Correlation between drug-induced liver injury in rats caused by Xianling Gubao oral preparation and extraction process / 中国中药杂志

In light of the liver injury risk associated with the oral administration of Xianlin Gubao oral preparation, this study compared the differences in liver injury induced by two different extraction processes in rats and explored the correlation between hepatotoxicity and extraction process from the perspective of the differences in the content of the relevant components. Thirty male Sprague-Dawley(SD) rats were randomly divided into a normal group, tablet extract groups of different doses, and capsule extract groups of different doses, with 6 rats in each group. Each group received continuous oral administration for 4 weeks. The assessment of liver injury caused by different extracts was conducted by examining rat body weight, liver function blood biochemical indicators, liver coefficient, and liver pathological changes. In addition, a high-performance liquid chromatography(HPLC) method was established to simultaneously determine the content of icariin, baohuoside I, and bakuchiol in the extracts to compare the differences in the content of these three components under the two extraction processes. The results showed that both extracts caused liver injury in rats. Compared with the normal group, the tablet extract groups, at the studied dose, led to slow growth in body weight, a significant increase in triglyceride levels(P<0.05), a significant decrease in liver-to-brain ratio(P<0.05), and the appearance of hepatic steatosis. The capsule extract groups, at the studied dose, resulted in slow growth in body weight, a significant increase in aspartate aminotransferase levels(P<0.05), a significant decrease in body weight, liver weight, and liver-to-brain ratio(P<0.05), and the presence of hepatic steatosis and inflammatory cell infiltration. In comparison, the capsule extraction process had a higher risk of liver injury. Furthermore, based on the completion of the liquid chromatography method, the content of icariin and baohuoside Ⅰ in the capsule extract groups was 0.83 and 0.81 times that in the tablet extract groups, respectively, while the bakuchiol content in the capsule extract group was 29.80 times that in the tablet extract groups, suggesting that the higher risk of liver injury associated with the capsule extraction process may be due to its higher bakuchiol content. In summary, the differences in rat liver injury caused by the two extracts are closely related to the extraction process. This should be taken into consideration in the formulation production and clinical application.

Effects and mechanism of epimedium polysaccharide on solubility of icariin and baohuoside Ⅰ / 中国中药杂志

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.

HPLC characteristic chromatograms and quantitative analysis of Kunxian Capsules / 中草药

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.

Effect of processing excipient suet oil on formation and absorption of baohuoside Ⅰ-bile salt self-assembled micelles / 中国中药杂志

The fried method with suet oil,which can strengthen the effect of Epimedium in warming kidney and enhancing Yang,has been widely used in the processing of Epimedium in traditional Chinese medicine. Based on the formation mechanism of Epimedium flavonoids self-assembled micelles in vivo,the synergistic mechanism of processing excipient suet oil was investigated in this paper from the perspective of pharmaceutics. Baohuoside Ⅰ,as representative component of processed Epimedium,was selected as model drug.Average size and zeta potential were measured and the morphology of micelles was observed under transmission electron microscopy. Caco-2 monolayer cell model,rat intestinal perfusion model and in vivo serum drug concentration method were established to investigate the effect of suet oil on the formation and absorption of the baohuosideⅠ bile salt self-assembled micelles. Baohuoside Ⅰ can form selfassembled micelles under the action of sodium deoxycholate. While,adding suet oil into the baohuoside Ⅰ-bile salt micelles( BSDOC) can make it form a more stable system with a smaller average size,higher Zeta potential,lower polydispersity index( PDI) value,significantly improved encapsulation efficiency and drug loading,indicating that suet oil could significantly improve the micelle formation in vivo. In addition,the permeability coefficient of baohuoside Ⅰ in Caco-2 monolayer cells and the four intestinal organs( duodenum,jejunum,ileum and colon) was increased and the oral bioavailability was also improved after adding the suet oil to BS-DOC.All the results demonstrated that the suet oil can promote the formation and absorption of baohuoside Ⅰ self-assembled micelles,so as to enhance its synergistic effects.

Preparation method and pharmacological effect of baohuoside Ⅰ / 中国中药杂志

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.

Rapidly-identification of anti-inflammation candidates targeting Nuclear Receptor Retinoid X receptor-α from Epimedium brevicornum Maxim / 国际检验医学杂志

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 .

Determination of Psoralen, Isopsoralen, Icariin and BaohuosideⅠin Shengrong Yanling Pill by HPLC Elution Method / 中国中医药信息杂志

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.

Effect of baohuoside-Ⅰ on proliferation and cell cycle of human esophageal carcinoma cell Eca-109 / 中草药

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