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Aim To investigate the absorption of thalidomide in inflammatory bowel disease(IBD)SD rats compared with healthy rats to provide a basis for the safety and efficacy of thalidomide in clinical practice. Method The IBD rat model was induced by the 2, 4, 6-trinitrobenzene sulfonic acid, by which the rats were continuously intervened for six days. The general state and disease activity index of the rats were recorded every day. The rats in IBD group after modeling and control group were administered with thalidomide at a dose of 10 mg·kg-1. The blood sample of the rats was collected at different time points. After a comprehensive evaluation of morphological and histopathological results, the samples of rats with IBD were determined by proven high performance liquid chromatography-mass spectrometry,and the pharmacokinetic parameters were calculated and compared with the healthy rats. Results The body weight of rats in IBD group was obviously lower than that in control group and the disease activity index, score of colonic macroscopic morphous and histopathology were obviously higher than those in control group. The success rate of modeling was 62.5%. The pharmacokinetic results showed that the Cmax(P<0.05)and AUC(P<0.01)of the IBD group both increased by 2 to 3 times, but there was no significant difference in t1/2,Tmax,MRT and other parameters. Conclusions The rate and extent of oral thalidomide absorption of rats in the model of inflammatory bowel disease significantly increase compared to those of healthy rats, which may provide new considerations for clinical practice of thalidomide in the treatment of IBD.
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Mulberroside, a glycosylated stilbene, is the main bioactive constituent of white mulberry root-bark ( Sangbaipi) . It is widely used in many famous traditional Chinese medicine pre-scriptions to treat gout, arthritis, and rheumatism through pur-ging diuresis and relieving edema. In recent years, the pharma-cological activity of mulberroside has drawn extensive attention. With the utilization of the techniques and methods of modern pharmacology, a variety of biological activity and pharmacologi-cal effects of mulberroside are discovered gradually. The recent progress in the research on pharmacological effects of mulberro-side was reviewed in this paper to provide reference for the fur-ther development and comprehensive utilization.
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P-glycoprotein (P-gp), an ATP binding cassette protein, plays a major role in efflux transport of drugs and xenobiotics due to its abundant expression on several barriers. This study aimed to investigate the potential role of PKC/NF-κB-PXR signaling pathway in modulation of P-gp gene expression in human colon adenocarcinoma LS174T. The effect of PMA on MDR1 luciferase activity was investigated by PXR-MDR1 dual luciferase reporter gene assay. Real-time qPCR assay and Western blot analysis were used to study the gene expression of P-gp and NF-κB, respectively. Compared to the vehicle-treated group, PMA statistically decreased P-gp luciferase activity, mRNA expression and protein expression. Moreover, PMA treatment yielded a significant and dose-dependent increase in RelA/p65 translocation to nucleus. Meanwhile, a remarkable increase of the pho-IκBα status was observed in LS174T cells after treatment with PMA (1-100 nmol·L-1). In addition, knockdown of PKCα, NF-κB or PXR can significantly attenuate PMA-induced P-gp suppression.These results suggested that PKC/NF-κB-PXR signaling pathway might play crucial roles in modulation of P-gp gene expression.
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Objective To study the bioavailability and bioequivalence of erythromycin ethylsuccinate granules in healthy male volunteers.Methods In a randomized two-period crossover study,20 healthy male volunteers received single 500 mg test and reference formulations of erythromyein ethylsuccinate granules.The plasma concentrations of erythromycin were assayed by microbiological method.Results The parameters of test and reference preparations were as follows:T_(max)(0.86?0.22)and (0.80?0.13)h,C_(max)(2.13?0.64)and(2.16?0.61)mg/L,t_(1/2)(2.04?0.2)and(1.97?0.4)h,AUC_(0-t)(4.96?1.73)and(4.63?1.52)mg?h/L,respectively.There was no significant difference between the two preparations.The rela- tive bioavailahility of the test granules was(109.1?22.8)%.Conclusions The two preparations of erythromycin ethylsucci- nate granules are bioequivalent.
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<p><b>OBJECTIVE</b>To study the clinical pathological features and immunophenotype of follicular dendritic cell sarcoma (FDCS) with discussion on its diagnostic clues to improve diagnostic level.</p><p><b>METHODS</b>Five cases of FDCS were analyzed by clinical, pathologic and immunohistochemistry methods.</p><p><b>RESULTS</b>Five cases of FDCS were located in the cervical lymph node. Microscopically, the normal architectures were effaced by ovoid, spindle-shaped with fascicular, diffuse or whorled patterns and with rich lightly eosinophilic cytoplasm, syncytial appearance. Nuclei tend to show irregular clustering, scattered multinucleated giant cell. Nucleoli often distinct, sometimes prominent. Mitotic count variable, may show significant cellular pleomorphism. Immunohistochemical studies show that the tumor cells were positive for CD21, CD35, but negative for CD1a, CD34, CK and HMB45. Under electron microscopy, the tumor cells possessed long villus cytoplasmic processes and desmosome-like junctions, Birbeck granules were absent.</p><p><b>CONCLUSIONS</b>FDCS is a rare malignant tumor and differential diagnosis includes Langerhans cell sarcoma, interdigitating dentric cell sarcoma, malignant fibrous histocytoma, melanoma, metastatic spindle cell carcinoma and others. Immunohistochemistry and electron microscopy are necessary for a correct diagnosis.</p>