GC-MS comparison of fatty acids profile of oils extracted from viscera of Tainha (Mugil liza) and Tambaqui (Colossoma macropomum).

The commercial activity of the grey mullet (known as Tainha: TAI) and Tambaqui (TAM) generates tons of waste that can be turned into valuable resources. Therefore, this work aimed to chemically characterize and quantify the fatty acids profiles of the two fishes. GCMS quantification was performed by using calibration curves built from a standard that contains 19 FAME. The analysis revealed that visceral wastes from both fishes contain 16 fatty acids (FA) consisting of saturated (SFA), monounsaturated (MUFA) and polyunsaturated (PUFA). However, their compositions were different as FA side chains in TAI and TAM contain 12 to 20 and 13 to 22 carbon atoms, respectively. Also, the SFA amount in TAI was greater than in TAM. On the other hand, TAM is richer in MUFA and PUFA compared to TAI. Both have similar chemical compositions of ω-3 and ω-6 in PUFA and ω-5, ω-7, and ω-9 in MUFA.

Chitosan packaging functionalized with Cinnamodendron dinisii essential oil loaded zein: A proposal for meat conservation.

The nanoencapsulation of essential oils for biodegradable films functionalization is a viable alternative for the production of active food packaging. In this study, the Cinnamodendron dinisii Schwanke essential oil was nanoencapsulated using zein as wall material, and applied in chitosan matrix to produce an active nanocomposite film packaging for food conservation. The chemical composition of the Cinnamodendron dinisii Schwanke essential oil showed a variety of unexplored bioactive compounds, and 1,8-cineole was the major compound. The oil nanoencapsulation produced stable and homogeneous nanoparticles with zeta potential close to 30 mV and polydispersity index lower than 0.2. The nanoparticles size showed a size variation between 70 and 110 nm. The chitosan films obtained functionalized with nanoparticles demonstrated antioxidant activity and antimicrobial activity. The active packaging containing zein nanoparticles was efficient in the conservation of ground beef, stabilizing the deterioration reactions and preserving the color.

Insecticide activity of Baccharis dracunculifolia essential oil against Cochliomyia macellaria (Diptera: Calliphoridae).

The ethnobotanical uses of Brazilian plants for different injuries and diseases conjoined with local rich biodiversity represent an important resource for research and development. This study aimed to characterise BDEO and its in vitro activity on the third instar larvae (L3) of Cochliomyia macellaria. Groups of 20 L3 were placed on filter paper impregnated with increasing concentrations of 5-30% (v/v), equivalent to 0.79-4.77 µL/cm2, solubilised in ethanol or acetone. The major constituents of BDEO were ß-pinene (9.94%), D-limonene (9.59%), ß-nerolidol (7.93%), caryophyllene (7.69%), spathulenol (6.69), α-muurolene (6.74%) and α-pinene (5.31%). Lethal concentrations of 50% for BDEO on C. macellaria (LC50) after 24 and 48 h of exposure were 2.63 and 2.47 µL/cm2 for ethanol and 9.58 and 8.11 µL/cm2 for acetone, respectively. Furthermore, larvae cuticle abnormalities and adult deformity were observed. Our data confirm the effectiveness of BDEO as an ecofriendly product against blowflies.

Effects of 1,3,5-triphenyl-4,5-dihydro-1H-pyrazole derivatives on cell-cycle and apoptosis in human acute leukemia cell lines.

Pyrazoline is an important 5-membered nitrogen heterocycle that has been extensively researched. Ten derivatives were synthesized and tested for antileukemic effects on 2 human acute leukemia cell lines, K562 and Jurkat. The most cytotoxic of these derivatives, compound 21, was chosen for investigation of cytotoxicity mechanisms. The results obtained with selectivity calculations revealed that compound 21 is more selective for acute leukemia (K562 and Jurkat cell lines) than for other tumor cell lines. Moreover, compound 21 was not cytotoxic to normal cell lines, indicating a potential use in clinical tests. Compound 21 caused a significant cell cycle arrest in the S-phase in Jurkat cells and increased the proportion of cells in the sub G0/G1 phase in both cell lines. Cells treated with compound 21 demonstrated morphological changes characteristic of apoptosis in the EB/AO assay, confirmed by externalization of phosphatidylserine by the annexin V - fluorescein isothiocyanate method and by DNA fragmentation. An investigation of cytotoxicity mechanisms suggests the involvement of an intrinsic apoptosis pathway due to mitochondrial damage and an increase in the ratio of mitochondrial Bax/Bcl2. Pyrazoline 21 obeyed Lipinski's "rule of five" for drug-likeness. Based on these preliminary results, the antileukemic activity of compound 21 makes it a potential anticancer agent.

Modulatory effect of Senecio brasiliensis (Spreng) Less. in a murine model of inflammation induced by carrageenan into the pleural cavity.

ETHNOPHARMACOLOGICAL RELEVANCE: Senecio brasiliensis (Spreng) Less (S. brasiliensis), known as "Flor-das-almas", "Margaridinha" or "Maria mole", is used in folk medicine as an anti-inflammatory and to treat gastric ulcers and stomach pain. While the Senecio genus has been widely studied for its pharmacological activities to support its use in traditional medicine, few studies focus on the anti-inflammatory activities of the species. AIM OF THE STUDY: To investigate the anti-inflammatory activities of S. brasiliensis, a specie native to Brazil, using a murine model of pleurisy induced by carrageenan. MATERIAL AND METHODS: The flowers of S. brasiliensis were air-dried for 3 days and subjected to ethanol (96%) extraction for 7 days to obtain the crude extract (CE). The CE was subjected to acid-base extraction to obtain the alkaloid fraction (AF). The hexane (HEX), dichloromethane (DCM) and ethyl acetate (EtOAc) fractions were obtained by extracting from CE with different solvents. The alkaloids senecionine (Sen), integerrimine (Int) and senecionine N-oxide were obtained from AF by chromatographic fractionation and a mixture of 1,4-, 3,4-, 3,5- and 4,5-dicaffeoylquinic acids (DCQs) were obtained from the EtOAc fraction. The isolated alkaloids were identified through spectroscopic analysis of IR, NMR and LC-MS coupled with electrospray ionization mass spectrometry (ESI-MS), and the dicaffeoylquinic acids through the hierarchical key method. Swiss mice were used in the in vivo experiments. We evaluated the effect of the CE, its derived fractions (AF, HEX, DCM and EtOAc), and the isolated compounds (Sen, Int, N-oxide senecionine, and DCQs) on: leukocyte migration, exudate concentrations, myeloperoxidase (MPO) and adenosine-deaminase (ADA) activities, and tumor necrosis factor-α (TNF-α), interleukin 1ß (IL-1ß) and interleukin 17A levels in the fluid leakage from the pleural cavity using a mouse model of pleurisy induced by carrageenan. The effects of the isolated compounds, Sen, Int, N-oxide senecionine and DCQs, were also analyzed for their ability to inhibit p65 phosphorylation (p-p65) in the nuclear factor-kappa B (NF-κB) pathway in the lung tissue. MPO and ADA were analyzed by colorimetric assays, and the cytokines and protein p65 levels were determined using an enzyme immunoassay (EIA). RESULTS: The CE, its EtOAc and AF fractions, and its isolated compounds (Sen, Int and DCQs), significantly reduced leukocyte migration (P < 0.05), MPO and ADA activities (P < 0.01), and TNF-α (P < 0.05), and IL-17A levels (P < 0.01). The CE, the EtOAc and AF fractions, and the DCQs also decreased IL-1ß levels (P < 0.01). The isolated compounds, Sen, Int and the DCQs, inhibited p65 phosphorylation (NF-κB) (P < 0.05). CONCLUSION: This study demonstrated that S. brasiliensis has important anti-inflammatory properties that are capable of inhibiting activated leukocytes by decreasing neutrophil migration. This effect may be attributed to the inhibition of pro-inflammatory cytokines and the reduction of the NF-κB pathway. The compounds Sen, Int, and DCQs may be responsible for the anti-inflammatory actions of S. brasiliensis.

The mechanism of action of ursolic acid as insulin secretagogue and insulinomimetic is mediated by cross-talk between calcium and kinases to regulate glucose balance.

BACKGROUND: The effect of in vivo treatment with ursolic acid (UA) on glycemia in hyperglycemic rats and its mechanism of action on muscle were studied. METHODS: The UA effects on glycemia, glycogen, LDH, calcium and on insulin levels were evaluated after glucose tolerance curve. The ß-cells were evaluated through the transmission electron microscopy. UA mechanism of action was studied on muscles through the glucose uptake with/without specific insulin signaling inhibitors. The nuclear effect of UA and the GLUT4 expression on muscle were studied using thymidine, GLUT4 immunocontent, immunofluorescence and RT-PCR. RESULTS: UA presented a potent antihyperglycemic effect, increased insulin vesicle translocation, insulin secretion and augmented glycogen content. Also, UA stimulates the glucose uptake through the involvement of the classical insulin signaling related to the GLUT4 translocation to the plasma membrane as well as the GLUT4 synthesis. These were characterized by increasing the GLUT4 mRNA expression, the activation of DNA transcription, the expression of GLUT4 and its presence at plasma membrane. Also, the modulation of calcium, phospholipase C, protein kinase C and PKCaM II is mandatory for the full stimulatory effect of UA on glucose uptake. UA did not change the serum LDH and serum calcium balance. CONCLUSIONS: The antihyperglycemic role of UA is mediated through insulin secretion and insulinomimetic effect on glucose uptake, synthesis and translocation of GLUT4 by a mechanism of cross-talk between calcium and protein kinases. GENERAL SIGNIFICANCE: UA is a potential anti-diabetic agent with pharmacological properties for insulin resistance and diabetes therapy.

Betulinic acid and 1,25(OH)2 vitamin D3 share intracellular signal transduction in glucose homeostasis in soleus muscle.

The effect of betulinic acid on glycemia and its mechanism of action compared with 1,25(OH)2 vitamin D3 in rat muscle were investigated. Betulinic acid improved glycemia, induced insulin secretion and increased the glycogen content and glucose uptake in muscle tissue. Additionally, the integrity of both PI3K and the cytoskeleton is necessary for the stimulatory action of betulinic acid in glucose uptake. The genomic effect was apparent, since cycloheximide and PD98059 nullified the stimulatory effect of betulinic acid on glucose uptake. Therefore, although this compound did not modify the DNA transcription, the protein translation was significantly improved. Also, betulinic acid increased the GLUT4 immunocontent and its translocation was corroborated by GLUT4 localization at the plasma membrane (after 180 min). On the other hand, the effect of 1,25(OH)2 vitamin D3 on glucose uptake is not mediated by PI3K and microtubule activity. In contrast, the nuclear activity of 1,25(OH)2 vitamin D3 is necessary to trigger glucose uptake. In addition, the increased DNA transcription and GLUT4 immunocontent provide evidence of a mechanism by which 1,25(OH)2 vitamin D3 contributes to glycemia. In conclusion, betulinic acid acts as an insulin secretagogue and insulinomimetic agent via PI3K, MAPK and mRNA translation and partially shares the genomic pathway with 1,25(OH)2 vitamin D3 to upregulate the GLUT4. In summary, betulinic acid regulates glycemia through classical insulin signaling by stimulating GLUT4 synthesis and translocation. In addition, it does not cause hypercalcemia, which is highly significant from the drug discovery perspective.