Steroidal Dimer by001 Inhibits Proliferation and Migration of Esophageal Cancer Cells via Multiple Mechanisms

Abstract

Following our previous success in identifying new steroid-based anticancer agents, we herein disclosed the structural requirements for retaining high potency against cancer cells and associated modes of action. The structurally novel steroidal dimer by001 inhibited growth of different esophageal cancer cells and colony formation at low micromolar levels, elevated cellular ROS levels and caused mitochondrial dysfunction. Mechanistic studies showed that by001 induced cell death through the mitochondria and death receptor-mediated apoptotic pathways and autophagy induction, as well as inhibited migration.

Knockdown of Kremen2 Inhibits Tumor Growth and Migration in Gastric Cancer

“…The cell viability assay was performed on days 1, 2, 3, 4, and 5. The percent of cytotoxicity was calculated using the following formula: %Cell viability = (absorbance of experimental well-absorbance of blank)/(absorbance of untreated control well-absorbance of blank)×100% ( 12 ).…”

Heterocyclic steroids: Synthetic routes and biological characteristics of steroidal fused bicyclic pyrimidines

“…[32] Also, dimeric steroids (ie, cephalostatin I (8), ritterazines A (9), and crellastatin A ( 10)) (Figure 1) demonstrated potent cytotoxic activities against different cancer cell lines. [33,34] Hence, the efficacy of some dimeric steroids (5) as anti-cancer drugs has been studied by Wang et al [35] since the mechanics of action of the compounds has not been studied on a large scale using MTT assay. Accordingly, dimeric steroid fused to triazolopyrimidine ring system at the Ring-D of steroid skeleton verified potent cytotoxicity against EC109, TE-1, SH-SY5Y, PC-3, SMMC-7721, MGC803, and GES-1 cancer cells relative to the results of DHEA and 5-fluorouracil.…”