Perillyl alcohol has been studied in the treatment of cancer disease. However, its high toxicity is a drawback, which can be overcome by its incorporation in nanostructured systems. The aim of this work was to develop and validate a chromatographic method for determination of perillyl alcohol encapsulation efficiency in a polymeric nanoparticles formulation and evaluation of the presence of related degradation products. Perillyl alcohol was subjected to forced conditions of hydrolysis (acidic, alkaline and neutral), oxidation, photolysis and thermal stress, as suggested in the International Conference of Harmonization (ICH) guidelines. The drug showed significant degradation under acidic conditions. The degradation products could be adequately separated on an XBridge C18 column (100 × 2.1 mm, 3.5 µm) using isocratic elution (350 µL min−1) of water/acetonitrile (65 : 35, v/v) at 210 nm. Data from validation studies demonstrated that the method is selective, linear (coefficient of determination (R2) > 0.999) over the range of 20.0-80.0 µg mL−1, precise (relative standard deviation (RSD) < 2.0%), accurate (98.07 to 101.99%) and robust for minor changes. The method was successfully applied to determine the encapsulation efficiency of perillyl alcohol in polymeric nanoparticles, both for product development and for quality control purposes. After nanoparticles production, the presence of degradation products was not observed indicating that the single-emulsion solvent-evaporation technique used does not favor chemical degradation of the drug.

Nesse estudo, nós avaliamos o efeito da nicotina sobre a oxidação da LDL pelo sistema MPO/H2O2/Cl- e o efeito do HOCl sobre a LDL e alguns de seus componentes, tais como metil linoleato, vitamina E e o aminoácido triptofano. Nicotina, em concentração micromolar, amplia a oxidação do triptofano, livre em solução ou presente na LDL. A nicotina promove a diminuição da formação de dienos conjugados e consumo de oxigênio no sistema metil linoleato/HOCl, e houve evidência que sugere aumento na formação de clorohidrinas. O aumento da oxidação da vitamina E pelo HOCl também foi observada na presença de nicotina. Esses dados mostram que a interação da nicotina e HOCl pode promover alterações bioquímicas significativas na partícula de LDL e alguns de seus componentes envolvidos na patogênese de doenças cardiovasculares e de outras doenças.

In this study, the effect of nicotine on the LDL oxidation by the MPO/H2O2/Cl- system and the effect of HOCl on LDL and some of its components, such as methyl linoleate, vitamin E and the amino acid tryptophan were explored. Nicotine, in micromolar concentrations, enhanced the tryptophan oxidation, either present in LDL or free, in solution. Nicotine also decreased the formation of conjugated dienes and oxygen consumption in a methyl linoleate / HOCl system, and there was evidence to suggest an increase in chlorohydrin formation. Acceleration of the vitamin E oxidation by HOCl was also observed in the presence of nicotine. These data show that the interaction of nicotine and HOCl can promote significant biochemical modifications in LDL particle and some of its components involved in the pathogenesis of cardiovascular and other diseases.

Cogumelos apresentam propriedades nutricionais e medicinais bastante empregadas na manutenção da saúde humana e têm sido considerado por pesquisadores como possíveis fontes de seqÜestradores de radicais livres. Neste trabalho, as propriedades antioxidantes de extratos aquosos de Agaricus blazei Murill, produzidos por maceração e decocção, são demonstrados in vitro. A resistência à oxidação é demonstrada através de três mecanismos: i) inibição de processos oxidativos enzimáticos, with 100% de inibição da HRP (horseradish peroxidase) e MPO (myeloperoxidase); ii) inibição do estresse oxidativo celular, com 80% de inibição do oxidative burst de neutrófilos polimorfonucleares (PMN) e iii) ação direta sobre espécies reativas, com 62% e 87% de supressão do HOCl e ânion superóxido (O2• –), respectivamente. A partir destes dados, concluise que o extrato aquoso deste cogumelo tem significativa capacidade antioxidante, indicando sua possível aplicação para propósitos nutracêuticos e medicinais.

Mushrooms possess nutritional and medicinal properties that have long been used for human health preservation and that have been considered by researchers as possible sources of free radical scavengers. In this work, the antioxidant properties of water extracts from Agaricus blazei Murill, produced by maceration and decoction, are demonstrated in vitro. Resistance to oxidation is demonstrated through three mechanisms: i) inhibition of enzymatic oxidative process, with 100% inhibition of HRP (horseradish peroxidase) and MPO (myeloperoxidase); ii) inhibition of cellular oxidative stress, with 80% inhibition of the oxidative burst of polymorphonuclear neutrophils (PMNs); and iii) direct action over reactive species, with 62% and 87% suppression of HOCl and superoxide anion radical (O2• –), respectively. From the data, it was concluded that the aqueous extract of A. blazei has significant antioxidant activity, indicating its possible application for nutraceutical and medicinal purposes.

Astilbin (5,7,3’,4’-tetrahydroxy-2,3-dihydroflavonol-3-ß-o-rhamnoside), a flavonoid with a large range of biological activities, was isolated from Dimorphandra mollis, a shrub common to the Brazilian Cerrado. The purpose of this study is to verify the effects of astilbin on myeloperoxidase (MPO) and horseradish peroxidase (HRP), and its antioxidant activity against hypochlorous acid (HOCl) and total antioxidant activity (TAC) by the 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation (ABTS•+). Astilbin inhibited MPO and HRP activities in a concentration-dependent relationship and effectively scavenged HOCl. The TAC by ABTS•+ of astilbin (IC50 ~ 20 mM) was higher than that of uric acid, which was used as a positive control. These data demonstrate that astilbin is a potent antioxidant and that it inhibits MPO and HRP activities efficiently.

There is abundant evidence that reactive oxygen species are implicated in several physiological and pathological processes. To protect biological targets from oxidative damage, antioxidants must react with radicáis and other reactive species faster than biological substrates do. The aim of the present study was to determine the in vitro antioxidant activity of aqueous extracts from leaves of Bauhinia forficata Link (Fabaceae - Caesalpinioideae) and Cissus sicyoides L. (Vitaceae) (two medicinal plants used popularly in the control of diabetes mellitus), using several different assay systems, namely, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) decolorization, superoxide anión radical (0(2)•-) scavenging and myeloperoxidase (MPO) activity. In the ABTS assay for total antioxidant activity, B. forficata showed IC50 = 8.00±0.07 μg/mL, while C. sicyoides showed IC50 = 13.0±0.2 μg/mL. However, the extract of C. sicyoides had a stronger effect on 0(2)•- (IC50 = 60.0±2.3 μg/mL) than the extract of B. forficata (IC50 = 90.0±4.4 μg/ mL). B. forficata also had a stronger inhibitory effect on MPO activity, as measured by guaiacol oxidation, than C. sicyoides. These results indicate that aqueous extracts of leaves of B. forficata and C. sicyoides are a potential source of natural antioxidants and may be helpful in the prevention of diabetic complications associated with oxidative stress.