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Objective To investigate the effect of the Shaofu zhuyu decoction on the changes of the body writhing behavior,inflammatory reaction and COX-2 expression of the rats with the primary dysmenorrhea. Methods Fifty SD female rats were randomly divided into blank control group,model control group,high,middle and low dose of Shaofu zhuyu decoction groups,10 in each group.Dysmenorrhea rat model was established by treating with estradiol benzoate and oxytocin.Effect of Shaofu zhuyu decoction of different doses on writhing behavior,changes of endometritis cells and COX-2 expression in uterine smooth muscle of dysmenorrhea rats were observed. Results In the model control group,latency of the body writhing behavior was shortened and the total score was high,many inflammatory cells (especially for neutrophils) infiltrated in endometrium and uterine smooth muscle,immunohistochemistry showed that brown granules were found in the cytoplasm of smooth muscle cells of uterus,and COX-2 expression was positive in uterine smooth muscle cells.As compared with the model control group,writhing latency increased,total score decreased in both the high and middle dose of Shaofu zhuyu decoction groups,and infiltration of a small number of inflammatory cells was seen in the endometrium and smooth muscle(P<0.01);COX-2 expression was decreased (P<0.01) especially for the high dose of Shaofu zhuyu decoction group.As compared with the model control group,the latency of the low dose of Shaofu zhuyu decoction group was significantly increased,and the total score was decreased(P<0.01),but there was no significant difference in inflammatory cell infiltration and COX-2 expression (P>0.05). Conclusion A potential mechanism by which Shaofu zhuyu decotion treats primary dysmenorrhea may be related with alleviating pain,inhibiting inflammatory responses,and down-regulating expression of COX-2.
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Ardipusilloside-I is a natural triterpenoid saponin, which was isolated from Ardisia pusilla A. DC. The aim of the study was to evaluate the stimulation of ardipusilloside-I on gastrointestinal motility in vitro and in vivo. The experiment of smooth muscle contraction directly monitored the contractions of the isolated jejunal segment (IJS) in different contractile states, and the effects of ardipusilloside-I on myosin were measured in the presence of Ca²⁺-calmodulin using the activities of 20 kDa myosin light chain (MLC₂₀) phosphorylation and myosin Mg²⁺-ATPase. The effects of ardipusilloside-I on gastro emptying and intestinal transit in constipation-predominant rats were observed, and the MLCK expression in jejuna of constipated rats was determined by western blot. The results showed that, ardipusilloside-I increased the contractility of IJS in a dose-dependent manner and reversed the low contractile state (LCS) of IJS induced by low Ca²⁺, adrenaline, and atropine respectively. There were synergistic effects on contractivity of IJS between ardipusilloside-I and ACh, high Ca²⁺, and histamine, respectively. Ardipusilloside-I could stimulate the phosphorylation of MLC₂₀ and Mg²⁺-ATPase activities of Ca²⁺- dependent phosphorylated myosin. Ardipusilloside-I also stimulated the gastric emptying and intestinal transit in normal and constipated rats in vivo, respectively, and increased the MLCK expression in the jejuna of constipation-predominant rats. Briefly, the findings demonstrated that ardipusilloside-I could effectively excite gastrointestinal motility in vitro and in vivo.
Subject(s)
Animals , Rats , Ardisia , Atropine , Blotting, Western , Epinephrine , Gastric Emptying , Gastrointestinal Motility , Histamine , In Vitro Techniques , Muscle, Smooth , Myosin Light Chains , Myosin-Light-Chain Kinase , Myosins , Phosphorylation , SaponinsABSTRACT
Objective To investigate the interaction of pullulan acetate nanoparticles (PANs) and bovine serum albumin (BSA),and to provide the basis for in vivo pharmacokinetic study of PANs.Methods Mixed solutions of different concentration of PANs and BSA solution was prepared,the interaction was studied by fluorescence quenching method and circular dichroism (CD) measurement.Apparent quenching constant (Kq) between the PANs and BSA was calculated,and the anti-stress effect induced by urea and heating of PANs-BSA solution was observed.Results The fluorescence spectrum of BSA was affected by PANs on density-related manner,and Kq calculated by the modified Stern-Volmer plot increased from 2.64×104 to 3.55 ×l05 with the concentration of PANs increased from 0.015 mg/ml to 0.25 mg/ml.With the denaturation of urea or heating,the CD spectrum of PANs-BSA and free BSA had the similar variation tendency.Conclusions The fluorescence spectrum display results show that interaction between PANs and BSA exists,but the interaction does not protect the BSA from degeneration by urea and heating.
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Objective To explore the effect of adiponectin on the pathophysiology and treatment of type 2 diabetes. Methods 50 patients with newly diagnosed type 2 diabetes were given insulin intensive therapy.Body mass index(BMI), blood lipids, blood glucose, insulin and adiponectin were measured before and after the insulin treatment.36 healthy persons were selected to match for sex and age with diabetes patients. Results In type 2 diabetes patients, before insulin intensive treatment,the level of adiponcetin was 4.28(2.11-6.38)μg/L and arose to 12.26(8.22-16.00)μg/L after 12.6±2.1 day insulin treatment.In healthy persons, the level of adiponectin was 9.56(7.92-11.61)μg/L.There was significant difference among the three groups.Adiponectin was negatively correlated with BMI and triglyceride and positively correlated with insulin action index (IAI) and high density lipoprotein (HDL). Conclusions Adiponectin plays a major role in the pathophysiology and treatment of newly diagnosed type 2 diabetes.
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Objective To compare the efficacy of insulin aspart and human soluble insulin on postprandial glucose control and blood glucose excursion in type 2 diabetic patients managed with insulin pump therapy. Methods All of 345 hospitalized type 2 diabetic patients were randomized divided into two groups. One group underwent insulin pump therapy with insulin aspart (aspart group, 173 cases),another group with human soluble insulin (humulin R group, 172 cases). Capillary glucose concentrations were measured at 9 time points,including preprandial,2 hours postprandial,bedtime (22:00),midnight(0:00) and 3:00 every day during the treatment. The change of blood glucose at each time point and the variation of postprandial blood glucose excursion was compared between the two groups. The frequency of hypoglycemia was also evaluated. Results After treatment, fasting blood glucose and post breakfast and post dinner blood glucose levels were decreased more significantly in the aspart group than those in the humulin R group. And a significantly smaller postprandial blood glucose excursion was shown in the aspart group compared with that in the humulin R group (P< 0.05). The time to achieve good glycemic control in the aspart group was (4.40 ± 2.16) d, significantly shorter than that in the humulin R group[(5.68 ± 2.29) d](P< 0.05). The incidence of hypoglycemia was significantly lower in the aspart group (P <0.05). Conclusion Insulin aspart results in better control of blood glucose and less glycemic variability compare with human soluble insulin in type 2 diabetic patients during delivery by continuous subcutaneous insulin infusion.
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Objective To explore the application of continuous subcutaneous insulin infusion (CSII) in elderly type 2 diabetic patients. Methods Elderly group(n = 415) and control group (n= 461) received the transient CSII intensive treatment. The different regiments and the incidence of hypoglycemia were observed between the two groups. Results The average duration reaching the target blood glucose and the insulin dosage at the target time were similar between the two groups (P>0.05). The insulin basal rate in the elderly patients was lower than that in control group. The incidence of hypoglycemia, especially at night, was significantly higher in the elderly patients.Conclusions CSII could control blood glucose effectively in elderly type 2 diabetic patients, but the basal insulin dosage should be decreased to reduce the risk of hypoglycemia.
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Aim To study the antitumor and immunological regulation effects of ardipusilloside-Ⅰ(ADS-Ⅰ) on tumor-bearing mice of S180, H22, EAC and L1210. Methods The tumor-bearing mouse model was made through injecting cancer cells in the right limb oxter(or in abdominal cavity), and the mice were administrated orally with ADS-Ⅰfor 8 days. Then we detached the tumor and counted the inhibition rate of tumor growth. Incorporation of ()~3H-TdR was used to assess the proliferation of T spleen lymphocyte cells; phagocytosis of abdominal cavity macrophage was measured with the method of chicken red blood cells. Results ADS-Ⅰ was proved to be effective on the tumor-bearing mice of S180, H22 and EAC, and the maximal inhibition rate of the dose of 100 mg?kg~(-1) was 38.7%, 48.6% and 50.0%, respectively;ADS-Ⅰ promoted the proliferation of T spleen lymphocyte cells,and strengthened the phagocytosis of macrophage in the tumor-bearing mice significantly. Conclusion ADS-Ⅰ can inhibit the growth of transplanted tumor,and improve the immunological function of tumor-bearing mice.
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Objective To prepare ?-CD(?-cyclodextrin) inclusion compounds and PEG- 4000[poly-(ethylene glycol) 4000] solid dispersions of mefenamic acid (MFA)in order to improve its dissolution. Methods The inclusion compounds of MFA were prepared using saturated ?-CD solution method by orthogonal test. The solid dispersions were prepared using melt-cool process with PEG- 4000 as a carrier. The inclusion compounds and solid dispersions were identified by differential scanning calorimetry (DSC) gram and their dissolution rates were tested in pH8.0 buffer solution. Results The suitable condition for preparing ?-CD inclusion compounds of MFA industrially was the weight ratio of 1∶4 between MFA and ?-CD, agitating for 4 h at 70 ℃. The suitable proportion for preparing solid dispersions of MFA was the weight ratio of 1∶4 between MFA and PEG- 4000. Conclusion Dissolution rates of MFA are apparently improved in inclusion compounds and PEG- 4000 solid dispersions, and the solubility of MFA is apparently increased by 2～3 times in inclusion compounds and PEG- 4000 solid dispersions.