0, 999. Determing whether the d-or 1-isomer of MP are present in urine will helpdetermint the source of MP. In this case,the concentration of d-MP is about 11 and 10 times higherthan 1-MP in urine and liver, respectively. The results suggest that the person from whom thesamples were obtained probably had aceess to MP from an illicit source.

Gastrodin (GAS) is the major bioactive component of the extracts from the rhizome of Gastrodia elata Blume. The aim of this study is to investigate the transport of GAS in Caco-2 cells and the interaction of P-glycoprotein and GAS. The apparent permeability coefficients (Papp) of GAS were measured as a function of directions and concentrations. It was demonstrated that the efflux ratio was < 2.0 over the range of 50-500 micromol x L(-1) of GAS from bi-directional transport studies. The transport rate of GAS was dependent on the concentrations. Papp of GAS was not affected by transport directions, GAS concentration or the classical inhibitors of P-glycoprotein (verapamil and GF 120918). The cellular accumulation of GAS in Bcap37/MDR1 cells transected with hMDR1 gene, was similar to that in Bcap37 cells. The accumulation in both cell lines was concentration dependent. GAS did not affect the accumulation of Rhodamine 123 in Bcap37/MDR1 cells over the range of 50-500 micromol x L(-1). It indicated that the transport of GAS in Caco-2 cell monolayers mainly is by passive paracellular transport pathway. P-glycoprotein did not participate in the absorption of GAS in the intestine or the transport across the blood-brain barrier.

Objective To summarize the nursing strategies for the patients with anti-neutrophil cytoplasmic antibody associated with vasculitis and renal damage.Methods The nursing histories of 10 patients with anti-neutrophil cytoplasmic antibody associated with vasculitis and renal damage were retrospectively analyzed to summarize the nursing strategies.Results Nine of them were discharged after improvement. Seven of them had marked decrease in serum creatinine, 2 survived by hemodialysis at the outpatient section and 1 died of severe pulmonary infection.Conclusion Such strategies as close observation of patients, prevention of complications and mental care are important for the curative effect and nursing quality for the patients with anti-neutrophil cytoplasmic antibody associated with vasculitis and renal damage.

AIM To express recombinant human cytochrome P450 3A4 mutants CYP3A4.3, CYP3A4.4, CYP3A4.5 and CYP3A4.18, and to employ them for in vitro metabolism studies of CYP3A4. METHODS Use Bac-to-Bac baculovirus expression system to recombinant baculovirus carrying cDNA of CYP3A4 mutants CYP3A4.3, CYP3A4.4, CYP3A4.5 and CYP3A4.18. Spodoptera frugiperda 9 (Sf9), cells were co-infected by recombinant viruses of CYP3A4 mutants, human NADPH-P450 oxidoreductase and cytochrome b5 to obtain recombinant proteins CYP3A4.3, CYP3A4.4, CYP3A4.5 and CYP3A4.18 with metabolic activity. RESULTS The mRNA transcription of CYP3A4 mutants in Sf9 cells were validated by RT-PCR. Testosterone and 7-benzyloxy-4-(trifluoromethyl) coumarin were metabolized by the lysates of Sf9 cells infected by the recombinant viruses. CONCLUSION CYP3A4 mutants CYP3A4.3, CYP3A4.4, CYP3A4.5 and CYP3A4.18 with metabolic activity were successfully expressed by baculovirus-insect cell expression system. The results indicated that recombinant CYP3A4. 5 showed lower activity comparing to the wild type protein towards testosterone, while CYP3A4. 18 with higher activity, and for CYP3A4.3 and CYP3A4.4 showing similar activity to the wild type protein.

Zebrafish is widely used as a model organism in the process of drug discovery. It expresses drug metabolizing enzymes like cytochrome P450 (CYP450), uridine 5'-diphospho-glucuronosyltransferase (UGT) and nuclear receptors like pregnane X receptor (PXR), aryl hydrocarbon receptor (AHR), etc. This article summarized the profiles of main drug metabolizing enzymes and nuclear receptors, and reviewed the advances on xenobiotics metabolism in zebrafish.

Humans ; Inactivation, Metabolic ; Pharmaceutical Preparations ; metabolism

Objective To provide a technique of preparation recombinant hALR by gene engineering in larger scale.Methods Construct hALR(human augmenter of liver regeneration) protein expression vector pGEX-3X-hALR,induce the expreesion of hALR,and pruified the protein by affinity chromatography.Results Succeed in constructing the vector pGEX-3X-hALR and obtained the recombinant hALR protein.Conclusion The mothed could be used for preparation recombinant hALR by gene engineering in larger scale.

The chemical constituents of the marine sponge Haliclona sp. collected from the South China Sea have been studied. An alkanoid 1 and an aryl acid 2 were isolated from the marine sponge and the structure of 1 and 2 were respectively elucidated as 1,3 -dimethylxanthine and p - hydroxybenzoic acid by spectroscopic analysis and elemental analysis.

Objective To investigate the effect of Hydroxychloroquine plus Leflunomide on the lipid profile and disease activity index in patients with rheumatoid arthritis (RA).Methods A total of 140 elderly patients with RA who met the American College of Rheumatology (ACR) criteria were treated with Hydroxychloroquine (Group A,n =70) or leflunomide combined with hydroxychloroquine (Group B,n=70),and 100 healthy volunteers were selected as controls.The lipid profile was compared between the patient groups and control group.Lipid levels,Disease Activity Score 28 (DAS28),erythrocyte sedimentation rate (ESR) and C-reactive protein (CRP) were measured before treatment and 6 months after treatment between Group A and Group B.Results Compared with the control group,RA patients exhibited higher levels of total cholesterol (TC,P＜0.05),low-density lipoprotein cholesterol (LDL-C,P＜0.05) and triglycerides (TG,P＜0.01),and lower levels of high-density lipoprotein cholesterol (HDL-C,P＜0.05).After 6 months of treatment,the disease activity index (DAS28,P＜0.01),the duration of morning stiffness (P＜0.01),ESR,CRP,swollen joint count (SJC) and tender joint count (TJC) decreased in RA patients,compared with controls (P＜0.01 or 0.05).HDL-C levels increased and LDL-C levels decreased in Groups A and B after treatment,compared with pretreatment (P＜0.05 for all).After treatment,TC levels decreased in Group B,compared with Group A (P＜ 0.05),while TG levels had no significant difference between the two groups (P＞0.05).TC and LDL-C levels,ESR,CRP,DAS28,SJC and TJC were lower in Group B than in Group A (all P＜0.05).Conclusions Hydroxychloroquine in combination with Leflunomide therapy can not only control inflammation but also improve the lipid profile,and is more effective than single-drug therapy.The combination may reduce the risk of atherosclerosis and cardiovascular events in patients with RA.

Verification of scientific literature novelty assessment is the final step in writing the literature novelty assessment report and is closely related with its academic level.The key points in verifying novelty assessment of medical literature were thus analyzed with examples in this paper, including the scientific and technical points, literature novelty assessment points, retrieval terms, retrieval strategies, and conclusion of literature novelty assessment.