基于机器学习的药物血浆蛋白结合率的预测

预测药物在血浆中的蛋白结合率,有助于了解药物的药代动力学特征,对药物发现的早期研究有重要的参考价值.本研究收集了 2452个临床药物的血浆蛋白结合率信息,用Molecular Operating Environment(MOE)和Mordred两种软件计算分子描述符,将算得的分子描述符作为模型的输入特征.使用极端梯度提...     

胰岛素样生长因子2通过磷酯酰肌醇-3激酶/蛋白激酶B信号通路调控人卵巢颗粒细胞增殖的机制

目的 检测胰岛素样生长因子2(IGF2)对人卵巢颗粒细胞(KGN细胞)增殖的调控作用及作用机制.方法 将体外培养的KGN细胞,分不同浓度IGF2处理组(对照组和25 μg/L、50 μg/L、100μg/L IGF2组)和磷酯酰肌醇-3激酶/蛋白激酶B(PI3K/Akt)信号通路干预组(以LY294002干预处理将细胞...     

Heterotopic lung transplant: a feasible approach to compensate for organ shortages

Lung transplants are still limited by the shortage of suitable donor lungs, especially during the coronavirus disease 2019 pandemic. A heterotopic lung transplant (HLTx), as a flexible surgical procedure, can maximize the potential of donor lungs in an emergency, but its widespread use is hindered by difficulties in anastomosis and paucity of outcome data. We performed a retrospective review of 4 patients, each of whom received an HLTxs over 1 year, including 1 left-to-right single HLTx, 2 right-to-left single HLTxs and 1 lobar HLTx (right upper lobe-to-left). The median recipient age was 58.5 years (46–68); 3 patients were male. The postoperative hospital stay was 33 days (30–42). One recipient lived for 10 years and died of bronchiolitis obliterans syndrome; the others were alive with no major morbidity at 12 to 31 months after the operation with a 1-year survival of 100%. The follow-up chest images showed that transplanted lungs could be inflated well and adapted morphologically to fill the thoracic cavity in the short and long term. This study demonstrates that an HLTx is a feasible alternative to a conventional lung transplant in emergency cases and could be considered in selected patients at advanced medical centres.     

炙甘草汤和生脉散加减治疗小儿气阴亏虚型病毒性心肌炎的临床观察

目的 探讨炙甘草汤和生脉散加减治疗小儿气阴亏虚型病毒性心肌炎(VMC)的临床效果.方法 选取2018年3月至2020年3月于灵宝市第一人民医院接受治疗的93例气阴亏虚型VMC患儿,依据抽签法分为对照组(n=46)与观察组(n=47).两组均接受常规治疗,在此基础上,对照组采用灸甘草汤治疗,观察组采用炙甘草汤和生脉散加减...     

急性缺血性卒中血管内治疗技术培训模式研究——急性缺血性卒中血管内治疗培训班经验介绍

目的 探讨培训介入医师急性缺血性卒中血管内治疗技术的方法和模式.方法 对中国卒中学会国际卒中介入培训学院,首都医科大学附属北京天坛医院主办的"急性缺血性卒中血管内治疗培训班"学员进行血管内治疗技术理论和实践培训,并通过实践工作后1年进行毕业答辩,对学员的培训成果进行检验.结果 完成培训并在实际工作中开展急性缺血性卒中血...     

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.     

Iridoid glycosides extracted from Zhizi (Fructus Gardeniae) decrease collagen-induced platelet aggregation and reduce carotid artery thrombosis in an in vivo rat model

Objective

To investigate the anti-platelet aggregation and antithrombotic effects in rats of iridoid glycosides extracted from Zhizi (Fructus Gardeniae).

Methods

The present study evaluated the antithrombotic activity of iridoid glycosides (IGs) in a rat model of carotid artery thrombosis. The effects on coagulation, such as thromboplastin time (APTT), thrombin time (TT) and prothrombin time (PT), and the effect on collagen-induced platelet aggregation in vivo were investigated. Rats were intragastrically administered IGs (50, 100 or 200 mg/kg) twice daily for 3 days.

Results

IGs were shown for the first time to have an antithrombotic action through the inhibition of platelet aggregation, with little effect on the coagulation time of peripheral blood. Our results also showed that IGs may significantly and dose-dependently reduce arterial thrombus load in a model of carotid artery thrombosis and inhibit collagen-induced platelet aggregation in rats. IGs (100 or 200 mg/kg) had no significant effect on APTT and PT, but did lengthen TT at a higher dose.

Conclusion

These data, together with the previously reported neuroprotective effects of IGs in rats with cerebral ischemia, suggest that the antithrombotic action of IGs may potentially contribute to the treatment of cerebral ischemic diseases, including cerebral apoplexy.     

3-乙酰基-11-羰基-β-乳香酸在大鼠体内的代谢途径研究

目的 研究3-乙酰基-11-羰基-β-乳香酸(AKBA)在大鼠体内的代谢途径.方法 大鼠ig AKBA 60 mg/kg后,收集胆汁、尿液及粪便,应用高效液相色谱-四级杆-离子阱质谱(HPLC-QTRAP-MS)技术分析AKBA在大鼠体内的代谢途径.结果 共检测到除原形药物外的15个代谢产物,提示AKBA在大鼠体内的主要代谢途径为去乙酰化、单羟基化、脱氢化及葡萄糖醛酸结合物.结论 AKBA在大鼠体内经历了广泛的Ⅰ相、Ⅱ相代谢,产生的代谢产物主要通过粪便及胆汁排泄;利用QTRAP技术的自动切换扫描(IDA)软件及增强型产物离子(EPI)扫描功能,能够快速得到高质量的MS2谱图,为AKBA代谢产物的鉴定提供了有效的检测手段.     

电子医疗数据中不同疗程使用丹参多酚酸盐对肝肾功能指标变化影响的分析

为了解注射用丹参多酚酸盐不同使用疗程对肝肾功能的影响,从全国18家大型三甲医院的医院信息系统(hospital information system,HIS)中提取使用丹参多酚酸盐年龄在18~80岁患者,共10 470例,根据使用的不同疗程对用药前后7d有2次谷草转氨酶(AST)、谷丙转氨酶(ALT)、血肌酐(Cr)和血尿素氮(BUN)测指标的患者分组,连续用药时间>14 d者定义为观察组,≤14 d者定义为对照组,连续用药时间>31 d者不纳入分析。各指标观察组与对照组人数分别为:ALT(268/1 465),AST(2.70/1 585),Cr(278/1 582),BUN(278/1 611)。运用倾向评分方法对2组进行协变量平衡后,基于未加权logistic回归、倾向评分加权logistic回归、结合协变量调整倾向性评分加权logistic回归,对2组的肝肾功能进行分析。结果显示3种logistic回归分析显示2组患者的ALT,AST,Cr指标发生异常的可能性无显著统计学差异,连续用药时间>14 d可能会增加BUN指标发生异常的风险,综合分析尚不能说明不同疗程使用丹参多酚酸盐会引起病人肝肾毒性损害,仍需大样本前瞻性随机对照实验进一步深入研究。     

抗痛风胶囊对急性痛风性关节炎的作用及下调关节软骨组织MMP-1蛋白表达

目的:观察抗痛风胶囊对大鼠急性痛风性关节炎(AGA)的治疗作用及对软骨组织基质金属蛋白酶-1(MMP-1)蛋白表达的影响。方法:大鼠足踝关节注射尿酸钠悬液诱导AGA,容积法检测踝关节肿胀程度,HE染色观察关节软骨组织的病理组织学变化,免疫组织化学染色及图像分析检测关节软骨内MMP-1蛋白表达。结果:抗痛风胶囊0.3 mg/kg和1.2 mg/kg连续灌胃给药5d,明显减小AGA大鼠足容积,第5d关节肿胀抑制率高达70%～90%。HE染色后显微镜下观察,可见模型组大鼠足踝关节软骨组织细胞排列紊乱、出现充血、肿胀和关节表面的破坏,抗痛风胶囊治疗后,明显改善其病理组织学变化。免疫组织化学检测可见,与模型组比较,抗痛风胶囊和秋水仙碱(0.8mg/kg)均明显下调软骨细胞MMP-1蛋白的表达,其平均光密度值明显降低。结论:抗痛风胶囊对AGA具有明显治疗作用,且降低AGA大鼠关节软骨组织MMP-1蛋白表达可能该药缓解关节炎症肿胀的主要作用机制之一。