Celso Luiz Salgueiro Lage

Produtos naturais para o controle da transmissão da dengue: atividade larvicida de Myroxylon balsamum (óleo vermelho) e de terpenóides e fenilpropanóides

The bioassay-guided fractionation of the hexane extract obtained from the medicinal plant Myroxylon balsamum (red oil) was conducted in preparative thin layer chromatography on silica gel. The obtained fractions and some terpenoids and phenylpropanoids were assayed as larvicidal on third instar Aedes aegypti larvae, NPPN colony. The results indicate that the sesquiterpene nerolidol was the active constituent in the extract and that the sesquiterpenes were more active than the monoterpenes and phenylpropanoids utilized in this study. Lipophilicity seems to be an important property for the activity since the compounds with hydroxyl, carbonyl and methoxyl groups were less active. The results confirm also that essential oils can be a good tool for the control of dengue.

Análise do óleo essencial de folhas de três quimiotipos de Lippia alba (Mill.) N. E. Br. (Verbenaceae) cultivados em condições semelhantes

A composicao do oleo essencial de Lippia alba apresenta variacao quantitativa e qualitativa, levando a separacao em quimiotipos. O trabalho tem como objetivo analisar o oleo essencial de folhas de tres quimiotipos de Lippia alba, provenientes de diferentes regioes do Brasil, cultivados em condicoes semelhantes, a fim de verificar se as diferencas na composicao do oleo devem-se a fatores ambientais ou a variacao genetica infraespecifica e se a floracao influencia o rendimento e a composicao do oleo. Os quimiotipos produtores de citral, carvona e linalol, foram denominados Lippia alba 1, 2 e 3, respectivamente. Os oleos essenciais foram extraidos por hidrodestilacao de folhas e analisados por cromatografia com fase gasosa e cromatografia com fase gasosa acoplada ao espectrometro de massas. O melhor rendimento foi obtido das plantas no estagio vegetativo. A composicao do oleo essencial manteve-se inalterada para os tres quimiotipos apos cultivo em condicoes semelhantes e tambem nao variou qualitativamente durante o crescimento vegetativo e floracao. Os dados obtidos reforcam a ideia que as diferencas na composicao do oleo essencial dos quimiotipos refletem variacoes genotipicas entre as plantas e que a extracao de oleo essencial de L. alba deve ser efetuada na fase de crescimento vegetativo, quando e maior o rendimento do oleo e a porcentagem dos componentes majoritarios.

Biochemical behaviour of norbixin during in vitro DNA damage induced by reactive oxygen species

Naturally occurring antioxidants such as carotenoids are extensively studied for their potential in reducing the risk for cancer and other chronic diseases. In the present study, the radical-scavenger activity of the food additive norbixin, a water-soluble carotenoid extracted from Bixa orellana seeds and commercialized as annatto, was evaluated under conditions of DNA damage induced by reactive oxygen species, particularly by hydroxyl radicals. The cell-free scavenger activity of norbixin was evaluated using plasmid DNA as target molecule and Sn2+ or Fe2+ as oxidant. The addition of H2O2 enhanced DNA breakage induced by metal ions, particularly Fe2+. Under these conditions, norbixin started to protect plasmid DNA against single- and double-strand breakage at a metal:norbixin ratio of 1:1 (Sn2+) and 1:10 (Fe2+). However, at lower ratios to Sn2+, norbixin enhanced Sn2+-induced DNA breakage (P < 0.05). The ability of norbixin to protect genomic DNA against oxidative damage was assessed in murine fibroblasts submitted to H2O2-induced oxidative stress and the results were evaluated by the comet assay. Under low serum conditions (2 % fetal bovine serum (FBS)), a protective effect of norbixin against H2O2-induced DNA breakage was inversely related to its concentration, a protection ranging from 41 % (10 microm) to 21 % (50 microm). At higher concentrations of norbixin, however, oxidative DNA breakage was still enhanced, even in the presence of a high serum concentration (10 % FBS). Under normal conditions, norbixin per se has no detectable genotoxic or cytotoxic effects on murine fibroblasts. The antimutagenic potential of norbixin against oxidative mutagens was also evaluated by the Salmonella typhimurium assay, with a maximum inhibition of 87 % against the mutagenicity induced by H2O2. Although plasmid DNA and Ames data indicated that norbixin can protect DNA against oxidative damage, it seems to be a risky guardian of genomic DNA as it can also increase the extent of oxidative damage.

Norbixin ingestion did not induce any detectable DNA breakage in liver and kidney but caused a considerable impairment in plasma glucose levels of rats and mice

From the seeds of Bixa orellana are extracted the carotenoids bixin and norbixin that have been widely used for coloring food. In this study, the toxicity of norbixin, purified or not (annatto extract containing 50% norbixin), was investigated in mice and rats after 21 days of ingestion through drinking water. Mice were exposed to doses of 56 and 351 mg/kg (annatto extract) and 0.8, 7.6, 66 and 274 mg/kg (norbixin). Rats were exposed to doses of 0.8, 7.5 and 68 mg/kg (annatto extract) and 0.8, 8.5 and 74 mg/kg (norbixin). In rats, no toxicity was detected by plasma chemistry. In mice, norbixin induced an increase in plasma alanine aminotransferase activity (ALT) while both norbixin and annatto extract induced a decrease in plasma total protein and globulins (P < 0.05). However, no signs of toxicity were detected in liver by histopathological analysis. No enhancement in DNA breakage was detected in liver or kidney from mice treated with annatto pigments, as evaluated by the comet assay. Nevertheless, there was a remarkable effect of norbixin on the glycemia of both rodent species. In rats, norbixin induced hyperglycemia that ranged from 26.9% (8.5 mg/kg norbixin, to 52.6% (74 mg/kg norbixin, P < 0.01) above control levels. In mice, norbixin induced hypoglycemia that ranged from 14.4% (0.8 mg/kg norbixin, P < 0.05) to 21.5% (66 mg/kg norbixin, P < 0.001) below control levels. Rats and mice treated with annatto pigments showed hyperinsulinemia and hypoinsulinemia, respectively indicating that pancreatic beta-cells were functional. More studies should be performed to fully understand of how species-related differences influences the biological fate of norbixin.

Increased antioxidant activity and changes in phenolic profile of Kalanchoe pinnata (Lamarck) Persoon (Crassulaceae) specimens grown under supplemental blue light.

Antioxidant compounds protect plants against oxidative stress caused by environmental conditions. Different light qualities, such as UV‐A radiation and blue light, have shown positive effects on the production of phenols in plants. Kalanchoe pinnata (Lamarck) Persoon (Crassulaceae) is used for treating wounds and inflammations. Some of these beneficial effects are attributed to the antioxidant activity of plant components. We investigated the effects of blue light and UV‐A radiation supplementation on the total phenol content, antioxidant activity and chromatographic profile of aqueous extracts from leaves of K. pinnata. Monoclonal plants were grown under white light, white plus blue light and white plus UV‐A radiation. Supplemental blue light improved the antioxidant activity and changed the phenolic profile of the extracts. Analysis by HPLC of supplemental blue‐light plant extracts revealed a higher proportion of the major flavonoid quercetin 3‐O‐α‐l‐arabinopyranosyl (1→2) α‐l‐rhamnopyranoside, as well as the presence of a wide variety of other phenolic substances. These findings may explain the higher antioxidant activity observed for this extract. Blue light is proposed as a supplemental light source in the cultivation of K. pinnata, to improve its antioxidant activity.

Influence of cultivation conditions, season of collection and extraction method on the content of antileishmanial flavonoids from Kalanchoe pinnata.

ETHNOPHARMACOLOGICAL RELEVANCE Leaves from Kalanchoe pinnata (Lamarck) Persoon (Crassulaceae) are popularly used for healing wounds. Its antileishmanial properties are established in experimental animals, and its active flavonoid components have been identified. AIM OF THE STUDY In this study, we attempted to standardize the extract from K. pinnata leaves by evaluating the influence of season of harvest, sunlight exposure and method of extraction on antileishmanial flavonoids content. MATERIALS AND METHODS HPLC-DAD-MS was used to identify and quantify the active antileishmanial flavonoids in different extracts. ANOVA test for analyses of variance followed by the Tukey test of multiple comparisons were used in the statistical analysis. The antileishmanial potential was assessed by the activation of nitric oxide production by murine macrophage using the Griess method. RESULTS We demonstrated that active flavonoids were significantly more abundant when the leaves were collected in the summer, and that aqueous extraction at 50°C allowed the highest flavonoid extraction. The benefit of sunlight exposure was confirmed in plants cultivated under direct sunlight when compared with those that grown under shade. Under sunny conditions the yield of the most active antileishmanial favonoid quercitrin was increased by 7-fold. All aqueous extracts tested were capable to enhance the macrophage nitric oxide production. However, hot aqueous extract from leaves collected in summer exhibited the higher activity, in agreement with HPLC-DAD-MS analysis tendency. In addition, with the aim of reducing the individual chemical variations of the plant constituents and optimizing the production of the active extract, it was obtained in vitro monoclonal KP specimens that were easily adapted to field conditions and were able to produce antileishmanial flavonoids. CONCLUSION Our study reports the better conditions of cultivation, harvest and extraction protocol for obtaining a K. pinnata extract exhibiting the highest antileishmanial activity. Additionally, we propose the flavonoids quercetin 3-O-α-L-arabinopyranosyl (1→2)-α-L-rhamnopyranoside and quercitrin, as satisfactory chemical markers for standardization purposes.

Influence of growth regulators in biomass production and volatile profile of in vitro plantlets of Thymus vulgaris L.

In vitro shoots of thyme (Thymus vulgaris L.) were established, and the effects of the auxin indole-3-acetic (IAA) acid and the cytokinins benzyladenine (BA), zeatin (ZEA), and kinetin (KIN) at 1.0, 5.0, and 10.0 microM on rooting, biomass production, and volatile compounds production by these plants were investigated. The volatiles were extracted by solid phase microextraction (SPME) and analyzed by gas chromatography. The highest biomass shoot growth was obtained with BA at 5.0 microM, while IAA at all concentrations tested achieved 100% rooting frequency. The three major compounds were gamma-terpinene (22.8-38.8%), p-cymene (13.8-27.9%), and thymol (6.5-29.0%). Quantitative changes of these compounds were observed in response to the effect of varying growth regulators concentrations in the culture medium. Growing Thymus vulgaris L. plants in media supplemented with IAA at 1.0 microM increased volatile compounds such as thymol by 315%. Nevertheless, the same major compounds were produced in all treatments and no qualitative changes were observed in the volatile profile of thyme plants.

Potential use of Piper nigrum ethanol extract against pyrethroid-resistant Aedes aegypti larvae

Fractionation of Piper nigrum ethanol extract, biomonitored by assays on pyrethroid-resistant Aedes aegypti larvae yielded isolation of the larvicidal amides piperolein-A and piperine. Comparing LC50 values, the ethanol extract (0.98 ppm) was the most toxic, followed by piperolein-A (1.46 ppm) and piperine (1.53 ppm).

What is the Destiny of Patents of Brazilian Universities

The power of patent is expressed when the innovative product or process goes to market, and the exclusive right that patent ensures generates the market power, and the holder possibility to obtain competitive advantage over competitors. Thus, it becomes compelling the discussions on the universities need for transformation of patent applications efforts into granted patents, which could be negotiated with a higher degree of juridical certainty and, consequently, higher value added. To establish an Index of Patents Granting, and understand the importance of Technological Innovation Nuclei for the increase of this index, it was developed a survey on the number of patents granted to Brazilian universities and evaluated the structure of Technological Innovation Nuclei of these universities. From the survey on the granting cases, it was verified that the universities presenting, among other characteristics, better structured Technological Innovation Nuclei stood out.

Kinetin Enhanced Linalool Production by in vitro Plantlets of Lippia alba

Abstract Lippia alba Mill. N. E. Br (Verbenaceae) is an aromatic shrub widely distributed in Brazil where the infusion of its leaves is used in folk medicine due to sedative and antispasmodic properties. This study presents data about quantitative variation of the major volatile constituents of the linalool producing L. alba chemotype. The volatiles were extracted by solid phase microextraction (SPME) from plants cultivated in soil (mother plants), from in vitro plantlets grown in Murashige & Skoog (MS) medium and from in vitro plantlets grown in MS medium with growth regulators. The content of α-pinene, (Z)-3-hexenyl acetate and α-gurjunene was greater in the mother plants than in plantlets, whereas the content of sabinene, myrcene, 1,8-cineole and p-mentha-1,5,8-triene was lower. The addition of 0.23 μM of IAA to the medium significantly enhanced sabinene and myrcene contents. The addition of 0.92 μM of kinetin significantly increased the 3(S)-(+)-linalool level.