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Objective: To investigate the mechanism of Qingkailing Injection in the treatment of coronavirus disease 2019 (COVID-19). Methods: The active components and target proteins of Gardeniae Fructus, Isatidis Radix, Lonicerae Japonicae Flos, and other materials in Qingkailing Injection were obtained by means of literature search and TCMSP. Uniprot database was used to search the target genes corresponding to the active ingredients, and Cytoscape 3.7.2 was used to construct the drug-compound-target network. The enrichment analysis of KEGG pathway was carried out with the help of DAVID database to predict its mechanism. Core active components and potential targets of anti-COVID-19 drugs were verified by molecular docking. Results: The drug-compound- target network consisted of five drugs, 62 compounds and 70 targets. The KEGG pathway enrichment analysis included 41 signaling pathways (P < 0.05), which were mainly involved in cell apoptosis, Fc epsilon RI signaling pathway, TNF signaling pathway, etc. Molecular docking results showed that acacetin and syrigin had strong affinity with potential targets of anti-COVID-19 drugs. Conclusion: In this study, the effect of Qingkailing Injection has the characteristics of multiple components, multiple targets and multiple pathways. The active component, acacetin, can regulate the apoptosis pathway and TNF pathway by acting on CASP3, CASP8, FASLG, and other targets, so as to realize the potential therapeutic effect on COVID-19.
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Objective::The effects of three different doses of borneol on acute myocardial infarction (AMI) model rats and the effects on oxidative stress factors were compared to provide reference for elucidation of the dose-effect relationship and mechanism of anti-myocardial infarction. Method::Healthy adult male SPF SD rats were randomly divided into sham operation group, model group, solvation model group, nitroglycerin group, Borneolum high, medium and low dose(0.6, 0.3, 0.15 g·kg-1) group, l-Borneolum and Borneolum syntheticum high, medium, low dose(0.2, 0.1, 0.05 g·kg-1) group, a total of 13 groups, 20 in each group. Gavage was performed at 20 mL·kg-1 once a day for 3 days of continuous preventive administration. The sham operation group and the model group were given the same volume of distilled water, and the solvation model group was given the same volume of 5% polysorbate 80.On the third day of the pre-administration, 30 minutes after the last dose, the left anterior descending coronary artery was ligated to make a model, and the successful rats were treated for 3 days. BL-420N biological system analyzer was used to record the ST-segment amplitude and hemodynamic changes. Rat body weight and cardiac weight were weighed to calculate cardiac viscera coefficients, 2, 3, 5-triphenyl tetrazolium chloride (TTC) staining was used to calculate the myocardial infarction rate. Hematoxylin-eosin (HE) staining was used to evaluate the degree of myocardial pathological damage. According to the kit requirements, serum levels of lactate dehydrogenase (LDH), aspartate amino-transaminase (AST), creatine kinase isoenzyme (CK-MB) and oxidative stress factors superoxide dismutase (SOD), malondialdehyde (MDA) were detected. Result::Compared with the sham operation group, the ST segment amplitude of the model group significantly increased after 5 minutes, the left ventricular diastolic blood pressure (LVDP) value increased significantly, and the measured maximum shortening velocity (Vpm) value of the left ventricular myocardial contraction component significantly decreased. The organ coefficient and myocardial infarction rate were extremely significantly increased, and the myocardial pathological tissue was severely damaged. The serum CK-MB, AST, LDH, and MDA contents were significantly increased (P<0.05, P<0.01). Compared with the solvation model group, the Borneolum and l-Borneolum in the middle and low, and the Borneolum syntheticum high dose groups could significantly inhibited the abnormal elevation of ST segments at different time points. The Borneolum and l-Borneolum high, medium, low, and Borneolum syntheticum high dose groups significantly increased the left ventricular systolic blood pressure (LVSP) value and decrease the LVDP value (P<0.01). The Borneolum medium, low, and l-Borneolum high, medium, Borneolum syntheticum high dose groups significantly increased the maximum rate of left ventricular pressure rise (dp/dt max) and Vpm value (P<0.05, P<0.01). The Borneolum and l-Borneolum medium, low dose groups significantly reduced rat cardiac organ coefficients. The Borneolum high, medium, low and l-Borneolum, Borneolum syntheticum medium, low dose groups significantly improved myocardial infarction in rats (P< 0.05, P<0.01). The Borneolum low, l-Borneolum high, medium, and Borneolum syntheticum high groups also significantly improved the degree of pathological damage (P<0.01). High dose of l-Borneolum significantly reduced CK-MB content, medium and low dose of l-Borneolum significantly reduced AST activity, medium and low dose of l-Borneolum, high, medium and low dose of Borneolum syntheticum significantly reduced LDH activity (P<0.05, P<0.01). Serum SOD activity of rats in l-Borneolum high, medium, and Borneolum syntheticum high dose groups increased significantly (P<0.05, P<0.01). Serum MDA levels in Borneolum high, medium, low, and l-Borneolum high, middle dose groups significantly decreased (P<0.01). Conclusion::Three kinds of borneol in different dose groups can play different degrees of myocardial protection. Under the experimental conditions, there was a trend of l-Borneolum>Borneolum>Borneolum syntheticum in improving the efficacy of myocardial infarction, the dose-effect of Borneolum was negatively correlated, Borneolum syntheticum was positively correlated, and no significant dose-effect relationship between l-Borneolum.
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OBJECTIVE： To study the in vitro inhibitory effects and antioxidant activity of different solvent extracts of Boehmeria nivea leaves against influenza A virus（H1N1）， and to expand the medicinal parts of B. nivea and develop natural antiviral and antioxidant drugs. METHODS： The leaves of B. nivea were extracted with 95％ ethanol. The ethanol extract was dissolved by water heating， and extracted with different solvents to obtain petroleum ether phase， trichloromethane phase， ethyl acetate phase， n-butanol phase and aqueous phase extracts of B. nivea leaves. The toxicity of aqueous extract of B. nivea leaves （50-400 μg/mL） on Madin-Darby canine kidney （MDCK） cell line was investigated. Using ribavirin as positive control， MDCK cells were attacked by influenza A virus（H1N1）. Western blotting assay was used to detect the expression of nucleoproteins （NP） in viral infected cells after treated with same concentrations of petroleum ether phase， trichloromethane phase， ethyl acetate phase， n-butanol phase and aqueous phase extracts of B. nivea leaves （100 μg/mL）， different concentrations of aqueous phase extract solution of B. nivea leaves （50， 100， 200， 400 μg/mL） and different concentrations of ribavirin solution （0.31， 0.63， 1.25 μg/mL）. Using vitamin C as a positive control， hydroxyl radical（·OH） scavenging test， DPPH radical scavenging test and reduction test were used to investigate in vitro antioxidant activity of the extracts. RESULTS： Aqueous phase extract of B. nivea leaves with concentration less than 400 μg/mL was nontoxic to MDCK cells. The petroleum ether phase， trichloromethane phase， ethyl acetate phase and aqueous phase extracts at 100 g/mL could significantly reduce the expression of NP protein in influenza A virus（H1N1） infected cells （P＜0.01）. Different concentrations （50-400 μg/mL） of aqueous extract could significantly reduce the protein expression of NP （P＜0.01） in concentration-dependent manner. The in vitro antioxidant activity of petroleum ether phase and ethyl acetate phase was similar to that of vitamin C. CONCLUSIONS： B. nivea leaves extract have better anti-influenza A virus（H1N1） effects in vitro， and the extracts of petroleum ether phase and ethyl acetate phase show good antioxidant activity in vitro.
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Objective:To investigate interleukin-32 (IL-32)(rs28372698A/T,rs12934561C/T and rs11861531C/T) genetic susceptibility in patients with multiple sclerosis(MS)by case-control study,which provides a theoretical foundation for high-risk population with MS.Methods:A total 580 MS patients and 650 healthy controls were included in this study,polymerase chain reaction-single base extension (PCR-SEB) was used to test DNA sequencing,and serum levels of IL-32 were determined by enzyme-linked im-munosorbent assay.Results:The genotype and allele frequency of IL-32 (rs28372698A/T) had significantly differences compared with healthy controls (P=0.007,P=0.033),however,there were no statistical differences in rs12934561C/T and rs11861531C/T between the two groups (P>0.05).T-T-T haploid genotype in patients with MS was higher than control groups(P=0.012),and T-T-T haploid genotype was associated with increased risk of MS(OR=1.968,95% CI:1.968-1.352).Serum levels of IL-32 in patients with MS was increased compared with control groups[(399.08 ± 156.85)pg/ml vs (239.99 ± 88.35)pg/ml,P= 0.001].The serum IL-32 concentrations in MS patients with AT and TT genotype were higher compared with MS patient with AA genotype[(465.53±172.40) pg/ml vs(295.86±103.96)pg/ml,P<0.01;(491.15±133.65)pg/ml vs(295.86±103.96)pg/ml,P<0.01].Conclusion:Our study found that an association between IL-32(rs28372698) gene polymorphism and MS,and serum levels of IL-32 were influenced by IL-32 gene polymorphism in patients with MS,suggesting a theoretical basis for individualized diagnosis and treatment of MS patients.
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Objective To observe the effect of massage combined with wearing personalized myopia-lens on the prevention and control of children myopia based on the theory of treating disease before its onset. Methods A total of 117 non-myopia students (involving with 234 eyes)aged 7-8 years old were divided into three groups. Group A was treated with massage combined with wearing personalized myopia-lens,group B was treated with wearing personalized myopia-lens, and group C had no any treatment. Eyesight examination was performed for the 3 groups every 6 months in the following 6 continuous years. Six years later,the incidence of myopia,diopter and eye axis difference were compared among the 3 groups. Results (1)The incidence of myopia in group A, B and C was 24.3％,32.1％,56.3％ respectively. The incidence of group A and B was lower than that of group C (P < 0.05), and group A showed a decreasing trend of incidence of myopia as compared with group B (P >0.05).(2)The diopter difference of group A,B,C in the 6 years was(-0.5642 ± 0.1759)D,(-1.3156 ± 0.7267) D,(-2.4125 ± 1.4842) D respectively, and the differences between group A and B, and those between group A and C were statistically significant (P < 0.01). The axial growth in group A,B and C in the 6 years was (1.1577 ± 0.3332)mm,(1.2955 ± 0.4011)mm,(1.5545 ± 0.6067) mm respectively,and the differences between group A and B,and those between group A and C were statistically significant (P < 0.01). Conclusion The myopia comprehensive therapy of massage combined with wearing personalized myopia-lens is effective on preventing the occurrence of myopia and reducing the incidence of myopia.
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As a recognized precancerous disease, the chronic atrophic gastritis (CAG) has a low diagnosis rate at an early stage due to its atypical symptoms. While massive studies have shown that changes in the serum gastric function parameters including pepsinogen (PG) and gastrin 17 (G17) levels which can be reflected by the functional and morphological status of the gastric mucosa, moreover, H. pylori plays a catalytic role in mucosal atrophy and intestinal metaplasia, indirectly affects the values of the above items. In this article, we discussd the progress in the diagnosis of atrophic gastritis and the risk assessment of gastric cancer based on serum gastric function tests.
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Aim To investigate the effects of aralosdie C (SMC)isolated from aralosides on contractile func-tion and calcium transients in ischemia / reperfusion(I/R)-induced rat myocardial injury and the role of CaMK II. Methods The cardiomyocytes were divided into control group,I/ R group,I/ R + SMC group,KN-93+ I/ R + SMC group. The effect of SMC on the con-tractile function and calcium transient of I/ R cells was measured by cell shrinkage and ion concentration sim-ultaneous detection system. Results SMC(8 μmol· L - 1 )improved the contractile function of I/ R cardio-myocytes and the calcium transients,and SMC in-creased the rate of calcium transient and [Ca2 +]i up /down regulation significantly. While CaMK II was blocked by KN-93,the effect of SMC on contractile function and calcium transients was weakened. Con-clusions SMC can significantly improve the systolic function and calcium transients of cardiomyocytes in I/R rats,and the protective effect of SMC on cardiomyo-cytes may be related to CaMK II.
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Objective To assess the limit of detection(LOD),sensitivity and specificity of collodial gold immunochrom-atography(GICA)products purchased from two manufacturers under special environmental conditions.Methods The sensitivity and specificity of GICA made in InTec Products, INC.and Beijing WANTAI Biological Pharmacy Enterprise Co., LTD.for detecting HBsAg, anti-HCV and anti-Treponema pallidum(TP)serum samples were evaluated under different conditions(conventional facilities,simulated hot and humid environments and simulated low pressure and hypoxia environments)according to the protocol of kits.LOD was estimated by detecting the standard materials obtained from the National Center for Clinical Laboratory(NCCL)of China.Results LOD for syphilis improved from 2 NCU to 1 NCU using GICA from InTec Products in hot and humid environments.The extreme conditions did not influence the specificity of GICA from the two manufacturers in the course of detection of clinical samples,but the sensitivity of detection was affected.For InTec Products,the sensitivity of hepatitis B virus and syphilis detection was improved in hot and humid environments,but was reduced in low pressure and hypoxia environments.In addition,the sensitivity of hepatitis C virus detection by InTec Products decreased in hot and humid environments.As for WANTAI products,the sensitivity of hepatitis B virus detection was reduced under extreme conditions and that of hepatitis C virus was only influenced by hot and humid environments. Interestingly, extreme conditions had no impact on the sensitivity of syphilis.Conclusion LOD of InTec Products is better than that of the WANTAI products for detection of standard materials from blood-borne diseases.In the process of detecting clinical samples,the sensitivity of the two manufacturers′GICA is influenced by extreme conditions, with the specificity unchanged.Overall, WANTAI products are more stable than those of InTec, and are also less influenced by extreme conditions.
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<p><b>OBJECTIVE</b>To explore the risk factors for acute respiratory distress syndrome (ARDS) in children receiving surgeries for critical and complex congenital heart disease (CCHD).</p><p><b>METHODS</b>According to the 2011's Berlin definition of ARDS, the clinical data were collected from 75 children without ARDS (group I) and 80 children with ARDS (group II) following surgeries for CCHD performed in the Department of Cardiac Surgery of our hospital from January, 2009 to May, 2014. Univariate analyses and logistic regression were used to analyze the risk factors contributing to the occurrence of ARDS following the surgeries.</p><p><b>RESULTS</b>In the 80 patients who developed ARDS postoperatively in group II, 27 had mild ARDS, 25 had moderate ARDS, and 28 had severe ARDS; death occurred in 17 (21%) cases. Univariate analyses showed that 23 parameters were significantly different between groups I and II (P<0.05), including weight; preoperative PCO2, left ventricular ejection fraction, pulmonary artery pressure, pulmonary infection, and coagulation abnormalities; early postoperative serum globulin; intraoperative aortic cross clamp (ACC) time; cardiopulmonary bypass (CPB) time; operation time; blood loss and blood transfusion amount intraoperatively and during the first 8 h after operation; lactic acid level immediately after the operation and its maximum increasing rate within 24 h postoperatively; postoperative serum levels of albumin and creatinine; serum levels of B-type natriuretic peptide, procalcitonin, C-reactive protein, and prealbumin 24 h after operation; and age. Logistic regression analyses showed that intraoperative ACC time, CPB time, the maximum increasing rate of lactic acid within 24 h after operation, serum procalcitonin 24 h after operation and intraoperative blood loss were independent risk factors for postoperative ARDS.</p><p><b>CONCLUSION</b>The risk factors of ARDS identified in these children can predict the occurrence of ARDS following the surgeries and timely interventions can improve the success rate in treatment of postoperative ARDS in children with CCHD.</p>
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Designing of natural product-like compounds using natural products as template structures is an important strategy for the discovery of new drugs. Gambogic acid (GA), which is a Garcinia natural product with a unique caged xanthone scaffold, inhibits potent antitumor activity both in vitro and in vivo. This review summarized the researches on the identification of the antitumor pharmacophore of GA, and the design, structural optimization and structure-activity relationship (SAR) of natural product-like caged xanthones based on it.
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Humans , Antineoplastic Agents , Chemistry , Pharmacology , Biological Products , Chemistry , Pharmacology , Cell Line, Tumor , Cell Proliferation , Drug Screening Assays, Antitumor , Garcinia , Chemistry , Molecular Structure , Structure-Activity Relationship , Xanthones , Chemistry , PharmacologyABSTRACT
Objective To study the anti-HBV constituents from Corydalis saxola. Methods The constituents were repeatedly purified by column chromatography and were identified on the basis of spectral analysis and comparison of their spectral data with those previously reported. Compounds isolated in large amounts were assayed against HBV. Results Sixteen compounds were identified to be dihydrosanguinarine (1), d-corydaline (2), cavidine (3), stylopine (4), 6-acetonyl-5, 6-dihydrosanguinarine (5), dihydrochelerythrine (6), tetrahydropalmatine (7), adlumidine (8), (-)-salutaridine (9), palmatine (10), protopine (11), berberine (12), coptisine (13), thalifaurine (14), dehydroapocavidine (15), and (+)-magnoflorine (16). Compounds 5, 6, 8-11, 13, and 16 with high amounts were chosen to detect anti-HBV activities. Compounds 5 and 8 were moderately active, compounds 11 and 16 showed weak inhibitory effects, while compound 6 exihibited the most potent activity against HBsAg and HBeAg secretions in HepG 2.2.15 cell line, followed by compound 9. Conclusion Compounds 1, 4-6, 8, 9, 13, 14, and 16 are isolated from C. saxicola for the first time. Compound 10 is the main constituent and compound 6 exihibits the most potent activity against HBV.