Animals ; Calcitonin Gene-Related Peptide ; pharmacology ; Ischemic Postconditioning ; Male ; Myocardial Reperfusion Injury ; prevention & control ; Myocardium ; metabolism ; Rats ; Rats, Sprague-Dawley

Objective To measure the temperature sensation threshold of trunk skin in healthy adults. Methods The threshold of cold sensation, warm sensation, cold pain sensation and heat pain sensation of trunk skin key points (T3, T7 and T11) were measured with Thermal Sensory Analyzer in 123 healthy adults. Results The thresholds of cold, warm, cold pain and heat pain sensations were obtained. The standard deviation of cold and warm threshold was less than that of heat pain. The range of cold sensation threshold was the largest. The heat pain sensation threshold increased with segmental declining and the sensation threshold increased with age. Conclusion Normal reference value should be established variously with the segment and age. The threshold of cold, warm varies less, while the threshold of cold pain and heat pain varies too much.

Depression is a serious mental illness with a high incidence. At present, we do not fully understand the specific pathological mechanisms of depression, and the efficacy of drug treatments is very limited. Recent studies have shown that epigenetic changes that occur in specific brain regions may be a key mechanism by which environmental factors to interact with individuals to influence the risk of depression. Therefore, drugs that target epigenetic regulation may become a new direction for the development of antidepressants. Histone deacetylase inhibitors (HDACi) are a class of compounds that inhibit histone deacetylase activity, which has been reported to be associated with depression; this article addresses the use of HDACi in preclinical studies, and their potential therapeutic role and limitations of use in depression.

AIMTo study the chemical constituents of Polygala aureocauda Dunn..

METHODSChemical compounds were isolated by column chromatography and their structures were determined mainly by spectroscopic means (UV, IR, MS, 1HNMR, 13CNMR, HMQC, HMBC).

RESULTSThree compounds were isolated and identified as 3-hydroxy-1,4-dimethoxyxanthone (I), 1, 7-dihydroxy-2, 3-methylendioxyxanthone (II), 7-hydroxy-1-methoxy-2, 3-methylendioxyxanthone (III).

CONCLUSIONCompounds I-III were isolated from Polygala aureocauda Dunn. for the first time, whereas compound I is a new xanthone.

Molecular Conformation ; Molecular Structure ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Polygala ; chemistry ; Xanthones ; chemistry ; isolation & purification

AIMTo study the active constituents of Swertia davidi Franch..

METHODSChromatography was used to isolate and purify the chemical components, their structures were identified by spectral analysis.

RESULTSThree compounds were identified as 1,7-dihydroxy-3,8-dimethoxyxanthone (gentiacaulein) (V), 1,8-dihydroxy-3,7-dimethoxyxanthone (methylswertianin) (VI) and 1,8-dihydroxy-3,4,7-trimethoxyxanthone (VII).

CONCLUSIONCompound VII is a novel xanthone, named daviditin A, the others were isolated from Swertia davidi Franch. for the first time.

Molecular Structure ; Plants, Medicinal ; chemistry ; Swertia ; chemistry ; Xanthones ; chemistry ; isolation & purification

Objective To compare the effects of moxibustion at different temperatures on blood lipid and TRPV1 in dorsal root ganglion with hyperlipidemia rats; To verify the correlation between efficacy of adjusting fat of moxibustion with activating of TRPV1. Methods The rat model of hyperlipidemia was made by high fat diet. 60 SD mice were randomly divided into four groups: control group, model control group, the 38 ℃ moxibustion group and the 45 ℃ moxibustion group, with 15 mice in each group. Acupoints Shenque and Zusanli were chosen under moxibustion for 10 minutes each time, once another day, for 4 weeks, in the 38 ℃ moxibustion group and the 45 ℃moxibustion group. Blood was taken after intervention, and blood TC, TG, LDL-C and HDL-C of the mice were detected by oxidase method; the dorsal root ganglion was taken to detect the expression of TRPV1 mRNA by real-time fluorescence quantitative PCR. Results Compared with model group, blood lipid indexes in moxibustion groups had different changes, with statistical significance compared with 45 ℃ moxibustion group (P<0.05, P<0.01), and there was statistical significance between 38 ℃ moxibustion group and 45 ℃ moxibustion group (P<0.01); there was statistical significance in TRPV1 mRNA of dorsal root ganglion among 45 ℃ moxibustion group and other three groups (P<0.01). Conclusion The correlation between efficacy of adjusting fat of moxibustion with activating of TRPV1 has been confirmed.

Recombinant humanized anti-ricin monoclonal antibody (MIL50) is a recombinant humanized monoclonal antibody targeting ricin. In this study, an ELISA method was used to establish a method for the determination of MIL50 in macaque serum, and a cross design method was used. Twelve rhesus monkeys were intravenously injected 1 mg·kg^-1 test preparation (MIL50 freeze-died powder injection) and reference preparation (MIL50 liquid preparation) to determine the plasma concentration of MIL50 at different time points, and the pharmacokinetic parameters were analyzed to compare the pharmacokinetic characteristics of MIL50 liquid preparation and freeze-died powder injection in rhesus monkeys. Animal welfare and experimental procedures follow the regulations of the Animal Ethics Committee of the Chinese Academy of Medical Sciences and Use of Laboratory Animals and the regulations derived by the Animal Care and Welfare Committee of the Institute of Radiation Medicine, Academy of Military Medical Sciences (IACUC-DWZX-2020-503). The results showed that there was no significant difference between C_max and AUC_0-5d in the two groups. The liquid preparation was the reference preparation, with C_max ratio of 101.6% and AUC_0-5d ratio of 101.9%, the 90% confidence interval of C_max was 79.42%-129.92%, and the 90% confidence interval of AUC_0-5d was 85.72%-121.18%. These results suggested that different dosage forms of MIL50 had certain differences in the changes of blood drug concentration in rhesus monkeys.

Objective To investigate the relationship between the activation of RhoA and thrombin-induced neuron injury in the cortex of fetal rats. Methods The neurons from the fetal ratcortex were culturedin vitro for 8 d; and then,they were treated by thrombin at different concentrations (0,1,10,30 and 100 U/mL) for 3 h,and by 30 U/mL thrombm at different times (0,0.5,1,3 and 6 h);Western blotting was used to examine the effects of these different treatments on the activation of RhoA.The neurons were pretreated with Exoenzyme C3,the RhoA inhibitor,for 0.5 h,and incubated with 30 U/ml thrombin for 3 h; and then,Western blotting was employed to examine the activation of Rho A; besides that,the injuries of these neurons with the presence and absence of Exoenzyme C3 were observed by Hoechst33258 staining and CCK-8 assay.Results The activation of RhoA expressing in membrane with the treatment of 30 U/mL thrombin for 3 h was significantly increased as compared with that under the treatment of 0 U/mL (P＜0.05); and the total RhoA showed no significant changes with the treatment of all concentrations. The 3 h site with thrombin (30 U/mL) could more significantly induce R hoA expression as compared with other time sites (P＜0.05),and the total RhoA showed no significant changes under the treatment of all time sites. Pretreatrnent of neurons with Exoenzyme C3 could significantly down-regulate RhoA level as compared with those without pretreatment (P＜0.05); meanwhile,Hoechst33258 staining indicated that the number of brightly stained neurons in the Exoenzyme C3presence group was dramatically decreased as compared with that in the Exoenzyme C3 absence group (P＜0.05), and CCK-8 assay showed that the cell survival rate in Exoenzyme C3 absence group significantly decreased as compared with that in the Exoenzyme C3 presence group (P＜0.05).Conclusion RhoA in membrane is related to the thrombin-induced neuron injury in the cortex of fetal

OBJECTIVETo study changes in the levels of systematic and airway local oxidative stress in patients in different stages of chronic obstructive pulmonary diseases (COPD), and explore the association between oxidative stress and glucocorticoid receptor (GR) level in the peripheral blood leukocytes.

METHODSThe levels of malonaldehyde (MDA), glutathione (GSH), superoxide dismutase (SOD) and glutathione peroxidase (GSH-PX) in induced sputum and plasma, as well as GR levels in peripheral blood leukocytes and plasma levels of cortisol and adrenocorticotrophic hormone (ACTH), were examined in 33 patients with acute exacerbations of COPD (AECOPD, group A), 27 with stable COPD (group B), and 28 healthy volunteers (including 15 smokers as group C, and 15 nonsmokers as group D).

RESULTSMDA level in induced sputum and plasma decreased, whereas the levels of GSH, SOD and GSH-PX increased significantly in the order of groups A, B, C, and D (P<0.05). The activity of SOD in induced sputum and plasma were significantly lower in group C than in group D. No significant difference was noted in the other oxidative stress indices between groups C and D (P>0.05). The plasma levels of cortisol and ACTH showed no significant difference between the 4 groups, while the GR level in peripheral blood leukocytes increased significantly in the order of groups A, B, C and D (1565-/+719, 2069-/+488, 2739-/+926, and 4793 -/+1415 U, respectively, P<0.05). After controlling for the factor of smoking status, the plasma and sputum SOD activity were both positively correlated to GR, with the partial correlation coefficient of 0.512 and 0.564, respectively (P<0.001).

CONCLUSIONPatients in different stages of COPD, especially those with AECOPD, may sustain systematic and local oxidation and anti-oxidation imbalance. Decreased SOD activity may contribute to GR level decrement in peripheral blood leukocytes in these patients.

Aged ; Female ; Glutathione Peroxidase ; metabolism ; Humans ; Leukocytes ; metabolism ; Male ; Middle Aged ; Oxidative Stress ; Pulmonary Disease, Chronic Obstructive ; metabolism ; Receptors, Glucocorticoid ; metabolism ; Superoxide Dismutase ; metabolism

OBJECTIVETo assess the efficacy and safety of azosemide in patients with edema and ascites.

METHODSA multicentral, randomized, double-blind, controlled clinical trial was applied. All 223 patients (cardiac edema 92, hepatogenic edema 63, renal edema 68) were randomized to azoesmide and furosemide group, and all patients were treated for 2 weeks. Patients with cardiac or renal edema took azosemide (30 mg/d) or furosemide (20 mg/d); patients with hepatogenic edema took azosemide (60 mg/d) or furosemide (40 mg/d). The dosage were adjusted to azosemide 60 mg/d (cardiac, renal edema), 90 mg (hepatogeic edema); or furosemide 40 mg/d (cardiac, renal edema), 60 mg (hepatogeic edema), if diuretic effects were not obtained at the end of third day.

RESULTSAt the end of the study, the weight changes were (2.87+/-3.10) kg and (2.81 +/-2.84) kg; the total effective rate of edema lessen was 89.19% and 89.81%; the total effective rate of heart function improvement was 64.44% and 66.66%; the 24 h urine output increased (321.85 +/-669.52) ml and (273.80 +/-645.72) ml for azosemide and furosemide, respectively. The total effective rate of ascites lessen (tested by B-ultrasound) was 89.28% and 86.66%; abdominal girth decreased (5.20 +/-3.58) cm and (5.03 +/-3.74) cm for azosemide and furosemide, respectively. The adverse event rate was 23.01% in azosemide group and 21.01% in furosemide group; the main adverse effects were hypokalemia, hyperuricemia, hypertriglyceridemia and thirsty.

CONCLUSIONAzosemide could effectively lessen edema, improve heart function and decrease ascitesûit is well tolerated and is particularly useful for the diuretic treatment.

Adolescent ; Adult ; Aged ; Ascites ; drug therapy ; etiology ; Diuretics ; adverse effects ; therapeutic use ; Double-Blind Method ; Edema ; drug therapy ; etiology ; Edema, Cardiac ; drug therapy ; etiology ; Female ; Heart Failure ; complications ; Humans ; Kidney Diseases ; complications ; Liver Cirrhosis ; complications ; Male ; Middle Aged ; Sulfanilamides ; adverse effects ; therapeutic use