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The present study aims to investigate the effects of the main components(aesculin, berberine hydrochloride, and anemoside B4) in the butyl alcohol extract of Baitouweng Decoction(BAEB) on the chemotaxis of neutrophils induced by dimethyl sulfoxide(DMSO). HL60 cells were cultivated in RPMI-1640 complete medium, and transferred into a 6-well plate(2 × 10~5 per mL) with 4 mL in each well, followed by incubation with DMSO at 1.3% for five days. The morphologic changes of cells were observed under an inverted microscope. The CD11 b expression after DMSO induction was analyzed by flow cytometry. The effects of aesculin, berberine hydrochloride, and anemoside B4 on the cell proliferation and migration were detected by CCK8 assay and Transwell assay, respectively. The effects of the main components on the production and polarization of F-actin protein were also examined by flow cytometry and laser confocal microscopy. PI3 K/Akt signaling pathway was checked by Western blot. As revealed by the results, neutrophil-like HL60 cells were observed after DMSO induction. The CD11 b expression in these cells increased significantly as indicated by the flow cytometry. Additionally, 100 μg·mL~(-1) aesculin, 8 μg·mL~(-1) berberine hydrochloride, and 80 μg·mL~(-1) anemoside B4 were potent in inhibiting the migration of neutrophils and reducing F-actin expression. Berberine hydrochloride was verified to be capable of diminishing phosphorylated PI3 K/Akt protein expression. The findings indicate that aesculin, anemoside B4, and especially berberine hydrochloride in the BAEB can inhibit the chemotaxis of neutrophils, which is possibly achieved by the inhibition of F-actin and PI3 K/Akt signaling pathway.
Subject(s)
1-Butanol , Berberine/pharmacology , Chemotaxis , Drugs, Chinese Herbal/pharmacology , NeutrophilsABSTRACT
Objective: To investigate the active ingredients of chicory on uric acid-lowering, and make a preliminary study on the safety as well as mechanism of uric acid-lowering. Methods: Fifty quails were evenly randomized into five groups, namely normal group, model group, benzbromarone (20 mg/kg) group, high-dose and low-dose mixture groups (150, and 50 mg/kg), 10 quails in each group. Except for the normal group, the quails in other groups were given high purine diet (ordinary forage mixed with 15 g/kg of yeast extract powder) to induce hyperuricemia model. And then we observed the changes of UA, ALT, AST, Cr, BUN, XOD, and ADA levels in serum during the treatment. Results: During the molding period, model group of serum UA level significantly increased (P 0.05) in 7-21 d; The XOD and ADA levels showed different degrees of inhibition. Conclusion: Chlorogenic acid, aesculin, as well as chicoric acid has the effect on lowering serum uric acid level in quail hyperuricemia model, which may be associated with reducing the activities of XOD and ADA levels.
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Objective To develop a HPLC method for determination of aesculin, aesculetin,baicalin and ellagic acid in Xielining tablets. Methods The hypersil C18 column was used with the flow rate of 1. 1 mL·min-1 . The mobile phase A consisted of methanol-acetonitrile(4∶1),the mobile phase B consisted of 0. 1% phosphoric acid solution; The detection wave-lengths were λ1 =334 nm(aesculin and aesculetin),λ2 = 280 nm(baicalin),and λ3 = 254 nm(ellagic acid). Results There was a good linear relationship between the peak area values and concentrations of aesculin,aesculetin,baicalin and ellagic acid. The quantitation range of aesculin,aesculetin,baicalin and ellagic acid was 0. 058 6 -1. 172 0 μg( r = 0. 999 2), 0. 015 4 -0. 308 0 μg(r=0. 999 8),0. 447 2-8. 944 0 μg(r=0. 999 6),and 0. 072 6-1. 452 0 μg(r=0. 999 5), respectively. The aver-age recovery was 97. 24% (RSD=0. 78% ),97. 76% (RSD=1. 11% ),98. 43% (RSD=0. 93% ) and 96. 89% (RSD=0. 62% ), respectively. Conclusion The method is convenient,accurate,sensitive,reproducible and may be used in the determination of aesculin, aesculetin,baicalin and ellagic acid in Xielining tablets.
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Objective: To optimize the purification process of total coumarin from Fraxini Cortex using macroporous resin. Methods: The single factor methods have been used to investigate the choice of type, adsorption performance, and desorption performance and the purification of the total coumarin from Fraxini Cortex by macroporous resin. The adsorption rate, resolution, resolution rate, and transfer rate of the total coumarin from Fraxini Cortex, four kinds of coumarin constituents, such as aesculin, aesculetin, fraxin, and fraxetin were used as examining indexes. Results: The ADS-5 was the most suitable type for the purification of total coumarin from Fraxini Cortex among the seven kinds of macroporous resin. Adsorption parameters: Crude drug-the resin was 0.8 g/g which was the sample amount; The concentration of sample solution was 0.75 g crude drug/mL; The pH value of sample liquid was 4.0-4.3 (liquid sample); The speed of the sample through the resin column was 2-4 BV/h. Elution parameters: The volume of the water cleaning fluid impurities was 1 BV; The elution solvent was 25% ethanol; The elution speed was 2 BV/h; The elution volume was 3 BV. After the purification, the transfer rate of total coumarin from Fraxini Cortex was 74.27%, the transfer rate of four kinds of coumarin was 83.06%, the extract rate of total coumarin was 7.35%, the removal of impurities was 14.00%, among which the content of total coumarin was 54.72%, the contents of the four kinds of components were 36.01%, the total coumarin extraction yield was 4.02%. Conclusion: This method to purify the total coumarin from Fraxini Cortex using ADS-5 can get better purification effect, the purification process is also stable.
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Objective To study the preventive effect and mechanism of aesculin on intestinal mucosa in rats with experimental ulcerative colitis (UC) . Methods Forty specific-pathogen free SD rats were randomly divided into normal group, model group, salicylazosulfapyridine (SASP, 600 mg/kg) group and aesculin (EH, 100 mg/kg) group, 10 in each group. Rats in model group, SASP group and EH group were given enema with trinitrobenzene sulfonic acid ( TNBS, 100 mg/kg) for the establishment of UC model. The rats in SASP group and EH group were given gastric gavage of SASP and aesculin respectively. At the end of experiment, the serum levels of tumor necrosis factor alpha ( TNF-α) and interleukin 10 ( IL-10) were detected by enzyme-linked immunosorbent assay (ELISA) . The general state, histological features of intestinal mucosa and serum TNF-αand IL-10 levels of rats in each group were compared. Results Aesculin significantly improved the general state and relieved the inflammation of the colonic mucosa of UC rats. The disease activity index ( DAI) scores and tissue damage index (TDI) scores in the model group were significantly higher than those in the normal group ( P<0.01) . The DAI scores and TDI scores in the medication groups were significantly lower than those in the model group (P<0.01) . The serum TNF-αlevel was significantly higher and IL-10 level was significantly lower in the model group than the normal group ( P<0.01) . After treatment, TNF-α was decreased and IL-10 was increased in SASP group and EH group as compared with the model group (P<0.01) . Conclusion Aesculin has certain therapeutic effect on TNBS-induced UC in rats through significantly relieving the symptoms of UC rats. The mechanism may be related with the inhibition of TNF-α secretion and the increase of IL-10 expression, and then improving the disorder of intestinal immune function.
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Objective To study the effect of escin on proteinuria and renal function of BXSB mice. Methods BXSB mice were divided randomly into group A (control group), B (steroid treatment group), C(steroid combined with high-dose esein treatment group) and D (streroid combined with low-doze escin group). The proteinufia and renal function were detected by albustix and automatic biochemistry analyzer after a month's treatment. Results Group C reduced the level of proteinuria and parameters of renal function (BUN and Cr) significantly when compared with other three groups (P<0.05). Conclusion Escin can reduce the level of proteinuria and protect renal function of BXSB mice.
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OBJECTIVE: To study the equilibrium solubility of aesculin and its apparent oil/water partition coefficient,and to provide basis for absorption mechanism study.METHODS: Equilibrium solubility of aesculin at the pH of 1.2～8.0 was determined by saturation method.The apparent oil/water partition coefficients of aesculin were determined by shaking flask method.RESULTS: The equilibrium solubility of aesculin at the pH of 1.2～6.8 was fluctuated slightly;it increased rapidly at the pH of 7.4;the maximum equilibrium solubility of aesculin was obtained at the pH of 8.0(10.58 g?L-1).The oil/water partition coefficient of aesculin changed slowly at the pH of 1.2～6.0;it decreased significantly at the pH of 6.0;the minimum oil/water partition coefficient was obtained at the pH of 8.0(0.03).CONCLUSIONS: The equilibrium solubility of aesculin and its apparent oil/water partition coefficient are associated with the pH of medium.The reason that aesculin has no effect on uric acid after oral administration is relevant to poor gastrointestinal tract absorption ability.
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OBJECTIVE: To establish a method for the determination of aesculin and aesculetin in Jiuxiang zhixie tablets.METHODS: HPLC method was developed to quantitative determination.Thermo C18(250 mm?4.60 mm,5?m) column was adopted.The mobile phase consisted of acetonitrile-0.1%H3PO4(12 ∶ 88)with flow rate of 1.0 mL?min-1 and the detection wavelength of 334 nm.The column tempreture was set at 30℃.RESULTS: The linear range of aesculin was 80～800 ng(r=0.999 8).The average recovery was 100.1%(RSD=1.89%,n=9).The linear range of aesculetin was 32.96～329.6 ng(r=0.999 5).The average recovery of aesculetin was 101.5%(RSD=2.42%,n=9).CONCLUSION: The method is simple,accurate for the content determination of Jiuxiang zhixie tablet.
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AIM:To research the absorption mechanism of aesculin across Caco-2 monolayer model.METHODS:The Caco-2 cell monolayers drug transport model was assigned to study the double transport mechanism of aesculin to explore the absorption of aesculin according as time and drug concentration determined through HPLC and the P_ app was calcalated.RESULTS:In the Caco-2 monolayer model,the transport of aesculin form Apical to Basolateral was similar to the transport form basolateral to apical.CONCLUSION:The main mechanism of the aesculin intestinal absorption in the Caco-2 monolayer model is passive transference.
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Objective: To determine the contents of aesculin and aesculetin in periderms and leaves of Cortex Fraxini among differnet provenances. Methods: HPLC was used with acetonitrile-water(15∶85) as the mobile phase and detected wavelength at 348nm. C 18 column was adopted. Results: The calibration curves were linear. The value of correlation coefficient were 0.9992 and 0.9994, respectively. The average recovery of aesculin was 98.2% and aesculetin was 99.2%. RSD were 2.24% and 2.15%, respectively. The quality differences of Cortex Fraxini among different provenances were remarked. The quality of Cortex Fraxini from Shanxi province was the best. Conclusion: The method is applied in determination and analytics of content of Cortex Fraxini and is rapid, simple and easy to carry out. The method is with the feature of accuracy, repetition and stability.