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ObjectiveTo explore the difference of learning and memory function between permanent cerebral ischemia and ischemia-reperfusion rat models by filament-occluded method after three weeks of natural recovery, and to observe the changes of brain structure. MethodsA total of 21 SPF male Sprague-Dawley rats were randomly divided into sham group (n = 7), permanent ischemia group (n = 7) and ischemia-reperfusion group (n = 7). The latter two group underwent left middle cerebral artery occlusion, and the ischemia-reperfusion group was reperfused after 90 minutes of ischemia. All the rats were tested with Morris Water Maze 16 to 22 days after modeling, to record escape latency in the navigation experiment, as well as first latency, platform quadrant swimming time ratio and distance ratio, boundary swimming time ratio and distance ratio, average speed, and the swimming path in the space exploration experiment. On the 22nd day after modeling, four rats with similar Longa scores in each group were scanned by magnetic resonance by diffusion tensor imaging, to measure the fractional anisotropy (FA) of cerebral ischemic cortex, striatum, hippocampus and their corresponding contralateral regions, to calculate ratio of FA (rFA); as well as the volume of infarct (VI) and ratio of VI (rVI). ResultsFor navigation experiment, the escape latency decreased in all the groups with the time (F = 36.202, P < 0.001), but it was not significant for the permanent ischemia group (F = 4.004, P > 0.05). The escape latency was longer in the permanent ischemia group than in the other two groups at each time points (P < 0.05). For space exploration experiment, the boundary time ratio and distance ratio were more in the permanent ischemia group and the ischemia-reperfusion group than in the sham group (P < 0.017), and the first latency was longer in the permanent ischemia group than in the sham group (P < 0.017). The swimming path of ischemia-reperfusion group and sham operation group was better than that of the permanent ischemia group. FA and rFA in left cortex and striatum were less in the permanent ischemia group and the ischemia-reperfusion group than in the sham group (P < 0.05), while FA and rFA of left cortex and FA of left striatum were less in the permanent ischemia group than in the ischemia-reperfusion group (P < 0.05). The VI and rVI were larger in the permanent ischemia group than in the ischemia-reperfusion group (t > 4.185, P < 0.01). FA and rFA of left cortex and striatum correlated with escape latency, boundary time ratio and distance ratio (|r| > 0.498, P < 0.05). The VI and rVI correlated with escape latency and boundary time ratio (|r| > 0.538, P < 0.05). ConclusionCognitive impairment is more severe in the rat model of permanent cerebral ischemia, which may relate to the larger damage of structure of nerve fibers in ischemic cortex and striatum, and larger infarct size.
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As the famous Chinese patent medicine, Yinhua Miyanling Tablets, which was derived from ancient prescription denominated Bazhengsan, has not only the effects in clearing away heat and purging pathogenic fire, removing dampness and relieving stranguria, but also have the functions of detoxifying and tonifying. A great number of scientific studies have demonstrated that Yinhua Mi-yanling Tablets played significant roles in destroying harmful microbes and resisting inflammatory and diuresis. Compared with antibiotics, traditional antibacterial Chinese patent medicine Yinhua Miyanling Tablets has the advantage in bacterial resistance in long-term use. Fundamental studies about the content of pharmaceutical ingredients and the modern pharmacology of Yinhua Miyanling Tablets were collected and summarized, which conduces to indicating the active ingredients of Yinhua Miyanling Tablets with the medicinal efficacy from the molecular level and the internal mechanism of Yinhua Miyanling Tablets in the treatment of urinary tract infection(UTI) from the scientific perspective. In the field of clinical research, literatures associated with Yinhua Miyanling Tablets for the treatment of UTI were summarized and analyzed in terms of treatment type, administration mode, dosage, frequency of medication, course, efficiency, side effects and whether combined with healthy lifestyle. These literatures confirmed the medicinal values and the application prospect of Yinhua Miyanling Tablets in treating UTI, especially acute UTI, which provides a scientific theoretical foundation and a correct direction for the clinical application of Yinhua Miyanling Tablets. In conclusion, this article contributes to the standardization of Yinhua Miyanling Tablets in the treatment of UTI, in the expectation of giving the scientific guidance for clinical practice.
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Humans , Drugs, Chinese Herbal , Therapeutic Uses , Medicine, Chinese Traditional , Research , Tablets , Urinary Tract Infections , Drug TherapyABSTRACT
A questionnaire survey of 1 000 clinicians having experience in treating uncomplicated lower urinary tract infections from different levels of hospitals was conducted to mainly evaluate the applicability and effectiveness of clinical application of clinical practice guideline on traditional Chinese medicine therapy alone or combined with antibiotics for uncomplicated lower urinary tract infection(hereinafter referred to as Guideline). The research was conducted with the three-level quality control strictly throughout the process, and the data was real and reliable. The survey's results showed that: most clinicians considered that the Guideline had good clinical applicability. The availability and price of the recommended medicine were moderate. Traditional Chinese medicine had obvious features and advantages in treating lower urinary tract infection for it could reduce the usage of antibiotics and shorten the course of antibiotic application. In the recommendation section, clinicians proposed increasing medication guidance, updating the Guideline timely, as well as increasing treating methods and techniques, strengthen propaganda and promotion, and improve the use of evidence-based methods. In the evaluation of effectiveness, the majority of clinicians agreed that the definition in both traditional Chinese medicine (TCM) and Western medicine and differential diagnosis in the Guideline were accurately described and the basic principle of treatment as well as the treating method of TCM were recommended appropriately. The TCM formulas and Chinese patent medicine had good effect. Some clinicians suggested refining the syndrome differentiation of stranguria. Some clinicians considered that the formulas and herbs recommended in Guideline didn't have obvious effect and some had doubts about the manipulation of fumigation and washing in the part of other methods recommended in Guideline. Moreover, specification and procedure of manipulation of fumigation and washing using herbs and the acupuncture included in characteristic TCM therapy treating uncomplicated lower urinary tract infection remained to be developed.
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Humans , Acupuncture Therapy , Anti-Bacterial Agents , Diagnosis, Differential , Drugs, Chinese Herbal , Medicine, Chinese Traditional , Urinary Tract InfectionsABSTRACT
Urinary tract infection (UTI) in traditional Chinese medicine (TCM) belongs to the category of stranguria. This article describes the unsatisfactory situations in clinical practice such as antibiotics abuse, increasing of drug-resistant bacteria, high recurrence rate, etc. According to evidence-based medicine, literatures as evidence are collected for summarizing and analyzing and the result shows the advantages of TCM of relieving symptoms, reducing the dosage of antibiotics, less side effects, lower recurrence rate, etc. In the field of fundamental research, literatures associated with UTI are also summarized and analysed from several perspectives, such as causes, pathogenesis, syndrome differentiation, pharmacological effects of Chinese herbal medicine, working mechanism of non-drug therapy, etc and the result presents that integrated treatment of TCM in UTI has significant advangtages and its own characteristic.
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In the present study, the effects of six Coptidis alkaloids (berberine, epiberberine, coptisine, jatrorrhizine, palmatine and magnoflorine) on liver microsomes UGTs and UGT1A1 activities in rats and mice were investigated in vitro and in vivo to study the mechanism of metabolic drug-drug interactions of Coptidis Rhizoma with other drugs. In vitro rat and mice liver microsomal incubation systems combined with UDPGA were applied, as well as mice liver microsomes after administration of six Coptidis alkaloids. 4-Nitrophenol and β-estradiol were selected as substrates to determine activities of UGTs and UGT1A1 by UV and HPLC, respectively. According to the in vitro rat study, berberine, epiberberine, coptisine and jatrorrhizine significantly inhibited rat liver microsome UGTs activity, particularly epiberberine showed the strongest inhibition. UGT1A1 activity was lowly inhibited by jatrorrhizine, with IC₅₀ at about 227 μmol•L⁻¹, whereas coptisine and magnoflorine significantly activated UGT1A1. According to the in vitro mice study, berberine, coptisine, jatrorrhizine and palmatine significantly inhibited mice liver microsome UGTs activity, and the six alkaloids all significantly activated UGT1A1. According to the in vivo mice study, UGTs activity was significantly activated only in berberine group, while UGT1A1 activity was significantly activated only in jatrorrhizine group. In conclusion, the effects of Coptidis alkaloids on UGT activity showed significant differences in species and between in vitro and in vivo. Meanwhile, the changes in structures of Coptidis alkaloids also have a big impact on UGT activity, which may be one of the causes for the drug-drug interactions between Coptidis Rhizoma and other drugs.
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To predict the mechanism of liver injury induced by Genkwa Flos, we investigated the effect of chloroform extract on UGTs and UGT1A1 activities of the liver microsomes in rat and human. In the present study, 4-nitrophenol(4-NP) and β-estradiol were elected as substrates to determine activities of UGTs and UGT1A1 by UV and HPLC. The results showed that there were 1.00% of apigenin, 6.40% of hydroxygenkwanin and 18.38% of genkwanin in chloroform extract; and total diterpene mass fraction was 31.40%. Compared with the control group, chloroform extract could significantly inhibit the activity of UGTs in rat liver microsomes(RLM) system, while the inhibitory effect was not obvious in human liver microsomes(HLM) system. UGT1A1 activity was inhibited by chloroform extract in rat liver microsomes and human liver microsomes (based on genkwanin, IC₅₀=8.76, 10.36 μmol•L⁻¹). The inhibition types were non-competitive inhibition(RLM) and uncompetitive inhibition(HLM). In conclusion, the results indicated that chloroform extract showed different inhibitory effects on UGTs and UGT1A1 activity, which may be one of the mechanisms of liver injury induced by Genkwa Flos.
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@#There are many ways to prepare middle cerebral artery occlusion (MCAO) rat model. The focal cerebral ischemia model es-tablished by the suture-occluded method is widely accepted as an ideal focal cerebral ischemia model, which can be used in the basic and clinical study of cerebral vascular diseases. However, it still has the defects of high technical requirement, large model difference and high animal mortality. A variety of focal cerebral ischemia models were established by changing the retention time of the thread, the road the thread plugging into, the type of thread bolt and the depth of the thread plugging. This article compared different suture-occluded method, as well as the suture-occluded method to other modeling methods, different cerebral ischemia models may be different in the pathophysiology of cerebral infarction, and the effects may also be different.
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Objective To explore the effect of exercise training on learning and memory ability in rats with focal cerebral ischemia, and to analyze the changes of brain tissue structure of rats after exercise training through diffusion tensor imaging (DTI). Methods Twenty-four SPF male Sprague-Dawley rats were randomly divided into sham operation group (n=8), natural recovery group (n=8) and exercise training group (n=8). The left middle cerebral artery occlusion (MCAO) model was established. The exercise training group received running wheel training 24 hours after modeling, for 14 days. All groups were tested by the Morris water maze 15 days after modeling. The latency in the navigation experiment, as well as the first latency, boundary swimming time ratio, the boundary swimming distance ratio, the average speed and the swimming path in the space exploration experiment were recorded. Four rats with similar Longa scores in each group received rou-tine magnetic resonance imaging and DTI scanning, the fractional anisotropy (FA), axial diffusivity (λ‖), and radial diffusivity (λ⊥) of isch-emic cortex and hippocampal lesion and contralateral side were measured. Results In the navigation experiment, the latency of three groups showed a downward trend along with training days (P0.05), while it was shorter in the exercise train-ing group than in the natural recovery group in the same time (P2.627, P2.521, P0.05). The swimming paths in the exercise training group and the sham operation group were better than that of the natural recovery group. The FA and rFA in the left cortical area were higher in the sham operation group than in the exercise training group and the natural recovery group (P0.05). There was no significant difference in the FA in the right cortical area among three groups (F=0.532, P=0.607). Theλ⊥,λ‖, rλ‖and rλ⊥in the left cortical area were lower in the sham opera-tion group than in the natural recovery group (P0.05). There was no significant difference in theλ⊥andλ‖in the right cortical area among three groups (F0.05). There was no significant difference in the FA,λ⊥,λ‖and rFA, rλ⊥and rλ‖in the bilateral hippo-campal interest area among three groups (F0.05). The rFA, rλ‖, rλ⊥and leftλ⊥ were correlated with the latency in the space ex-ploration experiment in the Morris water maze test (P<0.05), in which the correlation coefficient of rλ⊥was the highest (r=0.761, P<0.01). Conclusion Proper exercise training can improve the learning and memory ability of rats with focal cerebral ischemia, and can promote the repair of nerve fiber damage and reduce the vascular edema. In addition, the rFA, rλ‖, rλ⊥andλ⊥of ischemic cortex may be predictors of cognitive function recovery in rats after focal cerebral ischemia, especially rλ⊥.
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To predit the mechanism of metabolic drug-drug interactions of hydroxygenkwanin with other drugs, we investigated the inhibition inhibitory effect of hydroxygenkwanin on UGTs and UGT1A1 activities of different liver microsomes. In the present study, 4-nitrophenol (4-NP) and β-estradiol were elected as substrates to determine activities of UGTs and UGT1A1 by UV and HPLC, respectively. The results showed that, hydroxygenkwanin significantly inhibited UGTs activity in rat, mouse and human liver microsomes. UGT1A1 activity was inhibited by hydroxygenkwanin to varying degrees, with IC₅₀ about 190, 10.93, 20.07, 76.31 μmol•L⁻¹ in mouse liver microsome(MLM), rat liver microsome (RLM) and recombinant UGT1A1, and human liver microsome (HLM), respectively. The inhibition types were competitive inhibition (RLM, HLM) and linear mixed-typed linear inhibition (recombinant UGT1A1). The order for the inhibitory intensity was RLM>rUGT1A1>HLM>MLM. In conclusion, hydroxygenkwanin has an inhibitory effect on UGTs and UGT1A1 activities of different liver microsomes, with differences in species, indicating its potential drug interactions based on UGT1A1 enzyme. This study aims to provide a reliable experimental basis for its further research and development of hydroxygenkwanin, and provide theoretical reference for the clinic drug combination research.
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Objective To explore the effects of early exercise on motor function and the mechanism in rats after focal cerebral ischemia. Methods 21 Sprague-Dawley male rats were divided into control group (n=7), natural recovery group (n=7) and exercise training group (n=7), and the latter 2 groups were modeled with middle cerebral artery occlusion. The exercise training group received wheel running exercise 24 hours after modeling for 14 days. They were assessed with Rogers score and beam balance test 21 days after modeling. 4 rats in each group received routine MRI and diffusion tensor imaging (DTI) scanning. The fractional anisotropy (FA) and apparent diffusion coefficient (ADC) of ischemic (L) and contralateral side (R) were measured, and the rate of them (L/R, r) was calculated. Results There was significant difference in Rogers score among the groups (Z=-0.786, P0.05). Beam balance score of the natural recovery group was significantly different from the control group and the exercise training group (F=38.11, P0.05). The LFA of the natural recovery group was significantly different from the control group (P0.05);while the rFA of the natural recovery group was significantly different from the control group and the exercise training group (F=19.30, P0.05). LFA and rFA strongly correlated with all the behavior scores (r=-0.90--0.70, P0.05). DTT showed that the direction and density of neural fibers were significantly asymmetrical in the natural re-covery group and the exercise training group, and more symmetrical in the exercise training group. Conclusion Early exercise can promote the neural functional recovery in rats after focal cerebral ischemia, which may associate with the improve of conduction of fibers.
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Using pesticides has double effects
On one hand, it contributes to pests control and regulates the growth of crops; On the other hand, it does harm to the environment
To develop ecological agriculture should not only emphasize the output level of agriculture to pursuit of economic efficiency, but also need to keep the ecological environment protected and focus on the social benefits during the development of the industry. As a large agricultural country in the world, China is vigorously promoting the development of ecological agriculture, which is bound to put forward to developing the pesticide industry and green ecological development requirements to promote the transformation and upgrading of agricultural pharmaceutical industry
This paper discusses the mechanism of pesticide pollution on the ecological environment and analyzes China's agricultural problems in the pharmaceutical industry. Then study on the development of Chinese green pesticides and try to find the proper paths of agricultural pharmaceutical to achieve industrial upgrading
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To figure out the stability and intestinal bacteria metabolites of rats in vitro of astragaloside IV ( AST), this research was done to explore the stability of AST in the artificial gastric juice. artificial intestinal juice and rat liver homogenate and the metabolism in rat intestinal in vitro. HPLC was used to calculate the remaining rate of AST in biological samples by measuring the content of AST, while metabolites were determined by combining the methods of TLC, HPLC and LC-MS/MS. It turned out that AST was difficult to metabolize in the artificial gastric juice, artificial intestinal juice and rat liver. Also, the metabolic pathway of AST was stepped by deglycosylation. Firstly, AST was converted to its secondary etabolites (6-O-β-D-glucopyranosyl- cycloastragenol, CMG) by removal of xylose moiety at C-3, then transformed into cycloastragenol (CAG) after hydrolytic removal of the glucose moiety at C-6. All the results suggested that the metabolism of AST in vivo occurs mainly in the intestinal by hydrolysis of glycosyl. In conclusion, hydrolysis of intestinal flora is the main reason that AST metabolizes.
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Animals , Rats , Bacteria , Metabolism , Chromatography, High Pressure Liquid , Drug Stability , Intestines , Microbiology , Liver , Metabolism , Rats, Sprague-Dawley , Saponins , Chemistry , Metabolism , Tandem Mass Spectrometry , Triterpenes , Chemistry , MetabolismABSTRACT
Epiberberine, one of the most important isoquinoline alkaloid in Coptidis Rhizoma, possesses extensive pharmacological activities. In this paper, the liquid chromatography-tandem mass spectrometry (LC-MS/MS) was used to study phase I and phase II metabolites. A Thermo HPLC system (including Surveyor AS, Surveyor LC Pump, Surveyor PDA. USA) was used. The cocktail probe drugs method was imposed to determine the content change of metoprolol, dapsone, phenacetin, chlorzoxazone and tolbutamide simultaneously for evaluating the activity of CYP2D6, CYP3A4, CYP1A2, CYP2E1 and CYP2C9 under different concentrations of epiberberine in rat liver microsomes. The result showed that epiberberine may have phase I and phase II metabolism in the rat liver and two metabolites in phase I and three metabolites in phase II are identified in the temperature incubation system of in vitro liver microsomes. Epiberberine showed significant inhibition on CYP2D6 with IC50 value of 35.22 μmol L(-1), but had no obvious inhibiting effect on the activities of CYP3A4, CYP1A2, CYP2E1 and CYP2C9. The results indicated that epiberberine may be caused drug interactions based on CYP2D6 enzyme. This study aims to provide a reliable experimental basis for its further research and development of epiberberine.
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Animals , Male , Rats , Berberine , Chemistry , Metabolism , Chromatography, High Pressure Liquid , Cytochrome P-450 CYP2D6 , Metabolism , Cytochrome P-450 CYP2D6 Inhibitors , Chemistry , Metabolism , Drugs, Chinese Herbal , Chemistry , Metabolism , Microsomes, Liver , Metabolism , Molecular Structure , Rats, Sprague-Dawley , Tandem Mass SpectrometryABSTRACT
<p><b>OBJECTIVE</b>The theory of strain energy density (SED) was combined with finite element analysis to investigate alveolar bone remodeling of the mandibular first molar with different levels of periodontal attachment under mastication loading.</p><p><b>METHODS</b>Three-dimensional finite element models of the mandibular first molar with different levels of periodontal attachment were established. Based on SED theory, the user material subroutine (UMAT) (used by ABAQUS software) was developed by ourselves to simulate the remodeling process of mandibular bone. The stress distributions and bone density changes were analyzed under different mastication loading. The influence of loading magnitude on alveolar bone remodeling with different levels of periodontal attachment was investigated.</p><p><b>RESULTS</b>The results showed that the neck of buccal, lingual regions and root apex area experienced a higher stress. The stress and the density of alveolar bone increased gradually with the enhancing of the bite force at the beginning. Then the density would appear declining when the bite force exceeded the extreme load. The extreme load reduced from 420 N to 240 N with the periodontal attachment falling from normal to 1/2 of root length also. And the remodeling rate of the bone was faster as the loading increasing.</p><p><b>CONCLUSION</b>The capability of the periodontal tissue for supporting the teeth will drop gradually as the periodontal attachment level dropping. And the decline of bone density also appeared in earlier time. The change of density is associated with mastication loading during the bone remodelling. And reducing the occlusal force properly to the molar with different attachment level is benefit for clinical treatment and prognosis of periodontal disease.</p>