive subtype of breast cancer, is characterized by deficiency of estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor receptor-2 (HER2)
The present study aimed to explore the underlying mechanism for the anti-metastasis effect of VSP-17, with special emphasis on the expression of E-cadherin
After evaporation of the solvents under reduced pressure, the crude product was purified on a silica gel column using EtOAc/petroleum ether (1:9) to obtain the pure 3 (2.94 g, 80%) as a white solid
Summary
Triple-negative breast cancer (TNBC), an aggressive subtype of breast cancer, is characterized by deficiency of estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor receptor-2 (HER2). The global breast cancer mortality is declining, which is partially due to progress in early diagnosis of breast cancer, but the TNBC subtype is still the main cause of human death according to “Cancer Statistics, 2017” [1]. Agents that have an anti-metastasis effect are valuable for TNBC treatment. TNBC metastasis, a stage of breast cancer cells where the disease has spread to distant sites beyond the blood vessel and the axillary lymph nodes. After the intravasation into the circulatory system through the bloodstream or lymph channels, cells extravasate to a distant site and proliferate at the metastatic site of breast cancer cells. Increasing evidence has shown that the Molecules 2018, 23, 121; doi:10.3390/molecules23010121 www.mdpi.com/journal/molecules
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