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1.
Acta Pharmaceutica Sinica ; (12): 2495-2504, 2021.
Article in Chinese | WPRIM | ID: wpr-886946

ABSTRACT

italic>Helicobacter pylori (H. pylori) can cause a variety of digestive tract diseases, the serious may develop into gastric cancer. Nowadays, H. pylori infection rate exceeds 50%, and its eradication rate is declining due to the continuous increase of drug resistance, leading to the occurrence of plenty of stubborn infections, which seriously threaten human health. At present, it is difficult to achieve satisfactory curative effect by increasing the types of antibiotics combination or increasing their dose. In this review, the clinical treatments of H. pylori were introduced. Proceed from the characteristics and pathological background of H. pylori infection that makes H. pylori difficult to eradicate, the research advances of drug delivery strategies for improving H. pylori eradication rate were reviewed, such as strategies that could increase drug concentration in stomach (e.g. drug delivery systems with gastric acid-stabilized ability), increase drug concentration in H. pylori colonization sites (e.g. drug delivery systems with gastric retention or H. pylori targeted abilities), overcome H. pylori resistance (metal nanoparticles, anti-biofilm delivery systems), enhance host immune response (vaccine preparation) and so on. Novel drug delivery systems, such as cell membrane coating technology and phage therapy, are comparatively rare in the field of anti-H. pylori, but have broad application prospects. This review would provide reference for the development and application of therapeutic strategies to improve H. pylori eradication rate.

2.
Article in Chinese | WPRIM | ID: wpr-905951

ABSTRACT

Objective:Based on fingerprint, index component content and dry extract yield, a quality evaluation method for substance benchmark of Xiebaisan was established to study the key quality attributes, to explore the quantitative transfer relationship between decoction pieces and substance benchmark, and to preliminarily formulate the quality standard of substance benchmark of Xiebaisan. Method:The substance benchmark of Xiebaisan was prepared according to the records of ancient formulas, fingerprints of 15 batches of decoction pieces and substance benchmarks were collected by high performance liquid chromatography (HPLC) and the index components were determined with the mobile phase of acetonitrile-0.05% phosphoric acid solution for gradient elution. The dry extract yield, fingerprint similarity and transfer rate of index components were combined to study the quantity value transmitting. Result:Ten characteristic peaks were identified in fingerprint of the substance benchmark and two characteristic peaks from stir-fried Mori Cortex, four characteristic peaks from baked Lycii Cortex, four characteristic peaks from Glycyrrhizae Radix et Rhizoma Praeparata cum Melle. Mulberroside A, liquiritin and glycyrrhizic acid were used as index components for the determination, the contents of mulberroside A, liquiritin and glycyrrhizic acid in substance benchmark of Xiebaisan were 2.69%-4.26%, 0.09%-0.17% and 0.09%-0.16%, and their transfer rates were (31.37±4.14)%, (36.12±4.03)% and (12.25±0.88)%, respectively. The similarity of fingerprint of substance benchmarks was good, the fingerprint similarities of 14 batches of substance benchmarks and control fingerprint were >0.9. The dry extract yield of substance benchmark of Xiebaisan ranged from 8.09% to 11.29%. Conclusion:The established quality evaluation method of substance benchmark of Xiebaisan is scientific and reasonable, and the transfer process of decoction pieces to substance benchmarks is stable and controllable. The preliminary quality standard of the substance benchmark can provide basis and reference for the development of modern preparations of Xiebaisan in the future.

3.
Acta Pharmaceutica Sinica ; (12): 1-7, 2019.
Article in Chinese | WPRIM | ID: wpr-778678

ABSTRACT

BCS Ⅱ drugs are characterized by low solubility and high permeability. Improving their solubility is considered an important approach to improve its oral absorption. Recent strategies to increase the solubility of poorly-soluble drugs may unexpectedly result in greatly depressed permeability, ultimately leading to failure in improving oral absorption. Based on the mathematics of membrane permeability coefficient of a drug, the membrane/aqueous partition coefficient is dependent on the drug's solubility in the gastrointestinal milieu, suggesting a unique interplay between the solubility and permeability of the drug, and treating the one irrespectively of the other may be insufficient. When we focus on the increase of drug solubility and overlook the efficacy of drug permeability, the positive effect of increased solubility to drug oral absorption might be traded off by depressed permeability. To provide rational formulary designs, by optimizing excipients and evaluation, this review summarizes solubility- permeability interplay for different types of solubilizing techniques, such as cyclodextrin, surfactants-based vehicle, cosolvent, amorphous solid dispersions, other infectors such as P-gp transporters and new techniques for simultaneous evaluation of drug solubility and permeability.

4.
Acta Pharmaceutica Sinica ; (12): 61-65, 2019.
Article in Chinese | WPRIM | ID: wpr-778667

ABSTRACT

Cyclodextrin can increase the solubility of poorly soluble drugs, but also decrease the permeability of poorly soluble drugs in inclusion complexes simultaneously, which partially or completely counteracts the contribution of improvement in solubility to the oral absorption of poorly soluble drugs. If a competing agent is added to the system to compete binding sites of cyclodextrins with drugs, drug permeability can be improved by increasing the concentration of free drugs in the inclusion complex system. In this paper, a rapid in vitro screening method for competing agents of cyclodextrin inclusion complex is proposed based on the principle that good drug permeability is in accord with good cell uptake. The equilibrium constants between drugs and hydroxypropyl-beta-cyclodextrin (HPCD) were determined by phase equilibrium solubility method. Cinnarizine (CN) with a high equilibrium constant was selected as a competing agent, coumarin 6 (C6) and 9-octadecyl berberine (BD) with smaller equilibrium constants were selected as model drugs. Both changes of solubility and uptake by Caco-2 and A549 cells of C6 and BD were investigated different concentrations of CN to the HPCD solution of C6 and BD. The results showed that the uptake of C6 and BD increased in a CN concentration-dependent manner, and the solubility of C6 and BD in HPCD solution decreased with the prolongation of equilibrium time. It might be due to increased free drug concentrations that resulted from the competition of CN for drug binding sites with HPCD. In our study, in vitro cell uptake method was firstly used to validate the ability of CN as a competing agent to increase drug permeability (cell uptake). This method can be used for preliminarily screening of competing agents for drug-cyclodextrin inclusion complexes.

5.
Article in Chinese | WPRIM | ID: wpr-802025

ABSTRACT

Objective:To observe the effects of recipes for tonifying kidney and replenishing Qi, Zuoguiwan (ZG) and Yiqi Congming Tang(YQ) on memory capacity, expressions of learning and memory-related genes expression, and explore the changes in relevant epigenetic modification enzymes. Method:SD male rats with natural aging (24 months old) were used as animal models and randomly divided into aged control group, aged ZG group(12.12 g·kg-1), aged YQ group(10.18 g·kg-1), aged compound group(11.15 g·kg-1) and aged antagonist RU38486 group(5×10-3g·kg-1). Another 5 months old male SD rats were included as the young control group. Morris water maze method was used to observe the spatial learning and memory ability of the rats. The co-localizations of histone deacetylase 2 (HDAC2) and methyl CpG binding protein 2 (MeCP2) in hippocampus of rats in each group were observed by laser confocal microscope. The changes in expressions of glucocorticoid receptor (GR), synapsin1(Syn-1), HDAC2, and histone acetyltransferase 1(HAT1) proteins in hippocampus of each group were detected by Western blot, and mRNA expression of HDAC2 was detected by Real-time fluorescence quantitative polymerase Chain reaction (Real-time PCR). At the same time, the effects of ZG, YQ and compound decoction in alleviating the above-mentioned abnormal changes were observed. Result:Compared with the young control group(control group), the latency of the aged control group was significantly prolonged (PPPPPPPConclusion:ZG group, YQ group, and compound group can improve the spatial learning and memory abilities of aged rats by increasing the expression of learning-memory-associated protein GR and epigenetic modification enzyme HAT1, and reducing the expression of HDAC2 and the co-localization of HDAC2 protein and MeCP2 in the nucleus.

6.
Acta Pharmaceutica Sinica ; (12): 2040-2049, 2018.
Article in Chinese | WPRIM | ID: wpr-780086

ABSTRACT

Eighty percent of bacterial infections are related to the formation of bacterial biofilm. Compared with planktonic bacteria, bacterial biofilm is 10-1 000 times more resistant to antibiotics, which is the main cause of current bacterial drug resistance. A comprehensive understanding of the characteristics and resistance mechanisms of bacteria biofilm will help us treat the stubborn infections caused by the bacterial biofilm better and solve the problem of bacterial drug resistance. In this review, the composition and quorum sensing of bacterial biofilm, two major patterns of biofilm formation and drug resistance mechanisms were presented. Furthermore, representative compounds with anti-biofilm activity and compounds synergistic with antibiotics in anti-biofilm actions were introduced. Nano drug delivery strategies used for anti-biofilm in recent years as well as a novel drug delivery system-molecularly imprinted polymer was also introduced.

7.
Tianjin Medical Journal ; (12): 264-268, 2018.
Article in Chinese | WPRIM | ID: wpr-698020

ABSTRACT

Objective To analyze the curative effect and related influencing factors of hyperbaric oxygen combined with dexamethasone in the treatment of sudden deafness (SD). Methods The clinical data of 200 patients with SD, who were treated with hyperbaric oxygen combined with dexamethasone in our hospital from January 2014 to December 2016, were retrospectively analyzed.According to the curative effect,patients were divided into the effective group(n=182)and the ineffective group(n=18).Data of gender,age,time from onset to treatment,ears,hearing loss,the type of audiometric curve, dizziness, tinnitus, complications (hypertension or diabetes), plasma viscosity and serum C reactive protein (CRP) were compared between the two groups.Logistic regression analysis was used to screen risk factors influencing the curative effect of SD.Results The total response rate was 91.00%(182/200),and the ineffective rate was 9.00%(18/200).In the effective group patients aged > 50 years old, the time from onset to treatment was > 7 d, and the hearing loss was ≥ 60 dB. The proportions of high-frequency or stone-deaf audiometric curves, combined with dizziness, hypertension, diabetes, plasma viscosity ≥ 2 mPa·s and serum CRP level ≥ 20 μmol/L were significantly lower in the effective group than those in the ineffective group(P<0.05).Logistic regression analysis showed that age(>50 years old),time from onset to treatment(>7 d), hearing loss(≥60 dB), high-frequency or stone-deaf audiometric curves, combined with dizziness, hypertension, diabetes, plasma viscosity(≥2 mPa·s)and plasma CRP(≥20 μmol/L)were high risk factors for the curative effect of SD(P<0.05). Conclusion Hyperbaric oxygen combined with dexamethasone is an effective treatment for SD,but there are many factors affecting the curative effect. It is necessary to consider the clinical and pathological characteristics of patients in clinical treatment.

8.
Journal of Experimental Hematology ; (6): 1373-1377, 2017.
Article in Chinese | WPRIM | ID: wpr-301721

ABSTRACT

<p><b>OBJECTIVE</b>To study the effect of over-expression of KLF4 on the proliferation and apoptosis of K562 cells.</p><p><b>METHODS</b>The recombinant plasmid with over-expression of KLF4 was transfected into K562 cells by electroporation, then the obtained G418-resistant clones of K562 cells (K562/pEGFP-KLF4) were used as experimental group, and the vector control (K562/pEGFP-C1) and blank K562 cell control groups were set up at the same time. The expression of EGFP-KLF4 fusion protein in K562 cells was observed by fluorescence microscopy; the Western blot was performed to detect the level of KLF4 protein in the cells of each groups, the cell proliferation was tested by methylthiazolyl tetrazolium (MTT) assay, and the cell apoptosis was detected by flow cytometry.</p><p><b>RESULTS</b>Compared with K562/pEGFP-C1 group and blank K562 group, the level of KLF4 protein of K562/ pEGFP-KLF4 cells were significantly increased, and the over-expression ratio reached 74.07%(P<0.05). The proliferation ability of the over-expressing KLF4 K562 cells was inhibited significantly (P<0.05). However, the apoptosis of K562/pEGFP-ILK cells with over-expression of KLF4 was increased (P<0.05).</p><p><b>CONCLUSION</b>A stable over-expressing KLF4 protein K562 cell line with was constructed successfully, and the over-expression of KLF4 can inhibi proliferation and promote apoptosis of K562 cells.</p>

9.
Article in Chinese | WPRIM | ID: wpr-237873

ABSTRACT

<p><b>OBJECTIVE</b>To establish discriminant functions of diarrhea-predominant irritable bowel syndrome (IBS-D) by studying it from quantitative diagnosis angle, hoping to reduce interference of subjective factors in diagnosing and differentially diagnosing Chinese medical syndromes of IBS-D.</p><p><b>METHODS</b>A Chinese medical clinical epidemiological survey was carried out in 439 IBS-D patients using Clinical Information Collection Table of IBS. Initial syndromes were obtained by cluster analysis. They were analyzed using step-by-step discrimination by taking information of four Chinese medical diagnostic methods and serum brain-gut peptides (BGP) as variables.</p><p><b>RESULTS</b>Clustering results were Gan stagnation Pi deficiency syndrome (GSPDS), Pi-Wei weakness syndrome (PWWS), Gan stagnation qi stasis syndrome (GSQSS), Pi-Shen yang deficiency syndrome (PSYDS), Pi-Wei damp-heat syndrome (PWDHS), cold-damp disturbing Pi syndrome (CDDPS). Of them, GSPDS was mostly often seen with effective percentage of 34. 2%, while CDDPS was the least often seen with effective percentage of 5.5%. A total of 5 discriminant functions for GSPDS, PWWS, GSQSS, PSYDS, and PWDHS were obtained by step-by-step dis- crimination method. The retrospective misjudgment rate was 4.1% (16/390), while the cross-validation misjudgment rate was 15.4% (60/390).</p><p><b>CONCLUSION</b>The establishment of discriminant functions is of value in objectively diagnosing and differentially diagnosing Chinese medical syndromes of IBS-D.</p>


Subject(s)
Alarmins , Brain , Cluster Analysis , Diarrhea , Classification , Diagnosis , Hot Temperature , Humans , Irritable Bowel Syndrome , Classification , Diagnosis , Medicine, Chinese Traditional , Qi , Retrospective Studies , Surveys and Questionnaires , Yang Deficiency
10.
Article in Chinese | WPRIM | ID: wpr-297378

ABSTRACT

<p><b>OBJECTIVE</b>To explore the mechanism of three kinds extracts (saponins, volatile components, polysaccharide components) of Qingxin Kaiqiao Recipe (QKR) in improving learning and memory capabilities of Alzheimer's disease (AD) rats.</p><p><b>METHODS</b>A controlled comparison method was used. Totally 56 male SD rats were randomly divided into seven groups, i.e., the normal control group, the sham-operation group, the model group, the Aricept group, the saponin group, the benzene group, and the polysaccharide group, 8 in each group. AD rat model was established by bilateral hippocampus injection of Aβ1-40 (2 µL, 2.5 µg/µL). The next day after modeling rats in the saponin group, the benzene group, and the polysaccharide group, the saponin group, the Aricept group were intragastrically administered with saponin (at the daily dose of 9 mL/kg, 2.1 g/mL) , benzene (at the daily dose of 3.33 mL/kg, 5.7 g/mL) , polysaccharide (at the daily dose of 8.33 mL/kg, 2.28 g/mL), Aricept (at the daily dose of 1.67 mg/kg), respectively, once a day for 2 consecutive weeks from 10 am every day. Equal volume of normal saline was intragastrically administered to rats in the normal control group and the model group. Learning and memory capabilities were detected using water maze 2 weeks later. Expression levels of synaptotagmin-1 (Syt-1), interleukin-1β (IL-1β), glia fibrillary acidic protein (GFAP), and β-amyloid precursor protein (βAPP) in the cortex and hippocampus of AD rats were detected using immunohistochemistry.</p><p><b>RESULTS</b>Learning and memory capabilities could be improved by three kinds extracts of QKR. There was no statistical difference in the escape latency between the polysaccharide group and the model group (P >0. 05). The escape lacency was shortened in the rest treatment groups (P < 0.05). The escape latency was obviously prolonged in three kinds extracts of QKR groups, when compared with the Aricept group (P < 0.05, P < 0.01). Compared with the model group, times for crossing platforms were significantly increased in the saponin group and the Aricept group (P < 0.05). Compared with the Aricept group, average times for crossing platforms were significantly lessened in three kinds extracts of QKR groups (P < 0.01). Compared with the sham-operation group, expression levels of Syt-1, IL-1β, GFAP, and βAPP in the cortex and hippocampus were increased in the model group (P < 0.01). Compared with the model group, the expression of cortical Syt-1 increased in the saponin group and the benzene group; the expression of cortical IL-1β increased in the benzene group and the polysaccharide group; the expression of hippocampal GFAP increased in the three kinds extracts of QKR groups; expression levels of Syt-1, IL-1β, GFAP, and β-APP in the cortex and hippocampus decreased in the rest treatment groups (all P < 0.05, P < 0.01). Compared with the Aricept group, expression levels of Syt-1, IL-1β, GFAP, and βAPP in the cortex and hippocampus were significantly increased in three kinds extracts of QKR groups (P < 0.05, P < 0.01).</p><p><b>CONCLUSION</b>Three kinds extracts of QKR might play roles in anti-AD possibly by decreasing expression levels of Syt-1, IL-1β, GFAP, and βAPP in the cortex and hippocampus.</p>


Subject(s)
Alzheimer Disease , Amyloid beta-Protein Precursor , Animals , Disease Models, Animal , Drugs, Chinese Herbal , Pharmacology , Glial Fibrillary Acidic Protein , Hippocampus , Interleukin-1beta , Learning , Male , Memory , Rats , Rats, Sprague-Dawley , Saponins
11.
Article in Chinese | WPRIM | ID: wpr-294119

ABSTRACT

<p><b>OBJECTIVE</b>To study the protective effect of cerebrospinal fluid containing Qingxin Kaiqiao Fang on sodium dithionite (Na2S2O4)-induced PC12 cell injury, in order to provide basis for clinical application of the prescription.</p><p><b>METHOD</b>SD rats were orally administered with water decoction of Qingxin Kaiqiao Fang (7. 9 g . kg-1) once every 12 h, for a total of 7 times, in order to prepare cerebrospinal fluid containing Qingxin Kaiqiao Fang. The neurocyte injury model was established by adding Na2S2O4 with the final concentration of 8 m mol . L-1 into PC12 cells. With nimodipine (1 x 10(7)mol . L-1 ) as the positive control group, MTT method test was adopted to detect the impact of cerebrospinal fluid containing Qingxin Kaiqiao Fang on the activity of PC12 cells. The expression of Bax, Bel-2 and Caspase-3 mRNA was detected by RT-PCR.</p><p><b>RESULT</b>The cerebrospinal fluid containing Qingxin Kaiqiao Fang groups showed a significantly higher activity in PC12 cells than the model group, with decrease in expressions of Bax mRNA and Caspase-3 mRNA and increase in expression of Bel-2 mRNA. There were significant differences compared with the model group (P< 0. 05,P <0. 01).</p><p><b>CONCLUSION</b>Qingxin Kaiqiao Fang shows a notable protective effect on Na2S2 04-induced neurocyte injury.</p>


Subject(s)
Animals , Apoptosis , Cerebrospinal Fluid , Chemistry , Dithionite , Toxicity , Drugs, Chinese Herbal , Pharmacology , PC12 Cells , Proto-Oncogene Proteins c-bcl-2 , Metabolism , Rats , Rats, Sprague-Dawley
12.
Article in Chinese | WPRIM | ID: wpr-359313

ABSTRACT

<p><b>OBJECTIVE</b>To study effects of Qingxin Kaiqiao Recipe (QKR) and its volatile oil on the expressions of Abeta(25-35) glial fibrillary acidic protein (GFAP), beta-amyloid (Abeta), beta-amyloid precursor protein (betaAPP), and Caspase-3 in the cortex and hippocampus of Alzheimer's disease (AD) rats induced by injecting Abeta(25-35) into the bilateral amygdala.</p><p><b>METHODS</b>Totally 32 male SD rats were selected. The AD rat model was establish by injecting Abeta(25-35) from bilateral amygdala. After modeling they were randomly divided into the model group, the Donepezil Hydrochloride group [Donepezil Hydrochloride Tablet (1.67 mg/kg), abbreviated as the DH group], the QKR group (QKR Decoction, 12.67 mL/kg), and the volatile oil group (3.33 mL/kg), 8 rats in each group. Another 8 rats were selected as the normal control group. Equal volume of double distilled water was administered to rats in the normal control group and the model group by gastrogavage, once daily for 2 successive weeks. The Morris water maze test was performed by the end of medication. The escape latency and times of crossing the platform in the water maze test were recorded during the 1st day to the fifth day. The expressions of GFAP, Abeta, betaAPP, and Caspase-3 in the cortex and hippocampus of the rats in each group were detected by immunohistochemical assay.</p><p><b>RESULTS</b>Compared with the model group, the escape latency from the 3rd day to the 5th day was shortened, the expressions of GFAP, Abeta, betaAPP, and Caspase-3 decreased in the cortex and hippocampus, the times of crossing the platform increased in each medication group, showing statistical difference (P < 0.01, P < 0.05). Compared with the DH group, the expressions of Abeta in the cortex and hippocampus decreased, and the betaAPP expression increased in the QKR group. The expressions of GFAP, betaAPP, and Caspase-3 in the cortex and hippocampus increased in the volatile oil group. The escape latency from the 3rd day to the 5th day was obviously prolonged, and the times of crossing the platform decreased in the volatile oil group, showing statistical difference (P < 0.05, P < 0.01).</p><p><b>CONCLUSION</b>QKR could obviously improve the learning and memory capabilities of AD rats, which might be achieved through decreasing the expressions of GFAP, Abeta, betaAPP, and Caspase-3 in the cortex and hippocampus.</p>


Subject(s)
Alzheimer Disease , Drug Therapy , Metabolism , Animals , Caspase 3 , Metabolism , Cerebral Cortex , Metabolism , Disease Models, Animal , Drugs, Chinese Herbal , Therapeutic Uses , Glial Fibrillary Acidic Protein , Metabolism , Hippocampus , Metabolism , Male , Oils, Volatile , Rats , Rats, Sprague-Dawley
13.
Article in Chinese | WPRIM | ID: wpr-346456

ABSTRACT

<p><b>OBJECTIVE</b>To study the protective effect of cerebrospinal fluid containing Qingxin Kaiqiao recipe on PC12 cell injury induced by glutamate (Glu), in order to provide basis for the conical application of the recipe.</p><p><b>METHOD</b>SD rats were orally administered with decoction of Qingxin Kaiqiao recipe (7.9 g x kg(-1)) for three and a half days, 2 times a day, in order to prepare cerebrospinal fluid containing Qingxin Kaiqiao recipe. PC cells were divided into the normal group, the model group, the nimodipine group, the 10% normal CSF group, the 10% medicated CSF group, the 20% normal CSF group, the 20% medicated CSF group. Except for the normal group, other groups were cultured with PC12 cells and Glu with the final concentration of 20 mmol x L(-1) to establish the nerve cell injury model. Apart from the model group and the normal group, other groups were intervened with nimodipine, normal cerebrospinal fluid, and 10% and 20% medicated CSF. RT-PCR was used to detect the expression level of Bax mRNA, Bcl-2 mRNA and Caspase-3 mRNA, and MTT method was used to detect the activity of PC12 cells.</p><p><b>RESULT</b>The activity of PC12 cells of all of medicated CSF groups was higher than that of the model group, with the decrease in the expression of Bax mRNA and Caspase-3 mRNA and the increase in the expression of Bcl-2 mRNA. They showed a significant different with the model group (P < 0.01). The 20% medicated CSF group was superior than the 10% medicated CSF group (P < 0.01).</p><p><b>CONCLUSION</b>Qingxin Kaiqiao recipe shows an apparent protective effect on PC12 cells injured by Glu.</p>


Subject(s)
Animals , Apoptosis , Caspase 3 , Genetics , Cerebrospinal Fluid , Glutamic Acid , Toxicity , Male , Medicine, Chinese Traditional , Neuroprotective Agents , Pharmacology , PC12 Cells , Proto-Oncogene Proteins c-bcl-2 , Genetics , Rats , Rats, Sprague-Dawley
14.
Article in Chinese | WPRIM | ID: wpr-308602

ABSTRACT

<p><b>OBJECTIVE</b>To observe the protective effect of Qingxin Kaiqiao Fang containing cerebrospinal fluid on PC12 cell injury induced by Abeta25-35, in order to provide basis for clinical application of the formula.</p><p><b>METHOD</b>Sprague Dawley rats were orally administration with Qingxin Kaiqiao Fang (7.9 g x kg(-1)) twice a day for 3.5 days to prepare Qingxin Kaiqiao Fang containing cerebrospinal fluid. The nerve cell injury model was established by PC12 cells and Abeta25-35 with the concentration of 10 micromol x L(-1). The expressions of Bax, Bcl-2 and Caspase-3 mRNA were detected by immunohistochemical method in the PC12 cells.</p><p><b>RESULT</b>The Qingxin Kaiqiao Fang group showed a significant higher PC12 cell activity than the model group, with decrease in Bax mRNA and Caspase-3 mRNA expressions and increase in Bcl-2 mRNA expression. There was a significant difference from the model group (P < 0.05, P < 0.01).</p><p><b>CONCLUSION</b>Qinxin Kaiqiao Fang shows a significant protective effect on Abeta25-35-induced nerve cell injury.</p>


Subject(s)
Amyloid beta-Peptides , Toxicity , Animals , Apoptosis , Caspase 3 , Genetics , Cell Survival , Cerebrospinal Fluid , Male , Medicine, Chinese Traditional , Neuroprotective Agents , Pharmacology , PC12 Cells , Peptide Fragments , Toxicity , Proto-Oncogene Proteins c-bcl-2 , Genetics , Rats , Rats, Sprague-Dawley , bcl-2-Associated X Protein , Genetics
15.
Article in Chinese | WPRIM | ID: wpr-309283

ABSTRACT

<p><b>OBJECTIVE</b>To study the effects of Qingxin Kaiqiao Recipe (QKR) saponin on the expressions of Bax, Bcl-2, beta-amyloid (Abeta), and beta-amyloid precursor protein (betaAPP) in the cortex and hippocampus of Alzheimer's disease (AD) rats.</p><p><b>METHODS</b>Thirty-two SD rats of SPF grade were selected. Abeta 25 - 35 was injected into the bilateral amygdala to prepare the AD model. After modeling rats were randomly divided into the model group, the donepezil hydrochloride group (Donepezil Hydrochloride Tablet, 1.67 mg/kg), the QLR group (QLR Decoction, 12.67 mL/kg), and the saponin group (saponin, 6.30 mg/kg), 8 rats in each group. Another 8 rats were selected as the normal group. Rats in the normal group and the model group were given with equal volume of double distilled water by gastrogavage. The intervention was performed once daily for 2 successive weeks. The Morris water maze test was carried out by the end of medication. The escape latency and the platform crossing times were recorded during the 1 -5 days. The expressions of Bax, Bcl-2, Abeta, and betaAPP in the cortex and hippocampus were detected using immunohistochemical assay.</p><p><b>RESULTS</b>Compared with the model group, the 3rd - 5th day escape latency were all shortened in each medication group. The expressions of Bax, Abeta, and betaAPP decreased in the cortex and hippocampus. The numbers of platform crossing increased. The expression of Bcl-2 in the cortex increased. The expression of Bcl-2 in the hippocampus increased in the donepezil hydrochloride group and the QLR group with statistical difference (P<0.01, P<0.05). Compared with the donepezil hydrochloride group, the expression of betaAPP increased in the cortex and hippocampus of the saponin group. The expression of Abeta in the cortex and hippocampus decreased, the expression of Bax in the hippocampus decreased, and the expression of Bcl-2 in the cortex increased in the QLR group. The escape latency was obviously postponed at day 3 -5, the platform crossing times decreased, the expression of Bcl-2 in the cortex and hippocampus decreased in the saponin group, showing statistical difference (P<0.05, P<0.01).</p><p><b>CONCLUSION</b>QKR could significantly improve AD rats' learning, memory, and spatial capabilities, which might be achieved through decreasing the expressions of Bax, Abeta, and betaAPP in the cerebral cortex and hippocampus, and elevating the expression of Bcl-2.</p>


Subject(s)
Alzheimer Disease , Drug Therapy , Metabolism , Amyloid beta-Peptides , Metabolism , Amyloid beta-Protein Precursor , Metabolism , Animals , Cerebral Cortex , Metabolism , Drugs, Chinese Herbal , Pharmacology , Hippocampus , Metabolism , Male , Proto-Oncogene Proteins c-bcl-2 , Metabolism , Rats , Rats, Sprague-Dawley , Saponins , Pharmacology , bcl-2-Associated X Protein , Metabolism
16.
Article in Chinese | WPRIM | ID: wpr-338057

ABSTRACT

<p><b>OBJECTIVE</b>To study the effect of qingxin kaiqiao formula and saponin on the learning and memory ability and the expression of the apoptosis signal transducers Abeta and betaAPP in AD rat brain.</p><p><b>METHOD</b>The comparative observation method was adopted for the animal test. Forty male SD rats were randomly divided into five groups, namely the normal group, the model group, the aricept group, the qingxin kaiqiao formula group and the saponin group, with eight rats in each group. Abeta(25-35) (10 g x L(-1)) was injected into their bilateral amygdala to establish the AD rat model. Since the next day, they were intragastrically administered with Aricept (1.67 mg x kg(-1)), Qingxin Kaiqiao decoction (12.67 mL x kg(-1)), saponin (6.30 mg x kg(-1)) and double distilled water filling for 2 weeks to observe their spatial memory ability in a Morris water maze and study the expression of Caspase-3, Abeta and betaAPP in brain tissues by immunohistochemistry.</p><p><b>RESULT</b>Each traditional Chinese medicine groups showed significant improvement in the learning and memory ability of AD rats and notable differences (P < 0.05, P < 0.01) compared with the control group. The qingxin kaiqiao formula group and the saponin group showed a decrease in the expressions of Caspase-3, Abeta and betaAPP in cerebral cortex and hippocampus area, displaying notable differences (P < 0.01, P < 0.05) compared with the control group.</p><p><b>CONCLUSION</b>qingxin kaiqiao formula and saponin can obviously improve the learning and memory ability of AD rats with by decreasing the expression of Caspase-3, Abeta and betaAPP in cortex and hippocampus.</p>


Subject(s)
Alzheimer Disease , Drug Therapy , Genetics , Amyloid beta-Peptides , Genetics , Animals , Apoptosis , Caspase 3 , Metabolism , Cerebral Cortex , Metabolism , Disease Models, Animal , Drugs, Chinese Herbal , Pharmacology , Hippocampus , Metabolism , Learning , Male , Maze Learning , Memory , Rats , Rats, Sprague-Dawley , Saponins , Pharmacology , Time Factors
17.
Article in Chinese | WPRIM | ID: wpr-235194

ABSTRACT

<p><b>OBJECTIVE</b>To establish a chromatography-based method for simultaneous analysis of the concentrations of amoxicillin and clavulanate potassium in human blood.</p><p><b>METHODS</b>With paracetamol as the internal control, human plasma samples, after treatment with methanol for protein sedimentation and centrifugation, were loaded for analysis with high-performance liquid chromatography (HPLC). HPLC analysis was carried out using a C18 column (5 µm, 4.6 mm×150 mm) with the mobile phase of acetonitrile-PBS (0.05 mol/L) of 10:90 (pH 2.3), UV detection wavelength of 220 nm, flow rate of 1.0 ml/min, and column temperature of 25 degrees celsius;.</p><p><b>RESULTS</b>The retention time of acetaminophen for potassium clavulanate, amoxicillin sodium and the internal control was 5.3, 7.2, and 8.5 min, respectively, and no interference by the endogenous impurities in the plasma samples was found. Amoxicillin sodium showed a good linearity within the concentration range of 0.52-4.16 µg/ml (r(2)=0.9996), and potassium clavulanate had a good linearity within the range of 0.266-2.14 µg/ml (r(2)=0.9998). The minimum detectable concentrations of amoxicillin sodium and potassium clavulanate were 0.065 µg/ml and 0.066 µg/ml, respectively. The relative recoveries of amoxicillin sodium were 95.9%-96.5% (n=5), and those of clavulanate potassium were 92.5%-98.8% (n=5); the intra- and inter-day RSD of amoxicillin sodium was 1.84%-6.4% and 2.1%-7.8%, as compared to that of potassium clavulanate of 3.57%-8.6% and 1.8%-9.1%, respectively.</p><p><b>CONCLUSION</b>This method is simple, accurate, sensitive, specific and reproducible for analyzing the concentrations of amoxicillin and clavulanate potassium simultaneously in human plasma.</p>


Subject(s)
Amoxicillin , Blood , Chromatography, High Pressure Liquid , Methods , Clavulanic Acid , Blood , Drug Stability , Humans
18.
Article in Chinese | WPRIM | ID: wpr-336195

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effect of bortezomib on the apoptosis and drug sensitivity of endometrial cancer cell line Ishikawa cells.</p><p><b>METHODS</b>The IC50 of bortizomib, ADR, DDP and PTX in Ishikawa cells was determined using MTT method. After treatment with IC50 bortezomib for 6 and 12 h, the expressions of caspases-3, caspases-9 and bcl-2 genes were detected by RT-PCR, and the cell apoptotic rate and ROS level Ishikawa cells were evaluated by flow cytometry after treatment with half of the IC50 of the drugs for 24 h.</p><p><b>RESULTS</b>The IC50 of bortizomib, ADR, DDP, and PTX was 71.6 nmol/L, 0.572 micromol/L, 67.4 micromol/L and 719.5 nmol/L, respectively. Bortizomib significantly increased the mRNA expressions of caspases-3 and caspases-9 but decreased the expression of bcl-2. Compared with the treatment with agents alone, combined treatment of the cells significantly improved the cytotoxicity of the chemotherapeutic agents (P<0.05) and increased the ROS level and the apoptosis of the cells.</p><p><b>CONCLUSION</b>Bortizomib can inhibit the protein kinase to induce the apoptosis and enhance the chemosensitivity of Ishikawa cells.</p>


Subject(s)
Antineoplastic Combined Chemotherapy Protocols , Pharmacology , Apoptosis , Boronic Acids , Pharmacology , Bortezomib , Caspase 3 , Metabolism , Caspase 9 , Metabolism , Cell Line, Tumor , Drug Synergism , Endometrial Neoplasms , Pathology , Female , Humans , Inhibitory Concentration 50 , Protease Inhibitors , Pharmacology , Proto-Oncogene Proteins c-bcl-2 , Metabolism , Pyrazines , Pharmacology , Reactive Oxygen Species , Metabolism
19.
Article in Chinese | WPRIM | ID: wpr-268752

ABSTRACT

<p><b>OBJECTIVE</b>To investigate the effects of alpha-keto acid on the expression of neuropeptide Y in malnutrition rats with chronic renal failure.</p><p><b>METHODS</b>SD rats received 5/6 nephrectomy and were fed with 4% casein to establish models of malnutrition with chronic renal failure. Serum albumin, urea nitrogen, serum creatinine, type-1 insulin like growth factor and body weight of the rats were measured. The rat models were randomized into chronic renal failure group, alpha-keto acid group and normal control group, and after a 4-week treatment as indicated, neuropeptide Y mRNA levels in the hypothalamus were measured by RT-PCR in rats with surgically induced renal failure (two-stage subtotal nephrectomy). The blood neuropeptide Y of the rats were analyzed by radioimmunoassay.</p><p><b>RESULTS</b>Malnutrition occurred in chronic renal failure rats at the end of 10 weeks. Compared with those in the chronic renal failure group, the plasma neuropeptide Y concentrations in alpha-keto acid group were significantly lowered with substantially elevated neuropeptide Y mRNA expression in the hypothalamus.</p><p><b>CONCLUSION</b>alpha-keto acid capsule can improve malnutrition in rats with renal insufficiency possibly by up-regulating neuropeptide Y mRNA expression in the hypothalamus and reducing the level of blood neuropeptide Y.</p>


Subject(s)
Animals , Hypothalamus , Metabolism , Keto Acids , Pharmacology , Therapeutic Uses , Kidney Failure, Chronic , Blood , Male , Malnutrition , Blood , Drug Therapy , Neuropeptide Y , Blood , RNA, Messenger , Genetics , Rats , Rats, Sprague-Dawley
20.
Article in Chinese | WPRIM | ID: wpr-270153

ABSTRACT

<p><b>OBJECTIVE</b>To observe the effect of small interfering RNA (siRNA) targeting multidrug resistance-related protein (MRP) and bcl-2 genes in modulating drug resistance and apoptosis of K562 and K562/ADM cells.</p><p><b>METHODS</b>Two siRNA constructs targeting respectively bcl-2 and MRP genes, were synthesized and transfected either alone or in combination into K562 and K562/ADM cells via lipofectamine2000. MTT assay was used to evaluate the viability of the transfected cells at 24, 48 and 72 h Post-fransfection, and RT-PCR was performed to determine the mRNA levels of bcl-2 and MRP. The effects of MRP siRNA and bcl2 siRNA on the apoptosis and the protein expression of Bcl-2 and MRP were evaluated with flow cytometry.</p><p><b>RESULTS</b>In K562/ADM cells, the IC (50) decreased from 12.81 microg/ml (ADM group) to 3.74 microg/ml (ADM+MRP siRNA group), 6.82 microg/ml (ADM+bcl2 siRNA group) and 2.51 microg/ml (ADM+MRP siRNA+bcl2 siRNA). Similarly, in K562 cells, the IC50 decreased significantly from 6.75 microg/ml (ADM) to 3.22 microg/ml (ADM+MRP siRNA), 3.56 microg/ml (ADM+bcl2 siRNA) and 1.84 microg/ml (ADM+MRP siRNA+bcl2 siRNA) (P<0.05). Flow cytometry demonstrated significantly increased apoptosis of the cells following MRP siRNA and bcl2 siRNA transfection, which also resulted in significantly decreased expressions of MRP and bcl-2 proteins (P<0.05).</p><p><b>CONCLUSION</b>Treatment with both MRP and bcl-2 siRNAs inhibits the target gene expression, and increases the drug sensitivity and apoptosis of K562 and K562/ADM cells.</p>


Subject(s)
ATP Binding Cassette Transporter, Subfamily B , Genetics , Apoptosis , Genetics , Doxorubicin , Pharmacology , Drug Resistance, Neoplasm , Genetics , Humans , K562 Cells , Proto-Oncogene Proteins c-bcl-2 , Genetics , RNA, Small Interfering , Genetics , Transfection
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