ABSTRACT
Four unreported monoterpene indole alkaloids, tabernaecorymines B-E (1-4), together with twenty-one known indole alkaloids (5-25) were obtained from the stem bark of Tabernaemontana corymbosa. Their structures and absolute configurations were elucidated by extensive spectroscopy, quantum chemical calculations, DP4+ probability analyses and Mo2(OAc)4-induced electronic circular dichroism experiment. The antibacterial and antifungal activities of these compounds were evaluated and some of them showed significant activity against Staphylococcus aureus,Bacillus subtilis, Streptococcus dysgalactiae and Candida albicans.
Subject(s)
Tabernaemontana , Anti-Infective Agents , Antifungal Agents , Anti-Bacterial Agents , Indole AlkaloidsABSTRACT
OBJECTIVE To analyze quality maker （Q-marker） of Ka nggongyan soft capsule （KSC）. METHODS The fingerprints of 20 batches of KSC were established by ultra high performance liquid chromatography （UPLC）method. Similarity Evaluation System of TCM Chromatographic Fingerprint （2012 edition）were used to evaluate the similarity and confirm common peaks. The contents of norisoboldine ，leonurine hydrochloride ，forsythoside B ，acteoside，poliumoside and isoacteoside were determined by the same UPLC method. Targets and pathways related to KSC in the treatment of cervicitis were screened and analyzed by network pharmacology and molecular docking method to construct a “component-target-pathway”network，and analyze its potential Q-marker. RESULTS Twelve common peaks were identified in the fingerprints of 20 batches of KSC ，and the similarity was greater than 0.99. Six common peaks were identified ，including norisoboldine ，leonurine hydrochloride ，forsythoside B，acteoside，poliumoside and isoacteoside. The contents of the above 6 components were 1.336-1.774，0.093-0.143，4.970-5.888， 0.505-0.623，5.206-6.226 and 0.785-0.895 mg/g，respectively. By network pharmacology analysis ，14 key targets and 94 pathways were obtained ，and their binding energies to the core targets （protein kinase B 1，tumor necrosis factor ）were all less than －6.4 kJ/cal. CONCLUSIONS Six components such as norisoboldine and leonurine hydrochloride are potential Q-marker of KSC.
ABSTRACT
BackgroundDysimmunity plays a key role in diabetes, especially type 1 diabetes mellitus. Islet-specific autoantibodies (ISAs) have been used as diagnostic markers for different phenotypic classifications of diabetes. This study was aimed to explore the relationships between ISA titers and the clinical characteristics of diabetic patients.MethodsA total of 509 diabetic patients admitted to Department of Endocrinology and Metabolism at the Affiliated Hospital of Nantong University were recruited. Anthropometric parameters, serum biochemical index, glycosylated hemoglobin, urinary microalbumin/creatinine ratio, ISAs, fat mass, and islet β-cell function were measured. Multiple linear regression analysis was performed to identify relationships between ISA titers and clinical characteristics.ResultsCompared with autoantibody negative group, blood pressure, weight, total cholesterol (TC), low density lipoprotein cholesterol (LDL-C), visceral fat mass, fasting C-peptide (FCP), 120 minutes C-peptide (120minCP) and area under C-peptide curve (AUCCP) of patients in either autoantibody positive or glutamate decarboxylase antibody (GADA) positive group were lower. Body mass index (BMI), waist circumference, triglycerides (TGs), body fat mass of patients in either autoantibody positive group were lower than autoantibody negative group. GADA titer negatively correlated with TC, LDL-C, FCP, 120minCP, and AUCCP. The islet cell antibody and insulin autoantibody titers both negatively correlated with body weight, BMI, TC, TG, and LDL-C. After adjusting confounders, multiple linear regression analysis showed that LDL-C and FCP negatively correlated with GADA titer.ConclusionDiabetic patients with a high ISA titer, especially GADA titer, have worse islet β-cell function, but less abdominal obesity and fewer features of the metabolic syndrome.
ABSTRACT
BackgroundDysimmunity plays a key role in diabetes, especially type 1 diabetes mellitus. Islet-specific autoantibodies (ISAs) have been used as diagnostic markers for different phenotypic classifications of diabetes. This study was aimed to explore the relationships between ISA titers and the clinical characteristics of diabetic patients.MethodsA total of 509 diabetic patients admitted to Department of Endocrinology and Metabolism at the Affiliated Hospital of Nantong University were recruited. Anthropometric parameters, serum biochemical index, glycosylated hemoglobin, urinary microalbumin/creatinine ratio, ISAs, fat mass, and islet β-cell function were measured. Multiple linear regression analysis was performed to identify relationships between ISA titers and clinical characteristics.ResultsCompared with autoantibody negative group, blood pressure, weight, total cholesterol (TC), low density lipoprotein cholesterol (LDL-C), visceral fat mass, fasting C-peptide (FCP), 120 minutes C-peptide (120minCP) and area under C-peptide curve (AUCCP) of patients in either autoantibody positive or glutamate decarboxylase antibody (GADA) positive group were lower. Body mass index (BMI), waist circumference, triglycerides (TGs), body fat mass of patients in either autoantibody positive group were lower than autoantibody negative group. GADA titer negatively correlated with TC, LDL-C, FCP, 120minCP, and AUCCP. The islet cell antibody and insulin autoantibody titers both negatively correlated with body weight, BMI, TC, TG, and LDL-C. After adjusting confounders, multiple linear regression analysis showed that LDL-C and FCP negatively correlated with GADA titer.ConclusionDiabetic patients with a high ISA titer, especially GADA titer, have worse islet β-cell function, but less abdominal obesity and fewer features of the metabolic syndrome.
ABSTRACT
Background@#Dysimmunity plays a key role in diabetes, especially type 1 diabetes mellitus. Islet-specific autoantibodies (ISAs) have been used as diagnostic markers for different phenotypic classifications of diabetes. This study was aimed to explore the relationships between ISA titers and the clinical characteristics of diabetic patients. @*Methods@#A total of 509 diabetic patients admitted to Department of Endocrinology and Metabolism at the Affiliated Hospital of Nantong University were recruited. Anthropometric parameters, serum biochemical index, glycosylated hemoglobin, urinary microalbumin/creatinine ratio, ISAs, fat mass, and islet β-cell function were measured. Multiple linear regression analysis was performed to identify relationships between ISA titers and clinical characteristics. @*Results@#Compared with autoantibody negative group, blood pressure, weight, total cholesterol (TC), low density lipoprotein cholesterol (LDL-C), visceral fat mass, fasting C-peptide (FCP), 120 minutes C-peptide (120minCP) and area under C-peptide curve (AUCCP) of patients in either autoantibody positive or glutamate decarboxylase antibody (GADA) positive group were lower.Body mass index (BMI), waist circumference, triglycerides (TGs), body fat mass of patients in either autoantibody positive group were lower than autoantibody negative group. GADA titer negatively correlated with TC, LDL-C, FCP, 120minCP, and AUCCP.The islet cell antibody and insulin autoantibody titers both negatively correlated with body weight, BMI, TC, TG, and LDL-C. After adjusting confounders, multiple linear regression analysis showed that LDL-C and FCP negatively correlated with GADA titer. @*Conclusion@#Diabetic patients with a high ISA titer, especially GADA titer, have worse islet β-cell function, but less abdominal obesity and fewer features of the metabolic syndrome.
ABSTRACT
OBJECTIVE：To isolate and purify baicalin metabolites from rat bile ，and to study its effect on the proliferation of liver cancer HepG 2 cells. METHODS ：Totally of 6 SD rats were collected ，anesthetized and then intubated with bile ducts. They were given baicalin （168 mg/kg）intragastrically after the rats were awake as well as the bile sample 1 was collected during 24 h after intragastric administration. After processed ，bile sample 1 was preliminarily analyzed by HPLC. Another 5 SD rats were anesthetized and intubated in the same way as above ，and then given baicalin intragastrically （400 mg/kg）. The bile sample 2 was collected during 48 h after intragastric administration. After processed ，the bile sample 2 was isolated and purified by semi-preparative HPLC. The isolated metabolites were identified by using UV ，IR，MS and NMR ，as well as based on physical and chemical properties. MTT method combined with high content cell imaging analysis system was used to study the effect of the metabolites on the proliferation of HepG 2 cells. RESULTS ：Baicalin was mainly metabolized into metabolite 1 and metabolite 2 through bile. After isolation and purification ， they were identified as oroxylin A- 7-O-β-D-glucuronide and 2726719792@qq.com baicalein 6-O-β-D-glucuronide. The results of MTT assay showed that the metabolite 2 had a significant inhibitory effect 分析。E-mail：gaoxl@gmc.edu.cn on the proliferation of HepG 2 cells，and its IC 50 was 90 µg/mL；the results of high content cell imaging analysis showed that at a certain concentration metabolite 2 may inhibit proliferation by changing the mitochondrial distribution and membrane permeability of HepG 2 cells（studies on the pharmacological activities of metabolism 1 had been reported ，it was skipped in this study ）. CONCLUSIONS ：In this study ，two baicalin bile metabolites were successfully isolated and identified ，of which baicalein 6-O-β-D-glucuronide has a significant inhibitory effect on the proliferation of HepG 2 cells.
ABSTRACT
Objective To investigate the protective effects of stilbene glycoside(2,3,5,4'-tetrahydroxy-stilbene-2-O-β-D-glucoside,TSG) on 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced mice model of Parkinson's disease(PD).Methods Mice were randomly divided into the blank control group,the negative control group,the TSG high-dose group,the TSG low-dose group and the positive drug group(n=20 each).Mice were weighted daily to observe the changes of body weight,and mice motor and behavior function were tested by open field test.Level changes of α/β synuclein in brain cortex,cerebellum,midbrain,and hippocampal were detected by Western blot.Results Compared with the blank control group,the negative control group showed that the body weight was decreased (P ＜ 0.05).Compared with the negative control group,the body weight was increased in the TSG high-and low-dose groups and the positive drug group (P ＜ 0.05).The spontaneous behavior was impaired in the negative control group.Compared with the blank control group,the negative control group showed that the open field test showed traveled distance over a 10-min period was significantly shortened at 1 st,7th,28th days after testing(all P＜0.05).The trajectory of motor axons indicated that mice in the negative control group showed dyskinesia,but the groups of positive drug and high-and low-dose of TSG could reverse this dyskinesia.Compared with the blank control group,brain α/β synuclein protein levels were increased in the negative control group,and decreased in positive drug and TSG high-and low-dose groups (P ＜0.05).Conclusions Stilbene glycosides exert neuroprotective effects in MPTP-induced mice model of PD.
ABSTRACT
Viral infection is the main death cause of infectious diseases in China. The establishment of an animal model to mimic the progression of viral infectious diseases in humans is of great significance to the study of pathogenesis and prevention of viral infectious diseases. As a new animal model established and developed in recent years, tree shrew has showed obvious advantages and potentials compared with other non-human primates and mice which are commonly used as virus-infected animal models. In this paper, the biological advantages of tree shrew as a novel animal model of viral infectious diseases are summarized, including taxonomy, physiology and immunology. In addition, the latest application of tree shrew in the research of many viral infectious diseases such as hepatitis virus, herpes simplex virus, influenza virus and enterovirus infections are compared and summarized.
ABSTRACT
Objective To analyze the neuroimaging changes of tree shrew models of Alzheimer’ s disease.Methods Nineteen healthy adult female tree shrews were randomly divided into control (5 animals) and model group (14 animals). The model of Alzheimer’s disease was induced by intracerebroventricular injection of Aβ1-40 using a stereotaxic devise and proved successfully by visuospatial congnitive task.The in vivo microstructural changes in the brain of tree shrew AD models and control group (0, 1, 2, 3, 4 weeks) were observed on 1.5T MRI (T2WI), and on 7.0T MRI (12 week)(T2WI, DTI). Results Reference memory errors were increased in the model group at 3 or 4 weeks (P<0.05), and so working memory errors (P<0.05) and period of time to perform (P<0.05, P<0.05, P<0.01) from 2 to 4 weeks.Thus the model was proved to be established successfully.T2WI test and DTI test were carried out.Hippocampus atrophy of the model group at 3 and 4 weeks was observed compared with that at 0 or 1 week or 2 weeks on a 1.5T Philips Gyroscan.Compared with the control group, the temporal horn width in the model group was significantly increased (P<0.01) at 12 weeks on a 7.0T Bruker Biospec Scanner.DTI test at 12 weeks showed that ADC of bilateral hippocampus was up-regulated in the model group ( P<0.01 ) .In the color coded orientation view, loss of the corpus callosum fibers was obvious in the model group. Conclusions Intracerebroventricular injection of Aβ1-40 can lead to learing and memory impairment in tree shrews.There are abnomal MRI signal changes in the brain, and the temporal horn width, hypocampal apparent diffusion coefficient ( ADC) value and corpus callosum damage may provide reference value for the diagnosis of Alzheimer’ s disease.
ABSTRACT
Objective To investigate the anti-tumor effects of total saponins,extracted from stems and leaves ofParispolyphyllavar.yunnanensis. Methods Taking mouse stomach carcinoma MFC cell line,human mammary cancer cell line(MCF-7)and human cervical carcinoma cell line(Hela),and their tumor-bearing mice as models,the antitumor activity was carried out in vitro and in vivo. CCK-8 assay was used to determine the inhibitory effect in vitro. The tumor-bearing mice model was induced by tumor cell vaccination in normal mouse forelimb left axillary subcutaneous and these mice were randomized into NS group,cytoxan group(30 mg/kg),saponins high-dose,medium-dose and low-dose groups(60,30 and 15 mg/kg). They were given intraperitoneal injection once a day for consecutive 15 days. The tumor inhibition rate and survival of the tumor-bearing mice were measured. Results Saponins,extracted from both aboveground and underground ofP.polyphyllavar.yunnanensis could significantly inhibit the growth of MFC,MCF-7 and Hela cells in time- and dose-dependent manners. The tumor weight in each drug treated group was significantly lower than that in the control group. Conclusion Saponins,extracted from both aboveground and underground ofP.polyphyllavar.yunnanensis have antitumor activity.
ABSTRACT
Objective To evaluate the protective effects of Rosemary's chloroform extract on cerebral ischemia in mice and acute toxicity.Methods The protective of rosemary's chloroform extract on cerebral ischemia was observed and compared by the mice models of cerebral anoxia and ischemia,thrombus formation in vivo,and chloroform induced arrhythmias.Rosemary's Chloroform Extract was given orally to mice to evaluate acute toxicity.Results Rosemary's chloroform extract had different degrees of inhibition of collagen-the adrenaline induced thrombus formation,and prolonged acute ischemic mice brains off mouth breathing time and increase the number of mouth breathing (P ＜0.05 or P ＜0.01);Chloroform extract significantly reduced the incidence of chloroform induced ventricular arrhythmias.Acute toxicity results suggested that a female rat died in the next day of chloroform extract group,no additional toxicity was observed.Conclusion Rosemary's chloroforrm extract has significant protective effect on cerebral ischemia and hypoxia in mice.
ABSTRACT
Objective To investigate the expression levels of BDNF, trkB and ChAT mRNA and proteins in the brain of adult tree shrews ( Tupaia belangeri ) .Methods Quantitative real-time PCR was employed to detect the expression levels of BDNF, trkB and ChAT mRNA in the hippocampus, basal ganglia and frontal cortex of adult tree shrews.The expression levels of BDNF, trkB and ChAT proteins andβ-actin was used as internal standard.Results The expression level of BDNF mRNA was highest in the hippocampus of adult tree shrew, and there were significant differences between that in the hippocampus, and basal ganglia and frontal cortex (P0.05) in the expressions of trkB protein among the hippocampus, basal ganglia and frontal cortex of the adult tree shrews.There were no significant differences in expressions of ChAT mRNA and protein among the hippocampus, basal ganglia and frontal cortex in adult tree shrews ( P>0.05 ) . Conclusions The expression levels of ChAT mRNA were consistent with that of ChAT protein in the hippocampus, basal ganglia and frontal cortex of adult tree shrews, while the expression levels of BDNF and trkB mRNA were not consistent with their proteins, which might indicate that the transcriptional regulation pattern might be more complex.Tree shrew is a valuable animal model in the study of mechanism of BDNF/trkB gene expression.
ABSTRACT
Objective To evaluate the effect of the fast control scheme of schistosomiasis.Methods The fast control scheme of schistosomiasis was carried out,and the scheme mainly included dusting molluscicide,rapid immunodiagnosis screening and chemotherapy with praziquantel,environment modification,health education,etc.The control effects of the scheme were observed longitudinally.Results There were no infected snails found after the scheme was implemented from 2005 to 2008.The densities of living snails dropped from 1.48 snails/0.1 m~2 in 2004 to 0.71 snails/0.1 m~2 in 2008.The areas with snails dropped from 43.13 hm~2 in 2004 to 33.68 hm~2 in 2008.The infection rates of residents and cattle dropped to 0 in 2008.Conclusion The fast control scheme of schistosomiasis can control schistosomiasis fast.
ABSTRACT
<p><b>OBJECTIVE</b>To investigate the antioxidant and cytotoxic properties of five diarylheptanoids (1-5) isolated from the rhizomes of Zingiber officinale.</p><p><b>METHOD</b>Various models such as scavenging superoxide anions and 1,1-diphenyl-2- picrylhydrazyl (DPPH) radicals, inhibiting lipid peroxidation, as well as protecting of rat pheochromocytoma (PC12) cells induced by hydrogen peroxide (H2O2) were employed to assay the antioxidative effects of the diarylheptanoids. The cytotoxicities of compounds 1-5 were measured with MTT assays.</p><p><b>RESULT</b>The test compounds (1-5) showed promising DPPH inhibitory activities, and compound 5 exhibited the strongest DPPH scavenging activity with an IC50 value of (22.6+/-2.4) micromol x L(-1). Compounds 1, 3 and 4 showed potential anti-peroxidative effects with inhibitory rates of (66.3+/-15.4)%, (68.7+/-15.8)% and (72.2+/-10.6)%, respectively, at 100 microg x mL(-1). It could be observed that compounds 1, 3 and 4 demonstrated significant neuroprotective activities in a dose-dependent manner. Moreover, compound 3 exhibited certain cytotoxicities against human chronic myelogenous leukemia cells (K562) and its adriamycin-resistant cells (K562/ADR) with IC50 values of (34.9+/-0.6), (50.6+/-23.5) micromol x L(-1), respectively.</p><p><b>CONCLUSION</b>In vitro results demonstrated that five diarylheptanoids (1-5) isolated from the roots of Z. officinale were capable of scavenging radicals, inhibiting lipid peroxidation and protecting PC12 cells against the insult by H2O2. Additionally, compound 3 could inhibit the growth of K562 and K562/ADR cells.</p>
Subject(s)
Animals , Humans , Rats , Antioxidants , Toxicity , Cell Proliferation , Cytotoxins , Toxicity , Diarylheptanoids , Metabolism , Toxicity , Free Radicals , Metabolism , Ginger , Chemistry , Hydrogen Peroxide , Metabolism , K562 Cells , Oils, Volatile , Pharmacology , PC12 Cells , Rats, Sprague-DawleyABSTRACT
Object To develop and utilize a folk-medicine of Yunnan Province, Lethariella cladonioides (Nyl.) Krog. Methods The constituents were extracted with 80% ethanol and isolated with silica gel column chromatography. The structures were identified by physicochemical properties and spectral analysis. Results Two unknown constituents were elucidated from the extract as 3-aldehyde-6-methyl-2, 4-dihydroxy-ethyl-benzoate (Ⅰ), and 4-methyl-2, 6-dihydroxy-benzaldehyde (Ⅱ). Conclusion They are both new constituents obtained firstly.
ABSTRACT
Object To study the protective effect of Rodobryum roseum (Hedw) Limpr. on acute myocardial ischemia. Methods Rat acute myocardial ischemia models were prepared by ligating their left coronary arteries. Changes of their S-T segment was observed on lead Ⅱ dynamic ECG. Degree of ischemia was assessed by the extent of S-T segment elevation. Lactic dehydrogenase (LDH), creative phosphokinase (CPK), superoxide dismutase (SOD) and malondialdehyde (MDA) were determined at the same time. Results R. roseum can significantly alleviate S-T segment elevation, being most evident at the dose of 2 g/kg (P