The expression of the multidrug resistance (MDR) proteins may influence the outcome of treatment in patients with acute leukemia. The aim of this study was to determine the IC50 of cytotoxic drugs (cytosine arabinoside, ara-C and daunorubicin, dnr) using the in vitro 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)2H-tetrazolium, inner salt (MTS) assay method. A total of 82 newly diagnosed acute leukemia cases (43 adult myeloid leukaemia, AML cases and 39 acute lymphoblastic leukaemia, ALL cases) and 16 relapsed cases (8 AML cases and 8 ALL cases) were studied. The MTS assay was performed using two cytotoxic drugs, dnr and ara-C. Cells were incubated with different concentrations of drugs for 4 days and the IC50 was extrapolated from the viability curve. In newly diagnosed cases, we found that childhood ALL samples showed higher IC50 values of dnr (0.040 +/- 2.320) compared to adult AML samples (0.021 +/- 0.158). In contrast, newly diagnosed adult AML samples showed higher IC50 values of ara-C (0.157 +/- 0.529) compared to childhood ALL samples (0.100 +/- 2.350). In relapsed cases, two samples of childhood ALL showed IC50 values of dnr (0.910 +/- 1.760) and ara-C (1.310 +/- 2.390), which was higher compared to childhood AML samples (0.129 +/- 0.214 and 0.210 +/- 0.003, respectively). However, there was no correlation between IC50 values of these drugs tested with clinical outcome. In conclusion, we found that MTS assay is an easy, rapid and non laborious method to study in vitro drug resistance in acute leukaemia cases.
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Background: Alzheimer's Disease (AD) is the leading form of senile dementia, affecting ∼6 million Americans and having a national economic impact of $321 billion, numbers expected to double by 2050. The major pathological hallmarks of AD include Amyloid Beta (Aβ) plaques and Tau neurofibrillary tangles (NFT). The first goal of this research was to develop novel forms of carbon dots (CD) using various precursors.
View Article and Find Full Text PDFAlzheimers Dement
December 2024
Chitkara College of Pharmacy, Chitkara University, Rajpura, Punjab, India.
Background: The present study recapitulates the potency of the novel synthesized piperazine-benzoquinone derivative as a lead molecule selectively targeting AChE along with the antioxidative potential for the management of cognitive decline in Alzheimer's disease.
Method: Novel piperazine-benzoquinone derivative was synthesized implementing appropriate synthetic procedures and was characterized by various spectral and elemental techniques. The purity of this synthetic analogue was ascertained by TLC, melting point determination and elemental analyses.
J Cancer
January 2025
Department of Pharmacology, The Yancheng Clinical College of Xuzhou Medical University, The First people's Hospital of Yancheng, Yancheng, China.
Longikaurin A (LK-A), a naturally occurring ent-kaurane diterpenoid, has been identified as a promising anti-cancer agent. This study aims to elucidate the anti-tumorigenic effects of LK-A on oral squamous cell carcinoma (OSCC) cells and to unravel its underlying mechanisms. assays, including CCK-8 and EdU, were performed to assess cell viability and proliferation.
View Article and Find Full Text PDFTurk J Chem
November 2024
Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto, Japan.
The epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), pioneer members of the receptor tyrosine kinase subfamily, are frequently mutated and/or overexpressed in several types of human cancers, including nonsmall cell lung cancer (NSCLC) and breast cancer, which are leading causes of cancer-related deaths worldwide. EGFR and HER2-focused anti-NSCLC and antibreast cancer studies encouraged us to search for new potential agents. For this purpose, in the current work, naphthalene-linked pyrazoline-thiazole hybrids (- and -) were synthesized and examined for their antiproliferative effects on A549 NSCLC and MCF-7 breast cancer cell lines.
View Article and Find Full Text PDFNat Prod Res
January 2025
Chongqing Key Laboratory of New Drug Screening from Traditional Chinese Medicine, Integrative Science Center of Germplasm Creation in Western China (Chongqing) Science City, SWU-TAAHC Medicinal Plant Joint R&D Centre, College of Pharmaceutical Sciences, Southwest University, Chongqing, P. R. China.
Two new polyacetylenes, (5,12)-14-hydroxytetradeca-5,12-dien-8,10-diyn-1-yl 3-methylbut-2-enoate () and 5, 1'-(6,12)-1-hydroxytetradeca-6,12-dien-8,10-diyn-5-yl 2-methylbutanoate (), together with two known ones, (2,8)-12--methylbutyryltetradeca-2,8-diene-4,6-diyne-1,14-diol (), and ()-5-[5-(but-3-en-1-yn-1-yl)thiophen-2-yl]pent-2-en-4-yn-1-yl acetate () were isolated from the ethyl acetate extract of the roots of by various chromatographic methods, such as normal phase silica gel column, MPLC, and semi-preparative HPLC. Their structures were identified by kinds of spectroscopic methods including 1D NMR, 2D NMR, IR, UV, HR-ESI-MS, and ECD. Compound exhibited cytotoxic activities in HepG2 and Huh7 cells with IC values of 20.
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