Abstract The paper presents a modified and universally applicable diagnostic fragment‐ion‐based extension strategy (DFIBES) to efficiently process the information acquired by liquid chromatography‐electrospray ionization source in combination with hybrid ion trap high‐resolution time‐of‐flight mass spectrometry [LC‐(ESI)‐IT‐TOF/MS], facilitating structural determination of serial components contained traditional Chinese medicine prescription (TCMP). key advantage DFIBES is that it...

Resveratrol (Resv) has antitumorigenic and antimetastatic activities; however, the molecular mechanisms underlying inhibitory effects of Resv on invasion metastasis breast cancer cells are still a subject debate. In our study, we demonstrated that inhibited tumor cell proliferation growth. It also suppressed pulmonary by reversing transforming growth factor beta 1 (TGF-β1)-mediated EMT process. Meanwhile, anticarcinogenic were abolished autophagy blocker 3-methyladenine (3-MA) or Beclin...

ABSTRACT Aberrant activation of the RAS/RAF/MEK/ERK pathway occurs in more than 30% human cancers. As part this pathway, MEK1/2 has crucial roles tumorigenesis, cell proliferation, and inhibition apoptosis. At present, a number inhibitors are approved for treatment melanoma. However, have poor single‐drug efficacy solid tumors prone to drug resistance. A series compounds containing diarylamine skeleton phenylacrylamide (acrylamide) been designed synthesized paper. The most promising compound...

Non-small cell lung cancer (NSCLC) is the leading cause of morbidity and mortality worldwide. The prognosis patients has been significantly improved by chemotherapy, but acquired drug resistance remains a major obstacle to NSCLC treatment. Circular RNAs (circRNAs), which act as miRNA or protein sponges, are critically associated with development chemotherapy NSCLC. CircRNA sequencing was performed analyze differential expression circRNAs between A549 A549-GR cells. Chromogenic in situ...

The therapeutic use of glimepiride and gliclazide shows substantial inter-individual variation in pharmacokinetics pharmacodynamics human populations, which might be caused by genetic differences among individuals. aim this study was to assess the effect CYP2C9 OATP1B1 polymorphisms on metabolism transport gliclazide. uptake measured OATP1B1*1a, *5 *15-HEK293T cells, their using CYP2C9*1, *2 *3 recombinase LC-MS. Glimepiride cells had Vmax values 155 ± 18.7, 80 9.6, 84.5 8.2 pmol/min/mg,...

Hesperetin (HET) and naringenin (NGR) are flavanones found in citrus (oranges grapefruit) Aurantii Fructus Immaturus. The present study aims to investigate the inhibition potential of HET NGR derivatives towards one most important phase II drug-metabolizing enzymes-uridine diphosphate (UDP)-glucuronosyltransferases (UGTs). We used trifluoperazine as a probe substrate test UGT1A4 activity, recombinant UGT-catalyzed 4-methylumbelliferone glucuronidation was reaction for other UGT isoforms....

Shenmai injection (SMI), a mixture of Radix Ginseng and Ophiopogonis, is one the most popular herbal medicinal products widely used for treatment coronary atherosclerotic cardiopathy viral myocarditis. The purpose this study was to investigate effect SMI, in vivo vitro, on metabolic activities hepatic cytochrome CYP450 3A1/2, 2C6, 2E1, 1A2 rats. After single or multiple pretreatment with rats were administrated intravenously cocktail containing midazolam (1 mg/kg), diclofenac (0.5...

Sulfonylureas (SUs) such as glibenclamide, gliclazide, glimepiride, glipizide and gliquidone are one of the first oral medicines available for treatment type 2 diabetes widely used hyperglycaemia. The hepatic transporters, organic anion transporting polypeptide 1B1 (OATP1B1) 1B3 (OATP1B3), play an important role in disposition a variety drugs by mediating their uptake from blood into hepatocytes. Drug-drug interactions mediated OATP1B1/1B3 may result change drug substrates. inhibitory...

Hepatocellular carcinoma (HCC) is a type of liver cancer and leading cause cancer‑associated mortality. In China, ~466,000 patients are diagnosed with HCC it responsible for ~422,000 cases mortality each year. Surgery the most effective treatment available; however only suitable early‑stage HCC. Chemotherapy has been confirmed as necessary advanced HCC, although drug resistance may limit its clinical outcome. Low intensity ultrasound (LIUS) represents novel therapeutic approach to treat HCC;...

Shenmai injection (SMI) is derived from traditional Chinese herbal prescription Shendong yin and widely used for treating cardiovascular diseases. Ophiopogonin D (OPD) one of the main active components SMI. The hepatic uptake OPD mediated by organic anion-transporting polypeptides (OATPs/oatps) inhibited some other in This study aimed to identify SMI responsible inhibitory effects on rats explore compatibility mechanisms complex based OATPs/oatps. known effective fractions, Formula,...

A sensitive and specific liquid chromatography-electrospray ionization-mass spectrometry method for the identification quantification of pentoxyverine citrate guaifenesin in human plasma has been developed. After extraction from samples by ethyl acetate, internal standard analytes were separated high-performance chromatographic on a Shim-pack VP-ODS C(18) column (150 x 2.0 mm) using mobile phase consisting (methanol) B (0.4% glacial acetic acid 4 mmol/L ammonium acetate) (A:B, 43 : 57)....

Shenmai injection (SMI) is a popular herbal preparation that widely used for the treatment of atherosclerotic coronary heart disease and viral myocarditis. In our previous study, SMI was shown to differentially affect CYP3A4-mediated 1′-hydroxylation 4-hydroxylation midazolam (MDZ). The present study conducted identify active components in responsible differential effects on MDZ metabolism, using vitro incubation systems (rat human liver microsomes recombinant CYP3A4 system) measure MDZ....

Background: Oleanolic acid (OA) and its isomer ursolic (UA) have recently emerged as research foci based on their biologic activities. We previously demonstrated that UA can inhibit the activities of UGT1A3 UGT1A4, OA inhibits activity in liver microsomes. However, whether affect expression UGT1As HepG2 cells underlying regulatory mechanism remain unclear. Purpose: The present study aimed to explore effect mechanisms UGT1A1 pregnane X receptor (PXR) constitutive androstane (CAR) signaling...

Radix Ophiopogonis is often an integral part of many traditional Chinese formulas, such as Shenmai injection used to treat cardio-cerebrovascular diseases. This study aimed investigate the influence four active components on transport activity OATP1B1 and OATP1B3. The uptake rosuvastatin in OATP1B1-HEK293T cells were stimulated by methylophiopogonanone A (MA) ophiopogonin D' (OPD') with EC50 calculated be 11.33 ± 2.78 4.62 0.64 μM, respectively. However, there no remarkable influences...