Abstract
Background: Cancer is characterized by uncontrolled cell division caused by dysregulation of cell proliferation. Therefore, agents that impair cancer cell proliferation could have potential therapeutic value. Higher plants are considered to be a good source of anticancer agents, and several clinically tested chemotherapeutic agents have been isolated from plants or derived from constituents of plant origin.
Methods: In the present study, a prenylated flavone (isoglabratephrin) was isolated from aerial parts of Tephrosia apollinea using a bioassay-guided technique. Chemical structure of the isolated compound was elucidated using spectroscopic techniques (NMR, IR, and LC-MC), elemental analysis and confirmed by using single crystal X-ray analysis. The antiproliferative effect of isoglabratephrin was tested using three human cancer cell lines (prostate (PC3), pancreatic (PANC-1), and colon (HCT-116) and one normal cell line (human fibroblast). Results: Isoglabratephrin displayed selective inhibitory activity against proliferation of PC3 and PANC-1 cells with median inhibitory concentration values of 20.4 and 26.6 μg/ml, respectively. Isoglabratephrin demonstrated proapoptotic features, as it induced chromatin dissolution, nuclear condensation, and fragmentation. It also disrupted the mitochondrial membrane potential in the treated cancer cells. Conclusion: Isoglabratephrin could be a new lead to treat human prostate (PC3) and pancreatic (PANC-1) malignancies.Keywords: Isoglabratephrin, anticancer, apoptosis, X-ray crystallography, prenylated flavone.
Anti-Cancer Agents in Medicinal Chemistry
Title:Colorectal, Prostate and Pancreas Human Cancers Targeted Bioassay-guided Isolations and Characterization of Chemical Constituents from Tephrosia apollinea
Volume: 17 Issue: 4
Author(s): Loiy Elsir A. Hassan*, Muhammad Adnan Iqbal, Saad S. Dahham, Yasser M. Tabana, Mohamed B. Khadeer Ahamed and Amin M.S. Abdul Majid
Affiliation:
- EMAN Testing and Research Laboratory, School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800, Minden, Pulau Penang,Malaysia
Keywords: Isoglabratephrin, anticancer, apoptosis, X-ray crystallography, prenylated flavone.
Abstract: Background: Cancer is characterized by uncontrolled cell division caused by dysregulation of cell proliferation. Therefore, agents that impair cancer cell proliferation could have potential therapeutic value. Higher plants are considered to be a good source of anticancer agents, and several clinically tested chemotherapeutic agents have been isolated from plants or derived from constituents of plant origin.
Methods: In the present study, a prenylated flavone (isoglabratephrin) was isolated from aerial parts of Tephrosia apollinea using a bioassay-guided technique. Chemical structure of the isolated compound was elucidated using spectroscopic techniques (NMR, IR, and LC-MC), elemental analysis and confirmed by using single crystal X-ray analysis. The antiproliferative effect of isoglabratephrin was tested using three human cancer cell lines (prostate (PC3), pancreatic (PANC-1), and colon (HCT-116) and one normal cell line (human fibroblast). Results: Isoglabratephrin displayed selective inhibitory activity against proliferation of PC3 and PANC-1 cells with median inhibitory concentration values of 20.4 and 26.6 μg/ml, respectively. Isoglabratephrin demonstrated proapoptotic features, as it induced chromatin dissolution, nuclear condensation, and fragmentation. It also disrupted the mitochondrial membrane potential in the treated cancer cells. Conclusion: Isoglabratephrin could be a new lead to treat human prostate (PC3) and pancreatic (PANC-1) malignancies.Export Options
About this article
Cite this article as:
Hassan Elsir A. Loiy*, Iqbal Adnan Muhammad, Dahham S. Saad, Tabana M. Yasser, Ahamed B. Khadeer Mohamed and Majid M.S. Abdul Amin, Colorectal, Prostate and Pancreas Human Cancers Targeted Bioassay-guided Isolations and Characterization of Chemical Constituents from Tephrosia apollinea, Anti-Cancer Agents in Medicinal Chemistry 2017; 17 (4) . https://dx.doi.org/10.2174/1871520616666160926113711
DOI https://dx.doi.org/10.2174/1871520616666160926113711 |
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
-
Strategies for the Design of Non-peptide CCK2 Receptor Agonist and Antagonist Ligands
Current Topics in Medicinal Chemistry The Yin and Yang of microRNA Assay Methods
MicroRNA Metalloproteinases and Metalloproteinase Inhibitors in Age-Related Diseases
Current Pharmaceutical Design Immune System, Cell Senescence, Aging and Longevity - Inflamm-Aging Reappraised
Current Pharmaceutical Design Let-7a Could Serve as A Biomarker for Chemo-Responsiveness to Docetaxel in Gastric Cancer
Anti-Cancer Agents in Medicinal Chemistry Caffeic Acid, A Versatile Pharmacophore: An Overview
Mini-Reviews in Medicinal Chemistry Anti-Gene Strategies to Down-Regulate Gene Expression in Mammalian Cells
Current Pharmaceutical Design Natural Antioxidants: Therapeutic Prospects for Cancer and Neurological Diseases
Mini-Reviews in Medicinal Chemistry ABC Transporters in Neurological Disorders: An Important Gateway for Botanical Compounds Mediated Neuro-Therapeutics
Current Topics in Medicinal Chemistry miRNAs in Gastrointestinal and Liver Cancers: Their Perspectives and Clinical Applications
Current Pharmaceutical Design Prokinetic Agents and QT Prolongation: A Familiar Scene with New Actors
Current Drug Safety Neutralizing Endogenous VEGF Following Traumatic Spinal Cord Injury Modulates Microvascular Plasticity but not Tissue Sparing or Functional Recovery
Current Neurovascular Research From Single- to Multi-Target Drugs in Cancer Therapy: When Aspecificity Becomes an Advantage
Current Medicinal Chemistry Pharmacotherapies to Manage Bone Loss-Associated Diseases: A Quest for the Perfect Benefit-to-Risk Ratio
Current Medicinal Chemistry Anticancer Effects of the Organosilicon Multidrug Resistance Modulator SILA 421
Anti-Cancer Agents in Medicinal Chemistry Application of Bacterial Nanocellulose in Cancer Drug Delivery: A Review
Current Pharmaceutical Design Temporal Expression of miRNAs in Laser Capture Microdissected Palate Medial Edge Epithelium from Tgfβ3<sup>-/-</sup> Mouse Fetuses
MicroRNA Obesity and Inflammation: Colorectal Cancer Engines
Current Molecular Pharmacology Overview of Angiogenesis and the use of Bevacizumab in Patients with Malignant Gliomas
Current Signal Transduction Therapy Role of Histone Deacetylases (HDACs) in Epilepsy and Epileptogenesis
Current Pharmaceutical Design