Objective To observe the effect of recombinant human mannose-binding lectin (RhMBL)on the expression of Bcl-2 and p53 gene in thyroid cancer cell lines.Methods Two kinds of thyroid cancer cell lines( K1 cells and FTC-133 cells) were dealed with different concentrations of rhMBL( control group:0 mg/L;experimental group:1 mg/L),then total protein was extracted to detect the expression of Bcl-2 and p53 by Western Blot.Results The expression level of p53 and Bcl-2 were observed to be obviously down-regulated after incubation with RhMBL.( 1 ) K1 cells:There was significant difference on the expression of p53 and Bcl-2 between control group and experimental group [ p53:( 1.51 ± 0.29) vs (0.74 ±0.07),t =7.63 ; P =0.040;Bcl-2:( 1.20 ± 0.07 ) vs ( 0.59 ± 0.04 ),t =6.28,P =0.001 ] ; ( 2 ) FTC-133 cells:there was also significant difference on the expression of p53 and Bcl-2 between control group and experimental group [ p53:( 0.88 ±0.14) vs(0.35 ±0.08),t =3.29,P=0.003; Bcl-2:(1.07±0.11) vs (0.33 ±0.06),t =5.73,P=0.000 ].Conclusion Bcl-2 and p53 may play an important role on the induction of thyroid cancer cell apoptosis and inhibition its proliferation by RhMBL.

BACKGROUND:Recent studies have suggested that intranasal administration is one of the ways to target drugdelivery, and can effectively make the drug that cannot pass through the blood brain barrier by other pathways to bypass the blood brain barrier, resulting in targeted delivery to the brain. It provides a promising route for the treatment of central nervous system diseases. OBJECTIVE: To study the pharmacokinetic and brain-targeted channel-tropism tissue distribution character of cimicifugoside H-1 after nasal and intravenous administration in plasma and tissues in rats, in order to evaluate the feasibility of developing brain-targeted nasal delivery system of cimicifugoside H-1 by the passage between nose and brain in nasal olfactory area. METHODS: After intravenous injection and nasal administration of cimicifugoside H-1, the drug concentrations of plasma and channel-tropism organs (lung, spleen, stomach, large intestine, liver, kidney, brain, brain, cerebelum, cerebrospinal fluid, olfactory bulb and olfactory region) were detected. Drug-time curve was drawn. DAS program was used to select apartment model and pharmacokinetics parameters. RESULTS AND CONCLUSION:(1) The pharmacokinetics characters of cimicifugoside H-1 are rapidly absorbed and extensively distribution. Among major channel-tropism organs, drug concentrations were higher in the lung and brain than in the other organs. (2) Cimicifugoside H-1 could be straightly transported into brain by the intranasal administration. The molecule through olfactory mucosa in nasal cavity entered into olfactory bulb in arachno-hypostegal cavity, and then entered into olfactory region, cerebrospinal fluid, cerebrum and cerebelum gradualy. Olfactory bulb was the only way for drug molecule to go through nasal cavity into brain. (3) Compared with the intravenous injection, cimicifugoside H-1 through the intranasal administration has a significant

A novel series of fingolimod analogues containing diphenyl ether moiety were designed and synthesized based on the modification of immunosuppressive agent fingolimod used in the treatment of multiple sclerosis. Compounds were evaluated in vivo for lymphopenic activity and heart rate affection. Most compounds showed moderate lymphopenic activity. It is worth noting that compounds 6c, 6d and 14c-14e showed considerable immunosuppressive activities comparable to fingolimod. And compound 14e had no effect on heart rate.

Objective: To investigate the prevalence of postmenopausal osteoporosis (PMOP) and analyze its influencing factors among women at ages of 50 to 59 years in Dali Bai Autonomous Prefecture, Yunnan Province, so as to provide insights into the prevention of PMOP among menopausal women. Methods: Bai Ethnic menopausal women at ages of 50 to 59 years who received healthy examination at the Center of Healthy Examination, Dali Prefecture People's Hospital from June 2017 to May 2021 were selected as the study subjects, and subjects' demographic characteristics, living habits, history of diseases, family history of osteoporosis and history of parturition were collected using self-designed questionnaires. The height, body weight and bone density were measured, and fasting blood glucose, vitamin D3, blood lipids and liver functions were detected. The factors affecting the development of PMOP were identified using a multivariable logistic regression model. Results: Totally 2 000 questionnaires were allocated, and 1 584 valid questionnaires were recovered, with an effective recovery rate of 79.20%. The respondents had a mean age of ( 56.22±2.61 ) years, and mean body mass index ( BMI ) of ( 24.62±2.35 ) kg/m2. There were 497 respondents ( 31.38% ) with a family history of osteoporosis, and the prevalence of PMOP was 20.64%. Multivariable logistic regression analysis identified age ( OR=1.135, 95%CI: 1.074-1.196 ), age of menarche ( OR=1.138, 95%CI: 1.059-1.217 ), duration of menopause (OR=1.425, 95%CI: 1.228-1.622), number of parturition ( >2, OR=5.036, 95%CI: 2.972-7.101 ), smoking ( OR=2.594, 95%CI: 1.767- 3.421 ), alcohol consumption ( OR=2.051, 95%CI: 1.503-2.598 ), family history of osteoporosis ( OR=2.540, 95%CI: 1.769-3.311 ), hypertension ( OR=1.492, 95%CI: 1.406-1.578 ), diabetes ( OR=1.774, 95%CI: 1.581-1.967 ), total cholesterol ( OR=1.483, 95%CI: 1.251-1.716 ), triacylglycerol ( OR=1.801, 95%CI: 1.576-2.026 ), low-density lipoprotein cholesterol ( OR=1.614, 95%CI: 1.498-1.731 ), fasting blood glucose ( OR=1.192, 95%CI: 1.077-1.307 ), BMI ( OR=0.934, 95%CI: 0.862-0.993 ), outdoor activity ( ≥1 time/week, OR: 0.413-0.549, 95%CI: 0.329-0.637 ), age of menopause ( OR=0.909, 95%CI: 0.841-0.977 ), daily intake of calcium ( ≥600 mg, OR: 0.493-0.644, 95%CI: 0.389-0.786 ), vitamin D3 level ( ≥20 ng/mL, OR: 0.604-0.719, 95%CI: 0.523-0.853 ) and high-density lipoprotein cholesterol ( OR=0.658, 95%CI: 0.550-0.767 ) as factors affecting the development of PMOP. Conclusions The prevalence of PMOP in Dali Bai Autonomous Prefecture is similar to the nationwide level in China, and old age, smoking, alcohol consumption, a family history of osteoporosis and high blood lipid levels may increase the risk of PMOP.

Objective To analyze the application of dexmedetomidine in intracranial arterial stenting and its influence on the serum myocardial enzyme ,cardiac troponin I(cTnI) and left ventricular ejection fraction (LVEF). Methods From March 2015 to March 2017,94 cases with intracranial arterial stenting in the People's Hospital of Lishui were divided into control group and observation group by the random number table method ,with 47 cases in each group.The control group was treated with conventional anesthesia ,the observation group was treated with dexme-detomidine.The enzyme creatine phosphate kinase isoenzyme (CK -MB),creatine phosphate kinase (CK),cTnI, LVEF,inflammatory factor, neural function, brain oxygen metabolism and complications in the two groups were compared.Results After surgery,the CK-MB,CK,cTnI levels of the observation group were lower than those of the control group[(35.27 ±4.41) U/L,(488.30 ±61.03) U/L,(3.85 ±0.49) μg/L vs.(46.40 ±5.79) U/L, (611.21 ±76.40)U/L,(4.72 ±0.59)μg/L],the LVEF of the observation group was higher than that of the control group[(45.60 ±5.72)%vs.(43.12 ±5.39)%],the differences were statistically significant (t＝10.484,8.619, 7.777,2.163,all P＜0.05).The interleukin -6(IL-6) and interleukin -8(IL-8),tumor necrosis factor -α (TNF-α),S-100β,specificity enolization enzyme(NSE),cerebral metabolic rate of oxygen(ERO2),arterial blood oxygen saturation(PaO2),carotid venous blood oxygen saturation (SjvO2) of the observation group were better than those of the control group(t＝5.794,6.177,15.065,6.964,5.606,3.147,2.116,2.807,all P＜0.05).The inci-dence rate of complication of the observation group was lower than that of the control group (χ2＝17.091,P＜0.05). Conclusion Application of dexmedetomidine in intracranial arterial stenting can protect myocardium , inhibit the serum levels of myocardial enzyme ,cTnI rise,and is conducive to the recovery of LVEF.

A new coronavirus (SARS-CoV-2) has been identified as the etiologic agent for the COVID-19 outbreak. Currently, effective treatment options remain very limited for this disease; therefore, there is an urgent need to identify new anti-COVID-19 agents. In this study, we screened over 6,000 compounds that included approved drugs, drug candidates in clinical trials, and pharmacologically active compounds to identify leads that target the SARS-CoV-2 papain-like protease (PLpro). Together with main protease (M
Antiviral Agents/therapeutic use* ; Binding Sites ; COVID-19/virology* ; Coronavirus Papain-Like Proteases/metabolism* ; Crystallography, X-Ray ; Drug Evaluation, Preclinical ; Drug Repositioning ; High-Throughput Screening Assays/methods* ; Humans ; Imidazoles/therapeutic use* ; Inhibitory Concentration 50 ; Molecular Dynamics Simulation ; Mutagenesis, Site-Directed ; Naphthoquinones/therapeutic use* ; Protease Inhibitors/therapeutic use* ; Protein Structure, Tertiary ; Recombinant Proteins/isolation & purification* ; SARS-CoV-2/isolation & purification*