ABSTRACT
This study evaluated the effects of epimedium polysaccharide(EPS) on the solubility of icariin and baohuoside Ⅰ so as to preliminary explore its solubilization function and the underlying mechanism. The solubility of these two insoluble flavonoids in water and polysaccharide solutions was compared by high performance liquid chromatography, and the mechanism was investigated by diffe-rential scanning calorimetry(DSC) and critical micelle concentration determination. The results indicated that their solubilization in crude EPS solutions was concentration-dependent. The solubility of icariin and baohuoside Ⅰ in 20 mg·mL~(-1) EPS-1-1 was 9.05 times and 5.76 times that in water, respectively; while their solubility in 20 mg·mL~(-1) EPS-2-1 was 10.55 and 8.39 times that in water, respectively. The change of the DSC thermograms suggested the formation of new complexes from icariin and baohuoside Ⅰ with polysaccharides. The critical micelle concentrations proved the micellar properties of both EPS-1-1 and EPS-2-1. In short, EPS can significantly increase the solubility of icariin and baohuoside Ⅰ, the mechanism of which may be related to the formation of micellar complexes between EPS and insoluble flavonoids.
Subject(s)
Epimedium , Flavonoids , Polysaccharides , SolubilityABSTRACT
Objective: In order to provide a scientific basis for the quality control of Kunxian Capsules (KC), HPLC characteristics chromatogram combined with multi-components determination was established. Methods: The analysis was performed on Agilent Zorbax SB-C18 column (250 mm × 4.6 mm, 5 μm), using acetonitrile and 0.1% phosphoric acid solution as the mobile phase at a flow rate of 0.8 mL/min for gradient elution, the column temperature was 33 ℃, and the detection wavelength was 270 nm. The fingerprints of 15 batches of KC were established and evaluated by the similarity evaluation system of TCM (2012A version), hierarchical cluster analysis and discriminant analysis of partial least squares. Furthermore, the content of hyperoside, epimedin A, epimedin B, epimedin C, icariin and baohuoside Ⅰ were determined. Results: The HPLC fingerprint with 21 common peaks of KC was established, and the similarities of samples were over 0.9. The linearity relationships separated with hyperoside, epimedin A, epimedin B, epimedin C, icariin and baohuoside Ⅰ were good, and the contents of the above-mentioned components in 15 batches of preparations were 2.817-7.527, 7.287-9.103, 8.730-18.675, 33.377-70.371, 35.297-50.291 and 4.059-9.079 mg/g, respectively. Conclusion: The combination methods of HPLC characteristic chromatograms and simultaneous determinations of multiple components are rapid, simple and reproducible, which can provide methodological reference for the quality control of KC.
ABSTRACT
Epimedii Folium, a famous traditional Chinese medicine made of dried leaves of Epimedium brevicomu, E. pubescens, E. sagittatum or E. koreanum, has been applied in China for several thousand years as a medicine. It has the function of reinforcing kidney Yang, strengthening muscles and bones and dispelling rheumatism. Modern studies have shown that baohuoside Ⅰ has a low content in Herba Epimedii, but it has a wide range of pharmacological effects, such as anti-osteoporosis, anti-tumor, improving cognitive dysfunction, cerebral ischemia-reperfusion injury protection, and neuroprotection. More and more attention has been paid to the preparation methods and pharmacological effects of baohuoside Ⅰ due to its many biological activities and pharmacological effects. In this present research, in order to provide references for the better mass preparation and rational exploitation of baohuoside Ⅰ, we summarized and sorted out the preparation methods and pharmacological effects of baohuoside Ⅰ which were published in recent years.
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Objective To establish a method that can accurately and efficiently screen potential pharmaceutical agents targeting Nuclear Receptor Retinoid X receptor-α (RXRα) from Traditional Chinese Medicine .Methods Based on the principle of Receptor-Ligand Recognition ,the fusion protein of His-RXRαLBD and the active fractions were mixed to incubate for capturing and identif-ying potential ligand of RXRα,and then the identified ligand was evaluated for RXRα-dependent anti-inflammation effect .Results Baohuoside Ⅰ from Epimedium brevicornum Maxim .was identified as a RXRα binder ,and could induce RXRα-dependent anti-in-flammation effect .Conclusion The method was an efficient strategy to accurately identify active compounds from natural products , to expedite the discovery of natural RXRαregulator ,and also to share the thought with other receptors in identifying ligand .
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Objective To develop an HPLC method for determination of the contents of psoralen, isopsoralen, icariin and baohuosideⅠin Shengrong Yanling Pill. Methods Hypersil C18 column was used as the chromatographic column, with gradient elution, the flow rate of 1.1 mL/min, the mobile phase A of acetonitrile-methanol (2∶1), the mobile phase B of 0.1% glacial acetic acid solution, and detection wavelength of 246 nm (for psoralen and isopsoralen) and 270 nm (for icariin and baohuoside Ⅰ). Results There was a good linear relationship between the injection volume and peak area valued when the volume of psoralen, isopsoralen, icariin and baohuosideⅠwere within the range of 0.033 2-0.664 0 μg (r=0.999 8), 0.022 6-0.452 0 μg (r=0.999 1), 0.029 4-0.588 0 μg (r=0.999 5), and 0.024 2-0.484 0 μg (r=0.999 4), respectively. The average recovery rates were 97.48% (RSD=0.92%), 98.44% (RSD=1.39%), 99.13% (RSD=1.17%) and 98.71% (RSD=1.21%), respectively. Conclusion The method was convenient, accurate, sensitive and repeatable, and could be used in the content control method of psoralen, isopsoralen, icariin and baohuosideⅠin Shengrong Yanling Pill.
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Objective Effect of baohuoside-Ⅰ from Cortex Periplocae on cell cycle of human esophageal carcinoma cell Eca-109 and its mechanism were studied.Methods After treatment with baohuoside-Ⅰ at different concentration(12.5,25,and 50 ?g/mL)for 24,48,and 72 h,the inhibitory effect on proliferation of Eca-109 cells was analyzed by MTT method.After treatment with baohuoside-Ⅰ under different concentration(12.5,25,and 50 ?g/mL)for 48 h,cell cycle of Eca-109 cells were measured with flow cytometry(FCM);The expression of Cyclin B1 mRNA was detected by RT-PCR technique.The expression of Cyclin B1 protein was detected by Western blotting.Results Baohuoside-Ⅰ of 25 and 50 ?g/mL inhibited the proliferation of Eca-109 cells significantly in an effect-concentration manner(P