New pentacyclic triterpene from Potentilla atrosanguinea Lodd. as anticancer agent for breast cancer targeting estrogen receptor-α

Abstract

One new (compound 3) along with two previously known ursane type triterpenoids (compounds 1 and 2) were purified by chromatographic techniques from ethyl acetate extract of aerial parts of Potentilla atrosanguniea and characterized by HRMS, 1 D and 2 D-NMR. Compounds 1 (ursolic acid), 2 (euscaphic acid) and 3 (3α,20α-dihydroxy 2-oxo-urs-12-en-28-oic acid) were tested for their antiproliferative activity along with standard bazedoxifene. Compounds 1 and 3 were found to be of higher activity (3.71 and 6.05 μg/mL) as compared to compound 2 and bazedoxifene (IC₅₀: 24.53 and 17.87 μg/mL). Anti-estrogenic activity of three compounds on breast cancer (BC) were studied in vitro by accessing their antiproliferative activity and binding with estrogen receptor alpha (ER-α). All three compounds have effective binding affinity towards ER-α and decreased cell growth by downregulating the expression of mRNA and its translational protein as tested by semi-qRT-PCR and western blotting. In terms of effectiveness compounds 1 and 3 were found more active due to their antiproliferative, and antiestrogenic activity as compared to standard bazedoxifene.

Graphical Abstract

Keywords:

• Breast cancer
• estrogen receptor alpha
• Potentilla atrosanguinea
• western blotting
• qRT-PCR

Acknowledgement

Authors are thankful to CSIR, New Delhi for providing grant [38/(1434)/17/EMR-II] for conducting the research. Authors are also thankful to the Honourable Vice - Chancellor for providing the necessary facilities at Central University of Punjab, Bathinda, India.

Disclosure statement

Authors have no conflict of interests.

Additional information

Funding

Authors are thankful to CSIR, New Delhi for providing grant [38/(1434)/17/EMR-II] for conducting the research. Authors are also thankful to the Honourable Vice - Chancellor for providing the necessary facilities at Central University of Punjab, Bathinda, India