Assessment of the anticancer function of Coronilla orientalis MILLER through comprehensive in vitro and computational studies DOI Creative Commons
Halil I. Ciftci, Ayhan Oral, Yalçın Çoşkun

et al.

Turkish Journal of Biochemistry, Journal Year: 2025, Volume and Issue: unknown

Published: May 22, 2025

Abstract Objectives Although many synthetic anticancer drugs are available, a significant proportion of human therapeutics in the armamentarium derived from natural products. The aim this study to examine effects compounds against non-small cell lung cancer (NSCLC) and breast cancer, which remain among world’s greatest obstacles. Methods Coronilla orientalis MILLER (CO) was collected Erzincan, Türkiye, prepared, extracted with 70 % ethanol. CO then tested A549 NSCLC MCF-7 cells using MTT assay. To explore its potential mechanism, apoptotic kinase inhibitory were investigated Annexin V/ethidium homodimer III staining assay ADP-Glo assay, respectively. Molecular docking studies also performed for several major components ATP binding site EGFR. Results results showed that CO, IC 50 values 2.37 ± 0.59 μg/mL 7.60 1.18 μg/mL, exhibited activity cells, selectively cytotoxic between Jurkat PBMCs (healthy). CO-treated found undergo apoptosis inhibit revealed interaction some defined key residues Conclusions Taken together, research has shown great deal as an inhibitor function warrants further investigation.

Language: Английский

A Structural Insight Into Two Important ErbB Receptors (EGFR and HER2) and Their Relevance to Non‐Small Cell Lung Cancer DOI Creative Commons

Edanur Topalan,

Ahmet Büyükgüngör,

Melih Çiğdem

et al.

Archiv der Pharmazie, Journal Year: 2025, Volume and Issue: 358(4)

Published: April 1, 2025

ABSTRACT The epidermal growth factor receptor (EGFR) family, comprising tyrosine kinases (RTK) such as EGFR and HER2, plays a critical role in various signaling pathways related to cell proliferation, differentiation, growth. overactivation due aberrant can lead cancers, including non‐small lung cancer (NSCLC). To develop treatment for EGFR‐related NSCLC, several kinase inhibitors (TKIs) were designed: gefitinib, erlotinib, first‐generation; neratinib, dacomitinib second‐generation; osimertinib, lazertinib third‐generation, examples. However, the acquired resistance by mutations T790M C797S together with exon 20 insertion mutations, these drugs do not provide promising results NSCLC patients. development of fourth‐generation like EAI045 further innovative overcome this problem is must cure NSCLC. Among these, pyrazoline‐thiazole scaffolds are found effective EGFR‐HER2 against making them drug candidates. Although structures obtained so far family meaningful insights into mechanisms, quality quantity insufficient elucidate complete functions This review evaluates investigates their relation

Language: Английский

Citations

0
Assessment of the anticancer function of Coronilla orientalis MILLER through comprehensive in vitro and computational studies DOI Creative Commons
Halil I. Ciftci, Ayhan Oral, Yalçın Çoşkun

et al.

Turkish Journal of Biochemistry, Journal Year: 2025, Volume and Issue: unknown

Published: May 22, 2025

Abstract Objectives Although many synthetic anticancer drugs are available, a significant proportion of human therapeutics in the armamentarium derived from natural products. The aim this study to examine effects compounds against non-small cell lung cancer (NSCLC) and breast cancer, which remain among world’s greatest obstacles. Methods Coronilla orientalis MILLER (CO) was collected Erzincan, Türkiye, prepared, extracted with 70 % ethanol. CO then tested A549 NSCLC MCF-7 cells using MTT assay. To explore its potential mechanism, apoptotic kinase inhibitory were investigated Annexin V/ethidium homodimer III staining assay ADP-Glo assay, respectively. Molecular docking studies also performed for several major components ATP binding site EGFR. Results results showed that CO, IC 50 values 2.37 ± 0.59 μg/mL 7.60 1.18 μg/mL, exhibited activity cells, selectively cytotoxic between Jurkat PBMCs (healthy). CO-treated found undergo apoptosis inhibit revealed interaction some defined key residues Conclusions Taken together, research has shown great deal as an inhibitor function warrants further investigation.

Language: Английский

Citations

0