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folic acid and cancer

Jing Liu, Dujuan Zhao, Wenxiu He, Huiyuan Zhang, Zhonghao Li, Yuxia Luan
The anti-leukemia effect of cytarabine (Ara-C) is severely restricted by its high hydrophilic properties and rapid plasma degradation. Herein, a novel amphiphilic small molecular prodrug of Ara-C was developed by coupling a short aliphatic chain, hexanoic acid (HA) to 4-NH2 of the parent drug. Based on the amphiphilic nature, the resulting bioconjugate (HA-Ara) could spontaneously self-assemble into stable spherical nanoassemblies (NAs) with an extremely high drug loading (∼71wt%). Moreover, folate receptor (FR)-targeting NAs with high grafting efficient folic acid - bovine serum albumin (FA-BSA) conjugate immobilized on the surface (NAs/FA-BSA) was prepared...
October 19, 2016: Journal of Colloid and Interface Science
Yinping Huang, Kaili Mao, Baolin Zhang, Yingzheng Zhao
Monodispersed SPIONs (superparamagnetic iron oxide nanoparticles) co-coated with PEG and PEI polymers were prepared by an improved polyol method. To accomplish cancer-specific targeting properties, FA (folic acid) was then modified on the SPIONs via EDC/NHS method (FA-SPIONs). Doxorubicin (DOX) as an example anticancer drug was loaded within FA-SPIONs (DOX@FA-SPIONs), the DOX release rate of DOX@FA-SPIONs was much high in low pH PBS. The SPIONs, FA-SPIONs and DOX@FA-SPIONs with mean hydrodynamic diameters of 23, 40 and 67nm, respectively, performed excellent colloidal stability in PBS...
January 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
Aurélie Stallivieri, Ludovic Colombeau, Gulim Jetpisbayeva, Albert Moussaron, Bauyrzhan Myrzakhmetov, Philippe Arnoux, Samir Acherar, Régis Vanderesse, Céline Frochot
Recent researches in photodynamic therapy have focused on novel techniques to enhance tumour targeting of anticancer drugs and photosensitizers. Coupling a photosensitizer with folic acid could allow more effective targeting of folate receptors which are over-expressed on the surface of many tumour cells. In this study, different folic acid-OEG-conjugated photosensitizers were synthesized, characterized and their photophysical properties were evaluated. The introduction of an OEG does not significantly improve the hydrophilicity of the FA-porphyrin...
October 10, 2016: Bioorganic & Medicinal Chemistry
Caitlin G Howe, Xinhua Liu, Megan N Hall, Vesna Ilievski, Marie A Caudill, Olga Malysheva, Angela M Lomax-Luu, Faruque Parvez, Abu B Siddique, Hasan Shahriar, Mohammad N Uddin, Tariqul Islam, Joseph H Graziano, Max Costa, Mary V Gamble
BACKGROUND: Posttranslational histone modifications (PTHMs) are altered by arsenic, an environmental carcinogen. PTHMs are also influenced by nutritional methyl donors involved in one-carbon metabolism (OCM), which may protect against epigenetic dysregulation. METHODS: We measured global levels of three PTHMs, which are dysregulated in cancers (H3K36me2, H3K36me3, H3K79me2), in peripheral blood mononuclear cells (PBMCs) from 324 participants enrolled in the Folic Acid and Creatine Trial, a randomized trial in arsenic-exposed Bangladeshi adults...
October 20, 2016: Cancer Epidemiology, Biomarkers & Prevention
M Erdem, S Yalcin, U Gunduz
Conventional chemotherapy is the most valid method to cope with cancer; however, it has serious drawbacks such as decrease in production of blood cells or inflammation of the lining of the digestive tract. These side effects occur since generally the drugs used in chemotherapy are distributed evenly within the body of the patient and cannot distinguish the cancer cells from the healthy ones. In this study, folic acid (FA)-conjugated, polyethylene-coated magnetic nanoparticles (FA-MNPs), and doxorubicin (Dox)-loaded formulation (Dox-FA-MNPs) were prepared...
October 10, 2016: Human & Experimental Toxicology
Z Heger, T Eckschlager, M Stiborová, V Adam
BACKGROUND: Prostate cancer (PC) constitutes a heterogeneous group of diseases with high prevalence rates that are still increasing, particularly in western countries. Since 1980, prostate specific antigen (PSA) and other diagnostic approaches have been used for PC screening; however, some of these approaches are often deemed painful and cause invasive damage of tissue. Therefore, molecular approaches to PC diagnosis are attracting increasing attention, potentially providing patients with less stressful situations and providing better diagnoses and even prognostic information...
2016: Klinická Onkologie: Casopis Ceské a Slovenské Onkologické Spolecnosti
Suman Rana, Neena G Shetake, K C Barick, B N Pandey, H G Salunke, P A Hassan
The interfacial engineering of magnetic nanoparticles (MNPs) with specific functional groups or targeting ligands is important for their in vivo applications. We report here the preparation and characterization of bifunctional magnetic nanoparticles (BMNPs) which contain a carboxylic moiety for drug binding and an amine moiety for folate mediated drug targeting. BMNPs were prepared by introducing bioactive cysteine molecules onto the surface of undecenoic acid coated Fe3O4 magnetic nanoparticles (UMNPs) via a thiol-ene click reaction and then, folic acid was conjugated with these BMNPs through an EDC-NHS coupling reaction...
October 12, 2016: Dalton Transactions: An International Journal of Inorganic Chemistry
Yao Wang, Ping Huang, Minxi Hu, Wei Huang, Xinyuan Zhu, Deyue Yan
The distinct and complementary biochemical mechanisms of folic acid analog methotrexate (MTX) and cytidine analog gemcitabine (GEM) make their synergistic combination effectively. Unfortunately, such a combination faces severe pharmacokinetic problems and several transportation barriers. To overcome these problems, a new strategy of amphiphilic small molecule prodrug (ASMP) is developed to improve their synergistic combination effect. The ASMP was prepared by the amidation of the hydrophilic GEM with the hydrophobic MTX at a fixed ratio...
October 10, 2016: Bioconjugate Chemistry
Sheetal Parida, Chiranjit Maiti, Y Rajesh, Kaushik K Dey, Ipsita Pal, Aditya Parekh, Rusha Patra, Dibakar Dhara, Pranab Kumar Dutta, Mahitosh Mandal
BACKGROUND: Gold nanorods, by virtue of surface plasmon resonance, convert incident light energy (NIR) into heat energy which induces hyperthermia. We designed unique, multifunctional, gold nanorod embedded block copolymer micelle loaded with GW627368X for targeted drug delivery and photothermal therapy. METHODS: Glutathione responsive diblock co-polymer was synthesized by RAFT process forming self-assembled micelle on gold nanorods prepared by seed mediated method and GW627368X was loaded on to the reduction responsive gold nanorod embedded micelle...
October 6, 2016: Biochimica et Biophysica Acta
Gaurav Chauhan, Vianni Chopra, Amit Tyagi, Goutam Rath, Rakesh K Sharma, Amit K Goyal
Nano-graphene oxide (GO) nanometal composite (specifically nanogold and nanosilver) have shown to be a promising material for anticancer therapeutics. Owing to their high drug loading capacity, photothermal and synergizing effects, it is very important to exploit them for targeted chemo-thermal cancer therapeutics. In this work, gold nanoparticles (AuNPs) were selected as the composite metal, folic acid (FA) was taken as GO surface functionalization moiety for active tumor targeting of model anticancer drug Doxorubicin (Dox)...
October 6, 2016: European Journal of Pharmaceutical Sciences
C Fasolato, S Giantulli, I Silvestri, F Mazzarda, Y Toumia, F Ripanti, F Mura, F Luongo, F Costantini, F Bordi, P Postorino, F Domenici
Recent progress in nanotechnology and its application to biomedical settings have generated great advantages in dealing with early cancer diagnosis. The identification of the specific properties of cancer cells, such as the expression of particular plasma membrane molecular receptors, has become crucial in revealing the presence and in assessing the stage of development of the disease. Here we report a single cell screening approach based on Surface Enhanced Raman Scattering (SERS) microimaging. We fabricated a SERS-labelled nanovector based on the biofunctionalization of gold nanoparticles with folic acid...
October 6, 2016: Nanoscale
Shini Feng, Huijie Zhang, Ting Yan, Dandi Huang, Chunyi Zhi, Hideki Nakanishi, Xiao-Dong Gao
With its unique physical and chemical properties and structural similarity to carbon, boron nitride (BN) has attracted considerable attention and found many applications. Biomedical applications of BN have recently started to emerge, raising great hopes in drug and gene delivery. Here, we developed a targeted anticancer drug delivery system based on folate-conjugated BN nanospheres (BNNS) with receptor-mediated targeting. Folic acid (FA) was successfully grafted onto BNNS via esterification reaction. In vitro cytotoxicity assay showed that BNNS-FA complexes were non-toxic to HeLa cells up to a concentration of 100 μg/mL...
2016: International Journal of Nanomedicine
Hiroshi Tsukihara, Kenta Tsunekuni, Teiji Takechi
In colorectal cancer chemotherapy, the current standard of care includes combination therapy with 5-fluorouracil (5-FU) and leucovorin (LV). However, the factors that determine the LV-mediated enhancement of 5-FU antitumor activity are not fully understood. Therefore, we investigated the roles of thymidine synthase (TYMS), folate receptor 1 (FOLR1), dihydrofolate reductase (DHFR), phosphoribosylglycinamide formyltransferase (GART), methylenetetrahydrofolate dehydrogenase (MTHFD1), and methylenetetrahydrofolate reductase (MTHFR) in LV-mediated enhancement of 5-fluoro-2'-deoxyuridine (FdUrd) cytotoxicity in vitro as a model of 5-FU antitumor activity...
2016: PloS One
Cheng-Qiong Luo, Yoonjeong Jang, Lei Xing, Peng-Fei Cui, Jian-Bin Qiao, Ah Young Lee, Hyeon-Jeong Kim, Myung-Haing Cho, Hu-Lin Jiang
Lung cancer has been a leading cause of cancer mortality worldwide and aerosol-mediated gene therapy endows numerous advantages compared to other traditional modalities. Here, we reported a folic acid (FA)-modified hyperbranched polyspermine (HPSPE) with prominent biocompatibility for lung cancer cell targeted gene therapy. FA was decorated to the HPSPE via an amidation reaction and the physicochemical properties of nanoplexes formed with DNA were characterized. Gel electrophoresis study elucidated that the designed polymer was capable to condense DNA and protect it from degradation by DNase I...
September 25, 2016: International Journal of Pharmaceutics
Joseph Friedrich, Dara Khatib, Keon Parsa, Ariana Santopietro, G Ian Gallicano
With the increasing publicity of marijuana due to recent legislation, it is pertinent that the effects of fetal exposure to the drug are assessed. While in utero cannabis exposure has been associated with early pregnancy failure, birth defects and developmental delay, the mechanisms of such outcomes are largely unexplained. Furthermore, the use of cannabinoids in cancer treatment via growth inhibition and apoptosis may indicate how cannabis exposure likely harms a growing fetus. Cannabinoid signaling is required for proper pre-implantation development, embryo transport to the uterus, and uterine receptivity during implantation...
September 29, 2016: BMC Pharmacology & Toxicology
Sheng-Hui Chiu, Gangaraju Gedda, Wubshet Mekonnen Girma, Jem-Kun Chen, Yong-Chien Ling, Anil V Ghule, Keng-Liang Ou, Jia-Yaw Chang
: Herein, we synthesized an S, N, and Gd tri-element doped magnetofluorescent carbon quantum dots (GdNS@CQDs) within 10min by using a one-pot microwave method. Our results showed that these magnetofluorescent GdNS@CQDs have excellent fluorescent and magnetic properties. Moreover, GdNS@CQDs exhibited high stability at physiological conditions and ionic strength. These magnetofluorescent GdNS@CQDs were conjugated with a folic acid, denoted as FA-GdNS@CQDs, for targeting dual modal fluorescence/magnetic resonance (MR) imaging...
September 20, 2016: Acta Biomaterialia
Hanchun Yao, Li Su, Man Zeng, Li Cao, Weiwei Zhao, Chengqun Chen, Bin Du, Jie Zhou
Carbon dots (CDs) are one of the most highlighted carbon-based materials for biological applications, such as optical imaging nanoprobes, which are used for labeling cells in cancer treatment mainly due to their biocompatibility and unique optical properties. In this study, gadolinium (Gd)-complex-containing CDs were obtained through a one-step microwave method to develop multimodal nanoprobes integrating the advantages of optical and magnetic imaging. The obtained Gd-CDs exhibited highly fluorescent properties with excellent water solubility and biological compatibility...
2016: International Journal of Nanomedicine
S Sureshkumar, B Jothimani, T M Sridhar, Arul Santhosh, B Venkatachalapathy
Surface modified ZnO nanomaterial is widely used in the field of bioimaging worldwide due to its optical properties, electronic characteristics and biocompatibility. Fluorescent enhanced, Polyquaternium-7(PQ7) capped, ZnO hexagonal nano disks (ZnO-PQ7) were synthesised by simple wet chemical method. The structural and optical properties of ZnO-PQ7 hexagonal nano disks were characterized using XRD, UV-Visible, Fluorescence, HRTEM, EDAX and FTIR studies. The size of synthesised ZnO-PQ7 were around 30-45 nm as confirmed by HRTEM studies...
September 20, 2016: Journal of Fluorescence
Tiehong Yang, Wei Li, Xiao Duan, Lin Zhu, Li Fan, Youbei Qiao, Hong Wu
Polymeric micelles represent an effective delivery system for poorly water-soluble anticancer drugs. In this work, two types of CPT-conjugated polymers were synthesized based on poly(β-L-malic acid) (PMLA) derivatives. Folic acid (FA) was introduced into the polymers as tumor targeting group. The micellization behaviors of these polymers and antitumor activity of different self-assembled micelles were investigated. Results indicate that poly(ethylene glycol)-poly(β-L-malic acid)-campotothecin-I (PEG-PMLA-CPT-I, P1) is a grafted copolymer, and could form star micelles in aqueous solution with a diameter of about 97 nm, also that PEG-PMLA-CPT-II (P2) is an amphiphilic block copolymer, and could form crew cut micelles with a diameter of about 76 nm...
2016: PloS One
Mahmoud Jafari, Danial Heidari, Pedram Ebrahimnejad
Multifunctional nanomaterials showed great advantages in drug delivery. Folic acid (FA) binding protein, a glycosyl phosphatidyl inositol anchored cell surface receptor for folate, is overexpressed in several human tumors, whereas it is highly restricted in normal tissues. Therefore, in this study, FA, polyethylene glycol (PEG), and Fe3O4 nanoparticles multifunctionalized short multiwall carbon nanotubes (PEG-FA-SMWCNT@Fe3O4) were synthesized by conjugating folate, PEG, and magnetite nanoparticles with carboxylated multiwall carbon nanotubes...
2016: Iranian Journal of Pharmaceutical Research: IJPR
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