Search results for "VITRO"
showing 10 items of 2786 documents
Polyaspartylhydrazide Copolymer-Based Supramolecular Vesicular Aggregates as Delivery Devices for Anticancer Drugs
2008
In this paper we report on three different hydrophilic copolymers based on alpha,beta-polyaspartylhydrazide (PAHy) bearing butyric groups in the side chain (C 4) (PAHy-C 4) or a combination of butyric groups and positive charged residues ((carboxypropyl)trimethylammonium chloride, CPTACl) (PAHy-C 4-CPTA) that were synthesized and used for the preparation of new supramolecular vesicular aggregates (SVAs) containing gemcitabine as an antitumor drug. Gemcitabine-loaded SVAs containing synthesized PAHy derivatives were characterized from the physicochemical and technological point of view and the in vitro toxicity and anticancer activity on two different human cancer cell lines, i.e., CaCo-2 (h…
Folate-mediated targeting of polymeric conjugates of gemcitabine.
2005
The synthesis of two new macromolecular prodrugs for active tumor targeting was set up. Gemcitabine (2'-deoxy-2',2'-difluorocytidine) was conjugated to alpha,beta-poly(N-2-hydroxyethyl)-DL-aspartamide (PHEA) through succinyl or diglycolyl hydrolysable spacers. The targeting agent folic acid was attached to the macromolecular backbone through the aminocaproic spacer. The two conjugates [PHEA-(5'-succinylgemcitabine)-1'-carboxypentyl-folamide and PHEA-(5'-diglycolyl-gemcitabine)-1'-carboxypentyl-folamide], were purified and extensively characterised by spectroscopic (UV, IR and NMR) and chromatographic analyses to determine the correct chemical structure, the purity degree and the reaction yi…
Identification of Biphenyl-Based Hybrid Molecules Able To Decrease the Intracellular Level of Bcl-2 Protein in Bcl-2 Overexpressing Leukemia Cells
2009
With the aim of enhancing the structural complexity and diversity of an existing collection of bi- and terphenyl compounds, we synthesized hybrid molecules comprising of spirocyclic ketones (a complexity-bearing core) and bi/terphenyls (privileged fragments). Compounds 1, 3, 4, and 6 showed well-defined activity on apoptosis and differentiation, making them potential leads for development as new anticancer agents and chemical probes to study signaling networks in neoplastic cells.
Antimicrobial and antiproliferative activity of Peucedanum nebrodense (Guss.) Strohl.
2003
Abstract Acetone extract of Peucedanum nebrodense (Guss.) Strohl., a rare endemic species from the Madonie mountains (Sicily), was tested in vitro for its antimicrobial activity against bacterial reference strains and antiproliferative activity against K562 (human chronic myelogenous leukemia), HL-60 (human leukemia) and L1210 (murine leukemia) cell lines. The acetone extract showed antiproliferative IC 50 values in the range of 14–0.27 μg/ml.
Effects of soyasaponin I and soyasaponins-rich extract on the Alternariol-induced cytotoxicity on Caco-2 cells
2015
Abstract Alternariol (AOH) is a mycotoxin produced by Alternaria spp. Soyasaponin I (Ss-I) is present naturally in legumes, and it has antioxidant properties. Cytotoxic and genotoxic effects of AOH have been demonstrated previously in vitro. In the present study, the cytotoxicity of AOH, Ss-I, and soyasaponins-rich extract from lentils was investigated; as well as, the cytoprotective effects of Ss-I and lentil extracts against AOH induced-cytotoxicity on Caco-2 cells. Cytotoxicity was carried out using MTT and PC assays (AOH: 3.125–100 µM, Ss-I: 3.125–50 µM, and lentil extracts: 1:0–1:32) during 24 h of exposure. Only AOH showed cytotoxic effect. The reduction in cell proliferation ranged f…
Antioxidant effect derived from bioaccessible fractions of fruit beverages against H2O2-induced oxidative stress in Caco-2 cells
2008
Abstract This work evaluates the effect of bioaccessible fractions from fruit beverages against oxidative stress (OS) in Caco-2 cells. A fruit beverage (grape + orange + apricot) (with/without milk and/or iron/zinc) was subjected to in vitro gastrointestinal digestion, and bioaccessible fractions were incubated with Caco-2 cell cultures. Following preincubation, OS was induced with 5 mM H 2 O 2 . Intracellular reactive oxygen species (ROS), mitochondrial potential (Δ ψ m ), mitochondrial metabolism (MTT test), intracellular reduced glutathione (GSH) and superoxide dismutase activity (SOD) were measured. The data evidenced viable cultures with increased mitochondrial metabolism and GSH-Rd ac…
Drugs modulating the biological effects of peroxynitrite and related nitrogen species.
2007
The term “reactive nitrogen species” includes nitrogen monoxide, commonly called nitric oxide, and some other remarkable chemical entities (peroxynitrite, nitrosoperoxycarbonate, etc.) formed mostly from nitrogen monoxide itself in biological environments. Regardless of the specific mechanisms implicated in their effects, however, it is clear that an integrated pharmacological approach to peroxynitrite and related species is only just beginning to take shape. The array of affected chemical and pathological processes is extremely broad. One of the most conspicuous mechanisms observed thus far has been the scavenging of the peroxynitrite anion by molecules endowed with antioxidant activity. T…
Importance pharmacologique des dérivés polyphénoliques
1996
Summary The polyphenol derivatives possess many biological and pharmacological properties. However, the main therapeutical uses are limited to hepatoprotective and vasculoprotective activities of flavonoids (sensu largo). This rewiev will summarize some of the important and recently updated reports of in vitro and in vivo biological assays to show antioxidative, antihypertensive, antiphlogistic, antiviral, potent antitumoral and chimiopreventive activities.
Potential in vitro antioxidant, anti-inflammatory, antidiabetic, and anticancer effect of arachidonic acid-elicited basil leaves
2017
Abstract The study presents the impact of elicitation of basil with 0.01 µM (AA1), 1 µM (AA2) and 100 µM (AA3) arachidonic acid on the content and bioactivity of potentially bioavailable polyphenols. Elevated levels of phenolic compounds correlated with increased biological activity were observed in the extracts from basil (control and elicited) subjected to simulated gastrointestinal digestion in comparison to chemical and standard buffer extracts. Elicitation with AA1 and AA2 resulted in an 3-fold and more than 4-fold increase in the content of potentially bioavailable rosmarinic acid, respectively. In some cases, elicitation with arachidonic acid improved the pro-health properties of the…
Lidocaine inhibits potassium efflux and hemolysis in erythrocytes during oxidative stress in vitro.
2000
Lidocaine is a widely used local anesthetic agent. The aim of this work was to study the action of lidocaine on human red blood cells exposed to an oxidative stress in vitro. Blood was obtained from healthy volunteers. After separation from plasma, the erythrocytes were suspended in phosphate buffer. Oxidative stress was induced by incubation with a free radical generator, the 2,2' azobis (2-amidinopropane) hydrochloride (AAPH). Erythrocytes were incubated with or without lidocaine at two concentrations (36.93 and 73.85 microM) and with or without AAPH (20 mM). Electron paramagnetic resonance (EPR) spectroscopy was performed to identify the free radical species generated by AAPH using the s…