Development of Tripterygium glycosides nano-carries based on "nanoemulsion-gels" and its pharmacodynamics / 中国中药杂志

The aim of this study is to develop the Tripterygium glycosides nanoemulsion gels and investigate its pharmacodynamics. Oleic acid was used as oil phase, polyoxyethylene castor oil as surfaetant, and 1,2-propanediol as cosurfactant to screen the formula of Tripterygium glycoside nanoemulsion using the pseudo-temary phase diagrams. Then the nanoemulsion gels was prepared. The ICR mouse ears were sensitazated by 7% DNCB, and then were excited by 0.3% DNCB to stimulate the model of mouse chronic dermatitis and eczema. The concentrations of IFN-γ, IL-4 and IL-8 in mouse blood were determined by ELISA. The results showed that Tripterygium glycosides nanoemulsion gels could significantly inhibit the swelling of mouse ears(P < 0.01) and ameliorate the edama and erythema of model mouse ears skin. Also it could significantly decrease the expression of IFN-γ and IL-4 in model mouse blood. Tripterygium glycosides nanoemulsion gels had a good therapeutic effect on mouse model of dermatitis and eczema. It was expected to provide a new and long-acting exterernal preparation for the treatment of dermatitis and eczema.

Adiponectin decreases insulin receptor substrate-1 phosphorylation in the liver of OLETF rats possibly through nuclear factor-κB signaling pathway / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the effect of adiponectin (APN) on the insulin pathway in the liver of OLETF rats and explore its molecular mechanism.</p><p><b>METHODS</b>Twenty male OLETF rats and 10 male LETO rats were sacrificed at 8 and 32 weeks of age to examine the fasting blood glucose, serum insulin, adiponectin and blood lipid profiles. The APN, phosphotyrosine of insulin receptor substrate-1 (IRS-1), IKKβ and nuclear-κB (NF-κB) in the liver tissue were determined using ELISA, Western blotting or immunohistochemistry.</p><p><b>RESULTS</b>The plasma adiponectin level in OLETF rats was significantly lower than that of LETO rats since 8 weeks of age (P<0.01). At 32 weeks of age, the blood lipid levels of OLETF rats increased significantly (P<0.05) with inverse correlations to plasma adiponectin (P<0.01). The liver APN, py-IRS-1, IKKβ and NF-κB levels in OLETF rats differed significantly from those of LETO rats at both 8 and 32 weeks. At 32 weeks of age, the APN level of both rats were correlated to the levels of NF-κB and py-IRS-1 (P<0.01).</p><p><b>CONCLUSION</b>APN may decrease tyrosine phosphorylation of IRS-1 via the IKK/NFκB pathway and inhibit insulin signaling pathway in the liver, which contributes to hyperlipidemia, hyperglycemia and development of type 2 diabetes.</p>

Hypoadiponectinemia leads to insulin resistance in OLETF rats: a preliminary study / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the association between plasma adiponectin and insulin resistance in OLETF rats.</p><p><b>METHODS</b>Twenty male Otsuka Long-Evans Tokushima Fatty (OLETF) rats and 10 male Long-evans Tokushima Otsuka (LETO) rats underwent oral glucose tolerance test (OGTT) at 13 and 40 weeks of age. At 8, 32 and 40 weeks of age, the rats were sacrificed to measure the blood glucose, plasma insulin and adiponectin levels, and serum levels of TG, CHOL and FFA.</p><p><b>RESULTS</b>The plasma adiponectin level was significantly decreased in 8-week-old OLETF rats compared with that of LETO rats (P<0.05). The plasma insulin level, TG, CHOL, and FFA were significantly higher in OLETF rats than in LETO rats at 32 and 40 weeks of age.</p><p><b>CONCLUSION</b>A decreased plasma level of adiponectin preludes insulin resistance and is inversely correlated to insulin sensitivity. Hypoadiponectinemia may be an important reason leading to insulin resistance.</p>

Relationship between visceral fat depot and adiponectin mRNA level in the adipose tissue of OLETF rats / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the relationship between visceral fat depot and adiponectin level in OLETF rats.</p><p><b>METHODS</b>Twenty male OLETF rats and 10 male Long-Evans Tokushima Otsuka (LETO) rats were subjected to regular oral glucose tolerance test (OGTT). The rats were sacrificed at the ages of 8, 32 and 40 weeks for measurements of the body weight, blood glucose, blood lipid level, blood insulin, and weight of the visceral fat.</p><p><b>RESULTS</b>Compared with LETO rats, OLETF rats had significantly higher body weight and visceral fat with impaired glucose tolerance (P<0.05). OLETF rats also had higher blood insulin, TG, FFA and CHOL levels (P<0.05). The plasma adiponectin level was significantly lower in OLETF rats than in LETO rats at different ages (P<0.05). The adiponectin mRNA level in the adipose tissue of OLETF rats was comparable with that in LETO rats, but significantly decreased at 32 and 40 weeks of age (P<0.01).</p><p><b>CONCLUSION</b>Plasma adiponectin level is significantly correlated to insulin sensitivity and visceral fat depots in OLETF rats, but a lowered APN mRNA expression level is not the main reason for a decreased plasma adiponectin level in the early stage.</p>

Effect of Liuweidihuang pills in preventing diabetes mellitus in OLETF rats / 南方医科大学学报

<p><b>OBJECTIVE</b>To study the effects of Liuweidihuang pills in preventing diabetes in Otsuka Long-Evans Tokushima Fatty (OLETF) rats.</p><p><b>METHODS</b>Forty male OLETF rats were randomized equally into Liuweidihuang pill group and control group, with 10 male LETO rats as the normal control group. In Liuweidihuang pill group, the rats were given the pills intragastrically at the daily dose of 2.4 mg/kg since 8 weeks of age, and the rats in the other two groups received water instead. Blood glucose of the rats was determined by oral glucose tolerance test (OGTT), and the body weight and food intake were monitored on a weekly basis. At 8, 32 and 40 weeks, the rats were sacrificed and the expression level of adiponectin mRNA in the adipose tissue was detected using RT-PCR.</p><p><b>RESULTS</b>Treatment with Liuweidihuang pills significantly lowered the increment of the blood glucose and postponed the onset of hyperglycemia in the rats. Compared with the control group, the rats in Liuweidihuang pill group showed significantly increased expression of adiponectin mRNA in the adipose tissue. The rats receiving Liuweidihuang pills developed diabetes at 30 weeks of age with an incidence of 28.6% at 40 weeks, significantly lower than that in the control group (P<0.01).</p><p><b>CONCLUSION</b>Liuweidihuang pills can significantly increase the expression of adiponectin mRNA in the adipose tissue and decrease the incidence of type 2 diabetes in OLETF rats.</p>

Effects of Liuweidihuang pills on pancreatic islet structure in OLETF rats / 南方医科大学学报

<p><b>OBJECTIVE</b>To study the effects of Liuweidihuang pills on pancreatic islet structure in OLETF (Otsuka Long-Evans Tokushima Fatty) rats.</p><p><b>METHODS</b>Forty male OLETF rats were divided randomly into Liuweidihuang pills group (Liuwei group) and control group (n=20). Ten male LETO rats were used as normal control group (LETO group). The rats in Liuwei group were given Liuweidihuang pills at the daily dose of 2.4 mg/kg intragastrically since the age of 8 weeks. Blood glucose was determined by OGTT. The rats were sacrificed at 8, 32 and 40 weeks and the pancreatic tissue was isolated to examine the morphological changes of the pancreas by HE staining and Masson trichrome staining.</p><p><b>RESULTS</b>As the age of the rats increased, the pancreatic islets in the control group gradually showed fibrosis and islet atrophy, which were not found in Liuwei group. Masson staining visualized no fibrosis in Liuwei group. No significant pathological change occurred in the pancreatic islet of LETO rats. The rats in Liuwei group developed diabetes since 30 weeks of age and the incidence was 28.6% at 40 weeks, significantly lower than that in the control group (P<0.01).</p><p><b>CONCLUSION</b>Liuweidihuang pills can prevent degeneration of the pancreatic islets in spontaneous OLETF rats.</p>

Liuweidihuang pills reduces visceral fat deposition in Otsuka Long-Evans Tokushima Fatty rats / 南方医科大学学报

<p><b>OBJECTIVE</b>To investigate the effects of Liuweidihuang pills (LP) on visceral fat deposition in Otsuka Long-Evans Tokushima Fatty (OLETF) rats.</p><p><b>METHODS</b>Forty male OLETF rats were randomly divided into LP group and control group (n=20 per group), and 10 male Long-evans Tokushima Otsuka (LETO) rats were used as normal controls. The rats in LP group were given LP(2.4 mg/kg) daily by intragastric administration since the age of 8 weeks, and those in the other two groups were given water of the same volume by intragastric administration. Blood glucose of all the rats was determined by oral glucose tolerance test (OGTT) and visceral fat deposition examined after the rats were sacrificed.</p><p><b>RESULTS</b>OLETF rats had obviously greater amount of visceral fat than LETO rats (P<0.05) and administration of LP ameliorated the increment of visceral fat deposition in this type 2 diabetic model, producing significant effect at the age of 40 weeks (P<0.01).</p><p><b>CONCLUSION</b>LP may effectively decrease visceral fat deposition in OLETF rats.</p>

Percutaneous penetration of ketoprofen and ketoprofen isopropyl ester through a tissue engineering skin reconstructed with HaCaT cells / 药学学报

<p><b>AIM</b>To reconstruct of a tissue engineering skin in vitro for the study of the use of drug percutaneous penetration and metabolism.</p><p><b>METHODS</b>Dermal fibroblasts were embedded in collagen type I. HaCaT cells were seeded on the top of the gel. The skin was generated through air-liquid interface culture. Effects of various culture media on tissues morphology were investigated. Sections of the cultured skin were stained with hematoxylin and eosin and examined under microscope. Permeation and metabolism of ketoprofen and its isopropyl ester through the cultured skin were investigated.</p><p><b>RESULTS</b>HaCaT cells initially developed a multilayer epithelium at the air-liquid interface, but it showed a parakeratotic stratum corneum. Vitamin C enhanced cell proliferation obviously. Vitamin D3 promoted cell differentiation. And estradiol showed little effect on the tissue engineering skin. Ketoprofen isopropyl ester was hydrolyzed into ketoprofen when penetrated through the cultured skin, which resembled in the skin cell homogenates metabolism.</p><p><b>CONCLUSION</b>Cultured at the air-liquid interface, HaCaT cells developed a parakeratotic mutilayer epithelium. Enzyme activity was reserved. This cultured skin could serve as an appropriate model for drug percutaneous metabolism and skin irritation.</p>