Search results for "Therapeutic agent"

Recent discoveries of anticancer flavonoids.

2017

Abstract In this review we report the recent advances in anticancer activity of the family of natural occurring flavonoids, covering the time span of the last five years. The bibliographic data will be grouped, on the basis of biological information, in two great categories: reports in which the extract plants bioactivity is reported and the identification of each flavonoid is present or not, and reports in which the anticancer activity is attributable to purified and identified flavonoids from plants. Wherever possible, the targets and mechanisms of action as well as the structure-activity relationships of the molecules will be reported. Also, in the review it was thoroughly investigated t…

Evidence-Based Clinical Use of Nanoscale Extracellular Vesicles in Nanomedicine

2016

collaboration au projet H2020 European Cooperation in Science and Technology (COST) program European Network on Microvesicles and Exosomes in Health and Disease (ME-HAD); International audience; Recent research has demonstrated that all body fluids assessed contain substantial amounts of vesicles that range in size from 30 to 1000 nm and that are surrounded by phospholipid membranes containing different membrane microdomains such as lipid rafts and caveolae. The most prominent representatives of these so-called extracellular vesicles (EVs) are nanosized exosomes (70-150 nm), which are derivatives of the endosomal system, and microvesicles (100-1000 nm), which are produced by outward budding…

Natural payload delivery of the doxorubicin anticancer drug from boron nitride oxide nanosheets

2019

International audience; We studied the behavior of doxorubicin (DOX; an anticancer drug) molecules loaded on a boron nitride oxide nanosheet (BNO-NS) using the density functional theory (DFT), time-dependent density functional theory (TDDFT), and molecular dynamic (MD) simulation methods. We found that DOX molecules in pi-pi or covalent interaction with BNO-NS preserve their optical properties in water. Moreover, the BNO-NS vector allowed stabilizing the DOX molecules on a cellular membrane contrary to isolated DOX that randomly moved in the solvent box without any interaction with the cell membrane. From these results, we conclude that hydrophilic BNO-NS represents a good candidate for DOX…

THIOPYRANO[2,3-E]INDOL-2-ONES: ANGELICIN HETEROANALOGUES WITH POTENT PHOTOANTIPROLIFERATIVE ACTIVITY

2008

A new class of compounds, the thiopyrano[2,3-e]indol-2-ones, bioisosters of the angular furocoumarin angelicin, was synthesized with the aim of obtaining new photochemotherapeutic agents. In particular 7,8-dimethyl-thiopyranoindolone 6c s showed a remarkable phototoxicity and a great dose UVA dependence reaching IC(50) values at submicromolar level. This latter photoinduced a massive apoptosis and a remarkable photodamage to lipids and proteins. Although it did not intercalate DNA, it was able to cause photooxidation of DNA bases.

Echinoderm Antimicrobial Peptides to Contrast Human Pathogens

2013

Increased attention has been focused in marine invertebrates as a source of bioactive molecules for biomedical applications. Many bioactive molecules are part of the innate immune system. Some more recently isolated compounds, mainly from sea urchin and sea cucumber are antimicrobial peptides (AMP) active against Gram positive, Gram negative and fungi. In this review we described the most recent studies on AMP isolated from echinoderms. The AMP are little peptides <10 kDa with cationic charge and amphipathic structure. Recently, it was demonstrated that in the coelomocyte lysates of Paracentrotus. lividus and Holothuria tubulosa AMP are present with activity against staphylococcal and Pseud…

PHOTOCHEMOTHERAPEUTIC AGENTS: DESIGN, SYNTHESIS AND ANTITUMOR ACTIVITY

2009

Pyrrolo[3,2-h]quinazolines as Photochemotherapeutic Agents

2011

Heteroanalogues of angelicin, pyrrolo[3,2-h]quinazolines, were synthesized with the aim of obtaining new potent photochemotherapeutic agents. Many derivatives caused a significant decrease in cell proliferation in several human tumor cell lines after irradiation with UVA light (GI(50) =15.2-0.2 μM). Their phototoxicity effected apoptosis in Jurkat cells with the involvement of mitochondria (as determined by the loss of mitochondrial membrane potential and production of reactive oxygen species) and lysosomes. The phototoxicity of these compounds could be explained by lipid peroxidation.

Pyrrolo[3,4-h]quinolinones a new class of photochemotherapeutic agents

2011

Abstract Pyrrolo[3,4- h ]quinolin-2-ones were synthesized as nitrogen isosters of the angular furocoumarin angelicin, with the aim of obtaining new photochemotherapeutic agents with increased antiproliferative activity and lower undesired toxic effects. A versatile synthetic pathway was approached to allow the isolation of derivatives of the new ring system with a good substitution pattern on the pyrrole moiety. Photobiological screenings of the new compounds revealed a potent phototoxic effect and a great UVA dose dependence, reaching IC 50 values at submicromolar level. The induced cellular photocytotoxicity was related to apoptosis with the involvement of mitochondria and lysosomes, alte…

PEGylated graphene oxide (GO-PEG) as new carrier for chemotherapeutic agent delivery

2015

Graphene, a single layer of sp2 -hybridized carbon atoms arranged in a honeycomb two-dimensional (2-D) crystal lattice, has evoked enormous interest throughout the scientific community since its first appearance in 2004. Due to its unique structure and geometry, graphene possesses remarkable physical–chemical properties (including large specific surface area and biocompatibility) that enable it to be an ideal material for several of applications, ranging from quantum physics, nanoelectronics, energy research, catalysis and engineering of nanocomposites and biomaterials. In the area of nanomedicine, graphene and its derivatives can be exploited for a broad range of applications, including a …

Endothelial Progenitor Cells A New Real Hope?

2017

Chronic inflammatory diseases, such as cardiovascular diseases (CVDs), diabetes, Alzheimer’s disease (AD) and cancer, have a disproportionate prevalence with advancing age owing to the continuous growth in the aging population. This condition determines several medical, economic and social problems due to the dramatic increase in the number of affected individuals, who are not autonomous. Thus, research efforts are centred around reducing and/or delaying the onset and progression of these diseases by researching new strategies for early prevention and diagnosis. In this context, understanding the mechanisms involved in the tissue, organ protection and repair are imperative for the developme…