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Icariin (ICA) is one of the main active ingredient,isolated from Herba epimedii of Chinese medicine plant.It is generally used to treat osteoporosis,kidney dificiency and others.In this paper,the pharmacological effects of Icariin were summarized in the fields of anti-osteoporosis,antitumor,immunomodulation,improving reproduction,lowering blood sugar and protecting nervous system in the literatures.This paper provides a basic understanding of icariin for future studies.
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Obesity is associated with a number of metabolic abnormalities such as type 2 diabetes and has become a major health problem worldwide. In the present study, we investigated the effects of Epimedium koreanum Nakai (Herba Epimedii, HE) and its main constituent icariin on the adipocyte differentiation in 3T3-L1 preadipocytes. HE extract and icariin significantly reduced lipid accumulation and suppressed the expressions of PPARγ, C/EBPα, and SREBP-1c in 3T3-L1 adipocytes. They also inhibited fatty acid synthase (FAS), acyl-Co A synthase (ACS1), and perilipin. Moreover, HE extract and icariin markedly increased the phosphorylation of AMPK. These results indicated that HE extract and icariin can inhibit the adipocyte differentiation through downregulation of the adipogenic transcription factors, suggesting that HE containing icariin may be used as a potential therapeutic agent in the treatment and prevention of obesity.
Subject(s)
Animals , Mice , 3T3-L1 Cells , Adipocytes , Cell Biology , Metabolism , Adipogenesis , CCAAT-Enhancer-Binding Protein-alpha , Genetics , Metabolism , Epimedium , Chemistry , Flavonoids , Pharmacology , Lipid Metabolism , PPAR gamma , Genetics , Metabolism , Plant Extracts , Pharmacology , Sterol Regulatory Element Binding Protein 1 , Genetics , MetabolismABSTRACT
Objective:To explore the effect on sex hormone functional of extracts of Herba Epimedii /Fructus Ligustri Lucidi in osteoporosis rats.Methods:50 cases of 3 months Wistar rats were rando mly divided into normal group ,model group,extract low dose group(extract-L),extract middle dose group(extract-M),extract high dose group(extract-H),10 cases in each group,in addition to the normal group,other 4 groups were bulided OP model by filling and feeding retinoic acid for 15 d,then normal group and model group were filling physiological saline;extract-L,extract-M,extract-H were respectively feeding extracts of Herba Epimedii /Fructus Ligustri Lucidi at 50 mg/kg,100 mg/kg,200 mg/kg,both for 3 weeks.Measured the bone mineral density (BMD),observed the femoral pathology change of left femur with hematoxylin and eosin ( HE ) staining, measured trabecular bone tissue morphology related parameters ,analyzed the hormone receptor protein expression with immunohistochemistry .Results:The BMD of the whole femur ,femur head,and femur neck in normal group were all significantly higher than that of model group ,the BMD of the whole femur ,femur head, and femur neck in extract-M and extract-H group were all significantly higher than that of model group ,the BMD of the whole femur in extract-L group was significantly higher than that of model group ,the differences were statistically significant (P<0.05 or P<0.01).The bone trabecular number had significantly increased ,integrity,continuity improved significantly ,bone histomorphometry such as Tb.Ar, Tb.Th,and Tb.N in model group were decreased ,and Tb.Sp was increased,extract-M and extract-H group had remarkable effect on each index ,while extract-L group only had a remarkable effect on Tb .Ar and Tb.Th ( P<0.05 or P<0.01 ) , compared with model group.The expression of AR , ER in normal groups were significantly higher than that of model group , the expression of AR , ER in extract-H group was significantly higher than that of model group , the differences were statistically significant ( P<0.05 or P<0.01 ) . Conclusion:This study demonstrated that the combination with TFE and TIFL had potential protective effects on osteoporosis rats induced by retinoic acid .The combination with TFE and TIFL is able to increase BMD ,reverse pathological changes of bone tissue ,co-ordinate hormones of the hypothalamic-pituitary-gonadal axis ,and upregulate the expression of sex hormone receptors .
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Objective To optimize extraction technology of flavonesingredients from Herba Epimedii by uniform design. Methods Ultraviolet spectrophotometry was adopted to determine the content of total flavonoids. Content of epimedin A, epimedin B,epimedin C,icariin and baohuosideⅠ were determined by HPLC. U10?( 108 ) uniform design was used to conduct the multiple comprehensive evaluation of six ingredients and comprehensively analyze the influence of the concentration and amount of ethanol, extracting time on extraction of flavonesin gredients from Herba Epimedii. Results The uniform design experiment showed that 15-fold weight of 60% ethanol,extracting 2 times and each time with 165 min were the optimum extraction condition. Conclusion The method is easy and reasonable to handle,has stable and reliable results,and good repeatability and feasibility.It can be applied in industrial production.
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Objective:To determine the content of six main flavonoids in herba epimedii by self contrast with correction factor. Methods:HPLC was carried out with reversed-phase technique on an Agilent ZORBAX Eclipse XDB-C18 (150 mm × 4. 6 mm, 5 μm) column with the mobile phase consisting of acetonitrile-water with gradient elution. The detection wavelength was 268nm and the col-umn temperature was 30℃. The correction factor was established through the increase value of chromatographic peak area for the self internal standard. The relative retention time and spectrum reference method were used to determine the position of impurities. Re-sults:The relative retention time of epimedin A1 , epimedin A, epimedin B, epimedin C and baohuoside I was 0. 750,0. 810,0. 865, 0. 939 and 1. 651, respectively. The correction factor of them was 0. 998 6, 0. 998 7, 0. 998 8, 0. 989 4 and 0. 985 6, respectively. Conclusion:The self contrast with correction factor can be use to quantitatively determine the components with the same kind of chem-istry environment. The method is simple, efficient and accurate in the quantitative analysis of multi components in Chinese medicines.
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Herba Epimedii (named Yinyanghuo in Chinese) of the family Berberidaceae is one of the most famous traditional Chinese medicines (TCMs) recorded in the pharmacopoeia of the People's Republic of China.Total flavonoids of Epimedium (TFE) are considered to be its active components.TFE content was measured by ultraviolet method and its representative constituents,icariin and epimedin C,were determined by high performance liquid chromatography.The test results from 36 samples of 4 species showed that the contents differed significantly in different species.The average data of the summation (icariin and epimedin C) content were 20.83,7.61,14.43,23.29 mg/g in Epimedium pubescens Maxim.,E.koreanum Nakai.,E.brevicornum Maxim.,E.sagittatum (Sieb.Et Zucc.) Maxim.,respectively.Both E.sagittatum and E.pubescens performed better than the other two batches.E.sagittatum hardly has any circulation in Chinese herbal medicine market.The results showed that E.pubescens,which had much more amounts of icariin,epimedin C and TFE than those of other species,has a better quality and may be considered as potential anti-osteoporosis drug.
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OBJECTIVE:To optimize the extracting process of the total flavonoids from Herba Epimedii.METHODS: The extract technology of the total flavonoids from Herba Epimedii was optimized by orthogonal experiment with the yield of total flavonoids from Herba Epimedii as index and with the extraction temperature,extraction time,the ratio of solid to liquid and the concentration of ethanol as factors.RESULTS:The optimum extracting conditions for the total flavonoids from Herba Epimedii were as follows:the reflux extraction was conducted twice(1 hour/time) at 80 ℃ with 60% ethanol as solvent,and the ratio of solid to solution was 1∶10.CONCLUSION:The optimum extracting technology is simple and reasonable,and it serves as a good reference for the extracting process of the total flavonoids from Herba Epimedii.
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To elucidate the processing mechanism of Herba Epimedii from the new view of the intestinal absorption and metabolism.From analyzing the literatures of processing mechanism and togethering with the research of our lab,a new idea of processing mechanism of Herba Epimedii was brought:the pharmacologically active and easier absorbed flavonoids might be present more in the herbs when changing the heating processing parameters and thereby increased or maintained the efficacy.This thesis first pointed the new idea and method that the intestinal absorption and metabolism of herbs should be considered when studying the mechanism of processing.
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OBJECTIVE:To establish quality control method for rupining strapping.METHODS:The qualitation of Herba Epimedii,Rhizoma Bolbostemmae and fructus toosendan in rupining strapping was conducted by TLC.The principal drug-epimedium herb was determined by column chromatography-HPLC.RESULTS:Herba Epimedii,Rhizoma Bolbostemmae and fructus toosendan could all be identified in TLC.Good linear correlation of icariin was observed when the sample size was0.428?g～2.568?g(r=0.9998).The average recovery was94.57%(RSD=1.43%).CONCLUSION:The method is sensi-tive,accurate,and reproducible.It can be used for the quality control of rupining stripping.
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To investigate the mechanism of Herba Epimedii alcoho l extract for imp otence, Giess reagent was used to observe the effect of the alcohol extract of H erba Epimedii in mice and its effect on release of NO fro m human umbilical vein endothelial cells in vitro was also studied. The results showed that alcoh ol extract of Herba Epimdii had no effect on the release of NO. But the serum co llected from the mice after the medication of alcohol extract of Herba Epimedii for 120min and 180min promoted the production of NO, and the reaction reached th e peak at 120 min. It is indicated that the promotion of NO release from endothe lial cells may be one of the mechanisms of Herba Epimedii for impotence.
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Objective To observe the effects of total flavones from Herba Epimedii(TFHE)on the experimental myocardial ischemia and hemorheology of animals.Methods The model of acute myocardial ischemia of rats was established with pituitrin and the model of acute blood stasis was established with high-molecular dextran.The effects of TFHE on the electrocardiogram J-point of acute myocardial ischemia model and the hemorheology of acute blood stasis model were observed.Besides these,the effects of TFHE on coaglutaion time in mice were observed.Results As compared with the model groups,high-,middle-,and low-dosage groups(24,12,and 6 mg/kg)of TFHE could obviously improve the abnormal electrocardiogram J-point of acute myocardial ischemia model,also could effectively prevent the ascending of whole blood viscosity(high-,middle-,and low-shear rate),packed erythrocyte volume,and fibrinogen.High-and low-dosage groups(34 and 17 mg/kg)of TFHE could obviously lengthen the coaglutaion time in mice.Conclusion The results suggest that TFHE possesses protective effects on ischemic myocardium,which may better hemorheology,decrease the whole blood viscosity,prevent blood from coagulating and improve the circulatation of coronary artery.
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Objective To study the protective effects of total flavones of Herba Epimedii(TFE)on focal cerebral ischemia of rats.Methods Rat model of middle cerebral artery occlusion was established.With Jinnaduo as a positive control drug,the effect of TFE on the neurological behavior of cerebral ischemia rat,the cerebral water volume,the cerebral infarction area,the cerebral biochemistry and the pathologic change of brain were evaluated.Results TFE improved rats neurological behavior,decreased the cerebral water volume,reduced cerebral infarction area,increased ATPase and SOD activity,decreased MDA content,and also improved the pathological changes of ischemic brain.Conclusion TFE have the protective effect on cerebral ischemia in rats,its mechanism may be concerned about improving energy metabolism and anti-oxidation.
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To investigate the mechanism of Herba Epimedii alcohol extract for impotence, Giess reagent was used to observe the effect of the alcohol extract of Herba Epimedii in mice and its effect on release of NO from human umbilical vein endothelial cells in vitro was also studied. The results showed that alcohol extract of Herba Epimdii had no effect on the release of NO. But the serum collected from the mice after the medication of alcohol extract of Herba Epimedii for 120min and 180min promoted the production of NO, and the reaction reached the peak at 120 min. It is indicated that the promotion of NO release from endothelial cells may be one of the mechanisms of Herba Epimedii for impotence.
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Objective: To establish the quality standards for Jifukang Oral Solution. Methods: Fructus Corni, Fructus Ligustri Lucidi, Herba Epimedii were identified by TLC, and the content of astragalin A was determined by TLC scanning. Results: The Fructus Corni, Fructus ligustri licidi, Herba Epimedii could be identified by TLC. Astragalin A showed a good linear relationship at a range of 1.065～5.325?g,r=0.9991. The average recovery was 95.1%, and RSD was 2.0%. Conclusion: The methods are accurate and can be used for the quality control of Jifukang Oral Solution.
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Objective: To study the effects of supplemented Yang Supplementing Five Returning Decoction on the blood lipid and immune function of the model mouse. Methods: Supplemented Yang Supplementing Five Returning Decoction is composed of Yang Supplementing Five Returning Decoction, Herba Epimedii and propolis. The effects of two formulae, Yang Supplementing Five Returning Decoction and Supplemented Yang Supplementing Five Returning Decoction on the blood lipid, the functions of nonspecific immunity, humoral immunity and cellular immunity were investigated on the normal and hyperlipemia rat models and immunosuppressive mouse model. Results: Supplemented Yang Supplementing Five Returning Decoction could not only maintain the original formula functions of lowering TC. TG and LDL C of rats ( P
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AIM To investigate the changes of biochemical index of osteoporosis in rats induced by given total flavonoids of herba epimedii (HEF) . METHODS The rat osteoporosis was induced by given retinoic acid intragastrically, the biochemical index in serum (T, E 2, ALP, PTH, BGP, Osteocalcin ) and in urine (Ca, P, DPD and Cr) were determined after the rats were given HEF by low, middle and high dosages respectively, and were compared with the model group. The normal control and the positive control. RESULTS The E 2, T and BGP level in all three dosage groups were obviously higher than that of the model group. The Ca/Cr, DPD and PTH level were obviously lower than the model group. The content of Ca and P and the bone density in femur were similar with the normal control, and there was significant difference compared with the model group. CONCLUSION HEF prevents the rats treated by retinoic acid from becoming osteoporosis. The changes of biochemical index were consistent with the variation of bone density, indicating the great significance of biochemical index in diagnosis and treatment of osteoporosis.