fig8

Novel <i>N</i>-chloroacetyl-2-pyrazoline analogs with 2-naphthyl and ferrocenyl groups: targeting histamine receptor H1 to overcome colorectal cancer drug resistance

Figure 8. Clac10 (5c) and Clac12 (5e) suppress the growth of HCT116-tumor xenografts in mice. (A) Immunofluorescence reveals that compounds 5c (Clac10) and 5e (Clac12) reduce the number of proliferating cells (Ki67-positive nuclei) and increase the expression of cleaved caspase-3 in HCT116-xenograft tumors in mice; Quantification of Ki-67-positive cells (B) and cleaved caspase-3 staining (C) was performed; (D) Western blot analyses of tissue lysates from animals treated with 5c (Clac10) and 5e (Clac12) show significantly higher levels of cleaved PARP, indicating apoptosis, and reduced p-GSK3B expression, indicating inhibition of histamine-signaling. Data is presented as mean ± SEM. A statistical comparison was performed using an ordinary one-way ANOVA. PARP: Poly (ADP-ribose) polymerase; p-GSK3B: phosphorylated-glycogen synthase kinase 3 beta; SEM: standard error of the mean; ANOVA: analysis of variance.

Cancer Drug Resistance
ISSN 2578-532X (Online)

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