ABSTRACT
Aim To investigate the impact and mechanism of Weichang'an Pill(WCA),its ethanol extract(EE),water extract(WE),and active ingredients on the contraction of isolated rat ileum smooth muscles induced by acetylcholine(ACh). Methods In vitro tissue bath experiment,WCA,EE,WE,or their active ingredients were added under the action of ACh,and then the contraction tension of isolated ileum smooth muscle from rats was recorded. The binding affinity ofthe active ingredients to the muscarinic acetylcholine M3 receptor was explored by molecular docking. Results WCA,EE,and WE were able to considerably inhibit the excitatory contraction of the ileal smooth muscles induced by ACh. Costunolide,dehydrocostus lactone,santalol,muscone,emodin,chrysophanol,physcion,crotonoside,magnolol,and honokiol were also significantly effective against ACh-induced ileal smooth muscle contraction. Conclusions WCA,EE,WE,and their active ingredients may help to promote intestinal smooth muscle relaxation by blocking the binding of the M3 receptor on the membrane of ileal smooth muscle with ACh.
ABSTRACT
To conduct multiple-reaction monitoring(MRM) quantitative analysis with high-performance liquid chromatography coupled with mass spectrometry method, establish the quantification method of magnolol and honokiol in blood sample under negative ion mode with ibuprofen as internal standard, investigate the pharmacokinetic process of lignans constituents after oral administration of Weichang'an pill(WCA) at different doses, and provide theoretical basis to further reveal the material basis of WCA's anti-diarrhea effect. In the plasma samples, the linear relationship was good over the concentration range of 5.25 to 1 344.00 μg•L ⁻¹ for magnolol and 10.08 to 2 580.00 μg•L ⁻¹ for honokiol. The results of precision, stability, and extraction recovery tests showed that the determination method of plasma concentration for such compositions was stable and reliable. Dose-dependence was shown for magnolol and honokiol in the plasma concentration-time profile. The results indicated that the time to reach the maximum plasma concentration(Tmax) for lignanoids was 0.55-1.42 h, when the maximum plasma concentration(Cmax) could reach 996.36-2 330.96,189.87-1 469.43 μg•L ⁻¹ respectively for magnolol and honokiol. The lignanoids could be absorbed rapidly in the blood after oral administration of WAC pills, providing experimental basis to prove rapid and long-acting anti-diarrhea effect of WAC pills after oral administration.
ABSTRACT
Objective: To observe the effect of Weichang'an Pill on regulating the gastrointestinal motility and plasma motilin (MTL) level in liver stagnation and spleen deficiency type of functional dyspepsia (FD) rat model. Methods: Sixty rats were randomly divided into six groups (n = 10): control group, model group, Weichang'an pill high (50.4 mg/kg), medium(25.2 mg/kg) and low (12.6 mg/kg) dose (middle dose for clinical equivalent dose) groups, Domperidone Tablets group as positive control group, all groups were intragastric administered for 7 d. The gastric remnant rate and plasma MTL level in rats were measured after administration. Results: The gastric residual rate in Weichang'an pill high dose group and Domperidone Tablets group decreased significantly compared with the model group (P < 0.05); The plasma MTL levels in Weichang'an pill high dose group were significantly increased compared with the control group and model group (P < 0.05). The plasma MTL in Weichang'an pill dose group was significantly higher than that of model group (P < 0.05). Conclusion: Weichang'an Pill can regulate the MTL level so that improve gastric motility and furthermore play a therapeutic effect on FD.
ABSTRACT
Objective: To study the active constituents in the methanol extract of Weichang'an Pill (MEWP) and their anti-inflammatory activity. Methods: The HPLC method was used to anylyze the constituents in MEWP. The anti-inflammatory effects of MEWP were observed on the acute anti-inflammatory models of xylene-induced ear edema, carrageenan-induced paw edema, and acetic acid-induced vascular permeability; Meanwhile the chronic anti-inflammatory model of granuloma was induced by cotton pellet implantation. Results: Twelve active constituents in MEWP were analyzed, including costunolide and dehydro-α-curcumene from Aucklandiae Radix; naringin, hesperedin, and neohesperedin from Aurantii Fructus; magnolol and honokiol from Magnoliae Officinalis Cortex; aloe-emodin, rhein, emodin, chrysophanol, and physcion from Rhei. Radix et Rhizoma. At the dose of 800 mg/kg, the MEWP showed the inhibitory rate of 39.46% on the ear edema and 35.37% on the increasing of capillary permeability induced by acetic acid in mice. It could decrease the paw edema caused by carrageenan after 1 h and inhibit the granuloma induced by cotton pellet implantation. Conclusion: The MEWP could antagonize the reaction of inflammation.