ABSTRACT
Auranofin (AF) is used in clinic for the treatment of rheumatoid arthritis, repurposing of AF as an anticancer drug has just finished a phase I/II clinical trial, but the developmental toxicity of AF remains obscure. This study focused on its developmental toxicity by using zebrafish embryos. Zebrafish embryos were exposed to different concentrations (1, 2.5, 5, 10 µm) of AF from 2 h post-fertilization (hpf) to 72 hpf. At 72 hpf, two major developmental defects caused by AF were found, namely severe pericardial edema and hypopigmentation, when embryos were exposed to concentrations higher than 2.5 µm. Biochemical detection of oxidative stress enzyme combined with expressions of a series of genes related to oxidative stress, cardiac, metal stress and pigment formation were subsequently tested. The superoxide dismutase activity was decreased while malondialdehyde content was accumulated by AF treatment. The expression of oxidative stress-related genes (sod1, gpx1a, gst), pigment-related genes (mitfb, trp-1a) and one metal stress-related gene ctr1 were all decreased by AF exposure. The expressions of cardiac-related genes (amhc, vmhc) and one metal-related gene hsp70 were found to be significantly upregulated by AF exposure. These findings indicated the potential developmental toxicity of AF on zebrafish early development. Copyright © 2016 John Wiley & Sons, Ltd.
Subject(s)
Antirheumatic Agents/toxicity , Auranofin/toxicity , Embryonic Development/drug effects , Zebrafish , Animals , Edema/chemically induced , Edema/pathology , Embryo, Nonmammalian , Gene Expression Regulation, Developmental , Heart/drug effects , Hypopigmentation/chemically induced , Hypopigmentation/genetics , Hypopigmentation/pathology , Malondialdehyde/metabolism , Metals/toxicity , Oxidative Stress/drug effects , Stress, Physiological/drug effects , Superoxide Dismutase/metabolism , TeratogensABSTRACT
OBJECTIVE: To study the optimum parameters of the supercritical CO, fluid extraction of lotus leaves and chemical constituents of extractive matters. METHODS: Supercritical CO2 fluid extraction condition was selected by uniform design. The extraction pressure, extraction temperature, extraction time were three factors in the experiment. GC-MS was applied for analyzing the extraction. RESULTS: The optimum condition were obtained: the extraction pressure was 26 Mpa, the extraction temperature was 40 degrees C, the extracion time was 90 minutes. The major constituent was 1H-Pyrrole-2-carboxaldehyde, 1-ethyl-in extractive matters. CONCLUSION: Uniform design can optimize the CO2 Supercritical Fluid Extraction process quickly and accuratly with satisfactory results.
Subject(s)
Chromatography, Supercritical Fluid/methods , Drugs, Chinese Herbal/analysis , Gas Chromatography-Mass Spectrometry/methods , Lotus/chemistry , Plant Leaves/chemistry , Carbon Dioxide , Drugs, Chinese Herbal/isolation & purification , Fatty Acids/analysis , Fatty Acids/isolation & purification , Monoterpenes/analysis , Monoterpenes/isolation & purification , Plants, Medicinal/chemistry , Pressure , Reproducibility of Results , Technology, Pharmaceutical/methods , Temperature , Time FactorsABSTRACT
OBJECTIVE: To study the optimum inclusion process of clolloid mill for borneolumsyntheticum from Huoxuezhitong Capsules. METHODS: The study was carried out with orthogonal design. The borneol content in inclusion complex, the utilization ratio of borneol, and synthesis grading were used as evaluating indicator to review the effects of 3 factors, including the proportion of borneolumsyntheticum to beta-cyclodextrin (mol: mol), milling time and water addition. RESULTS: The optimum process were borneolumsyntheticum: beta-cyclodextrin was 1:1, the milling time was 40 min, water addition was double. CONCLUSION: The optimum process is feasible, and fit for industrial production, with the advantage of high utilization ratio, shot time and low energy consumption.
Subject(s)
Camphanes/analysis , Drugs, Chinese Herbal/chemistry , Oils, Volatile/analysis , Technology, Pharmaceutical/methods , beta-Cyclodextrins , Biological Availability , Capsules , Chromatography, Gas , Chromatography, Thin Layer , Drug Carriers , Drug Stability , Drugs, Chinese Herbal/analysis , Oils, Volatile/chemistry , Time Factors , Water/administration & dosageABSTRACT
OBJECTIVE: To study optimum inclusion process condition for volatile oil with beta-cyclodextrin (beta-CD). METHODS: The optimum preparation condition were investigated by orthogonal design. The influence of utilization beta-CD and oil, inclusion temperature and time were studied to determin the utilization ratio of volatile oil and oil-bearing rate. RESULTS: The optimum preparation conditions were established as: volatile oil: beta-CD was 1:10, the inclusion temperature was 60 degrees C and inclusion time was 3h. CONCLUSION: The method is convenient and can he used for mass production.
Subject(s)
Drugs, Chinese Herbal/chemistry , Lamiaceae/chemistry , Oils, Volatile , Technology, Pharmaceutical/methods , beta-Cyclodextrins , Analysis of Variance , Drug Carriers , Drug Combinations , Drug Stability , Drugs, Chinese Herbal/analysis , Oils, Volatile/analysis , Oils, Volatile/chemistry , Oils, Volatile/isolation & purification , Plants, Medicinal/chemistry , Temperature , Time Factors , beta-Cyclodextrins/chemistryABSTRACT
OBJECTIVE: To develop a HPLC method for determination of triptolide in tripterygium total terpenoids tablets. METHOD: A Lichrospher CN column was used with ethanol and water for gradient elution. The detection wavelength was set at 255 nm. RESULT: The linear relationship of the concentrations and peak areas was good in range of 0.742-59.4 microg x mL(-1) (r = 0.9998). The average recovery was 99.2%, RSD% = 1.7%. CONCLUSION: The method is simple, rapid and accurate and can be used for quality control of the tablets.
