Purpose The aim of this study is to detect apoptotic and cytotoxic/antiproliferative effects of a ligand substance and its metal derivatives. The substances were investigated by using an h-ras oncogene transformed rat embryo fibroblast cell line (5RP7). Methods The cytotoxic influences of dipyrido[3,2-a:2',3'c]phenazine ligand, dipyrido[3,2-a:2',3'c] phenazine-platinum(II) complex ([Pt(dppz)Cl]) and dipyrido[3,2-a:2',3'c] phenazine-gold(III) complex ([Au(dppz)Cl]Cl) were determined with MTT (3[4,5-dimetiltiyazol2-yl]-2,5-difeniltetrazolyum bromid) assay on 5RP7 cells. Results Dipyrido[3,2-a:2',3'c] phenazine, dipyrido[3,2-a:2',3'c] phenazine-platinum(II) complex ([Pt(dppz)Cl]) and dipyrido[3,2-a:2',3'c] phenazine-gold(III) complexes ([Au(dppz)Cl]Cl) caused significant increase in cytotoxicity in a dose and time dependent manner. The effects of dipyridophenazine ligand (dppz) and its metal derivatives on apoptosis were monitorized using cytotoxic dose (10 μM) DAPI fluorescent staining. It was shown that dppz and its compounds induced apoptosis. Conclusions These findings show that dpzz and its complexes can be studied as novel alternative chemotherapeutics in cancer treatment.
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http://dx.doi.org/10.1007/s10637-017-0559-4 | DOI Listing |
Cureus
November 2024
Child Psychiatry, Adana City Training and Research Hospital, Adana, TUR.
Objective: Autism Spectrum Disorder (ASD) is a neurodevelopmental condition that emerges in early childhood and is characterized by difficulties in social communication, repetitive behaviors, and restricted interests. The Ras homolog (Rho)/Rho-kinase signaling pathway plays a critical role in maintaining synaptic structure and function, as it regulates the actin cytoskeleton. This study aims to investigate the expression of the Ras homolog (Rho) family member A (), Rho-kinase 1 (), and Rho-kinase 2 () genes within this pathway in relation to ASD.
View Article and Find Full Text PDFJ Environ Manage
December 2024
Department of Orthopedics, Lanzhou University Second Hospital, Lanzhou University, Lanzhou, Gansu, 730030, PR China; The Second Clinical School, Lanzhou University, Lanzhou, Gansu, 730030, PR China; Orthopaedics Key Laboratory of Gansu Province, Lanzhou, Gansu, 730030, PR China. Electronic address:
Polyethylene terephthalate microplastics (PET-MPs) have emerged as a significant environmental concern due to their persistence and potential health hazards. Their role in degenerative diseases, particularly intervertebral disc degeneration (IVDD), remains poorly understood, highlighting the need for systematic evaluation of their molecular toxicity. In this study, network toxicology and molecular docking approaches were applied to investigate the toxicological mechanisms of PET-MPs-induced IVDD.
View Article and Find Full Text PDFFront Biosci (Landmark Ed)
December 2024
Research Centre for Medical Genetics, 115522 Moscow, Russia.
Background: There is a growing interest in exploring the biological characteristics of nanoparticles and exploring their potential applications. However, there is still a lack of research into the potential genotoxicity of fullerene derivatives and their impact on gene expression in human cells. In this study, we investigated the effects of a water-soluble fullerene derivative, C60[C6H4SCH2COOK]5H (F1), on human embryonic lung fibroblasts (HELF).
View Article and Find Full Text PDFDrug Des Devel Ther
December 2024
The First Affiliated Hospital of Zhejiang Chinese Medical University (Zhejiang Provincial Hospital of Chinese Medicine), Hangzhou, Zhejiang, 310006, People's Republic of China.
Purpose: Diabetes mellitus-induced erectile dysfunction (DMED) lacks targeted therapies. This study investigates the mechanisms and targets of Radix Paeoniae Rubra and Radix Angelicae Sinensis Granules (RAG) in treating DMED using network pharmacology and animal models.
Methods: We identified RAG's active ingredients and potential targets from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform.
Trends Cancer
December 2024
Charité - Universitätsmedizin Berlin, Institute of Pathology, Berlin, Germany; German Cancer Consortium (DKTK), Partner Site Berlin, German Cancer Research Center (DKFZ), Heidelberg, Germany; Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA; Department of Pharmacology, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA. Electronic address:
In 1982, the RAS genes HRAS and KRAS were discovered as the first human cancer genes, with KRAS later identified as one of the most frequently mutated oncogenes. Yet, it took nearly 40 years to develop clinically effective inhibitors for RAS-mutant cancers. The discovery in 2013 by Shokat and colleagues of a druggable pocket in KRAS paved the way to FDA approval of the first covalently binding KRAS inhibitors, sotorasib and adagrasib, in 2021 and 2022, respectively.
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