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

AIM:To investigate the effect of rhein on bleomycin-induced pulmonary fibrosis and the expression of microRNA-21 (miR-21) and transforming growth factor-β1 (TGF-β1)/Smad signaling molecules in rats.METHODS:A single dose of bleomycin was intratracheal injected into the SD rats to induce pulmonary fibrosis .After injection of bleo-mycin, the rats were randomly divided into low-, medium-and high-dose rhein treatment groups and model group .The rats that were instilled with normal saline intratracheally served as control group .After the treatment for 28 d, the pulmonary pathologic changes were observed under microscope with hematoxylin-eosin staining .The lung coefficient and hydroxypro-line content were also measured .The expression of miR-21 and the mRNA levels of TGF-β1 and Smad7 in the lung tissues were detected by real-time PCR.The protein levels of TGF-β1 and Smad7 were determined by Western blot .RESULTS:Rhein significantly attenuated the experimental alveolitis , pulmonary fibrosis , lung coefficient and hydroxyproline contents in the rats.Rhein obviously decreased the expression of miR-21,and the mRNA and protein levels of TGF-β1, but signifi-cantly increased the mRNA and protein levels of Smad 7 in the lung tissues .CONCLUSION: Rhein effectively prevents bleomycin-induced pulmonary fibrosis by inhibiting the expression of miR-21 and promoting the expression of Smad 7, thus regulating the TGF/Smad signaling pathway to decrease extracellular matrix deposition .

Objective To study the effect of fluoride on the expression of bcl-2 and Bax in chondrocyte in vitro, and investigate the mechanism of action of chondrocyte apoptosis induced by fluoride. Methods Articular chondrocytes of neonate rat were cultured in vitro and treated with 0(control),5,20,40 mg/L of fluoride,respectively, for 10 days. Then observed the u]trastructure of chondrocytes under eletronicmicroscope, and tested the expression of bcl-2 and Bax in chondrocyte in different groups by Western blotting. Results Abundant rough endoplasmic reticulums (RERs) and complete structure of mitochondria membranes were presented in globular chondrocytes in the control group and 5 mg/L group; but more lipid droplets and vacuoles were seen in the cytoplasm, and the structure of intracellular membranes became incomplete, and some shrieked chromatin and pyknosis were seen in the chondrocytes of the 20,40 mg/L groups. The expression of bcl-2 markedly decreased in 20 mg/L group(0.626 ± 0.042) and 40 mg/L group(0.531± 0.039) compared to the control group(0.876 ± 0.035,all P ＜ 0.01 ). And the expression of Bax significantly increased in 20 mg/L group(0.966 ± 0.047) and 40 mg/Lgroup ( 1 .289 ± 0.156) compared to the control group(0.642 ± 0.050, all P ＜ 0.01). But there was no statistical significant difference of the expression of bcl-2 or Bax between 5 mg/L group(0.885 ± 0.065,0.657 ± 0.045) and control group (all P ＞ 0.05 ). However there were statistical differences of expressions of bcl-2 and Bax between 20 and 40 mg/L groups(all P ＜ 0.01 ). Conclusions Twenty and 40 mg/L fluoride can cause damage to the ultrastructure of chondrocyte, and fluoride possibly promotes chondrocyte apoptosis by reducing the expression of antiapoptotic factor bcl-2 and increasing the expression of Bax.

?AlM: To investigate the expression of miR-181 in the lens tissue of cataract and the regulating mechanism of miR-181 on apoptosis of human lens epithelial cell.
?METHODS:Real time q-PCR was used to measure the expression of miR-181 in the anterior lens capsules of age - related cataract and human lens epithelial cell apoptosis model. miR- 181 mimic and inhibitor were transfected using Lipofectamine 2 000 to regulate the expression of miR-181, and then Real time q-PCR was used to verify transfection efficiency. Flow cytometry was used to detect the change of cell apoptosis rate.
? RESULTS: Compared with control group, the expression of miR-181 was significantly higher in both the anterior lens capsules of age-related cataract and human lens epithelial cell apoptosis model; the relative expression of miR-181 in lens epithelial cells transfected with miR-181 mimic was increased, whereas decreased in cells transfected with miR-181 inhibitor;the apoptosis rate of cells transfected with miR - 181 mimic was increased, while reduced in miR-181 inhibitor group. Each result was statistically significant (P<0. 01).
?CONCLUSlON:High expression of miR-181 is detected in anterior lens capsule of age-related cataract. miR-181 might play a certain role in the pathogenesis of cataract via promoting human lens epithelial cell apoptosis. miR-181 probably becomes a new approach for the nonoperative treatment of cataract, but the concrete mechanism still needs to be further studied.

ObjectiveTo study the effects of treadmill training on balance of convalescent stroke patients.Methods61 patients were divided into 2 groups :observed group(31 cases) and control group(30 cases).The patients of control group were trained with routine rehabilitation training program, the patients of observed group were trained with treadmill training in addition. They were evaluated with Berg balance scale before and 8 weeks after treatment. ResultsAfter training, either observed group or control group showed significant improvement at equilibrium function, but the equilibrium function improved more in observed group (P<0.05). ConclusionTreadmill training plays a positive role on balance recovery in convalescent stroke patients.