To investigate the impact of exercise on the expression of adiponectin and GLUT4 mR NA in type 2 diabetic rats, type 2 diabetic rat model was made. The diabetic rats were treated with swimming training for 8 weeks. The expression of adiponectin mRNA in perirenal fat and GLUT4mRNA in skeletal muscles were assessed by reverse transcription polymerase chain reaction (RT PCR) and the levels of blood glucose, serum insulin, and blood lipid were measured. Our results showed that the expression of adiponectin mRNA and GLUT4 mRNA in diabetic model group was decreased by 45 % (P＜0.01), 43 % (P＜0.01) respectively. The gene expression of adiponectin and GLUT4 was increased significantly in swimming group (P＜0.05 and P＜0.01, respectively).Compared with the model group, fasting insulin, TG, TC and FFA were decreased significantly in the training group (P＜0.05 or P＜0.01) as compared with model group. It is concluded that exercise can promote the expression of adiponectin mRNA and GLUT4 mRNA in type 2 diabetic rats,which may be one of the mechanisms responsible for the amelioration of insulin resistance in the rats.

Objective To study the anti-fatigue effect of methylphenidate hydrochloride oral fast dissolving films (MPH-OFDF) and its mechanism .Methods 60 mice were randomly divided into 6 groups as:normal control group (physiological sa-line) ,model group (physiological saline) ,Yiqiyangxue oral liquids positive group (7 .00 mg/kg) ,MPH-OFDF high-dose group (5 .20 mg/kg) ,MPH-OFDF middle-dose group (2 .60 mg/kg) and MPH-OFDF low-dose group (1 .30 mg/kg) .Besides the normal control group ,model group and positive group were orally administered ,the other groups are administered with the drug once daily sublingually daily for consecutive 15 days .The mice were put in the load-weighted swimming test 30 min after the last oral administration ,then the anti-fatigue effect was assessed based on recording exhausting swimming time and detec-ting the levels of serum lactale dehydrogenase (LDH) ,creatine kinase (CK) ,triglycerides (TG) in mice .Results Compared with control group ,the middle-dose and the high-dose MPH could prolong the exhausting swimming time (P<0 .05 ,P<0 .01) and decrease the activity of LDH and CK significantly (P<0 .05 ,P<0 .01);in addition the middle-dose MPH could decrease the content of TG (P<0 .05) .Conclusion The MPH had marked anti-fatigue effect that may be associated with reduced ser-um LDH ,CK and TG .

Objective To observe the changes of irisin in patients before and after hemodialysis (HD),as well as the differentiation of irisin change in patients with diabetes mellitus and protein energy waste.Methods Clinical parameters of patients on maintenance hemodialysis (MHD)in Shanxi People's Hospital from September 2016 to November 2016 were collected.A total of 33 cases were enrolled——14 cases of diabetic MHD group and 19 cases of non-diabetic MHD group as divided according to etiology.Based on the presence of protein energy waste,patients were also grouped into 17 cases with and 16 cases without protein waste.Before and after HD,the non parametric test was used to compare the changes of irisin in each group.Results After HD,the irisin value of 33patients with ERSD decreased,with the difference being statistically significant [0.666(0.218,1.365) ng/L vs 0.977(0.202,1.820) ng/L,P=0.01].The difference was not statistically significant in the diabetes MHD group;statistically significant in the non diabetes group [0.666(0.178,1.351) ng/L vs 0.913(0.100,1.497) ng/L,P ＜ 0.05];and not statistically significant in the protein energy group.The irisin of diabetic MHD group and non-diabetic MHD group were compared after HD:the difference was not statistically significant.Conclusions After HD,plasma irisin levels were reduced in patients with end-stage renal disease.Diabetes and protein wasting effects are not important for irisin at HD.

In this study, self-discriminating hybrid nanocrystals was utilized to explore the biological fate of quercetin hybrid nanocrystals (QT-HNCs) with diameter around 280 nm (QT-HNCs-280) and 550 nm (QT-HNCs-550) following oral and intravenous administration and the contribution of integral nanocrystals to oral bioavailability enhancement of QT was estimated by comparing the absolute exposure of integral QT-HNCs and total QT in the liver. Results showed that QT-HNCs could reside

Objective: Fufang Biejia Ruangan Tablet (FBRT) is widely used for the treatment of liver fibrosis. However, Hominis Placenta (HP), as an important adjuvant of FBRT, has been restricted for medicinal using due to the limited availability, ethical controversy and safety issues. The present study aimed to investigate the therapeutic effects of novel FBRT (N-FBRT) with sheep placenta (SP) as substitute for HP on liver fibrosis and explore its possible mechanisms. Different dosages of SP in N-FBRT were also evaluated. Methods: Rats were subcutaneously injected with CCl

The human Shwachman-Diamond syndrome (SDS) is an autosomal recessive disease caused by mutations in a highly conserved ribosome assembly factor SBDS. The functional role of SBDS is to cooperate with another assembly factor, elongation factor 1-like (Efl1), to promote the release of eukaryotic initiation factor 6 (eIF6) from the late-stage cytoplasmic 60S precursors. In the present work, we characterized, both biochemically and structurally, the interaction between the 60S subunit and SBDS protein (Sdo1p) from yeast. Our data show that Sdo1p interacts tightly with the mature 60S subunit in vitro through its domain I and II, and is capable of bridging two 60S subunits to form a stable 2:2 dimer. Structural analysis indicates that Sdo1p bind to the ribosomal P-site, in the proximity of uL16 and uL5, and with direct contact to H69 and H38. The dynamic nature of Sdo1p on the 60S subunit, together with its strategic binding position, suggests a surveillance role of Sdo1p in monitoring the conformational maturation of the ribosomal P-site. Altogether, our data support a conformational signal-relay cascade during late-stage 60S maturation, involving uL16, Sdo1p, and Efl1p, which interrogates the functional P-site to control the departure of the anti-association factor eIF6.
Crystallography, X-Ray ; GTP Phosphohydrolases ; chemistry ; metabolism ; Humans ; Protein Domains ; Ribosome Subunits, Large, Eukaryotic ; chemistry ; metabolism ; Saccharomyces cerevisiae ; chemistry ; metabolism ; Saccharomyces cerevisiae Proteins ; chemistry ; metabolism

OBJECTIVE To study the effects of self-assembled nanoparticles from Shaoy ao gancao decoction （SGD-SAN）on the in vitro release and intestinal absorption of the main components of Glycyrrhiza uralensis . METHODS Gancao single decoction （GSD），Shaoyao single decoction （SSD），mixed suspension of Shaoyao and Gancao single decoction （MSSGD）and SGD （i.e. Shaoyao-Gancao decoction ）were prepared ，and SAN was characterized. HPLC method was adopted to determine the contents of 7 main components （liquiritin apioside ， liquiritin， isoliquiritin apioside ， isoliquiritin， liquiritigenin， glycyrrhizic acid ， isoliquiritigenin）in G. uralensis . The dialysis bag method was used to investigate the effects of the formation of SGD-SAN on in vitro release of 7 main components in G. uralensis with pH 1.2 HCl solution and pH 6.8 phosphate buffered solution （PBS）as release media. Single-pass intestinal perfusion study was performed to investigate the effects of the formation of SGD-SAN on the intestinal absorption of 7 main components from G. uralensis . RESULTS SAN with particle size of 200-300 nm and polydispersity index of 0.3-0.5 was found in GSD ，MSSGD and SGD. GSD-SAN and MSSGD-SAN were in rod shape while SGD-SAN was irregularly spherical under transmission electron microscope. The results of in vitro release study showed that the formation of SGD-SAN could significantly increase in vitro release of liquiritigenin ，isoliquiritigenin and glycyrrhizic acid ，and had no effect on other components of G. uralensis in pH 1.2 HCl solution. The formation of SGD-SAN also had no effect on the release of each component from G. uralensis in pH 6.8 PBS. The results of intestinal perfusion experiments showed that the formation of SGD-SAN could significantly promote the absorption of each component from G. uralensis in the ileum. CONCLUSIONS- The formation of SGD-SAN significantly improves the in vitro release of poorly soluble components from G. uralensis and promotes the intestinal absorption of main components from G. uralensis ，which is the physical structure basis for the compatibility and synergy of Paeonia lactiflora and G. uralensis .

OBJECTIVE： To investigate the effects of crystal form on in vivo and in vitro behavior of Astilbin nanosuspensions （AT-NS）. METHODS： AT-NS1 and AT-NS2 were prepared by precipitation method and miniaturized media milling method respectively. The particle size and polydispersity index （PDI） were determined by laser particle size analyzer. X-ray diffraction （XRD）， scanning electron microscopy （SEM）， HPLC and paddle method were used to analyze and compare the structure characteristics， appearance morphology and in vitro dissolution of AT raw material， AT-NS1 and AT-NS2. Totally 15 healthy male SD rats were randomly divided into AT raw material， AT-NS1 and AT-NS2 group， with 5 rats in each group. They were given relevant medicine suspension 120 mg/kg （using water as solvent） intragastrically； blood samples  were collected from orbit before medication （0 min） and 5， 10， 20， 30， 60， 120， 240， 480 min after medication. Using rutin as internal standard， HPLC method was used to determine plasma concentration of AT in rats. Pharmacokinetic parameters were calculated by using DAS 2.0 software and then compared. RESULTS： The particle sizes of AT-NS1 and AT-NS2 were （212.48±0.32） nm and （226.36±2.29） nm， respectively； PDI were 0.129 3±0.026 3 and 0.254 7±0.012 4. XRD analysis showed AT-NS1 was amorphous， and AT-NS2 was crystalline. Diffraction peaks of both were different from those of AT raw material. SEM analysis showed that AT-NS1 and AT-NS2 were similar in morphology， and they were spherical and uniform in size； AT raw material was lump with large particle size and different sizes. Results of dissolution tests showed that accumulative dissolution of AT raw material， AT-NS1 and AT-NS2 were 4.54％， 35.01％， 12.22％ at 1 h； accumulative dissolution of them were 24.01％， 81.14％， 64.69％ at 12 h； accumulative dissolution of them were 36.04％， 84.47％， 85.86％ at 24 h， respectively. Results of pharmacokinetic study showed， compared with AT raw material group， cmax and AUC0-∞ of AT-NS1 and AT-NS2 groups as well as t1/2z of AT-NS1 group were increased significantly， while tmax of AT-NS1 group was significantly reduced significantly （P＜0.05）. Compared with AT-NS2 goup， cmax， AUC0-∞ and t1/2z of AT-NS1 group were increased significantly， while tmax was reduced significantly （P＜0.05）. CONCLUSIONS： When AT is prepared into NS， dissolution in vitro and oral absorption in vivo of AT are increased significantly. In a short time， the dissolution/absorption of amorphous NS is faster than crystalline NS.

Objective To investigate the molecular mechanism of taurine regulating the polarization of M2 macrophages by mitophagy. Methods THP-1 cells were divided into four groups: M0 group (THP-1 cells were treated by 100 nmol/L phorbol myristate ester for 48 hours to polarize into M0), M2 group (THP-1 cells were induced to polarize into M2 macrophages by 20 ng/mL interferon-4 (IL-4) for 48 hours), M2 combined with taurine groups (added with 40 or 80 mmol/L taurine on the basis of M2 macrophages). The mRNA expression of mannose receptor C type 1(MRC-1), C-C motif chemokine ligand 22(CCL22) and dendritic cell-specific ICAM-3 grabbing non-integrin (CD209) in M2 macrophages were detected by quantitative real-time PCR. Mitochondrial and lysosome probes were used to detect the number of mitochondria and lysosomes by multifunction microplate reader and confocal laser scanning microscope. The level of mitochondrial membrane potential (MMP) was detected by JC-1 MMP assay kit. The expression of mitophagy-related proteins PTEN-induced putative kinase 1 (PINK1) and microtubule-associated protein 1 light chain 3 (LC3) were detected by Western blot analysis. Results Compared with M0 group, the expression of MRC-1, CCL22, CD209 and PINK1, the number of mitochondria and the level of MMP in M2 group were significantly increased, whereas the number of lysosomes and LC3II/LC3I ratio were decreased. Compared with M2 group, the expressions of MRC-1, CCL22 and CD209, the number of mitochondria and the level of MMP in M2 combined with taurine group dropped significantly while the number of lysosomes was found increased, and the protein expression of PINK1 and LC3II/LC3I ratio were also increased. Conclusions The polarization of M2 macrophages is regulated by taurine to prevent excessive polarization via reducing the level of MMP, improving the level of mitophagy, reducing the number of mitochondria, and inhibiting the mRNA expression of polarization markers in M2 macrophages.
Mitophagy ; Taurine ; Macrophages/metabolism* ; Protein Kinases/metabolism* ; RNA, Messenger