注射用熊胆粉对大鼠脑血栓的影响

目的观察注射用熊胆粉对脑血栓、脑缺血动物模型的影响。方法观察注射用熊胆粉iv给药后对大鼠大脑中动脉血栓模型、不完全性脑缺血、血小板、血栓形成、血瘀大鼠血液流变性的影响。结果注射用熊胆粉可明显抑制大鼠体内外血栓的形成,降低血液黏度,改善血液流变性,抑制血小板聚集,降低血小板黏附性,改善血栓性缺血脑组织病变程度,降低毛细血管通透性,且可降低损伤脑组织中丙二醛(MDA)水平,保护超氧化物歧化酶(SOD)活性。结论注射用熊胆粉对脑缺血有保护和治疗作用。     

Selenium substituted axitinib reduces axitinib side effects and maintains its anti-renal tumor activity

Axitinib is a potent vascular endothelial growth factor receptor (VEGFR) inhibitor, which has a strong inhibitory effect on the three isoforms of VEGFR 1–3. Having strong therapeutic efficacy, its broad use is limited by its side effects such as hypertension, proteinuria, cardiovascular damage, and liver and kidney dysfunction. Selenium compounds are broadly reported to have a good protective effect on cardiovascular disease, inflammation, infection, and immune function. In this study, a selenium substitute of axitinib was synthesized, and its anti-renal cell carcinoma activity and side effects were investigated. The results of the study indicated that Se-axitinib had potent antitumor activity on renal cell carcinoma (RCC), alleviated vascular hyperpermeability, and also alleviated axitinib-related side effects including hypertension, liver dysfunction and kidney dysfunction significantly. Therefore, we suggest that Se-axitinib could be a solution to the severe side effects of VEGFR inhibitors and provide evidence to improve the outcome of RCC treatment.

Se-axitinib is a selenium substitution of sulfur in axitinib, which reduced the side effect of VEGFR inhibitors and maintained the potent anticancer activity of the original drug.     

The synthesis of the neuropeptide Met-enkephalin and two metabolic fragments labelled with 11C in the methionine methyl group

Starting from the corresponding N-benzyloxycarbonyl S-benzyl homocysteine peptide benzyl esters, Met-enkephalin and two metabolites, Gly-Phe-Met and Phe-Met, have been labelled with ¹¹C for application in positron emission tomography in vivo. All labelling experiments were accomplished in high radiochemical yields within 30–40 min from start of the [¹¹C]methyl iodide synthesis. Alkylations with this reagent were performed in liquid ammonia, using sodium to generate the free peptides with their reactive sulphide anions, essentially as previously described for [methyl-¹¹C]methionine. The products were purified by liquid chromatography (LC) to a radiochemical purity of 98% or better.     

Genotoxicity studies of benz[l]aceanthrylene

The genotoxicity of the cyclopenta-fused polycyclic aromatic hydrocarbon, benz[l]aceanthrylene (B[l]A), was evaluated in vitro using the L5178Y/TK+/- mouse lymphoma assay and in vivo using the mouse peripheral blood lymphocyte (PBL) culture system. The mutagenicity and sister chromatid exchange (SCE) inducing potential of B[l]A was then compared to that of benzo[a]pyrene (B[a]P). B[l]A appeared to be slightly less mutagenic than B[a]P at the TK locus, and each compound produced both small and large colony mutants indicating that they are clastogenic as well as mutagenic. Gross chromosome aberration analysis of treated L5178Y/TK+/- mouse lymphoma cells confirmed the clastogenicity of B[l]A in vitro. In the mouse PBL system, after administration by gavage, B[l]A was more cytotoxic and produced a sharper elevation in SCE frequency than B[a]P.     

安络小皮伞提取物特征图谱研究

摘 要 目的:采用高效液相色谱法建立安络小皮伞提取物的特征图谱。方法: 通过对安络小皮伞提取物1-苯基-3-甲基-5-吡唑啉酮（PMP）柱前衍生化,采用高效液相色谱法进行单糖组成分析。结果:安络小皮伞提取物特征图谱共检出 5个峰,其中已通过对照品确定5个色谱峰的归属,安络小皮伞提取物水解产物中含有甘露糖、半乳糖醛酸、葡萄糖、半乳糖、阿拉伯糖。结论:该方法简单,快速,灵敏度高,重现性良好,可作为控制安络小皮伞提取物内在质量的标准。     

芪月降脂片对高脂血症大鼠血脂代谢的影响

目的：观察芪月降脂片（QHT）对高脂血症大鼠血脂代谢的影响。 方法：Wistar大鼠随机分为正常对照组、高脂模型组、阳性对照组及QHT 1.75、3.50、7.00 g·kg^-1组。采用喂饲高脂饲料同时灌胃QHT,连续4周,观察QHT对大鼠高脂血症的预防作用;采用喂饲高脂饲料1周后灌胃QHT,连续3周,观察QHT对大鼠高脂血症的治疗作用。 结果：与高脂模型组比较,QHT预防和治疗方式给药均能明显降低实验性高血脂大鼠血清总胆固醇（TC）、甘油三酯（TG）和低密度脂蛋白胆固醇（LDL-C）含量、动脉硬化指数（AI）、TC/HDL-C及LDL-C/HDL-C比值（P<0.05或P<0.001）,治疗给药亦能明显提高实验性高脂血症大鼠血清高密度脂蛋白胆固醇（HDL-C）含量（P<0.05）。 结论：QHT对大鼠实验性高脂血症具有预防和治疗作用。     

IGF-1经PI3K/Akt依赖性途径保护TNF-α诱导的大鼠心肌细胞损伤

目的观察胰岛素样生长因子-1（IGF-1）对肿瘤坏死因子-α（TNF-α）处理的大鼠心肌细胞存活率的影响,并探讨其与PI3K/Akt通路的关系。方法心脏逆行灌流胶原酶消化方法分离大鼠的心肌细胞培养1 d后,分为对照组、TNF-α组、IGF-1＋TNF-α组以及IGF-1＋TNF-α＋LY294002组。光学显微镜下观察心肌细胞形态学变化,并用2,3-二苯基溴化四唑（MTT）法测定细胞的存活率。结果心肌细胞活数OD值在TNF-α组较对照组明显降低;IGF-1＋TNF-α组明显高于TNF-α组,与对照组比较无统计学差异;IGF-1＋TNF-α＋LY294002组明显低于IGF-1＋TNF-α组,与TNF-α组比较无统计学差异。结论IGF-1保护TNF-α诱导的大鼠心肌细胞凋亡,这种保护作用经PI3K/Akt通路依赖性机制。     

黑米花色苷提取物对大鼠抗过敏作用

目的观察黑米花色苷提取物(anthocyanin-rich extract from black rice,AEBR)的抗过敏作用并探讨其可能的作用机制。方法通过IgE诱导大鼠被动皮肤过敏反应(PCA)实验,用比色法测定黑米花色苷提取物在体内对肥大细胞影响;体外实验观察黑米花色苷提取物对IgE诱导组胺释放、细胞内钙摄入及其他炎性介子的影响。结果动物实验显示,AEBR高、中剂量组(300、150 mg/kg)明显抑制PCA实验,抑制率分别49.71%、30.40%。细胞实验显示,AEBR高、中剂量组(100、50μg/L)明显抑制组胺的释放(抑制率分别为75.56%、44.76%)、细胞内钙摄入(抑制率分别为64.75%、44.56%)以及肿瘤坏死因子-α(TNF-α)[黑米花色苷提取物(25、50、100μg/L)给药10 min使TNF-α蛋白表达分别下降7.8%、80%与85%]、白细胞介素6(IL-6)[黑米花色苷提取物(25、50、100μg/L)给药10min使IL-6蛋白表达分别下降5.6%,77%与84.1%]的释放(P<0.05)。结论黑米花色苷提取物抗过敏作用与抑制肥大细胞脱颗粒及炎性介子的...     

Gingival metastasis from primary hepatocellular carcinoma: a case report

Hepatocellular carcinoma (HCC) is one of the most common malignant tumors worldwide; however, cases with metastasis to the oral cavity are extremely rare. Herein, we report a 68-year-old man who was diagnosed with HCC. Ten months after surgical removal of the right half of his liver, the patient developed gingival metastasis. Unfortunately, the patient died 4 months after the diagnosis. We discuss treatment options, pathological results, and disease prognosis. When a mandibular gingival mass is found, metastatic tumors should be considered in the differential diagnosis. In this regard, the patient’s medical history and physical examination are valuable indicators for the diagnosis of mandibular gingival metastasis. This case provides a basis for the clinical diagnosis of metastatic HCC involving the oral cavity.     

左卡尼汀注射液治疗舒张性心力衰竭的临床疗效观察

目的:观察左卡尼汀注射液在舒张性心力衰竭治疗中的临床疗效。方法:选取我院2010年1月～2012年5月住院患者136例,随机分为对照组57例和治疗组79例,对照组常规给予琥珀酸美托洛尔、雷米普利、利尿剂等口服;治疗组在此治疗基础之上加用左卡尼汀注射液。比较治疗组和对照组治疗前后的心功能以及BNP、EV、AV、E/A比值、EDT和IRT各项指标。结果:治疗组无论在心功能改善上、心脏舒张功能指标和BNP测定值上均优于对照组,具有统计学意义。结论:左卡尼汀注射液明显改善舒张性心力衰竭患者临床症状和各项心脏舒张指标,优于常规治疗方法。