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Aim To explore the inhibitory effect of hawthorn leaves flavonoids (HLF) on human glioblastoma U87 cells. Methods U87 cells were cultured in vitro. The concentration of HLF was 25, 50, 100 mg . L¹ as drug concentration. The effects of HLF on the proliferation, migration, invasion and adhesion of U87 cells were detected by CCK-8 assay, scratch assay, Transwell assay and adhesion assay, and clone forming ability was detected by cell clonogenic assay. Results HLF inhibited the proliferation, migration, invasion and adhesion of U87 cells in a concentration-dependent manner, and the difference was statistically significant compared with control group (P < 0. 05). When HLF reached 50 mg . L¹ the inhibition of tumor growth was the most significant. Conclusion HLF has a certain inhibitory effect on glioma U87 cells.
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Objective To study the equilibrium solubility and oil/water partition coefficient of Hawthorn leaves flavonoids (HLF) components, and compare their similarity, to lay the foundation for the characterization of the overall water soluble and fat soluble HLF components. Methods Taking HLF components as model drug, rutin, quercetin, and hyperin as representative components. The HPLC method was used to determine the equilibrium solubility and apparent oil/water distribution coefficient (Papp) of the components at different pH values and water. The similarity was evaluated by the vector cosine method (cosines) and Grubbs method (Grubbs). Chromatographic conditions: The chromatographic column was Zorbax Eclipse Plus C18 column (250 mm × 4.6 mm, 5 μm), and the flow phase was acetonitrile (A) - 0.4% phosphate solution (B). The gradient elution program was 0—10 min (80% B), 10—11 min (80%—60% B), 11—20 min (60% B), 20—21 min (60%—80% B), and 21—25 min (80% B); The detection wavelength was 360 nm; The volume flow was 0.8 mL/min; The column temperature was 40 ℃. Results The equilibrium solubility and Papp of rutin, quercetin, hyperin were similar in different pH buffer solution and water. The solubility value of lutin, quercetin, and hyperoside in thebuffer solution of different pH were 0.998, 0.988, and 0.987, respectively. The cosine value of the apparent oil-water distribution coefficient was 0.976, 0.981, and 0.978, respectively. The cosine value was greater than 0.9. The Grubbs value of equilibrium solubility of lutin, quercetin and hyperoside were 1.057, 1.083, 1.124, 1.117, 1.022, 1.030, 1.082, and 1.112, respectively. The Grubbs values of the apparent oil-water distribution coefficient were 1.125, 1.107, 1.079, 1.034, 1.041, 1.037, 1.129, and 1.128. The results of Grubbs were less than G critical value of 1.153, and the similarity was good. Conclusion The similarity analysis reflects that the degree of dispersion of components objectively, which could increase the science of components evaluation and provide the basis for the formulation design of components of traditional Chinese medicine.
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0.05).But the P_ eff values were significantly increased in the presence of P-glycoportein(P-gp)inhibitor,verapamil or digoxin.CONCLUSION:Rhamnosylvitexin can be classified into high penetrating drug.Passive diffusion dominates the absorptive transport behavior of rhamnosylvitexin in HLF.There is not a preferential absorption zone in the intestine for rhamnosylvitexin.The absorption and secretion of rhamnosylvitexin in HLF are mediated by the efflux transport system,P-gp.