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OBJECTIVE To investigate the effects of Forsythia suspensa ethanol extract on the proliferation， migration and invasion of lung cancer cells NCI-H226. METHODS As research objects， lung cancer cells NCI-H226 were divided into control group， F. suspensa ethanol extract low-， medium- and high-concentration groups （5， 10， 20 mg/mL）， activator group [10 mg/mL F. suspensa ethanol extract+0.5 μmol/L nuclear factor kappa B （NF-κB） signaling pathway activator PMA]， inhibitor group （10 mg/mL F. suspensa ethanol extract+10 μmol/L NF-κB signaling pathway inhibitor BAY 11-7082） and positive control group （20 μg/mL cisplatin）. Except for the control group of cells without intervention， all other groups of cells were cultured with corresponding drugs for 24 hours； the proliferation， migration and invasion of cells were all detected， and the proliferation rate， migration rate， and the number of invading cells were also calculated； protein expressions of NF-κB p65， NF-κB inhibitory protein α （IκBα）， phosphorylated NF-κB p65 （p-NF-κB p65） and phosphorylated IκBα （p-IκBα） were determined. RESULTS Compared with control group， the proliferation rate， migration rate， and the number of invading cells as well as the protein expressions of p- IκBα and p-NF-κB p65 were decreased significantly in F. suspensa ethanol extract groups and positive control group （P＜0.05）. Compared with F. suspensa ethanol extract medium-concentration group， the proliferation rate， migration rate， and the number of invading cells as well as above protein expressions were all decreased significantly in inhibitor group （P＜0.05）， while those of activator group were increased significantly （P＜0.05）. CONCLUSIONS F. suspensa ethanol extract can inhibit the proliferation， migration and invasion of lung cancer cells NCI-H226， and the mechanism of which may be related to the inhibition of NF-κB signaling pathway.
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Metabolic reprogramming is a common phenomenon in cancer, with aerobic glycolysis being one of its important characteristics. Hypoxia-inducible factor-1α (HIF1Α) is thought to play an important role in aerobic glycolysis. Meanwhile, naringin is a natural flavanone glycoside derived from grapefruits and many other citrus fruits. In this work, we identified glycolytic genes related to HIF1Α by analyzing the colon cancer database. The analysis of extracellular acidification rate and cell function verified the regulatory effects of HIF1Α overexpression on glycolysis, and the proliferation and migration of colon cancer cells. Moreover, naringin was used as an inhibitor of colon cancer cells to illustrate its effect on HIF1Α function. The results showed that the HIF1Α and enolase 2 (ENO2) levels in colon cancer tissues were highly correlated, and their high expression indicated a poor prognosis for colon cancer patients. Mechanistically, HIF1Α directly binds to the DNA promoter region and upregulates the transcription of ENO2; ectopic expression of ENO2 increased aerobic glycolysis in colon cancer cells. Most importantly, we found that the appropriate concentration of naringin inhibited the transcriptional activity of HIF1Α, which in turn decreased aerobic glycolysis in colon cancer cells. Generally, naringin reduces glycolysis in colon cancer cells by reducing the transcriptional activity of HIF1Α and the proliferation and invasion of colon cancer cells. This study helps to elucidate the relationship between colon cancer progression and glucose metabolism, and demonstrates the efficacy of naringin in the treatment of colon cancer.
Subject(s)
Humans , Glycolysis , Colonic Neoplasms/metabolism , Hypoxia-Inducible Factor 1, alpha Subunit/metabolism , Phosphopyruvate Hydratase/metabolism , Flavanones/pharmacology , Cell Line, Tumor , Databases, Genetic , Cell Proliferation/drug effects , Transfection , Warburg Effect, OncologicABSTRACT
AIM: To establish a HPLC-UV method to determine sunitinib in rat plasma and mouse tissues, and to study its pharmacokinetics in rats and tissue distribution characteristics in mice. METHODS: The biotic samples were prepared by protein precipitation followed by a stereoselective analysis of sunitinib was achieved on Waters XBridgeTM C18 (4.6 mm×250 mm, 5 μm) with a mobile phase composing of methanol-0.02 mol/L sodium dihydrogen phosphate (70:30) at a flow rate of 1.0 mL/min. The detection wavelength was 310 nm, and the column temperature was 25 ℃. RESULTS: The calibration curve for rat plasma sunitinib was linear in the range of 0.019 2-15.34 μg/mL. The linear ranges in mice brain and kidney were 0.038 3-11.50 and 0.038 3-69.00 μg/mL, respectively. After intragastric administration of sunitinib at a dose of 20 mg/kg to rats, the pharmacokinetic characteristics were Tmax=9.0 h, Cmax=0.194 mg/L, t1/2=18.4 h, AUC(0-∞)=6.8 mg•L-1•h. And the absolute bioavailablity was 47.1%. It was indicated that sunitinib could permeate the blood brain barrier, but the concentration was lower in brain and higher in kidney. CONCLUSION: A HPLC-UV method for the determination of sunitinib in rat plasma and mouse tissues was established. The method is simple, rapid, reliable, and provides a reference for the clinical application of sunitinib.
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Objective To establish a method for efficient,accurate genotyping and nucleoside drug-resistant mutation analysis for hepatitis B virus ( HBV ).Methods The 48 HBV serum samples were collected from the Third People's Hospital of Taiyuan from July to August 2011,and HBV DNA were extracted using the commercial kit.The HBV whole genome and P gene were amplified and sequenced.Each HBV sample was genotyped by both constructing phylogenetic trees and genotyping software analysis.The results from two strategies were compared for every sample.Results A total of 48 HBV full genome sequences were identified into 12 B and 36 C genotype's by both constructing phylogenetic trees and genotyping software analysis,which was exactly the same as the analysis using P gene fragment sequencing.Seven forms of nucleoside drug-resistant mutation were found in the P gene for all the samples,with the ratio of 27.1％ ( 13/48 ),in which all the mutation forms were associated with lamivudine or adefovir,and no other nucleotide drugs-related resistance mutations existed.In addition,there were 11 B and 35 C genotype and 2 B/C hybrid type with the analysis using Real-time PCR genotyping for the 48 samples.Conclusion P gene sequencing can be used as a new clinical method for efficient,accurate HBV genotyping and resistant mutation analysis,which provides guidance for hepatitis B treatment.
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Objective To investigate the effect and monitoring point of continuous veno-venous hemofil-tration (CVVH) in patients with multiple organ dysfunction syndrome (MODS). Methods In 22 patients with MODS,a double lumen catheter was put into the central vein,and the CWH was performed with the BRAUN Diapact CRRT. The level of BUN,Scr,serum potassium and arterial blood gas were measured 30 minutes before and after CVVH. The plasma TNF-α、IL-1、IL-8 were measured by ELISA. Vital signs were monitored dur-hag treatment process. Results The vital signs of all patients` was stable, the levels of BUN,Scr and serum potassium decreased significantly after CVVH. The plasma concentrations of TNF-α,IL-1 and IL-8 gradually decreased. Conclusions CWH can improve the blood biochemical markers,remove inflammatory cytokines in plasma,stsblize the vital signs during treatment,which is suitable for patients with MODS.
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[Objective]To develop an HPLC method for the determination of berberine hydrochloride in GuZheNing liniment.[Methods]The chromatographic system consisted of Dimonsil C18 column and mobile phase of acetonitrile-50mmol?L-1 sodium dihydrogen phosphate(adjusted PH to 2.5 with H3PO4)(25:75).The flow rate was 1.0 mL?min-1,and the detective wavelength was at 348 nm.[Results]The calibration curve was linear in the range of 0.106～0.530 ?g(n=5).The method was proved to be repeatable with RSD 0.7%(n=6).4 batches of sample were analyzed and the Berberine Hydrochloride contents were 19.11,18.81,18.83,18.92mg/100mg,respectively.[Conclusion]The method is selective,simple and accurate,and could be used for the quality control of this preparation.
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[Objective] To develop an HPLC method for the determination of berberine hydrochloride in GuZheNing liniment.[Methods]The chromatographic system consisted of Dimonsil C18 column and mobile phase of acetonitrile—50mmol?L-1 sodium dihydrogen phosphate(adjusted PH to 2.5 with H3PO4)(25∶75).The flow rate was 1.0 mL?min-1,and the detective wavelength was at 348 nm.[Results]The calibration curve was linear in the range of 0.106～0.530 ?g(n=5).The method was proved to be repeatable with RSD 0.7%(n=6).4 batches of sample were analyzed and the Berberine Hydrochloride contents were 19.11,18.81,18.83,18.92mg/100mg,respectively.[Conclusion]The method is selective,simple and accurate,and could be used for the quality control of this preparation.