Abstract
Introduction: In the present study, we analyzed anti-proliferative and apoptosis induction activity of five phenolic compounds: echisoside, pleoside, chlorogenic acid, 4,5-Di-O-caffeoylquinic acid, and cynarin on AGS (adenocarcinoma gastric) cell line.
Method: These phenolic compounds were isolated from methanol extract of Dorema glabrum root. An MTT assay was conducted to evaluate the inhibitory effect on cancer cells. EB/AO staining was done to assess the mode of cell death and morphological changes of the cells’ nuclei. Cell cycle distribution of the cells was analyzed by flow cytometry, and for further confirmation of the pathway, mRNA levels of apoptosis cascade players were quantified by qRT-PCR.
Result: We found that echisoside, pleoside, chlorogenic acid, 4,5-Di-O-caffeoylquinic acid, and cynarin inhibited the proliferation of AGS cancer cells in vitro. Our data revealed that these compounds triggered morphological changes characteristic of apoptotic cell death. These compounds up-regulated bax and caspase3 expression and down-regulated cyclin D1, bcl2, VEGFA, c-myc and survivin. Moreover, cell population increased at the G1 phase, and a number of cells at the G2/M phase of the cell cycle decreased after treatment.
Conclusion: All these data suggest that phenolic compounds have a cytotoxic effect on gastric cancer cells and could trigger apoptosis. Besides cytotoxic activity, they could potentially arrest the cell cycle at the G1 phase.
Keywords: Caffeoylquinic acid, phloroacetophenone glycosides, gastric cancer, apoptosis, cell cycle.
Anti-Cancer Agents in Medicinal Chemistry
Title:Cell Cycle Arrest and Apoptosis Induction of Phloroacetophenone Glycosides and Caffeoylquinic Acid Derivatives in Gastric Adenocarcinoma (AGS) Cells
Volume: 18 Issue: 4
Author(s): Naser Jafari, Seyed Jalal Zargar*, Mohammad-Reza Delnavazi and Narguess Yassa
Affiliation:
- Department of Cell & Molecular Biology, School of Biology, College of Science, University of Tehran, Tehran,Iran
Keywords: Caffeoylquinic acid, phloroacetophenone glycosides, gastric cancer, apoptosis, cell cycle.
Abstract: Introduction: In the present study, we analyzed anti-proliferative and apoptosis induction activity of five phenolic compounds: echisoside, pleoside, chlorogenic acid, 4,5-Di-O-caffeoylquinic acid, and cynarin on AGS (adenocarcinoma gastric) cell line.
Method: These phenolic compounds were isolated from methanol extract of Dorema glabrum root. An MTT assay was conducted to evaluate the inhibitory effect on cancer cells. EB/AO staining was done to assess the mode of cell death and morphological changes of the cells’ nuclei. Cell cycle distribution of the cells was analyzed by flow cytometry, and for further confirmation of the pathway, mRNA levels of apoptosis cascade players were quantified by qRT-PCR.
Result: We found that echisoside, pleoside, chlorogenic acid, 4,5-Di-O-caffeoylquinic acid, and cynarin inhibited the proliferation of AGS cancer cells in vitro. Our data revealed that these compounds triggered morphological changes characteristic of apoptotic cell death. These compounds up-regulated bax and caspase3 expression and down-regulated cyclin D1, bcl2, VEGFA, c-myc and survivin. Moreover, cell population increased at the G1 phase, and a number of cells at the G2/M phase of the cell cycle decreased after treatment.
Conclusion: All these data suggest that phenolic compounds have a cytotoxic effect on gastric cancer cells and could trigger apoptosis. Besides cytotoxic activity, they could potentially arrest the cell cycle at the G1 phase.
Export Options
About this article
Cite this article as:
Jafari Naser , Zargar Jalal Seyed *, Delnavazi Mohammad-Reza and Yassa Narguess , Cell Cycle Arrest and Apoptosis Induction of Phloroacetophenone Glycosides and Caffeoylquinic Acid Derivatives in Gastric Adenocarcinoma (AGS) Cells, Anti-Cancer Agents in Medicinal Chemistry 2018; 18 (4) . https://dx.doi.org/10.2174/1871520618666171219121449
DOI https://dx.doi.org/10.2174/1871520618666171219121449 |
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
-
MIF and CD74 - Suitability as Clinical Biomarkers
Mini-Reviews in Medicinal Chemistry Radionuclide Imaging in Drug Development
Current Pharmaceutical Design Lactoferricin Derived From Milk Protein Lactoferrin
Current Pharmaceutical Design Oral Hypoglycemics: A Review of Chemicals Used to Treat Type 2 Diabetes
Current Bioactive Compounds Neuroinflammation and its Modulation by Flavonoids
Endocrine, Metabolic & Immune Disorders - Drug Targets Potential Uses of MicroRNA in Lung Cancer Diagnosis, Prognosis, and Therapy
Current Cancer Drug Targets Apoptosis Signaling Pathways in Anticancer Therapy
Current Cancer Therapy Reviews Design and Synthesis of Mannich bases as Benzimidazole Derivatives as Analgesic Agents
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry The Pivotal Role of Nitric Oxide: Effects on the Nervous and Immune Systems
Current Pharmaceutical Design Cheminfomatic-based Drug Discovery of Human Tyrosine Kinase Inhibitors
Current Topics in Medicinal Chemistry The Prolyl-Aminodipeptidases and their Inhibitors as Therapeutic Targets for Fibrogenic Disorders
Mini-Reviews in Medicinal Chemistry Cancer Therapy By Targeting Hypoxia-Inducible Factor-1
Current Cancer Drug Targets Inhaled Biologics: From Preclinical to Product Approval
Current Pharmaceutical Design Graphical Abstracts
Letters in Drug Design & Discovery Modulation of GSTP1-1 Oligomerization by Electrophilic Inflammatory Mediators and Reactive Drugs
Inflammation & Allergy - Drug Targets (Discontinued) Synthesis and Biological Evaluation of 3-Substituted-4-(4-methylthio phenyl)-1HPyrrole Derivatives as Potential Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Potent Chemopreventive Agents Against Pancreatic Cancer
Current Cancer Drug Targets Candida Infections and Human Defensins
Protein & Peptide Letters Inhibition of Polo-Like Kinase 1 by BI2536 Reverses the Multidrug Resistance of Human Hepatoma Cells In Vitro and In Vivo
Anti-Cancer Agents in Medicinal Chemistry Biological and Pharmacological Activities of Iridoids: Recent Developments
Mini-Reviews in Medicinal Chemistry