C.speciosa flavonoids on gastrointestinal smooth muscle relaxation effect and mechanism analysis_733

By Melvin Boyd,2014-10-30 11:44
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C.speciosa flavonoids on gastrointestinal smooth muscle relaxation effect and mechanism analysis_733

    C.speciosa flavonoids on gastrointestinal smooth muscle relaxation effect and mechanism analysis

     Abstract Objective To investigate the C.speciosa total flavonoids (FLC) on gastrointestinal smooth muscle relaxation and its related mechanisms. Methods The isolated rabbit jejunum, ileum and gastric fundus smooth muscle bioassay method to observe the FLC of the jejunum autonomy Ach-induced

    contraction and contraction, as well as ileum and gastric fundus of different agonists (Ach and CaCl2) response. Results

    FLC autonomy of the jejunum contraction and Ach-induced

    inhibition of contractile responses Jun Cheng; dose-

    dependently inhibited the Ca2-induced ileum contraction (P

    <0.01), and Ach induced contraction of gastric muscle strips,

    non-competitive antagonist Ach and the cumulative amount of CaCl2 dose-response curves, suppressing the maximum response. Conclusion FLC gastrointestinal smooth muscle relaxation and blocking VDC to reduce calcium influx and calcium release related to the role, but has nothing to do with the M

    cholinergic receptor antagonist.

     Key words C.speciosa gastrointestinal smooth muscle mechanism analysis of total flavonoids

     Abstract: ObjectiveTo elucidate the relaxant effects and related mechanisms of total flavone from Chaenomeles lagenaria Koidz (FLC) on relaxant gastrointestinal smooth muscles. MethodsThe relaxant effects and related mechanism of FLC were studied on the contraction of isolated rabbit jejunum, ileum and gastric fundus agonized by Ach and CaCl2. Results FLC

    inhibited the contraction of isolated jejunal autonomic and jejunum agonized by Ach. In the isolated rabbit gastric fundus or ileum, FLC were found to inhibit the contraction induced by Ach and CaCl2 in dose-dependent manner, and non-competitively

antagonize the Ach or CaCl2 cumulative dose-response curves

    with a lower maximal response, while Atr (atropine) competitively inhibited the gastric fundus contraction induced by Ach.ConclusionThe mechanisms of relaxant gastrointestinal smooth muscle of FLC is related to its blocking effect on the voltage dependent Ca2 channel (VDC), but is not related to muscarinic receptor blocking.

     Key words: FLC; Gastrointestinal smooth muscle; Mechanism analysis

     C.speciosa as tiegeng Rosaceae Chaenomeles lagenaria

    (Loisel) Koidz the fruits, the main produced in China, Anhui, Hubei and Sichuan provinces, of which the major ingredients include organic acids, such as flavonoids and saponins. C.speciosa for the clinical application base, I had room for

    its ethanol extract of the overall context of animal studies. Experimental results show that: C.speciosa ethanol crude extracts with gastrointestinal smooth muscle relaxation and analgesic effects [1,2], in order to explore one of the effective parts and in-depth efficacy mechanism, this

    experiment used C.speciosa flavonoids on gastrointestinal smooth muscle The relaxation mechanism was analyzed and discussed.

     1 Materials and methods

     1.1 Materials healthy rabbits of either sex, weighing 2.0

    ~ 3.0 kg, from the Experimental Animal Center of China Three Gorges University. C.speciosa from Changyang ziqiu by the Three Gorges University, Key Laboratory of Natural Medicine Professor Wang Yunzhi identification. C.speciosa total flavonoids (FLC) provided by the China Three Gorges University College of metaplasia, the preparation methods refer to literature [3] to ADS-17 macroporous resin purification

    derived FLC, temporary use double-distilled water when the

    concentration of the preparation of the corresponding spare.

    Acetylcholine (Acetylcholine chloride, Ach), Shanghai Reagent Factory 3. Verapamil (Verapamil, Ver) were purchased from Tianjin Pharmaceutical Group. Atropine Sulfate Injection (Atropine, Atr) were purchased from Wuhan Grand Pharmaceutical

    Group. ADS-17 macroporous resin, Nankai University Chemical

    Factory. Other reagents were commercially available analytical pure. Experiment with the Standard Tyrode solution (mmol / L): NaCl 136.9, KCl 2.68, CaCl2 1.80, MgCl2 1.05, NaH2PO4 0.42, Glucose 5.55. Calcium-free Tyrode solution without Calcium and plus 0.1 mmol / L EDTA, make it a non-calcium solution

    containing EDTA. In addition to calcium-free high-K Tyrode

    solution without calcium addition, KCl replaced by 40 mmol / L, substitution mmol / L of NaCl. PowerLab isolated organ

    perfusion instrument (Australia).

     1.2 Methods 24 h fasted rabbits, hit the first letter after dusk quickly clipping connected with the duodenum and the jejunum is about 2.0 cm from the ileocecal about 3 cm of ileum 1.5 ~ 2.0 cm, repeated washing with Tyrode solution lumen contents back; the same time, full-thickness gastric

    muscle specimens taken at about 2 cm × 2 cm, Tyrode solution

    rinse, press Vane's Preparation of gastric smooth muscle. Subjects specimens were placed with 10 ml of Tyrode solution (37 ? 0.5) ? of the bath, pH 7.2 ~ 7.4, even at the end of the tension specimens transducer and the other end fixed, the specimen tension load 1 g, the experiment continues which leads to 95% O2 5% CO2 gas mixture, the specimen tension

    changes recorded by tension transducer in isolated organ perfusion in the PowerLab instrument. Experimental drug concentrations used in calculating the final concentration according bath.

     Statistical analysis: Data to ? s said that the

    application of SPSS10.0 software, between the two groups using t test; mapping software used SigmaPlot2001.

     2 Results

     2.1 FLC autonomy in rabbit jejunum contraction and Ach-

    induced contraction of jejunum in Tyrode-liquid equilibrium

    after 30 min, resulting in the autonomy of the law and a constant contraction, by adding 0.01 mmol / L Ach to normal after the contraction frequency and the same, but the tension increased by about 30%, and then were added to 0.2%, 0.4% and 0.8% FLC, recorded in different experimental conditions, jejunal contraction frequency and tension changes were observed 10 min. The results in Table 1.

     2.2 FLC of the CaCl2-induced contraction of ileum smooth muscle experimental methods and conditions with the 2.1, the specimen after incubation for calcium-free Tyode fluid,

    showing that the autonomy ileum contraction gradually weakened, when the contraction frequency and tension was significantly affected by inhibition by adding CaCl2 2.0 mmol / L, can be seen ileum contraction rapid recovery, recording the changes in contraction amplitude and tension, with calcium-free Tyode wash samples three times, were added to 0.2%, 0.4% and 0.8% of the FLC, 5 min after adding CaCl2 2.0

    mmol of the same Act / L, compare samples before and after administration of CaCl2 contraction effects. The results in Table 2.

     Table 1 FLC autonomy in rabbit jejunum contraction and Ach-induced contraction effects (abbreviated)


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