Measurements of hydrocortisone and cortisone for longitudinal profiling of equine plasma by liquid chromatography–tandem mass spectrometry

The conventional detection of exogenous drugs in equine doping samples has been used for confirmation and subsequent prosecution of participants responsible. In recent years, alternative methods using indirect detection have been investigated due to the expanding number of pharmaceutical agents available with the potential of misuse. The monitoring of endogenous biomarkers such as hydrocortisone (HC) has been studied in equine urine with an international threshold of 1 μg/ml established; however, there is no current threshold for equine plasma. The aim of this research was to investigate plasma concentrations of HC and cortisone (C) in race day samples compared to an administration of Triamcinolone Acetonide (TACA). The reference population (n = 1150) provided HC (6 to 145 ng/ml) and C (0.7 to 13 ng/ml) levels to derive the HC to C ratio (HC/C). Population reference limits (PRLs) were proposed for HC/C values at 0.2 (lower) and 61 (upper). Administration of TACA resulted in down-regulation of HC/C values below the estimated PRLs for up to 96 h post-administration. This indirect detection period was longer than the detection of TACA for 72 h. The use of individual reference limits (IRLs) for HC/C values was investigated to support the Equine Biological Passport (EBP), an intelligence model developed by Racing NSW for longitudinal monitoring of biomarkers.     

颅脑损伤病人血皮质醇水平与伤情轻重及预后的关系

目的探讨颅脑损伤后病人的血皮质醇水平变化和颅脑损伤轻重分级的相关性，并探讨其对颅脑损伤预后的影响。方法回顾性分析57例颅脑损伤病人外伤后测得的血皮质醇水平，按照CCS评分分成轻中型和重型颅脑损伤组，并对所有病人随访半年。结果重型组病人的血皮质醇水平比轻中型组病人明显升高（0．01〈P〈0．05）。随访结果表明，伤后急性期血皮质醇水平越高，病人的死亡率和伤残率越高（P〈0．01）。结论颅脑损伤病人血皮质醇水平与损伤轻重程度相关，与病人的预后相关．     

THE ROLE OF THE ADRENAL CORTEX IN THE DEVELOPMENT OF MARASMUS

Rats maintained on low-protein diets and given injections of cortisone showed a great deficit in body weight. The protein concentration in muscle was low, but it was normal in the liver. Similar changes are also characteristic of marasmus. It is suggested that a high adrenocortical activity may be necessary for the development of the marasmic state.     

Management of optic neuritis

To improve understanding and effectiveness of therapy in optic nerve disease, various causes of so-called optic neuritis should be identified when possible. The clinical characteristics of demyelinating optic neuropathy can be contrasted with those of ischemic optic neuropathy, nutritional optic neuropathy, true optic nerve inflammation (e.g., luetic), optic nerve infiltration with tumor, and compression neuropathy caused by adjacent tumor. Radiologic studies and other means of investigating patients with optic neuritis are reviewed. Arguments in favor of, and against, treatment of presumed demyelinating optic neuritis are presented along with representative corticosteroid treatment regimens. The natural tendency toward spontaneous improvement of optic neuritis makes the effect of treatment difficult to assess.     

The effect of ibuprofen on the excretion of steroid metabolites

An inexpensive gas Chromatographic method is described that allows simultaneous measurement in urine of androsterone (A), aetiocholanolone (E), 11-hydroxyandrosterone (11-OA), 11-hydroxyaetiocholanolone (11-OE), pregnanediol (PD), pregnanetriol (PT), tetrahydrocortisone (THE) and tetrahydrocortisol (THF). Dehydroepiandrosterone was also resolved by the column.Ibuprofen was administered to five healthy normal males at a dose used therapeutically in rheumatoid arthritis (RA). The above urinary steroids were measured weekly during a control period, during a four week period of drug treatment and for four weeks after drug treatment had ceased.The excretion of A fell to a mean of 63% of the control value (P < 0.02) and returned to the control value within two weeks. 11-OA, which showed a greater variability than A, fell to the same extent (P < 0.1). No other steroid measured showed a change that could be related to the drug.     

The effect of cortisone on protein breakdown and synthesis in rat skeletal muscle

The effect of cortisone administration on the rates of muscle protein breakdown and synthesis has been studied in the rat extensor digitorum longus muscle. Cortisone acetate (100 mg/kg body weight/day) was administered intraperitoneally for 1–3 days. Muscle weight and protein content were significantly reduced by cortisone administration. Rates of protein breakdown were measured by tyrosine release from the isolated muscle into the intracellular pool and medium during a 2-h incubation with cycloheximide to block protein synthesis. Rates of protein synthesis were assayed by [¹⁴C]tyrosine incorporation into protein of the isolated muscle during a 2-h incubation. Cortisone administration inhibited significantly the rate of protein synthesis after 1–3 days treatment and also reduced significantly the rate of protein breakdown per muscle after 3 days treatment. The synthesis of myofibrillar and soluble proteins was affected to the same extent. These results strongly suggest that the effect of cortisone administration on muscle protein is mainly through its inhibition of protein synthesis rather than through an acceleration of protein breakdown.     

氢化可的松及其注射液有关物质检查

目的:对氢化可的松原料及其注射液中含有的有关物质进行测定。方法:采用高效液相色谱法进行分析,同时采用二极管阵列检测器进行杂质波谱扫描,液质联用法辅助确定主要杂质的结构。结果:氢化可的松和杂质峰分离良好,试验样品主要杂质确证为6,17,21β-三羟基孕甾-4-烯-3,20-二酮、表氢化可的松、17,21-二羟基孕甾-4-烯-3,20-二酮、可的松及泼尼松龙。结论:本法准确、灵敏,杂质检出性强,适用于氢化可的松及其注射液有关物质的测定。     

夏连颗粒(甲康)治疗亚急性甲状腺炎的临床研究

目的探讨纯中药制剂夏连颗粒(甲康)对亚急性甲状腺炎的临床疗效及停药后的复发率。方法对102例亚急性甲状腺炎随机分为三组;甲康治疗组(A 组),对照组分别为消炎痛、泼尼松(B 组)及甲康、消炎痛合用泼尼松(C组),观察其疗效、疗程及停药后的复发率。结果疗效;三组均全部治愈,无显著差异。疗程;A 组:4～6周(χ±SD:27.89±13.56天),B 组:4～6周(X±SD:31.71±14.32天),C 组:2～4周(18.79±9.72天)。A 组与 B 组比较无显著差异(P>0.05),但 C 组与 A、B 组比较有显著差异(P<0.05)。复发率:A 组3.22%(1/31),B 组21.21％(7/31),C 组2.63%(1/38)。A 组与 B 组比较有显著差异(P<0.05),A 组与 C 组比较无显著差异(P>0.05)。结论纯中药制剂夏连颗粒(甲康)对亚急性甲状腺炎治疗有效,特别是中西医药联合用药,疗效更佳,起效快、疗程短、复发率低。此项研究结果表明,夏连颗粒(甲康)可以应用于临床。     

Antcin A, a steroid-like compound from Antrodia camphorata, exerts anti-inflammatory effect via mimicking glucocorticoids

Aim:

To determine the active ingredient of Niuchangchih (Antrodia camphorata) responsible for its anti-inflammatory effects and the relevant molecular mechanisms.

Methods:

Five major antcins (A, B, C, H, and K) were isolated from fruiting bodies of Niuchangchih. Structural similarity between the antcins and 2 glucocorticoids (cortisone and dexamethasone) was compared. After incubation with each compound, the cytosolic glucocorticoid receptor (GR) was examined for its migration into the nucleus. Mo lecular docking was performed to model the tertiary structure of GR associated with antcins.

Results:

Incubation with cortisone, dexamethasone or antcin A (but not antcins B, C, H, and K) led to the migration of glucocorticoid receptor into the nucleus. The minimal concentration of antcin A, cortisone and dexamethasone to induce nuclear migration of glucocorticoid receptor was 10, 1, and 0.1 mol/L, respectively. The results are in agreement with the simulated binding affinity scores of these three ligands docking to the glucocorticoid receptor. Molecular modeling indicates that C-7 of antcin A or glucocorticoids is exposed to a hydrophobic region in the binding cavity of the glucocorticoid receptor, and the attachment of a hydrophilic group to C-7 of the other four antcins presumably results in their being expelled when docking to the cavity.

Conclusion:

The anti-inflammatory effect of Niuchangchih is, at least, partly attributed to antcin A that mimics glucocorticoids and triggers translocation of glucocorticoid receptor into nucleus to initiate the suppressing inflammation.