Preliminary studies of the cytotoxicity and photoprotective properties of Benzophenone and Lactone derivatives.

A Radia??o solar ultravioleta(RUV) pode induzir efeitos ? pele devidos a sua a??o direta ou indireta, por meio da gera??o de radicais livres. Esses efeitos podem provocar diversas les?es na pele humana como o c?ncer de pele. Como medida de prote??o da pele contra os efeitos da radia??o solar pode-se citar o uso de protetores solares, produtos t?picos adicionados de filtros solares UV sint?ticos com propriedades de absor??o e reflex?o de raios solares.Um fotoprotetor org?nico ideal deve proteger a pele contra os raios UVB (290-320 nm) e UVA (320-400 nm), possuir um fator de prote??o solar (FPS) seguro, ser fotoest?vel e n?o ser fotot?xico. Este trabalho objetiva em estudos preliminares de fotoprote??o dos derivados das Benzofenonas e Lactonas. Os produtos obtidos foram sintetizados e caracterizados por t?cnicas espectrosc?picas usuais e foram submetidos a ensaios de viabilidade celular frente ao MTT e determina??o do valor de prote??o solar (FPS) in vitro pelo m?todo espectrofotom?trico UV/VIS. Os espectros de IV, RMN de 1 H e RMN de 13C mostraram bandas e sinais em conformidades com as estruturas propostas para os compostos estudados. Os compostos 1 e2 apresentaram um FPS proporcional ? concentra??o analisada, ou seja, quanto maior a concentra??o, maior ? o Fator de Prote??o, por?m o composto 3 apresentou fator prote??o menor em concentra??es mais elevadas. No estudo de viabilidade celular, os compostos 1 e 2 n?o foram citot?xicos nas concentra??es avaliadas neste trabalho.Ultraviolet solar radiation can generate free radicals that damage skin and cause skin lesions or skin cancer. Sunscreens are a protective measure against the effects of solar radiation that protects the skin by absorbing or reflecting solar rays. Ideally, the sunscreen should protect the skin against UVB (290-320 nm) and UVA (320-400 nm) rays, be photostable and non-toxic. This work describes a preliminary study on the SPF of a benzophenone and a lactone derivative. The synthesized compounds were characterized by spectroscopic techniques, submitted to cell viability assays against MTT and SPF determined in vitro by UV/VIS spectroscopy measurements. The spectroscopic data was in agreement with the proposed structures of the compounds studied. The SPF was proportional to concentration, and in one case, the sun protection factor was lower at higher concentrations. The benzophenone derivatives were evaluated for toxicity by a cell viability study, and found to be non-cytotoxic at the tested concentrations

Preparation and characterization of a quercetin-tetraethyl ether-based photoprotective nanoemulsion.

Although Quercetin absorbs in the UVA/UVB electromagnetic region, it is limited for applications as a UV filter due to its low lipophilicity and capacity to penetrate the epidermis. In order to overcome this limitation, we synthetized and evaluated the photo protective properties of a derivative obtained from Quercetin. The derivative was prepared by alkylation of Quercetin with iodoethane and characterized by IR and NMR spectroscopy. The in vitro Solar Protection Factor was determined by the Mansur method and the cytotoxicity was evaluated using hepatocellular cell (Hep G2) cells. Finally, Quercetin and the corresponding derivative were incorporated in nanoemulsions. Nanoemulsions with particles sizes between 53 and 73 nm were obtained, and polydispersity indexes were around 0.1, indicating good homogeneity of the nanoemulsion particles. The cell viability study for the Quercetin derivative indicated a very low cytotoxicity profile. The chemical modification of Quercetin resulted in a promising compound with improved properties desirable for skin penetration and incorporation into sunscreen formulations

Evaluation of the, in vitro, photoprotetive capacity of Moringa oleifera oil for its use in sunscreen formulation

Moringa oleifera Lam is an Indian plant with applications in the agricultural and medical fields. The assets development capable of increasing the efficiency of sunscreens, mainly those of plant origin, due to their natural benefits, represents an increasing demand for cosmetology. The present study aims to identify by CG-MS the constituents of the most active oil and to evaluate the photoprotective capacity of Moringa oil, and its action in sunscreen formulations. Extracts of the oils from the Moringa seeds were evaluated for the Sun Protection Factor (SPF) observing the highest result for the dichloromethane extract. This extract showed low cytotoxic potential for human fibroblasts and it was incorporated into a sunscreen. The extract increased the SPF of the sunscreen and its effect may be related to fatty acids identified by GC-MS. The results showed the benefit of Moringa oil as a vegetable active in the sunscreen formulations by increasing the SPF of sunscreens in a natural and sustainable way.RESUMO Moringa oleifera Lam é uma planta indiana com aplicações nas áreas agrícolas e médica. O desenvolvimento de ativos capazes de aumentar a eficiência dos filtros solares, principalmente os de origem vegetal, devido aos seus benefícios naturais, representa uma demanda crescente por cosmetologia. O presente estudo tem como objetivo identificar por CG-MS os constituintes do óleo mais ativo e avaliar a capacidade fotoprotetora do óleo de Moringa, e sua ação em formulações de filtros solares. Os extratos dos óleos das sementes de Moringa foram avaliados quanto ao Fator de Proteção Solar (FPS), observando-se o maior resultado para o extrato de diclorometano. Este extrato apresentou baixo potencial citotóxico para fibroblastos humanos e foi incorporado a um protetor solar. O extrato aumentou o FPS do protetor solar e seu efeito pode estar relacionado aos ácidos graxos identificados por GC-MS. Os resultados mostraram o benefício do óleo de Moringa como ativo vegetal nas formulações de protetores solares por aumentar o FPS dos protetores solares de forma natural e sustentável. Palavras-chave: Moringa oleifera Lam; Formulações; Protetores solares; ácidos graxo

Preparation, characterization, and biological activity against Artemia salina of news copolymer PMMA-g-PEG derivatives incorporated with fluconazole.

The graft copolymer PMMA?g?PEG meets characteristics of their origin polymers: PMMA resistance and transparency and appropriate structure, including good solubility in water and organic solvents, lack of toxicity, and easy processing of the PEG, with inserted between the pharmacologically active polymers and can act as drugs or may be used as carriers for other drugs. The PMMA?G?PEG copolymer and their derivatives are synthesized previously and subsequently, the copolymer derivatives passed through the process of emulsification and incorporation of the drug fluconazole. Emulsified and Incorporated derivatives copolymers are characterized by Fourier?transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), differential thermal analysis (DTA), X?ray diffraction (XRD), and scanning electron microscopy (SEM) after the incorporation, in order to evaluate their effectiveness. The efficiency of incorporation is evaluated as well as the influence of polymer chain complexity in the incorporated fluconazole. Their toxicities are determined against Artemia salina Leach. The LD50 values have also been obtained for these copolymers

Compostos organofosforados pentavalentes: histórico, métodos sintéticos de preparação e aplicações como inseticidas e agentes antitumorais Organophosphorus pentavalent compounds: history, synthetic methods of preparation and application as insecticides and antitumor agents

<abstract language="eng">This paper is a review of the history, synthesis and application of organophosphorus compounds, especially of those of pentavalent phosphorus, such as phosphoramidates, phosphorothioates, phosphonates and phosphonic acids with insecticide and anticancer activities. The organophosphorus compounds with agrochemical applications show great structural variety, They include not only insecticides, but also fungicides, herbicides, and others. The large variety of commercially available organophosphorus pesticides is remarkable. Even more interesting is the high efficiency of some organophosphorus compounds as anticancer agents such as cyclophosphamide and its derivatives

Chemistry modification of PMMA-g-PEG copolymer.

Copolymers are polymers consisting of different repeat units and their production is usually motivated by the changing of polymers properties. An important application are the transportation of drugs within the organism with the aim of controlling the release of the substance. The synthesis of these new copolymers is based on simple semi-synthesis and low cost. The synthetic routes are based on the interaction of the graft copolymer (PMMA-g-PEG) with a variety of reagents such as acetic anhydride, acetic acid, methyl iodide, sulfuric acid and hydrochloric acid. The products from these reactions of esterification, methylation, acetylation and halogenation will be characterized by Fourier-transforminfrared spectroscopy (FTIR). The use of this technique allowed us to detect the main absorption bands related to the C?O bonds, C-Cl, R-COOR and CO, thus confirming the efficiency of modification reactions of the graft copolymer chain

Synthesis and characterization of new phosphorylated copolymers.

O rápido desenvolvimento da química de polímeros nos últimos anos tem acompanhado a introdução dos materiais poliméricos no campo da medicina. Polímeros com aplicações médicas podem ser subdivididos em dois grandes grupos: materiais usados em próteses e a produção de polímeros biologicamente ativos. Neste trabalho foram sintetizados copolímeros possuindo cadeia principal de poli (metacrilato de metila) e cadeias enxertadas de polietilenoglicol (COP GRAFT). A partir da síntese do copolímero enxertado inicial foram realizadas modificações em suas cadeias de modo a aumentar a possibilidade de incorporação de um fármaco que será utilizado em sistema de liberação controlada de medicamentos. Os novos compostos foram obtidos através de duas rotas sintéticas e os produtos formados ao final de cada etapa foram purificados e caracterizados. Através da técnica de infravermelho (FITIR) foi possível observar as bandas de absorções características das ligações P-H, P=O e P-O, que foram inseridas na cadeia do COP GRAFT durante a fosforilação, além das bandas de absorções características do copolímero, antes da fosforilação, como C=O e C-O. A caracterização térmica das amostras utilizando termogravimetria (TGA) e calorimetria diferencial de varredura (DSC) mostrou que apenas o copolímero de diisobutila apresentou temperatura de transição endotérmica e comportamentos de degradação compatíveis a de um polímero. Através da técnica de difração de raios X (XRD) foi possível observar uma modificação da cristalinidade das amostras, provavelmente devido a uma variação da conformação das cadeias após a inserção de novos grupos químicos. Nos cromatogramas obtidos pela técnica de cromatografia de permeação em gel (GPC) percebeu-se aumento de massa após a fosforilação com o grupo diisobutila no COPGRAFT. A reação de fosforilação foi eficiente na obtenção do copolímero de diisobutila e as técnicas aplicadas demonstraram que houve a modificação no copolímero enxertado.The rapid development in polymer chemistry has, in recent years, led to the introduction of polymeric materials in the field of medicine. Two major groups of polymers are used for medical applications: prosthetic and biologically active materials. We synthesized copolymers with the main chain consisting of poly (methyl methacrylate) and graft chains of poly(ethylene glycol) (COP GRAFT). Changes were made in the graft copolymer chains for a possible incorporation of a drug, such that it may be used for the controlled release of drugs. The synthesis of these new compounds is based on two synthetic routes and FTIR, differential scanning calorimetry (DSC), thermogravimetry (TGA) and X-ray diffraction (XRD) characterized the products formed at the end of each stage. Through FTIR we observed absorption bands characteristic of P-H, P=O and P-O bonds that were inserted into the polymer chain during phosphorylation of the COP GRAFT, beyond the absorption bands characteristic of the copolymer before phosphorylation, such as C=O and C-O. By TGA and DSC we observed that only the diisobutyl copolymer has endothermic transition temperature and degradation behavior consistent with a polymer. XRD results showed a structural and conformational change in crystallinity of modified chains. Molecular weight and polydispersity of COPGRAFT obtained by GPC increased after phosphorylation with diisobutyl group. The phosphorylation reaction was efficient in obtaining diisobutyl copolymer and the applied techniques confirmed the modification of the COPGRAFT chains

Trypanocidal activity of flavanone derivatives.

Chagas disease, also known as American trypanosomiasis, is classified as a neglected disease by the World Health Organization. For clinical treatment, only two drugs have been on the market, Benznidazole and Nifurtimox, both of which are recommended for use in the acute phase but present low cure rates in the chronic phase. Furthermore, strong side effects may result in discontinuation of this treatment. Faced with this situation, we report the synthesis and trypanocidal activity of 3-benzoyl-flavanones. Novel 3-benzoyl-flavanone derivatives were prepared in satisfactory yields in the 3-step synthetic procedure. According to recommended guidelines, the whole cell-based screening methodology was utilized that allowed for the simultaneous use of both parasite forms responsible for human infection. The majority of the tested compounds displayed promising anti-Trypanosoma cruzi activity and the most potent flavanone bearing a nitrofuran moiety was more potent than the reference drug, Benznidazole

Study of controlled release of PMMA-g-PEG copolymer and derivatives incorporated with the indomethacin drug.

Synthetic polymers are made up of repeated monomeric units, and this gives them a very versatile appearance, making them useful in many areas of science. One is the pharmaceutical, which correlates the properties of the polymer with the active principle, so they can be used as an excipient or in the controlled release system. The PMMA?g?PEG4000 has characteristics derived from its precursors, that are pharmacologically active. When we incorporate drugs into this structure, the polymer can act on the controlled release, lessening the toxic character of the drug and producing fewer side effects. In this work, incorporations of the drug indomethacin were made in the PMMA?g?PEG copolymer and derivatives (PMMA?g?PEG4000 ETIL and PMMA?g?PEG4000 ACET). The samples were characterized by infrared spectroscopy (FTIR), Scanning Electron Microscopy (SEM), thermogravimetric analysis (TGA), and atomic force microscopy (AFM) measurements. For each sample, the controlled release was performed in a total time of 4?h and the efficiency of the modified structures was verified