Five compounds (tenuifoliside C, tenuifoliside D, telephiose A, telephiose C and polygalaxanthone III) from polygala tenuifolia wild were incubated together with CYP probe substrate in human liver microsomes to investigate the inhibitory effect towards CYP450 enzyme. Phenacetin (CYP1A2), coumarin (CYP2A6), paclitaxel (CYP2C8), diclofenac (CYP2C9), S-mepheriytoin (CYP2C19), dextromethorphan (CYP2D6), chlorzoxazone (CYP2E1), midazolam (CYP3A) were selected as the isoforfn specific substrate. And the formation of paracetamol, 7-hydroxycoumarin, 6alpha-hydroxy paclitaxel, 4'-hydroxydiclofenac, dextrorphan, 6-hydroxychlorzoxazone, 1'-hydroxymidazolam, 4'-hydroxymephenytoin were detected respectively to measure the effect towards CYP450 by high-pressure liquid chromatography (HPLC). The result shows that five compounds from polygala tenuifolia willd significantly inhibit chlorzoxazone 6-hydroxylation catalyzed by CYP2E1, while showed no effect towards CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A. And IC50 value was 38.73, 54.14, 61.77, 62.22, 50.56 micromol x L(-1), respectively.
Cytochrome P-450 Enzyme System ; metabolism ; Esters ; pharmacology ; Glycosides ; pharmacology ; Humans ; Microsomes, Liver ; drug effects ; enzymology ; Oligosaccharides ; pharmacology ; Polygala ; chemistry ; Xanthones ; pharmacology

Objective To develop a clinically applicable approach to enhance repair of cartilage defects by constructing an in vivo non-viral gene transfer system targeting chondrocytes. Methods High molecular weight chitosan (HMWC) was degraded to produce low molecular weight chitosan (LM-WC) that was combined with transforming growth factor-β1 (TGF-β1) plasmid to form stable nano-sizc complexes. After being tested in vitro firstly, these nano-size complexes were injected into the knee joint of New Zealand white rabbit models with full-thickness cartilage defects to detect their feasibility of delive-ring the growth factor gent in vivo. Results The results showed that LMWC/DNA nano-sizc comple-xes could deliver the gone into the cultured chondroeytes and cartilage tissue efficiently in vitro. When used in vivo, LMWC/TGF-β1 gene nano-size complexes could enhance the transfection efficiency and prolong the expression of TGF-β1 gone. In the animal models of articular osteechondral defect of rabbits, better healing and gentler degeneration could be observed in comparison with the control. Conclusion In vivo transfection of LMWC/TGF-β1 nano-size complexe is a safe and effective method to early promote the repair of osteochondral defects.

Objective To investigate the differential diagnostic value of computed tomography (CT) combined with serum tumor markers in borderline ovarian tumors (BOT) and benign epithelial ovarian tumors (BET).Methods The CT data in 28 patients with BOT and 41 patients with BET,both confirmed by surgery and pathological,were analyzed retrospectively.Their preoperative serum carbohydrate antigen 125 (CA125),human epididymis secretory protein 4 (HE4) and carcinoembryonic antigen (CEA) detection results were collected.The CT images features and serum tumor markers levels were compared between the two groups.Results The difference in the appearance rate of tumor solid composition,thick septum and wall nodule between the two groups had statistical significance (x2 =25.135,5.240,5.066,P＜0.05).The serum CA125 level had statistical difference between the two groups (Z=3.202,P＜0.05),while serum HE4 and CEA levels had no statistically significant difference between the two groups(Z=0.330,1.122,P＞0.05).The optimal critical value,sensitivity and specificity of serum CA125 level in differential diagnosis of two kinds of tumor was 42.45 U/mL,53.6％ and 85.4％.The overall diagnostic rate of solid composition and thick septum for diagnosing the two kinds of tumor was 78.5 ％.The overall diagnostic rate of solid composition,thick septum and CA125 level for diagnosing the two kinds of tumor was 81.2％.Conclusion The appearance of solid composition,thick septum and serum CA125 level increase in epithelial ovarian tumor may help to identify BOT and BET.

Most drugs need to interact with cell membrane to reach the biological target, so that membrane affinity assay is an important early screening step in drug discovery. However, at present, the traditional oil-water distribution method is still used, a new, simple and accurate method for membrane affinity assay is urgently needed. In this study, according to the colorimetric principle, a new assay model based on polydiacetylene vesicles was optimized through a series of experiments including different concentrations of vesicle solution, temperature, or pH reaction environment. On this basis, tetracaine hydrochloride, 2-methylimidazole and histamine were used as model drugs to measure the membrane affinity constants and verify the between-batch precision of the optimized assay model (relative standard deviation less than 5%). In addition, polydiacetylene vesicles were stable for up to 180 days, demonstrating the potential application of the assay model. This strategy is simple, stable, reliable, with high reproducibility, low cost and easy to promote, which provided a new tool and a new direction for the high-throughput assay of membrane affinity.

OBJECTIVETo explore the effect of Rhodiola on the expression of iNOS mRNA in severe acute pancreatitis (SAP) associated renal injury rats.

METHODSA total of 72 healthy rats were randomly divided into the sham-operated group (S), the SAP associated renal injury group (M), and the Rhodiola-treated group (RHO), 24 in each group. Rats in S and M groups were peritoneally injected with 10 mL/kg saline 3h before modeling, while rats in the RHO group were peritoneally injected with 10 mL/kg Rhodiola Injection 3 h before modeling. The peripheral ligament of pancreas was bluntly dissociated in rats of M and RHO groups. The head of pancreas was occlused by nontraumatic blood vessel forceps 3 h later to establish the model. Eight rats were randomly selected from each group at 12, 24, and 36 h after modeling to detect levels of serum amylase, creatinine, and blood urea nitrogen. Serum levels of interleukin 1β (IL-1β) and interleukin 10 (IL-10) were detected by enzyme-linked immunosorbent assay (ELISA). Pathological changes of the left kidney were observed under light microscope. The expression of inducible nitric oxide synthase (iNOS) mRNA in the right kidney was detected with real time polymerase chain reaction (RT-PCR).

RESULTSCompared with the S group, serum levels of amylase, creatinine (Cr), blood urea nitrogen (BUN), IL-1β, IL-10, and iNOS mRNA expression significantly increased in the M group (P < 0.01). The function of kidney and pancreas were obviously improved in the RHO group than in the M group. Levels of IL-1β and iNOS significantly decreased, but IL-10 levels significantly increased in the RHO group with statistical difference (P < 0.05).

CONCLUSIONRhodiola had better protective effect on SAP associated renal injury, which might be achieved through inhibiting the expression of IL-1β, stimulating the expression of IL-10, down-regulating iNOS mRNA expression, reducing the generation of oxygen free radicals and NO damage to cells, and improving hypoxia tolerance capabilities of the kidney.

Amylases ; Animals ; Blood Urea Nitrogen ; Creatinine ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Interleukin-1beta ; Kidney ; Nitric Oxide Synthase Type II ; genetics ; metabolism ; Pancreas ; Pancreatitis ; drug therapy ; RNA, Messenger ; Rats ; Rats, Sprague-Dawley ; Rhodiola

OBJECTIVETo analyse the effects of buyang huanwu decoction (BYHWT) on differentially expressed genes during cerebral ischemia/reperfusion in rats with DNA microarray.

METHODcDNA microarray chips containing 512 cDNAs were made by Biostar Genechip Inc. Sprague-Dawley rats were subjected to 2 h of middle cerebral artery occlusion (MCAO) with an filament. Saline or BYHWT was given p.o. after onset of cerebral ischemia and brains were removed after 24 h of recirculation for mRNAs isolation. A differential measurment of mRNAs from post-ischemic and BYHWT treated animals was performed with microarray.

RESULTUp-and down-regulated genes were 69 and 80 in ischemic group. Up-and down-regulated genes were 25 and 6 in BYHWT treated group.

CONCLUSIONBYHWT regulates the differential expression genes after focal brain ischemia/reperfusion in rats, due to its mechanism of protecting cerebral ischemia/reperfusion injury.

Animals ; Brain Ischemia ; complications ; genetics ; Drugs, Chinese Herbal ; pharmacology ; Gene Expression Profiling ; Male ; Neuroprotective Agents ; pharmacology ; Oligonucleotide Array Sequence Analysis ; Rats ; Rats, Sprague-Dawley ; Reperfusion Injury ; etiology ; genetics

Objective Apoptosis was induced by oxidative stress in nerve cells after cerebral ischemia. It further breaks the dy-namic balance of mitochondrial division of fusion. This study aimed to investigate the effect of butylphthalide combined with edaravone treat-ment on the dynamic change of Drp1 and Mfn2 in rats with focal cere-bral ischemia cells and its protection mechanism. Methods 96 rats were divided into 4 groups according to random number table. The 4 groups were ischemia group,butylphthalide group,edaravone group and butylphthalide combined with edaravone groups(combine group),each group divided into three subgroups(3 d,7 d,14 d). Longa-Zea suppository method is adopted to establish the middle cerebral artery occlusion(MCAO)model.Butylphthalide group,edar-avone group and combine group were injected butylphthalide(0.4 g/kg)and/or edaravone(10 mL/kg)peritoneally 2 hours before surgery and 1 day after surgery. The same volume of isotonic saline was given at the same time of the other 3 groups in ischemia group. The cerebral cortex of the left ischemic region was obtained at the day 3,7,14. The evaluation of the curative effect was evaluated with neurological function score.HE staining was used to observe the cerebral cortex neuron morphological structure,protein and mRNA lev-el of Drp1 and Mfn2 was measured by western blot and RT-PCR. Results At the day 3,7,and 14,the neurological function score was higher in ischemia group than the other 3 groups(P<0.05). Compared with the combine group at day 3,7,and 14[(1.06± 0.18),(0.82±0.13),(0.57±0.10)],the neurological function score was elevated in butylphthalide group[(2.02±0.18),(1.23± 0.13),(0.86±0.10)]and edaravone group[(2.08±0.17),(1.23±0.13),(0.85±0.12)](P<0.05). At the same time point,com-pared with the ischemia group,Drp1 protein and mRNA levels were lower in the other 3 groups(P < 0.05)while Mfn2 protein and mRNA levels were elevated(P<0.05). Compared with the butylphthalide group and edaravone group,Drp1 protein and mRNA levels were lower in combine group(P<0.05)while Mfn2 protein and mRNA levels were elevated(P<0.05). Conclusion The protective effect of edaravone combined with butylphthalide is better than single use. Its mechanism may be related to the removing of oxygen free radicals and reducing oxidative stress by edaravone,and the protection of the mitochondria by butylphthalide.

Recently, the joint replacement has gradually become a common operation of orthopedics. It's also the hot spot in current investigations. The increasing number of reports about the 3D printing technology such as patient-specific instrumentation(PSI) is applied to hip and knee replacement. It plays an important role in supporting operation especially for complex cases. However, it is still at the primary stage. This article reviews the relevant literature, analyzes and collates the research status of the application of 3D printing PSI in total knee arthroplasty, and summarizes its effectiveness in the application of knee arthroplasty from the aspects of individual preoperative planning, intraoperative operation and postoperative functional recovery, especially complex knee surgery such as obesity and knee deformity. The necessity of clinical application is discussed, and the existing problems and controversies in the current clinical application are summarized in order to provide references for the future research direction and clinical application.
Arthroplasty, Replacement, Knee ; Humans ; Knee Joint ; Knee Prosthesis ; Postoperative Period ; Printing, Three-Dimensional

OBJECTIVETo investigate the relationship between the changes of amino acids contents in hippocampus of rats and electromagnetic pulse (EMP) exposure.

METHODSRats were decapitated and hippocampus were removed after EMP (6 x 10(4) V/m, rise time 20 ns, pulse width 30 micro s, 5 pulses in 2 minutes) irradiation, and contents of amino acids were detected with high performance liquid chromatograpy (HPLC).

RESULTSThe contents of aspartic acid (Asp) and glutamic acid (Glu) increased significantly 0, 3, 6 h after irradiation. The peak values of Asp [(17.25 +/- 1.63) pmol/ micro l] and Glu [(13.67 +/- 0.95) pmol/ micro l] were higher than those of control [(10.56 +/- 1.50), (6.94 +/- 1.10) pmol/ micro l respectively, P < 0.05]. Then both decreased gradually and reached the normal level 24 - 48 h after irradiation. The contents of glycine (Gly), taurine (Tau) and gamma-aminobutyric acid (GABA) also rose after exposure, the peak value of them [(4.51 +/- 0.60), (29.85 +/- 2.70), (5.14 +/- 0.73) pmol/ micro l respectively] were higher than those of control group [(2.18 +/- 0.31), (9.88 +/- 1.47), (2.84 +/- 0.67) pmol/ micro l, P < 0.05], then recovered 48 h after irradiation. The value of Glu/GABA increased immediately after exposure (3.45 +/- 0.25, P < 0.05), then decreased 24 h (1.62 +/- 0.23, P < 0.05) and recovered 48 h after exposure.

CONCLUSIONThe toxic effect of excess excitatory amino acids may be partly responsible for the early retardation (within 24 h) of learning of rats.

Amino Acids ; analysis ; Animals ; Chromatography, High Pressure Liquid ; methods ; Glutamic Acid ; analysis ; Hippocampus ; metabolism ; radiation effects ; Male ; Radiation ; Random Allocation ; Rats ; Rats, Wistar ; Time Factors

OBJECTIVETo evaluate the value of cardiac troponin I (CTnI) measurement in predicting anthracycline-induced cardiotoxicity in patients with breast cancer.

METHODSThis study was conducted among 186 breast cancer patients receiving anthracycline-based chemotherapy. Serum cTnI concentrations before and after each cycle of the chemotherapy and the left ventricular ejection fraction (LVEF) before and at the 2nd, 4th and 6th months of the treatment were recorded. According to serum cTnI concentration, the patients were divided into CTnI+ group (with serum CTnI concentration of no less than 0.1 ng/ml, n=60) and CTnI- (<0.1 ng/ml) group (n=126).

RESULTSNo patients in this series experienced cardiac heart failure (CHF). The number of patients with a LVEF reduction by over 10% from the baseline was 16 (26.7%) in CTnI+ group, as compared to 7 (5.6%) in CTnI- group, showing a significant difference between the two groups (P<0.01).

CONCLUSIONCTnI can be a useful marker for early prediction of anthracycline-induced cardiotoxicity in patients with breast cancer.

Adult ; Aged ; Anthracyclines ; adverse effects ; therapeutic use ; Antibiotics, Antineoplastic ; therapeutic use ; Biomarkers ; blood ; Breast Neoplasms ; drug therapy ; Cardiotoxins ; adverse effects ; Female ; Humans ; Middle Aged ; Myocardium ; metabolism ; Troponin I ; blood ; Young Adult