Background: Coumarins are naturally occurring plant metabolites and several synthetic coumarin analogues are known for their various pharmacological properties such as anticoagulant, antimicrobial, anticancer, antioxidant, anti-inflammatory and antiviral properties. Objective; Keeping this promising pharmacological properties in mind, in the present investigation, mono/dihalogenated coumarin analogues CMRN1-CMRN7 have been synthesized and evaluated for their anticancer activity.
Method: The cytotoxicity potential of the test compounds was evaluated against UACC-62, MCF-7 and PBM (Peripheral Blood Mononuclear) cell lines using MTT assay. The apoptotic potential of the coumarin compounds was evaluated against UACC-62 cell by assessing membrane change, mitochondria membrane potential, pro-apoptotic changes were investigated using the AnnexinV-PI staining, JC-1, caspase-3 enzyme kits respectively on flow cytometer.
Results: The test compounds CMRN1, CMRN2, CMRN4 and CMRN5 have strongly suppressed the cell proliferation of UACC-62 and MCF-7 cancer cell lines. Furthermore the test compounds CMRN1, CMRN2, CMRN4 and CMRN5 exerted antiproliferative effects through apoptosis induction against UACC-62.
Conclusion: Compounds CMRN1, CMRN2, CMRN4 and CMRN5 can be considered as lead compounds to arrive at a promising anticancer agents.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.2174/1871520616666160926112508 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Directed evolution of antimicrobial peptides using multi-objective zeroth-order optimization.
Brief Bioinform
November 2024
School of Computer Science and Technology, Harbin Institute of Technology, HIT Campus, Shenzhen University Town, Nanshan District, Shenzhen 518055, Guangdong, China.
Antimicrobial peptides (AMPs) emerge as a type of promising therapeutic compounds that exhibit broad spectrum antimicrobial activity with high specificity and good tolerability. Natural AMPs usually need further rational design for improving antimicrobial activity and decreasing toxicity to human cells. Although several algorithms have been developed to optimize AMPs with desired properties, they explored the variations of AMPs in a discrete amino acid sequence space, usually suffering from low efficiency, lack diversity, and local optimum.
View Article and Find Full Text PDFDeveloping novel Lin28 inhibitors by computer aided drug design.
Cell Death Discov
January 2025
The Vancouver Prostate Centre, Department of Urologic Sciences, University of British Columbia, 2660 Oak Street, Vancouver, BC, V6H 3Z6, Canada.
Lin28 is a key regulator of cancer stem cell gene network that promotes therapy-resistant tumor progression in various tumors. However, no Lin28 inhibitor has been approved to treat cancer patients, urging exploration of novel compounds as candidates to be tested for clinical trials. In this contribution, we applied computer-aided drug design (CADD) in combination with quantitative biochemical and biological assays.
View Article and Find Full Text PDFEnhanced nano-LC-MS for analyzing dansylated oral cancer tissue metabolome dissolved in solvents with high elution strength.
Anal Chim Acta
February 2025
Department of Biochemistry and Molecular Biology, Chang Gung University, Taoyuan, 333, Taiwan; Clinical Proteomics Core Laboratory, LinKou Chang Gung Memorial Hospital, Taoyuan, 333423, Taiwan. Electronic address:
Background: Tissue metabolomics analysis, alongside genomics and proteomics, offers crucial insights into the regulatory mechanisms of tumorigenesis. To enhance metabolite detection sensitivity, chemical isotope labeling (CIL) techniques, such as dansylation, have been developed to improve metabolite separation and ionization in mass spectrometry (MS). However, the dissolution of hydrophobic derivatized metabolites in solvents with high acetonitrile content limits the use of liquid chromatography (LC) systems with small-volume reversed-phase (RP) columns.
View Article and Find Full Text PDFCharacterization of Quality Marker for Mume Fructus Pulp by Ultra-Performance Liquid Chromatography-Quadrupole Time-of-Flight Mass Spectrometry-Based Untargeted Metabolomics Combined With Biological Activities.
Phytochem Anal
January 2025
College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China.
Introduction: As a widely used Chinese herbal medicine, Mume Fructus pulp (MFP) has rich nutritional value and biological activity, but its quality control research is relatively scarce.
Objectives: The objective of the study was to evaluate the quality difference between MFPs from different origins and its adulterant apricot pulp (APP), and to identify potential quality markers.
Methods: The chemical compositions were identified by untargeted metabolomics analysis based on ultra-performance liquid chromatography-quadrupole time-of-flight mass spectrometry combined with feature-based molecular networking.
Assessing chemical exposure risk in breastfeeding infants: An explainable machine learning model for human milk transfer prediction.
Ecotoxicol Environ Saf
January 2025
Department of Pharmacy, Jieyang People's Hospital, Jieyang, China.
Breast milk is essential for infant health, but the transfer of xenobiotic chemicals poses significant risks. Ethical challenges in clinical trials necessitate the use of in vitro predictive models to assess chemical exposure risks in breastfeeding infants. This study introduces an explainable machine learning model to predict the risk of chemical transfer through human milk.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!