The chemical composition and trypanocidal activity of volatile oils from Brazilian Caatinga plants.

Essential/volatile oils (EOs) from plants used in the traditional medicine are known as a rich source of chemically diverse compounds with relevant biological activities. In this work we analysed the chemical composition and the in vitro effects of EOs from leaves of Eugenia brejoensis (EBEO), Hyptis pectinata (HPEO), Hypenia salzmannii (HSEO), Lippia macrophylla (LMEO) and seeds of Syagrus coronata (SCEO) on Trypanosoma cruzi, the etiological agent of Chagas disease. The EOs were extracted through hydrodistillation and its chemical composition analysed by GC/MS. The trypanocidal activity against epi- and trypomastigotes was evaluated by optical microscopy and the cytotoxicity to mammalian cells by MTT. The effects of EOs on parasite infection in macrophages were estimated by determining the survival index and the percentage of infection inhibition. The cytotoxicity against mammalian cells was compared to those of parasite by determining the Selectivity Index (SI). Overall, 114 compounds were identified: The main constituents of EOS were: δ-cadinene (15.88%), trans-caryophyllene (9.77%) e α-Muurolol (9.42%) for EBEO; trans-caryophyllene (15.24%), bicyclogermacrene (7.33%) e cis-calamenene (7.15%) for HFEO; trans-caryophyllene (30.91%), caryophyllene oxide (13.19%) and spathulenol (5.68%) for HPEO; Xanthoxylin (17.20%) trans-caryophyllene (14.34%) and methyl-eugenol (5.60%) for HSEO; Thymol (49.81%), carvacrol (31.6%) and σ-cimene (10.27%) for LMEO and octanoic acid (38.83%) dodecanoic acid (38.45%) and decanoic acid (20.51%) for SCEO. All the tested oils showed an inhibitory effect on the growth and survival of all forms of T. cruzi and moderate cytotoxicity towards the mammalian cells (100 < CC50 < 500 µg/mL). The EO of E. brejoensis was the most effective against the parasite presenting higher Selectivity Index for trypo- (SI = 14.45) and amastigote forms (SI = 20.11). Except for SCEO, which was the most cytotoxic for both parasite and mammalian cells, all the oils demonstrated to be more selective for the parasite than the reference drug benznidazole. Taken together our results point the essential oils from Caatinga plants, especially Eugenia brejoensis, as promissory agents for the development of new drugs against Chagas disease.

Antimicrobial activity of Buchenavia tetraphylla against Candida albicans strains isolated from vaginal secretions.

CONTEXT: Buchenavia tetraphylla (Aubl.) RA Howard (Combretaceae: Combretoideae) is an ethnomedicinal plant with reported antifungal action. OBJECTIVE: This study evaluates the antimicrobial activity of B. tetraphylla leaf extracts against clinical isolates of Candida albicans. The morphological alterations, combinatory effects with fluconazole and the cytotoxicity of the active extract were analyzed. MATERIALS AND METHODS: Extracts were obtained using different solvents (hexane: BTHE; chloroform: BTCE; ethyl acetate: BTEE; and methanol: BTME). Antimicrobial activity was determined by the broth microdilution method using nine strains of C. albicans isolated from vaginal secretions and one standard strain (UFPEDA 1007). RESULTS: All extracts showed anti-C. albicans activity, including against the azole-resistant strains. The MIC values ranged from 156 to 2500 µg/mL for the BTHE; 156 to 1250 µg/mL for the BTCE; 625 to 1250 µg/mL for the BTME and 625 µg/mL to 2500 µg/mL for the BTEE. BTME showed the best anti-C. albicans activity. This extract demonstrated additive/synergistic interactions with fluconazole. Scanning electron microscopy analysis suggested that the BTME interferes with the cell division and development of C. albicans. BTME showed IC50 values of 981 and 3935 µg/mL, against J774 macrophages and human erythrocytes, respectively. This extract also enhanced the production of nitric oxide by J774 macrophages. DISCUSSION AND CONCLUSION: Buchenavia tetraphylla methanolic extract (BTME) is a great source of antimicrobial compounds that are able to enhance the action of fluconazole against different C. albicans strains; this action seems related to inhibition of cell division.

In vitro cell-based assays for evaluation of antioxidant potential of plant-derived products.

Several plant-derived compounds have been screened by antioxidant assays, but many of these results are questionable, since they do not evaluate the pharmacologic parameters. In fact, the development of better antioxidants stills a great challenge. In vitro cell-based assays have been employed to assess the antioxidant effect of various compounds at subcellular level. Cell-based assays can also reveal compounds able to enhance the antioxidant pathways, but without direct radical scavenging action (which could not be detected by traditional assays). These methodologies are general of easy implementation and reproducible making them suitable for the early stages of drug discovery. Hydrogen peroxide, a nonradical derivative of oxygen, can be employed as an oxidative agent in these assays due its biochemical properties (presence of all biological systems, solubility) and capacity to induce cell death. Truthfully, if their limitations are understood (such as difference on cell metabolism when in in vitro conditions), these cell-based assays can provide useful information about the pathways involved in the protective effects of phytochemicals against cell death induced by oxidative stress, which can be exploited to develop new therapeutic approaches.