ABSTRACT
To identify the pharmacodynamic material basis of root bark of Caesalpinia decapetala extract and clarify the dynamic changes and distribution characteristics of the compounds in vivo.UPLC-MS/MS was used for simultaneous determination of 3-deoxysappanchalcone, isoliquiritigenin, protosappanin B, and protosappanin B-10-O-ß-D-glucoside in plasma, heart, liver, spleen, lung, kidney, stomach and duodenum of rats, to further study the pharmacokinetics and tissue distribution of root bark of C.decapetala extract in rats.Statistical analysis of obtained data demonstrated that the established analytical methods of the four components in biological matrix met the requirements of biological sample determination.The pharmacokinetic parameters showed that the t_(1/2 z), T_(max), C_(max), AUC_(0-t), MRT_(0-t), and CL_(z/F) of each component were 4.57-13.47 h, 0.22-0.51 h, 27.60-6 418.38 µg·L~(-1), 112.45-11 824.25 h·µg·L~(-1), 3.89-9.01 h, and 9.85-96.87 L·h~(-1)·kg~(-1), respectively.The results of tissue distribution revealed that at different time points, the components were widely but unevenly distributed in the body.Specifically, they were more distributed in the stomach and duodenum, followed by liver, spleen, lung, and kidney, and the least distribution was observed in the heart.
Subject(s)
Caesalpinia , Drugs, Chinese Herbal , Animals , Chromatography, High Pressure Liquid/methods , Chromatography, Liquid/methods , Drugs, Chinese Herbal/analysis , Plant Bark/chemistry , Rats , Rats, Sprague-Dawley , Tandem Mass Spectrometry/methods , Tissue DistributionABSTRACT
AIM: To investigate the effect of DAPT (gamma-secretase inhibitor) on the growth of human tongue carcinoma cells and to determine the molecular mechanism to enable the potential application of DAPT to the treatment of tongue carcinoma. METHODOLOGY: Human tongue carcinoma Tca8113 cells were cultured with DAPT. Cell growth was determined using Indigotic Reduction method. The cell cycle and apoptosis were analyzed by flow cytometry. Real-time PCR and Immuno-Fluorescence (IF) were employed to determine the intracellular expression levels. RESULTS: DAPT inhibited the growth of human tongue carcinoma Tca8113 cells by inducing G0-G1 cell cycle arrest and apoptosis. The mRNA levels of Hairy/Enhancer of Split-1 (Hes-1), a target of Notch activation, were reduced by DAPT in a dose-dependent manner. Coincident with this observation, DAPT induced a dose-dependent promotion of constitutive Caspase-3 in Tca8113 cells. CONCLUSION: DAPT may have a therapeutic value for human tongue carcinoma. Moreover, the effects of DAPT in tumor inhibition may arise partly via the modulation of Notch-1 and Caspase-3.
Subject(s)
Amyloid Precursor Protein Secretases/antagonists & inhibitors , Antineoplastic Agents/pharmacology , Apoptosis/drug effects , Carcinoma/pathology , Dipeptides/pharmacology , Tongue Neoplasms/pathology , Antineoplastic Agents/administration & dosage , Basic Helix-Loop-Helix Transcription Factors/drug effects , Caspase 3/drug effects , Cell Line, Tumor , Cell Membrane/drug effects , Cell Nucleus/drug effects , Cyclin D1/drug effects , Dipeptides/administration & dosage , Dose-Response Relationship, Drug , G1 Phase/drug effects , Homeodomain Proteins/drug effects , Humans , Receptor, Notch1/drug effects , Repressor Proteins/drug effects , Resting Phase, Cell Cycle/drug effects , Transcription Factor HES-1ABSTRACT
OBJECTIVE: To evaluate the influence of different types of posts and cores on the final color of the IPS-Emperss 2 crown. METHODS: Five types of posts and cores (Cerapost with Empress cosmo, Cerapost with composite resin, gilded Ni-Cr alloy, gold alloy and Ni-Cr alloy) were made. The shifts in color of three points of IPS-Empress 2 crown surface (cervical, middle and incisal) with different posts and cores was measured with a spectroradiometer (PR-650). RESULTS: The L* a* b* values of zirconium oxide and gilded Ni-Cr alloy posts and cores with ceramic crown were the highest. The L* a* values of zirconium oxide posts composite cores were higher while the b* values were lower. The L* a* b* values of Ni-Cr alloy were lower than that of gold alloy and were the lowest. CONCLUSION: In combination with IPS-Empress 2 crown, zirconium oxide posts are suitable for routine use in the anterior dentition, and gilded Ni-Cr alloy and gold alloy posts and cores can be recommended for clinical practice. Ni-Cr alloy posts and cores can not be recommended for clinical practice.
