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anticancer drug research

Evelina Cardoso, Thomas Mercier, Anna Dorothea Wagner, Krisztian Homicsko, Olivier Michielin, Kim Ellefsen-Lavoie, Laurène Cagnon, Manuel Diezi, Thierry Buclin, Nicolas Widmer, Chantal Csajka, Laurent Decosterd
A sensitive and selective method of high performance liquid chromatography (HPLC) coupled to tandem mass spectrometry (MS/MS) has been developed for the simultaneous quantification of six anticancer protein kinase inhibitors (PKIs), dabrafenib, trametinib, vemurafenib, cobimetinib, pazopanib, regorafenib, and two active metabolites (regorafenib-M2 and regorafenib-M5) in human plasma. Plasma protein precipitation with methanol enables the sample extraction of 100 μL aliquot of plasma. Analytes are detected by electrospray triple-stage quadrupole mass spectrometry and quantified using the calibration curves with stable isotope-labeled internal standards...
February 8, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Liuqi Peng, Xuan Mei, Jun He, Jiekun Xu, Weiku Zhang, Ruizheng Liang, Min Wei, David G Evans, Xue Duan
2D nanomaterials have attracted considerable research interest in drug delivery systems, owing to their intriguing quantum size and surface effect. Herein, Gd3+ -doped monolayered-double-hydroxide (MLDH) nanosheets are prepared via a facile bottom-up synthesis method, with a precisely controlled composition and uniform morphology. MLDH nanosheets as drug carrier are demonstrated in coloading of doxorubicin and indocyanine green (DOX&ICG), with an ultrahigh drug loading content (LC) of 797.36% and an encapsulation efficiency (EE) of 99...
March 14, 2018: Advanced Materials
Yathisha Ug, Ishani Bhat, Iddya Karunasagar, Mamatha Bs
The rising interest to utilize nutritionally exorbitant fish proteins has instigated research activities in fish waste utilization. The development of newer technologies to utilize fish waste has fostered use of bioactive value-added products for specific health benefits. Enzymatically obtained Fish Protein Hydrolysate (FPH) is a rich source of biologically active peptides possessing anti-oxidant, anticancer, antimicrobial and anti-hypertensive activity. Isolating natural remedies to combat alarming negative consequences of synthetic drugs has been the new trend in current research promoting identification of antihypertensive peptides from FPH...
March 13, 2018: Critical Reviews in Food Science and Nutrition
Nan You, Jing Li, Xiaobing Huang, Ke Wu, Yichen Tang, Liang Wang, Hongyan Li, Na Mi, Lu Zheng
While >80% of the incidence occurs in sub‑Saharan Africa and East Asia, cases of hepatocellular carcinoma (HCC) have been rapidly increasing in Western countries. Despite its global importance, HCC is relatively under‑researched compared with other lethal cancer types, which is possibly due to the high complexity and heterogeneity of HCC. It has been reported previously that COMM domain‑containing protein 7 (COMMD7) is upregulated in HCC and promotes HCC cell proliferation by triggering C‑X‑C motif chemokine 10 (CXCL10) production...
March 8, 2018: Molecular Medicine Reports
Rafat Ali, Shalini Singh, Wahajul Haq
BACKGROUND: Smac mimetics (also known as IAP antagonist) are a new class of targeted drugs having a goal to suppress the IAPs, reestablishing the apoptotic pathways and inducing cancer cell death. Therefore, development of Smac mimetics was consideredan attractive strategy for the development of new anticancer drugs. Lots of review has been come in yesteryears which mainly discussed about biology of IAPs and their role in cancer development. But none of these reviews focused on the chemical synthesis of Smac mimetics...
March 12, 2018: Current Medicinal Chemistry
Yesi Shi, Xin Pang, Junqing Wang, Gang Liu
TRAIL is a member of the tumor necrosis factor superfamily that can largely trigger apoptosis in a wide variety of cancer cells, but not in normal cells. However, insufficient exposure to cancer tissues or cells and drug resistance has severely impeded the clinical application of TRAIL. Recently, nanobiotechnology has brought about a revolution in advanced drug delivery for enhanced anticancer therapy using TRAIL. With the help of materials science, immunology, genetic engineering, and protein engineering, substantial progress is made by expressing fusion proteins with TRAIL, engineering TRAIL on biological membranes, and loading TRAIL into functional nanocarriers or conjugating it onto their surfaces...
March 12, 2018: Advanced Healthcare Materials
Luisa Iacovelli, Rosamaria Orlando, Alessandro Rossi, Paola Spinsanti, Daniela Melchiorri, Ferdinando Nicoletti
In spite of the recent advancement in the molecular characterization of malignant gliomas and medulloblastomas, the treatment of primary brain tumors remains suboptimal. The use of small molecule inhibitors of intracellular signaling pathways, inhibitors of angiogenesis, and immunotherapic agents is limited by systemic adverse effects, limited brain penetration, and, in some cases, lack of efficacy. Thus, adjuvant chemo-therapy and radiotherapy still remain the gold standard in the treatment of grade-IV astrocytoma (glioblastoma multiforme) and medulloblastoma...
March 8, 2018: Current Opinion in Pharmacology
Maryam Alsadat Shetab Boushehri, Valentin Stein, Alf Lamprecht
Nanoparticles create exciting platforms for anticancer immunotherapy and vaccination, though their inherent immunomodulatory properties have remained underexploited. Ammonio methacrylate copolymers (AMC) are well-established excipients in pharmaceutical industry and components of controlled-release oral formulations. Here, we demonstrate that nanoscaling of type A and B AMC (Eudragit® RL and RS) endows these inactive ingredients immunostimulatory properties exploitable for cancer therapy. The particles induce the secretion of various pro-inflammatory cytokines and chemokines from the cells of innate immunity...
March 2, 2018: Biomaterials
Yanxue Liu, Kefeng Liu, Xiaomin Li, Shangzhen Xiao, Dan Zheng, Pengbo Zhu, Chunxiao Li, Jing Liu, Jing He, Jiandu Lei, Luying Wang
The application of non-toxic carriers to increase drug loading, multi-drug delivery, and extremely small size of nano-drugs to construct a tremendous transmission system is the goal for all researchers to be pursued. The proposal of natural pectin nano-platform for delivery of multiple drugs is critical for biomedical research, especially a particle size of below 100nm with high yield. Here we design a new core-shell structure pectin-eight-arm polyethylene glycol-ursolic acid/hydrooxycampothecin nanoparticle (Pec-8PUH NPs) through a special self-assembly method for stabilizing and dispersing particles, improving water-solubility, and achieving drug controlled release...
May 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
Marine Blanchet, Jean Michel Brunel
Bile acids or bile salts, belong to a large family of biological steroid derivatives found predominantly in the bile of mammals and other vertebrates. These amphipathic molecules possess numerous functions, including eliminating cholesterol from the body, driving the flow of bile to eliminate catabolites, emulsifying fat-soluble vitamins to enable their absorption, aiding in motility and in reducing the bacteria flora found in the small intestine and biliary tract. In this review, we investigate progress towards synthetic bile acid derivatives, with special emphasis on how they might be used for various biological applications and the challenges that remain in developing these compounds as potent drugs of the future especially in the field of microbiology (antimicrobial activities) and cancer (anticancer agents)...
March 8, 2018: Current Medicinal Chemistry
Kaja Bergant, Matej Janezic, Andrej Perdih
BACKGROUND: The family of DNA topoisomerases comprises a group of enzymes that catalyse the induction of topological changes to DNA. These enzymes play a role in the cell replication machinery and are, therefore, important targets for anticancer drugs - with human DNA topoisomerase IIα being one of the most prominent. Active compounds targeting this enzyme are classified into two groups with diverse mechanisms of action: DNA poisons act by stabilizing a covalent cleavage complex between DNA and the topoisomerase enzyme, transforming it into a cellular toxin, while the second diverse group of catalytic inhibitors, provides novel inhibition avenues for tackling this enzyme due to frequent occurrence of side effects observed during the DNA poison therapy...
March 6, 2018: Current Medicinal Chemistry
Sakineh Dadashpour, Saeed Emami
The indole scaffold is one of the most widespread heterocycles in the naturally occurring and synthetic bioactive compounds including anticancer agents. Due to its biodiversity and versatility, it has been a highly privileged motif for the target-based design and development of anticancer agents. In the last decade, many researchers have reported various indole-based compounds with distinct mechanisms involved in producing potential anticancer activities, indicating the importance of indole motif in the anticancer drug development...
February 24, 2018: European Journal of Medicinal Chemistry
Jie Yu, Changxi Wang, Qi Kong, Xiaxia Wu, Jin-Jian Lu, Xiuping Chen
BACKGROUND: As an anthracycline antibiotic, doxorubicin (DOX) is one of the most potent and widely used chemotherapeutic agents for various types of solid tumors. Unfortunately, clinical application of this drug results in severe side effects of cardiotoxicity. PURPOSE: We aim to review the research focused on elimination or reduction of DOX cardiotoxicity without affecting its anticancer efficacy by natural products. METHODS: This study is based on pertinent papers that were retrieved by a selective search using relevant keywords in PubMed and ScienceDirect...
February 1, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Pulakuntla Swetha Reddy, Kiran Bharat Lokhande, Shuchi Nagar, Vaddi Damodara Reddy, P Sushma Murthy, K Venkateswara Swamy
BACKGROUND: Gefitinib (lressa) is the most prescribed drug, highly effective to treat of non-small cell lung cancer; primarily it was considered targeted therapy is a kinase inhibitor. The non-small cell lung cancer caused by the mutation in the Epithelial Growth Factor Receptor (EGFR) gene, Iressa works by blocking the EGFR protein that helps the cancer cell growth. EGFR protein has lead to the development of anticancer therapeutics directed against EGFR inhibitor including Gefitinib for non-small cell lung cancer...
February 27, 2018: Current Computer-aided Drug Design
Francesco Petrella, Lorenzo Spaggiari
Two main fields of clinical applications of stem cells in thoracic surgery have been explored: (a) regenerative medicine, that is a branch of translational research in tissue engineering and molecular biology dealing with the replacement, engineering or regeneration of cells, tissues and organs to restore normal function; (b) drug loading and delivery, that is an emerging field proposing stem cells as vectors to deliver anti-cancer agents for targeted therapies.Bronchopleural fistula is a pathological connection between the bronchus and the pleural cavity that may develop after lung resection, thus causing pleural empyema due to colonization by resident airway bacteria; stem cells and regenerative medicine approach can effectively contribute to impaired bronchial healing, thus preventive a septic and ventilator catastrophe...
March 1, 2018: Advances in Experimental Medicine and Biology
Md Wasimul Haque, Shakti Prasad Pattanayak
Background: Breast cancer (BC), because of its invasive characteristics, is one of the most common and deadliest cancers among the female population around the world. Research has demonstrated that AhR signaling also plays a vital role in BC initiation and development as well. Therefore, blocking this pathway to natural interferences paves a new channel for the prevention of BC. Several natural compounds such as flavonoids possess the anticancer activities against different cancers. Objective: The present study has been designed to estimate the chemotherapeutic potential of taxifolin (TAX) against 7,12-dimethylbenz(a)anthracene (DMBA)-induced mammary carcinoma in Sprague-Dawley rats...
January 2018: Pharmacognosy Magazine
Maren Sack-Zschauer, Elif Karaman-Aplak, Claudia Wyrich, Soumen Das, Thies Schubert, Hajo Meyer, Christoph Janiak, Sudipta Seal, Wilhelm Stahl, Peter Brenneisen
The biomedical application of cerium oxide nanoparticles (nanoceria) is a focal point of research for a few years. The biochemical effects of nanoceria depend on various factors including particle size, oxidation state of cerium, oxygen vacancies on the surface, use of dispersants or coatings, pH and cell type. Due to their autocatalytic redox-activity, these particles are considered to act as a specific anti-cancer tool with less side effects on healthy cells and tissues, as the particles kill tumor cells, while protecting healthy cells from oxidative damage...
December 1, 2017: Journal of Biomedical Nanotechnology
Yi Wang, Huaiyi Huang, Qianling Zhang, Pingyu Zhang
Chiral natural biological molecules, such as nucleic acids and proteins, guide the research of chiral compounds. Chiral metal-based drugs are currently an interesting and rapidly growing field in anticancer research. This perspective focuses on chiral metal compounds with application in cancer chemotherapy. The different chiral metal-based anticancer agents and the extent to which the chiral resolution affects their biological properties are discussed. This perspective will aid the design of new potent and efficient chiral metal-based anticancer drugs that exploit their unique properties combined with their potential selectivity toward targeted chiral biomolecules...
February 26, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
Harpreet Singh, Amrita Mishra, Arun Kumar Mishra
BACKGROUND: Since ancient times, species of Cleome genus are used to cure various ailments in human beings and same is stated in traditional treatises. Each part of the plant has its own significance, therefore, in background of its significance, upto date information in systematic manner is required. PURPOSE: The present review embarks on variety of naturally occurring compounds that have been isolated from various species of Cleome genus. The present study furnishes an overview of all naturally isolated compounds diterpenes, triterpenoids, trinorterpenoids, flavonol glycoside, coumarinolignoids, dipyridodiazepinone, essential oils, sesquiterpenes, flavonoids, carboxylic acid derivatives, lactone derivatives, sterols and pharmacological activities of various species of Cleome genus...
February 21, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Raimundo Gonçalves de Oliveira Júnior, Christiane Adrielly Alves Ferraz, Jackson Roberto Guedes da Silva Almeida, Raphaël Grougnet, Valérie Thiéry, Laurent Picot
PURPOSE: Tumor cells are spontaneously or adaptively resistant to chemotherapeutic drugs, eventually leading to the selection of multiresistant cells responsible for tumor growth and metastasis. Chemosensitization of tumor cells to conventional drugs using non-toxic natural products is a recent and innovative strategy aiming to increase the cytotoxic efficiency of anticancer drugs, limit their toxic side effects and delay the appearance of acquired chemoresistance. This systematic review summarizes data obtained from preclinical studies reporting the use of natural products to sensitize tumor cells to chemotherapeutic agents...
February 21, 2018: Fitoterapia
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