OBJECTIVE: To obtain and mutate a marine Bacillus megaterium to resolute pharmaceutical intermediate, 3-chloro-1,2-epoxypropane. METHODS: From marine sediment, a 3-chloro-1,2-epoxypropane-resolute strain was isolated and mutated by ultraviolet rays and N+ ion. RESULTS: The strain was identified as Bacillus megaterium on the basis of biophysical and biochemical test. The optimum salinity for growth was 2%, and the result of optimum salinity showed that the microbe was a typical marine microorganism. A positive mutant exhibited excellent resolution with ee value of 99% and yield of 42%. CONCLUSION: The marine bacillus megaterium shows a large potential for industrial production.

Objective A method was developed for determination of the total triterpene glycosides in different sea cucumbers.Methods A holostane triterpene glycoside called Echinoside A was taken as the reference standard.Triterpene glycosides were reacted with vanillin and perchloric acid.The sea cucumbers were extracted by 60% ethanol and partitioned between water and n-butanol to gain the total triterpene glycosides.The contents of total triterpene glycosides in 11 kinds of sea cucumbers were determined with the standard curve.And the relationships of the triterpene glycosides content among different sea cucumber species,growth environment,process technique,etc.were discussed by the value of TG/P(triterpene glycosides content /protein content).Results The determination wavelength was confirmed to be 560nm and the standard curve was determined as y-1.3414x-0.0077.The ab-sorbance was of a good linearity in the mass range of 0-0.5mg with R2 =0.9994.The recovery of this method was(99.01?2.82)% and the relative standard deviation was 4.68%.Conclusion The method has been proved to be convenient,reliable and suitable for the analysis of triterpene glycosides in sea cucumbers.

During the washing process of coarse bear gall powder extracts, it is necessary to adjust the amount of ethyl acetate according to the properties of raw materials, which aims to improving the yield and purity of the final product. In the research, using NIR spectra to reflect the comprehensive properties of coarse bear gall powder extracts, the process is optimized in a flexible way. Forty batches experiments are designed according to the weight ratio of ethyl acetate and coarse extracts of bear gall powder. The NIR spectra of the coarse extracts of bear gall powder are collected and processed using principal component analysis (PCA) method. The first 8 principal components combined with the amount of the ethyl acetate are used as the input variables, and calibration models are established to predict the yield and purity of the final product 30 batches are used as calibration set, which is used to establish the models, and other 10 batches are used as validation set, which is used for the performance appraisal of the established models. The correlation coefficients of the calibration, inner cross-validation and external validation for the purity model are 0.902, 0.896 and 0.883, respectively, and the RMSEC, RMSECV and RMSEP are 1.22%, 1.48% and 1.59%, respectively. The correlation coefficients of the calibration, inner cross-validation and external validation for the yield model are 0.921, 0.859 and 0.916, respectively, and the RMSEC, RMSECV and RMSEP are 1.39%, 1.65% and 1.53% respectively. This work demonstrated that NIR spectra combined with technology parameter could be used to predict the yield and purity of the final product. Using the established models, the most appropriate amount of the ethyl acetate can be determined according to the properties of the coarse bear gall powder extracts, and the yield and purity of the final product can be improved.
Acetates ; chemistry ; Animals ; Gallbladder ; chemistry ; Medicine, Chinese Traditional ; Powders ; chemistry ; Principal Component Analysis ; methods ; Spectroscopy, Near-Infrared ; methods ; Ursidae

In this paper, NIRS (near infrared spectroscopy)-based total quality control system for the Tanreqing injection was introduced briefly. By analyzing and summing up the significance and difficulties, several important problems of the practical applications which need urgent solutions are proposed. And also the applicationprospect of NIRS is fully discussed and put forward in the end.
Drug Compounding ; standards ; Drugs, Chinese Herbal ; administration & dosage ; analysis ; standards ; Injections ; Quality Control ; Reproducibility of Results ; Spectroscopy, Near-Infrared ; methods

Water soluble extract (WSE) is an important index for the quality evaluation of Astragali Radix (AR). In this study, the WSE of the wild AR from Shanxi province (SX) and the cultivated AR from Gansu Province (GS) were compared. The WSEs of two types of AR were determined according to the appendix of Chinese pharmacopoeia. Then the WSEs were subjected to NMR analysis, and the obtained data were analyzed using HCA, PCA, OPLS-DA, microarray analysis, and Spearman rank analysis. In addition, the Pearson correlation of differential metabolites were also calculated. The results showed that the WSE content of GS-AR (37.80%) was higher than that of SX-AR (32.13%). The main constituent of WSE was sucrose, and other 18 compounds, including amino acids, organic acids, were also detected. Multivariate analysis revealed that SX-AR contained more choline, succinic acid, citric acid, glutamate, taurine and aspartate, while GS samples contained more sucrose, arginine and fumaric acid. In addition, the Pearson correlations between different metabolites of the two types of AR also showed apparent differences. The results suggested that the WSE of two types of AR differs not only in the content, but also in the chemical compositions. Thus, the cultivation way is important to the quality of AR. This study supplied a new method for the comparison of extract of herbal drugs.
Arginine ; analysis ; Aspartic Acid ; analysis ; Choline ; analysis ; Citric Acid ; analysis ; Drugs, Chinese Herbal ; analysis ; chemistry ; Fumarates ; analysis ; Glutamic Acid ; analysis ; Magnetic Resonance Spectroscopy ; Multivariate Analysis ; Phylogeography ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Succinic Acid ; analysis ; Sucrose ; analysis ; Taurine ; analysis

Bicyclol with benzyl alcohol structure, is a poorly water-soluble drug, used for the treatment of chronic hepatitis B. To increase the drug solubility and oral bioavailability, a Bicyclol-phospholipid complex was studied on its preparation, formation mechanism, and the influence on drug physicochemical properties and oral absorption. The complex was prepared by a solvent evaporation method. The optimal formulation was selected by orthogonal experimental design, and a reasonable evaluating method of the complexation rate was established. Various methods, such as differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and 31P nuclear magnetic resonance (31P-NMR), were used to explore the phase state and formation mechanism of the complex. The solubility of drug in complex was investigated in water/n-octanol. Preliminary study of its absorption and liver tissue distribution in rats was also carried out. The results showed that Bicyclol and phosphatidylcholine can be complexed entirely in the molar ratio 1 : 2. Bicyclol was dispersed in phospholipids as amorphous state. They were combined by intermolecular hydrogen bond due to charge transfer effect which occurred between the two polarities of the double bond between phosphorus and oxygen (P=O) of phosphatidylcholine and benzalcohol group of Bicyclol. The solubility of the complex compared to the active pharmaceutical ingredient (API) was effectively enhanced 5.75 times in water and 7.72 times in n-octanol, separately. In addition, drug concentrations were also enhanced 43 times in plasma and 13 times in liver with one hour after administering the complex to rats via oral gavage. All of these indicated that Bicyclol with benzalcohol group can interact with phospholipids to form complex, improving drug's physicochemical properties, thus further increasing its absorption and target tissue distribution. This study also provided theoretical reference for the research of other benzalcohol derivatives complexed with phospholipids.
1-Octanol ; Animals ; Biological Availability ; Biphenyl Compounds ; pharmacokinetics ; Calorimetry, Differential Scanning ; Chemistry, Pharmaceutical ; Phospholipids ; pharmacokinetics ; Rats ; Solubility ; Spectroscopy, Fourier Transform Infrared ; Tissue Distribution ; X-Ray Diffraction

Fosfomycin (FOM) is an antibiotic with a small relative molecular weight (138.1) and a long half-life, and has a unique chemical structure and antibacterial mechanisms. It exerts a bactericidal activity by inhibiting the early synthesis of bacterial cell walls. It is also a broad-spectrum antibiotic with a good drug tolerance and compliance and a low pressure to bacterial resistance, but no cross-resistance with other antibiotics. Recent studies show the effectiveness of FOM in the treatment of acute uncomplicated urinary tract infections and urogenital tract infections as well, such as prostatitis and epididymitis. This review focuses on the clinical application of FOM in the treatment of infectious diseases of the urogenital tract.
Anti-Bacterial Agents ; therapeutic use ; Epididymitis ; drug therapy ; Fosfomycin ; therapeutic use ; Humans ; Male ; Male Urogenital Diseases ; drug therapy ; Prostatitis ; drug therapy ; Urinary Tract Infections ; drug therapy

Objective To investigate the roles of different effective dosages of morphine on incision pain in rats.Methods Clean-degree male SD rats were randomly allocated to three groups(n=11): normal saline group(NS group),low-dose morphine group(LM group,0.6 mg/kg) and high-dose morphine group(HM group,6 mg/kg).After administration of morphine twice at 30 min interval,the incision pain models of rats were prepared according to the Brennan's method.Morphine was administered once again following the operation,while the NS group was administrated isovolumic normal saline.Then the mechanical threshold of rats was detected with von Frey filaments from the pre-operation to the 8th postoperative day,and the hyperalgesia induced by morphine on the praxiology level was explored. ResultsThe values of mechanical threshold postoperation in each group were significantly lower than those of the baseline.The mechanical threshold of HM group was significantly higher than the NS group on the second day postoperation(P

Objective To explore the methods and clinical value of transrectal ultrasound (TRUS) in detecting rectal gastrointestinal stromal tumor(GIST) with head scanning probe.Methods A total of 12 patients had the ultrasonic examination through the rectum with the head scanning probe.Preoperative ultrasonic findings were compared with the pathological results.Results Of the 12 patients,the patients were divided into three groups,including 3 cases with low-degree severity,6 cases with moderate-degree severity and 6 cases with high-degree severity.The lymph node metastasis was not found near intestines.Rectal GIST appeared as a hypoechoic mass with clear limit、regular form and expanded growth under TRUS.The CDFI showed abundant flow in the tumor and TRUS had an overall accuracy rate of 75.0%(9/12)in the diagnosis of rectal GIST.The accuracy of TRUS in the staging diagnosis of rectal GIST was 83.3%(10/12).Conclusion The TRUS with the head scanning probe is of great value for pre-operative diagnosis and staging of rectal GIST.Rectal water window and felicitous check-up technique can enhance the accuracy of TRUS.

Objective To investigate the diagnostic value of the recombinant surface antigen 1 (rSAG1) in immunodiagnosis of toxoplasmosis. Methods Isopropyl β-D- 1 -thio-galaetopyranoside (IPTG) was used to induce the expression of recombinant plasmid pET28a-SAG1 of Escherich coli(pET28a-SAG1/BL21 ). The expression products (rSAG1) of pET28a-SAG1/BL21 were identified by Western blotting. The serum of mice infected with Toxoplasma gondii tachyzoites, normal mouse serum and the serum from 10 toxoplasma gondii patients were used as primary anti-Toxoplasma gondii antibodies, and the rSAG1 gene products were identified by Western blotting, by which the diagnostic value of rSAG1 in Toxoplasmosis was compared. Results After induction and purification, rSAG1 protein was obtained and its relative molecular mass was 38.5 × 103. The fusion protein could be recognized by the serum of mouse infected with Toxoplasma gondii tachyzoites, rSAG1 of expression products of surface membrane antigen SAG1 gene from Toxoplasma Gondii could be detected in 4 cases from 10 patients by Westem blotting.Conclusion The rSAG1 has a potential value in the immunodiagnosis of Toxoplasmosis.