Antihyperglycemic activity of crude extract and isolation of phenolic compounds with antioxidant activity from Moringa oleifera Lam. leaves grown in Southern Brazil.

The antihyperglicemic activity of crude extract from Moringa oleifera leaves and isolation of phenolic compounds with antioxidant activity using bioguided assay were employed by the first time in leaves cultivated in Brazil. The hydroalcoholic extract (HE) was produced by using ethanol:water (80:20 v/v) and purified by solid-liquid procedure using solvents in ascending order of polarity. The ethyl acetate fraction (Fr-EtOAc) presented high antioxidant potential and it was purified using chromatographic techniques rendering isolated compounds that were identified from the spectral data. The HE extract (500 mg kg-1) was adimistrated in diabetic rats induced by streptozotocin and chemical markers and lipid peroxidation in liver and kidney were evaluated. The Fr-EtOAc showed high antioxidant potential by FRAP reduction method (1678 µmol Fe2+ g-1), DPPH and ABTS scavenging methods (526.7 and 671.5 µmol TEAC g-1 respectively) and ORAC assay (3560.6 µmol TEAC g-1). Therefore, the Fr-EtOAc was purified and yielded three bioactive subfractions (S-12, S-13 abd S-15) that were rechromatoghaphed in HPLC-SemiPrep. After that, two main bioactive glycosylated flavonoids (isoquercitrin and astragalin) and phenolic acid (3-O-caffeoylquinic acid) were obtained. Additionally, the HE extract provided protection against oxidative damage in liver and kidney of diabetic rats ameliorating endogenous antioxidant defenses by increase catalase (CAT), glutathione S-transferase (GST) and non-protein thiol groups (NPSH) levels as well as decreased the lipid peroxidation in these tissues. Our results indicate that three phenolic compounds with high antioxidant activity were isolated and, the chemical composition of HE crude extract, rich in flavonoids glycosylated could be intimately related to antihyperglycemic action. So, it is possible to suggest that these compounds may be used as chemical biomarkers for this plant in Brazil, ensuring quality and supporting the use of aerial parts in tradicional medicine.

Fumigant activity of essential oils from Cinnamomum and Citrus spp. and pure compounds against Dermanyssus gallinae (De Geer) (Acari: Dermanyssidae) and toxicity toward the nontarget organism Beauveria bassiana (Vuill.).

Dermanyssus gallinae(De Geer) (Acari: Dermanyssidae) is the main ectoparasite associated with laying poultry. This mite is commonly controlled by the application of synthetic chemical insecticides, wich lead to the selection of resistant populations and formation of residues in eggs. Thus, new molecules must be developed to control D. gallinae. This work evaluated the toxicity of essential oils (EOs) from Cinnamomum cassia, Cinnamomum camphora, Cinnamomum camphora var. linalooliferum, Citrus aurantium, Citrus aurantium var. bergamia, Citrus aurantifolia and Citrus reticulata var. tangerine against D. gallinae. Additionally, the chemical profiles of the most bioactive EOs were analyzed by gas chromatography coupled with mass spectrometry (GC-MS) and the major compounds were subjected to new tests using D. gallinae. The most toxic EOs against D. gallinae were evaluated for the nontarget entomopathogenic fungus Beauveria bassiana (Unioeste 88). The EOs from C. cassia (LC50 = 25.43 ± 1.0423 µg/cm3) and C. camphora var. linalooliferum (LC50 = 39.84 ± 1.9635 µg/cm3) were the most active in the fumigant bioassay and caused mortality rates of 96 and 61%, respectively. The GC-MS analysis revealed that the major constituents of EOs from C. cassia and C. camphora var. linalooliferum were trans-cinnamaldehyde and linalool, respectively. The pure compounds, trans-cinnamaldehyde (LC50 = 68.89 ± 3.1391 µg/cm3) and linalool (LC50 = 51.45 ± 1.1967 µg/cm3), were tested on D. gallinae and showed lower toxicity than the EOs. Thus, the compounds were not the only active substances produced by C. cassia and C. camphora var. linalooliferum; moreover synergism may have occurred between the substances. The EOs from C. cassia and C. camphora var. linalooliferum were also toxic to B. bassiana (Unioeste 88). Thus, EOs from C. cassia and C. camphora var. linalooliferum are promising candidates for use in D. gallinae control, but cannot be used in conjunction with the fungus B. bassiana.

Baccharis dracunculifolia (Asteraceae) essential oil displays anti-inflammatory activity in models of skin inflammation.

ETHNOPHARMACOLOGICAL RELEVANCE: Baccharis dracunculifolia (Asteraceae) is a commonly used plant in traditional medicine known as "alecrim-do-campo". Popularly it has been used as an immunostimulant, antibiotic, anti-inflammatory among other applications. So far, only a few studies have investigated the B. dracunculifolia anti-inflammatory effect and none has investigated the effectiveness of essential oil on skin diseases. AIM OF THE STUDY: The study aimed at evaluating the topical anti-inflammatory activity of B. dracunculifolia essential oil (BdEO) in mice models of acute and chronic skin inflammation. MATERIALS AND METHODS: BdEO was obtained from leaves and it was analyzed with Gas Chromatograph. Topical anti-inflammatory activity of BdEO (0.1, 0.3 and 1.0 mg/ear) was evaluated in Arachidonic Acid or TPA-induced acute and chronic skin inflammation in mice. Parameters such edema, cell migration and keratinocytes proliferation were evaluated. In addition, safety and a possible mechanism of action for BdEO essential oil were also investigated. RESULTS: Our results indicate that mainly terpenoids compounds compose BdEO. In addition, topical treatment with BdEO inhibited inflammatory parameters in both acute and chronic models of skin inflammation. This protective effect was associated with reduced edema formation, smaller cellular influx into the inflamed tissue and reduction of keratinocytes hyperproliferation. Although BdEO appears to exert its anti-inflammatory effect through a corticosteroid pathway, no local or systemic side effects were observed. CONCLUSION: Taken together, the present results showed that the essential oil obtained by hydrodistillation from B. dracunculifolia leaf samples exhibit remarkable topical anti-inflammatory properties. Therefore, our study demonstrated evidence for BdEO topical anti-inflammatory efficacy and safety, suggesting that it could be considered for developing of a new phytotherapeutic formulation as treatment for skin diseases.

Expanding the anti-inflammatory potential of Moringa oleifera: topical effect of seed oil on skin inflammation and hyperproliferation.

ETHNOPHARMACOLOGICAL RELEVANCE: Popularly used in India and sub-Hymalaian region, Moringa oleifera (Moringaceae) is associated with healing properties demonstrated in its use as treatment of acute and chronic skin diseases. Our study aimed at investigating the effects of M. oleifera seed oil (MOSO) in animal models for inflammatory and hyperproliferative skin conditions. MATERIALS AND METHODS: MOSO was analyzed using gas chromatography/mass spectrometry. The anti-inflammatory and anti-hyperproliferative effects of treatment with either MOSO or oleic acid (OA), its main constituent, was evaluated. Acute and chronic inflammation was induced by applying 12-O-Tetradecanoylphorbol-13-acetate (TPA) and acute inflammation with either Arachidonic Acid (AA) or Phenol onto the ear of Swiss mice. Systemic activity and the influence of glucocorticoid receptors (GC) was also evaluated. RESULTS: Topical application of MOSO and OA inhibited ear edema caused by TPA, and Phenol. Only MOSO inhibited ear edema induced by AA. Neutrophil migration was also inhibited by treatment with MOSO. Topical application of MOSO, but not OA, significantly reduced chronic skin inflammation and epidermal hypertrophy induced by multiple TPA applications. Pre-treatment with GC antagonist mifepristone reversed the anti-inflammatory effect of MOSO and OA on the TPA model. Repeated administration of MOSO show a similar effect to dexamethasone on thymus weight, though MOSO did not present any influence on skin thickness, as well as in the weight of the spleen, adrenal gland and lymph node. CONCLUSION: The results suggest that MOSO is effective as a treatment for skin diseases that rely on keratinocyte hyperproliferation. OA is also effective in acute inflammation. Both MOSO and OA depend on GC activation for anti-inflammatory effect but do not exhibit the same adverse effects seen in topical treatment with dexamethasone. We hereby evidence the use of MOSO as a topical anti-inflammatory agent in inflammatory skin diseases, thus, expanding its therapeutic potential.

Chemical composition, antioxidant and anti-inflammatory activities of the essential oils from male and female specimens of Baccharis punctulata (Asteraceae).

ETHNOPHARMACOLOGICAL RELEVANCE: Baccharis punctulata (Asteraceae), popularly known as "Chíllka saru saru" in Bolivia, has been used by rural communities in Bustillo Province of the Potosi Department for treatment of asthma, luxations and contusions. AIM OF THE STUDY: To analyze the chemical composition of the essential oils obtained from leaves of female (BPF) and male (BPM) specimens and evaluate their anti-inflammatory and antioxidant properties. MATERIAL AND METHODS: Chemical composition analyses of Baccharis punctulata essential oils isolated by hidrodistillation from leaves of male and female specimens were performed by GC-FID-MS. The in vivo anti-inflammatory activity was evaluated using the model of TPA (12-O-tetradecanoylphorbol-13-acetate) induced ear edema, and the polymorphonuclear cell migration was evaluated by mieloperoxidase (MPO) and analyzed histologically. To measure the reactive oxygen species (ROS) in the inflamed tissue, the DCFH-DA fluorescent probe was used. The chemical in vitro antioxidant activity of essential oils was determined using the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) free radical assay. RESULTS: The chemical analysis showed high proportion of sesquiterpenes in the volatiles samples obtained from BPM, such as δ-elemene (14.29%), germacrene D (11.29%) and bicyclogermacrene (10.90%), and in the sample from BPF, bicyclogermacrene (42.44%), germacrene D (21.18%) and ß-caryophyllene (14.06%). A statistical difference (p < 0.05) on chemical composition between both essential oils was observed. Topical administration of both BPM and BPF essential oils was able to inhibit the formation of TPA-induced edema in the treated groups. Isolated administration of TPA promoted an increase in MPO enzyme activity, and inhibition of the increase of MPO activity was observed when animals were treated with BFP at concentrations of 0.1 mg/ear (13.69 ±â€¯0.20%), 0.3 mg/ear (22.35 ±â€¯0.11%), and 1.0 mg/ear (44.98 ±â€¯0.27%). Topical treatment with BPM was able to inhibit MPO activity at 22.40 ±â€¯0.29% (0.1 mg/ear), 36.49 ±â€¯0.07% (0.3 mg/ear) and 52.19 ±â€¯0.28% (1.0 mg/ear). The positive control of dexamethasone (DEXA, 0.1 mg/ear) was able to revert the increase in the enzymatic activity of MPO caused by TPA (65.16%). Histological analysis showed that topical application of TPA promoted intense cellular infiltration. This inflammatory parameter was reduced with the topical application of the BPF and BPM oil samples as well as with DEXA. The results observed in the ROS and DPPH tests suggest that both samples were able to reduce the inflammatory cells influx and have in vitro antioxidant properties, respectively. CONCLUSIONS: This study presents, for the first time, the chemical composition of the essential oils obtained from leaves of male and female specimens of Baccharis punctulata, and their anti-inflammatory and antioxidant activities. The results presented by the volatile samples in our biotests support traditional uses of this plant species.