Identification of bioactive compounds and cytogenotoxicity of the essential oil from the leaves of Croton heliotropiifolius Kunth.

Croton heliotropiifolius Kunth, popularly known as "quince" and "velame," contains a high concentration of volatile oils in the leaves, and widely used in folk medicine as an antiseptic, analgesic, sedative, anti-inflammatory, spasmolytic and local anesthetic. The objectives of this investigation were to (1) identify the phytochemical compounds and (2) assess the cytogenotoxicity of the essential oil extracted from the leaves of C. heliotropiifolius Kunth. The oil was extracted utilizing hydrodistillation and phytochemical profile determined using gas chromatography and mass spectrometry (GCMS). In the toxicogenetics analysis, Allium cepa roots were exposed to 1% dimethylsulfoxide or methylmethanesulfonate (MMS, 10 µg/ml) negative and positive controls, respectively, and to C. heliotropiifolius oil at 6 concentrations (0.32; 1.6; 8; 40; 200 or 1000 µg/ml). The phytochemical profile exhibited 40 chromatographic bands, and 33 compounds identified. α-pinene (16.7%) and 1,8-cineole (13.81%) were identified as the major compounds. Some of these identified secondary metabolites displayed biological and pharmacological activities previously reported including antiseptic, analgesic, sedative, anti-inflammatory as well insecticidal, antiviral, anti-fungal actions. In the A. cepa test, C. heliotropiifolius leaves oil induced cytotoxicity at concentrations of 0.32, 1.6 or 200 µg/ml and genotoxicity at 200 or 1000 µg/ml as evidenced by increased presence of micronuclei and significant chromosomal losses. Based upon our observations data demonstrated that the essential oil of C. heliotropiifolius leaves contain monoterpene hydrocarbons, and oxygenated monoterpenes, sesquiterpenes, and oxygenated sesquiterpenes which are associated with cytotoxic and genotoxic responses noted in on A. cepa cells.

Development of Chlorhexidine Digluconate and Lippia sidoides Essential Oil Loaded in Microemulsion for Disinfection of Dental Root Canals: Substantivity Profile and Antimicrobial Activity.

The dental intracanal disinfection is crucial to achieve the success of endodontic treatment, avoiding the maintenance of endodontic infections. Chlorhexidine digluconate can act as an irrigating agent for it. However, it can cause tissue irritation in high concentrations. Therefore, combinations with other antimicrobial agents and more efficient therapeutic alternatives are studied, which make it possible to administer drugs more safely and with minimal adverse effects. Thus, the objective of this study was the development of a microemulsion containing chlorhexidine digluconate and essential oil of Lippia sidoides to be used for disinfection of dental root canals and to evaluate its profile of substantivity and antimicrobial activity. The microemulsions were obtained through phase diagrams, using the spontaneous formation method. We completed a physical-chemical characterization and evaluate the stability of the microemulsions, in addition to the substantivity profile in a bovine root dentin model, and in vitro antibacterial effect on Enterococcus faecalis. A method for quantifying chlorhexidine was developed using UV-Vis spectroscopy. The microemulsions showed acid pH, conductivity above 1.3 µScm-1, and dispersion index similar to water. The microemulsions showed antimicrobial inhibition halos similar to the commercial gel conventionally used, but with four times more substantivity to dentinal tissues. Microemulsions were obtained as a therapeutic alternative to formulations available on the market, presenting themselves as a system with great potential for the administration of drugs for disinfection of root canals.

Caracterización química y evaluación de las propiedades antioxidantes y antimicrobianas del aceite de pulpa de frutas de Mauritia flexuosa L. f. / Chemical characterization and evaluation of antioxidant and antimicrobial properties of the pulp oil of fruits of Mauritia flexuosa L. f

Este estudio tuvo como objetivo caracterizar las propiedades químicas, antioxidantes y antimicrobianas del aceite de pulpa de Mauritia flexuosa L. f. (Arecaceae). La identificación química se realizó por cromatografía de gases acoplada a espectrometría de masas. Se caracterizaron las propiedades fisicoquímicas. La capacidad antioxidante se ha verificado eliminando los radicales libres, reduciendo y quelando el hierro. La actividad antimicrobiana se evaluó mediante la concentración inhibitoria mínima y la acción moduladora de los antibióticos. Los principales ácidos grasos identificados fueron ácido esteárico, ácido palmítico y ácido oleico. La acidez y el índice de saponificación están dentro de los límites establecidos por la Agencia Nacional de Vigilancia Sanitaria. El aceite mostró actividad antioxidante moderada y actividad antimicrobiana contra las cepas de Candida. También mostró efectos sinérgicos, especialmente acerca de cefotaxima contra Bacillus cereus. Los resultados sugieren el potencial de la especie como antioxidante y en terapia antimicrobiana.

This study aimed to characterize the chemical, antioxidant and antimicrobial properties of the pulp oil of Mauritia flexuosa L. f. (Arecaceae). Chemical identification was performed by gas chromatography coupled to mass spectrometry. The physicochemical properties were characterized. Antioxidant capacity has been verified by eliminating of free radicals, reducing and chelation of iron. The antimicrobial activity was evaluated by the minimum inhibitory concentration and the modulatory action of antibiotics. The major fatty acids identified were stearic acid, palmitic acid and oleic acid. The acidity and the saponification index are within the limits established by the National Sanitary Surveillance Agency. The oil showed moderate antioxidant activity and antimicrobial activity against Candida strains. It also showed synergistic effects, especially on cefotaxime against Bacillus cereus. The results suggest the potential of the species as an antioxidant and in antimicrobial therapy.

Anti-inflammatory and anti-edematogenic action of the Croton campestris A. St.-Hil (Euphorbiaceae) essential oil and the compound ß-caryophyllene in in vivo models.

BACKGROUND: Inflammation makes up a set of vascularized tissue reactions acting in the defense of the body against harmful stimuli. Natural products are a lower cost alternative with better benefit, often used in popular medicine in the treatment of inflammatory processes. Several species from the genus Croton have scientifically proven anti-inflammatory action. PURPOSE: This study aims to analyze the chemical composition of the Croton campestris A. St.-Hil essential oil (EOCC), derived from fresh leaves, as well as to evaluate the anti-inflammatory potential and the possible mechanisms of action of the EOCC and its constituent ß-caryophyllene. METHODS: The assays were performed in in vivo models of acute and chronic inflammation. Initially, the chemical composition of the EOCC was determined and its oral toxicity was evaluated, followed by the evaluation of its topical antiedematogenic effect through acute and chronic ear edema induced by Croton oil. For the systemic verification of an anti-inflammatory action, the abdominal contortions, formalin test, paw edema induced by carrageenan, dextran, histamine and arachidonic acid models, as well as a peritonitis test, vascular permeability and granuloma assays were performed. RESULTS: The evaluation of the essential oil chemical composition revealed the presence of ß-caryophyllene (15.91%), 1,8-cineol (16.98%) and germacrene-D (14.51%) as its main constituents. The EOCC had no relevant clinical toxicity on oral administration, with an LD50 of more than 5000 mg/kg. The tested substances showed anti-inflammatory action in the abdominal contortions, paw edema induced by carrageenan, dextran, histamine and arachidonic acid models, the formalin test, peritonitis test and vascular permeability; however, ß-caryophyllene had no significant effect on the granuloma assay. This suggests as a hypothesis that both substances tested showed significant influence on the arachidonic acid and histamine pathway reducing edema in these models. CONCLUSION: The tested substances have a clinically safe profile, additionally the EOCC and ß-caryophyllene presented relevant anti-inflammatory activity. This study supports the hypothesis that ß-caryophyllene, in association with other constituents present in the EOCC such as 1,8-cineole, contributed to the anti-inflammatory effect observed, in addition to suggesting that one of the mechanisms of action probably involves the inhibition of cytokines with the involvement of the arachidonic acid and histamine pathways.

Antifungal Susceptibility of Candida Species Isolated from Horticulturists with Onychomycosis in Piauí, Brazil.

BACKGROUND: We aimed to assess susceptibility pattern of Candida species isolated from horticulturists with onychomycosis to four antifungal drugs and to compare the effectiveness of conventional identification methods with matrix-assisted laser desorption/ionization mass spectrometry (MALDI-TOF MS). METHODS: This study was conducted in a community garden located in Teresina, State of Piauí, Brazil, in the year 2014. The samples were identified through phenotypic methods and per MALDI-TOF MS, being used PCR as definitive identification test. The susceptibility pattern to four antifungal drugs was determined according to Clinical and Laboratory Standards Institute (CLSI). RESULTS: Fourteen clinical isolates from seven different species were identified by the phenotypic method and by MALDI-TOF MS, with an observed concordance of 71.4% between the two methods. C. albicans (28.6%), C. parapsilosis (21.4%), C. guilliermondii and C. metapsilosis (both with 14.3%) were the most frequent species. With the exception of C. krusei, all species were sensitive to the tested antifungal. CONCLUSION: This is the first study of antifungal susceptibility of Candida in Piauí, Brazil. With the exception of C. krusei, no species showed resistance to the antifungal drugs used. This study suggests constants updates from the public databases used in MALDI-TOF MS to provide a rapid and accurate mycological diagnosis.

Evaluation of toxic, cytotoxic, mutagenic, and antimutagenic activities of natural and technical cashew nut shell liquids using the Allium cepa and Artemia salina bioassays.

The cashew nut releases a substance that is known as cashew nut shell liquid (CNSL). There are both natural (iCNSL) and technical (tCNSL) cashew nut shell liquids. This study used an Artemia salina bioassay to evaluate the toxic effects of iCNSL and tCNSL cashew nut shell liquids. It also evaluated the toxicity, cytotoxicity, and mutagenicity of CNSL and its effects on the damage induced by copper sulfate (CuSO4·5H2O) on the meristems' root of Allium cepa. Effects of the damage induced by CuSO4·5H2O were evaluated before (pre-), during (co-), and after (post-) treatments. The iCNSL contained 94.5% anacardic acid, and the tCNSL contained 91.3% cardanol. The liquids were toxic to A. salina. Toxicity, cytotoxicity, and mutagenicity were observed with iCNSL compared with the negative control. Similarly, iCNSL failed to inhibit the toxicity and cytotoxicity of CuSO4·5H2O. The tCNSL was not toxic, cytotoxic, or mutagenic in any of the concentrations. However, the lowest iCNSL concentrations and all of the tCNSL concentrations had preventive, antimutagenic, and reparative effects on micronuclei and on chromosomal aberrations in the A. cepa. Therefore, protective, modulating, and reparative effects may be observed in the A. cepa, depending on the concentration and type of CNSL used.

Evaluation of p-cymene, a natural antioxidant.

CONTEXT: Several studies have demonstrated that essential oils and their major components have antioxidant activity. p-Cymene is a monoterpene and a major constituent of essential oils of various species of plants. OBJECTIVE: This paper evaluated the antioxidant potential of p-cymene in the hippocampus of mice by determining the levels of thiobarbituric acid reactive substances (TBARS), nitrite content, and activity of catalase (CAT) and superoxide dismutase (SOD). MATERIALS AND METHODS: Swiss mice were intraperitoneally treated with 0.05% Tween 80 dissolved in 0.9% saline solution, ascorbic acid 250 mg/kg, and p-cymene at doses of 50, 100, and 150 mg/kg, respectively. After treatment, all groups were observed for 24 h, afterwards, the groups were euthanized for removal of the brain and dissection of the hippocampus. RESULTS: The results of treatment with p-cymene were a significant decrease in lipid peroxidation and nitrite content at a dose of CYM 50: 65.54%, CYM 100: 73.29%, CYM 150: 89.83%, and CYM 50: 71.21%; CYM 100: 68.61% and CYM 150:67%, respectively, when compared with the control group. The results showed that at all tested doses, p-cymene produces an increase in SOD and catalase activity significantly at a dose of CYM 50: 22.7%, CYM 100: 33.9%, CYM 150: 63.1%, and CYM 50: 119.25%, CYM 100: 151.83% and CYM 150: 182.70%, respectively, when compared with the vehicle-treated group. DISCUSSION AND CONCLUSION: The result of this study shows that p-cymene has an antioxidant potential in vivo and may act as a neuroprotective agent in the brain. This compound may present a new strategy in the development of treatment for many diseases in which oxidative stress plays an important pathophysiological role.

In vitro antileishmanial activity and cytotoxicity of essential oil from Lippia sidoides Cham.

Leishmaniasis is a widespread tropical infection caused by different species of Leishmania protozoa. There is no vaccine available for Leishmania infections and conventional treatments are very toxic to the patients. Therefore, antileishmanial drugs are urgently needed. In this study we have analyzed the effects of essential oils from Lippia sidoides (LSEO) and its major compound thymol on the growth, viability and ultrastructure of Leishmania amazonensis. The essential oil and thymol showed significant activity against promastigote forms of L. amazonensis, with IC(50)/48 h of 44.38 and 19.47 µg/mL respectively. However, thymol showed toxicity against peritoneal macrophages and low selectivity against the promastigotes when compared with the crude LSEO. On the other hand, no cytotoxic effect was observed in macrophages treated with the crude essential oil. Incubation of L. amazonensis-infected macrophages with LSEO showed a marked reduction in amastigote survival within the macrophages. Significant morphological alterations as accumulation of large lipid droplets in the cytoplasm, disrupted membrane and wrinkled cells were usually seen in treated parasites. The LSEO's activity against both promastigote and the amstigote forms of L. amazonensis, together with its low toxicity to mammalian cells, point to LSEO as a promising agent for the treatment of cutaneous leishmaniasis.