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Aim To investigate TY501′s role in bleo-mycin ( BLM )-induced pulmonary fibrosis in rats. Methods Forty rats were randomly divided into 5 groups, including the sham operation, BLM, PFD, TY501(high and low dose) groups. After administra-tion of BLM intratracheally, PFD and TY501 were giv-en in each group daily, according to the dosage de-signed during 21 days. Lung coefficient, PaO2 were tested before killing the rats. The contents of ALB, ALP, LDH, GSH, HYP were detected by regent kit respectively. PCⅢ and COL4 were determined by ELISA. Results ( 1 ) Some indicators of alveolitis in early stage of IPF: the contents of lung coefficient in three treatment groups were lower and PaO2 was higher than those in BLM group ( P<0. 05 ); compared with BLM group, the contents of ALB, ALP, LDH in the treatment groups reduced on 21 st day ( P<0. 05 );the expression of GSH in BLM group was increased for feedback regulation and higher than the treatment groups and the sham operation group (P<0. 05);(2) some indicators of pulmonary interstitial fibrosis in late stage of IPF:the expressions of HYP, PCⅢand COL4 were reduced after the treatment. There were signifi-cant differences compared with BLM group ( P <0. 05 ) . Conclusions TY501 is valuable for the ther-apy of IPF, the same as the positive drug pirfenidone. TY501 attenuates BLM-induced pulmonary fibrosis, which may be related to the affection of TGF-βpathway and inhibition of MMPs.
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Erythropoietin (EPO) is an active glycoprotein synthesized by kidney. The physiological function of regulat?ing the synthesis of erythrocytes by EPO makes it as a clinical drug for treatment of anemia resulted from chronic kidney fail?ure. However, its short biological half-life makes frequent administration, which limits its wide clinical utility since the tough burden and pain on patients. Therefore, the development of EPO derivatives with good efficacy, less adverse reaction and long duration has been a hot spot in the field during several decades. There are currently many different variants of EPO derivatives including erythropoiesis stimulating agents (ESAs) on the market. This article aims to summarize the recent re?search progress in the development of erythropoietin derivatives, specially focusing on EPO mimetic peptides (EMP).
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Objective To investigate the protective effects of purified effective component group in extract from Xiaoshuan Tongluo(CGXT)formula on chronic brain ischemia in rats.Methods CGXT 75,150,and 300 mg/kg or vehicle were ig administered daily for four weeks to rats with bilateral common carotid arteries ligation(BCCAL).From the day 24 to 28 after BCCAL,Morris water maze was performed to assess the learning and memory impairment of rats.Four weeks after BCCAL,brain gray and white matter damage were assessed.Results In Morris test,the mean escape latency of rats in the CGXT(150 and 300 mg/kg)groups was significantly shorter than that in the vehicle group.CGXT also attenuated the neuronal damage in hippocampus and cortex and reduced the pathological damage in the optic tract and corpus callosum.Conclusion CGXT could improve learning and memory impairment resulted from BCCAL in rats.These results provide the experimental basis for the clinical use of CGXT in stroke treatment and may help in investigation of multimodal therapy strategies in ischemic cerebrovascular diseases including stroke.
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Objective To elucidate potential activities of phthalides and terpenoids from Angelica sinensis by theoreticaldocking calculation.Methods Eleven components of phthalides and terpenoids were selected as ligand.Thecrystalline structures of targets related to common diseases were used as the receptors for calculation.Thecalculations were conducted with Schr(o)dinger software package.The grading standard of selectivity was developedaccording to G-score between ligands and receptors.Results Selective targets of phthalides and terpenoids wererelated to nevous system diseases,cancer,pain,diabetes,cardiovascular disease,liver cirrhosis,nephrotic syndrome,inflammatory diseases,rheumatoid arthritis,dermatosis,leukemia,microbial inflections,immune diseases,andhypercholesterolemia.In addition to the medical treatments reported in the literature,our research also indicated thatthese two classes of compounds may be used for tumor,diabetes,rheumatoid arthritis,dermatosis,leukemia,livercirrhosis,and nephrotic syndrome.According to our research,the effects of phthalides and terpenoids may be not sostrong.Conclusion The effects of phthalides and terpenoids on diseases founded through virtual evaluation accord greatly with those reported in experiment and clinic.The combination of computer-aided drug evaluation technique and experiment is definitely an important and fast way to investigate the effects and mechanisms of traditional Chinese medicine.
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Objective Astrgaloside Ⅳ derivative (ASId) is one of Astragaloside Ⅳ (ASI) derivatives with higher water-solubility and may have more druggability than ASI. The present study aims at observing the effects of ASId on cardiovascular parameters in chronic heart failure in rats. Methods Using echocardiographic and haemodynamic measurements, the effects of ASId on congestive heart failure (CHF) induced by ligation of the left coronary artery in rats were investigated.ventricle (LV) pressure (dp/dt) in ASId treated groups were significantly increased. Both LV volumes in diastole and in systole were decreased significantly after ASId treatment, accompanied with a trend towards normalization of relative stress. ASId treatment also inhibited compensatory hypertrophy of depressed heart. Conclusion ASId could improve cardiac functions and inhibite compensatory hypertrophy and LV remodelling, which suggests the possibility of ASId as a new therapeutic drug for the treatment of CHF.
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Objective To explore the investigation method of complicated and profound traditional Chinese herbal medicine,the potential action mechanisms of flavonoids from Scutellaria baicalensis were studied by docking calculation.Methods In total, eight flavonoids (aglycones and their glicosides) from S. baicalensis were selected as ligands.The crystalline structures of targets related to common diseases were used as the receptors for calculation. The calculations were conducted with Schr(o)dinger software package. The grading standard of selectivity was developed according to G-score between ligands and receptors. Results Twenty-six pharmacologic actions have been reported.Among all effects in literature, nine of them can be deduced from the docking calculation of aglycone. From glycosides with grade ++, 25 reported effects can be estimated by calculation. Apparently, the target selectivity of aglycones and their glycosides are different form the virtual evaluation. The virtual evaluation results of glycosides were closer to the reported effects. Conclusion Our proposed virtual evaluation method seems an effective way to investigate the complicated system of traditional Chinese herbal medicine. It suggests that aglycones may be effective as the form of glucoside in vivo, and metabolism is a very important factor for virtual evaluation.
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<p><b>OBJECTIVE</b>To examine the effects of procaine and lidocaine on intracellular Ca(2+) release from sarcoplasmic reticulum ryanodine-sensitive Ca(2+) stores.</p><p><b>METHODS</b>The experiment was performed on hippocampal slices from 60-80 g male Mongolian gerbils. Levels of intracellular Ca(2+) concentration in the slices were measured by microfluorometry. The slices were perfused with 50 mmol/L KCl containing medium for 30 seconds. Then, the medium was switched to physiological medium. After 5 min of incubation, the slice was perfused with 20 mmol/L caffeine containing physiology medium for 2 min. Following incubation, the slice was superfused with physiological medium until the end of the experiment. The effects of procaine and lidocanin (100 micro mol/L) on caffeine-evoked Ca(2+) release were evaluated by adding them to the medium after high K(+) medium perfusion.</p><p><b>RESULTS</b>Caffeine induced a marked increase in intracellular Ca(2+) concentration which was then decreased 12% upon the addition of procaine (P < 0.05); however, lidocaine, did not induce a similar inhibitory reaction.</p><p><b>CONCLUSION</b>Procaine inhibits ryanodine-receptor mediated Ca(2+) release from intracellular Ca(2+) stores, while lidocaine may inhibit Ca(2+) release through other mechanisms.</p>
Subject(s)
Animals , Male , Anesthetics, Local , Pharmacology , Calcium , Metabolism , Gerbillinae , Hippocampus , Metabolism , Lidocaine , Pharmacology , Procaine , Pharmacology , Ryanodine , Pharmacology , Ryanodine Receptor Calcium Release Channel , PhysiologyABSTRACT
With DQOL (diabetes quality of life) scale, quality of life was evaluated before and after diabetic education in 136 type 2 diabetic patients. The Cronbach′s ? of DQOL scale was from 0.809 to 0.849, suggesting that the DQOL scale did effectively reflect the life quality of type 2 diabetic patients.
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Linaoxin, a herhal preparatlon composed of Salvia miiltiorrhiza, Ligusticum wallichii,Pueraria lobata,and Polygonum multiflorum etc., at doses of O. 25 and o. 5g/kg (ig)significantly improved the neural symptoms of experimental cerehral infarction and reduced the size of infarcted area in rats. At the same doses it also significantly prolonged the hreathing time of mice after decapitation and showed effects on brain energyrnetabolism including the increase of brain ATP and phosphocreatine (Pcr)leveIs and decrease of brain lacticacid (LA)level. Linaoxin suspension at concentrations of l:
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A simple, rapid and sensitive method for reversed phase HPLC determination of N-acetyl-L-tryptophan (N-ATRP) and its metabolite L-tryptophan (TRP) in rabbit serum was developed based on their intrinsic fluorescence using excitation and emission wavelengths of 280 and 360 nm, respectively. The separation of two amino acids was achieved on an ODS C18 column with a mobile phase of 0. 1 mol ?L-1 NaAc-25% methanol (pH 5. 7) at a flow rate of 0. 5 ml ?min-1. The calibration curves for N-A-TRP and TRP provided the linear range about1.0 - 17. 0mg ?L-1(r=0. 9962 and 0.9978, respectively). The recoveries greater than 98% and good reproducibility were achieved with rabbit serum. The concentration-time curve of N-ATRP after iv administration was determined in rabbits. Results showed that N-ATRP was quickly converted to TRP with a half-life of 8. 5 min. The decrese of N-ATRP accorded well with the rise of TRP.
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Objective To investigate the effects of control status scale for diabetes (CSSD70), designed by diabetes center of Ruijin Hospital, in type 2 diabetes patients. Methods The correlations between CSSD70 and age, gender, duration of diabetes, educational backgrounds, insulin use, instruments for diabetes control, diabetes family history, symptoms at the onset of diabetes, complications, random plasma glucose and HbA_(1c) were analysed in 136 type 2 diabetes patients. The correlation between CSSD70 and another national questionnaires DQOL was analysed, and in order to determine the validity and stability of CSSD70, 30 patients were asked to complete the scales twice within one week. Results The coherent results in CSSD70 and DQOL were obtained, but CSSD70 was more comprehensive and sensitive. Almost all factors included in this study were related to CSSD70 total score and sub-scale score. The stability of CSSD70 was fine, and a close relationship between total score and sub-scale score was found. Conclusion The CSSD70 appears to be a good scale in evaluating the functional health status in type 2 diabetes, and is suitable for Chinese patients in evaluating diabetes control.
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The relationships of therapeutic regime, glycemic control and quality of life with depression were observed in 193 type 2 diabetic patients. The results showed that 46.6% of the diabetic patients manifested depression in various degrees; the depression status was correlated with age or duration of diabetes; the patients under insulin treatment showed more marked depression than the other patients (P