Laboratory of Natural Product Chemistry, Department of Pharmaceutical Sciences & Natural Products, Central University of Punjab, Ghudda, India.
Department of Microbiology, Central University of Punjab, Ghudda, India.
Nat Prod Res. 2022 Sep;36(17):4358-4363. doi: 10.1080/14786419.2021.1986495. Epub 2021 Oct 4.
One new (compound ) along with two previously known ursane type triterpenoids (compounds and ) were purified by chromatographic techniques from ethyl acetate extract of aerial parts of and characterized by HRMS, 1 D and 2 D-NMR. Compounds (ursolic acid), (euscaphic acid) and (3,20-dihydroxy 2-oxo-urs-12-en-28-oic acid) were tested for their antiproliferative activity along with standard bazedoxifene. Compounds and were found to be of higher activity (3.71 and 6.05 μg/mL) as compared to compound and bazedoxifene (IC: 24.53 and 17.87 μg/mL). Anti-estrogenic activity of three compounds on breast cancer (BC) were studied by accessing their antiproliferative activity and binding with estrogen receptor alpha (ER-). All three compounds have effective binding affinity towards ER- 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 and were found more active due to their antiproliferative, and antiestrogenic activity as compared to standard bazedoxifene.
一种新的（化合物）以及两种先前已知的五环三萜（化合物和）通过色谱技术从地上部分的乙酸乙酯提取物中分离出来，并通过高分辨率质谱、1D 和 2D-NMR 进行了表征。化合物（熊果酸）、（euscaphic 酸）和（3,20-二羟基 2-氧代-urs-12-烯-28-羧酸）与标准 bazedoxifene 一起测试了其抗增殖活性。与化合物和 bazedoxifene（IC：24.53 和 17.87μg/mL）相比，化合物和（ursolic acid）具有更高的活性（3.71 和 6.05μg/mL）。通过评估其对乳腺癌（BC）的增殖活性和与雌激素受体 alpha（ER-）的结合，研究了三种化合物的抗雌激素活性。所有三种化合物都对 ER-具有有效的结合亲和力，并通过下调 mRNA 及其翻译蛋白的表达来降低细胞生长，这通过半定量 qRT-PCR 和 Western blot 进行了测试。就有效性而言，与标准 bazedoxifene 相比，化合物和由于其抗增殖和抗雌激素活性而被发现更有效。
