Search

Senna crotalarioides is used in traditional medicine to treat inflammation. The aim of this work was to investigate the anti-inflammatory and cytotoxic activities and the possible mechanism of action of the chloroform extract washed with hexane of S. crotalarioides (CESC). The anti-inflammatory effect was tested on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear edema in mice. The levels of TNF-α, IL-1β, IL-6 and IL-10 were determined in macrophages J774A.1 stimulated by lipopolysaccharide (LPS). The cytotoxic activity was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay against six human cancer cell lines: HeLa (cervical cancer), SKLU-1 and A549 (lung cancer), LNCaP (prostate cancer), SW620 (colon cancer) and MCF7 (breast cancer). The composition of the CESC was determined by GC-MS analysis, and standardized by HPLC-ELSD with ursolic acid as the phytochemical marker. CESC inhibited ear edema 61.45%. In chronic ear edema, CESC diminished the inflammation by 53.77%. CESC decreased TNF-α, IL-1β and IL-6 concentrations, and increased the concentration of IL-10. The extract showed IC50 values on HeLa, SKLU-1, A549, LNCaP, SW620 and MCF7 by 48, 21, 8.16, 6.82, 1.81, 4.06 and 12.5 μg/mL, respectively. The main components were ursolic acid, 1-octacosanol, stigmasterol, β-sitosterol, 1-triacontanol, (Z, Z) hexadec-9-enoic acid octadec-9-enyl ester. CESC might be useful for developing a phytomedicine with anti-inflammatory and cytotoxic activities.

Background Drugs used for the treatment of diseases associated with chronic inflammation, such as cancer and rheumatoid arthritis have the potential to cause undesirable side-effects, which might result in patients ending treatment prematurely. However, plants are a viable option for the treatment of inflammatory diseases. In this study, we assessed the in vivo and in vitro anti-inflammatory activity, and the antitumor effects of the chloroform extract of Salvia ballotiflora (ECL). The pro-apoptotic effects of ECL in CT26 cells were also determined. Methods The chloroform extract of Salvia ballotiflora (ECL) was standardized using 19-deoxyicetexone (DEOX) as a phytochemical marker. The anti-inflammatory activity of ECL was determined on acute and chronic inflammatory models using the TPA-induced mouse ear edema assay. The antitumor activity of ECL was evaluated by the subcutaneous inoculation of CT26 cells on the back of Balb/c mice. In vitro CT26 cell death induced by ECL was determined by Annexin V/propidium iodide staining assay using flow cytometry. ECL and the diterpenes isolated from the chloroform extract included 19-deoxyicetexone (DEOX), icetexone (ICT), and 7,20-dihydroanastomosine (DAM), which were tested in LPS-stimulated J774A.1 macrophages to quantify pro-inflammatory cytokine levels. The in vitro anti-arthritic activity of ECL was determined using the bovine serum protein (BSP) denaturation assay. Results ECL exerted anti-inflammatory activities in acute (84% of inhibition, 2 mg/ear) and chronic models (62.71%, at 100 mg/kg). ECL showed antitumor activity at 200 mg/kg and 300 mg/kg, reducing tumor volume by 30 and 40%, respectively. ECL (9.5 μg/mL) induced in vitro apoptosis in CT26 cells by 29.1% (48 h of treatment) and 93.9% (72 h of treatment). ECL (10 μg/ml) decreased levels of NO (53.7%), pro-inflammatory cytokines IL-6 (44.9%), IL-1β (71.9%), and TNF-α (40.1%), but increased the production of the anti-inflammatory cytokine IL-10 (44%). The diterpenes DEOX, ICT, and DAM decreased levels of NO (38.34, 47.63, 67.15%), IL-6 (57.84, 60.45, 44.26%), and TNF-α (38.90, 31.30, 32.83%), respectively. ECL showed in vitro antiarthritic activity (IC50 = 482.65 μg/mL). Conclusions ECL exhibited anti-inflammatory and anti-tumor activities. Furthermore, the diterpenes DEOX, DAM, and ICT showed anti-inflammatory activity by reducing levels of NO, TNF-α, and IL-6.

The parameters of the Gordon-Taylor equation ( Tgs , k ), the Chen equation ( E , B ) and the maximally freeze-concentrated phase ( Tm' , Tg’ x s ' ) have been regarded as necessary data for construction of state diagrams of sugar-rich foods. These parameters are significantly influenced by the sugar mass fractions; thus mathematical models for constructing the state diagram parameters based on the type and mass fraction of the main solutes of fruits are required. Experiments using model food systems and validation experiments using fruit juices were designed in this work with the purpose of developing, calibrating and validating the performance of mathematical models. Differential Scanning Calorimetry (DSC) was used to evaluate the thermal transitions of 19 model food systems with well-controlled chemical composition and of 5 fruit juices. Mathematical expressions of Tgs , k , E , B , Tg' , Tm' , x s ' as a function of mass fraction of fructose ( X F ), glucose ( X G ), sucrose ( X S ), pectin ( X P ) and citric acid ( X A ) and their interactions were developed. A statistical validation (α = 0.05) showed that solute composition-based mathematical models developed in this study are suitable and accurate for construction of state diagrams of real sugar-rich foods in which only the knowledge of their solid mass fraction is required.

The objective of this research was to obtain a ripened gouda-type cheese added with probiotic bacteria (Bifidobacterium lactis) and a prebiotic ingredient (Nutriose®FB), evaluating its potential as a functional food. The probiotic bacteria were encapsulated by spray drying using reconstituted skim milk (RSM) and a mixture of b-cyclodextrin-arabic gum (BC-AG) like encapsulant agents. Latterly, these ingredients were added during the production of gouda-type cheeses and microbiological as well as physicochemical evolution were assessed during ripening. At the end of this process, cheeses were subjected to gastrointestinal simulated conditions to evaluate probiotic survival. Results showed that the survival of microencapsulated cells was above 1010 CFU.g-1 in the probiotic powder and it is maintained above 108 CFU.g-1 in the cheese, during all the ripening process (40 days). Furthermore, tests carried out on the final product indicate that the probiotic bacteria resist the gastrointestinal conditions, remaining viable at a high concentration (> 107 CFU.g-1). An important aspect is that probiotic bacteria (Bifidobacterium lactis) and soluble fiber (Nutriose®FB) do not affected the physicochemical parameters of the gouda-type cheese. In conclusion, symbiotic gouda-type cheese obtained guarantees a beneficial effect to consumer, while keeps intrinsic physicochemical properties of the original cheese.

Yield and composition of seed oil (SO) from eight variants of prickly pear were evaluated. Oil extraction was performed by maceration-percolation (MP) and by cold press (CP). Characterization and quantification of fatty acids and phytosterols was performed by CG/EM. Cytotoxicity and proliferative activities in vitro of the extracted SO were evaluated on fibroblast cell culture. Oil yield was quite variable between variants, higher with MP method (6.2–15.5%) than with CP method (0.5–6.1%). Oil analysis from the eight variants revealed the predominance (mg/g) of linoleic acid (664.5–761.0 and 605.4–787.8), followed by oleic acid (92.7–198.8 and 115.2–199.4), palmitic acid (25.6–56.2 and 2.9–6.1), and stearic acid (15.5–36.1 and 2.9–5.2) for CP and MP respectively. Regarding phytosterols, β-sitosterol was predominant (11.6–58.3 mg/100 g of seed), over γ-tocopherol (16.6–23.8 mg/100 g of seeds) for MP and CP, respectively. By adding 50 µM of CP oil, cell death due to UV radiation of human dermic fibroblasts was reduced. Prickly pear seed, as a residue of the juice industry, contain compounds with potential commercial value.

Salvia tiliifolia Vahl (Lamiaceae) is used for the empirical treatment of pain and inflammation. The diterpenoid tilifodiolide (TFD) was isolated from Salvia tiliifolia. The in vitro anti-inflammatory effects of TFD (0.1-200 µM) were assessed using murine macrophages stimulated with LPS and estimating the levels of pro-inflammatory mediators for 48 h. The in vivo anti-inflammatory activity of TFD was assessed using the carrageenan-induced paw edema test for 6 h. The antinociceptive effects of TFD were evaluated using the formalin test and the acetic acid induced-writhing test. The effects of TFD on locomotor activity were assessed using the open field test and the rotarod test. TFD inhibited the production of TNF-α (IC50 = 5.66 µM) and IL-6 (IC50 = 1.21 µM) in macrophages. TFD (200 mg/kg) showed anti-inflammatory effects with similar activity compared to 10 mg/kg indomethacin. The administration of TFD induced antinociception in the phase 1 (ED50 = 48.2 mg/kg) and the phase 2 (ED50 = 28.9 mg/kg) of the formalin test. In the acetic acid assay, TFD showed antinociceptive effects (ED50 = 32.3 mg/kg) with similar potency compared to naproxen (ED50 = 36.2 mg/kg). In the presence of different inhibitors in the acetic acid assay, only the co-administration of TFD and naloxone reverted the antinociceptive activity shown by TFD alone. TFD did not affect locomotor activity in mice. TFD exerts in vitro and in vivo anti-inflammatory activity and in vivo antinociceptive effects.

Ulomoides dermestoides are used as a broad-spectrum medical insect in the alternative treatment of various diseases. Preliminary volatilome studies carried out to date have shown, as the main components, methyl-1,4-benzoquinone, ethyl-1,4-benzoquinone, 1-tridecene, 1-pentadecene, and limonene. This work focused on the production of metabolites and their metabolic variations in U. dermestoides under stress conditions to provide additional valuable information to help better understand the broad-spectrum medical uses. To this end, VOCs were characterized by HS-SPME with PEG and CAR/PDMS fibers, and the first reported insect essential oils were obtained. In HS-SMPE, we found 17 terpenes, six quinones, five alkenes, and four aromatic compounds, in the essential oils, 53 terpenes, 54 carboxylic acids and derivatives, three alkynes, 12 alkenes (1-Pentadecene, EOT1: 77.6% and EOT2: 57.9%), 28 alkanes, nine alkyl disulfides, three aromatic compounds, 19 alcohols, three quinones, and 12 aldehydes were identified. Between both study approaches, a total of 171 secondary metabolites were identified with no previous report for U. dermestoides. A considerable number of the identified metabolites showed previous studies of the activity of pharmacological interest. Therefore, considering the wide variety of activities reported for these metabolites, this work allows a broader vision of the therapeutic potential of U. dermestoides in traditional medicine.

Preclinical Research The diterpene ent-dihydrotumanoic acid (DTA) was among the compounds isolated from Gymnosperma glutinosum (Spreng) Less (Asteraceae). There are no reports regarding the pharmacological effects of DTA. Cytotoxicity against cancer cells (1-250 µM), and the antibacterial (50-1400 µM) activity of DTA were evaluated using the MTT assay, and the minimum inhibitory concentration test, respectively. The antidiarrheal (1-100 mg/kg p.o.) and anti-inflammatory (2 mg/ear) effects of DTA were evaluated using castor oil and 12-O-tetradecanoylphorbol-13-acetate, respectively. The antinociceptive and sedative effects of DTA (1-100 mg/kg p.o.) were evaluated using two models of chemically-induced nociception, and the pentobarbital-induced sleeping time test, respectively. The antinociceptive mechanism of DTA was evaluated using the acetic acid writhing test with inhibitors related to pain processing pathways. The effects of DTA (10-100 mg/kg p.o.) on locomotor activity were evaluated using the rotarod test. DTA lacked cytotoxic activity (IC50 > 100 µM) on cancer cells, possessed moderate antibacterial effects against B. subtillis (MIC= 175 µM), moderate antidiarrheal and anti-inflammatory effects, and minimal vasorelaxant effects. In the formalin test, DTA showed antinociceptive effects in both phases. In the acetic acid test, DTA showed antinociceptive activity (ED50 = 50.2 ± 5.6 mg/kg) with potency similar to that of naproxen (NPX; ED50 =33.7 ± 4.5 mg/kg) an effect blocked by naloxone implicating an opioid mechanism. DTA also exerted antidiarrheal activity and showed no sedative effects or changes in locomotor activity in mice. Drug Dev Res 78 : 340-348, 2017. © 2017 Wiley Periodicals, Inc.

Context: A previous study demonstrated that the chloroform extract of Salvia connivens Epling (Lamiaceae) has anti-inflammatory activity. Objective: Identification of the active components in the dicholorometane extract (DESC), and, standardization of the extract based in ursolic acid. Material and methods: DESC was prepared by percolation with dichlromethane and after washed with hot hexane, its composition was determined by CG-MS and NMR, and standardized by HPLC. The anti-inflammatory activity was tested on acute TPA-induced mouse ear oedema at doses of 2.0 mg/ear. The cell viability of macrophages was evaluated by MTT method, and pro- and anti-inflammatory interleukin levels were measured using an ELISA kit. Results: Ursolic acid, oleanolic acid, dihydroursolic acid and eupatorin were identified in DESC, which was standardized based on the ursolic acid concentration (126 mg/g). The anti-inflammatory activities of DESC, the acid mixture, and eupatorin (2 mg/ear) were 60.55, 57.20 and 56.40% inhibition, respectively, on TPA-induced ear oedema. The IC50 of DESC on macrophages was 149.4 μg/mL. DESC (25 μg/mL) significantly reduced TNF-α (2.0-fold), IL-1β (2.2-fold) and IL-6 (2.0-fold) in macrophages stimulated with LPS and increased the production of IL-10 (1.9-fold). Discussion: Inflammation is a basic response to injuries, and macrophages are involved in triggering inflammation. Macrophage cells exhibit a response to LPS, inducing inflammatory mediators, and DESC inhibits the biosynthesis of the pro-inflammatory and promote anti-inflammatory cytokines. Conclusion: DESC has an anti-inflammatory effect; reduced the levels of IL-1β, Il-6 and TNF-α; and increases IL-10 in macrophages stimulated with LPS. Ursolic acid is a good phytochemical marker.

Gymnosperma glutinosum (Spreng) Less (Asteraceae) is a shrub used in traditional medicine for the treatment of inflammatory and renal diseases. The ent-dihydrotucumanoic acid (DTA) is a diterpene obtained from G. glutinosum. This study evaluated the antioxidant, genotoxic, and diuretic properties of DTA, as well as its in vitro and in vivo anti-inflammatory actions. The antioxidant actions of DTA were assessed with the 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), ferric reducing antioxidant power (FRAP), and 2,2'-diphenyl-1-picrylhydrazyl (DPPH) assays, the genotoxic action was assessed with the comet assay, and the diuretic effects of DTA were assessed using metabolic cages. The anti-inflammatory actions were evaluated using primary murine peritoneal macrophages stimulated with LPS and the λ-carrageenan-induced hind paw edema test. DTA lacked antioxidant (IC50 > 25,000 μg/mL) activity in the ABTS, FRAP, and DPPH assays. DTA at 500-1,000 μg/mL showed moderate genotoxicity. In LPS-stimulated macrophages, DTA showed IC50 values of 74.85 μg/mL (TNF-α) and 58.12 μg/mL (NO), whereas the maximum inhibition of IL-6 (24%) and IL-1β (36%) was recorded at 200 μg/mL. DTA induced in vivo anti-inflammatory effects with ED50 = 124.3 mg/kg. The in vitro anti-inflammatory activity of DTA seems to be associated with the decrease in the release of TNF-α and NO. DTA promoted the excretion of urine (ED50 = 86.9 mg/kg), Na+ (ED50 = 66.7 mg/kg), and K+ (ED50 = 8.6 mg/kg). The coadministration of DTA with L-NAME decreased the urinary excretion shown by DTA alone. Therefore, the diuretic activity is probably associated with the participation of nitric oxide synthase. In conclusion, DTA exerted anti-inflammatory and diuretic effects, but lacked antioxidant effects.

Salvia tiliifolia is used in folk medicine as a relaxant agent and for the treatment of diarrhea and neurodegenerative diseases. Tilifodiolide (TFD) is a diterpene obtained from this plant. The purpose of this work was to evaluate the antidiarrheal, vasorelaxant, and neuropharmacological actions of TFD. These effects were selected based on the folk medicinal use of S. tiliifolia. The antidiarrheal activity of 1-50 mg/kg p.o. TFD was assessed with the castor oil related tests. The vasorelaxant effect of TFD (0.9-298 μM) was performed with smooth muscle tissues from rats, and its mechanism of action was evaluated using different inhibitors. The sedative, anxiolytic, and antidepressant effects of 1-100 mg/kg TFD were assessed. The possible mechanisms of action of the anxiolytic and antidepressant effects of TFD were evaluated using inhibitors. TFD exhibited antidiarrheal (ED50 = 10.62 mg/kg) and vasorelaxant (EC50 = 48 ± 3.51 μM) effects. The coadministration of TFD with N(ω)-nitro-L-arginine methyl ester (L-NAME) or 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ), reverted the vasorelaxant action showed by TFD alone. TFD exerted anxiolytic actions (ED50 = 20 mg/kg) in the cylinder exploratory test, whereas TFD (50 mg/kg) showed antidepressant actions in the tail suspension test by 44%. The pretreatment with 2 mg/kg flumazenil partially reverted the anxiolytic actions of TFD, whereas the pretreatment with 1 mg/kg yohimbine abolished the antidepressant effects of TFD. In summary, TFD exerted antidiarrheal activity by decreasing the intestinal fluid accumulation and vasorelaxant effects mediated by nitric oxide and cyclic guanosine monophosphate. TFD showed anxiolytic and antidepressant effects by the partial involvement of gamma-Aminobutyric acid (GABA) receptors and the possible participation of α2-adrenoreceptors, respectively.

BACKGROUND Inulin and other fructans are synthesized and stored in mezcal agave (Agave salmiana). Fructans provide several health benefits and have excellent technological properties, but only few data report their physiological effect when added in the diet. RESULTS Here, we studied the physiological effects of fructans obtained from A. salmiana when added in the diet of Wistar rats. Results showed favorable changes on Wistar rats when the fructans was added to their diet, including the decrease of the pH in the feces and the increase of the number of lactic acid bacteria (CFU g−1) (Lactobacillus spp. and Bifidobacterium spp.), even these changes were enhanced with the synbiotic diet (fructans plus B. animalis subsp. lactis). Synbiotic diet, developed changes in the reduction of cholesterol and triglycerides concentrations in serum, with statistical differences (P < 0.05). Histological analysis of colon sections showed that synbiotic diet promoted colon cells growth suggesting that fructans from A. salmiana confer beneficial health effects through gut microbiota modulation. CONCLUSION Our data underline the advantage of targeting the gut microbiota by colonic nutrients like specific structure of fructans from A. salmiana, with their beneficial effects. More studies are necessary to define the role of fructans to develop more solid therapeutic solutions in humans. © 2016 Society of Chemical Industry

Essential oils can be used as an alternative to using synthetic insecticides for pest management. Therefore, the insectistatic and insecticidal activities of the essential oil of aerial parts of Salvia ballotiflora (Lamiaceae) were tested against the fall armyworm Spodoptera frugiperda (Lepidoptera: Noctuidae). The results demonstrated insecticidal and insectistatical activities against this insect pest with concentrations at 80 µg·mL(-1) resulting in 20% larval viability and 10% pupal viability. The larval viability fifty (LV50) corresponded to a concentration of 128.8 µg·mL(-1). This oil also increased the duration of the larval phase by 5.5 days and reduced the pupal weight by 29.2% withrespect to the control. The GC-MS analysis of the essential oil of S. ballotiflora showed its main components to be caryophyllene oxide (15.97%), and β-caryophyllene (12.74%), which showed insecticidal and insectistatical activities against S. frugiperda. The insecticidal activity of β-caryophyllene began at 80 µg·mL(-1), giving a larval viability of 25% and viability pupal of 20%. The insectistatic activity also started at 80 µg·mL(-1) reducing the pupal weight by 22.1% with respect to control. Caryophyllene oxide showed insecticidal activity at 80 µg·mL(-1) giving a larval viability of 35% and viability pupal of 20%.The insectistatic activity started at 400 µg·mL(-1) and increased the larval phase by 8.8% days with respect to control. The LV50 values for these compounds were 153.1 and 146.5 µg·mL(-1), respectively.

Chemical reactivity descriptors of indol-4-ones obtained via density functional theory (DFT) and hard–soft acid–base (HSAB) principle were calculated to prove their contribution in antifungal activity. Simple linear regression was made for global and local reactivity indexes. Results with global descriptors showed a strong relationship between antifungal activity vs. softness (S) (r = 0.98) for series I (6, 7a–g), and for series II (8a–g) vs. chemical potential (µ), electronegativity (χ) and electrophilicity (ω) (r = 0.86), p < 0.05. Condensed reactivity descriptors sk+, ωk− for different fragments had strong relationships for series I and II (r = 0.98 and r = 0.92). Multiple linear regression was statistically significant for S (r = 0.98), η (r = 0.91), and µ/ω (r = 0.91) in series I. Molecular electrostatic potential maps (MEP) showed negative charge accumulation around oxygen of carbonyl group and positive accumulation around nitrogen. Fukui function isosurfaces showed that carbons around nitrogen are susceptible to electrophilic attack, whereas the carbon atoms of the carbonyl and phenyl groups are susceptible to nucleophilic attack for both series. The above suggest that global softness in conjunction with softness and electrophilicity of molecular fragments in enaminone systems and pyrrole rings contribute to antifungal activity of indol-4-ones.

Context: Gymnosperma glutinosum (Spreng.) Less. (Asteraceae) is a bush used for the empirical treatment of pain, fever, and cancer. An ent-neo-clerodane diterpene (2-angeloyl ent-dihydrotumanoic acid; ADTA) was isolated from G. glutinosum. Objective: This study evaluates the cytotoxic, anti-inflammatory, and antinociceptive effects of ADTA. Materials and methods: The cytotoxic effects of ADTA (1–350 μM) were evaluated using the MTT assay with human tumorigenic (SW-620, MDA-MB231, SKLU1, SiHa, and PC-3), and non-tumorigenic (HaCaT) cells for 48 h. The in vitro anti-inflammatory effects of ADTA (0.23–460 μM) were assessed using murine peritoneal macrophages stimulated with LPS and estimating the levels of pro-inflammatory mediators for 48 h. The antinociceptive effects of ADTA (25–100 mg/kg p.o.) were evaluated using two in vivo models of chemical-induced nociception during 1 h. Results: ADTA lacked cytotoxic activity (IC50> 100 μM) on tumorigenic cells. In non-tumorigenic cells (HaCaT), ADTA exerted low cytotoxic effects (IC50 = 273 μM). ADTA, at concentrations of 115 μM or higher, decreased the release of pro-inflammatory mediators. The maximum antinociceptive effects of ADTA in the acetic acid-induced abdominal constrictions by ADTA was found at 100 mg/kg (63%), whereas in the formalin test at phase 1 and phase 2, ADTA (100 mg/kg) decreased the licking time by 47 and 71%, respectively. Conclusion: The results indicate that ADTA, obtained from G. glutinosum, exerts moderate in vitro anti-inflammatory and in vivo antinociceptive effects, but lacks cytotoxic effects on human cancer cells.

The development of antifungal drugs that inhibit lanosterol 14-α-demethylase (CYP51) via non-covalent ligand interactions is a strategy that is gaining importance. A series of novel tetraindol-4-one derivatives with 1- and 2-(2,4-substituted phenyl) side chains were designed and synthesized based on the structure of CYP51 and fluconazole. The antifungal activities of these derivatives against eight human pathogenic filamentous fungi and yeast strains were evaluated in vitro by measuring the minimal inhibitory concentrations. Nearly all tested compounds 8a-g displayed activity against Candida tropicalis, Candida guilliermondii and Candida parapsilosis with a minimum inhibitory concentration (MIC) value until 8 µg mL(-1), on the other hand compounds 7a-g showed activity against Aspergillus fumigatus with a MIC value of 31.25 µg mL(-1). A molecular modeling study of the binding interactions between compounds 6, 7d, 8g and the active site of MtCYP51 was conducted based on the computational docking results.

Organogelation is a promising alternative to provide structure and texture to vegetable oils and stability to solid-like water-in-oil emulsions. Within this framework, we investigate the effect of monoglycerides (MG; 0%–0.5%) in the microstructure, thermal and textural behavior of organogelled emulsions developed with candelilla wax (CW; 0.5%–4%), safflower oil, and water (20%). The emulsions were prepared by homogenization (200 bars) at 65 °C, cooling to 45 °C or 47 °C (Tout), and then storage at 5 °C for 24 h. To evaluate the effect of shearing and water addition we also developed CW–MG organogels (i.e., no water added) under similar conditions. Both systems were analyzed for solid phase content (SPC), texture, and microstructure. Independent of Tout, as CW and MG concentration increased in both systems the SPC increased also (P

Pectin from the cladode flour of Opuntia ficus indica was extracted at different ethylenediaminetetraacetate concentrations (10 or 20 %), temperatures (40 or 80 °C), pH values (2 or 11), and times (10, 20, 30 40, 50 or 60 min). The effects of the extraction conditions on the yield, purity, and chemical composition of pectin were assessed. The highest pectin yield was observed for pectin obtained under alkaline conditions and 20 % of EDTA. However, pectin produced from alkaline extractions had a lower content of GalA than pectin produced from acid extractions. Higher temperatures favored the extraction of pectin under acid conditions, but these conditions diminished the arabinose content of pectins in a time-dependent manner. The tested extraction conditions caused only slight changes in the molecular weight of the extracted pectin as a function of time.

The fructan separation from a model sugar solution and natural agave juice was studied using a stirred-cell nanofiltration unit operated in concentration mode. Hydrophilic cellulose membrane with MWCO of 1000 Da was used. The experimental conditions were varied to predict the influence of pressure (0.14–0.350 MPa) and feed concentration (0.15–0.25 g/mL) on the initial permeate flux and solute retained fraction (SRF) values of the process. Response surface plots (p

A new process for obtaining dibenzo[c,f][1,2,5]thiadiazepines (DBTDs) and their effects on GABA(A) receptors of guinea pig myenteric neurons are described. Synthesis of DBTD derivatives began with two commercial aromatic compounds. An azide group was obtained after two sequential reactions, and the central ring was closed via a nitrene to obtain the tricyclic sulfonamides (DBTDs). Whole-cell recordings showed that DBTDs application did not affect the holding current but inhibited the currents induced by GABA (I(GABA)), which are mediated by GABA(A) receptors. These DBTDs effects reached their maximum 3 min after application and were: (i) reversible, (ii) concentration-dependent (with a rank order of potency of 2c = 2d > 2b), (iii) mediated by a non-competitive antagonism, and (iv) only observed when applied extracellularly. Picrotoxin (which binds in the channel mouth) and DBTDs effects were not modified when both substances were simultaneous applied. Our results indicate that DBTD acted on the extracellular domain of GABA(A) channels but independent of the picrotoxin, benzodiazepine, and GABA binding sites. DBTDs used here could be the initial model for synthesizing new GABA(A) receptor inhibitors with a potential to be used as antidotes for positive modulators of these receptors or to induce experimental epilepsy.

In this study we investigated the combined effect of shearing and cooling rate in the rheology of organogels developed in high oleic safflower oil by (R)-12-hydroxystearic acid (HSA), its primary amide derivative [(R)-12-hydroxyoctadecanamide, HOA], and the N-octadecyl derivative of HOA [(R)-N-octadecyl-12-hydroxyoctadecanamide, OHOA]. The experimental set up to develop the organogels involved: 1). The use of quiescent (0s-1) or shearing (300, 600, and 1200s-1) conditions during cooling the gelator solutions (2%) just until achieving the gelator's melting temperature (TM) in the vegetable oil, to then continuing the cooling under static conditions until achieving 15°C) The use of cooling rate protocols involving a constant cooling rate of 1°C/min (CR1) or 10°C/min (CR10) in the shearing and static stages, or variable cooling rates in each stage (i.e., VR1-10 or VR10-1). The elasticity of the organogels (G') was measured while cooling under static conditions, once the systems achieved 15°C, and after 60min at this temperature. The rheological results obtained at 15°C showed a cooling rate and molecular weight-dependent effect of shearing on G'. We propose that the molecular relaxation time of gelator molecules, and its increase as molecular weight increases and as temperature decreases, plays an important role on the gelator's susceptibility to go through a shear induced crystallization process. Therefore, high molecular weight molecules like OHOA (551.97Da) would remain stretched by shearing longer times than HSA (300.49Da) and HOA (299.49Da). Thus, when shearing was applied while cooling at the higher cooling rate (i.e., CR10 and VR10-1), the stretched OHOA molecules would lead to the development of mesophase precursors that upon further cooling under quiescent conditions, crystallize developing a well-structured organogel. In contrast, stretched low molecular weight molecules (i.e., HSA and HOA) with shorter relaxation time would dissolve back to the isotropic state during cooling. Additionally, the rheological results of HSA and HOA organogels suggested that the shear induced crystallization process might be dependent on the gelator polarity also. These results show that the application of shear and the extent of its application as temperature decreases until achieving TM, have important implication on the self-assembly of gelator molecules, and therefore in the organization and rheology of the three-dimensional crystal network of the organogel.

VOx/ZrO 2 /SiO 2 catalysts were synthesized via grafting of vanadium and zirconium alkoxides over Aerosil 380. With these materials the formation of benzaldehyde from butane was possible in a one-pot synthesis, where oxidative dehydrogenation (ODH) for the formation of butadiene is coupled with a Diels–Alder reaction for the formation of benzaldehyde. Experiments performed with a catalyst where the support was modified with Ce instead of Zr, give a material that under the reaction conditions studied does not yield benzaldehyde, showing that acidity plays an important role in the formation of this compound.

Fructans were extracted fromAgave salmianajuice, characterized and subjected to hydrolysis process using a commercial inulinase preparation acting freely. To compare the performance of the enzymatic preparation, a batch of experiments were also conducted with chicory inulin (reference). Hydrolysis was performed for 6 h at two temperatures (50,60∘C) and two substrate concentrations (40, 60 mg/ml). Hydrolysis process was monitored by measuring the sugars released and residual substrate by HPLC. A mathematical model which describes the kinetics of substrate degradation as well as fructose production was proposed to analyze the hydrolysis assessment. It was found that kinetics were significantly influenced by temperature, substrate concentration, and type of substrate (P<0.01). The extent of substrate hydrolysis varied from 82 to 99%. Hydrolysis product was mainly constituted of fructose, obtaining from 77 to 96.4% of total reducing sugars.

The chemical composition of the essential oil from Hesperozygis marifolia was analyzed by gas chromatography-mass spectrometry (GC-MS), and fourteen compounds were identified. (R)-pulegone (40.75%), isomenthone (30.34%) and menthone (4.46%) were found to be the main components of the oil. The essential oil at a concentration of 2.0 mg/mL and (R)-pulegone at concentration of 0.8 mg/mL completely inhibited the growth of Aspergillus flavus Link. The fungicidal effects of this essential oil warrant further research into its potential for commercial use.

Ethnopharmacological importance Cecropia obtusifolia Bertol (Cecropiaceae) is a plant extensively used for the empirical treatment of type 2 diabetes in Mexico. Although some of its hypoglycemic principles have been described, their mechanisms of action remain unclear. Aim of the study To investigate the anti-diabetic mechanisms of Cecropia obtusifolia aqueous extract (CAE) and its active compound chlorogenic acid (CGA). Materials and methods Non-toxic concentrations of CAE and CGA were assayed on the adipogenesis and 2-NBDglucose uptake in 3T3-F442A murine adipocytes. Results Added to adipogenic medium, CAE 70 μg/ml induced a modest increment (20%) in 3T3 adipogenesis whereas CGA did not affect adipogenesis at any of the tested concentrations (0.1–100 μM). Both preparations stimulated 2-NBDG uptake in adipocytes by 51% (CAE) and 176% (CGA) in the absence of insulin, and by 174% (CAE) and 404% (CGA) in the presence of the hormone. CAE and CGA also stimulated the 2-NBDG uptake in insulin-resistant 3T3 adipocytes by 35% and 141%, respectively, compared with the incorporation shown by insulin-sensitive adipocytes stimulated by the hormone. The potency of CGA to stimulate 2-NBDG uptake was comparable to the anti-diabetic drug rosiglitazone. Conclusion Cecropia obtusifolia and CGA exert their anti-diabetic effects stimulating glucose uptake in both insulin-sensitive and insulin-resistant adipocytes without appreciable pro-adipogenic effects.

We investigated the anti-inflammatory activity ofSenecio salignus. This medicinal plant is often used in Mexico for the treatment of fever and rheumatism. Chloroform and methanol extracts of the plant were tested on 12-O-tetradecanoylphorbol-13-acetate- (TPA-) induced edema in mice ears. The methanol extract of the plant inhibited edema by36±4.4% compared with the control, while the chloroform extract exhibited an even greater level of inhibition (64.1%). The chloroform extract was then fractionated, and the composition of the active fraction was determined by GC-MS. The anti-inflammatory activity of this fraction was then tested on TPA-induced ear edema in mice, and we found that the active fraction could inhibit edema by 46.9%. The anti-inflammatory effect of the fraction was also tested on carrageenan-induced paw edema in rats at doses of 100 mg/kg; a58.9±2.8% reduction of the edema was observed 4 h after administration of carrageenan, and the effect was maintained for 5 h.

Conjugated linoleic acid (CLA) is a group of isomers of linoleic acid (LA) with a conjugated double-bond system that occurs in trace amounts in natural oils. As result of the beneficial properties on the health, bioactive isomers of CLA (cis9,trans11-CLA and trans10,cis12-CLA) have been industrially produced by alkali isomerization of LA. A large amount of studies regarding the CLA production might be found; however, new approaches as the use of microwave irradiation have been recently suggested. Here, we develop an efficient and sustainable method to selectively produce bioactive CLA by microwave-assisted isomerization of LA using propylene glycol as solvent. The investigated reaction variables were solvent/LA mass ratio (1:1–6:1), catalyst/LA mass ratio (0.25:1–0.6:1), temperature (160–180°C), catalyst type (KOH or NaOH), and reaction time. The results showed that: (i) KOH increased the production of conjugated trans-trans isomers; (ii) a considerable reduction of propylene glycol on the reaction was possible using NaOH; and (iii) the reaction time was drastically reduced in comparison to conventional heating. Thus, the optimum conditions for the cis9,trans11-CLA and trans10,cis12-CLA production (91.21% in equimolar ratio) were: NaOH at a catalyst/LA mass ratio of 0.5:1 and solvent/LA mass ratio of 1:1 at 160°C during 4 min. Practical applications: CLA has been subject of growing interest in nutrition and the food industry due to its wide range of biological activities including anti-carcinogenic and anti-atherogenic properties. Here, the chemical synthesis of CLA by microwave-assisted alkali isomerization was studied in order to lower the production costs by decreasing both, the propylene glycol content (the most expensive solvent used for this kind of reaction) and the reaction time. In comparison to conventional heating, reaction time was drastically reduced by employing microwave heating while the selective synthesis of cis9,trans11-CLA and trans10,cis12-CLA was achieved at low solvent conditions when the reaction conditions were optimized. In this sense, the methodology developed in this work could be used in order to obtain more efficiently and sustainably the bioactive forms of CLA, which in turn could be used in the manufacture of functional foods or dietary supplements. cis9,trans11-CLA and trans10,cis12-CLA were selectively synthetized through basic catalysis of linoleic acid in propylene glycol under microwave irradiation.

The composition of a chloroform seed extract of C. papaya was determined by GC-MS. Nineteen compounds were identified, with oleic (45.97%), palmitic (24.1%) and stearic (8.52%) acids being the main components. The insecticidal and insectistatic activities of the extract and the three main constituents were tested. Larval duration increased by 3.4 d and 2.5 d when the extract was used at 16,000 and 9,600 ppm, respectively, whereas the pupal period increased by 2.2 d and 1.1 d at the same concentrations. Larval viability values were 0%, 29.2%, and 50% when the extract was applied at 24,000, 16,000, and 9,600 ppm, respectively; pupal viability was 42.9% and 66.7% at 16,000 and 9,600 ppm; and pupal weight decreased by 25.4% and 11.5% at 16,000 and 9,600 ppm. The larval viability of the main compounds was 33.3%, 48.5%, and 62.5% when exposed to 1,600 ppm of palmitic acid, oleic acid, or stearic acid, respectively.

A series of benzimidazolylbenzenesulfonamide compounds containing electron-releasing and electron-withdrawing substituents were synthesized and tested for their in vitro antibacterial activity. Two BZS compounds showed strong antibacterial activity against methicillin-resistant Staphylococcus aureus and Bacillus subtilis. Quantitative studies of their structure-activity relationship using a simple linear regression analysis were applied to explore the correlation between the biological activity and the charges on acidic hydrogen atoms in the synthesized compounds.

Many medicinal herbs are used in folk medicine without taking into account their toxicity. Hamelia patens Jacq. (Rubiaceae), a Mexican endemic species, is used for the empirical treatment of pain. The aim of this work was to evaluate the toxicity and antinociceptive effects of ethanolic extracts of H. patens leaves. The toxicity of H. patens leaves (500–5000 mg/kg) was evaluated in acute (14 days) and subacute (28 days) assays. In the subacute assay, a blood analysis (both hematology and chemistry) was carried out. The antinociceptive effects of H. patens leaves (50–200 mg/kg) were evaluated using thermal-induced nociception (hot plate) and the chemical-induced nociceptive tests (acid acetic and formalin). In the acute toxicity test, the LD50 estimated for H. patens leaves was 2964 mg/kg i.p. and >5000 mg/kg p.o., whereas in the subacute test HPE did not affect hematological or biochemical parameters. In chemical-induced nociception models, H. patens (100 and 200 mg/kg p.o.) showed antinociceptive effects with similar activity than 100 mg/kg naproxen. In the hot plate test, HPE at 100 mg/kg (17%) and 200 mg/kg (25%) showed moderate antinociceptive effects. HPE could be a good source of antinociceptive agents because of its good activity and low toxicity. Keywords: Hamelia patens, Antinociceptive, Toxicity, Gas chromatography–mass spectrometry, Traditional medicine

Administradores Investigadores Estudiantes