Biological Evaluation of Newly synthesized Spebrutinibm Analogues: Potential Candidates with Enhanced Activity and Reduced Toxicity Profiles.

Abstract

Background: Undoubtedly, cancer is regarded as a major concern for researchers alongside the whole humanity for its high mortality rates. At this moment, there must be some researchers working hard to design, synthesize, and biologically investigate the effects of some potential candidates to fight back cancer. Materials and methods: In previous unpublished work, the authors successfully designed, synthesized, characterized a potential two spebrutinib analogues. Consequently, these analogues were evaluated with the employment of MCF-7, HCT116, and MDCK cell lines. Results: In respect to the spebrutinib standard, one of these analogues has superior activity against MCF-7 cell line (IC50; 10.744 µg/mL against 13.566 µg/mL for spebrutinib) and an enhanced toxicity profile on MDCK cell line (IC50; 8.653 mg/mL against 4.011 mg/mL for spebrutinib). Conclusion: The two compounds showed good activity against breast and colon cell lines and enhanced toxicity profile against normal kidney cell line in respect to spebrutinib standard.

Investigation of the association between habitual dietary FODMAP intake, metabolic parameters, glycemic status, and anthropometric features among apparently healthy overweight and obese individuals

“…This study found that higher consumption of moderate FODMAP and low FODMAP groups was associated with lower WHR and higher FFM. To explain this association, we have proposed the following hypothesis: a moderate increase in FODMAP consumption was linked to an absolute rise and a relative abundance of microbiota that produce SCFAs [ 41 – 43 ]. Peroxisome proliferator-activated receptor-γ (PPAR-γ) is a transcription factor whose activity can be modulated by SCFA in this.…”

Dietary Antioxidant Quality Score (DAQS), serum lipids, markers of glucose homeostasis, blood pressure and anthropometric features among apparently metabolically healthy obese adults in two metropolises of Iran (Tabriz and Tehran): a cross-sectional study

“…A prospective cohort study which included 12,245 individuals found that the risk of hypertension was significantly increased in the lowest quartile of vitamin A intake levels [68]. Nitric oxide (NO) is crucial for controlling blood pressure and flow because to its vasodilatory actions [69], NO pathways were shown to be affected by vitamin A, which may contribute to endothelial function [66,70]. Some of the mechanistic pathways involved in the association between DAQS and blood pressure is illustrated in Figure 1.…”

The Evaluation of Antiproliferative Effect of Imatinib Derivatives against Breast and Colon Cell-Lines

“…Obeying a restricted protocol that was revealed extensively in previous work, 14 the cell lines were prepared, and the time of the drug candidate application was optimized to be 24 hours. After that, the MTT stock and working solutions were prepared to get homogenized solutions of the cell-medium with 10% MTT to be utilized in the cell-lines.…”

“…[11][12][13] In previous work, our team has designed, synthesized, and characterized three potential imatinib derivatives. 14 In this work, the authors aimed to evaluate these derivatives biologically.…”