Abstract
A physiologically stable thiolate gold(I) derivative [Au(Spyrimidine)(PTA-CH2Ph)]Br has shown inhibition in colon cancer proliferation of Caco-2/TC7, Caco-2/PD7 and HTC-116-luc2 cell lines via apoptotic pathway and S-phase arrest in the cell cycle. Intraperitoneal injection of [Au(Spyrimidine)(PTA-CH2Ph)]Br in athymic nude mice inoculated with HTC-116-luc2 cells prolonged their survival and greatly inhibited tumour growth, near to disappearance. Low concentration of gold in urine and blood were detected in mice after 48 h of administration of 5 mg/kg body weight (bw) of the gold complex and non-organ (kidney and liver) damage has been detected after gold treatment. The results obtained suggested that the thiolate gold(I) derivative shown here could be considered as a candidate for therapeutic treatment in colon cancer.
Keywords: Apoptosis, colon cancer, gold(I), histopathology, in vivo, PTA, Thiolate.
Anti-Cancer Agents in Medicinal Chemistry
Title:In Vivo Anticancer Activity, Toxicology and Histopathological Studies of the Thiolate Gold(I) Complex [Au(Spyrimidine)(PTA-CH2Ph)]Br
Volume: 15 Issue: 6
Author(s): Elena Garcia-Moreno, Sonia Gascon, Jose A. Garcia de Jalon, Eduardo Romanos, M Jesus Rodriguez-Yoldi, Elena Cerrada and Mariano Laguna
Affiliation:
Keywords: Apoptosis, colon cancer, gold(I), histopathology, in vivo, PTA, Thiolate.
Abstract: A physiologically stable thiolate gold(I) derivative [Au(Spyrimidine)(PTA-CH2Ph)]Br has shown inhibition in colon cancer proliferation of Caco-2/TC7, Caco-2/PD7 and HTC-116-luc2 cell lines via apoptotic pathway and S-phase arrest in the cell cycle. Intraperitoneal injection of [Au(Spyrimidine)(PTA-CH2Ph)]Br in athymic nude mice inoculated with HTC-116-luc2 cells prolonged their survival and greatly inhibited tumour growth, near to disappearance. Low concentration of gold in urine and blood were detected in mice after 48 h of administration of 5 mg/kg body weight (bw) of the gold complex and non-organ (kidney and liver) damage has been detected after gold treatment. The results obtained suggested that the thiolate gold(I) derivative shown here could be considered as a candidate for therapeutic treatment in colon cancer.
Export Options
About this article
Cite this article as:
Garcia-Moreno Elena, Gascon Sonia, Garcia de Jalon A. Jose, Romanos Eduardo, Rodriguez-Yoldi Jesus M, Cerrada Elena and Laguna Mariano, In Vivo Anticancer Activity, Toxicology and Histopathological Studies of the Thiolate Gold(I) Complex [Au(Spyrimidine)(PTA-CH2Ph)]Br, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (6) . https://dx.doi.org/10.2174/1871520615666150129211440
DOI https://dx.doi.org/10.2174/1871520615666150129211440 |
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
-
Vector Delivery Methods and Targeting Strategies for Gene Therapy of Brain Tumors
Current Gene Therapy Advances in Molecular Therapeutic Approaches to Patients with Malignant Gliomas
Current Signal Transduction Therapy Merlin, a “Magic” Linker Between the Extracellular Cues and Intracellular Signaling Pathways that Regulate Cell Motility, Proliferation, and Survival
Current Protein & Peptide Science The Secretin/Pituitary Adenylate Cyclase-Activating Polypeptide/ Vasoactive Intestinal Polypeptide Superfamily in the Central Nervous System
Central Nervous System Agents in Medicinal Chemistry Mapping the High Throughput SEREX Technology Screening for Novel Tumor Antigens
Combinatorial Chemistry & High Throughput Screening Interrelation of Major Depression and Antidepressant Transcriptomics
Current Psychopharmacology Nanoparticle Systems Modulating Myeloid-Derived Suppressor Cells for Cancer Immunotherapy
Current Topics in Medicinal Chemistry Combination Therapy of Intraperitoneal Rapamycin and Convection- Enhanced Delivery of Nanoliposomal CPT-11 in Rodent Orthotopic Brain Tumor Xenografts
Current Cancer Drug Targets Fibroblast Growth Factor Receptor Signaling in Cancer Biology and Treatment
Current Signal Transduction Therapy The Design of Amphiphilic Polymeric Micelles of Curcumin for Cancer Management
Current Medicinal Chemistry Targeting Apoptotic Signaling Pathways in Human Lung Cancer
Current Cancer Drug Targets Insights into the Role of Matrix Metalloproteinases and Tissue Inhibitor of Metalloproteinases in Health and Disease
Current Chemical Biology Molecular Approaches Target to Immunotherapy for HPV-Associated Cancers
Current Cancer Drug Targets Considering Autotaxin Inhibitors in Terms of 2D-QSAR and 3D-Mapping- Review and Evaluation
Current Medicinal Chemistry Anionic Host Defence Peptides from the Plant Kingdom: Their Anticancer Activity and Mechanisms of Action
Protein & Peptide Letters Patent Selections
Recent Patents on DNA & Gene Sequences Targeting the EGFR-family for Therapy: Biological Challenges and Clinical Perspective
Current Pharmaceutical Design EGFR-Targeting Monoclonal Antibodies in Head and Neck Cancer
Current Cancer Drug Targets Conference Report (The XVth International Symposium of Brain Edema and Cellular Injury)
CNS & Neurological Disorders - Drug Targets The Use of Herbal Medicine in Cancer-related Anorexia/ Cachexia Treatment Around the World
Current Pharmaceutical Design