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1.
Nat Prod Res ; 38(4): 589-593, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-36855235

RESUMO

Synergistic bioassay-guided isolation of the extracts of Artemisia rupestris L, which belongs to the family Asteraceae, afforded two acetylenic spiroketal enol ethers, namely rupesdiynes A (1) and B (2). Their structures were determined based on spectroscopic analysis and experimental and calculated ECD investigations. The two compounds exhibited synergistic activity and were able to reduce the minimum inhibitory concentration (MIC) of oxacillin four-fold, with a fractional inhibitory concentration index (FICI) of 0.5 in combination with oxacillin against the oxacillin-resistant EMRSA-16. Biofilm formation inhibitory and Ethidium bromide (EtBr) efflux assay were further employed to verify the possible mechanism of the synergistic antibacterial effect. Additionally, molecular docking studies were conducted to investigate the binding affinities of the two compounds with penicillin-binding protein 2a (PBP2a) of EMRSA-16. Taken together, rupesdiynes A (1) and rupesdiyne B (2) showed moderate synergistic activity against EMRSA-16 with oxacillin via inhibiting biofilm formation and efflux pump activity, respectively.


Assuntos
Artemisia , Furanos , Staphylococcus aureus Resistente à Meticilina , Compostos de Espiro , Simulação de Acoplamento Molecular , Acetileno/metabolismo , Acetileno/farmacologia , Alcinos/farmacologia , Éteres/metabolismo , Éteres/farmacologia , Extratos Vegetais/química , Antibacterianos , Oxacilina/farmacologia , Oxacilina/metabolismo , Testes de Sensibilidade Microbiana , Sinergismo Farmacológico
2.
Trop Anim Health Prod ; 56(1): 21, 2023 Dec 19.
Artigo em Inglês | MEDLINE | ID: mdl-38112933

RESUMO

Globally, the price of soybean meal, the most common proteinaceous ingredient in livestock diets, has become highly expensive prompting a search for alternative ingredients. Hemp seed cake is a promising alternative but could be limited by its high neutral detergent fiber and ether extract contents which impede nutrient intake and digestibility. However, some ruminant species such as goats have superior ability to digest high fiber and ether extract diets. Thus, the current research evaluated nutrient intake and digestibility, rumen fermentation, and microbial protein synthesis of goats fed hempseed cake as a substitute for soybean meal in finisher diets. A total of 25 Kalahari Red castrates (27 ± 3 kg, 4-5 months old) were assigned to five dietary treatments (5 goats/ diet) in a completely randomized design. A maize-lucerne-based finishing diet was formulated with hempseed cake substituting soybean meal as the primary protein ingredient at 0, 25, 50, 75, or 100 g/kg dry matter. Ether extract intake exhibited a positive linear trend (P ≤ 0.05) while crude protein intake and microbial nitrogen supply exhibited a negative linear trend (P ≤ 0.05) with dietary inclusion of hempseed cake. However, feeding hempseed cake did not influence (P > 0.05) apparent nutrient digestibility, rumen fermentation parameters and nitrogen use efficiency. In conclusion, the substitution of soybean meal for hempseed cake decreased crude protein intake and microbial nitrogen supply in goat finisher diets without compromising nutrient digestibility and nitrogen use efficiency. The study recommends partial or full replacement of soybean meal with hempseed cake in goat finisher diets.


Assuntos
Digestão , Cabras , Animais , Ração Animal/análise , Dieta/veterinária , Ingestão de Alimentos , Éteres/metabolismo , Fermentação , Glycine max , Cabras/metabolismo , Nitrogênio/metabolismo , Extratos Vegetais/metabolismo , Rúmen/metabolismo
3.
Trop Anim Health Prod ; 55(6): 385, 2023 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-37906370

RESUMO

This study aimed to estimate the magnitude of the effects of dietary inclusion of peanut skins (PS) byproduct (Arachis hypogea L.) on intake, total-tract digestibility, and rumen fermentation of cattle via meta-analysis. Data were collected following the PRISMA methodology. Nine manuscripts and a graduate thesis met the inclusion criteria from 1983 to 2010. The effect size was estimated by calculating the weighted raw mean differences (RMD) between PS vs. control diets. The RMD was compared with a robust variance estimation method followed by a meta-regression and a dose-response analysis fitting the diet characteristics like crude protein content (CP), NDF content, ether extract content (EE), tannin content, and PS level in diet (0 to 40%) as covariates. Dietary PS decreased (P < 0.01) total-tract CP digestibility (52.0 vs. 64.3%), final body weight (371.5 vs. 397.9 kg), and average daily gain (1.14 vs. 1.44 kg/day) among treatment comparisons. Likewise, PS decreased total VFA (92.6 vs. 107.6 mmol/L) and NH3-N (8.22 vs. 12.1 mg/dL), but no effects were observed on rumen pH (6.47 vs. 6.14) and VFA molar proportions. Despite the between-cluster variance, dietary PS increased the ether extract digestibility (77.5 vs. 70.2%) among treatment comparisons. The subset and dose-response analysis revealed that PS should not exceed 8% (DM basis) in the diet to prevent negative effects on CP digestibility and animal performance. In conclusion, the results of this meta-analysis do not support the dietary inclusion of PS in cattle diets beyond 8%.


Assuntos
Arachis , Fabaceae , Bovinos , Animais , Rúmen/metabolismo , Fermentação , Ração Animal/análise , Dieta/veterinária , Suplementos Nutricionais/análise , Extratos Vegetais/farmacologia , Éteres/metabolismo , Éteres/farmacologia , Digestão
4.
Fitoterapia ; 166: 105458, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-36796458

RESUMO

A series of novel chalcone derivatives containing pyrazole oxime ethers were designed and synthesized. The structures of all the target compounds were determined by NMR and HRMS. The structure of H5 was further confirmed via single-crystal X-ray diffraction analysis. The results of biological activity test showed that some of the target compounds exhibited significant antiviral and antibacterial activities. The test results of EC50 value against tobacco mosaic virus showed that H9 had the best curative and protective effect, and the EC50 value of curative activity of H9 was 166.9 µg/mL, which was superior to ningnanmycin (NNM) 280.4 µg/mL, the EC50 value of protective activity of H9 was 126.5 µg/mL, which was superior to ningnanmycin 227.7 µg/mL. Microscale thermophoresis (MST) experiments demonstrated that H9 (Kd = 0.0096 ± 0.0045 µmol/L) exhibited a strong binding ability with tobacco mosaic virus capsid protein (TMV-CP), which was far superior to ningnanmycin (Kd = 1.2987 ± 0.4577 µmol/L). In addition, molecular docking results showed that the affinity of H9 to TMV protein was significantly higher than ningnanmycin. The results of against bacterial activity showed that H17 has a good inhibiting effect against Xanthomonas oryzae pv. oryzae (Xoo), the EC50 value of H17 was 33.0 µg/mL, which was superior to the commercial drugs thiodiazole copper (68.1 µg/mL) and bismerthiazol (81.6 µg/mL), and the antibacterial activity of H17 was verified by scanning electron microscopy (SEM).


Assuntos
Chalcona , Chalconas , Vírus do Mosaico do Tabaco , Chalconas/farmacologia , Estrutura Molecular , Chalcona/farmacologia , Simulação de Acoplamento Molecular , Éteres/metabolismo , Éteres/farmacologia , Antivirais/química , Antibacterianos/química , Relação Estrutura-Atividade , Testes de Sensibilidade Microbiana
5.
J Anim Sci ; 1012023 Jan 03.
Artigo em Inglês | MEDLINE | ID: mdl-36444860

RESUMO

Two experiments were conducted to determine the digestible energy and metabolizable energy contents, as well as the apparent ileal digestibility and standardized ileal digestibility of amino acids in full-fat soybean fed to growing pigs. Ten full-fat soybean samples were collected from different areas in China and used in two experiments in this study. In Exp. 1, 66 growing pigs (initial body weight = 18.48 ± 1.2 kg) were randomly allotted to 1 of 11 diets (n = 6) including a corn basal diet and 10 experimental diets formulated by replacing the corn with 30% full-fat soybean. In Exp. 2, 11 growing pigs (initial body weight = 50.45 ± 3.2 kg) were surgically equipped with a T-cannula in the distal ileum and arranged in a 6 × 11 Youden square design with 11 diets and 6 periods. The diets included an N-free diet based on cornstarch and sucrose and 10 experimental diets formulated with full-fat soybeans as the sole source of amino acids. Chromic oxide was added into the diets as an indigestible maker to calculate the digestibility of the amino acids. Results showed that there was considerable variation in neutral detergent fiber, acid detergent fiber, and trypsin inhibitor contents in the 10 full-fat soybean samples with a coefficient of variation greater than 10%. On a dry matter basis, the averaged digestible energy and metabolizable energy values in the 10 full-fat soybean samples were 4,855 and 4,555 kcal/kg, respectively, both were positively correlated with the ether extract content. The best-fitted prediction equations for digestible energy and metabolizable energy of full-fat soybean were: digestible energy, kcal/kg = 3,472 + 94.87 × ether extract - 97.63 × ash (R2 = 0.91); metabolizable energy, kcal/kg = 3,443 + 65.11 × ether extract - 36.84 × trypsin inhibitor (R2 = 0.91). In addition, all full-fat soybean samples showed high apparent ileal digestibility and standardized ileal digestibility values in amino acids and were all within the range of previously published values. Those values significantly varied among different samples (P < 0.05) for most amino acids, except for glycine and proline. In conclusion, full-fat soybean is a high-quality protein ingredient with high ileal digestibility of amino acids when fed to growing pigs, and the metabolizable energy value of full-fat soybean could be predicted based on its ether extract and trypsin inhibitor contents.


Full-fat soybean is an excellent protein source supplied in swine diets, especially in weaned and growing stages. However, the high price limits its utilization in practice, so it is vital to accurately evaluate the available energy and digestible amino acids contents in full-fat soybean to better formulate a least-cost diet. Ten full-fat soybean samples were collected from different areas in China, and two experiments were conducted to evaluate the energy concentration and amino acids digestibility of full-fat soybean and to establish the corresponding prediction equations. The averaged digestible and metabolizable energy of FFSB were 4,855 and 4,555 kcal/kg (dry matter basis), and the best-fitted prediction equations for digestible energy and metabolizable energy of full-fat soybean were: digestible energy, kcal/kg = 3,472 + 94.87 × ether extract − 97.63 × ash; metabolizable energy, kcal/kg = 3,443 + 65.11 × ether extract − 36.84 × trypsin inhibitor. Except for glycine and proline, the digestibility of other amino acids significantly varied among 10 full-fat soybean samples but all were within the range of previously published values. In addition, all the amino acids exhibited high digestibility, indicating that full-fat soybean is a protein ingredient with high quality.


Assuntos
Aminoácidos , Glycine max , Suínos , Animais , Glycine max/química , Aminoácidos/metabolismo , Digestão , Detergentes/metabolismo , Inibidores da Tripsina/metabolismo , Ração Animal/análise , Dieta , Íleo/metabolismo , Éteres/metabolismo , Extratos Vegetais , Fenômenos Fisiológicos da Nutrição Animal , Zea mays/metabolismo
6.
J Dairy Sci ; 106(1): 233-244, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36333132

RESUMO

Lactation diets dependent on rumen undegradable protein (RUP) sources derived from soybean meal (SBM) products are generally high in Lys and poor in Met. We conducted an experiment to evaluate the effects of increasing dietary RUP and altering digestible AA supply by inclusion of heat-treated soybean meal (HTSBM) or high-protein corn dried distillers grains with soluble (DDGS) on performance in mid-lactation dairy cows. Twenty-four Holstein cows (200 ± 40 d in milk and 30.0 ± 3.92 kg/d of milk yield) blocked according to parity, milk yield, and days in milk were used in a 3 × 3 Latin square design experiment with 21-d periods. Treatments were (1) control (CON), a diet with 6.0% RUP containing 15.9% SBM as the main protein source; (2) HTSBM, a diet with 6.7% RUP containing 4.4% HTSBM partially replacing SBM; and (3) high-protein DDGS (FP; FlexyPro, SJC Bioenergia), a diet with 6.9% RUP containing 5.34% FP partially replacing SBM and ground corn. Diets had similar crude protein (16.9%) and net energy of lactation. Data were submitted to ANOVA using the mixed procedure of SAS software (SAS Institute Inc.). Treatment differences were evaluated using orthogonal contrasts: (1) increasing RUP (SBM vs. HTSBM + FP) and (2) altering digestible AA supply (HTSBM vs. FP). Cows fed HTSBM and FP had greater intake (values in parentheses represent treatment means of CON, HTSBM, and FP, respectively) of neutral detergent fiber (7.14, 7.35, and 7.69 kg/d), crude protein (4.27, 4.37, and 4.51 kg/d), and ether extract (0.942, 0.968, and 1.04 kg/d) compared with cows fed CON. Feeding FP resulted in greater intake of neutral detergent fiber and ether extract compared with HTSBM. Cows fed HTSBM and FP had lower sorting index for feed particles <4 mm than cows fed CON (1.029, 1.008, and 1.022). Feeding FP resulted in greater intake of feed particles <4 mm compared with HTSBM. Treatments containing HTSBM or FP tended to decrease organic matter digestibility (72.4, 71.2, and 71.1%), but no other effects were detected in digestibility of neutral detergent fiber, crude protein, or ether extract. No evidence for differences among treatments was detected in excretion of purine derivatives in milk and urine. Milk yield was greater in cows fed HTSBM or FP than in cows fed CON (28.0, 28.9, and 28.8 kg/d, respectively). Cows fed HTSBM or FP tended to have greater energy-corrected milk and protein yield compared with those fed CON. Milk protein concentration was greater in DDGS cows than those in the HTSBM group (3.45 and 3.40%, respectively). No differences were detected in milk fat yield and concentration, milk urea nitrogen, feed efficiency, or serum concentrations of urea and glucose. Overall, increasing dietary RUP by feeding HTSBM or FP improved intake of nutrients and milk yield without affecting feed efficiency. Altering digestible AA supply while maintaining similar dietary RUP had negligible effects on performance of cows.


Assuntos
Ração Animal , Zea mays , Gravidez , Feminino , Bovinos , Animais , Zea mays/metabolismo , Ração Animal/análise , Temperatura Alta , Detergentes/metabolismo , Farinha , Lactação , Rúmen/metabolismo , Dieta/veterinária , Glycine max/metabolismo , Proteínas Alimentares/metabolismo , Nutrientes , Ureia/metabolismo , Éteres/metabolismo , Extratos Vegetais/metabolismo
7.
Trop Anim Health Prod ; 54(6): 340, 2022 Oct 10.
Artigo em Inglês | MEDLINE | ID: mdl-36214928

RESUMO

An experiment was conducted to see how replacing soybean meal with chickpea grains (CHPE) affected the performance, milk production, digestibility, nitrogen (N) balance, and blood metabolites of Awassi ewes. Thirty Awassi ewes with an initial body weight of 53.2 ± 2.31 kg and aged between 4 and 5 years were selected and randomly assigned to different feeding treatments (10 ewes per diet). Dietary dry matter (DM) was (1) 0 g/kg CHPE (CON); (2) 150 g/kg CHPE (CHPE150); and (3) 300 g/kg CHPE (CHPE300). The costs of these diets were determined using current ingredient prices. The experiment lasted 9 weeks. During the trial, ewes and their lambs were kept in individual pens. Daily nutrient intake was monitored. Every 2 weeks, the body weight (BW), milk output, and composition of the ewes were measured. In comparison to the CON diet, adding the CHPE to the experimental diets lowered feed costs (US$) per ton by 11% for CHPE150 and 21% for CHPE300. The CHPE300 group had a lower (P < 0.05) consumption of neutral detergent fiber (NDF) than the CHPE150 group, while the CON group had the highest (P < 0.05) intake of NDF. The intake of ether extract (EE) (g/d) was higher (P < 0.05) in the ewes fed the CHPE300 compared to the ewes fed CHPE150, and it was lowest in ewes fed the CON diet. When the ewes were fed the CHPE300 and the CHPE150 diets, the total solids (g/kg) in each kg of milk produced per day was higher (P < 0.05) than when they were fed the CON diet. The cost per kg of milk produced by the ewes was lowered (P < 0.05) when the CHPE was added to their diets. When the ewes on the CHPE300 and the CHPE150 diets were compared to the ewes on the CON diet, crude protein (CP) digestibility was higher (P < 0.05). The EE digestibility was higher (P < 0.05) for the CHPE300 group, while the CHPE150 group had an intermediate outcome. The CHPE300 group had lower amounts of N in their feces and urine (P < 0.05) than the other groups. The retention of N (g/100 g) in the ewes fed the CHPE300, and the CHPE150 diets was higher (P < 0.05) than in the ewes fed the CON diet. As a result, the current research demonstrates that part of soybean meal and barley grain could be replaced with chickpeas in the diets of lactating Awassi ewes.


Assuntos
Cicer , Lactação , Ração Animal/análise , Animais , Peso Corporal , Cicer/metabolismo , Detergentes/metabolismo , Dieta/veterinária , Fibras na Dieta/metabolismo , Digestão , Éteres/metabolismo , Feminino , Leite/metabolismo , Nitrogênio/metabolismo , Extratos Vegetais/metabolismo , Rúmen/metabolismo , Ovinos , Carneiro Doméstico/metabolismo , Glycine max/metabolismo
8.
Biol Trace Elem Res ; 200(12): 5218-5225, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34997923

RESUMO

This study aimed to investigate the effects of different levels of zinc oxide nanoparticles on broilers' performance, nutrient digestibility, carcass criteria, and blood biochemistry. A total of 120 1-day-old unsexed broiler chickens (Ross 308) were fed zinc oxide nanoparticles at different levels (0, 20, 40, or 60 mg/kg) in their diets. Each treatment included 6 replicate pens with 5 birds each. The experiment lasted 42 days. The brooding temperatures were 37.8 °C, 35.8 °C, and 29.9 °C during 1-10 days, 11-21 days, and 22-42 days of age, respectively. The results revealed that dietary supplementation of nanoparticles of zinc oxide at 20, 40, and 60 mg/kg diet significantly improved body weight, body weight gain, and feed conversion ratio showing linear effects (P < 0.05) compared to the birds fed the control diet under hot climatic conditions. Dietary addition of zinc oxide nanoparticles at 20, 40, and 60 mg/kg linearly increased (P < 0.05) the nutrient digestibility of crude protein, crude fiber, and ether extract compared to the control group. Birds fed the supplemented diets had improved liver and kidney function without any negative effects on zinc, inorganic phosphorus, triiodothyronine (T3), and thyroxine (T4) levels in serum compared to the control. Diets supplemented with zinc oxide nanoparticles linearly (P < 0.05) improved the dressing percent and reduced abdominal fat percent compared to the control group. In view of the above findings, it can be concluded that dietary supplementations of zinc oxide nanoparticles at 20, 40, and 60 mg/kg resulted in improved growth performance, nutrient digestibility, carcass criteria, and liver and kidney functions of broiler chickens under hot environmental conditions.


Assuntos
Nanopartículas , Óxido de Zinco , Ração Animal/análise , Fenômenos Fisiológicos da Nutrição Animal , Animais , Galinhas/metabolismo , Dieta/veterinária , Suplementos Nutricionais , Éteres/metabolismo , Fósforo/metabolismo , Extratos Vegetais/metabolismo , Tiroxina , Tri-Iodotironina , Aumento de Peso , Zinco/metabolismo , Óxido de Zinco/farmacologia
9.
Chembiochem ; 19(19): 2081-2087, 2018 10 04.
Artigo em Inglês | MEDLINE | ID: mdl-30059599

RESUMO

The copper(I)-mediated azide-alkyne cycloaddition (CuAAC) of 3'-propargyl ether and 5'-azide oligonucleotides is a particularly promising ligation system because it results in triazole linkages that effectively mimic the phosphate-sugar backbone of DNA, leading to unprecedented tolerance of the ligated strands by polymerases. However, for a chemical ligation strategy to be a viable alternative to enzymatic systems, it must be equally as rapid, as discriminating, and as easy to use. We found that the DNA-templated reaction with these modifications was rapid under aerobic conditions, with nearly quantitative conversion in 5 min, resulting in a kobs value of 1.1 min-1 , comparable with that measured in an enzymatic ligation system by using the highest commercially available concentration of T4 DNA ligase. Moreover, the CuAAC reaction also exhibited greater selectivity in discriminating C:A or C:T mismatches from the C:G match than that of T4 DNA ligase at 29 °C; a temperature slightly below the perfect nicked duplex dissociation temperature, but above that of the mismatched duplexes. These results suggest that the CuAAC reaction of 3'-propargyl ether and 5'-azide-terminated oligonucleotides represents a complementary alternative to T4 DNA ligase, with similar reaction rates, ease of setup and even enhanced selectivity for certain mismatches.


Assuntos
Alcinos/metabolismo , Azidas/metabolismo , Química Click/métodos , Reação de Cicloadição/métodos , DNA/metabolismo , Éteres/metabolismo , Oligonucleotídeos/metabolismo , Cobre/química , DNA Ligases/metabolismo , Replicação do DNA , Cinética , Especificidade por Substrato
10.
Artigo em Inglês | MEDLINE | ID: mdl-28885583

RESUMO

The migration and accumulation of octachlorodipropyl ether (OCDPE) in soil-tea systems were investigated using a gas chromatography-electron capture detector (GC-ECD) method in young and old tea gardens. When the residual concentration of OCDPE was 100 g a.i. hm-2 in soils, the peak concentrations of OCDPE in fresh leaves of young and old tea plants were 0.365 mg/kg and 0.144 mg/kg, taking 45 days and 55 days, respectively. Equations for the accumulation curves of OCDPE in fresh leaves of young and old tea plants were Ct = 0.0227e0.0566t (R² = 0.9154) and Ct = 0.0298e-0.0306t (R² = 0.7156), and were Ct = 3.8435e0.055t (R² = 0.9698) and Ct = 1.5627e-0.048t (R² = 0.9634) for dissipation curves, with a half-life of 14.4 days and 12.6 days, respectively. These results have practical guiding significance for controlling tea food safety.


Assuntos
Camellia sinensis/metabolismo , Éteres/análise , Sinergistas de Praguicidas/análise , Folhas de Planta/metabolismo , Poluentes do Solo/análise , Cromatografia Gasosa , Monitoramento Ambiental , Éteres/metabolismo , Inocuidade dos Alimentos , Jardins , Meia-Vida , Sinergistas de Praguicidas/metabolismo , Poluentes do Solo/metabolismo
11.
Environ Monit Assess ; 188(10): 551, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-27604890

RESUMO

The dissipation behavior of octachlorodipropyl ether (OCDPE) residues in fresh tea shoots and in tea prepared under field conditions was investigated, and the transfer of residues from brewed tea to tea infusion was determined. OCDPE levels in tea shoots, prepared tea, tea infusion, and spent tea leaves were determined using a sensitive and simple method. The dissipation of OCDPE is fairly slow in tea shoots and prepared tea, with half-life values of 5.10 and 5.46 days, respectively. The degradation rates of OCDPE residues in tea processing were 23.9-43.1 %. The terminal residues of OCDPE in tea shoots and prepared tea samples after 20 and 30 days of OCDPE application were higher than 0.01 mg/kg. However, OCDPE's transfer rates from brewed tea to tea infusion were only 6.0-14.8 %. Further studies on risk assessment of OCDPE residue in tea on the basis of the relationship of OCDPE in prepared tea and infusion are warranted.


Assuntos
Camellia sinensis/metabolismo , Monitoramento Ambiental/métodos , Éteres/análise , Resíduos de Praguicidas/análise , Sinergistas de Praguicidas/análise , Chá/química , Camellia sinensis/química , Camellia sinensis/crescimento & desenvolvimento , Éteres/metabolismo , Contaminação de Alimentos/análise , Resíduos de Praguicidas/metabolismo , Sinergistas de Praguicidas/metabolismo , Brotos de Planta/química , Brotos de Planta/crescimento & desenvolvimento , Brotos de Planta/metabolismo
12.
Drug Dev Ind Pharm ; 39(10): 1523-30, 2013 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-23003006

RESUMO

Angelica gigas Nakai and its components are known to have neuroprotective, antiplatelet, and anticancer activities. The present study evaluated the in vitro and in vivo biopharmaceutical characterization of Angelica gigas component substances, including decursin (the main substance), decursinol angelate (decursin isomer), JH714 (ether form of decursin) and epoxide decursin (epoxide form of decursin). Decursin, decursinol angelate and JH714 exhibited acceptable metabolic stability (>50%) in liver microsomes from human and higher bound fraction (>90%) in human plasma operating ultrafiltration. Decursin and decursinol angelate in CYP1A2 and CYP2C19 indicated less than 50% CYP activity, suggesting inhibition of the CYP isoforms using Vivid® CYP screening kit. JH714 only showed an apparent permeability coefficient of <10 × 10⁻6 cm/s in MDCK cells, suggesting that it is poorly absorbed. Blood brain barrier permeability was examined after oral administration to male Sprague-Dawley (SD) rats, and pharmacokinetic studies were performed after oral and intravenous administration of 10 mg/kg compounds. Decursin, decursinol angelate and JH714 showed ratios of compound concentration in brain with respect to plasma (Cbrain/Cplasma) of >1.5, suggesting good brain/plasma ratio at 0.5, 1, 3, and 5 h. In contrast, Cbrain/Cplasma was <0.5 for epoxide decursin. For all test compounds, >1.5% of the dose remained in GI tract after 8 h, and the excretion rate in urine was <0.5% which suggests that gastro intestinal tract may be major site of disposition following oral administration. Finally, these results may be useful for the design of dosage regimens of decursin and its derivatives.


Assuntos
Antineoplásicos Fitogênicos/farmacocinética , Benzopiranos/farmacocinética , Butiratos/farmacocinética , Fármacos Neuroprotetores/farmacocinética , Angelica/química , Animais , Antineoplásicos Fitogênicos/administração & dosagem , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/metabolismo , Hidrocarboneto de Aril Hidroxilases/antagonistas & inibidores , Hidrocarboneto de Aril Hidroxilases/metabolismo , Benzopiranos/administração & dosagem , Benzopiranos/química , Benzopiranos/metabolismo , Biotransformação , Barreira Hematoencefálica/metabolismo , Butiratos/administração & dosagem , Butiratos/química , Butiratos/metabolismo , Citocromo P-450 CYP1A2/metabolismo , Inibidores do Citocromo P-450 CYP1A2 , Citocromo P-450 CYP2C19 , Cães , Inibidores Enzimáticos/administração & dosagem , Inibidores Enzimáticos/química , Inibidores Enzimáticos/metabolismo , Inibidores Enzimáticos/farmacocinética , Compostos de Epóxi/administração & dosagem , Compostos de Epóxi/química , Compostos de Epóxi/metabolismo , Compostos de Epóxi/farmacocinética , Éteres/química , Éteres/metabolismo , Éteres/farmacologia , Etnofarmacologia , Humanos , Absorção Intestinal , Células Madin Darby de Rim Canino , Masculino , Medicina Tradicional do Leste Asiático , Microssomos Hepáticos/metabolismo , Fármacos Neuroprotetores/administração & dosagem , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/metabolismo , Ratos , Ratos Sprague-Dawley
13.
Free Radic Res ; 45(4): 461-8, 2011 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-21235282

RESUMO

Selenoethers attached to functional groups through propyl chain viz., bis(3-carboxypropyl)selenide (SeBA), bis(3-hydroxypropyl)selenide (SePOH) and bis(3-aminopropyl)selenide dihydrochloride (SePAm), have been examined for their ability to inhibit peroxyl radical mediated DNA damage, peroxyl radical scavenging ability and glutathione peroxidase (GPx) like activity. The DNA damage was monitored by gel electrophoresis, bimolecular rate constants for scavenging of model peroxyl radical were determined by pulse radiolysis and the GPx activity was followed by their ability to reduce hydrogen peroxide in the presence of glutathione utilizing NADPH decay and HPLC analysis. Among these compounds, SeBA showed maximum DNA protecting activity and it was also the most efficient in scavenging peroxyl radicals with the highest GPx mimicking activity. Quantum chemical calculations confirmed that SeBA with the highest energy level of HOMO (highest occupied molecular orbital) is the easiest to undergo oxidation and therefore exhibits better radical scavenging, GPx mimicking and DNA protecting activity than SePOH or SePAm.


Assuntos
Antioxidantes/metabolismo , Éteres/metabolismo , Sequestradores de Radicais Livres/síntese química , Glutationa Peroxidase/metabolismo , Compostos de Selênio/química , Antioxidantes/síntese química , Tetracloreto de Carbono/análogos & derivados , Tetracloreto de Carbono/metabolismo , Cromatografia Líquida de Alta Pressão , Dano ao DNA , Éteres/síntese química , Sequestradores de Radicais Livres/metabolismo , Glutationa/metabolismo , Mimetismo Molecular , NADP/metabolismo , Oxirredução , Plasmídeos/metabolismo , Radiólise de Impulso , Ácido Selênico , Selênio/química , Selênio/metabolismo , Soluções
14.
Phytochemistry ; 68(6): 797-801, 2007 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-17258245

RESUMO

Oxygenated polyunsaturated fatty acids synthesized via the lipoxygenase pathway play a role in plant responses to pathogen attack. In solanaceous plants, the preferential stimulation of the 9-lipoxygenase pathway in response to pathogen infection leads to the formation of the divinyl ether-containing polyunsaturated fatty acids colneleic and colnelenic acid, as well as hydroxy and trihydroxy polyunsaturated fatty acids. To functionally assess the role of divinyl ethers, transgenic potato plants were generated which express an RNA interference construct directed against the pathogen-inducible 9-divinyl ether synthase. Efficient reduction of 9-divinyl ether synthase transcript accumulation correlated with reduced levels of colneleic and colnelenic acid. However, in response to infection with virulent Phytophthora infestans, the causal agent of late blight disease, no significant differences in pathogen biomass could be detected suggesting that the levels of antimicrobial divinyl ethers are not critical for defense against Phytophthora infestans in a compatible interaction.


Assuntos
Ácidos Graxos Insaturados/metabolismo , Solanum tuberosum/metabolismo , Compostos de Vinila/metabolismo , Éteres/química , Éteres/metabolismo , Ácidos Graxos Monoinsaturados/química , Ácidos Graxos Monoinsaturados/metabolismo , Ácidos Graxos Insaturados/química , Modelos Químicos , Estrutura Molecular , Oxirredução , Phytophthora/crescimento & desenvolvimento , Doenças das Plantas/microbiologia , Folhas de Planta/genética , Folhas de Planta/metabolismo , Folhas de Planta/microbiologia , Plantas Geneticamente Modificadas , Solanum tuberosum/genética , Solanum tuberosum/microbiologia , Compostos de Vinila/química
15.
Rapid Commun Mass Spectrom ; 17(8): 800-10, 2003.
Artigo em Inglês | MEDLINE | ID: mdl-12672134

RESUMO

The extent to which electrochemistry on-line with electrospray mass spectrometry can be used to mimic cytochrome P450 catalyzed oxidations has been investigated. Comparisons on the mechanistic level have been made for most reactions in an effort to explain why certain reactions can, and some cannot, be mimicked by electrochemical oxidations. The EC/MS/MS system used successfully mimics in cases where the P450 catalyzed reactions are supposed to proceed via a mechanism initiated by a one-electron oxidation, such as N-dealkylation, S-oxidation, P-oxidation, alcohol oxidation and dehydrogenation. The P450 catalyzed reactions initiated via direct hydrogen atom abstraction, such as O-dealkylation and hydroxylation of unsubstituted aromatic rings, generally had a too high oxidation potential to be electrochemically oxidized below the oxidation potential limit of water, and were not mimicked by the EC/MS/MS system. Even though the EC/MS/MS system is not able to mimic all oxidations performed by cytochrome P450, valuable information can be obtained concerning the sensitivity of the substrate towards oxidation and in which position of the molecule oxidations are likely to take place. For small-scale electrochemical synthesis of metabolites, starting from the drug, the EC/MS/MS system should be very useful for quick optimization of the electrochemical conditions. The simplicity of the system, and the ease and speed with which it can be applied to a large number of compounds, make it a useful tool in drug metabolism research.


Assuntos
Sistema Enzimático do Citocromo P-450/metabolismo , Eletroquímica/métodos , Espectrometria de Massas/métodos , Oxigênio/metabolismo , Álcoois/metabolismo , Aldeídos/metabolismo , Alquilação , Aminas/metabolismo , Éteres/metabolismo , Hidroxilação , Estrutura Molecular , Oxirredução , Fenóis/metabolismo , Fósforo/metabolismo , Enxofre/metabolismo
16.
Plant Cell ; 11(3): 485-94, 1999 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-10072406

RESUMO

We conducted a study of the patterns and dynamics of oxidized fatty acid derivatives (oxylipins) in potato leaves infected with the late-blight pathogen Phytophthora infestans. Two 18-carbon divinyl ether fatty acids, colneleic acid and colnelenic acid, accumulated during disease development. To date, there are no reports that such compounds have been detected in higher plants. The divinyl ether fatty acids accumulate more rapidly in potato cultivar Matilda (a cultivar with increased resistance to late blight) than in cultivar Bintje, a susceptible cultivar. Colnelenic acid reached levels of up to approximately 24 nmol (7 microgram) per g fresh weight of tissue in infected leaves. By contrast, levels of members of the jasmonic acid family did not change significantly during pathogenesis. The divinyl ethers also accumulated during the incompatible interaction of tobacco with tobacco mosaic virus. Colneleic and colnelenic acids were found to be inhibitory to P. infestans, suggesting a function in plant defense for divinyl ethers, which are unstable compounds rarely encountered in biological systems.


Assuntos
Ácidos Graxos/biossíntese , Phytophthora , Doenças das Plantas , Solanum tuberosum/metabolismo , Éteres/metabolismo , Ácidos Graxos Monoinsaturados/metabolismo , Ácidos Graxos Insaturados/metabolismo , Lipoxigenase/metabolismo , Oxirredução , Folhas de Planta/metabolismo , Plantas Tóxicas , Nicotiana/metabolismo , Compostos de Vinila
17.
J Anim Sci ; 75(2): 430-6, 1997 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-9051466

RESUMO

Growth performance and utilization of nutrients and energy in three high-oil corn varieties (5.4 to 9.7% ether extract) and regular corn (4.2% ether extract) were compared in three experiments using growing pigs. Twenty-four 25-kg crossbred barrows were used in Exp. 1 to evaluate nutrient and energy digestibility in the three high-oil corn varieties and regular corn. Four diets were formulated to contain 97% of one of four varieties of corn (Control, TC1, TC2, and X122 varieties) and 3% minerals and vitamins. Digestibilities of nitrogen and ether extract were similar (P > .05) for regular corn and all three varieties of high-oil corn. The digestible energy concentrations (kcal/g; as-fed basis) for control, TC1, TC2, and X122 corn varieties were 3.29, 3.57, 3.4, and 3.41, respectively, with control lower (P < .05) than TC2 or X122 and TC1 higher (P < .05) than TC2 or X122. Metabolizable energy concentrations averaged 98.4% of digestible energy concentrations. In Exp. 2, four diets formulated to contain 79% of one of the four corn varieties, 18.25% 48% CP soybean meal, 2.45% vitamins and minerals, and .3% lysine.HCl were fed to 24 crossbred barrows (six pigs per diet) in a nutrient and energy balance study similar to the Exp. 1. Results were similar to those obtained in Exp. 1. The same four diets that were used in Exp. 2 were fed to 40 (10/diet) 20-kg crossbred pigs (20 barrows and 20 gilts) in a 28-d growth performance study (Exp. 3). Gain:feed ratios were .39, .43, .42, and .42 and growth rates (kg/d) were .68, .74, .70, and .72 for diets containing control, TC1, TC2, and X122 corn varieties, respectively. These translate to 8 to 10% improvement in feed efficiency and a numerical improvement in weight gain (3 to 9%) when high-oil corn was fed as compared with control corn. The results of nitrogen, ether extract, and energy balance and feeding experiments with growing pigs indicate efficient utilization of nutrients in diets containing high-oil corn.


Assuntos
Óleo de Milho/normas , Ingestão de Energia/fisiologia , Metabolismo Energético/fisiologia , Suínos/crescimento & desenvolvimento , Suínos/fisiologia , Animais , Óleo de Milho/química , Óleo de Milho/metabolismo , Digestão/fisiologia , Éteres/análise , Éteres/metabolismo , Feminino , Masculino , Nitrogênio/análise , Nitrogênio/metabolismo , Distribuição Aleatória , Suínos/metabolismo
18.
Lipids ; 30(6): 541-6, 1995 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-7651082

RESUMO

We investigated the effects of perilla oil containing a high level of alpha-linolenic acid on in vivo phospholipid metabolism, particularly three subclasses of choline glycerophospholipids (CGP) and ethanolamine glycerophospholipids (EGP), in rat kidney. After three weeks of feeding, a significantly lower proportion (by 35%) of the alkylacyl subclass of CGP was found in the perilla oil, as compared to corn oil-fed animals. The alkylacyl species of EGP was also higher in the perilla oil than in the corn oil-fed animals. These alterations were accompanied by a remarkably lower proportion of arachidonic acid and a higher level of eicosapentaenoic acid (EPA) in all six subclasses of CGP and EGP in the perilla oil-fed animals. The levels of linoleic acid were even higher in the diacyl subclasses of CGP and EGP in the perilla oil group, suggesting that desaturase and elongase enzymes prefer n-3 to n-6 fatty acids as substrates for diacyl species. These data are useful in defining the effects of alpha-linolenic acid on the biosynthesis of renal phospholipids and on the replacement of n-6 with n-3 fatty acids in the six CGP and EGP subclasses.


Assuntos
Gorduras Insaturadas na Dieta/farmacologia , Éteres/metabolismo , Rim/metabolismo , Fosfolipídeos/metabolismo , Ácido alfa-Linolênico/farmacologia , Animais , Ácido Araquidônico/metabolismo , Óleo de Milho/administração & dosagem , Gorduras Insaturadas na Dieta/administração & dosagem , Ácido Eicosapentaenoico/metabolismo , Feminino , Rim/efeitos dos fármacos , Fosfatidilcolinas/metabolismo , Fosfatidiletanolaminas/metabolismo , Ratos , Ratos Endogâmicos F344 , Ácido alfa-Linolênico/administração & dosagem
19.
J Anim Sci ; 68(2): 483-9, 1990 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-2312437

RESUMO

Twenty-four steers initially averaging 221 kg BW were used to evaluate the effects of lysocellin and calcium (Ca) level on performance and ruminal and plasma characteristics. Lysocellin at 0 or 22 mg/kg of diet and Ca at .3 or .6% were fed in a 2 X 2 factorial arrangement of treatments. Steers in individual pens had ad libitum access to a diet consisting of 80% corn silage and 20% (DM basis) of a protein, mineral and vitamin supplement. Ruminal fluid and blood samples were collected on d 42 and 85 of the 113-d trial. Steers fed the .6% Ca diet gained faster and required less feed/unit of gain than those fed the .3% Ca diet (P less than .05). There was a tendency for a lysocellin X Ca interaction for gain and feed efficiency (P less than .10). Lysocellin tended to depress performance when fed with .3% Ca, but it tended to improve gain and feed efficiency when fed with .6% Ca. Molar proportions of propionate were higher and those of acetate were lower (P less than .01) for steers fed lysocellin. Ruminal-soluble Zn, Fe and Cu levels were higher (P less than .01) in steers fed lysocellin. Ruminal-soluble Ca (P less than .01) was higher and ruminal-soluble P and Na were lower (P less than .01) in steers fed .6% Ca. Plasma K was higher (P less than .05) in steers fed .6% Ca but it was lower (P less than .05) in steers fed lysocellin. Results of this study indicate that dietary Ca affects certain metabolic responses to lysocellin in growing cattle.


Assuntos
Antibacterianos/metabolismo , Cálcio/metabolismo , Bovinos/metabolismo , Rúmen/metabolismo , Animais , Antibacterianos/administração & dosagem , Cálcio/administração & dosagem , Bovinos/sangue , Dieta , Éteres/administração & dosagem , Éteres/metabolismo , Furanos , Ionóforos , Masculino , Silagem , Zea mays
20.
Biochem J ; 257(2): 389-97, 1989 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-2539084

RESUMO

The terminal adipose differentiation of Ob1771 cells, characterized by glycerol-3-phosphate dehydrogenase activity and triacylglycerol accumulation, was studied in serum-free hormone-supplemented medium containing growth hormone, tri-iodothyronine, insulin, transferrin and fetuin. Arachidonic acid was able to substitute for a crude adipogenic fraction isolated from fetal bovine serum but not for growth hormone or tri-iodothyronine. Arachidonic acid was also able to increase in a rapid and dramatic manner cyclic AMP production; moreover it was able to amplify the adipose conversion promoted by other agents elevating cyclic AMP concentrations and to induce inositol phospholipid breakdown. Both phorbol 12-myristate 13-acetate, a protein kinase C activator and ionomycin, a Ca2+-mobilizing agent, showed potent synergy with agents elevating cyclic AMP concentrations for the promotion of adipose conversion, whereas 8-bromo cyclic GMP and 4 alpha-phorbol 12,13-dibutyrate were ineffective. The triggering of both the cyclic AMP and inositol phospholipid pathways was accompanied by a single round of cell division, and within a few days all the cells became differentiated. Similar results were obtained, after exposure to arachidonic acid, with preadipose 3T3-F442A cells and with rat adipose precursor cells in primary culture. The availability of arachidonic acid from intracellular stores and/or of exogenous origin should play a major role for the onset of critical mitoses leading to terminal differentiation in pre-adipose cells.


Assuntos
Tecido Adiposo/metabolismo , Ácidos Araquidônicos/metabolismo , Mitose , Tecido Adiposo/citologia , Animais , Ácido Araquidônico , Diferenciação Celular , Linhagem Celular , AMP Cíclico/metabolismo , GMP Cíclico/análogos & derivados , GMP Cíclico/metabolismo , Éteres/metabolismo , Inositol/metabolismo , Ionomicina , Camundongos , Camundongos Endogâmicos C57BL , Dibutirato de 12,13-Forbol/metabolismo , Fosfolipídeos/metabolismo , Ratos , Acetato de Tetradecanoilforbol/metabolismo
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