Rutaecarpine (Rut) is a type of indole quinazoline alkaloid exracted from Ruticarpum. Studies showed that Rut has a wide range of pharmacological effects, such as anti-hypertension, anticancer, anti-inflammation, anti-thrombus formation. Currently, many scholars are committed to developing it into a new antihypertensive and anti-inflammatory drug with all new mechanisms. But studies found that Rut is a highly fat-soluble drug with low water and oil solubility. Its high insolubility is the main obstacle in its oral absorption and application, which greatly reduced its bioavailability. Therefore, hydroxypropyl-beta-cyclodextrin (HP-beta-CD) was used as the inclusion material to prepare Rut-HP-beta-CD inclusion complex in this experiment, in order to increase its water solubility and bioavailability. In this experiment, the inclusion complex was prepared by the stirring-freeze-dry method. The preparation process was optimized by the orthogonal test, with the inclusion rate as the index, and molar ratio between host and guest molecules, inclusion temperature, time and stirring speed as the impacting factors. Moreover, the inclusion complex was verified by detecting the apparent solubility, thin layer chromatography, microscopic identification, melting point detection and dissolution study. The results showed that under the conditions of the molar ratio between Rut and HP-beta-CD of 1: 1, temperature at 60 degrees C, inclusion time of 4h and stirring speed at 600 r x min(-1), the inclusion rate of Rut-HP-beta-CD reached 91.04%. Therefore, the preparation process of Rut-HP-beta-CD inclusion under the optimum conditions is simple and feasible, with a highest inclusion rate and reproducibility, and could significantly improve Rut's solubility and bioavailability, and provide a reliable experimental basis for its clinical application.
2-Hydroxypropyl-beta-cyclodextrin ; Alkaloids ; chemistry ; Chemistry, Pharmaceutical ; methods ; Drug Carriers ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Rutaceae ; chemistry ; Solubility ; beta-Cyclodextrins ; chemistry

Objective To evaluate the efficacy and safety of infliximab plus methotrexate combination therpy in Chinese with rheumatoid arthritis patients.Methods This was a double-blind placebo-controlled phaseⅢclinical trial,173 patients who had active rheumatoid arthritis were randomised to placebo(n=86)or infliximab(n=87)group on a background of a stable dosage of methotrexate.Patients were assessed at weeks 0,2,6,14 and 18.Results At week 2,the American College of Rheumatology(20)response criteria,which represent a 20% improvement from baseline,the same results with swollen joint count,tender joint count,du- ration of morning stiffness,VAS score,CRP,ESR were achieved in 52.9% of patients,compared with 14.0% of patients receiving placebo plus methotrexate.A 20% improvement was achieved in 75.9% of infliximab plus methotrexate at week 18,compared with 48.8% of patients on placebo plus methotrexate(P=0.0003).A 50% improvement was achieved in 43.7% of infliximab plus methotrexate at week 18,compared with 25.6% of pa- tients on placebo plus methotrexate(P=0.011).Infliximab was well-tolerated;withdrawals for adverse events as well as the occurrence of serious adverse events or serious infections were similar to those in the placebo group.There was only one case of tuberculosis in the treatment group.Conclusion Treatment with infliximab plus methotrexate is more effective than methotrexate alone in patients with active rheumatoid arthritis.It has rapid onset of effect and the efficacy is persistent.

OBJECTIVETo explore method of recombinant gene lentivirus containing LIM mineralization protein-1 (LMP-1) in transfecting bone marrow mesenchymal stem cells (BMSC), and to observe the effect of gene LMP-1 on proliferation effect and expression of BMSC.

METHODSSix clean SD rats aged 4 weeks were selected, bone marrow mesenchymal stem cells were extracted under sterile conditions and cultured to the third generation, then divided into three groups:control group (the third generation of BMSC), lentiviral vector transfection group (PGC-FU-GFP and Polybrene were injected into the third generation of BMSC) and recombinant gene transfection group (PGC-FU-LMP-1-GFP and Polybrene transfection were injected into the third generation of BMSC). After 48 hours' transfection, fluorescent expression were detected under immuno-fluorescence microscopy; lentiviral transfection efficiency were detected by flow cytometry; effect of lentiviral transfection on BMSC were evaluated by MTT; gene expression of transfected cells were determined by Western Blot.

RESULTS1) The third generation of BMSC was cultured successfully,and transfected with MOI:100. After 48 hours, green fluorescent expression were detected and transfection efficiency was 67% under immuno-fluorescence microscopy; 2) Compared to control group, there were no statistical differences between control group and other two groups; 3) Western blot teast showed that 72KDa specific band was observed in recombinant gene transfection group and its size was similar to LMP-1 fusion protein (50 kDa+28 kDa=78 kDa).

CONCLUSIONThere is no effect of recombinant gene lentivirus containing LIM on BMSC, and can effectively influence the expression of LMP-1.

Adaptor Proteins, Signal Transducing ; genetics ; metabolism ; Animals ; Cell Proliferation ; Cells, Cultured ; Cytoskeletal Proteins ; genetics ; metabolism ; Female ; Genetic Therapy ; Genetic Vectors ; genetics ; metabolism ; Humans ; LIM Domain Proteins ; genetics ; metabolism ; Lentivirus ; genetics ; metabolism ; Male ; Mesenchymal Stromal Cells ; cytology ; metabolism ; virology ; Osteoporosis ; genetics ; physiopathology ; therapy ; Rats ; Rats, Sprague-Dawley

In the present paper, the theory and practice of acupuncture and moxibustion therapy by a clinical point of view are explored and summarized. Such concepts as the total treatment amount, the unit treatment amount, the immediate treatment amount, the overtreatment amount, the inferior treatment amount and the measurement of treatment amount are proposed and discussed. The basic constituent elements of treatment amount of acupuncture and moxibustion, i. e. acupuncture, moxibustion, cupping, acupoint injection, electroacupuncture are summarized. It is held that the treatment amount of acupuncture and moxibustion in condition of suitable controlling is the fundamental guarantee for the best clinical therapeutic effect, the key to which include correct acupuncture manipulation, rational selection acupoints for the prescriptions, suitable acupuncture therapy combination, the variety of treatment amount assignment being related with the state of disease and so on. The overtreatment amount and the inferior treatment amount must be avoided.
Acupuncture Points ; Acupuncture Therapy ; Humans ; Moxibustion

Pure culture of Phlebopus portentosus was inoculated in the roots of coffee tree. The results indi-cated that the young fruit bodies would come out around the rhizomes of host tree after inoculation in 30 to 90 days, single or cluster, 3 to 4 days for mature, weight 20.0 g to 62.0 g. Brown rhizomorph and hyphae can be seen on the seedlings`rhizome, main root and side root while nothing is on the tip of the root.It was found that rhizomorph on the surface of roots would die after inoculation in 90 days in pot.

Objective To evaluate the clinical parameters that can predict whether a patient can get significant improvement at the 10th week,or whether a patient can have an extended length of remission after discontinuing the infusion in ankylosing spondylitis(AS)patients treated with three standard infusions of in- fliximab.Methods Sixty-three AS patients were given three infusions of 5 mg/kg of infliximab at week 0,2 and 6;and were evaluated serially before each infusion and week 10.Afterwards.patients were followed by telephone interview until their disease activity was≥60% of the baseline level.At that point,disease was con- sidered to relapse.Clinical parameters at baseline as well as at week 2 were used to identify factors which might predict an improvement at week 10,or predict a delayed relapse.A predictor was regarded as being use- ful if the area under the curve(AUC)more than 0.75 when analyzed by receiver operator calculations(ROC). Results No parameters at baseline have sufficient predictive value.However,ASAS20(Assessment in Anky- losing Spondylitis International working Group criteria)at week 2 predicts improvement at week 10.and also duration of remission after discontinuing the infliximab at week 6.Conclusion The response to one pulse of infliximab is the best predictor of subsequent response as well as rate of relapse after discontinuing the inflix- imab.

OBJECTIVETo investigate the expression of cyclooxygenase-2 (COX-2) in different prostate cancer (PCa) cell lines and its role in the acquisition of invasive and metastatic potentials of PCa.

METHODSWe detected the expressions of COX-2 in prostate cancer cell lines LNCaP, C4-2, IF11, IA8 and PC-3 with different metastatic potentials by Western blotting and RT-PCR, and analyzed their roles in the invasion and metastasis of different PCa cell lines.

RESULTSWestern blotting and RT-PCR showed that the expression of the COX-2 protein was high in PC-3, but absent in IF11, IA8, LNCaP and C4-2 (P < 0.05), and it was consistent with the expression of COX-2 mRNA.

CONCLUSIONCOX-2 expresses differently in PCa cell lines with different metastatic potentials. The overexpression of COX-2 may be associated with the high invasion and metastasis of PC-3, but not with the metastasis of other cell lines.

Cell Line, Tumor ; Cyclooxygenase 2 ; metabolism ; Humans ; Male ; Neoplasm Metastasis ; Prostatic Neoplasms ; metabolism ; pathology ; RNA, Messenger ; genetics

The purpose of this study is to summarize teaching experiences on channel and acupoints. The method of classified teaching is put forward and approached to explore the law of acupoint teaching. It is held that the method could reduce randomness and enhance appropriateness, rationality and scientific validity of the teaching. Class hours are thus optimized and the best teaching result achieved. Acupoints are classified into 4 categories of core points, focal points, regular points and ordinary points according to their use frequency and theoretical importance. Classification methods, principles and categories are then determined. And content of courses, teaching techniques and requirements are introduced as well. Suggestions are offered on enriching teaching contents, for instance, paraphrasing of the acupoint names, indications, point prescriptions and clinical experiences. Thus the conclusion is made that it is imperative to reform the conventional sort of acupoints classified by only focal points and ordinary points as well as the related teaching methods.
Acupuncture ; education ; standards ; Acupuncture Points ; Cyclobutanes ; Humans ; Teaching ; standards

Objective Type 1 diabetes mice model was established to investigate the changes of key enzymes involved in testosterone synthesis in testes of early diabetic mice.Methods Tatolly 20 male C57 mice were randomly divided into two groups:control and diabetic groups,and the diabetes mice were ip administered with a single dose of 150 mg/kg Streptozotocin.Four weeks after confirmation of diabetic model,the serum and testis were collected for further study.The qRT-PCR method was used to measure the expression of LHR and steroidogenesis synthetase StAR,P450scc,3β-HSD6,P450c17a1,and 17β-HSD3 mRNA.ELISA assay was performed to measure the levels of testosterone and luteinizing hormone (LH) in serum,and the enzymatic activities of 3β-HSD1,1P450c17 and 17β-HSD3 in testis tissue.Results Compared to control group,the levels of testosterone and LH of diabetic group declined significantly (P ＜ 0.05) after four weeks.The mRNA levels of LHR,StAR,CYP11a1,Hsd3b6,CYP17a1 and Hsd17b3,and enzymatic activities of 3β-HSD6,P450c17 and 17β-HSD3 were also decreased significantly compared with control group (P ＜ 0.05,0.01 and 0.001).Conclusion Expression of key enzymes of testosterone synthesis in testis of early diabetic mice decreases significantly.

OBJECTIVETo discuss mass spectrum characterization of five valepotriates including 'monoene' type (didrovaltrate), 'diene' type (valtrate, acevaltrate) and 'four-olefinic' type (baldrinal and homobaldrinal) by electrospray ionization tandem mass spectrometry (ESI-MS(n)).

METHODThis study was carried out on the basis of electrospray ionization tandem mass spectrometric method and analysis of multistage fragments.

RESULTThe fragmentation patterns and structural assignment of 'monoene' type, 'diene' type and 'four-olefinic' type valepotriates in ESI-MSn under positive mode were summarized.

CONCLUSIONThe compounds have a strong pyrolysis rules and it can provide reference date for valepotriates in rapid structural identification, quantitative analysis and pharmacokinetic study.

Drugs, Chinese Herbal ; chemistry ; Iridoids ; chemistry ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry