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1.
Pine kraft-anthraquinone (kraft-AQ) pulp was bleached in alkaline solution with hydrogen peroxide catalyzed by either [L(1)Mn(IV)(micro-O)(3)Mn(IV)L(1)](PF(6))(2)] (C1) or [LMn(IV)(2)(micro-O)(3)] (ClO(4))(2) (C2) at 60 and 80 degrees C for 120 min with a catalyst charge of 10 ppm on pulp. The resulting bleached pulp was hydrolyzed with cellulase to obtain insoluble and soluble residual lignins. The alkaline bleaching effluents were acidified to precipitate alkaline-soluble lignins. These lignin preparations were then characterized by 2D heteronuclear multiple-quantum coherence (HMQC) NMR spectroscopic techniques. The results showed that biphenyl (5-5) and stilbene structures of the residual lignin in the pulp are preferentially degraded in both the C1- and C2-catalyzed bleachings, whereas beta-O-4, beta-5, and beta-beta structures undergo degradation to a lesser extent. In both cases, the degradation of the residual lignin increased with the increase in reaction temperature from 60 to 80 degrees C. Thus, the result of C1-catalyzed delignification is not in agreement with the observed decrease in the disappearance rate for substrates in the C1-catalyzed oxidation of lignin model compounds with hydrogen peroxide when the reaction temperature is increased from 60 to 80 degrees C. In addition, the resulting residual lignins in the C2-catalyzed bleaching at 80 degrees C are less degraded than the corresponding lignins in the C1-catalyzed bleaching at both 60 and 80 degrees C. Thus, C1 is more effective than C2 as catalyst in the binucleus Mn(IV) complex-catalyzed bleaching of pine kraft-AQ pulp with hydrogen peroxide.  相似文献   

2.
The mineral composition of taro ( Colocasia esculenta (L.) Schott) was analyzed to develop a method to distinguish taro produced in Japan and China. The concentrations of 15 elements (Al, Ca, Cl, Mg, Mn, Br, Co, Cr, Cs, Fe, K, Na, Rb, Sc, Zn) were assayed using instrumental neutron activation analysis. The concentrations of NO(3)(-), SO(4)(2-), H(2)PO(4)(-), Cl(-), malate, and oxalate were measured by ion chromatography. The mean concentrations of H(2)PO(4)(-), Co, Cr, and Na significantly differed (P < 0.01) between taro grown in Japan and that grown in China. Discriminant analysis was performed to identify the most efficient combination of elements and compounds to discriminate the taro geographic origin. The highest percentage of correct classification was achieved with a two-variable model including H(2)PO(4)(-) and Co (100% for Japanese, 93.75% for Chinese). Principal component analysis and cluster analysis using all of the assayed elements and compounds were also conducted to determine which elements significantly accounted for the variation of the taro mineral composition. We report on the potential of H(2)PO(4)(-) and Co concentrations to differentiate taro grown in China and Japan and discuss the sources of variability in the taro mineral composition of our samples.  相似文献   

3.
The suitability of [2,2,4,4-(2)H(4)]sarsasapogenone (1b), [2,2,4,4-(2)H(4)]sarsasapogenin (2b), and [2,2,4,4-(2)H(4)]episarsasapogenin (3b) as isotopically labeled dosing substrates to determine the levels of free and conjugated sapogenins present in feces from sheep grazing saponin-containing plants implicated in the development of ovine heptagenous photosentization diseases was investigated. A 1:4 mixture of [2,2,4,4-(2)H(4)]sarsasapogenin (2b) and [2,2,4,4-(2)H(4)]episarsasapogenin (3b), obtained by reduction of [2,2,4,4-(2)H(4)]sarsasapogenone (1b), was found to retain 94% of incorporated deuterium, when dosed to one sheep. The recovery of the dosed mixture of genins 2b and 3b was calculated to be 85%. Considerable loss of deuterium and a lower recovery of genin material were observed when [2,2,4,4-(2)H(4)]sarsasapogenone (1b) was dosed.  相似文献   

4.
The lignin component found in both water insoluble (WI) and water and alkali insoluble (WIA) fractions derived from SO(2)-impregnated steam-exploded eucalyptus chips (SEE) was isolated and characterized. Dioxane lignins with a sugar content lower than 2% (w/w) were obtained after each material was treated with commercial cellulases. The C9 formulas of both SEE-WI and SEE-WIA dioxane lignins were C(9)H(6.83)N(0.04)O(2.24)(OCH(3))(1.21)(OH(aro))(0.56)(OH(ali))(0. 77) and C(9)H(8.65)N(0.29)O(1.97)(OCH(3))(0.90)(OH(aro))(0. 46)(OH(ali))(1.02), respectively. The weight-average molecular weight (M(w)) of the SEE-WI lignin corresponded to 3.85 kDa, whereas the SEE-WIA lignin had an M(w) of 3.66 kDa for the same polydispersity of 2.4. The SEE-WIA lignin was shown to be more thermally stable than the SEE-WI lignin, requiring temperatures in the range of 520 degrees C for complete degradation. FTIR and (1)H NMR analyses of both untreated and peracetylated lignin fractions showed that (a) the alkali insoluble lignin contained a relatively higher degree of substitution in aromatic rings per C9 unit and that (b) alkaline extraction removed lignin fragments containing appreciable amounts of phenolic hydroxyl groups.  相似文献   

5.
Recently a new assay method that can quantify the singlet oxygen absorption capacity (SOAC) of antioxidants was proposed. In the present work, kinetic study of the reaction of singlet oxygen ((1)O(2)) with carotenoids and vegetable extracts has been performed in ethanol/chloroform/D(2)O (50:50:1, v/v/v) solution at 35 °C. Measurements of the second-order rate constants (k(Q)(S)) and the SOAC values were performed for eight kinds of carotenoids and three kinds of vegetable extracts (red paprika, carrot, and tomato). Furthermore, measurements of the concentrations of the carotenoids included in vegetable extracts were performed, using a HPLC technique. From the results, it has been clarified that the total (1)O(2)-quenching activity (that is, the SOAC value) for vegetable extracts may be explained as the sum of the product {Σ k(Q)(Car-i)(S) [Car-i](i)} of the rate constant (k(Q)(Car-i)(S)) and the concentration ([Car (i)]) of carotenoids included in vegetable extracts.  相似文献   

6.
Synthesis of some new substituted [3-(3-chloro-4-fluorophenyl)-2-oxo-3,4-dihydro-2H-2lambda(5)-benzo[e][1,3,2]oxazaphosphinin-2-yl]-(aryl/alkyl)methanols (7a-k) based on the Pudovick reaction was accomplished in the presence of niobium pentoxide (Nb(2)O(5)) without using an external chiral ligand. Nb(2)O(5) appears to form the metal complex intermediate catalyst system (6) by reacting with 3-(3-chloro-4-fluoro-phenyl)-3,4-dihydrobenzo[e][1,3,2]oxazaphosphinine-2-oxide (4), which not only directs the Pudovick addition reactions of aldehyde but also increases the yields and purity of the products. These compounds exhibited a lethal effect on whip smut of sugarcane and were degraded in the environment in the presence of bacteria and fungi to nontoxic phosphate residues that act as possible plant nutrients. Thus, a new class of benzooxazaphosphininyl methanol derivatives that act in synergy both as antipathogens and as plant nutrients in the environment have been discovered.  相似文献   

7.
We conducted batch experiments for ten metals [Mg, Cr(III), Fe(III), Co, Ni, Cu, Zn, Sr, Cd, Pb] and four soil samples of different composition to determine the relation of the soluble fraction (’intensity’︁) to an adsorbed or precipitated metal pool (’quantity’︁) and, thus, to investigate the buffer function of soils. The soil samples were spiked with 6 to 12 exponentially increasing metal doses added as metal nitrates. The native metal pool involved in sorption processes was characterized by an extraction with 0.025 M (NH4)2EDTA (pH 4.6). The quantity-intensity (Q/I) relations of eight metals [except Cr(III) and Fe(III)] were governed by sorption and complexation processes and can be fitted by Freundlich isotherms. Q/I relations for Cr(III) and two soils indicate a sorption maximum, which can be approximated with the Langmuir isotherm. In a calcareous soil high Cr doses induced the precipitation of a Cr oxide. The solution concentrations of Fe are primarily a function of the pH-dependent solubility of ferrihydrite. For all metals pH was the predominant factor controlling the partitioning between the solid and the liquid phase. Drastic losses in the buffer function of soils primarily occurred in the slightly acidic range. Furthermore, adsorption was also metal specific. On the basis of median Freundlich K values, adsorption increased in the order [median KF values and KF range (mg kg—1) in brackets]: Mg (2.9: 0.9—19) < Sr (4.7: 0.6—21) << Co (17.7: 1.1—143) < Zn (26.7: 1.8—301) = Ni (27.6: 2.4—120) < Cd (71: 2.5—405) << Cr(III) (329: 45—746) < Cu (352: 30—1200) < Pb (1730: 76—4110).  相似文献   

8.
Isotopically labeled D-glucose, D-fructose, 1-deoxy-D-fructose, and 6-deoxyhexoses were applied to detached ripening strawberry (Fragaria x ananassa) fruits, and the incorporation of the isotopes into the key strawberry aroma compounds 2,5-dimethyl-4-hydroxy-3(2H)-furanone (DMHF, 1) and 2,5-dimethyl-4-methoxy-3(2H)-furanone (DMMF, 2) was determined by gas chromatography-mass spectrometry. In contrast to previous reports the data clearly showed that 6-deoxy-D-fructose/6-deoxy-D-glucose and 1-deoxy-D-fructose are not natural precursors of the furanones. However, isotopically labeled 1 and 2 were observed after the application of [1-(2)H]-, [2-(2)H]-, and [6,6-(2)H(2)]-D-glucose as well as [U-(13)C(6)]-, [1-(13)C]-, [1-(2)H]-, [6,6-(2)H(2)]-D-fructose. The isotope label of [4-(2)H]-D-glucose was not recovered in the furanones. In contrast, [2-(2)H]-D-glucose was converted to [1- or 6-(2)H]-1 and [1- or 6-(2)H]-2 by the strawberry fruits. The observed isotope shift can be explained by the catalysis of phosphohexose isomerase in the course of the biogenesis of the hydroxyfuranone (1) and the methoxyfuranone (2) from D-glucose. Thus, the applied D-glucose is metabolized to D-fructose-6-phosphate prior to the transformation into the furanones.  相似文献   

9.
Fatty acid (FA) selectivity of immobilized Candida antarctica B lipase was assessed as influenced by various cosubstrate systems for ester synthesis. Reaction mixtures contained a homologous series of even-chain n-acyl donor (C(4)(-)(16)) substrates (FA or their methyl esters, FAME) and a single alcohol cosubstrate (propanol, 2-propanol, or their acetate derivatives) in hexane. Multiple FA optima were often observed, with preferences for C(6) (or C(4)) followed by C(14) and sometimes C(10). The degree of selectivity among acyl donors was modest (up to 1.28-2.60, based on ratios of selectivity constants) and was dependent on the choice of cosubstrate system. Acyl group selectivity ranged up to 1.31-1.36 for [FA + alcohol], 1. 48-2.60 for [FAME + alcohol], 1.30-1.72 for [FA + alcohol acetate], and 1.28-1.88 [FAME + alcohol acetate] reaction systems. General shifts in selectivity were observed between short-chain (C(4)(-)(8)) and long-chain (C(10)(-)(16)) FA as groups with propanol cosubstrate, whereas shifts in reaction selectivity were observed toward specific FA(s) for 2-propanol cosubstrate. Selectivity among a series of alcohol cosubstrates ranged up to 13-fold in esterification reactions with C(6) FA.  相似文献   

10.
The catalytic oxidation of 2alpha,4alpha-dimethyl-8-oxabicyclo[3.2. 1]oct-6-en-3-one with osmium tetraoxide and excess hydrogen peroxide resulted in the formation of 2alpha,4alpha-dimethyl-6, 7-exo-isopropylidenedioxy-8-oxabicyclo[3.2.1]octan-3-one (2), with 91% yield. Addition of aryllithium reagents to this compound resulted in the formation of the aromatic alcohols (6a-h) with 48-76% yield. These alcohols were treated with thionyl chloride in pyridine, and the corresponding alkenes (7a-h) were obtained with 46-80% yield. The effect of compounds 6a-h and 7a-h on the root growth of Sorghum bicolor was evaluated at a concentration of 6.6 microg g(-)(1). The alcohols 6a-h caused an inhibitory effect (8-100%) on the S. bicolor radicle growth. The three most active compounds were 6e (aryl = p-methylphenyl), 6g (aryl = p-chlorophenyl), and 6h (aryl = p-fluorophenyl) and caused 100% inhibition. The effect of alkenes 7a-h was less pronounced and varied from 15% to 46% inhibition. Another experiment was carried out in a greenhouse to evaluate the effect of alcohols 6e, 6g, and 6h, at a 6.6 microg g(-)(1) dose, against Cucumis sativus, S. bicolor and the weeds Bidens pilosa, Desmodiumtortuosum, and Pennisetum setosum. All three compounds showed an inhibitory effect on the development of the aerial parts (26-73%) and roots (13-79%) of the weeds and crops.  相似文献   

11.
本文介绍了用塞曼石墨炉原子吸收测定蔬菜、水果及其制品中Ｃｒ和Ｃｏ的方法。样品经高温灰化，以磷酸二氢铵作基体改良剂，用平台热解涂层石墨管进行样品测定。经１１组白菜参考样测定验证，铬和钴的相对偏差分别为８．４％和９．０％；两组不同浓度的铬和钴的加标回收率分别９３－１０１％和９４－１０５％。铬和钴的检出限分别为０．４１μｇ／１和０．３９μｇ／ｌ。本法也适用于其它生物样品中Ｃｒ和Ｃｏ的测定。  相似文献   

12.
On the basis of the recent findings that "biogenic amines" can also be formed during thermal food processing from their parent amino acids in a Strecker-type reaction, the formation of 3-aminopropionamide, the biogenic amine of asparagine, was investigated in model systems as well as in thermally processed Gouda cheese. The results of model studies revealed that, besides acrylamide, 3-aminopropionamide was also formed in amounts of 0.1-0.4 mol % when asparagine was reacted in the presence of either glucose or 2-oxopropionic acid. Results of a second series of model experiments in which [(13)C(4)(15)N(2)]-asparagine ([(13)C(4)(15)N(2)]-Asn) and unlabeled 3-aminopropionamide were reacted together in the presence of glucose revealed a >12-fold higher efficacy of 3-aminopropionamide in acrylamide generation as compared to asparagine. Both [(13)C(3)(15)N(2)]-3-aminopropionamide and [(13)C(3)(15)N(1)]-acrylamide were formed during [(13)C(4)(15)N(2)]-Asn degradation in a ratio of about 1:4, supporting the idea that 3-aminopropionamide is a transient intermediate in acrylamide formation. In this study, 3-aminopropionamide was identified and quantified for the first time in foods, namely, in Gouda cheese. Although the fresh cheese contained low amounts of 3-aminopropionamide, its concentrations were much increased to approximately 1300 mug/kg after thermal processing. In isotope labeling studies, performed by administering to the cheese [(13)C(4)(15)N(2)]-Asn in a ratio of 1:2 as compared to the "natural" concentrations of asparagine, similar ratios of unlabeled/labeled 3-aminopropionamide and unlabeled/labeled acrylamide were determined. Thus, 3-aminopropionamide could be verified as a transient intermediate of acrylamide formation during food processing.  相似文献   

13.
Tobacco plants (Nicotiana tabacum L. cv NC82) were supplied with (NH4)2SO4 or NH4Cl at root-zone pH of 6.0 and 4.5 in hydroponic culture for 28 days. Dry matter accumulation, total N and C content, and leaf area and number were not affected by the NH4+ source or root-zone pH. Plants supplied with NH4Cl accumulated up to 1.2 mM Cl g DW-1, but accumulated 37% less inorganic H2PO4- and 47% less SO4(2-) than plants supplied with (NH4)2SO4. The large Cl- accumulation resulted in NH4Cl- supplied plants having a 31% higher inorganic anion (NO3-, H2, PO4-, SO4(2-), and Cl-) charge. This higher inorganic anion charge in the NH4Cl-supplied plants was balanced by a similar increase in K+ charge. Plants supplied with NH4Cl accumulated greater concentrations of Cl- in leaves (up to 5.1% of DW) than plants supplied with (NH4)2SO4 (less than -% DW). Despite the high Cl- concentration of leaves in NH4Cl supplied plants, these plants showed no symptoms of Cl- toxicity. This demonstrates that toxicity symptoms are not due solely to an interaction between high Cl- concentration in tissue and NH4+ nutrition. The increase in root-zone acidity to pH 4.5 from 6.0 did not induce toxicity symptoms.  相似文献   

14.
Certain bioregulators were studied in relation to nitrogen metabolism of pepper plants (Capsicum annuum L. cv. Lamuyo). Plants were grown under controlled conditions and submitted to regular fertilization with macro- and micronutrients. Treatments were as follows: nontreated control (T0); fosfonutren [essential amino acids and micronutrients (46.9 mg L(-)(1))] (T1); biozyme [GA(3) (32.2 mg L(-)(1)) plus IAA (32.2 mg L(-)(1)) plus zeatin (83.2 mg L(-)(1)) plus chelated micronutrients] (T2); and GA(3) [16 mg L(-)(1)] (T3). The concentrations of NO(3)(-), organic N, amino acids, and proteins, the activities of nitrate reductase (NR) and nitrite reductase (NiR), and finally the foliar dry weight and yield were analyzed. The results indicated that the application of certain bioregulators, such as fosfonutren (T1), which contain amino acids can cause a negative effect on the efficiency and utilization of NO(3)(-), resulting in a drastic loss in growth and yield, even under the control treatment, in which no bioregulator was applied. On the contrary, the application of certain bioregulators based principally on the combination of different hormones, as in the case of biozyme (T2), increased NO(3)(-) assimilation under our experimental conditions, due possibly to a greater availability of these bioregulators in the leaves and increased NR and NiR activities. This appears to explain why the T2 treatment gave the greatest foliar dry weight and fruit yield per plant in the experiment.  相似文献   

15.
The effects of the chloride salts LiCl, CaCl(2), MgCl(2), AlCl(3), EuCl(3), and FeCl(3) and the iron salts FeCl(2), FeCl(3), Fe(NO(3))(3), FeSO(4), and Fe(2)(SO(4))(3) on water conductance of exocarp segments (ES) and rates of water uptake into detached sweet cherry fruit (Prunus avium L. cv. Adriana, Early Rivers, Namare, Namosa, and Sam) were studied. ES were excised from the cheek of mature fruit and mounted in stainless steel diffusion cell; water penetration was monitored gravimetrically from donor solutions containing the above mineral salts into a PEG 6000 (osmolality = 1.14 osM, pH 4.8, 25 degrees C) receiver solution. Conductance of ES was calculated from the amount of water taken up per unit of surface area and time by dividing by the gradient in water activity across ES. LiCl, CaCl(2), MgCl(2), FeCl(2), and FeSO(4) had no significant effect on conductance, but AlCl(3), FeCl(3), Fe(NO(3))(3), and Fe(2)(SO(4))(3) significantly reduced conductance compared to water only as a donor. Also, EuCl(3) lowered conductance; however, this effect was not always significant. Effects of salts on water conductance of ES and rates of water uptake into detached fruit were closely related (R 2 = 0.97***). Upon application of an FeCl(3)-containing donor conductance decreased instantaneously. FeCl(3) concentrations of <6.6 x 10(-)(4) M had no effect on conductance, but concentrations at or above this threshold decreased conductance. FeCl(3) lowered water conductance at a receiver pH of 4.8, but not at pH < or =2.6. The effect of FeCl(3) on conductance was largest in cv. Namare and smallest in cv. Adriana. There was no significant effect of FeCl(3) on conductance for transpiration. Formation of aluminum and iron oxides and hydroxides in the exocarp as a result of a pH gradient between donor and receiver solution is discussed as the potential mechanism for Fe(3+) and Al(3+) reducing conductance for water uptake.  相似文献   

16.
Measurements of the singlet oxygen ((1)O(2)) quenching rates (k(Q) (S)) and the relative singlet oxygen absortpion capacity (SOAC) values were performed for 16 phenolic antioxidants (tocopherol derivatives, ubiquinol-10, caffeic acids, and catechins) and vitamin C in ethanol/chloroform/D(2)O (50:50:1, v/v/v) solution at 35 °C. It has been clarified that the SOAC method is useful to evaluate the (1)O(2)-quenching activity of lipophilic and hydrophilic antioxidants having 5 orders of magnitude different rate constants from 1.38 × 10(10) M(-1) s(-1) for lycopene to 2.71 × 10(5) for ferulic acid. The logarithms of the k(Q) (S) and the SOAC values for phenolic antioxidants were found to correlate well with their peak oxidation potentials (E(p)); the antioxidants that have smaller E(p) values show higher reactivities. In previous works, measurements of the k(Q) (S) values for many phenolic antioxidants were performed in ethanol. Consequently, measurements of the k(Q) (S) and relative SOAC values were performed for eight carotenoids in ethanol to investigate the effect of solvent on the (1)O(2)-quenching rate. The k(Q) (S) values for phenolic antioxidants and carotenoids in ethanol were found to correlate linearly with the k(Q) (S) values in ethanol/chloroform/D(2)O solution with a gradient of 1.79, except for two catechins. As the relative rate constants (k(Q)(AO) (S)/k(Q)(α-Toc) (S)) of antioxidants (AO) are equal to the relative SOAC values, the SOAC values do not depend on the kinds of solvent used, if α-tocopherol is used as a standard compound. In fact, the SOAC values obtained for carotenoids in mixed solvent agreed well with the corresponding ones in ethanol.  相似文献   

17.
Sorption of ionizable compounds of pyridines and aromatic carboxylic acids into low-density polyethylene (LDPE) film was investigated as a function of pH ranging from 4 to 7. The sorptions for pyridines were increased with increasing pH. Within the range examined, pH 7 was observed to promote the highest degree of sorption. When the pH increased by one unit from 6 to 7, the sorptions for 2-propylpyridine and 2,4,6-trimethylpyridine were both increased approximately 3.8 and 10.5 times, respectively. At pH 4, the sorption for the pyridines entirely disappeared. In contrast, the sorptions for aromatic carboxylic acids increased with decreasing pH. Within the range examined, pH 4 was observed to promote the highest degree of sorption. The magnitude of sorption for pyridines and carboxylic acids apparently depended on the affinity (delta(c)) of these compounds for LDPE film. Another factor affecting the sorption at various pHs was the pK(a) of these compounds; the sorption greatly decreased with the ionization degree of these compounds. To elucidate the phenomena, the following thermodynamic sorption equation was applied: S = S(0)gamma exp[V(v){(delta(w) - delta(v))(2) - delta(c)(2))/RT}. The plots of ln S for pyridines vs the term of the equation gave an insufficient relationship (r = 0.519). In contrast, taking into account the ratio (chi(i)()) of concentration of un-ionized compound to total concentration, the improvement for the equation was made: S' = S/chi(i)() = S(0)gamma exp[V(v){(delta(w) - delta(v))(2) - delta(c)(2))/RT}. The plots of ln S' vs the term of the equation gave a better relationship (r = 0.884). Furthermore, the equation was also applicable for the sorption behavior of carboxylic acids into LDPE (r = 0.769).  相似文献   

18.
Two kinds of Schiff base metal complexes of 2-hydroxy-1-naphthaldehyde-2-amino-5-phenylthiazole (HANPTS), Mn(II)(HNAPTS)(2) and Fe(III)(HNAPTS)(2), were synthesized and used to mimic the active group of horseradish peroxidase (HRP). The catalytic characteristics of the mimic enzymes in the oxidation reaction of ascorbic acid (AsA) with the OOH group in polyethylene glycols (PEGs) have been studied by a spectrophotometric method. Fe(III) has remarkable coordinated catalysis to Mn(II)(HNAPTS)(2); as a result, the catalytic ability of Fe(III)-Mn(II)(HNAPTS)(2) is 75% of that of HRP. The possible mechanism of the reaction was discussed. The linear relationship between deltaA(265)(AsA) and OOH group concentrations was in the range of 1.5 x 10(-6) to 9.0 x 10(-4) mol/L. The proposed method was successfully applied to the determination of the OOH group level in different molecular weight PEGs.  相似文献   

19.
Disposition kinetic behavior and metabolism studies of metamitron and its metabolite in terms of the parent compound were carried out in black Bengal goats after a single oral administration of a nontoxic oral dose at 30 mg kg(-1) of body weight. Metamitron was detected in the blood sample at 5 min (2.23 +/- 0.04 microg mL(-1)), maximum at 1 h (3.43 +/- 0.02 microg mL(-1)) and minimum at 12 h (0.41 +/- 0.01 microg mL(-1)), after a single oral administration. Metabolite [3-methyl-6-phenyl-1,2,4-triazin-5(4H)-one] in terms of the parent compound was detected in the blood sample at 5 min (0.47 +/- 0.006 microg mL(-1)), maximum at 6 h (5.12 +/- 0.02 microg mL(-1)) and minimum at 96 h (1.06 +/- 0.016 microg mL(-1)), after a single oral administration. The t(1/2 K) and Cl(B) values of metamitron were 3.63 +/- 0.05 h and 1.36 +/- 0.016 L kg(-1) h(-1), respectively, whereas the t(1/2K)(m) and Cl(B)(m) values of the metabolite were 38.15 +/- 0.37 h and 0.091 +/- 0.001 L kg(-1) h(-1), respectively, which suggested long persistence of the metabolite in blood and tissues of goat. Metamitron was excreted through feces and urine for up to 48 and 72 h, whereas the metabolite was excreted for up to 168 and 144 h, respectively. Metabolite alone contributed to 96 and 67% of combined recovery percentage of metamitron and metabolite against the administered dose in feces and urine of goat, respectively. All of the goat tissues except lung, adrenal gland, ovary, testis, and mammary gland retained the metabolite residue for up to 6 days after administration.  相似文献   

20.
O-[1-Ethyl-2-(3-trifluoromethylphenoxy)]ethyl-N-benzylcarbamate exhibits a marked inhibition of carotenoid biosynthesis. Forty-one analogues were synthesized and assayed for plant-type phytoene desaturase (PDS) and zeta-carotene desaturase (ZDS) inhibition in a cell-free system using recombinant enzymes obtained from Escherichia coli transformants. The target enzyme of all carbamates synthesized in this study is PDS and not ZDS; no inhibition of ZDS was observed using a 10(-4) M inhibitor concentration. Four compounds, O-[1-ethyl-2-(3-trifluoromethylphenoxy)]ethyl-N-(2-phenylethyl)carbamate (23), O-[1-ethyl-2-(3-trifluoromethylphenoxy)]ethyl-N-(2-chlorobenzyl)carbamate (25), O-[1-ethyl-2-(3-trifluoromethylphenoxy)]ethyl-N-(2-chlorobenzyl)carbamate (26), and O-[1-methyl-2-(3-trifluoromethylphenoxy)]ethyl-N-benzylcarbamate (30), were the most potent PDS inhibitors. Their pI(50) values, the negative logarithms of the molar concentration that produces a 50% inhibition, were 7.5, representing the same inhibitory activity as norflurazon. With respect to a structure-activity relationship the oxygen atom of the phenoxy group and a carbamate structure in O-(1-ethyl-2-phenoxy)ethyl-N-aralkylcarbamates studied were found to be essential for strong PDS inhibitors. Also, introduction of an ethyl group at the alpha-position of the ethylene bridge between the phenoxy group and the carbamate was important for a strong PDS inhibitor. Substituents at the 2- and/or 3-position of the phenoxybenzene ring were found to be favorable to a strong PDS inhibition of the analogues.  相似文献   

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