1.Preparation process of rutacarpine-hydroxypropyl-beta-cyclodextrin inclusion complex.
Chun-Lin YAN ; Ji ZHANG ; Yong HOU ; Gui-Ping XUE ; Shu WANG ; Qing-Ya ZHAO
China Journal of Chinese Materia Medica 2014;39(5):828-832
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
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Alkaloids
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chemistry
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Chemistry, Pharmaceutical
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methods
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Drug Carriers
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chemistry
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Drugs, Chinese Herbal
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chemistry
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Rutaceae
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chemistry
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Solubility
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beta-Cyclodextrins
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chemistry
2.Infliximab versus placebo in rheumatoid arthritis patients receiving concomitant methotrexate:a randomized double blind phase Ⅲ trial in China
Yong HOU ; Feng-Chun ZHANG ; Feng HUANG ; Donghai WU ; Chun-De BAO ; Li-Qing NI ; Chen YAO ;
Chinese Journal of Rheumatology 2003;0(11):-
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.
3.Effects of recombinant gene lentivirus containing LIM mineralization protein-1 on proliferation effect and expression of bone marrow mesenchymal stem cells in rats.
Chang-sheng LIANG ; Chuan XIANG ; Zeng-yong WEI ; Hui-ming HOU ; Ying-ze QIN ; Xiao-chun WEI
China Journal of Orthopaedics and Traumatology 2013;26(12):1023-1027
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
4.Discussion on the treatment amount of acupuncture and moxibustion.
Chinese Acupuncture & Moxibustion 2009;29(8):670-674
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
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Acupuncture Therapy
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Humans
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Moxibustion
5.Semi-artificial Simulate Cultivation of Phlebopus portentosus and the Durability of Hyphae on Host Roots
Kai-Ping JI ; Ming-Xia HE ; Chun-Xia ZHANG ; Jing LIU ; Wen-Bing WANG ; Jian-Yong HOU ;
Microbiology 1992;0(03):-
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.
6.ASAS20 at week 2 predicts subsequent improvement as well as the rate of relapse of ankylosing spondylitis infused with three pulses of infliximab
Jian ZHU ; Feng HUANG ; Li-Yun ZHANG ; Jiang-Lin ZHANG ; Feng-Chun ZHANG ; Yong HOU ; Deen YU ;
Chinese Journal of Rheumatology 2001;0(05):-
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.
7.Expression of COX-2 in different human prostate cancer cell lines and its significance.
Jia-Hui ZHAO ; Yong-Guang JIANG ; Chun-Ting WU ; Yong LUO ; Zhu HOU ; Da-Lin HE
National Journal of Andrology 2010;16(8):689-692
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
8.Effects of scalp catgut embedding on SOD, NO, MDA in the rat with Parkinson's disease.
Xiao-Xia XIE ; Suo-Tang KOU ; Zhi-Hong PU ; Chun-Ying HOU ; Yong-Ping TIAN
Chinese Acupuncture & Moxibustion 2007;27(10):753-756
OBJECTIVETo explore the mechanism of scalp catgut embedding for treatment of Parkinson's disease.
METHODSParkinson's disease model rats were prepared, and randomly divided into a model group, scalp acupuncture group, medication group, with a control group set up. The scalp acupuncture group were treated with catgut embedding at "the chorea-trembling conroued area" lateral to "Baihui" (GV 20) and the medication group with intra-gastric perfusion of L-dopa suspension. After treatment for 30 days, behavior indexes were investigated and malondialdehyde (MDA) and nitric oxide (NO) contents and superoxide dismutase (SOD) activity in the brain were detected.
RESULTSMDA content in the brain of the model rats were significantly decreased (P < 0.01), NO level significantly increased (P < 0.05) by scalp catgut embedding, with no significant change of SOD activity (P > 0.05); and the behavior indexes and tissue and form of the brain had significant improvement.
CONCLUSIONScalp catgut embedding has regulative action on anti-oxidant enzyme system in the Parkinson's disease rats, has significant improvement of cells, tissues and form of the brain.
Acupuncture Therapy ; methods ; Animals ; Catgut ; Female ; Male ; Malondialdehyde ; analysis ; Nitric Oxide ; analysis ; Parkinson Disease ; metabolism ; therapy ; Rats ; Rats, Wistar ; Scalp ; Superoxide Dismutase ; metabolism
9.Protection and mechanism of shenqi compound for diabetic angiopathy model rats.
Yong-He HU ; Jun HOU ; De-Zhi ZHENG ; Dan-Dan LI ; Xin-Zhong HAO ; Chun-Guang XIE ; Lian DU ; Qing NI ; Yi SHEN ; Jing LI
Chinese Journal of Integrated Traditional and Western Medicine 2014;34(9):1078-1085
OBJECTIVETo investigate the protective effect and mechanism of Shenqi Compound on diabetic angiopathy modeled rats.
METHODSTotally 18 SD rats were randomized into 3 groups, i.e., the normal control group, the diabetic mellitus (DM) group, and Shenqi Compound group, 6 in each group. The DM rat model was established by feeding high-fat diet (to induce hyperlipidemia) +intraperitoneal injection of small dose streptozotocin (STZ). Shenqi Compound was given to rats in the Shenqi Compound group at the daily dose of 2 g/kg. Equal volume of normal saline was given to rats in the model group and the normal control group by gastrogavage. All treatment was lasted for 12 weeks. Then 2-D and ultrasonic integrated backscatter technique were used to evaluate structural and functional changes of abdominal aorta in the progression of diabetic macroangiopathy. The fibrosis degree of the aorta vessel and myocardium capillaries were observed by using HE and Masson trichrome staining. The tension of the aortic vascular ring was determined. The transforming growth factor beta (TGF-beta) mRNA expression was detected by real time PCR (RT-PCR). The protein expression of TGF-beta, collagen I, collagen III, connective tissue growth factor (CTGF), and phosphorylation P38 MAPK were detected by Western blot.
RESULTSCompared with the normal control group, abdominal aortic systolic inner diameter, diastolic inner diameter, Peterson elastic modulus, stiffness index, and backscatter integral significantly increased; the rangeability of integral backscatter and the extension coefficient of cross section significantly decreased in the DM group (all P < 0.05). After 12 weeks aforesaid indices were obviously improved in the Shenqi Compound group (P < 0.05). Results of HE and Masson staining showed that the fibrosis degree of the aorta vessel and myocardium capillaries was obviously alleviated in rats of the Shenqi Compound group (P < 0.05). Results of the aortic vascular ring tension showed that acetylcholine induced vasodilatation and maximum diastolic percent were obviously elevated in the Shenqi Compound group (P < 0.05). Compared with the normal control group, the mRNA expression of TGF-beta, and the protein expression of TGF-beta, collagen I, and collagen III, and phosphorylation of P38 MAPK all significantly increased in the DM group (P < 0.05). Compared with the DM group, the mRNA expression of TGF-beta, and the protein expression of TGF-beta, collagen I, and collagen III, and phosphorylation of P38 MAPK all decreased (P < 0.05).
CONCLUSIONSShenqi Compound could effectively improve the arterial function in diabetic marcoangiopathy and microvascular dysfunction. The mechanism might be due to the down-regulating the expression of TGF-beta, and further suppressing the phosphorylation of P38 MAPK, reducing the synthesis of collagen I and collagen III, therefore, ameliorating arterial and myocardial interstitial fibrosis.
Animals ; Collagen Type I ; metabolism ; Collagen Type III ; metabolism ; Diabetes Mellitus, Experimental ; drug therapy ; Diabetic Angiopathies ; prevention & control ; Drugs, Chinese Herbal ; pharmacology ; Male ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Transforming Growth Factor beta1 ; metabolism ; p38 Mitogen-Activated Protein Kinases ; metabolism
10.Classified teaching of acupoints: standardized teaching in Jingluo Shuxue Xue (Channels and Acupoints science).
Shu-Wei HOU ; Zu-Bin MA ; Yong-Chun LI
Chinese Acupuncture & Moxibustion 2010;30(10):865-869
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
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education
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standards
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Acupuncture Points
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Cyclobutanes
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Humans
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Teaching
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standards