The microbial transformation of buflomedil by Cunninghamella blakesleana AS 3.153 was studied, as well as a microbial model which can be used to mimic metabolism of buflomedil in mammal was established. Experiments were conducted to screen the capabilities of four strains of Cunninghamella species to transform buflomedil, in which C. blakesleana AS 3.153 was selected for a preparative biotransformation. Furthermore, the microbial model was established based on the transformation condition optimization. The parent drug and its metabolites produced by C. blakesleana AS 3.153 were detected by liquid chromatography-mass spectrometry method and three metabolites were identified while two of them were new found metabolites. Two major metabolites, para-O-desmethyl buflomedil and 12-C-oxidated buflomedil, were isolated by semi-preparative HPLC. Based on the comparison between different species, the microbial transformation of buflomedil by C. blakesleana AS 3.153 is more similar to the metabolism of buflomedil in human and Beagle dog than that in rat.
Adult ; Animals ; Biotransformation ; Chromatography, High Pressure Liquid ; Cunninghamella ; metabolism ; Dogs ; Female ; Humans ; Male ; Molecular Structure ; Pyrrolidines ; chemistry ; pharmacokinetics ; Rats ; Rats, Wistar ; Spectrometry, Mass, Electrospray Ionization ; Young Adult

Multi-central randomized controlled method was used to scientifically verify indications of 33 acupoints and provide definite clinical basis for the indications of single acupoint. Of the 52 studies, 40 studies showed that the therapeutic effect in acupuncture observation groups were better than the control group; 11 studies showed similar therapeutic effect of the two groups, and 1 study showed the acupuncture observation group was worse than the control group. Therefore, results indicate that in a certain observation cycle, acupuncture at single acupoint have different effects on diseases.
Acupuncture Points ; Humans ; Randomized Controlled Trials as Topic

OBJECTIVETo explore the therapeutic effects of posterior osteotomy and long-segment internal fixation in the treatment of senile thoracolumbar kyphotic deformity and provide the reference for operative treatment.

METHODSFrom April 2007 to April 2010, 19 older patients with thoracolumbar kyphotic deformity were respectively analyzed. There were 12 males and 7 females with an average age of 62 years (ranged, 58 to 74 years). Among patients, 11 cases were old fracture, 3 cases were ankylosing spondylitis, and 5 cases were old spinal tuberculosis. According to preoperative Frankel classification, 12 cases were grade E, 4 cases were grade D, 2 cases were C and 1 case was grade B. All patients were treated by posterior osteotomy and long-segment internal fixation and followed up above 1 year. VAS score preoperative, 2 weeks and 1 year after operation, Cobb's angle,n erve function and complication were observed.

RESULTSVAS score preoperative, 2 weeks and 1 year after operation separately was (7.0 +/- 1.2),(1.1 +/= .7) and (1.3 +/- .8); while Cobb's angle separately was (44.1 +/- .9), (10.9 +/- .1) and (11.5 +/- .8); there was significant difference in VAS score and Cobb's angle between preoperative and 2 weeks after operation (P < 0.05) w hile no significant difference between 2 weeks and 1 year after operation (P > 0.05). Eighteen cases met the standard of osseous fusion, 1 case occurred nonunion, but not looseness 1 year after operation. Nerve function: 3 cases changed grade E from 4 cases with grade D, 2 cases with grade C changed to grade D, 1 case with grade B changed to grade

CONCLUSIONPosterior osteotomy and long-segment internal fixation for the treatment of senile thoracolumbar kyphotic deformity can receive a good short-time effects.

Aged ; Female ; Fracture Fixation, Internal ; adverse effects ; methods ; Humans ; Kyphosis ; surgery ; Lumbar Vertebrae ; surgery ; Male ; Middle Aged ; Osteotomy ; adverse effects ; methods ; Retrospective Studies ; Thoracic Vertebrae ; surgery

OBJECTIVETo evaluate the clinical value of different regional lymph node staging system and to establish a predictive prognostic model for stage III( colon cancer.

METHODSA total of 256 Patients with stage III( colon cancer from January 1999 to December 2008 were identified from the China Medical University Cancer and underwent radical surgery. Based on information on regional lymph nodes, lymph nodes were staged LNR staging using pN stage in the 7th edition of the AJCC, the jN stage of the JGR, and LNR-stage on the basis of Log-rank statistics, respectively. Using the linear trend chi-square test, likelihood ratio Chi-square test, concordant index(c-index) to evaluate the homogeneity, monotonicity, and discrimination power of the staging system. Univariate and multivariate analyses were used to determine the clinical and pathological prognostic impact factors. After relevant diagnostic models were established, the Akaike Information Criterion (AIC) value was calculated to compare and identify the best diagnostic model.

RESULTSLog-rank statistics found that 0.11 and 0.39 were the optimal cut-off point. LNR staging system included LNR1 (LNR<0.11), LNR2 (0.11,0.39), and LNR3(0.39,1). The concordance indices were 0.624 for pN, 0.611 for jN, and 0.700 for LNR. The heterogeneity was the lowest for LNR. Cox regression model was used to establish prognostic models for pN, jN, and LNR, and the AIC was 99.937, 71.631, and 65.548, respectively. The prognostic value was the highest for LNR.

CONCLUSIONLNR staging is the ideal staging system for stage III( colon cancer patients, which is better than the latest version of the current AJCC pN stage and JGR jN staging.

China ; Colonic Neoplasms ; pathology ; Humans ; Lymph Nodes ; Lymphatic Metastasis ; Multivariate Analysis ; Neoplasm Staging ; Prognosis

The paper is aimed to establish a methods for identication of pearl powder and conch powder from different origins. Hermetic aluminum pan was used to encapsulate samples. The optimal testing conditions were: heating rate 10 degrees C x min(-1), sample weight 3 mg and nitrogen gas flow rate 40 mL x min(-1). The enthalpy values of pearl powder and conch powder was obvious different. Identication of pearl powder and conch powder by DSC is a practical method for its accuracy, convenience and practificality.
Animal Shells ; chemistry ; Animals ; Calorimetry, Differential Scanning ; methods ; China ; Discriminant Analysis ; Pinctada ; chemistry ; classification ; Powders ; chemistry

OBJECTIVETo investigate the effect of Qingpeng paste (QP) on collagen-induced arthritis (CIA) in rats.

METHODCIA was established in female Wistar rats with injection of type II bovine collagen at the base of the tail of animals. CIA rats were treated daily with external administration of different doses of QP or voltaren beginning on the day after the onset of arthritis (day 1) until day 20. Paw swelling rate and the serum levels of IL-1 beta were determined. Moreover, the expression of TNF-alpha and IL-alpha and histopathological changes in the arthritic joints were also observed.

RESULTQP markedly suppressed the paw swelling rate of arthritic rat, reduced the expression of TNF-alpha and IL-alpha in synovial membrane. Histopathological changes in the arthritic joints were also significantly ameliorated in the QP-treated versus vehicle-treated rats. However, the elevated serum levels of IL-1 beta in arthritic rats were not influenced by QP.

CONCLUSIONThe present findings demonstrate the protective property of QP on collagen-induced arthritis, mechanisms underlying it may be related to reduce the expression of IL-1alpha and TNF-alpha in synovial membrane.

Animals ; Arthritis, Rheumatoid ; chemically induced ; drug therapy ; metabolism ; pathology ; Collagen Type II ; adverse effects ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Female ; Gene Expression Regulation ; drug effects ; Interleukin-1alpha ; metabolism ; Interleukin-1beta ; metabolism ; Rats ; Rats, Wistar ; Synovial Membrane ; drug effects ; metabolism ; Tumor Necrosis Factor-alpha ; metabolism

OBJECTIVETo improve the water solubility and biological activity of neoligans (magnolol and honokiol) and test the antitumor activity of the modified compounds.

METHODSThe glycosylated products of magnolol and honokiol were obtained by enzymatic synthesis using a UDP-glycosyltransferase (YjiC) from Bacillus. The products were characterized by high-performance liquid chromatography (HPLC), liquid chromatography-mass spectrometry (LC-MS), and nuclear magnetic resonance (NMR) analysis. MTT assay was used to detect the growth inhibition of 4 human cancer cell lines induced by the compounds.

RESULTSWe obtained two glucosides of neolignans (magnolol and honokiol) for the first time by enzymatic synthesis using a UDP-glycosyltransferase. Based on the spectroscopic data, the glucosides were identified as magnolol-2- O-β-D-glucopyranoside (1) and honokiol-4'-O-β-D-glucopyranoside (2). Compounds 1-4 exhibited moderate anti-proliferative activities against the 4 human cancer cell lines, with IC50 values ranging from 9.41 to 111.21 µmol/L.

CONCLUSIONThe glycoslated products show enhanced water solubility and drug sensitivity against SMMC7721 cells, suggesting their value as potential therapeutic drugs.

Antineoplastic Agents, Phytogenic ; chemistry ; Biphenyl Compounds ; chemistry ; Cell Line, Tumor ; Chromatography, High Pressure Liquid ; Glucosides ; chemistry ; Glycosylation ; Humans ; Lignans ; chemistry ; Magnetic Resonance Spectroscopy ; Mass Spectrometry

OBJECTIVETo explore the molecular mechanism of exocrine immune inflammatory injury of Sjögren's Syndrome and the intervention of Banxia Qinlian Decoction (BQD).

METHODSTotally 18 female NOD mice were randomly divided into the model group, the positive drug group, and the BQD group, 6 in each group. Six female BALB/c mice were recruited as a blank control group. Mice in the blank control group and the model group were gavaged with deionized water at the daily dose of 0.1 mL/10 g body weight. Tripterygium Tablet was administered by gastrogavage to mice in the positive group at the daily dose of 10 mg/kg. BQD was administered by gastrogavage to mice in the BQD group at the daily dose of 60 g crude drugs/kg. After 12 weeks of medication, mice were sacrificed. Their eyeballs were excised and blood collected. Tissues of bilateral parotids and submandibular glands were kept. mRNA transcriptional levels of IL-17, IL-6, type 3 muscarinic acetylcholine receptors (M3R), aquaporin protein-5 (AQP5) were detected by RT-PCR. Expression levels of M3R and AQP5 protein were detected by Western blot. Protein expression levels of IL-17 and IL-6 were detected by ELISA.

RESULTSCompared with the normal group, mRNA transcriptional levels and protein expression levels of IL-17, IL-6, M3R, and AQP5 were significantly up-regulated in the model group (P < 0.01). Compared with the model group, mRNA transcriptional levels and protein expression levels of IL-17, IL-6, M3R, and AQP5 were significantly down-regulated in the positive drug group and the BQD group with statistical difference (P < 0.01, P < 0.05). Compared with the BQD group, mRNA-transcriptional levels of IL-17, IL-6, and M3R, as well as M3R and AQP5 protein expression levels were significantly down-regulated in the positive drug group (all P < 0.01).

CONCLUSIONThe molecular mechanism of BQD in inhibiting SS exocrine neurotoxic injury might be possibly related to regulating Th17/IL-17 immune inflammatory way.

Animals ; Aquaporin 5 ; metabolism ; Disease Models, Animal ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Female ; Interleukin-17 ; metabolism ; Interleukin-6 ; metabolism ; Mice ; Mice, Inbred BALB C ; Mice, Inbred NOD ; Sjogren's Syndrome ; drug therapy ; immunology ; Submandibular Gland ; Th17 Cells ; Up-Regulation

OBJECTIVETo investigate the effect of Compound Qingqin Liquid (CQL) on the expression level of angiotensin II (Ang II) and COX-2 mRNA transcription and protein expression in the renal tissue of rats with uric acid nephropathy.

METHODSSD rats were randomly divided into the blank control group, the model group, the positive drug group, the high, moderate, and low dose CQL group according to number randomization principle. The model was established by gastrogavage of adenine, accompanied with yeast feeding. Distilled water was given by gastrogavage to rats in the blank control group and the model group. Allopurinol at the daily dose of 9.33 mg/kg was given by gastrogavage to rats of the positive control group. CQL at the daily dose of 3.77 g/kg, 1.89 g/kg, and 0.09 g/kg was respectively given by gastrogavage to rats in the high, moderate, and low dose CQL groups. All treatment lasted for 6 weeks. Rats were randomly divided at week 4 (3 in the blank control group, and 6 in the rest groups), and the rest rats were killed at week 6. The renal tissue was extracted. The expression level of Ang II and COX-2 mRNA transcription were detected by RT-PCR. The expression level of Ang II was detected by ELISA. The expression level of COX-2 protein was detected by Western blot and immunohistochemical assay.

RESULTSCompared with the blank control group, except the mRNA expression of Ang II at week 4, the mRNA and protein expression of Ang II and COX-2 obviously increased at week 4 and 6 in the model group (P < 0.01, P < 0.05). The COX-2 protein expression at week 4 was obviously lower in the high and moderate dose CQL groups than in the model group and the low dose CQL group (P < 0.05); the average integral of optical density value was obviously lower in the positive control group than in the model group. Except the mRNA expression of Ang II in the high dose CQL group at week 6, the mRNA and protein expression of Ang II obviously decreased in the positive control group and each dose CQL group (P < 0.01, P < 0.05). Of them, the effects were better in the high and moderate dose CQL groups than in the positive control group and the low dose CQL group (P < 0.05, P < 0.01). Besides, the mRNA expression of COX-2, the average integral of optical density value were obviously lower in the positive control group and each dose CQL group than in the model group (P < 0.05). The protein expression of COX-2 was obviously lower in the high and moderate dose CQL groups than in the model group (P < 0.05). Of them, the mRNA expression of COX-2 was better in the moderate dose CQL group than in the positive control group (P < 0.05); the protein expression of COX-2 was better in the high dose CQL group than in the low dose CQL group (P < 0.05).

CONCLUSIONCQL was capable of lowering the expression level of Ang II, COX-2 mRNA transcription and protein expression, thus suppressing the inflammatory pathological injury of the renal tissue.

Angiotensin II ; metabolism ; Animals ; Cyclooxygenase 2 ; genetics ; metabolism ; Disease Models, Animal ; Drugs, Chinese Herbal ; pharmacology ; Kidney ; metabolism ; Kidney Diseases ; drug therapy ; metabolism ; Male ; RNA, Messenger ; genetics ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Uric Acid

OBJECTIVETo investigate the effect of compound qingqin liquid (CQL) on Toll-like receptor 2 (TLR2) and toll-like receptor 4 (TLR4) in rats with urate nephropathy, and to explore its renal protection mechanism.

METHODSTotally 55 SD rats were randomly divided into 5 groups, i.e., the normal control group (n =5), the model group (n =10), the positive drug group (n=10), and the high-, medium-, low-dose CQL groups (n=10) respectively. The urate nephropathy model was induced by intragastrically administering adenine and feeding yeast. Distilled water was intragastrically administered at the daily dose of 10 mL/kg to rats in the normal control group and the model group. Allopurinol was intragastrically administered at the daily dose of 9.33 mg/kg to rats in the positive control group. CQL was intragastrically administered at the daily dose of 3.77, 1.89, 0.94 g/kg to rats in the high-, medium-, and low-dose CQL groups. Rats of each group were executed in batches at the 4th and 6th week respectively. Their kidney tissues were taken out to determine the mRNA transcription level of TLR2 and TLR4 by reverse transcription-polymerase chain reaction (RT-PCR). The protein expression level of TLR2 and TLR4 were determined by Western blot. The protein expression level of TLR4 was also detected by immunohistochemical assay.

RESULTSAt week 4 and 6, the protein expression of TLR2 and TLR4 as well as the mRNA transcription of TLR4 increased in the model group, when compared with the control group (P < 0.05, P < 0.01). Compared with the model group, there was no statistical difference in the transcription level of TLR2 mRNA or TLR4 mRNA among the 3 CQL groups (P > 0.05) at week 4 and 6. Additionally, at week 6, the protein expression of TLR4 and TLR2 could be reduced by CQL (P < 0.05, P < 0.01).

CONCLUSIONCQL might protect kidney tissue against inflammatory injury by inhibiting the protein expression levels of TLR2 and TLR4.

Animals ; Disease Models, Animal ; Drugs, Chinese Herbal ; pharmacology ; Kidney ; drug effects ; metabolism ; Kidney Diseases ; drug therapy ; metabolism ; Male ; RNA, Messenger ; genetics ; Rats ; Rats, Sprague-Dawley ; Toll-Like Receptor 2 ; genetics ; metabolism ; Toll-Like Receptor 4 ; genetics ; metabolism ; Uric Acid