Abstract
Background: Retinoids which are vitamin A (Retinol) derivatives have been suggested to mediate the inhibition of cancer cell growth and apoptosis. It has been reported that all trans retinoic acid (ATRA) exhibited suppressive effects on different types of leukemia including chronic myelogenous leukemia.
Objective: In the present study, we aim to find out the effects of 6 synthetic N-(3,5,5,8,8-pentamethyl-5,6,7,8- tetrahydronaphthalene-2-yl)-carboxamide derivatives (compound 6-12) on cell viability and apoptotic pathways in K562 human chronic myelogenous leukemia cell line.
Methods: Cell viability and apoptosis were examined by spectrophotometric thiazolyl blue tetrazolium bromide (MTT) and caspase-3 assay, western blot, RT-PCR and flow cytometry.
Results: Our results indicated that compound 6 (5-(1,2-Dithiolan-3-yl)-N-(3,5,5,8,8-pentamethyl-5,6,7,8- tetrahydronaphthalen-2-yl)pentanamide), 8 (4-(3,4-Dimethoxyphenyl)-N-(3,5,5,8,8-pentamethyl-5,6,7,8- tetrahydronaphthalen-2-yl)butanamide) and 11 (E-3-(4-Hydroxy-3-methoxyphenyl)-N-(3,5,5,8,8-pentamethyl- 5,6,7,8-tetrahydronaphthalen-2-yl)acrylamide) exhibited apoptotic effects in K562 human chronic myelogenous leukemia cell line and induced caspase 3, PARP cleavage, Bax/Bcl-2 ratio, Bad and Bim gene expressions.
Conclusion: Some retinoid derivatives tested in this study induced apoptosis of K562 cells which suggest that these compounds may serve as potential agents in the treatment of chronic myelogenous leukemia.
Keywords: Retinoids, chronic myelogenous leukemia, apoptosis, cancer, K562, tetrahydronaphthalene.
Anti-Cancer Agents in Medicinal Chemistry
Title:Apoptotic Effects of Some Tetrahydronaphthalene Derivatives on K562 Human Chronic Myelogenous Leukemia Cell Line
Volume: 17 Issue: 14
Author(s): Asli Koc*, Tulin Ozkan*, Yalda Hekmatshoar, A. Selen Gurkan-Alp, Fugen Aktan, Zeliha Buyukbingol, Asuman Sunguroglu, Erdem Buyukbingol and Arzu Zeynep Karabay*
Affiliation:
- Department of Biochemistry, Faculty of Pharmacy, Ankara University, Ankara,Turkey
- Department of Medical Biology, Faculty of Medicine, Ankara University, Ankara,Turkey
- Department of Biochemistry, Faculty of Pharmacy, Ankara University, Ankara,Turkey
Keywords: Retinoids, chronic myelogenous leukemia, apoptosis, cancer, K562, tetrahydronaphthalene.
Abstract: Background: Retinoids which are vitamin A (Retinol) derivatives have been suggested to mediate the inhibition of cancer cell growth and apoptosis. It has been reported that all trans retinoic acid (ATRA) exhibited suppressive effects on different types of leukemia including chronic myelogenous leukemia.
Objective: In the present study, we aim to find out the effects of 6 synthetic N-(3,5,5,8,8-pentamethyl-5,6,7,8- tetrahydronaphthalene-2-yl)-carboxamide derivatives (compound 6-12) on cell viability and apoptotic pathways in K562 human chronic myelogenous leukemia cell line.
Methods: Cell viability and apoptosis were examined by spectrophotometric thiazolyl blue tetrazolium bromide (MTT) and caspase-3 assay, western blot, RT-PCR and flow cytometry.
Results: Our results indicated that compound 6 (5-(1,2-Dithiolan-3-yl)-N-(3,5,5,8,8-pentamethyl-5,6,7,8- tetrahydronaphthalen-2-yl)pentanamide), 8 (4-(3,4-Dimethoxyphenyl)-N-(3,5,5,8,8-pentamethyl-5,6,7,8- tetrahydronaphthalen-2-yl)butanamide) and 11 (E-3-(4-Hydroxy-3-methoxyphenyl)-N-(3,5,5,8,8-pentamethyl- 5,6,7,8-tetrahydronaphthalen-2-yl)acrylamide) exhibited apoptotic effects in K562 human chronic myelogenous leukemia cell line and induced caspase 3, PARP cleavage, Bax/Bcl-2 ratio, Bad and Bim gene expressions.
Conclusion: Some retinoid derivatives tested in this study induced apoptosis of K562 cells which suggest that these compounds may serve as potential agents in the treatment of chronic myelogenous leukemia.
Export Options
About this article
Cite this article as:
Koc Asli*, Ozkan Tulin *, Hekmatshoar Yalda , Gurkan-Alp Selen A., Aktan Fugen, Buyukbingol Zeliha, Sunguroglu Asuman , Buyukbingol Erdem and Karabay Zeynep Arzu*, Apoptotic Effects of Some Tetrahydronaphthalene Derivatives on K562 Human Chronic Myelogenous Leukemia Cell Line, Anti-Cancer Agents in Medicinal Chemistry 2017; 17 (14) . https://dx.doi.org/10.2174/1871521409666170412122811
DOI https://dx.doi.org/10.2174/1871521409666170412122811 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Targeting Glioblastoma: The Current State of Different Therapeutic Approaches
Current Neuropharmacology CD26/Dipeptidyl Peptidase IV as a Novel Therapeutic Target for Cancer and Immune Disorders
Mini-Reviews in Medicinal Chemistry Role of P-Glycoprotein in the Intestinal Absorption of Tanshinone IIA, a Major Active Ingredient in the Root of Salvia miltiorrhiza Bunge
Current Drug Metabolism Interactions of Iron Oxide Nanoparticles with the Immune System: Challenges and Opportunities for their Use in Nano-oncology
Current Pharmaceutical Design Differential Enhancement of T Helper Type 1 (Th1)/Th2 Cytokine Production by Natural Killer T Cells Through Negative Feedback Regulation with Cytokine-conditioned Dendritic Cells
Current Immunology Reviews (Discontinued) MicroRNAs Patents: The Road From Bench to Bedsides for Cancer Treatment
Recent Patents on DNA & Gene Sequences Gut Microbiota of Obese, Type 2 Diabetic Individuals is Enriched in Faecalibacterium prausnitzii, Akkermansia muciniphila and Peptostreptococcus anaerobius after Weight Loss
Endocrine, Metabolic & Immune Disorders - Drug Targets Mechanisms for Targeted Delivery of Nanoparticles in Cancer
Current Pharmaceutical Design Impact of SINEs and LINEs on the Mammalian Genome
Current Genomics FAK and Nanog Cross Talk with p53 in Cancer Stem Cells
Anti-Cancer Agents in Medicinal Chemistry Implication of CYP24A1 Splicing in Breast Cancer
Anti-Cancer Agents in Medicinal Chemistry HDAC Inhibitors-New Generation of Target Specific Treatment
Mini-Reviews in Medicinal Chemistry Nutrition in Adult Patients with Inflammatory Bowel Disease
Current Drug Targets Smart Inulin-Based Polycationic Nanodevices for siRNA Delivery
Current Drug Delivery Chemical and Medicinal Versatility of Dithiocarbamates: An Overview
Mini-Reviews in Medicinal Chemistry Statins and Protein Prenylation in Cancer Cell Biology and Therapy
Anti-Cancer Agents in Medicinal Chemistry Recent Innovations in Antibody-Mediated, Targeted Particulate Nanotechnology and Implications for Advanced Visualisation and Drug Delivery
Current Nanoscience Impact of Nutrients on the Functioning of Intestinal Goblet Cells: Health and Therapeutic Perspectives
Current Nutrition & Food Science Defective HIF Signaling Pathway and Brain Response to Hypoxia in Neurodegenerative Diseases: Not an “Iffy” Question!
Current Pharmaceutical Design Rational Targeting of Peroxisome Proliferating Activated Receptor Subtypes
Current Medicinal Chemistry