Objective To investigate the characteristics of materiome release kinetics of Liuwei Dihuang Pills (LDP), and to evaluate its visualization. Methods According to the 2015 edition of Chinese Pharmacopia, using the evaluation methods of release kinetics of Chinese material medica to determine the materiomics release kinetics and the releasecharacteristic of LDP by the paddle method. Then f2 fit factor was calculated and evaluated on other types of LDP in comparison with water-bindered pills and condensed pills as, which are two most common preparations in the market. Moreover, materiome release spectrum and release increment spectrum were used, hoping to quantify, integrate and visualise the materiome release characteristics of different types of LDP. Results The kinetic characteristics of the LDP accord with the Weibull release model, T50 and Td were calculated, and there are significant differences between different types of pills (P < 0.05) in addition to condensed pills and water pills. Also, some differences and similarities in the materiomics release characteristic by f2 fit factor were found in the study. Materiome release spectrum and release increment spectrum can be used to quantify, integrate and visualise the materiome release characteristics of LDP on different types. Conclusion The materiomics release kinetics can be applied to quantify, integrate and visualise the materiome release characteristic of LDP on different types. Basically in agreement with the saying, “water pills from the facilitation, honey pills take the slow, paste pills from the late of, wax-wrapped pills take the difficult”.

Objective: To investigate the relationship among powder particle size, cell wall-breaking rate, and dissolution of Liuwei Dihuang Pill (LDP) in vitro. Methods: Particle size and cell wall-breaking rate of four kinds of LDP were measured by laser particle size instrument and optical microscope. The loganin and paeonol were taken as indexes, the feature of dissolution for the above four kinds of LDP was examined by grouting method. Results: There were significant differences in the distribution of particle size, wall-breaking rate, and dissolution among different crushing degrees of LDP. With the decrease of the powder particle size, the wall-breaking rate and relative cumulative dissolution of loganin and paeonol increased. The rate of characteristic cell wall-breaking in the micro powder of Corni Fructus, Alismatis Rhizoma, and Moutan Cortex could reach 100%. Conclusion: Moderately changing degree of smash could cause cell wall-breaking rate changes, so as to control effective ingredient the dissolution rate and extent of Chinese medicine.

Objective: To study the analgesic effects of aqueous extract from Asari Radix et Rhizoma (ARR) combined with Nimodipine and its mechanism. Methods: Forty healthy male Wistar rats were r andomly divided into control, model, ARR, Nimodipine, and ARR+Nimodipine groups. Except the control group, the neuropathic pain models of rats were produced in the rest groups by the ligation of sciatic nerve. Rats in each group were ig administered for two weeks after operation. The aqueous extract (200 mg/kg) from ARR was given to rats in ARR group, Nimodipine (40 mg/kg) was given to rats in Nimodipine group, and the aqueous extract (200 mg/kg) from ARR was given to rats after 30 min administration of Nimodipine (40 mg/kg) in ARR+Nimodipine group, and physiological saline was given to rats in the control and model groups. Thermal paw withdrawal latency and mechanical paw withdrawal reflex threshold of rats in each group were measured on one day before operation and on the days 1, 3, 5, 9, and 14 after 30 min of administration. Results: The thermal paw withdrawal latency and mechanical paw withdrawal reflex threshold of rats in each group were not significantly different before and after the operation (P>0.05). The thermal paw withdrawal latency and mechanical paw withdrawal reflex threshold of rats in the model group were significantly lower than those in the control group at various time points after the operation (P<0.05 and 0.01). The thermal paw withdrawal latency and mechanical paw withdrawal reflex threshold of rats in ARR and Nimodipine groups were significantly higher than those in the model group from the day 5 after the operation (P<0.05 and 0.01). The thermal paw withdrawal latency and mechanical paw withdrawal reflex threshold of rats in ARR+Nimodipine group were significantly higher than those in the model group from the day 3 after the operation (P<0.05 and 0.01), and were significantly higher than those of both in ARR and Nimodipine groups from the day 5 after the operation (P<0.05 and 0.01). Analgesic effects of ARR+Nimodipine group were better than those of separate ARR and Nimodipine groups. Conclusion: The aqueous extract from ARR combined with Nimodipine has the ideal analgesic effects.

Objective To improve the diagnosis and treatment of xanthogranulomatous pyelonephri- tis(XGP).Methods The clinical data of 18 cases(5 males and 13 females;mean age,47 years)with XGP were analyzed.Of them,6 had the lesion on the left,and 12 on the right.Before operation,XGP was mis- diagnosed as renal calculus with hydronephrosis in 4 cases,ureteral calculus with severe hydronephrosis in 3 cases,renal tuberculosis in 3 cases and renal carcinoma in 8 cases.Results Of the 18 cases,7 were diag- nosed to have XGP by frozen section during operation and 11 cases had a definite diagnosis by pathological examination after nephrectomy.After a follow-up of 6-124 months,no recurrence was observed in all these 18 cases.Conclusions Preoperative diagnosis of XGP is difficult.This disease is clinically characterized by foam cells in urine smear,low-density value of kidney CT and ineffective antibiotic therapy.Combined a- nalysis of clinical data and improvement of clinical recognition of XGP is the key to avoiding delayed diagno- sis or misdiagnosis of XGP.

As one of the major sources of infection, viruses could infect all organisms including bacteria, plants, animals, and humans. Infectious diseases caused by viruses pose a great threat and damage to human health and economic activities all over the world. Adaptor-associated protein kinase 1 (AAK1) is a member of the Ark1/Prk1 family of serine/threonine kinases and a specific key kinase regulating the phosphorylation of AP-2 protein μ2 subunit T156. In the past, AAK1 has been regarded as a feasible biological target for the treatment of nerve pain. Recently, scientists have found that inhibiting AAK1 can regulate endocytosis and inhibit virus invasion into cells. Therefore, AAK1 could be the potential target of anti-virus therapy. This paper reviews the research progress of small molecule AAK1 inhibitors in the field of antiviral, analyzes the future research directions and challenges, and provides new ideas for the development of antiviral drugs targeting AAK1.

This study is designed to obtain recombinant human acetylcholinesterase (rhAChE) and apply it in screening acetylcholinesterase inhibitors. The rhAChE was overexpressed in HEK293 cells transfected by plasmid of pCMV-AChE with the cationic liposome and rhAChE was found to be secreted into cell culture medium. AChE activity was assayed according to modified Ellman method to obtain kinetic parameters. IC so50 values for donepezil compounds of rhAChE were calculated to determine their activities of inhibition. The results showed that Km value was 151.9 micromol.L-1 donepezil inhibited rhAChE in a mixed competitive-noncompetitive way (Ki= 16.03 nmol.L-1, Ki = 18.36 nmol.L-1) and that most new compounds tested exhibited high activities of inhibition on rhAChE. The study suggests that rhAChE is available to be applied in screening AChE inhibitors in vitro.
Acetylcholinesterase ; genetics ; metabolism ; Cholinesterase Inhibitors ; analysis ; pharmacology ; HEK293 Cells ; Humans ; Indans ; analysis ; pharmacology ; Inhibitory Concentration 50 ; Kinetics ; Piperidines ; analysis ; pharmacology ; Plasmids ; Recombinant Proteins ; genetics ; metabolism ; Transfection

Objective To evaluate the in vitro antibacterial activity of fusidic acid against P.acnes.Methods Fifty strains of P.acnes were clinically isolated from Huashan Hospital,Fudan University from March to September 2013.The minimum inhibitory concentrations (MICs) of several antibacterial agents including fusidic acid against these P.aches isolates were determined by using the agar dilution method according to the recommendations of Clinical and Laboratory Standards Institute (CLSI).Data were analyzed using the WHONET 5.4 software.Results Among the 50 P.acnes isolates,90％ were sensitive to fusidic acid,90％ to moxifloxacin,54％ to clindamycin,46％ to erythromycin,but 100％ were resistant to metronidazole.The minimum concentration required to inhibit the growth of 50％ organisms (MIC50) and 90％ organisms (MIC90) were 0.5 and 1.0 mg/L respectively for fusidic acid,whereas clindamycin and erythromycin both showed higher MIC90 values (＞ 128 mg/L).At the concentration of 128 mg/L,clindamycin inhibited the growth of 70％ of the P.acnes isolates,and erythromycin inhibited the growth of 48％ of them,while the growth of all the isolates was inhibited by fusidic acid at 2 mg/L.Conclusion Fusidic acid exhibits excellent antibacterial activity against clinical isolates of P.acnes in vitro.

Two thermotolerant, ethanol-producing yeast cultures: THFY-4 and THFY-16 were isolated from 381 nature samples. THFY-4 can grow on 30% glucose plate at 51 ℃,while THFY-16 can grow on the same medium at 45℃.After preliminary ide ntification, THFY-4 was identified as Kluyveromyces sp. and THFY-16 belon gs to Saccharomyces genus. The ethanol fermentation experiment shows that T HFY-4 can only produce 4.88% (v/v) ethanol from 20% glucose after 60 hours, wh ile THFY-16 can produce 11.44% ethanol under the same condition. When using s accharified Canna edulis Ker wort as fermentation medium, 9.43%(v/v) ethanol we re produced from 16.1% glucose, which is 91.0% of the theoretical yield.

Objective To study the effects of the inhibition of nuclear factor kappa-B ( NF-κB) , on the hepatic heat shock protein 70 (HSP70) expression as well as on the changes of hepatic function and ultrastructure in a rodent model of hemonhageic shock. Method Hemorrhagic shock was produced by inducing bilateral femoral fractures in male Wistar rats. Intraperitoneal injection of pyrrolidine dithiocarbamate(PDTC)was used to inhibit NF-κB activation 1 hour before induction of shock. A total of 66 adult male Wistar rats were randomly divided into 3 groups: control group (Control, n = 6), trauma shock (TS, n = 30), and NF-κB inhibition followed by trauma shock (NF-κB inhibition, n =30). Measurements of hepatic NF-KB and HSP70, hepatic function bio-markers, TNF-α and IL-6 were obtained 0.5, 2, 4, 6, 8 hours after trauma. Histopathological changes in liver tissues were also noted. Hepatic expression of NF-κB was determined by using electrophoretic mobility shift assay, while HSP70 was assayed by western blot and analyzed with computer imaging. Results In rats with trauma shock, both hepatic NF-κB activity and HSP70 expression increased significantly compared to the control group, reaching peaks at 6 hour post injury. Serum alanine transferase (ALT) and total bilirubin (TB) also rose significantly,reaching peaks at 8 hours post trauma. Light microscopy revealed hepatic congestion with infiltration of inflammatory cells into hepatic sinusoid in the TS group at 8 hours. Inhibiting the activity of NF-κB one hour before trauma significantly decreased expression of HSP70 at 6 hours post trauma [16.9±4.4 (NF-κB inhibition) vs. 23.0±1.7 (TS), P ＜ 0.05]. In addition,levels TNF-α and IL-6 in the liver tissue also decreased, and hepatic congestion as well as hepatic cell degeneration were ameliorated, showing minimal inflammatory infiltrates in the hepatic sinusoids. NF-κB inhibition also significantly lowered the levels of ALT and TB at 4 hours post trauma [ALT, 540.8 ±66.2 nmol/L (NF-KB inhibition) vs. 640.6±80.2 nmol/L (TS), P ＜ 0.05; TB,2.3±0.3 mol/L (NF-κB inhibition) vs. 4.7 ±1.1 mol/L (TS), P ＜ 0.05]. Conclusions NF-κB and HSP70 are involved in the pathogenesis of hepatic injury during hemorrhagic shock, and the degree of NF-κB activity and HSP70 expression may be consistent with the extent of hepatocellular damage. Inhibition of NF-κB helps ameliorate liver injury due to trauma shock.