The present study aimed at the evaluation of Passiflora coccinea (Aubl.) antioxidant and photo protective in vitro activities, looking forward to their application as antiaging or sunscreen agents in cosmetic formulations. Methanolic and glycolic leaf extracts were prepared by three methods: ultrasound assisted extraction (UAE, 30 min.), maceration at room temperature (72 h) and maceration at 30 ºC (72 h). The antioxidant activities of the extracts were measured by DPPH and ORAC-FL assays and they were incorporated into a cosmetic emulsion to have their sun protection factor (SPF) measured spectrophotometricaly. The antioxidant activity of the emulsions were measured by DPPH and ORAC as well. C-glycosyl-flavones were identified in the extracts by ESI-MS/MS, in comparision with standards. The UAE methanolic extract and the maceration at 30 ºC glycolic extract were submmited to HPLC-DAD analysis and isovitexin was quantifyed in both by a validated method. The methanolic extract antioxidant activity was independent of the extraction method, higher than reported for other species of Passiflora and detectable when incorporated into the emulsion formulation. Maceration at 30oC was the most suitable method for glycolic extraction and its antioxidant activity was lower than the value presented by the methanolic extracts. None of the extracts exhibited a SPF value. Isovitexin in the UAE methanolic extract was 12.67 times higher than the most active glycolic extract, aside of their similar chromatographic profiles. Although a SPF value was not detected, the results indicate that P. coccinea can be a potential new source of antioxidants for topical antiaging formulations.

Abstract The objective of this study was to evaluate the effects of Cymbopogon citratus essential oil and its main compound (citral) against primary dental colonizers and caries-related species. Chemical characterization of the essential oil was performed by gas chromatography/mass spectroscopy (GC/MS), and the main compound was determined. Antimicrobial activity was tested against Actinomyces naeslundii, Lactobacillus acidophilus, S. gordonii, S. mitis, S. mutans, S. sanguinis and S. sobrinus. Minimum inhibitory and bactericide concentrations were determined by broth microdilution assay for streptococci and lactobacilli reference, and for clinical strains. The effect of the essential oil on bacterial adhesion and biofilm formation/disruption was investigated. Negative (without treatment) and positive controls (chlorhexidine) were used. The effect of citral on preformed biofilm was also tested using the same methodology. Monospecies and microcosm biofilms were tested. ANOVA or Kruskal-Wallis tests were used (α=0.05). Cytotoxicity of the essential oil to human keratinocytes was performed by MTT assay. GC/MS demonstrated one major component (citral). The essential oil showed an inhibitory effect on all tested bacterial species, including S. mutans and L. acidophilus. Essential oil of C. citratus (10X MIC) reduced the number of viable cells of lactobacilli and streptococci biofilms (p < 0.05). The essential oil inhibited adhesion of caries-related polymicrobial biofilm to dental enamel (p < 0.01). Citral significantly reduced the number of viable cells of streptococci biofilm (p < 0.001). The essential oil showed low cytotoxicity to human keratinocytes. Based on these findings, this study can contribute to the development of new formulations for products like mouthwash, against dental biofilms.

AbstractIn this study, antiproliferative and antioxidant activities of crude extracts (hexane, ethyl acetate and methanol) from leaves and stem of Chresta sphaerocephala DC., Asteraceae, were investigated. Antiproliferative activity was tested in vitro against ten human cancer cells and against VERO (no cancer cell). Antioxidant activities were determined using DPPH and ORAC-FL assays and the total phenolic content was estimated by Folin–Ciocalteu method. Hexane and ethyl acetate extracts (leaves and stem) exhibited antiproliferative activity against cancer cell lines with total growth inhibition (TGI) between 50.40 and 250 µg/ml. For VERO cell, TGI values were >250 µg/ml for all extracts, except to hexane extract of the stem (TGI 80.92 µg/ml). In an initial evaluation, ethyl acetate and methanol extracts (leaves and stem) have shown levels of phenolic compounds between 6.94 and 30.96 mg GAE/kg in Folin–Ciocalteu assay, DPPH free-radical scavenging activity with SC50 in the range of 75.22 and 400 µg/ml and antioxidant capacity between 290.08 and 1088 µmol TE/g of extract in ORAC-FL assay. HPLC-DAD and ESI-MS analysis allowed the identification of flavonoids in the methanol extract from the leaves of C. sphaerocephala. Three steroids and nine triterpenoids were identified in the bioactive hexane extracts using HRGC.

<p>The phytochemical investigation of the stem bark of <italic>Annona pickelii</italic> yielded four steroids (β-sitostenone, β-sitosterol, stigmasterol and campesterol), three lignans (eudesmin, magnolin and yangambin), twelve alkaloids (liriodenine, lysicamine, atherospermidine, anonaine, analobine, asimilobine, discretamine, stepholidine, coclaurine, orientaline, juziphine and stepharine), and a benzenoid (2-methoxybenzoic acid). These compounds support their recent reclassification from <italic>Rollinia</italic> to <italic>Annona</italic>, and that it is a typical species of the family Annonaceae. Significant antifungal and antioxidant activities were found for the methanol crude extract as well as for the lignans eudesmin, magnolin, yangambin and the alkaloid discretamine. In addition, several items of NMR data for the alkaloids were reviewed and unequivocally described in this work.</p>

Activity guided fractionation of Sinningia allagophylla (Mart.) Wiehler ethanolic extract yielded a new benzochromene 8-methoxylapachenol, besides seven known compounds: lapachenol, sitosteryl oleate, sitosteryl linoleate, stigmasteryl oleate, stigmasteryl linoleate, dunniol and tectoquinone. Extract, fractions, and compounds lapachenol, 8-methoxylapachenol, and dunniol were tested in vitro against human cancer cell lines U251 (glioma, CNS), MCF-7 (breast), NCI-ADR/RES (drug-resistant ovarian), 786-0 (kidney), NCI-H460 (lung, no small cells), PC-3 (prostate), OVCAR-3 (ovarian), HT-29 (colon), K562 (leukemia) and against VERO, a normal cell line. The most active compound was dunniol, which inhibited the growth of U251, MCF-7, NCI-ADR/RES, OVCAR-3 and K562 cell lines.

Phytochemical investigation of the hexane extract from the stem of Xylopia laevigata led to the isolation of the ent-kaurane diterpenoids, ent-kaur-16-en-19-oic acid, 4-epi-kaurenic acid, ent-16β-hydroxy-17-acetoxy-kauran-19-al, ent-3β-hydroxy-kaur-16-en-19-oic acid, and ent-16β,17-dihydroxy-kauran-19-oic acid, as well as spathulenol and a mixture of β-sitosterol, stigmasterol and campesterol. The identification of the compounds was performed on the basis of spectrometric methods including GC-MS, IR, and 1D and 2D NMR. Potent larvicidal activity against Aedes aegypti larvae with LC50 of 62.7 µg mL-1 was found for ent-3β-hydroxy-kaur-16-en-19-oic acid. This compound also showed significant antifungal activity against Candida glabrata and Candida dubliniensis with MIC values of 62.5 µg mL-1.

The essential oil obtained by hydrodistillation from fresh leaves of Casearia lasiophylla Eichler, Salicaceae, was analyzed by gas capillary (GC/FID and GC/MS). The cytotoxicity of the leaves essential oil was tested in vitro againstU251 (glioma), UACC-62 (melanoma), MCF-7 (breast), NC1-ADR/RES (ovarian-resistant), NCI-H460 (lung), PC03 (prostate), OVCAR-3 (ovarian), HT-29 (colon) and K562 (leukemia) human cancer cells and against VERO (no cancer cell). The yield of oil was 0.02%. Fifty two compounds were identified, representing 87.1% of the total of the oil. The main components were identified as germacrene D (18.6%), β-caryophyllene (14.7%), δ-cadinene (6.2%), and α-cadinol (5.4%). The oil exhibited antiproliferative activity against all cell lines (TGI<100 µg/mL), with exception of NCI-H460 cell line (TGI 191.31 µg/mL). The highest activity was observed against UACC-62 (TGI 7.30 µg/mL), and K562 (TGI 7.56 µg/mL) cell lines. The observed activity could be related to high content of germacrene D and β-caryophyllene, compounds known as cytotoxic.

Neste trabalho foram utilizados dois distintos secadores (leito de jorro e spray dryer) para a produção de extratos secos de Bauhinia forficata Link (Leguminosae, Caesalpinoideae) obtendo-se um produto seco com elevada qualidade em termos de suas propriedades físicas e químicas. Análises qualitativas obtidas por CLAE revelam que os perfis cromatográficos dos compostos flavonóides presentes nos extratos secos não apresentaram significativas mudanças durante a secagem quando comparados aos perfis obtidos para os extratos concentrados. Em geral, a secagem por leito de jorro acarreta menores perdas dos flavonóides totais do que a secagem em spray drying. A atividade antioxidante dos extratos secos foi examinada pelos métodos de (DPPH•) e peroxidação lipídica induzida por Fe+2 (LPO). Uma pequena redução na atividade sequestradora de radicais livres observada para os extratos secos pode ser associada com a ocorrência de reações oxidativas, decomposição e/ou perdas de compostos termolábeis induzidas pelo calor.

Two distinct drying methods (spouted bed and spray drying) were used for production of dried extracts of Bauhinia forficata Link (Leguminosae, Caesalpinoideae). High-quality powder products in terms of physical and chemical properties were obtained. HPLC fingerprints revealed that the chromatographic profiles of flavonoid compounds present in the dried extract did not change significantly, due to drying. In general, the spouted bed drying caused a degradation of total flavonoids than was lower than that of the spray drying. Antioxidant properties of the dried extract, examined by their radical scavenging activity using 2,2-diphenyl-1-picrylhydrazyl radical (DPPH•) and inhibition of lipid peroxidation induced by Fe+2 assays (LPO), confirmed their antioxidant potential. The slight reduction in scavenging activity of the dried extracts may be associated with the occurrence of oxidative reactions, decomposition or losses of thermolabile compounds, induced by the heat.

Alternanthera tenella Colla extracts are used in Brazilian traditional folk medicine to treat a variety of infectious diseases as well as inflammation and fever. In this work, the immunomodulatory, anti-inflammatory and potential toxic effects of cold (CAE) and hot (HAE) aqueous extracts of A. tenella were investigated in vivo. In addition, we analyzed the phytochemical properties of both extracts. BALB/c mice were immunized in vivo with sheep red blood cells and concomitantly inoculated intraperitoneally (i.p.) with each extract (50, 100 or 200 mg/kg). Specific antibody-producing cells were enumerated using plaque-forming cell assays (PFC) and anti-SRBC IgG and IgM serum levels were measured via enzyme-linked immunosorbent assay. Body and lymphoid organ weights were determined after treatments in order to evaluate toxic effects. Carrageenan-induced paw edema was employed to investigate anti-inflammatory activity in mice inoculated i.p. with CAE or HAE (200 or 400 mg/kg). Phytochemical screening was performed using spectrometric and chromatographic approaches and revealed that CAE possessed higher tannin and flavonoid levels than HAE. PFC numbers were increased after treatment with CAE (100 mg/kg) four days after immunization, as were the serum antibody titers after four and seven days, suggesting immunostimulatory activity through modulation of B lymphocyte functions. Body and organ weights did not show major changes, suggesting that extracts administered to mice did not induce significant toxicity. Both extracts had significant anti-inflammatory activity in the paw edema assay. These results suggested that aqueous extracts from A. tenella contained several chemical compounds that possess positive and/or negative modulator effects on the immune system, which appeared to correlate with tannin and flavonoid levels in those extracts. In summary, these studies provide important insight into the biological activities of A. tenella.

O fracionamento dos extratos bioativos de Chresta scapigera proporcionou o isolamento de triterpenos e flavonóides, dentre os quais acetato de beta-amirina (1), acetate de 11alfa,12-oxidotaraxeril (2) e lupeol (3), assim como os flavonóides apigenina (6), caenferol (7), crisoeriol (8) e luteolina (9) mostraram-se ativos contra formas amastigotas de Leishmania amazonensis, enquanto, apenas os flavonóides (6), (7) e (9) apresentaram toxicidade contra as formas tripomastigotas de Trypanosoma cruzi.

Fractionation of bioactive crude extracts of Chresta scapigera led to the isolation of four triterpenes and five flavonoids, among them beta-amyrin acetate (1), 11alpha,12alpha-oxidetaraxeryl acetate (2) and lupeol (3), as well as the flavonoids apigenin (6), kaempferol (7), crysoeriol (8) and luteolin (9) were active against Leishmania amazonensis amastigotes-like stages, while only the flavonoids (6), (7) and (9) showed toxicity towards bloods trypomastigote forms of Trypanosoma cruzi.

As atividades tripanocida, leishmanicida, antibacteriana e antifungica dos extratos brutos de Chresta exsucca foram investigadas. Formas tripomastigotas do Trypanosoma cruzi, formas amastigotas de Leishmania amazonensis e vinte cepas de microrganismos, incluindo bactérias Gram-positivas, Gram-negativas e leveduras, foram utilizadas nos ensaios biológicos. Os melhores resultados foram obtidos para a atividade leishmanicida. A composição química dos extratos hexânicos e etanólicos dessa espécie foi determinada empregando-se técnicas cromatográficas como HRGC e HPLC-ESI-MS, respectivamente. Esteróides, triterpenos e flavonóides foram identificados.

Crude extracts of Chresta exsucca were investigated for their in vitro trypanocidal, leishmanicidal, antibacterial and antifungal activities. Trypomastigote forms of Trypanosoma cruzi, amastigote-like forms of Leishmania amazonensis and twenty strains of microorganisms including Gram-positive and Gram-negative bacteria and yeasts were utilized in the bioassays. The best results were found for the leishmanicidal activity. The chemical composition of hexanic and ethanolic extracts of this species was determinate using chromatographic techniques as HRGC and HPLC-ESI-MS, respectively. Steroids, triterpenes and flavonoids were identified.

Os extratos diclorometânicos e etanólicos de folhas e caule de Chromolaena squalida e de folhas e flores de Chromolaena hirsuta foram avaliados quanto à atividade antimicrobiana. Oito flavonóides e cinco esteróides foram desafiados frente a 22 cepas indicadoras, incluindo bactérias (Gram-positivas e Gram-negativas) e leveduras. Todos os extratos brutos, flavonóides e esteróides ensaiados mostraram atividade antimicrobiana, principalmente frente a bactérias Gram-positivas.

The crude extracts (dichloromethanic and ethanolic) and some compounds (8 flavonoids and 5 steroids) isolated from Chromolaena squalida (leaves and stems) and Chromolaena hirsuta (leaves and flowers) have been evaluated against 22 strains of microorganisms including bacteria (Gram-positive and Gram-negative) and yeasts. All crude extracts, flavonoids and steroids evaluated have been shown actives, mainly against Gram-positive bacteria.