AIM: To research the processed products of Rhizoma Atractylodis Macrocephalae at the level of sesquiterpene lactones from it. METHODS: Sesquiterpene lactones were separated by the silica gel column and layer preparation, and the active substances were determined by HPLC. RESULTS: Atractylone、atractylolide Ⅰ, atractylolide Ⅲ, and biepiasterolid were separated from Rhizoma Atractylodis Macrocephalae. Atractylone was (0.535 8)%, atractylolide Ⅰ was (0.044 0)% and actractylolide Ⅲ was (0.081 4)% in Atractylodis stir-fried with wheat bran determined by HPLC. CONCLUSION: The method has good accuracy and repeatability and it can be used for the quality control of Rhizoma Atractylodis Macrocephalae.

An α-amylase inhibitor (α-AI) was isolated from white kidney beans (Phaseolus vulgaris. L) by ethanol fractional precipitation, ion exchange chromatography and gel filtration column chromatography. It was a homogeneity glycoprotein demonstrated by SDS-PAGE and gel filtration on CL-6B. The glycoprotein contained 88.2% protein and was rich in aspartic acid, glutamic acid, leucine, threonine and serine. The carbohydrate moiety was consisted of Man, Glc, Gal and Xyl in a mole ratio of 2.42∶1.50∶1.52∶1.00. The glycan and the core protein backbone was connected by O-linkage as determined by β-elimination reaction. The continuous oral administration of the α-AI (150 mg·kg-1·d-1 ) for 7 days can lower fasting blood glucose and 300 mg·kg-1 ·d-1 α-AI for 7 days can improve the sugar tolerance on alloxan-dependent diabetic model rats. The result showed the α-AI obtained from white kidney beans had good hypoglycemic effect on alloxan induced diabetic rats and may have high potential pharmaceutical value as a regulative digestive-starch degradation in patients suffering from diabetes.

Adult ; Aged ; Aged, 80 and over ; Humans ; Middle Aged ; Pneumoconiosis ; diagnostic imaging ; Radiography, Thoracic ; methods ; Tomography, X-Ray Computed ; X-Ray Film

Objective To explore the optimal HbAlc diagnostic cutpoint in different glucose tolerance populations in the plateau region.Methods (1) 472 diabetes mellitus (DM) patients and highrisk groups accepting diabetes screening in the First Affiliated Hospital of Kunming Medical College (217 males and 255 females,≥20 years old,median age 54 years old) were collected,oral glucose tolerance test (OGTT) and HbAlc were tested.(2) the research subjects were divided into normal glucose adjustment group (NGT),Impaired fasting glucose group (IFG) and (or) Impaired glucose tolerance IGT group and diabetes mellitus (DM) group.The receiver-operating characteristic curve (ROC) was explored to determine the optimal HbA1c diagnostic cut point for IFG,IGT and DM status respectively.Results The average HbA1 c values of NGT,IFG and (or) IGT,DM groups were (6.06 ± 0.11) ％,(6.63 ± 0.11) ％,(8.70 ± 2.08)％ respectively,for IFG and IGT groups,the optimal HbA1c diagnostic cut points were 6.7％ and 6.6％,respectively; If use either FBG or 2 h PG to diagnose DM,the corresponding optimal HbA1 c diagnostic cut point was 7.1％ ; If use anyone of FBG or 2hPG to diagnose DM,the corresponding optimal HbA1c diagnostic cut point was 7.0％ ; If both FBG and 2hPG were used to diagnose DM,the corresponding optimal HbA1 c diagnostic cut point was 7.1％.Conclusion Preliminarily confirm the optimal HbA1c diagnostic cut point in different glucose tolerance populations in the plateau region of Kunming,and provide the evidence for further clinical application of HbA1c.

We designed and synthesized eighteen lycorine derivatives with five different structural types, and evaluated their antiviral activities on a HCoV-OC43-infected H460 cell model. Structure-activity relationships suggested that the introduction of appropriate substituents on the 6N atom of lycorine was beneficial to activity. Compound 6a gave a good activity with the half effective concentration (EC₅₀) and selectivity index (SI) values of 2.36 μmol·L^-1 and 16.52, respectively. Surface plasmon resonance (SPR) result indicated that 6a might target the non-structural protein 12 (NSP12) subunit in RNA-dependent RNA polymerase (RdRp) of SARS-CoV-2 with the dissociation constant (K_D) value of 1.36 μmol·L^-1. Molecular docking indicated that 6a might act on nidovirus RdRp-associated nucleotidyltransferase (NiRAN) catalytic center of NSP12, distinct from the mechanism of nucleoside-like drugs such as remdesivir. This study provides scientific data for the development of lycorine derivatives into a new class of anti-SARS-CoV-2 small molecule inhibitors.

OBJECTIVETo explore the experimental conditions for H2O2 to injure astrocytes and the effect of baicalin in protecting neurons and astrocytes from oxidative stress injury.

METHODSNeurons and astrocytes from forebrain of rats were cultured in vitro and treated with H2O2, baicalin and combination of the two, respectively. The cell viability or survival rate was determined using MTT.

RESULTSEffects of H2O2 in different concentrations on survival rate of astrocytes showed significant difference (F = 28.569, P < 0.01) in a dose-dependent manner. Degrees of H2O2 injury, with the same concentration of H2O2, on cells with different seeding density were also significantly different (F = 5.439, P < 0.01), and dose-dependently. Baicalin didn't influence the survival rate of neurons and astrocytes when the concentration was within 2.5-40 mumol/L (for neurons, F = 0.49, P > 0.05; for astrocytes, F = 1.001, P > 0.05), but baicalin showed significant antagonism to the injury of oxidative stress (for neurons, F = 24.384, P < 0.01; for astrocytes, F = 5.000, P < 0.01). The higher the concentration of bainalin, the higher the cell survival rate.

CONCLUSIONA model of astrocytes oxidative injury induced by H2O2 is established. Baicalin shows no toxicity on neurons and astrocytes when the concentration is within 2.5-40 mumol/L, but could antagonize the H2O2 caused oxidative injury on cells in a dose-dependent manner.

Animals ; Animals, Newborn ; Astrocytes ; pathology ; Cells, Cultured ; Flavonoids ; pharmacology ; Hydrogen Peroxide ; Neurons ; pathology ; Neuroprotective Agents ; pharmacology ; Oxidative Stress ; Rats ; Rats, Sprague-Dawley

Objective To evaluate the efficacy of intravenous recombinant human brain natriuretic peptide in acute anterior myocardial infarction complicated with heart failure.Methods Two hundred patients suffered from acute anterior myocardial infarction complicated with heart failure were randomly divided into two groups:rhBNP group ( n =100) and control group ( n =100 ).All patients were given conventional treatment,patients in rhBNP group were given rhBNP on the basis of conventional therapy.The clinical effectiveness including the improvement of cardiac function,cardiac ultrasound data,the incidence of hospital adverse cardiac events,and six month follow-up were compared between the two groups.Results The degree of decompensation and Killip class in rhBNP group were better than those of control group after treatment ( improved dyspnea:significantly improved:36 vs 27 ; improved:49 vs 46; no improvement:11 vs 20 ; deterioration:4 vs 7 ; Ridit value:0.4618 vs 0.5382,P =0.043) ( Killip class:significantly improved:26 vs 20; improved:56 vs 45; no improvement:14 vs 25 ; deterioration:4 vs 10; Ridit value:0.4553 vs 0.5447,P =0.017 ).After treatment for one week,The LVEF improvement in rhBNP group was more remarkable than that of control group ( [ 53.0 ± 5.2 ] ％vs.[ 50.0 ±:6.2 ] ％,P =0.014).The occurrence rate of angina ( 13.0％ vs.27.0％,P =0.013 ),heart failure ( 18.0％ vs.32.0％,P =0.022) and major adverse cardiac events(MACE) ( 17.0％ vs.30.0％,P =0.030) inrhBNP group was lower than that in control group.During 6 months follow-up period,event-free survival in rhBNP group was higher than that in control group ( 69.0％ vs.55.0％,P =0.041 ).Conclusion Transvenous injection of rhBNP combined with other routine treatment can improve cardiac function in patients with myocardial infarction in acute anterior myocardial infarction.It can also decrease adverse cardiac events during hospitalization and increase event-free survival in 6 months follow-up period.

Objective To study the immune regulatory effect of natural killer cell(NKT) in the early stage of murine liver injury induced by type 5 adenovirus(Ad5). Methods Animal models were con-structed by injected C57BL/6 mice with 1.5×109-3×109 PFU Ad5 into the tail vein. Liver injury of mouse at day 0, 1, 2, 3, 4, 5 after infection was determined by HE staining and serum ALT/AST(alanine amin-otransferase/aspartate aminotransferase) level. Flow cytometry analysis was used to measure the proportion of lymphocytes, expression of Fas/FasL on the surface of NKT cells and level of IL-4, IFN-γ/in NKT cell plasma in the infected mouse liver. RT-PCR was applied to semi-quantify the chemokines and their receptors mRNA in infected mouse liver. Results NKT cells of mouse increased significantly at day 1 after infected with high titer Ads(3×109 PFU), expression of FasL on NKT cell and plasma IL-4, IFN-γ/level in NKT cells were also up-regulated, hence the obviously infiltration of lymphocytes in routine liver. Comparing with high titer Ads infection, low titer Ads infection (1.5×109 PFU) lead to little change of NKT cell proper-tion, and fewer infiltration of lymphocytes in murine liver. Hepatic chemokine RANTES, 1P-10, and MIP-1β mRNA expression in C57BL/6 was up-regulated 2 d after intravenous administration of 3×109 PFU Ad5. Corresponding chemokine receptor CCR5, CCR1, CXCR3 mRNA expression was up-regulated 3 d after in-fection. Conclusion NKT cells play an important role in lymphocytes recruitment into the liver of mouse in-fected with AdS, which may relate to up-regulatio of the plasma IL-4, IFN-γ level and expression of FasL of NKT cells, therefore facilitating the production of chemokines, e.g. IP-10 and Mig.

Objective:To explore the risk factors of spontaneous rupture of hepatocellular carcinoma (HCC), and to analyze the prognosis of transcatheter arterial embolization (TAE) in the treatment of spontaneous rupture of HCC.Methods:From January 2008 to December 2018, at Tianjin Third Central Hospital, 126 patients diagnosed with spontaneous rupture of HCC (spontaneous rupture group) and in the same period 252 patients diagnosed as HCC without rupture (non-spontaneous rupture group) were retrospectively selected. Independent sample t test, Mann-Whitney U test and chi-square test were used to compare the general data, laboratory test results and imaging results between spontaneous rupture group and non-spontaneous rupture group. Multivariate logistic regression was used to analyze the independent risk factors of spontaneous rupture of HCC. Kaplan-Meier method and log-rank test were used for survival analysis of 92 patients treated with TAE and 31 patients treated with conservative treatment in patients with spontaneous rupture of HCC, and multivariate Cox proportional hazard regression was used to analyze the independent prognostic factors of patients treated with TAE. Results:The proportions of tumor maximum diameter ≥5 cm, tumors mainly located in segment Ⅱ, Ⅲ, Ⅳ and Ⅵ of the liver, tumors protruding height from the surface of liver ≥1 cm, liver cirrhosis and portal vein thrombosis (PVT) in spontaneous rupture group were all higher than those in non-spontaneous rupture group (46.8%, 59/126 vs. 35.7%, 90/252; 61.1%, 77/126 vs. 46.0%, 116/252; 73.0%, 92/126 vs. 18.7%, 47/252; 81.7%, 103/126 vs. 69.0%, 174/252; 20.6%, 26/126 vs. 11.5%, 29/252), and the level of fibrinogen is lower than that in non-spontaneous rupture group ((3.07 ±1.38) g/L vs. (3.92±1.13) g/L), and the differences were statistically significant ( χ2=4.343, 7.644, 106.780, 6.918 and 5.628, t=-3.276, all P<0.05). The results of multivariate logistic regression analysis showed that the location of tumors in segment Ⅱ, Ⅲ, Ⅳ, Ⅵ of the liver, the height of tumors protruding from the surface of liver ≥1 cm, liver cirrhosis and the fibrinogen was lower than the lower limit of the reference value were independent risk factors of spontaneous rupture of HCC (odds ratio ( OR)=1.354, 5.726, 1.152, 1.892; 95% confidence interval ( CI) 1.062 to 2.008, 1.049 to 19.575, 1.016 to 1.895, 1.267 to 3.346; all P<0.05). Among 92 patients with spontaneous rupture of HCC treated with TAE, the TAE technical success rate and clinical success rate were 100.0% (92/92) and 93.5% (86/92), respectively. Thirty-one patients received conservative treatment. The median survival time of the patients treated with TAE was 243 d (38 d, 377 d), which was about 10 times that of the patients who accepted conservative treatment (23 d (9 d, 51 d)). The 1-month, 3-month, 6-month, 1-year and 3-year survival rates of the patients treated with TAE were 72.8%, 50.8%, 46.0%, 31.1% and 13.6%, respectively, and those of patients who accepted conservative treatment were 25.8%, 17.2%, 11.5%, 5.7% and 0, respectively; and the differences in survival rates between the two groups were statistically significant ( χ2=34.606, P<0.01). Log-rank test analysis showed that initial hemoglobin <60 g/L, C grade of liver function, total bilirubin (TBil)≥50 μmol/L, complicated with portal vein tumor thrombus, hepatic lobe embolism during TAE, and tumor maximum diameter ≥10 cm were all correlated with poor survival rates of patients with spontaneous rupture of HCC after TAE ( χ2=3.752, 4.146, 22.318, 4.087, 5.685 and 7.893, all P<0.05). The results of multivariate Cox proportional hazard regression analysis showed that TBil ≥ 50 μmol/L, hepatic lobe embolism during TAE, and tumor maximum diameter ≥10 cm were independent factors of poor prognosis of spontaneous rupture of HCC treated with TAE ( OR=25.873, 8.415, 18.620; 95% CI 4.916 to 126.005, 1.136 to 27.319, 2.754 to 84.368; all P<0.05). Conclusions:In HCC patients with tumors located in segments Ⅱ, Ⅲ, Ⅳ and Ⅵ of the liver, the height of tumors protruding from the surface of liver ≥1 cm, liver cirrhosis or the fibrinogen is lower than the lower limit of the reference value, close attention should be paid to the risk of spontaneous tumor rupture. TAE is an effective treatment for acute spontaneous rupture of HCC, and the prognosis of patients treated with TAE is better than that of patients receiving conservative treatment. However, patients with TBil ≥50 μmol/L, hepatic lobe embolism during TAE and tumor maximum diameter ≥10 cm have a poor prognosis after TAE treatment.

Non-small-cell lung carcinoma (NSCLC) is one of the most frequently diagnosed malignancies worldwide.Previous studies have shown that microRNA-449b (miR-449b) functions as a tumor suppressor in many cancers.However,the role of miR-449b in NSCLC is still unknown.In the present study,miR-449b was significantly downregulated in NSCLC samples and cell lines.Bioinformatics analysis revealed that 3'-UTR region of leucine rich repeat containing G protein-coupled receptor 4 (LGR4) mRNA had putative complementary sequences to miR-449b,which was further confirmed by the luciferase assay.Western blotting showed that restoration of miR-449b in NSCLC cells decreased the expression of LGR4.Interestingly,over-expression of miR-449b inhibited growth and invasion of NSCLC cells in vitro.Furthermore,ectopic expression of LGR4 reversed miR-449b-suppressed proliferation and invasion of NSCLC cells.Therefore,the data of the present study demonstrate that miR-449b inhibits tumor cell growth and invasion by targeting LGR4 in NSCLC.