Adult ; Cholesteatoma, Middle Ear ; Humans ; Male

Febuxostat, as a xanthine oxidase inhibitor, is a classic anti-gout drug with significant therapeutic effects and good tolerability. The structures of febuxostat and its derivatives can be divided into two parts: a substituted phenyl ring and a five-membered or six-membered heterocyclic ring with a carboxyl substitution. This paper reviewed the research progress of febuxostat derivatives in recent ten years and classified the structure-activity relationships of various febuxostat derivatives. Exploring the action mechanisms and structure-activity relationships of xanthine oxidase inhibitors might be significant for the rational design and development of new anti-gout chemical entities.

From original concept and literature of acupoint, the concept and clinical significance of ashi method is discussed, which clarifies that the essence of ashi method is to locate the acupoints by patients' sensitivity on force. The clinical application of heat-sensitive moxibustion has illustrated that positioning method of this therapy is based on the appearance of heat-sensitive moxibustion sensation. Although both types are based on patients' feeling, positioning method of heat-sensitive moxibustion stands on a new angle and uses a new method to locate acupoint. Therefore, it is believed that the positioning method of heat-sensitive moxibustion is the inheritance and development of ashi method.
Acupuncture Points ; China ; History, Ancient ; Humans ; Medicine in Literature ; Moxibustion ; history ; methods ; Sensation

This study examined the effect of saponins from Tupistra chinensis Bak (STCB) on the growth of sarcoma S-180 cells in vitro and in mouse xenografts as well as the underlying mechanisms.Cell proliferation was assessed by MTT assay.Cell cycle distribution was determined by flow cytometry.Sarcoma S-180 tumor-bearing mice were treated with different doses of STCB with 10 μg/mL 5-fluorouracil (5-Fu) as a positive control.The activity of nuclear factor (NF)-κB was detected by gel mobility shift assay.The mRNA level of NF-κB was determined by real-time quantitative RT-PCR.The results showed that in vitro STCB inhibited the growth of S-18 0 cells in a concentration-dependent manner,which was accompanied by cell cycle arrest at S-phase.In vivo STCB significantly inhibited the growth of S-180 tumor mouse xenografts in a dose-dependent manner with apparent induction of cell apoptosis.Moreover,STCB inhibited the activity of NF-κB p65 and reduced the expression of NF-κB p65 mRNA in mouse xenografts.It was concluded that STCB inhibits the proliferation and cell cycle progression of S-180 cells by suppressing NF-κB signaling in mouse xenografts.Our findings suggest STCB is a promising agent for the treatment of sarcoma.

OBJECTIVETo study the plasma protein binding rate of methyl protodioscin.

METHODThe ultrafiltration was employed to determine the plasma protein binding rate of methyl protodioscin. The plasma concentrations of methyl protodioscin were measured by HPLC-MS-MS.

RESULTThe plasma protein binding rate of methyl protodioscin with rat plasma at the concentration of 20.0, 100 and 200 microg x mL(-1) were (94.6 +/- 0.16)%, (91.6 +/- 0.35)% and (86.10 +/- 0.60)%, respectively, while the plasma protein binding rate of methyl protodioscin with normal human plasma at the above concentrations were (82.11 +/- 5.12)%, (84.54 +/- 0.32)% and (88.52 +/- 1.02)%, respectively.

CONCLUSIONThe binding rate of methyl protodioscin with plasma protein is high.

Animals ; Antineoplastic Agents ; metabolism ; Blood Proteins ; metabolism ; Calibration ; Chromatography, High Pressure Liquid ; Diosgenin ; analogs & derivatives ; metabolism ; Female ; Humans ; Male ; Protein Binding ; Rats ; Saponins ; metabolism ; Sensitivity and Specificity ; Tandem Mass Spectrometry ; Ultrafiltration

BACKGROUNDDocetaxel (DOC) therapy is well tolerated and shows high response rates in patients with hormone refractory prostate cancer (HRPC). There are many reports on the effect of rapamycin (RPM) on the treatment of carcinogenesis. The goal of this study was to test whether RPM could enhance the susceptibility of both androgen-dependent and -independent prostate carcinoma cells to DOC.

METHODSProstate cancer (PC) cell lines (LNCap, PC3 and AILNCap) were cultured and treated with RPM and DOC alone or in combination. The effects of therapeutic agents on cells were determined by the WST-1 assay. Apoptosis induction was confirmed by flow cytometric analysis. The apopcyto caspase colorimetric assay kit was applied to measure the activities of caspases 3 and 9. The antitumor effects of RPM and DOC against PC cells were also assessed in nude mice using four randomized groups: control, RPM, DOC and combination drug therapy by measuring tumor size. All the animals tolerated both RPM and DOC without significant weight loss.

RESULTSRPM and DOC caused dosage-dependent growth suppression of PC cells. RPM could increase the susceptibility of PC cells to DOC significantly, and combined treatment with RPM and DOC caused synergistic growth suppression in all examined PC cell lines by isobolographic analysis. Both RPM and DOC significantly induced apoptosis in a dosage-dependent manner. RPM (10 nmol/L), DOC (1 nmol/L), and combined treatment induced apoptosis rate were 8%, 17% and 38%, respectively (the control was 2%). RPM could promote the apoptosis induced by DOC in PC cell lines. Both RPM and DOC significantly increased the caspase activity in a dosage-dependent manner. The relative activities of caspase 9 in control, RPM, DOC and RPM + DOC groups were 0.22 +/- 0.02, 0.36 +/- 0.06, 0.47 +/- 0.05 and 0.84 +/- 0.08, respectively. The relative activities of caspase 3 were 0.21 +/- 0.02, 0.24 +/- 0.05, 0.42 +/- 0.06 and 0.81 +/- 0.09, respectively. Either RPM or DOC alone significantly inhibited the growth of PC cells in nude mice compared to the control. The combination of RPM and DOC produced a significant reduction in tumor volume when compared to RPM or DOC alone. After 5-week treatment, the tumor sizes of LNCap in control, RPM, DOC and RPM + DOC groups were (570 +/- 56) mm(3), (412 +/- 41) mm(3), (425 +/- 46) mm(3) and (221 +/- 26) mm(3), respectively.

CONCLUSIONSRPM could significantly increase the susceptibility of both androgen-dependent and -independent PC cells to DOC; the synergy of RPM and DOC was demonstrated. RPM enhanced the DOC-induced upregulation of caspase activity, resulting in an increasing number of cells in sub-G1 phases. The synergy of the combined treatment might be observed in both androgen-dependent and -independent PC cell lines.

Animals ; Antineoplastic Agents ; therapeutic use ; Cell Line, Tumor ; Drug Synergism ; Flow Cytometry ; Humans ; Male ; Mice ; Mice, Nude ; Prostatic Neoplasms ; drug therapy ; Random Allocation ; Sirolimus ; therapeutic use ; Taxoids ; therapeutic use ; Xenograft Model Antitumor Assays

OBJECTIVETo identify the mutation in transforming growth factor-beta1 gene (TGF beta1) in a Chinese patient with Camurati-Engelmann disease(CED).

METHODSDenaturing high-performance liquid chromatography (DHPLC) analysis was performed on the whole seven coding exons and exon-intron boundaries, then the mutation was identified by direct sequencing.

RESULTSMutation screening of TGF beta1 in this patient revealed a heterozygous missense mutation R218H in exon 4.

CONCLUSIONThe identification of the mutation could provide essential data for subsequent therapy and genetic counseling.

Base Sequence ; Camurati-Engelmann Syndrome ; genetics ; China ; Chromatography, High Pressure Liquid ; DNA Mutational Analysis ; Humans ; Male ; Mutation ; Polymerase Chain Reaction ; Transforming Growth Factor beta1 ; genetics ; Young Adult

Using the qualified rates of particles as the evaluation indexes, the impact tactors of one-step pelletization technology of Jiuwei Xifeng granules were selected from six factors by the Plackett-Burman experimental design and the levels of non-significant factors were identified. According to the Plackett-Burman experimental design, choosing the qualified rates of particles and angle of repose as the evaluation indexes, three levels of the three factors were selected by Box-Behnken of central composite design to optimize the experimental. The best conditions were as follows: the fluid extract was sprayed with frequency of 29 r . min-1, inlet air temperature was 90 °C, the frequency of fan was 34 Hz. Under the response surface methodology optimized scheme, the average experimental results are similar to the predicted values, and surface methodology could be used in the optimization of one-step pelletization for Chinese materia medica.
Air Movements ; Analysis of Variance ; Drug Compounding ; methods ; Drugs, Chinese Herbal ; chemistry ; Hot Temperature ; Models, Theoretical ; Research Design ; Tablets

OBJECTIVEGas-containing encephalo-meningitis is very rare. There have only been a few cases reported in the literature. The majority of neonatal cases reported in literature died. We report a case of a 5-day-old neonate who developed diffuse pneumocephalus from Enterobacter cloacae septicemia and intracranial infection.

METHODThis neonate was initially treated with penicillin and mezlocillin. He also received phototherapy, intravenous infusion, correction of acidosis and other supportive therapy. Complete blood count, C-Reactive protein, cranial CT scan, blood culture, cerebrospinal fluid culture and biochemistry were tested repeatedly.

RESULTSThis neonate's condition deteriorated after admission. He developed respiratory distress, increased muscle tone and decreased level of consciousness. His WBC and C-reactive protein were elevated, while blood gas, electrolytes, liver enzymes and renal function were within normal range initially. Cranial CT scan was done which demonstrated diffuse pneumocephalus. He was transferred to a higher level hospital for further management at the request of the family. Blood culture done in our hospital subsequently showed growth of Enterobacter cloacae. The infant developed seizures and further deterioration in level of consciousness after transfer. Antibiotics were switched to penicillin and ceftizoxime. Cranial CT scan repeated 2 days after transfer showed hydrocephalus and some resolution of pneumocephalus. Cerebrospinal fluid (CSF) was aspirated from the lateral ventricles two weeks after admission. CSF culture also showed growth of Enterobacter cloacae. Antibiotic was switched to imipenem according to antibiotic sensitivity. His general condition was improved. Blood and CSF cultures were negative 1 month after admission. His head circumference at discharge was 34.6 cm. Repeat cranial CT scan at 4 month of age demonstrated severe hydrocephalus, diffuse leukomalacia and calcification. This infant suffered significant neurodevelopmental deficit. Muscle tone was diffusely increased. Head circumference at 9 month of age was 48.4 cm.

CONCLUSIONThis case suggests the importance of Enterobacter cloacae infection in the newborns. Our analysis of 34 cases of Enterobacter cloacae infection showed that 93.75% - 100% were sensitive to quinolones, 94.12% were sensitive to imipenem, 73.33% were sensitive to gentamicin, 50% were sensitive to piperacillin-tazobactam. Enterobacter cloacae is generally not sensitive to penicillin, first and second generation cephalosporins (0 - 21.4%). Enterobacter cloacae septicemia and intracranial infection in neonates have a high mortality rate and can result in severe neurodevelopmental deficit in survivors.

Enterobacter cloacae ; Enterobacteriaceae Infections ; pathology ; Humans ; Infant, Newborn ; Male ; Meningitis ; microbiology ; Pneumocephalus ; microbiology

Objective: To assess the relationship between the characteristic of drug resistance in Pseudomonas aeruginosa and the syndrome of traditional Chinese medicine(TCM)in ICU.Methods: The 73 strains of Pseudomonas aeruginosa were isolated from sputum specimenpatients of in-patients in our ICU from March 2005 to February 2006.The data of the drug sensitivity test in vitro was analysised.The relation between the syndrome of TCM and drug resistance in Pseudomonas aeruginosa was probed.Results: The 73 strains of Pseudomonas aeruginosa were drug resistant to majority kinds of anti-infective except Piperacillin-Tazobactam,Piperacillin,Cefoperazone-Sulbactam,and Amikacin.The mains syndromes of TCM of all patients infected Pseudomonas aeruginosa were deficiency-excess complex(虚实夹杂证) and excess pattern(实证)(97.26%).The mains of deficiency-excess complex(虚实夹杂证) were Qi vacuity and phlegm obstruction(气虚痰阻证)and Yin vacuity internal heat(阴虚热郁证).The mains of excess pattern(实证) were phlegm-heat(痰热郁阻证)and phlegm-stasis(痰瘀互阻证).Conclusions: Combined ?-lactam antibiotics and aminoglycoside antibiotics is the first selection to treat the multidrugresistant Pseudomonas aeruginosa.Indentifing patterns and determining treatment in TCM could be tried in the treatment of patients infected Pseudomonas aeruginosa.