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Six new cytochalasans-namely, aspergicytochalasins A-F (1-6)-together with five known analogs were isolated and characterized from the endophytic fungus Aspergillus sp. from the medicinal plant Lonicera japonica. The structures of the new compounds were established by NMR and MS methods as well as single crystal X-ray diffractions. Compounds 3 and 4 showed weak antibacterial activities to Staphylococcus aureus, with MIC values of 128 and 64 µg/mL, respectively. Compounds 1, 3, 5 and 6 showed inhibitory activities on NO production, with IC50 values less than 40 µM.
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OBJECTIVE@#To observe the effect of acupuncture at "Feishu" (BL 13) + "Dingchuan" (EX-B 1) and "Kongzui" (LU 6) + "Yuji" (LU 10) for the airway remodeling in asthma rats based on the transforming growth factor-β1 (TGF-β1)/ Smad family member 3 (Smad3) signaling pathway; and explore the efficacy difference between the two acupoint combinations.@*METHODS@#Forty SPF male SD rats, aged 4 weeks, were randomly divided into a blank group (n = 10) and a modeling group (n = 30). The ovalbumin (OVA) sensitization method was used to establish asthma model in the modeling group. After successful model preparation, the rats of the modeling group were randomized into a model group, an acupuncture at "Feishu" (BL 13) + "Dingchuan" (EX-B 1) (AAF) group, and acupuncture at "Kongzui" (LU 6)+"Yuji" (LU 10) (AAK) group, with 10 rats in each one. Starting from day 15 of the experiment, 5 min after motivating, acupuncture was applied to "Feishu" (BL 13) + "Dingchuan" (EX-B 1) and "Kongzui" (LU 6)+"Yuji" (LU 10) in the AAF group and the AAK group respectively. The intervention was delivered for 30 min each time, once daily, lasting 3 weeks consecutively. Using lung function detector, the airway resistance (RL) and dynamic compliance (Cdyn) of the lungs were detected. The histomorphology of lung tissues was detected with HE staining and Masson staining, and the mRNA and protein expression of TGF-β1 and Smad3 in lung tissues was detected with the real-time PCR and Western blot methods.@*RESULTS@#Compared with the blank group, RL was increased and Cdyn was decreased in the rats of the model group (P<0.01); and RL was reduced and Cdyn was increased in the AAF group and the AAK group when compared with those in the model group (P<0.01, P<0.05). The rats of the model group had bronchial lumen stenosis, inflammatory cell infiltration, collagen fibre hyperplasia and thickened smooth muscle in the lung tissues when compared with those in the blank group; and in comparison with the model group, all of the above morphological changes were attenuated in the AAF group and the AAK group. Besides, these morphological changes of the lung tissues were more alleviated in the AAF group when compared with those in the AAK group. In comparison with the blank group, the mRNA and protein expression of TGF-β1 and Smad3 of the lung tissues was increased in the model group (P<0.01), and it was reduced in the AAF group and the AAK group when compared with that in the model group (P<0.05, P<0.01). The mRNA expression of TGF-β1 and Smad3 was lower in the AAF group when compared with that in the AAK group (P<0.05).@*CONCLUSION@#Acupuncture at either "Feishu" (BL 13)+"Dingchuan" (EX-B 1) or "Kongzui" (LU 6)+"Yuji" (LU 10) reduces the airway remodeling in the rats with asthma, which may be related to the down-regulation of mRNA and protein expression of TGF-β1 and Smad3. The better efficacy is obtained with acupuncture at "Feishu" (BL 13)+"Dingchuan" (EX-B 1).
Subject(s)
Male , Animals , Rats , Rats, Sprague-Dawley , Transforming Growth Factor beta1/genetics , Airway Remodeling , Acupuncture Therapy , Signal Transduction , Asthma/therapy , Constriction, Pathologic , Anti-Asthmatic AgentsABSTRACT
OBJECTIVE@#To explore the mechanisms of Buyang Huanwu Decoction (BYHWD) modulating the gut microbiome and trimethylamine oxide (TAMO) to exert cardioprotective effects.@*METHODS@#Ligation of the left anterior descending coronary artery was performed in rats to induce heart failure (HF). Except for the sham-operation group (n=10), 36 operation-induced models were randomized into 3 groups using a random number table (n=12 in each group): the model group, the BYHWD group (15.02 g/kg BYHWD), and the positive group (4.99 g/kg metoprolol succinate). After 4-week treatment (once daily by gavage), echocardiography was applied to evaluate the cardiac function and the Tei index (the ratio of ventricular isovolumic contraction time (IVCT) and isovolumic diastolic time (IVRT) to ejection time (ET)) was calculated; hematoxylin-eosin (HE) staining was observed to characterize the pathology of the myocardium and small intestinal villi. D-lactic acid was detected by an enzyme-linked immunosorbent assay (ELISA). Expressions of occludin, claudin-1, and zonula occludens (ZO-1) were detected by Western blot. 16S ribosomal ribonucleic acid (16S rRNA) sequencing was used to explore the changes in the intestinal flora. TMAO was detected via liquid chromatography-tandem mass spectrometry (LC-MS/MS).@*RESULTS@#In the echocardiography, the Tei index was considerably lower in the positive and BYHWD groups compared with the model group (P<0.05). Besides, BYHWD improved the pathology of myocardium and small intestine of HF rats and lowered the D-lactic acid content in the serum, when compared with the model group (P<0.05). BYHWD also improved the expression of occludin and claudin-1 (P<0.05); in the gut microbiota analysis, BYHWD slowed down modifications in the structure distribution of gut microbiota and regulated the diversity of intestinal flora in HF rats. The content of TMAO in the serum was significantly lowered by BYWHT compared with the model group (P<0.05).@*CONCLUSION@#BYHWD may delay progression of HF by enhancing the intestinal barrier structure, and regulating intestinal flora and TAMO.
Subject(s)
Rats , Animals , Rats, Sprague-Dawley , Gastrointestinal Microbiome , Chromatography, Liquid , Claudin-1 , Occludin , RNA, Ribosomal, 16S , Tandem Mass Spectrometry , Drugs, Chinese Herbal/pharmacology , Heart FailureABSTRACT
To clarify the content characteristics of mineral elements in different Artemisia argyi germplasm resources and their relationship with the quality properties of Artemisiae Argyi Folium, this study measured the content of 10 mineral elements including nitrogen(N), phosphorus(P), potassium(K), calcium(Ca), magnesium(Mg), aluminum(Al), manganese(Mn), iron(Fe), copper(Cu), and zinc(Zn) in 100 Artemisia argyi germplasm samples. Besides, their relationship with the quality properties of Artemisiae Argyi Folium was explored by correlation analysis, path analysis, and cluster analysis. The results demonstrated that the variation coefficient of the 10 mineral elements in Artemisiae Argyi Folium ranged from 12.23% to 64.38%, and the genetic diversity index from 0.97 to 3.09. The genetic diversities of N, P, and Zn were obvious. As revealed by the correlation analysis, N, P, and K showed strong positive correlations with each other. Except that Mg and Al were negatively correlated, Ca, Mg, Al, Mn, Fe, Cu, and Zn were positively correlated. The correlation analysis of mineral elements with the quality properties of Artemisiae Argyi Folium proved the significant correlations of 17 pairs of characters. According to the path analysis, P, K, Ca, and Mn greatly affected the yield of Artemisiae Argyi Folium, P, K, and Mg the output rate of moxa, N, P, and K the content of total volatile oil, P and K the content of eucalyptol, and P, K, and Ca the content of eupatilin. The 100 germplasm samples were clustered into three groups. Specifically, in cluster Ⅰ, the enrichment capacity of P, K, and Mg elements was strong, and the comprehensive properties of mineral elements were better, implying good development potential. Ca, Mn, Fe, and Zn elements in cluster Ⅱ and N and Al in cluster Ⅲ displayed strong enrichment capacities. This study has provided new ideas for resource evaluation and variety breeding of A. argyi and also reference for fertilizer application.
Subject(s)
Artemisia/genetics , Iron , Minerals/analysis , Plant Breeding , Plant Leaves/chemistryABSTRACT
NOD-like receptor (NLR) family pyrin domain-containing-3 (NLRP3) inflammasome is implicated in inflammation-associated diseases such as multiple sclerosis, Parkinson's disease, and stroke. Targeting the NLRP3 inflammasome is beneficial to these diseases, but few NLRP3 inflammasome-selective inhibitors are identified to date. Essential oils (EOs) are liquid mixtures of volatile and low molecular-weight organic compounds extracted from aromatic plants, which show various pharmacological activities, including antibacterial, antifungal, antiviral, antioxidant, and anti-inflammatory properties. In this study we screened active ingredients from essential oils, and identified 1,2,4-trimethoxybenzene (1,2,4-TTB) as a selective NLRP3 inflammasome inhibitor. We showed that 1,2,4-TTB (1 mM) markedly suppressed nigericin- or ATP-induced NLRP3 inflammasome activation, thus decreased caspase-1 activation and IL-1ß secretion in immortalized murine bone marrow-derived macrophages (iBMDMs) and in primary mouse microglia. Moreover, 1,2,4-TTB specifically inhibited the activation of NLRP3 inflammasome without affecting absent in melanoma 2 (AIM2) inflammasome activation. We further demonstrated that 1,2,4-TTB inhibited oligomerization of the apoptosis-associated speck-like protein containing a CARD (ASC) and protein-protein interaction between NLRP3 and ASC, thus blocking NLRP3 inflammasome assembly in iBMDMs and in primary mouse macrophages. In mice with experimental autoimmune encephalomyelitis (EAE), administration of 1,2,4-TTB (200 mg · kg-1 · d-1, i.g. for 17 days) significantly ameliorated EAE progression and demyelination. In conclusion, our results demonstrate that 1,2,4-TTB is an NLRP3 inflammasome inhibitor and attenuates the clinical symptom and inflammation of EAE, suggesting that 1,2,4-TTB is a potential candidate compound for treating NLRP3 inflammasome-driven diseases, such as multiple sclerosis.
Subject(s)
Benzene Derivatives/therapeutic use , Encephalomyelitis, Autoimmune, Experimental/drug therapy , Encephalomyelitis, Autoimmune, Experimental/metabolism , NLR Family, Pyrin Domain-Containing 3 Protein/antagonists & inhibitors , NLR Family, Pyrin Domain-Containing 3 Protein/metabolism , Animals , Benzene Derivatives/pharmacology , Cell Line, Transformed , Female , Macrophages, Peritoneal/drug effects , Macrophages, Peritoneal/metabolism , Mice , Mice, Inbred C57BL , Mice, KnockoutABSTRACT
To systemically evaluate the benefits and side effects of Shensong Yangxin Capsules( SYC) in the adjuvant treatment of stable angina pectoris( SAP). Chinese and English databases( PubMed,EMbase,the Cochrane Library,CBM,CNKI,VIP,Wan Fang database) were retrieved to collect the randomized controlled trials( RCTs) about therapeutic efficacy of SYC combined with routine drug( trial group) vs routine drug( control group) in the treatment of SAP. The methodological quality of the RCTs was evaluated based on the cochrane risk of bias assessment tool. The data were extracted and Meta-analyzed by Reviewer Manager 5. 3. TSA 0. 9 software was used for trial sequential analysis( TSA) of the total effective rate of symptoms improvement. A total of 15 RCTs with 1 316 participants were included. RESULTS:: of Meta-analysis showed that the total effective rate of angina symptoms improvement( RR = 1. 15,95% CI[1. 09,1. 21],P<0. 001) of trial group were significantly higher than those of control group,with statistical significance,the total effective rate of electrocardiograms( ECG) improvement( RR = 1. 10,95% CI[0. 94,1. 29],P = 0. 25) of trial group were significantly higher than those of control group,but the difference was not statistically significant. After treatment,the improvement of the total time of 24 h general ischemia( SMD =-1. 21,95%CI[-1. 97,-0. 45],P = 0. 002),the ST-segment depression amplitude( SMD =-1. 30,95%CI [-1. 52,-1. 09],P<0. 001),the duration of angina pectoris attack( SMD =-1. 16,95% CI[-1. 36,-0. 95],P< 0. 001),the angina pectoris attack every week( SMD =-0. 80,95%CI[-1. 10,-0. 50],P<0. 001),the onsumption of nitroglycerin every week( SMD=-0. 72,95%CI[-1. 05,-0. 39],P<0. 001) in the trial group were better than that of the control group,and the difference was statistically significant. Besides,the improvement of the blood lipid and high sensitivity C reactive protein( hs-CRP) in the trial group were better than those of the control group after treatment,and the difference was statistically significant( P< 0. 001). Funnel plots and Egger's linear regression showed that there was no publication bias. By sensitivity analysis,it showed that the results of this study were stable and reliable. No obvious adverse drug reactions were observed in all studies. TSA analysis showed that the evidence of Meta-analysis was reliable. SYC combined with routine Western medicine treatment for SAP can improve the total effective rate of angina pectoris,reduce 24 h total ischemia time,ST segment depression amplitude,duration of angina pectoris attack,frequency of angina pectoris attack and nitroglycerin dosage,and also can improve blood lipid and hs-CRP levels.
Subject(s)
Humans , Adjuvants, Pharmaceutic , Angina, Stable , Drug Therapy , C-Reactive Protein , Capsules , Drugs, Chinese Herbal , Therapeutic Uses , Electrocardiography , Lipids , Blood , Randomized Controlled Trials as TopicABSTRACT
On the basis of an outline on Governor Vessel acupoints electroacupuncture ,endogenous neurotrophic factor expres?sion,grafted adult stem cell-derived neurons integrating to spinal host neuron circuit for repairing spinal cord injury ,it is summa?rized that mechanism of a combination of Governor Vessel acupoints electroacupuncture and grafted adult stem cells improving the tis?sue microenvironment of spinal cord injury to reestablish neuron conduction pathway. Governor Vessel acupoints electroacupuncture stimulate meningeal branch of spinal nerve in rat spinal cord transected or demyelinated. The stimulation message is input into spinal cord through afferent nerve,which activates spinal cord cells synthesizing and secreting neurotrophin-3(NT-3). The NT-3 can pro?mote the survival,differentiation and migration of exogenous neural stem cells(NSC)and bone marrow mesenchymal stem cells (MSC)expressing tyrosine kinase receptor C(TrkC)at the injury/graft site or demyelination/graft site in the spinal cord transected or demyelinated. The combined therapeutic strategy may replace and protect host neurons injured ,perfect tissue microenvironment in?jured,promote nerve fiber regenerating,and improve motor evoked potential of cerebral cortex and motor function of paralysis limbs.
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With the method of substance flow analysis (SFA), the study provided an analytical framework for phosphorus cycle on civil food production and consumption system that was demonstrated by four life stages-food production, food processing, consumption and waste handling. Furthermore, a case study was carried out in Hefei City, for the year 2008. The SFA results show that the total demand of phosphorus reaches 5 475.86 t in the food production and consumption of Hefei City in 2008; approximately 242.57 t P leaves the system, and around 1 710.84 t P is emitted via waste discharge to the surface water, the rest is transformed as the stocks in the system. The effluent of excessive fertilizer in agriculture plays an important role for the huge phosphorus load, as well as the civil sewage. In the end, the study provided some suggestions on improving the use efficiency of phosphorus and reducing phosphorus discharge into surface water.
Subject(s)
Food , Phosphorus/analysis , Water Pollutants, Chemical/analysis , Water Pollution/prevention & control , Agriculture , China , EutrophicationABSTRACT
<p><b>OBJECTIVE</b>To observe the therapeutic effect of warming needle moxibustion on prolapse of lumbar intervertebral disc.</p><p><b>METHODS</b>Seventy-eight cases were randomly divided into a test group and a control group, 39 cases in each group. The control group were treated with acupuncture at Shenshu (BIL 23), Mingmen (GV 4), Yaoyangguan (GV 3) and Weizhong (BL, 40), etc. , and the test group with acupuncture at the same acupoints as in the control group plus warming needle moxibustion at Mingmen (GV 4), Yaoyangguan (GV 3) and Weizhong (BL 40).</p><p><b>RESULTS</b>The total effective rate of 94.9% in the test group was significantly better than 71.8% in the control group (P < 0.01). The incidence rate of needling sensation propagating along the channel (84.6%) in the test group was significantly higher than 56.4% in the control group (P < 0.01).</p><p><b>CONCLUSION</b>The warming needle moxibustion stimulating the needling sensation propagating along the channel has a better therapeutic effect on prolapse of lumbar intervertebral disc.</p>
Subject(s)
Adult , Aged , Female , Humans , Male , Middle Aged , Intervertebral Disc Displacement , Therapeutics , Lumbar Vertebrae , Moxibustion , MethodsABSTRACT
OBJECTIVE@#To investigate the effect of yizhi jiannao granule concentration fluid (YCF) on the behavior, the apoptosis rate of hippocampus neuron and the expression of apoptosis gene Bcl-2, Bax in senescence accelerated mice Senile-Prone/8 (SAMP/8), and to discuss some mechanism of traditional chinese medicine YCF in improving the capability of learning and memory.@*METHODS@#Forty 6-month old SAMP/8 mice were randomly divided into the old group, huperzine A (Hup-A) group and YCF group. Ten 4-month old SAMP/8 mice were served as a young control group. Four groups were given different drugs for 8 weeks, their behavior changes were observed, and the hippocampus were taken out to examine the apotosis rate by flow cytomeutry (FCM) and the expression of Bcl-2, Bax mRNA by RT-PCR.@*RESULTS@#In the YCF group, the escape latency was significantly shortened, the time of swim in the platform quadrant significantly increased, the apoptosis rate of hippocampus neural decreased; the level of Bcl-2 mRNA and the rate of Bcl-2/Bax increased, and the level of Bax mRNA decreased.@*CONCLUSION@#Yizhi jiannao granule can decrease the neuron apoptosis rate and the Bax level, increase the Bcl-2 level, and modulate the rate of Bcl-2/Bax in SAMP/8 brain, which is probably part of the mechanisms of inhibiting the apoptosis and improving learning and memory.
Subject(s)
Animals , Mice , Aging , Pathology , Physiology , Apoptosis , Behavior, Animal , Drugs, Chinese Herbal , Pharmacology , Hippocampus , Pathology , Learning , Memory , Neurons , Pathology , Proto-Oncogene Proteins c-bcl-2 , Genetics , RNA, Messenger , Genetics , Random Allocation , bcl-2-Associated X Protein , GeneticsABSTRACT
Akt/protein kinase B is a major cell survival pathway through phosphorylation of proapoptotic proteins Bad and Bax and of additional apoptotic pathways linked to Forkhead proteins glycogen synthase kinase-3beta and ASK1. To further explore the mechanism by which Akt regulates cell survival, we identified an Akt interaction protein by yeast two-hybrid screening. It is highly homologous to ARG-binding protein 2 (ArgBP2) with splicing exon 8 of the coding region of the ArgBP2. As two splicing isoforms (ArgBP2alpha and -beta) of ArgBP2 have been identified (Wang, B., Golemis, E. A., and Kruh, G. D. (1997) J. Biol. Chem. 272, 17542-17550), it was named ArgBP2gamma. ArgBP2gamma contains four Akt phosphorylation consensus sites, a SoHo motif, and three Src homology (SH) 3 domains and binds to C-terminal proline-rich motifs of Akt through its first and second SH3 domains. It also interacts with p21-activated protein kinase (PAK1) via its first and third SH3 domains, indicating the SH3 domains of ArgBP2gamma as docking sites for Akt and PAK1. Akt phosphorylates ArgBP2gamma in vitro and in vivo. Expression of ArgBP2gamma induces PAK1 activity and overrides apoptosis induced by ectopic expression of Bad or DNA damage. Nonphosphorylatable ArgBP2gamma-4A and SH3 domain-truncated mutant ArgBP2gamma inhibit Akt-induced PAK1 activation and reduce Akt and PAK1 phosphorylation of Bad and antiapoptotic function. These data indicate that ArgBP2gamma is a physiological substrate of Akt, functions as an adaptor for Akt and PAK1, and plays a role in Akt/PAK1 cell survival pathway.