Search results for "folic acid"
showing 10 items of 92 documents
18 F-click labeling and preclinical evaluation of a new 18 F-folate for PET imaging.
2013
Background The folate receptor (FR) is a well-established target for tumor imaging and therapy. To date, only a few 18 F-folate conjugates via 18 F-prosthetic group labeling for positron emission tomography (PET) imaging have been developed. To some extent, they all lack the optimal balance between efficient radiochemistry and favorable in vivo characteristics. Methods A new clickable olate precursor was synthesized by regioselective coupling of folic acid to 11-azido-3,6,9-trioxaundecan-1-amine at the γ-position of the glutamic acid residue. The non-radioactive reference compound was synthesized via copper-catalyzed azide-alkyne cycloaddition of 3-(2-(2-(2-fluoroethoxy)ethoxy)ethoxy)prop-1…
Multi-Functional Nanogels for Tumor Targeting and Redox-Sensitive Drug and siRNA Delivery
2016
(1) Background: A new family of nanosystems able to discern between normal and tumor cells and to release a therapeutic agent in controlled way were synthetized by e-beam irradiation. This technique permits to obtain biocompatible, sterile, carboxyl-functionalized polyvinylpyrrolidone (PVP-co-acrylic acid) nanogels (NGs); (2) Methods: Here, we performed a targeting strategy based on the recognition of over-expressed proteins on tumor cells, like the folate receptor. The selective targeting was demonstrated by co-culture studies and flow cytometry analysis, using folate conjugated NGs. Moreover, nanoparticles were conjugated to a chemotherapeutic drug or to a pro-apoptotic siRNA through a gl…
Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Folic Acid.
2018
This work presents a review of literature and experimental data relevant to the possibility of waiving pharmacokinetic bioequivalence studies in human volunteers for approval of immediate-release solid oral pharmaceutical forms containing folic acid as the single active pharmaceutical ingredient. For dosage forms containing 5 mg folic acid, the highest dose strength on the World Health Organization Essential Medicines List, the dose/solubility ratio calculated from solubility studies was higher than 250 mL, corresponding to a classification as "not highly soluble." Small, physiological doses of folic acid (≤320 μg) seem to be absorbed completely via active transport, but permeability data f…
in vitro biological evaluation of folate-functionalized block copolymer micelles for selective anti-cancer drug delivery.
2008
The main objective of this study was to evaluate the ability of folic acid-functionalized diblock copolymer micelles to improve the delivery and uptake of two poorly water-soluble anti-tumor drugs, tamoxifen and paclitaxel, to cancer cells through folate receptor targeting. The diblock copolymer used in this study comprised a hydrophilic poly[2-(methacryloyloxy)ethyl phosphorylcholine] (MPC) block, carrying at the chain end the folate targeting moiety, and a pH-sensitive hydrophobic poly[2-(diisopropylamino)ethyl methacrylate] (DPA) block (FA-MPC-DPA). The drug-loading capacities of tamoxifen- and paclitaxel-loaded micelles were determined by high performance liquid chromatography and the m…
Synthesis of Novel Folic Acid-Functionalized Biocompatible Block Copolymers by Atom Transfer Radical Polymerization for Gene Delivery and Encapsulati…
2005
Two synthetic routes to folic acid (FA)-functionalized diblock copolymers based on 2-(methacryloyloxy)- ethyl phosphorylcholine [MPC] and either 2-(dimethylamino)ethyl methacrylate [DMA] or 2-(diisopropylamino) ethyl methacrylate [DPA] were explored. The most successful route involved atom transfer radical polymerization (ATRP) of MPC followed by the tertiary amine methacrylate using a 9-fluorenylmethyl chloroformate (Fmoc)-protected ATRP initiator. Deprotection of the Fmoc groups produced terminal primary amine groups, which were conjugated with FA to produce two series of novel FA-functionalized biocompatible block copolymers. Nonfunctionalized MPC-DMA diblock copolymers have been previou…
Caracterización de la suplementación de folatos en el embarazo a partir de la combinación de sistemas de información sanitaria.
2012
ResumenObjetivosExplorar la utilidad de la combinación de los sistemas de información sanitaria de la Agencia Valenciana de Salud (AVS) para caracterizar la suplementación de folatos en la población de embarazadas de la Comunidad Valenciana.MétodosCohorte de todas las mujeres que parieron en hospitales de la AVS durante 2009, que fueron seguidas retrospectivamente en la historia clínica electrónica ABUCASIS y el sistema GAIA de gestión de la prescripción para identificar el consumo de folatos en los 3 meses previos y posteriores a la concepción.ResultadosDe los 38.069 partos realizados en 2009 en hospitales de la AVS, 37.040 (97,3%) pudieron incluirse en los análisis. Un 34,0% de las mujere…
The knowledge of women with epilepsy on motherhood
2017
Wstęp: Padaczka jest jedną z najczęstszych chorób neurologicznych. Na całym świecie cierpi na nią ok. 50 mln osób, z czego połowa to kobiety. Pomimo że ciąża w przebiegu epilepsji zaliczana jest do ciąż wysokiego ryzyka, na podstawie wielu obserwacji przyjmuje się, że szansa urodzenia zdrowego dziecka przez kobietę z padaczką wynosi ponad 90%, ale ryzyko wystąpienia wad wrodzonych jest 2–3-krotnie wyższe niż w przypadku ciąży u kobiety zdrowej. Wynika to głównie z faktu stosowania leków przeciwpadaczkowych. Materiał i metody: Badaniami objęto 139 kobiet chorych na padaczkę, w wieku od 18 do 40 lat, będących pod opieką poradni neurologicznych na terenie województwa śląskiego. Badania przepro…
Current and New Insights in the Sustainable and Green Recovery of Nutritionally Valuable Compounds from Stevia rebaudiana Bertoni.
2015
International audience; The South American plant Stevia rebaudiana Bertoni is a great source of noncaloric sweeteners (steviol glycosides), mainly concentrated in its leaves, but also has important antioxidant compounds (vitamin C, polyphenols, chlorophylls, and carotenoids) and other important macro- and micronutrients such as folic acid and all of the essential amino acids except tryptophan. Traditionally, conventional methods have been used to recover nutritionally valuable compounds from plant food matrices. However, nowadays, the need for obtaining greener, sustainable, and viable processes has led both food industries and food scientists to develop new processes in full correspondence…
Trichinella spiralisThymidylate Synthase: Developmental Pattern, Isolation, Molecular Properties, and Inhibition by Substrate and Cofactor Analogues
1996
Abstract Thymidylate synthase specific activity was found to remain at a constant level in crude extracts from muscle larvae, isolated (1-15 months after infection) by pepsin-HCl digestion, as well as from adult worms ofTrichinella spiralis.The enzyme was purified and its molecular (monomer mol. wt 35 kD) and kinetic (sequential mechanism with the Kmvalues 3.1 and 19 μM for dUMP and N5,10-methylenetetrahydrofolate, respectively) properties determined. 5-Fluoro-dUMP was a competitive, slow-binding inhibitor of the parasite enzyme. N5,10-methylenetetrahydrofolate analogues 10-propargyl-5,8-dideazafolate (CB3717), ZD1694, BW1843U89, and AG337 were weaker inhibitors of the parasite than regener…
Inhibition of Folic Acid Uptake by Catechins and Tea Extracts in Caco-2 Cells
2006
In this present study it was aimed to determine whether the catechins contained in green tea and the whole extracts of Camellia sinensis (Theaceae) inhibit the uptake of folic acid by Caco-2 cell monolayers. Our results indicate that (-)-epigallocatechin 3-gallate (EGCG) and (-)-epicatechin 3-gallate (ECG) inhibit cellular folic acid uptake with IC50 values of 34.8 micromol/L and 30.8 micromol/L, respectively. Furthermore, green and black tea extracts were also found to inhibit folic acid uptake with IC50 values of approximately 7.5 and 3.6 mg/mL, respectively. According to these results, simultaneous intake of tea and folic acid may inhibit intestinal folic acid absorption. The consequence…