Isolation of antibacterial activity constituents of total flavonoids from sophora flavescens and simultaneous determination of seven flavonoids by HPLC / 中国药学杂志

OBJECTIVE: To study the chemical constituents of the total flavonoids from Sophora flavescens and establish a method for simultaneous determination of seven compounds. METHODS: The compounds were isolated by chromatography on silica gel and ODS column and their structures were elucidated by spectroscopic analysis. The samples were analyzed on a Dikma C18 column (4.6 mm × 250 mm, 5 μm) ; gradient elution was performed using mobile phase composed of methanol (A) and water (B); the detection was carried out using a photodiode array detector at 280 nm. RESULTS: Seven compounds were isolated and their structures were identified as kuratidine (1), sophoraflavanone G (2), kurarinone (3), isoanhydroicaritin (4), isoxanthohumol (5), formononetin (6), and trifolirhizin (7). The calibration curve was linear within 8.70-87.00, 44.25-442.50, 128.10-1 281.00, 9.40-94.00, 48.40-484.00, 14.20-142.00, and 25.70-257.00 μg·mL-1 for kuraridine, sophoraflavanone G, kurarinone, isoanhydroicaritin, isoxanthohumol, formononetin, and trifolirhizin, respectively (r > 0.999 0), and the extraction recoveries varied from 95% to 105%. CONCLUSION: The main chemical components contributing to antibacterial activity of total flavonoids may be sophoraflavanone G, kurarinone, and isoxanthohumol. The method is simple, rapid, accurate, and can be used simultaneously to determine the contents of the seven active ingredients.

Kurarinone promotes TRAIL-induced apoptosis by inhibiting NF-kappaB-dependent cFLIP expression in HeLa cells

This study was designed to investigate the effects of the prenylated flavonoid kurarinone on TNF-related apoptosis inducing ligand (TRAIL)-induced apoptosis and its underlying mechanism. A low dose of kurarinone had no significant effect on apoptosis, but this compound markedly promoted tumor cell death through elevation of Bid cleavage, cytochrome c release and caspase activation in HeLa cells treated with TRAIL. Caspase inhibitors inhibited kurarinone-mediated cell death, which indicates that the cytotoxic effect of this compound is mediated by caspase-dependent apoptosis. The cytotoxic effect of kurarinone was not associated with expression levels of Bcl-2 and IAP family proteins, such as Bcl-2, Bcl-xL, Bid, Bad, Bax, XIAP, cIAP-1 and cIAP-2. In addition, this compound did not regulate the death-inducing receptors DR4 and DR5. On the other hand, kurarinone significantly inhibited TRAIL-induced IKK activation, IkappaB degradation and nuclear translocation of NF-kappaB, as well as effectively suppressed cellular FLICE-inhibitory protein long form (cFLIPL) expression. The synergistic effects of kurarinone on TRAIL-induced apoptosis were mimicked when kurarinone was replaced by the NF-kappaB inhibitor withaferin A or following siRNA-mediated knockdown of cFLIPL. Moreover, cFLIP overexpression effectively antagonized kurarinone-mediated TRAIL sensitization. These data suggest that kurarinone sensitizes TRAIL-induced tumor cell apoptosis via suppression of NF-kappaB-dependent cFLIP expression, indicating that this compound can be used as an anti-tumor agent in combination with TRAIL.

Clinical observation of Pre-S1 antigens in interferon combination with kurarinone therapy / 中国基层医药

Objective To observe the clinical significance and laboratory diagnostic values of Pre-S1 antigens (Pre-S1)and its relativity to HBeAg and HBV-DNA after using interferon in association with kurarinone.Methods The content of Pre-S1 and HBV-M was detected by ELISA and the levels of HBV-DNA were detected by flores- cence quantitative PCR(FQ-PCR)in 100 serum samples of patients with HBV infection and patients after an antivi- ral treatment.Results Matched control in 50 serum of HBsAg-positive and detectable HBV-DNA cases,both 29 samples in 30 HBeAg-positive cases and 17 samples in 20 HBeAg-negative cases Pre-S1s were positive.Treatment set 50 serum of patients after taking two courses of an antiviral treatment for HBV infection,drawing blood to observe related markers,5 cases of effect set were turned into negative for serologic markers and virologic markers.19 cases of valid set,serologic markers were various and the HBV-DNA copies descended 2-3 orders of magnitude.26 cases of invalid set,serologic markers were not various,and 30 % samples of the HBV-DNA copies descended 1～2 orders of magnitude.Conclusion It was supplementary for Pre-S1 to indicate HBV expression when the HBeAg varied.It also provided detcctable laboratory markers in HBV infectivity,replication and therapeutic efficiency evaluation.

Clinical Effect of Combination of Kurarinone and Thymosin ?_1 on Patients with Chronic Hepatitis B / 医学研究杂志

Objective To study the clinical effect of combination of kurarinone and thymosin ?_1 for injection in treating chronic hepatitis B.Method One hundred and fifty-six patients with chronic hepatitis B were randomized into two groups,additional KR combined thymosin ?_1 for injection was given to treated group,and KR to control group.The therapeutic course for them was 6 months.We compared the serum ALT、 hepatitis B virological markers、T lymphocyte response before and 6 months after treatment.Results After treatment,the results showed that the levels of CD_3+、CD_4+、CD_4+/CD_8+ T cell in CHB patients of treatment were much higher than control groupnt.The ratio HBeAg and HBV-DNA loss were increased,the difference was significant(P

HPLC Determination of Contents of Four Flavonoids in Different Samples of Sophora flavescens Ait.in the Market / 中药新药与临床药理

Objective To determine the contents of four fiavonoids(trifolirhizin,nor-kurarinone,xanthonumal and kuraridin)in 25 samples of Sophora flavescens Air.in the market.Methods The determination was carried out on Phe- nomenex Luna C_(18)column(250 mm?4.6 mm,5?m),using Acetonitrile-H_2O as mobile phase,at a flow rate of 1.0 mL/min and detected at the wavelength of 310 nm for trifolirhizin,294 nm for nor-kurarinone and,365 nm for xan- thonumal and kuraridin,and column temperature at 35℃.Results The contents of 4 flavonoids in 25 samples of Sophora flavescens Air.in market were in the ranges of 0.05 %～0.32 % for trifolirhizin,0.05 %～0.51% for nor- kurarinone,0.55?10~(-3)%～4.87?10~(-3)% for xanthonumal and 0.06 %～0.23 % for kuraridin.Conclusion The contents of 4 flavonoids in the samples from the market vary notably,and this should be taken into the quality control of Sophora flavescens Ait.