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1.
Toxicokinetic behavior and metabolism studies of metamitron and its effect on the cytochrome P(450) content of liver microsomal pellet were carried out in black Bengal goats after a single oral administration at 278 mg kg(-1) and consecutive oral administration of 30 mg kg(-1) for 7 days. Metamitron was detected in the blood sample at 0.08 h (12.0 +/- 0.87 microg mL(-1)), maximum at 4 h (84.3 +/- 8.60 microg mL(-1)) and minimum (14.6 +/- 1.67 microg mL(-1)) at 36 h blood sample after a single oral administration. The absorption rate constant was 0.69 +/- 0.09 h(-1). The Vd(area) (2.00 +/- 0.08 L kg(-1)) and t(1/2)beta (8.98 +/- 0.70 h) values suggested wide distribution and long persistence of the compound in the body. The values of T approximately B (0.80 +/- 0.04), F(c) (0.55 +/- 0.01), Cl(B) (0.15 +/- 0.00 L kg(-1) h(-1)), and K(21) (0.41 +/- 0.03 h(-1)) suggested that metamitron retained in the blood compared to that in the tissue. Maximum concentration of metamitron residue was found in the adrenal gland followed by bile on day 4 of single oral administration. The higher Cl(R) compared to Cl(H) value indicated the excretion of the major portion (34-40%) through urine compared to feces (20-26%). Maximum concentrations of metamitron and its metabolite, deaminometamitron, were excreted through urine and feces at 48 and 24 h samples, respectively. The recovery of metamitron including its metabolite in terms of parent compound varied from 69.3 to 80.1%, of which contribution of metabolite in terms of parent compound varied from 53.1 to 63.0%. Repeated oral administration of metamitron at 30 mg kg(-1) for 7 days caused induction of the cytochrome P(450) content of liver microsomal pellet of goat, suggesting oxidative deamination of metamitron.  相似文献   

2.
Toxicokinetic behavior, recovery, and metabolism studies of ACTP ester and its effect on cytochrome P(450) content of liver microsomal pellet were carried out in black Bengal goat after a single intravenous administration of 11.88 mg kg(-1) and consecutive oral administration of 79.22 mg kg(-1) for 7 days. ACTP ester achieved a maximum blood concentration of 42.64 +/- 4.26 microg mL(-1) at 0.08 h after intravenous administration followed by a sharp decline until 0.5 h, and the minimum blood concentration was recorded at 36 h (1.93 +/- 0.14 microg mL(-1)) postdosing. The kinetic behavior of ACTP ester followed a "two-compartment open model". Comparatively shorter alpha (0.81 +/- 0.02 h(-1)) and greater t1/2 (alpha) (0.86 +/- 0.03 h) indicated a slower rate of distribution of ACTP ester in goat. The t1/2(beta)()) (14.83 +/- 1.49 h) and V(d(area)) (0.91 +/- 0.19 L kg(-1)) suggested a longer elimination phase with general distribution in all compartments of the body. The higher T/B and K12/K21 values associated with a lower f(c) value suggested longer persistence in the tissue compartment at higher concentration. The higher Cl(R) compared to Cl(H) indicated the major amount was eliminated by the kidney. Maximum concentration of ACTP ester including its metabolites, triclopyr acid and trichloropyridinol, was excreted through urine at 48 h. The recovery of ACTP ester including metabolites after repeated nontoxic oral dose administration was 70.09%, of which recovery from feces was 4.45%, suggesting the major portion of administered ACTP ester was absorbed through the gastrointestinal tract of the goat. All of the tissues contained ACTP ester and its metabolites. ACTP ester did not alter the cytochrome P(450) content of the liver tissue following repeated nontoxic oral dose administration for 7 days.  相似文献   

3.
Cycloalliin, an organosulfur compound found in garlic and onion, has been reported to exert several biological activities and also to remain stable during storage and processing. In this study, we investigated the pharmacokinetics of cycloalliin in rats after intravenous or oral administration. Cycloalliin and its metabolite, (3R,5S)-5-methyl-1,4-thiazane-3-carboxylic acid, in plasma, urine, feces, and organs was determined by a validated liquid chromatography-mass spectrometry method. When administered intravenously at 50 mg/kg, cycloalliin was rapidly eliminated from blood and excreted into urine, and its total recovery in urine was 97.8% +/- 1.3% in 48 h. After oral administration, cycloalliin appeared rapidly in plasma, with a tmax of 0.47 +/- 0.03 h at 25 mg/kg and 0.67 +/- 0.14 h at 50 mg/kg. Orally administered cycloalliin was distributed in heart, lung, liver, spleen, and especially kidney. The Cmax and AUC0-inf values of cycloalliin at 50 mg/kg were approximately 5 times those at 25 mg/kg. When administered orally at 50 mg/kg, cycloalliin was excreted into urine (17.6% +/- 4.2%) but not feces. However, the total fecal excretion of (3R,5S)-5-methyl-1,4-thiazane-3-carboxylic acid was 67.3% +/- 5.9% (value corrected for cycloalliin equivalents). In addition, no (3R,5S)-5-methyl-1,4-thiazane-3-carboxylic acid was detected in plasma (<0.1 microg/mL), and negligible amounts (1.0% +/- 0.3%) were excreted into urine. In in vitro experiments, cycloalliin was reduced to (3R,5S)-5-methyl-1,4-thiazane-3-carboxylic acid during anaerobic incubation with cecal contents of rats. These data indicated that the low bioavailability (3.73% and 9.65% at 25 and 50 mg/kg, respectively) of cycloalliin was due mainly to reduction to (3R,5S)-5-methyl-1,4-thiazane-3-carboxylic acid by the intestinal flora and also poor absorption in the upper gastrointestinal tract. These findings are helpful for understanding the biological effects of cycloalliin.  相似文献   

4.
[Phenyl(U)-(14)C] and [triazole(3)-(14)C]flusilazole ([(bis 4-fluorophenyl)]methyl(1H-1,2,4-triazole-1-ylmethyl)silane; I) were extensively metabolized when fed to lactating goats (Capra hircus). The primary metabolites identified in goat tissues and milk were bis(4-fluorophenyl)(methyl)silanol (II) and 1H-1,2,4-triazole (III). Concentrations of total radiolabeled residues in the milk ranged from 0.09 to 0.74 microg/mL. Concentrations of radiolabeled residues found in tissues when the [(14)C] label was in the phenyl or triazole position, respectively, were 13.5 and 3.54 microg/g (liver), 8.74 and 0.75 microg/g (kidney), 0.41 and 0.52 microg/g (leg muscle), and 4.07 and 0.94 microg/g (back fat). Urine contained an additional major metabolite identified as [bis(4-fluorophenyl)](methyl)silylmethanol (IV) and its glucuronic acid conjugate (V). With either labeled form of flusilazole, the majority of the recovered radiolabel was excreted in urine or feces.  相似文献   

5.
Chickens were used to investigate plasma disposition of florfenicol after single intravenous (i.v.) and oral dose (20 mg kg-1 body weight) and to study residue depletion of florfenicol and its major metabolite florfenicol-amine after multiple oral doses (40 mg kg-1 body weight, daily for 3 days). Plasma and tissue samples were analyzed using a high-performance liquid chromatography (HPLC) method. After i.v. and oral administration, plasma concentration-time curves were best described by a two-compartment open model. The mean [ +/- standard deviation (SD)] elimination half-life (t1/2beta) of florfenicol in plasma was 7.90 +/- 0.48 and 8.34 +/- 0.64 h after i.v. and oral administration, respectively. The maximum plasma concentration was 10.23 +/- 1.67 microg mL-1, and the interval from oral administration until maximal concentration was 0.63 +/- 0.07 h. Oral bioavailability was found to be 87 +/- 16%. Florfenicol was converted to florfenicol-amine. After multiple oral dose (40 mg kg-1 body weight, daily for 3 days), in kidney and liver, concentrations of florfenicol (119.34 +/- 31.81 and 817.34 +/- 91.65 microg kg-1, respectively) and florfenicol-amine (60.67 +/- 13.05 and 48.50 +/- 13.07 microg kg-1, respectively) persisted for 7 days. The prolonged presence of residues of florfenicol and florfenicol-amine in edible tissues can play an important role in human food safety, because the compounds could give rise to a possible health risk. A withdrawal time of 6 days was necessary to ensure that the residues of florfenicol were less than the maximal residue limits or tolerance established by the European Union.  相似文献   

6.
Toxicokinetic behavior, recovery and metabolism of napropamide (a pre-emergent herbicide) and its effect on Cytochrome P(450) of liver microsomal pellet were studied following a single high-dose oral administration of 2.5 g kg(-1) and continuous (7 days) oral administration of 500 mg kg(-1) in black Bengal goat. Napropamide was detected in blood at 15 min and the maximum quantity was recovered at 3 h after administration. The absorption rate constant (Ka) value was low indicating poor absorption from the gastrointestinal tract. High elimination half-life (t(1/2) beta) and low body clearance (Cl(B)) values coupled with higher transfer of compound from tissue to central compartment (K(21)) suggest that napropamide persisted in the blood for a long time, i.e., after 72 h of oral administration. The recovery percentage of napropamide, including metabolites, from goats varied from 75.94 to 80.08 and excretion of the parent compound through feces varied from 18.86 to 21.59%, indicating that a major portion of the orally administered napropamide was absorbed from the gastrointestinal tract of goat. Napropamide significantly increased the Cytochrome P(450) content of liver microsomal pellet. The recovery of metabolites from feces, urine, and tissues ranged from 4.2--6.2, 40.81--49.42, and 2.7--11.6%, respectively, during a 4--7 day period. The material balance of napropamide (including metabolites) following a single high-dose oral administration at 2.5 g kg(-1) during 4--7 days after dosing was found to be in the range of 75--80%.  相似文献   

7.
The leaves and fine stems, bark, and trunk wood oils of Aniba canelilla showed yields ranging from 0.2 to 1.3%. The main volatile constituent identified in the oils was 1-nitro -2-phenylethane (70.2-92.1%), as expected. The mean of DPPH radical scavenging activity (EC 50) of the oils (198.17 +/- 1.95 microg mL(-1)) was low in comparison with that of wood methanol extracts (4.41 +/- 0.12 microg mL(-1)), the value of which was equivalent to that of Trolox (4.67 +/- 0.35 microg mL(-1)), used as antioxidant standard. The mean amount of total phenolics (TP) (710.53 +/- 23.16 mg of GAE/g) and this value calculated as Trolox equivalent antioxidant capacity (TEAC) (899.50 +/- 6.50 mg of TE/g) of the wood methanol extracts confirmed the high antioxidant activity of the species. On the other hand, in the brine shrimp bioassay the values of lethal concentration (LC50) for the oils (21.61 +/- 1.21 microg mL(-1)) and 1-nitro-2-phenylethane (20.37 +/- 0.99 microg mL(-1)) were lower than that of the wood methanol extracts (91.38 +/- 7.20 microg mL(-1)), showing significant biological activities.  相似文献   

8.
The present study provides evidence for the involvement of protein in cloud instability of natural orange juice. No heat-coagulable proteins were found in the serum. Insoluble cloud matter (ICM) was heat-flocculated following enzymatic pectin degradation (EPD). The degree of flocculation depended on temperature (from approximately 50 to 75 degrees C) and was highest at pH 3.5. The fresh juice contained about 6.5 and 1.8 mg mL(-1) of ICM and alcohol-insoluble solids of the serum (AISS), respectively. The ICM and the AISS contained, respectively, proteins (182+/-14 and 119+/-3 microg mg(-1)), galacturonic acid (37+/-6.6 and 175+/-1 microg mg(-1)), and neutral sugars (350+/-44 and 338+/-22 microg mg(-1)). EPD resulted in removal of a marked portion of the pectin and was accompanied by partial removal of neutral sugars (mainly glucose and galactose) and some proteins from the pectic polymer in both AISS and ICM. Under electrophoresis, proteins of the AISS included bands in the range of 20-52 kDa and 10-14 kDa and those of the ICM at 22 and 50 kDa.  相似文献   

9.
The sorption efficiency of indigenous rice (Oryza sativa) bran for the removal of organics, that is, benzene, toluene, ethylbenzene, and cumene (BTEC), from aqueous solutions has been studied. The sorption of BTEC by rice bran is observed over a wide pH range of 1-10, indicating its high applicability to remove these organics from various industrial effluents. Rice bran effectively adsorbs BTEC of 10 microg mL(-1) sorbate concentration from water at temperatures of 283-323 +/- 2 K. The effect of pH, agitation time between solid and liquid phases, sorbent dose, its particle size, and temperature on the sorption of BTEC onto rice bran has been studied. The pore area and average pore diameter of rice bran by BET method are found to be 19 +/- 0.7 m(2) g(-1) and 52.8 +/- 1.3 nm. The rice bran exhibits appreciable sorption of the order of 85 +/- 3.5, 91 +/- 1.8, 94 +/- 1.4, and 96 +/- 1.2% for 10 microg mL(-1) concentration of benzene, toluene, ethylbenzene, and cumene, respectively, in 60 min of agitation time using 0.1 g of rice bran at pH 6 and 303 K. The sorption data follow Freundlich, Langmuir, and Dubinin-Radushkevich (D-R) models. Sorption capacities have been computed for BTEC by Freundlich (32 +/- 3, 61 +/- 14, 123 +/- 28, and 142 +/- 37 m mol g(-1)), Langmuir (6.6 +/- 0.1, 7.5 +/- 0.13, 9.5 +/- 0.22, and 9.4 +/- 0.18 m mol g(-1)), and D-R isotherms (11 +/- 0.5, 16 +/- 1.3, 30 +/- 2.2, and 33 +/- 2.5 m mol g(-1)), respectively. The Lagergren equation is employed for the kinetics of the sorption of BTEC onto rice bran and first-order rate constants (0.03 +/- 0.002, 0.04 +/- 0.003, 0.04 +/- 0.003, and 0.05 +/- 0.004 min(-1)) have been computed for BTEC at their concentration of 100 mug mL(-1) at 303 K. Studies on the variation of sorption with temperatures (283-323 K) at 100 mug mL(-1) sorbate concentration gave thermodynamic constants DeltaH (kJ mol(-1)), DeltaG (kJ mol(-1)), and DeltaS (J mol(-1) K(-1)). The results indicate that the sorption of organics onto rice bran is exothermic and spontaneous in nature under the optimized experimental conditions selected. This sorbent has been used successfully to accumulate and then to determine benzene, toluene, and ethylbenzene in wastewater sample.  相似文献   

10.
Luteoin is one of the main flavones and the crucial effective component of peanut hull extract (PHE). The present paper aims to elucidate the absorption mechanism of luteolin and clarify whether its absorption occurs primarily at a specific site of the intestine by an in situ single-pass intestinal perfusion (SPIP) model. Moreover, the paper investigates the difference in absorption of luteolin when it is administered in PHE form and as pure luteolin by the SPIP model and in vivo pharmacokinetics studies. Results showed that the effective permeability ( P eff) and absorption rate constant ( k a) of pure luteolin(5.0 microg/mL) in duodenum and jejunum were not significantly different, but markedly higher than that in the colon and ileum. The P eff and k a of luteolin in jejunum were concentration-independent, and the ATP inhibitor (DNP) did not influence P eff and k a of pure luteolin. However, the P eff and k a of luteolin in PHE were significantly greater than that of pure luteolin. The pharmacokinetics study showed that following oral administration of a single dose of pure luteolin (14.3 mg/kg) or PHE (= 14.3 mg/kg of luteolin) in rats, the peak concentration of luteolin in plasma ( C max) and the area under the concentration curve (AUC) for pure luteolin were 1.97 +/- 0.15 microg/mL and 10.7 +/- 2.2 microg/mL.h, respectively. These parameters were significantly lower than those of the PHE group ( P < 0.05), C max = 8.34 +/- 0.98 microg/mL and AUC = 20.3 +/- 1.3 microg/mL.h, respectively. It can be concluded that luteolin is absorbed passively in the intestine of rats and that its absorption is more efficient in the jejunum and duodenum than in the colon and ileum. The bioavailability of luteolin in PHE form is significantly greater than that of pure luteolin.  相似文献   

11.
After oral administration of [4-(3)H]EGCg to rats, the radioactivity in blood, major tissues, urine, and feces was measured over time. The radioactivity in blood and most tissues remained low for 4 h postdose, began to increase after 8 h, peaked at 24 h, and then decreased. Major urinary excretion of radioactivity occurred in the 8-24 h period, and the cumulative radioactivity excreted by 72 h was 32.1% of the dose. The radioactivity in the feces was 35.2% of the dose within 72 h postdose. In the case of rats pretreated with antibiotics (antibiotic-pretreated rats), the radioactivity levels of the blood and urine were definitely lower than those in rats not pretreated with antibiotics (normal rats). The radioactivity recovered in the antibiotic-pretreated rat urine was estimated to be only (1)/(100) of that in the normal rat urine. These results clearly demonstrated that the radioactivity detected in the blood and urine of normal rats mostly originated from degradation products of EGCg produced by intestinal bacteria. Furthermore, a main metabolite in the normal rats was purified and identified as 5-(5'-hydroxyphenyl)-gamma-valerolactone 3'-O-beta-glucuronide (M-2). In feces of the normal rats, EGC (40.8% of the fecal radioactivity) and 5-(3',5'-dihydroxyphenyl)-gamma-valerolactone (M-1, 16.8%) were detected. These results suggested that M-1 was absorbed in the body after degradation of EGCg by intestinal bacteria, yielding M-1 with EGC as an intermediate. Furthermore, M-2 was thought to be formed from M-1 in the intestinal mucosa and/or liver, then to enter the systemic circulation, and finally to be excreted in the urine. Taking into account all of the above findings, a possible metabolic route of EGCg orally administered to rats is proposed.  相似文献   

12.
Methylsulfonylmethane (MSM) is a sulfur-containing compound found in a wide range of human foods including fruits, vegetables, grains, and beverages. More recently, it has been marketed as a dietary supplement worldwide. The objective of this study was to evaluate the pharmacokinetic profile and distribution of radiolabeled MSM in rats. Male Sprague-Dawley rats were administered a single oral dose of [35S]MSM (500 mg/kg), and blood levels of radioactivity were determined at different time points for up to 48 h. Tissue levels of radioactivity at 48 and 120 h and urine and fecal radioactivity levels were measured at different time points for up to 120 h following [35S]MSM administration to rats. Oral [35S]MSM was rapidly and efficiently absorbed with a mean tmax of 2.1 h, Cmax of 622 microg equiv/mL, and AUC0-inf of 15124 h.microg equiv/mL. The t1/2 was 12.2 h. Soft tissue distribution of radioactivity indicated a fairly homogeneous distribution throughout the body with relatively lower concentrations in skin and bone. Approximately 85.8% of the dose was recovered in the urine after 120 h, whereas only 3% was found in the feces. No quantifiable levels of radioactivity were found in any tissues after 120 h, indicating complete elimination of [35S]MSM. The results of this study suggest that [35S]MSM is rapidly absorbed, well distributed, and completely excreted from the body.  相似文献   

13.
Genistein (4',5,7-trihydroxyisoflavone), a naturally occurring phenolic compound, possesses well-known preventive activity in breast and prostate cancer, cardiovascular diseases, and postmenopausal problems. The aim of this study is to investigate the distribution and dose-dependent absorption, metabolism, and excretion of genistein in rats. Genistein was orally administered to rats at different doses. At various time intervals, blood, bile, and urine samples were collected and incubated with glucuronidase to hydrolyze the glucuronidated genistein. Genistein was detected by HPLC. High levels of glucuronidated genistein were detected in the plasma, bile, and urine after genistein administration. When genistein was administered to rats at 6.25, 12.5, and 50 mg x kg (-1) doses, the AUC (0- t) values for genistein were 23.5, 80.9, and 177.9 mg x min x L (-1); the oral absolute bioavailabilities were 21.9, 33.5, and 19.0%; the AUC (0- t) values of glucuronidated genistein were 173.8, 470.7, and 1721.2 mg x min x L (-1), respectively. The cumulative biliary excretion of genistein respective to each dose was 42.6 +/- 6.5, 75.2 +/- 18.9, and 126.6 +/- 34.8 microg; the cumulative biliary excretion of glucuronidated genistein was 108.5 +/- 35.2, 423.5 +/- 158.3, and 853.7 +/- 320.8 microg for each dose, respectively. The cumulative urinary excretion of genistein was 34.8 +/- 10.8, 187.3 +/- 67.0 and 213.6 +/- 30.6 microg for each dose, respectively; the cumulative levels of glucuronidated genistein excreted in the urine were 217.8 +/- 52.1, 583.1 +/- 106.9, and 1108.4 +/- 88.1 microg, respectively. These results indicated that at high doses absorption, biotransformation, and excretion of genistein occurred in a nonlinear dose-dependent manner. Therefore, the results of these pharmacokinetic studies raise important questions about the therapeutic significance of consuming large quantities of genistein, genistein analogues, or soy-based neutraceuticals.  相似文献   

14.
Many reports have described the bioavailability of anthocyanins; however, most of these reports investigated only the amount of anthocyanins excreted in urine. In the present study, we calculated the pharmacokinetic bioavailability of anthocyanins in rats by measuring the plasma concentration of delphinidin-3-rutinoside that had been administered orally or intravenously. Delphinidin-3-rutinoside was primarily absorbed in the blood and excreted into urine as unmetabolized forms with a T(max) of 26.3 min and a C(max) of 0.285 +/- 0.071 micromol/L. We detected small amounts of the metabolite 4'-O-methyl-delphinidin-3-rutinoside in the plasma, but we detected neither anthocyanidin (aglycone) nor glucuro- or sulfoconjugates. For the 8 h period after intake, delphinidin-3-rutinoside and 4'-O-methyl-delphinidin-3-rutinoside were excreted to urine at 795 +/- 375 and 12.3 +/- 2.91 nmol, respectively. Relative to intravenous injection, oral administration of delphinidin-3-rutinoside resulted in complete bioavailability (0.49 +/- 0.06%). Analysis of delphinidin-3-rutinoside plasma concentrations in bile cannulated rats revealed that, for the 8-h period after intake, the intact delphinidin-3-rutinoside excretion ratio in bile was 11% of the excretion ratio of 4'-O-methyl-delphinidin-3-rutinoside, 1.91 +/- 0.35 nmol versus 17.4 +/- 8.67 nmol, respectively. Setting the bile duct cannulation in a Bollman-type cage, however, significantly increased the bioavailability of orally administered delphinidin-3-rutinoside (18.14 +/- 6.24%). This effect appears to stem immobilization stress by reducing gastrointestinal motility. The cumulative excretion of delphinidin-3-rutinoside and 4'-O-methyl-delphinidin-3-rutinoside in urine and bile was 2.67 +/- 1.24% (w/w) of the dose ingested. Studies report that several metabolites are formed after oral ingestion of anthocyanins. Examples include glucuronyl from cyanidin-3-glucoside and both glucuronyl and sulfate conjugates from pelargonidin-3-glucoside. Our results indicate that delphinidin-3-rutinoside might be metabolized differently from cyanidin-3-glucoside and pelargonidin-3-glucoside.  相似文献   

15.
The metabolic pattern of the imidazole fungicide prochloraz [N-propyl-N-[2-(2,4,6-trichlorophenoxy)ethyl]imidazole-1-carboximide] was investigated in rainbow trout (Oncorhynchus mykiss). Following a single oral administration of [(14)C]prochloraz, levels 4.3 +/- 4.1 and 3.9 +/- 1.8% of the dose were excreted in the bile after 48 h in male and female animals, respectively. Urinary radioactivity accounted for 1.3 +/- 0.4 and 2.4 +/- 1.1% of the dose over the same period in males and females. Metabolites from both matrices were separated by reversed-phase HPLC with radioactive detection and analyzed by positive and/or negative electrospray ionization mass spectrometry. No unchanged prochloraz was detected in the analyzed excreta. The major biotransformation products in bile were the aldehyde corresponding to the cleavage of the imidazole ring, N-2-(2,4,6-trichlorophenoxy)ethylurea, and the glucuronide conjugate of 2,4,6-trichlorophenoxyethanol. In urine, the major metabolite was 2,4,6-trichlorophenoxyacetic acid. On the basis of enzymatic hydrolysis by beta-glucuronidase and LC-MS analyses, this study demonstrates that rainbow trout are able to biotransform prochloraz, mainly as glucuronide conjugates.  相似文献   

16.
Metamitron (1) does not undergo hydrolysis at pH 1-8 and up to 5 M H(2)SO(4). The product of its two-electron reduction, 1, 6-dihydrometamitron (2), on the other hand, undergoes at pH <3 relatively fast hydrolysis. The dependence of the measured rate constant on acidity indicates that the completely protonated form (AH(2)(2+)) predominating in strongly acidic media undergoes hydrolysis slower than the species bearing one less proton (AH(+)). The latter most reactive species is present in highest concentration in solutions of pH between 0 and 2. This species is protonated on the 2,3-azomethine bond and yields as final products 2-hydrazino-2-phenylacetic acid (4) and acethydrazide (5). Kinetic, polarographic, and spectrophotometric measurements indicated for the first dissociation an average value pK(a) = -0.8, for the second pK(a) = 0.95. These observations together with the easy reduction of the 1,6-bond in metamitron (1) indicate that in nature the cleavage of metamitron may be preceded by its reduction to 1, 6-dihydrometamitron (2), which is then hydrolyzed. Thus, anaerobic, reductive conditions are likely preferable for the total microbial degradation of metamitron.  相似文献   

17.
The present study examined the involvement of proteins in cloud flocculation of Valencia orange juice. Marked differences in cloud instability were found between juices of different harvest dates. Heating of enzymatic pectin degraded juice from April and June harvests resulted in development of clumps and their precipitation. Although the juice from both harvesting dates remained hazy, the juice of April harvest was more turbid than that from June. Usually clarification increases as the temperature increases from ambient to 125 degrees C. Clarification occurred at pH 2.5-4.5 and was maximal at pH 3.5. The clarification of the April harvest juice was markedly lower than that of the June harvest. The fresh juice contained about 5.2 and 1.7 mg mL(-1) insoluble cloud matter (ICM) and alcohol-insoluble serum solids (AISS), respectively. The ICM and the AISS, respectively, contained: proteins (244.5+/-8.7 and 132+/-1.8 microg mg(-1)), galacturonic acid (40+/-0 and 120+/-0 microg mg(-1)) and neutral sugars (270+/-39 and 329+/-23 microg mg(-1)). Enzymatic pectin degradation resulted in removal of a marked portion of the pectin, and was accompanied by partial removal of neutral sugars (mainly glucose and galactose) and some proteins from the pectic polymer in both AISS and ICM. Proteins of the AISS included major bands at 10-14, 20, and 28 kDa and those of the ICM bands at 22, 24, 26, and 45 kDa.  相似文献   

18.
Chrysanthemum morifolium extract (CME) has the protective effect on cardiovascular diseases. Luteolin and apigenin are two major bioactive components in vivo when CME is orally administrated to experimental animal. The present paper shows the study of the absorption and excretion of luteolin and apigenin in rats after a single oral dose of CME (200 mg/kg). The levels of luteolin and apigenin in plasma, urine, feces, and bile were measured by HPLC after deconjugation with hydrochloric acid or beta-glucuronidase/sulfatase. The results showed that the plasma concentrations of luteolin and apigenin reached the highest peak level at 1.1 and 3.9 h after dosing, respectively. The area under the concentration-time curves (AUC) for luteolin and apigenin were 23.03 and 237.6 microg h mL-1, respectively. The total recovery of the dose was 37.9% (6.6% in urine; 31.3% in feces) for luteolin and 45.2% (16.6% in urine; 28.6% in feces) for apigenin. The cumulative luteolin and apigenin excreted in the bile was 2.05% and 6.34% of the dose, respectively. All of the results suggest apigenin may be absorbed more efficiently than luteolin in CME in rats, and both luteolin and apigenin have a slow elimination phase, with a quick absorption, so a possible accumulation of the two flavonoids in the body can be hypothesized.  相似文献   

19.
Antihypertensive properties of spinach leaf protein digests   总被引：5，自引：0，他引：5  
Leaf protein containing approximately 50% rubisco (ribulose bisphosphate carboxylase/oxygenase) was obtained from fresh spinach leaf with the use of a simple extraction method. Pepsin and pepsin-pancreatin digests of spinach leaf protein have potent angiotensin-I converting enzyme inhibitory properties with IC(50) values of 56 and 120 microg/mL, respectively. Both digests of leaf protein have antihypertensive effects after oral administration to spontaneously hypertensive rats (SHR) with minimum effective doses of 0.25 and 0.5 g/kg, respectively. The maximum antihypertensive effect for the pepsin digest was observed 4 h after oral administration, while for the pepsin-pancreatin digest, the maximum effect was observed 2 h after oral administration. Undigested spinach leaf protein did not exert any significant antihypertensive effect after oral administration to SHR at doses of 0.5 and 1 g/kg. Obtained results show that the pepsin digest of leaf protein may be useful in treatment of hypertension.  相似文献   

20.
Two lactating goats were given a daily oral dose of either [UL-aniline-(14)C; AN] or [triazolopyrimidine-7,9-(14)C; TP]cloransulam-methyl for 5 consecutive days. Each animal received a dietary equivalent of approximately 10 mg/kg of test material, approximately 2225 times the realistic maximum dietary exposure for a dairy animal. Milk, urine, and feces samples were collected in the morning and afternoon for each animal. Each goat was sacrificed within 23 h of receiving the last dose, and the liver, kidneys, samples of blood, fat, muscle, and gastrointestinal tract contents, and urine from the bladder were collected. All of these samples were analyzed for (14)C content. Cloransulam-methyl (CM) was rapidly excreted by the animals, with 99.9% of the recovered radioactivity appearing in the urine and feces. Radiochemical analysis showed very low residues, with the highest being in the kidneys at 0.122 and 0. 128 mg equiv of CM/kg (AN and TP labeled compounds, respectively). Radioactive residues were extracted and fractionated from kidney, liver, and milk. Analysis showed approximately 0.066 mg/kg CM in the kidney but <0.003 mg/kg in the liver. Only one metabolite, cloransulam, was identified (in liver, 9.5% of total radioactive residue; 0.005 mg/kg). All other metabolites were present at lower levels. Sulfonanilide bridge cleavage was not a significant degradation route for cloransulam-methyl in ruminants. These data indicated a very low bioaccumulation potential for cloransulam-methyl and its metabolites in ruminants. For a ruminant exposed to anticipated levels of cloransulam-methyl in its diet, parent and metabolites, in total, would not be expected to exceed 50 ng/kg in the kidney and liver.  相似文献   

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