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1.
In the present study, we investigated time course changes of water status including relative water content (RWC), leaf osmotic potential (ΨΠ), stomatal conductance (gs), proline (Pro), chlorophyll fluorescence (Fv/Fm) and total chlorophyll content in the Arabidopsis thaliana under PEG-induced drought stress after exogenous ABA treatment. To a better explanation for the role of ABA in the water status of A. thaliana to drought stress, wild-type (Columbia) and ABA-deficient mutant (aba2) of A. thaliana were used in the present study. Moreover, three weeks old Arabidopsis seedlings were applied exogenously with 50 μM ABA and exposed to drought stress induced by 40% PEG8000 (−0.73 MPa) for 6 h, 12 h and 24 h (hours). Our findings indicate that RWC of wild-type and aba2 started to decrease in the first 12 h and 6 h of PEG-induced drought stress, respectively. However, exogenous treatment of 50 μM ABA increased their RWC under drought stress. On the other hand, while ΨΠ of both genotypes started to decrease in the first 6 h of drought stress, these declines in ΨΠ were prevented by ABA treatment under stress throughout the experiment; it was more pronounced in aba2 at 24 h. While the highest increase in gs was obtained in aba2 after 24 h stress, ABA-induced highest decrease in gs was obtained in the same genotype during 12 h, as compared to PEG-treated group alone. On the other hand, Pro content increased in all treatment groups of ABA-deficient mutant aba2 at 12 h and 24 h. However, Pro content in ABA + PEG treated aba2 plants was higher than in PEG- and ABA-treated plants alone at the end of the 24 h. Drought stress decreased Fv/Fm and total chlorophyll contents of both genotypes while 50 μM ABA alleviated these reductions during drought stress, as compared to PEG stressed plants. On the other hand, 50 μM ABA treatment alone did not create any remarkable effect on Fv/Fm and total chlorophyll contents.These findings indicate that exogenous ABA showed an alleviative effect against damage of drought stress on relative water content, osmotic potential, stomatal conductance, proline, chlorophyll fluorescence and total chlorophyll content of both genotypes during 24 h of drought stress treatment.  相似文献   

2.
Phenolic content and antioxidant potential of lentil sprouts may be enhanced by treatment of seedlings in abiotic stress conditions without any negative influence on nutritional quality.The health-relevant and nutritional quality of sprouts was improved by elicitation of 2-day-old sprouts with oxidative, osmotic, ion-osmotic and temperature stresses. Among the sprouts studied, those obtained by elicitation with osmotic (600 mM mannitol) and ion-osmotic (300 mM NaCl) shocks had the highest total phenolic content levels: 6.52 and 6.56 mg/g flour, respectively. Oxidative stress significantly enhanced the levels of (+)-catechin and p-coumaric acid. A marked elevation of the chlorogenic and gallic acid contents was also determined for sprouts induced at 4 °C and 40 °C. The elevated phenolic content was translated into the antioxidant potential of sprouts, especially the ability to reduce lipid oxidation. A marked elevation of this ability was determined for seedlings treated with 20 mM, 200 mM H2O2 (oxidative stress) and 600 mM mannitol (osmotic stress); about a 12-fold, 8-fold and 9.5-fold increase in respect to control sprouts. The highest ability to quench free radicals was observed in sprouts induced by osmotic stress (IC50- 4.91 and 5.12 mg/ml for 200 mM and 600 mM mannitol, respectively). The highest total antioxidant activity indexes were determined for sprouts elicited with 20 mM H2O2 and 600 mM mannitol: 4.0 and 3.4, respectively. All studied growth conditions, except induction at 40 °C, caused a significant elevation of resistant starch levels which was also affected in a subsequent reduction of starch digestibility.Improvement of sprout quality by elicitation with abiotic stresses is a cheap and easy biotechnology and it seems to be an alternative to conventional techniques applied to improve the health promoting phytochemical levels and bioactivity of low-processed food.  相似文献   

3.
The combined effects of salt stress and gibberellic acid (GA3) on plant growth and nutritional status of maize (Zea mays L. cv., DK 647 F1) were studied in a pot experiment. Treatments were (1) control (C): nutrient solution alone, (2) salt stress (S): 100 mM NaCl, (3) S + GA1: 100 mM NaCl and 50 ppm GA3 and (4) S + GA2: 100 mM NaCl and 100 ppm GA3. Salt stress (S) was found to reduce the total dry matter, chlorophyll content, relative water content (RWC), but to increase proline accumulation, superoxide dismutase (SOD; EC 1.15.1.1), peroxidase (POD; EC 1.11.1.7) and polyphenol oxidase (PPO; 1.10.3.1) enzyme activities and electrolyte leakage. GA3 treatments overcame to variable extents the adverse effects of NaCl stress on the above physiological parameters. GA3 treatments reduced the activities of enzyme in the salt-stressed plants. Salt stress reduced some macro and micronutrient concentrations but exogenous application of GA3 increased these to levels of control treatment. Foliar application of GA3 counteracted some of the adverse effects of NaCl salinity with the accumulation of proline which maintained membrane permeability and increased macro and micronutrient levels.  相似文献   

4.
Obstructive sleep apnea (OSA) is characterized by recurrent apnea during sleep that may unbalance oxidative stress, increasing atherosclerosis. Among oxidative stress markers, 15-F2t-isoprostane is considered one of the most sensitive and specific metabolites of lipid peroxidation. To explore the relationship between urinary 15-F2t-isoprostane with sleep apnea severity and carotid modifications in nonobese OSA patients, 31 nonobese sleep apnea patients were studied, along with 10 lean subjects without OSA. Patients were assessed by polysomnography, blood pressure measurement, and ultrasonography to determine the carotid intima–media thickness (IMT). Urinary 15-F2t-isoprostanes were measured by liquid chromatography–tandem mass spectrometry. Urinary 15-F2t-isoprostane concentrations were increased in severe OSA patients compared to control subjects (20.2 ± 7.3 vs 12.3 ± 2.8 ng/mmol creatinine; P = 0.020). Mean carotid IMT was correlated with 15-F2t-isoprostane (r = 0.532; P < 0.001) and with the apnea–hypopnea index (r = 0.345; P = 0.029). 15-F2t-Isoprostane level was related to the night time spent at SaO2 < 90% (r = 0.478; P = 0.002), the apnea–hypopnea index (r = 0.465; P = 0.003), and the mean nocturnal SaO2 (r = ? 0.424; P = 0.007). These results showed a relationship between lipid peroxidation, carotid intima–media thickness, and intermittent hypoxia in nonobese OSA patients, thus reinforcing the hypothesis that oxidative stress could be involved in the early atherosclerotic process.  相似文献   

5.
In response to an osmotic stress, Dunaliella tertiolecta osmoregulates by metabolizing intracellular glycerol as compatible solute. Upon the application of a salt stress to 0.17 M or 0.7 M NaCl grown D. tertiolecta cells, rates of total glycerol synthesis were substantially higher than that arising from photosynthetic 14CO2 fixation into glycerol. The source of this extra carbon is the reserve starch pool. The contribution of carbon from the starch breakdown to glycerol synthesis was estimated from the difference between the total glycerol synthesized and that arising from 14CO2 fixation. The maximum observed flux of carbon from 14CO2 to glycerol from photosynthesis was of the order of 15–20 μmol 14C-glycerol mg−1 Chl h−1, whereas the total glycerol synthesis reached about 70 μmol glycerol mg−1 Chl h−1. The contribution of products of starch breakdown to glycerol synthesis increased progressively with increasing salt stress. In light, contrary to prevailing assumptions, both the photosynthesis and the starch breakdown contribute carbon to glycerol biosynthesis. The relative contributions of these two processes in the light, while cells were actively photosynthesizing, depended on the magnitude of the salt stress. On application of dilution stress, the flux of carbon from newly photosynthetically fixed 14CO2 into glycerol was reduced progressively with increasing dilution stress that was also accompanied by a decline in total glycerol contents of the cell. The maximum observed rate of glycerol dissimilation was about 135 μmol glycerol mg−1 Chl h−1.  相似文献   

6.
Optimization of intravascular shear stress assessment in vivo   总被引:1,自引:0,他引:1  
The advent of microelectromechanical systems (MEMS) sensors has enabled real-time wall shear stress (WSS) measurements with high spatial and temporal resolution in a 3-D bifurcation model. To optimize intravascular shear stress assessment, we evaluated the feasibility of catheter/coaxial wire-based MEMS sensors in the abdominal aorta of the New Zealand white (NZW) rabbits. Theoretical and computational fluid dynamics (CFD) analyses were performed. Fluoroscope and angiogram provided the geometry of aorta, and the Doppler ultrasound system provided the pulsatile flow velocity for the boundary conditions. The physical parameters governing the shear stress assessment in NZW rabbits included (1) the position and distance from which the MEMS sensors were mounted to the terminal end of coaxial wire or the entrance length, (Le), (2) diameter ratios of aorta to the coaxial wire (Daorta /Dcoaxial wire=1.5–9.5), and (3) the range of Reynolds numbers (116–1550). At an aortic diameter of 2.4 mm and a maximum Reynolds number of 212 (a mean Reynolds number of 64.2), the time-averaged shear stress (τave) was computed to be 10.06 dyn cm?2 with a systolic peak at 33.18 dyn cm?2. In the presence of a coaxial wire (Daorta /Dcoaxial wire=6 and Le=1.18 cm), the τave value increased to 15.54 dyn cm?2 with a systolic peak at 51.25 dyn cm?2. Real-time intravascular shear stress assessment by the MEMS sensor revealed an τave value of 11.92 dyn cm?2 with a systolic peak at 47.04 dyn cm?2. The difference between CFD and experimental τave was 18.5%. These findings provided important insights into packaging the MEMS sensors to optimize in vivo shear stress assessment.  相似文献   

7.
8.
Trace elements and oxidative stress are associated with glycemic control and diabetic complications in type 1 diabetes mellitus. In this study, we analyzed the levels of serum copper, zinc, superoxide dismutase (SOD) activity, and malondialdehyde (MDA) and urinary MDA and 8-hydroxy-2′-deoxyguanosine (8-OHdG) in 33 type 1 diabetic patients with optimal and suboptimal glycemic control (HbA1C < 9.0%) and 40 patients with poor glycemic control (HbA1C  9%) and 27 age- and sex-matched non-diabetic controls to evaluate the differences between these markers in different glycemic control states. Diabetic patients, especially poor-glycemic-control subjects (HbA1C  9%), exhibited significantly lower levels of serum zinc and increased levels of serum copper (and, therefore, increased serum copper-to-zinc ratios), serum SOD, blood MDA, and urinary MDA and 8-OHdG, relative to non-diabetic subjects. Furthermore, significant correlations existed in these patients between the serum copper, serum copper-to-zinc ratio, and urinary MDA (all p < 0.001) and the levels of urinary 8-OHdG (p = 0.007) and HbA1C. Our results suggest that high serum copper levels and oxidative stress correlate with glycemic control. Therefore, strict glycemic control, decreased oxidative stress, and a lower copper concentration might prevent diabetic complications in patients with type 1 diabetes mellitus.  相似文献   

9.
Several studies suggest that exercise is associated with elevated oxidative stress which diminishes NO bioavailability. The aim of the present study was to investigate a potential link between NO synthesis and bioavailability and oxidative stress in the circulation of subjects performing high-intensive endurance exercise. Twenty-two male healthy subjects cycled at 80% of their maximal workload. Cubital venous blood was taken before, during and after exercise, and heparinized plasma was generated. Plasma concentrations of nitrite and nitrate were quantified by GC–MS and of the oxidative stress biomarker 15(S)-8-iso-PGF by GC–MS/MS. pH and pCO2 fell and HbO2 increased upon exercise. The duration of the 80% phase (d80) was 740 ± 210 s. Subjects cycled at 89.2 ± 3.3% of their peak oxygen uptake. Plasma concentration of nitrite (P < 0.01) and 15(S)-8-iso-PGF (P < 0.05) decreased significantly during exercise. At the end of exercise, plasma nitrite concentration correlated positively with d80 and performed work (w80) (each P < 0.05). Changes in nitrate concentration also correlated positively with d80 (P < 0.05) and w80/kg (P < 0.01). These findings provide evidence of a favorable effect of nitrite on high-intensive endurance exercise. The lack of association between 15(S)-8-iso-PGF and NO bioavailability (nitrite concentration) and NO biosynthesis (nitrate concentration) suggest that oxidative stress, notably lipid peroxidation, is not linked to the l-arginine/NO pathway in healthy male subjects being on endurance exercise.  相似文献   

10.
A new generation of chroman/catechol hybrids bearing heterocyclic five-membered rings, such as 1,2,4-oxadiazole 1,3,4-oxadiazole, 1,2,3-triazole, tetrazole and isoxazole, were designed and synthesized. The activity of the new derivatives against oxidative stress induced neuronal damage, was evaluated using glutamate-challenged hippocampal HT22 cells.Compound 3 in which a 3,4-dimethoxyphenyl moiety, is directly attached to the 1,2,4-oxadiazole ring was the most active among the 2-substituted chroman analogues, with EC50 = 254 ± 65 nM. Concerning the 5-subtituted chroman analogues, isoxazole derivative 29 exhibited the strongest activity (EC50 = 245 ± 38 nM). However, 29 was cytotoxic at concentrations higher than 1 μM, while the triazole analogue 24 (EC50 = 801 ± 229 nM), was non-toxic at all concentrations tested.  相似文献   

11.
12.
Marine bivalves such as the hard shell clams Mercenaria mercenaria and eastern oysters Crassostrea virginica are affected by multiple stressors, including fluctuations in temperature and CO2 levels in estuaries, and these stresses are expected to be exacerbated by ongoing global climate change. Hypercapnia (elevated CO2 levels) and temperature stress can affect survival, growth and development of marine bivalves, but the cellular mechanisms of these effects are not yet fully understood. In this study, we investigated whether oxidative stress is implicated in cellular responses to elevated temperature and CO2 levels in marine bivalves. We measured the whole-organism standard metabolic rate (SMR), total antioxidant capacity (TAOC), and levels of oxidative stress biomarkers in the muscle tissues of clams and oysters exposed to different temperatures (22 and 27 °C) and CO2 levels (the present day conditions of ~ 400 ppm CO2 and 800 ppm CO2 predicted by a consensus business-as-usual IPCC emission scenario for the year 2100). SMR was significantly higher and the antioxidant capacity was lower in oysters than in clams. Aerobic metabolism was largely temperature-independent in these two species in the studied temperature range (22–27 °C). However, the combined exposure to elevated temperature and hypercapnia led to elevated SMR in clams indicating elevated costs of basal maintenance. No persistent oxidative stress signal (measured by the levels of protein carbonyls, and protein conjugates with malondialdehyde and 4-hydroxynonenal) was observed during the long-term exposure to moderate warming (+ 5 °C) and hypercapnia (~ 800 ppm CO2). This indicates that long-term exposure to moderately elevated CO2 and temperature minimally affects the cellular redox status in these bivalve species and that the earlier observed negative physiological effects of elevated CO2 and temperature must be explained by other cellular mechanisms.  相似文献   

13.
Comprehensive studies to identify species-specific drivers of survival to environmental stress, reproduction, growth, and recruitment are vital to gaining a better understanding of the main ecological factors shaping species habitat distribution and dispersal routes. The present study performed a field-based assessment of habitat distribution in the invasive carabid beetle Merizodus soledadinus for the Kerguelen archipelago. The results emphasised humid habitats as a key element of the insect’s realised niche. In addition, insects faced food and water stress during dispersal events. We evaluated quantitatively how water availability and trophic resources governed the spatial distribution of this invasive predatory insect at Îles Kerguelen. Food and water stress survival durations [in 100%, 70%, and 30% relative humidity (RH) conditions] and changes in a set of primary metabolic compounds (metabolomics) were determined. Adult M. soledadinus supplied with water ad libitum were highly tolerant to prolonged starvation (LT50 = 51.7 ± 6.2 d). However, food-deprived insect survival decreased rapidly in moderate (70% RH, LT50 = 30.37 ± 1.39 h) and low (30% RH, LT50 = 13.03 ± 0.48 h) RH conditions. Consistently, body water content decreased rapidly in insects exposed to 70% and 30% RH. Metabolic variation evidenced the effects of food deprivation in control insects (exposed to 100% RH), which exhibited a progressive decline of most glycolytic sugars and tricarboxylic acid cycle intermediates. Most metabolite levels were elevated levels during the first few hours of exposure to 30% and 70% RH. Augmented alanine and lactate levels suggested a shift to anaerobic metabolism. Simultaneously, peaks in threonine and glycolytic sugars pointed to metabolic disruption and a progressive physiological breakdown in dehydrating individuals. Overall, the results of our study indicate that the geographic distribution of M. soledadinus populations is highly dependent on habitat RH and water accessibility.  相似文献   

14.
Nickel (Ni) may impair plant water balance through detrimental effects on the belowground level. Bilberry (Vaccinium myrtillus L.) plants were grown in a mesic heath forest-type soil and subjected to Ni sulphate (NiSO4·6H2O) concentrations of 0, 10, 50, 100 and 500 mg m−2 during an entire growing season in northern Finland (65°N). Biomass of belowground rhizomes, and tissue water content (TWC) and anthocyanin concentrations of aerial shoots were determined from mature plants in order to study rhizospheric Ni stress, and its possible long-distance effects on aerial shoots. As the major proportion of biomass of bilberry is invested in belowground parts, it was hypothesised that Ni-induced rhizospheric disturbance causes water stress in aerial shoots and increases their anthocyanin concentrations for osmotic regulation. Uptake of Ni from the soil to the rhizome and aerial shoots was measured with X-ray fluorescence spectrometry. Ni concentrations in the soil and rhizome exhibited a dose–response relationship, but the concentrations in the rhizome were about 10-fold lower (<3 mg Ni kg−1) than those in the soil (<30 mg Ni kg−1). Translocation of Ni from the rhizome to aerial shoots did not occur, as Ni concentrations in shoots remained at 1 mg Ni kg−1. Although Ni concentrations in the rhizome were below the threshold values of Ni toxicity (i.e. 10–50 mg Ni kg−1), Ni decreased the rhizome biomass. Anthocyanins decreased in aerial shoots along with the Ni accumulation in the rhizome, while TWC was unaffected. The result suggests that anthocyanins are not involved in osmotic regulation under Ni stress, since anthocyanins in aerial shoots responded to the Ni concentrations in the rhizome despite the lack of water stress.  相似文献   

15.
《Aquatic Botany》2005,83(3):187-192
We investigated the effect of intraspecific competition on growth parameters and photosynthesis of the salt marsh species Atriplex prostrata Boucher in order to distinguish the effects of density-dependent growth inhibition from salt stress. High plant density caused a reduction of 30% in height, 82% in stem dry mass, 80% in leaf dry mass, and 95% in root dry mass. High density also induced a pronounced 72% reduction in leaf area, 29% decrease in length of mature internodes and 50% decline in net photosynthetic rate. The alteration of net photosynthesis paralleled growth inhibition, decreasing from 7.6 ± 0.9 μmol CO2 m−2 s−1 at low density to 3.5 ± 0.4 μmol CO2 m−2 s−1 at high density, indicating growth inhibition caused by intraspecific competition is mainly due to a decline in net photosynthesis rate. Plants grown at high density also exhibited a reduction in stomatal conductance from 0.7 ± 0.1 mol H2O m−2 s−1 at low density to 0.3 ± 0.1 mol H2O m−2 s−1 at high density and a reduction in transpiration rate from 6.0 ± 0.3 mmol H2O m−2 s−1 at low density to 4.3 ± 0.3 mmol H2O m−2 s−1 at high density. Biomass production was inhibited by an increase in plant density, which reduced the rate of photosynthesis, stomatal conductance and leaf area of plants.  相似文献   

16.
Dihydropyrimidones 137 were synthesized via a ‘one-pot’ three component reaction according to well-known Biginelli reaction by utilizing Cu(NO3)2·3H2O as catalyst, and screened for their in vitro β-glucuronidase inhibitory activity. It is worth mentioning that amongst the active molecules, compounds 8 (IC50 = 28.16 ± .056 μM), 9 (IC50 = 18.16 ± 0.41 μM), 10 (IC50 = 22.14 ± 0.43 μM), 13 (IC50 = 34.16 ± 0.65 μM), 14 (IC50 = 17.60 ± 0.35 μM), 15 (IC50 = 15.19 ± 0.30 μM), 16 (IC50 = 27.16 ± 0.48 μM), 17 (IC50 = 48.16 ± 1.06 μM), 22 (IC50 = 40.16 ± 0.85 μM), 23 (IC50 = 44.16 ± 0.86 μM), 24 (IC50 = 47.16 ± 0.92 μM), 25 (IC50 = 18.19 ± 0.34 μM), 26 (IC50 = 33.14 ± 0.68 μM), 27 (IC50 = 44.16 ± 0.94 μM), 28 (IC50 = 24.16 ± 0.50 μM), 29 (IC50 = 34.24 ± 0.47 μM), 31 (IC50 = 14.11 ± 0.21 μM) and 32 (IC50 = 9.38 ± 0.15 μM) found to be more potent than the standard d-saccharic acid 1,4-lactone (IC50 = 48.4 ± 1.25 μM). Molecular docking study was conducted to establish the structure–activity relationship (SAR) which demonstrated that a number of structural features of dihydropyrimidone derivatives were involved to exhibit the inhibitory potential. All compounds were characterized by spectroscopic techniques such as 1H, 13C NMR, EIMS and HREI-MS.  相似文献   

17.
A pot experiment was carried out with tomato (Lycopersicon esculentum Mill.) cv. “Target F1” in a mixture of peat, perlite, and sand (1:1:1) to investigate the effects of supplementary calcium sulphate on plants grown at high NaCl concentration (75 mM). The treatments were: (i) control (C), nutrient solution alone; (ii) salt treatment (C + S), 75 mM NaCl; (iii) salt plus calcium treatment 1 (C + S + Ca1), 75 mM NaCl plus additional mixture of 2.5 mM CaSO4 in nutrient solution; (iv) salt plus calcium treatment 2 (C + S + Ca2), 75 mM NaCl plus additional mixture of 5 mM CaSO4 in nutrient solution. The plants grown under salt stress produced low dry matter, fruit weight, and relative water content than those grown in standard nutrient solution. Supplemental calcium sulphate added to nutrient solution containing salt significantly improved growth and physiological variables affected by salt stress (e.g. plant growth, fruit yield, and membrane permeability) and also increased leaf K+, Ca2+, and N in tomato plants. The effects of supplemental CaSO4 in maintaining membrane permeability, increasing concentrations of Ca2+, N, and K+ and reducing concentration of Na+ (because of cation competition in root zone) in leaves could offer an economical and simple solution to tomato crop production problems caused by high salinity.  相似文献   

18.
The introduced shrub Tamarix ramosissima invades riparian zones, but loses competitiveness under flooding. Metabolic effects of flooding could be important for T. ramosissima, but have not been previously investigated. Photosynthesis rates, stomatal conductance, internal (intercellular) CO2, transpiration, and root alcohol dehydrogenase (ADH) activity were compared in T. ramosissima across soil types and under drained and flooded conditions in a greenhouse. Photosynthesis at 1500 μmol quanta m−2 s−1 (A1500) in flooded plants ranged from 2.3 to 6.2 μmol CO2 m−2 s−1 during the first week, but A1500 increased to 6.4–12.7 μmol CO2 m−2 s−1 by the third week of flooding. Stomatal conductance (gs) at 1500 μmol quanta m−2 s−1 also decreased initially during flooding, where gs was 0.018 to 0.099 mol H2O m−2 s−1 during the first week, but gs increased to 0.113–0.248 mol H2O m−2 s−1 by the third week of flooding. However, photosynthesis in flooded plants was reduced by non-stomatal limitations, and subsequent increases indicate metabolic acclimation to flooding. Root ADH activities were higher in flooded plants compared to drained plants, indicating oxygen stress. Lower photosynthesis and greater oxygen stress could account for the susceptibility of T. ramosissima at the onset of flooding. Soil type had no effect on photosynthesis or on root ADH activity. In the field, stomatal conductance, leaf water potential, transpiration, and leaf δ13C were compared between T. ramosissima and other flooded species. T. ramosissima had lower stomatal conductance and water potential compared to Populus deltoides and Phragmites australis. Differences in physiological responses for T. ramosissima could become important for ecological concerns.  相似文献   

19.
Bisindole analogs 117 were synthesized and evaluated for their in vitro β-glucuronidase inhibitory potential. Out of seventeen compounds, the analog 1 (IC50 = 1.62 ± 0.04 μM), 6 (IC50 = 1.86 ± 0.05 μM), 10 (IC50 = 2.80 ± 0.29 μM), 9 (IC50 = 3.10 ± 0.28 μM), 14 (IC50 = 4.30 ± 0.08 μM), 2 (IC50 = 18.40 ± 0.09 μM), 19 (IC50 = 19.90 ± 1.05 μM), 4 (IC50 = 20.90 ± 0.62 μM), 7 (IC50 = 21.50 ± 0.77 μM), and 3 (IC50 = 22.30 ± 0.02 μM) showed superior β-glucuronidase inhibitory activity than the standard (d-saccharic acid 1,4-lactone, IC50 = 48.40 ± 1.25 μM). In addition, molecular docking studies were performed to investigate the binding interactions of bisindole derivatives with the enzyme. This study has identified a new class of potent β-glucouronidase inhibitors.  相似文献   

20.
A series of unsymmetrically disubstituted urea derivatives 128 has been synthesized and screened for their antiglycation activity in vitro. Compounds 26 (IC50 = 4.26 ± 0.25 μM), 1 (IC50 = 5.8 ± 0.08 μM), 22 (IC50 = 4.26 ± 0.25 μM), 6 (IC50 = 6.4 ± 0.02 μM), 5 (IC50 = 6.6 ± 0.26 μM), 2 (IC50 = 7.02 ± 0.31 μM), 3 (IC50 = 7.14 ± 0.84 μM), 27 (IC50 = 7.27 ± 0.36 μM), 4 (IC50 = 8.16 ± 1.04 μM), 21 (IC50 = 8.4 ± 0.15 μM), 23 (IC50 = 9.0 ± 0.35 μM) and 13 (IC50 = 15.22 ± 6.7 μM) showed an excellent antiglycation activity far better than the standard (rutin, IC50 = 41.9 ± 2.3 μM). This study thus provides a series of potential molecules for further studies of antiglycation agents.  相似文献   

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