This study was to investigate the chemical constituents of the aerial part of Zygophyllumfabago, by phytochemical methods. The compounds were isolated by silica gel and Sephadex LH-20 column chromatographies from the EtOAc extract. Their structures were characterized by various spectroscopic data (1H-NMR, 13C-NMR, MS) and comparison with the literature. As a result, thirteen compounds were isolated and their structures were identified as 1-hydroxyhinesol(1), hinesol(2), atractylenolactam(3), beta-eudesmol (4), 5alpha-hydroperoxy-beta-eudesmol(5), 12-hydroxy-valenc-1(10)-en-2-one(6), pubinernoid A(7), (6S,7E)-6-hydroxy-4,7-megastigmadien-3,9-dione(8), 3-hydroxy-5alpha, 6alpha-epoxy-beta-ionone (9), (3S,5R, 6S, 7E)-3, 5, 6-trihydroxy-7-megastigmen-9-one(10), (6R,7E,9R)-9-hydroxy-4,7-megastigmadien-3-one(11), (S)-3-hydroxy-beta-ionone(12), and blumenol A(13). Compounds 1-7 were sesquiterpenoids and 8-13 were megastigmane type norsesquiterpenoids. All the compounds were obtained from Z. fabago for the first time, and compound 1 was a new natural product.
Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Molecular Structure ; Spectrometry, Mass, Electrospray Ionization ; Terpenes ; chemistry ; isolation & purification ; Zygophyllum ; chemistry

AIMTo determine phenytoin sodium by a highly accurate nephelometric titration.

METHODSThe titration operating conditions were optimized and the solubility product constant of phenytoin silver precipitation was determined.

RESULTSThe result of the titration is comparable to those of control experiments.

CONCLUSIONThe proposed method has been found to be accurate, precise, specific, reproducible, and linear.

Nephelometry and Turbidimetry ; methods ; Phenytoin ; analysis ; Reproducibility of Results ; Solutions ; Titrimetry ; methods

Objective To evaluate the diagnostic value of conventional and dynamic contrast- enhanced MRI in lymphoma of the orbit.Methods Thirteen cases of lymphoma of the orbit,including B-C (10 cases),T-C (1 case),T-NK-C (1 case)lymphoma,and multiple myeloma (1 case),were studied using conventional MR and dynamic contrast-enhanced MR imaging with 3D fast spoiled gradient echo sequence.Calculated values included time to peak (Tpeak),washout ratio (WR),slope and enhancement ratio (ER),and time-intensity curves (TICs),and Tpeak,WR,slope and ER were calculated preoperatively.Results Eleven of the 13 lymphomas of the orbit was seen in the anterior portion of the orbit including eyelid and lacrimal gland.On conventional MRI,10 cases showed iso-intensity on T_1WI and T_2WI and all 13 cases showed moderate enhancement after contrast administration.TIC of all 13 cases showed rapid enhancing and wash-out,Tpeak was (58.7?8.5)s,and WR was (30.9?9.4)%.The accurate diagnosis with only conventional MRI was achieved in 6 out of 13 cases,while the accurate diagnosis was achieved in all 13 cases by using combined conventional MRI and dynamic enhanment MRI.Conclusion onventional MRI combined with dynamic contrast-enhanced MRI is useful for the diagnosis of lymphoma of the orbit.

Gastrectomy ; Humans ; Laparoscopy ; Stomach Neoplasms/surgery*

Accidents, Occupational ; statistics & numerical data ; China ; epidemiology ; Humans

OBJECTIVETo investigate the expression of follistatin-like protein 1 (FSTL-1) in bone metastasis of prostate cancer (BMPC), the correlation of serum FSTL-1 with the chronic inflammatory factor interleukin-6 (IL-6) and bone morphogenetic protein 6 (BMP6) , and the clinical application value of serum FSTL-1 in BMPC.

METHODSUsing ELISA, we measured the expression levels of serum FSTL-1, IL-6, and BMP6 in 35 patients with BMPC and another 30 with benign prostatic hyperplasia (BPH) and performed correlation analysis on the data obtained.

RESULTSCompared with the BPH controls, the BMPC patients showed a significantly decreased expression of serum FSTL-1 ([34.45 ± 12.35] μg/L vs [20.23 ± 8.69] μg/L, P < 0.01) and increased levels of IL-6 ([11.21 ± 8.62] μg/L vs [23.56 ± 20.12] μg/L, P < 0.05) and BMP6 ([293.50 ± 39.72] μg/L vs [428.30 ± 178.40] μg/L, P < 0.05). There was a significant negative correlation between the level of serum FSTL-1 and those of IL-6 and BMP6 in the BMPC patients, with correlation coefficients of -0.971 and -0.972, respectively (P < 0.05).

CONCLUSIONThe expression of serum FSTL-1 decreases in patients with bone metastasis of prostate cancer, and it is correlated with the levels of inflammatory factor and cell transformation factor. This finding offers a novel biological marker for the development and progression of prostate cancer as well as a new biological target factor for its intervention.

Aged ; Biomarkers, Tumor ; blood ; Bone Morphogenetic Protein 6 ; blood ; Bone Neoplasms ; blood ; secondary ; Disease Progression ; Follistatin-Related Proteins ; blood ; Humans ; Interleukin-6 ; blood ; Male ; Prostatic Hyperplasia ; blood ; Prostatic Neoplasms ; blood ; pathology

HLA-A* 2402 is one of the most frequently encountered HLA-A alleles in East Asian populations. In order to study the CD8+ T cell responses in Chinese populations, we have described the generation and functional test of HLA-A* 2402 tetramer loaded with HCMV pp65(341-349) peptide (QYDPVAALF, QYD). The cDNA of HLA-A* 2402 heavy chain was cloned by RT-PCR from one of the donors. DNA fragment encoding the ectodomain of HLA-A* 2402 heavy chain fused at its carboxyl-terminal a BirA substrate peptide (BSP) was amplified by PCR with the cloned heavy chain cDNA as a template. The wild-type gene of HLA-A* 2402-BSP was not expressed in Escherichia coli (E. coli), while mutant HLA-A* 2402-BSP gene with optimized codons was overexpressed as inclusion bodies in E. coli. Furthermore, the soluble HLA-A* 2402-QYD monomers were generated by in vitro refolding of washed inclusion bodies in the presence of beta2-microglobulin and QYD peptide. The tetramer was subsequently formed by mixing HLA-A* 2402-QYD monomers with streptavidin-PE at a molar ratio of 4:1. Flow cytometry analysis indicated that this tetramer possessed binding activity with specific CTL from HLA-A24+ donors and the frequencies of tetramer-binding CTL were 0.09% - 0.37% within total CD8+ T cells. This tetrameric agent provides a powerful tool to explore the secrets of CTL responses against HCMV antigens in HLA-A* 2402 individuals.
Amino Acid Sequence ; CD8-Positive T-Lymphocytes ; cytology ; metabolism ; Carbon-Nitrogen Ligases ; metabolism ; Electrophoresis, Polyacrylamide Gel ; Escherichia coli ; genetics ; Escherichia coli Proteins ; metabolism ; Flow Cytometry ; Gene Expression ; HLA-A Antigens ; chemistry ; genetics ; metabolism ; HLA-A24 Antigen ; Humans ; Oligopeptides ; genetics ; metabolism ; Phosphoproteins ; chemistry ; genetics ; metabolism ; Protein Multimerization ; Recombinant Fusion Proteins ; chemistry ; genetics ; metabolism ; Repressor Proteins ; metabolism ; Substrate Specificity ; T-Lymphocytes, Cytotoxic ; cytology ; metabolism ; Viral Matrix Proteins ; chemistry ; genetics ; metabolism

The release behavior of single pellet was investigated by LC/MS/MS method with tamsulosin hydrochloride (TSH) as the model drug of the research and then the pellets were divided into four groups according to the drug loading. Comparison of dissolution profiles of each group and capsule were performed using f1 and f2 factor methods to study the difference and similarity. The release profiles of single pellet, each group and capsule were analyzed using principle component analysis (PCA). The particle system was built through Matlab to get the target release profile. The result of this research demonstrated the release behavior of single pellet correlated well with the drug loading. While the dissolution profile of capsule as a reference, the similarity factor of dissolution profiles of the lower drug loading groups were 62.2, 67.1, 53.9, respectively and, 43.3 for highest drug loading group. The particle systems with different pellet distribution and same release profiles were built through release behavior of single pellet. It is of significance to investigate the release behavior of single pellets for studying the release regularity of multiple-unit drug delivery system.
Capsules ; Chemistry, Pharmaceutical ; Chromatography, Liquid ; Delayed-Action Preparations ; Drug Delivery Systems ; Drug Liberation ; Principal Component Analysis ; Sulfonamides ; administration & dosage ; chemistry ; Tandem Mass Spectrometry ; Technology, Pharmaceutical

AIMTo simplify the study on the effect of relative humidity and temperature on drug stability.

METHODSThe stability of penicillin potassium as a model was studied with programmed humidifying and heating.

RESULTSResults of our programmed humidifying and heating experiments are comparable to those of traditional experiment at constant humidity and temperature.

CONCLUSIONProgrammed humidifying and heating experiments are applicable to drug stability study.

Drug Stability ; Hot Temperature ; Humidity ; Penicillins ; chemistry

AIMTo produce poly (lactic-co-glycolic acid) (PLGA) microspheres, containing a staphylokinase variant (K35R, DGR) with reduced immunogenecity and antiplatelet aggregation activities, which allowed the preservation of protein stability during both particle processing and drug release.

METHODSDGR-loaded microspheres were fabricated using a double emulsion-solvent evaporation technique. The effects of preparative parameters, such as stirring rate, polymer concentration, and the excipients of both internal and external aqueous phase (W2), on DGR encapsulation efficiency and microsphere characteristics were investigated. In vitro and in vivo release of DGR were conducted and the cause for instability of DGR during release was also investigated.

RESULTSModerate ultrasonic treatment of aqueous DGR/dichloromethane mixtures caused approximately. Eighty four per cent DGR denaturation. However, the activity recovery of DGR almost amounted to 100% when 2% polyvinyl alcohol (PVA) was addled into the aqueous phase. It was found that NaCl in the external water phase significantly increased DGR encapsulation efficiency. Furthermore, NaCl in the external water phase played a role in determining size and surface morphology of microsphere. In vitro release test showed a burst release of DGR from microspheres, followed by sustained release of 50% total activity over 15 days. In vivo experiments showed that DGR released from microspheres sustained 5 days. Denaturation of DGR within microspheres might be resulted from acidic microclimate.

CONCLUSIONThe stability of DGR was effectively protected during microencapsulation and a relatively high encapsulation efficiency of DGR was obtained. PLGA microspheres could be an effective carrier for DGR.

Animals ; Area Under Curve ; Drug Carriers ; Drug Compounding ; Drug Delivery Systems ; Escherichia coli Proteins ; administration & dosage ; genetics ; pharmacokinetics ; Genetic Variation ; Lactic Acid ; Male ; Metalloendopeptidases ; administration & dosage ; genetics ; pharmacokinetics ; Microspheres ; Particle Size ; Polyglycolic Acid ; Polymers ; Rabbits