解聚复肾宁治疗早期2型糖尿病肾病

目的: 探讨解聚复肾宁治疗早期糖尿病肾病（DN）的临床疗效。 方法: 研究对象为我院收治的120例早期2型DN患者,将其随机分为解聚复肾宁组、厄贝沙坦组、解聚复肾宁+厄贝沙坦组、对照组。每组各30例,12周为1疗程,观察各组治疗前后相关指标的变化。 结果: 解聚复肾宁组治疗后空腹血糖、24 h尿微量白蛋白排泄率、血肌酐、糖化血红蛋白等指标显著好转,血清和尿液中血管紧张素Ⅱ（AngⅡ）,结缔组织生长因子（CTGF）均显著降低,解聚复肾宁和厄贝沙坦联合治疗明显优于两类药物单独应用（P<0.05）。 结论: 解聚复肾宁对早期2型DN疗效确切,可延缓病情进展,提高患者的生活质量,值得临床推广使用。     

中国近视患者的角膜厚度与屈光度关系的研究

目的　了解我国近视眼患者角膜厚度 ,及其与屈光度的相互关系 ,并给出由屈光度预测角膜厚度的回归方程 ,为准分子激光原位角膜磨镶术 (LASIK)手术设计提供参考依据。方法　应用OrbscanⅡ眼前节系统对 45 9例近视眼患者角膜厚度进行检测 ,包括角膜中央直径为 2mm及角膜中周部上方、颞上、颞侧、颞下、下方、鼻下、鼻侧、鼻上、上方 9个直径为 2mm的测量区 (距视轴3mm)的平均角膜厚度 ;屈光度由 -0 5D至 -2 3 5D不等 ;并对各方位角膜厚度与屈光度作直线相关 ,如有相关性则进行回归分析。结果　中国近视眼患者角膜厚度以中央区最薄 ,鼻上方最厚 ,近视眼患者角膜最薄点多位于颞下方 ( 5 2 72 % ) ;颞下及颞侧角膜厚度与屈光度呈线性负相关 (相关系数r分别为 -0 117、 -0 10 7,P <0 0 5 0 ) ;其它部位与屈光度无相关关系 ;角膜厚度彩色地形图中均为圆形最多 ,依次为椭圆形、偏心圆形、偏心椭圆形。结论　中国近视眼患者角膜厚度的改变多位于颞下及颞侧 ,且角膜厚度随近视度数增加有变薄倾向 ;而最薄点、中央区、颞上、鼻下、鼻侧、鼻上、上方、下方角膜厚度与近视度数增加无关 ;OrbscanⅡ眼前节系统能了解角膜厚度分布情况 ,在角膜屈光手术中具有广泛应用前景     

基于近红外光谱技术对山茱萸炮制程度的质量评价

目的 采用近红外光谱技术建立山茱萸饮片中5-羟甲基糠醛含量的快速无损检测方法,并用于快速判别山茱萸饮片的炮制程度。方法 以54个样本作为校正集,运用偏最小二乘法建立定量校正模型并进行优化。以9个样本作为验证集,进行含量预测。结果 校正模型决定系数为0.925 6,相对分析误差为5.06,交叉验证均方根误差为0.022 0,外部验证均方差为0.019 3,光谱预测值与真值之间的相关性较好。结论 该法可直接用于中药山茱萸中5-羟甲基糠醛含量的快速预测,为快速判断山茱萸炮制程度提供可能。该方法具有操作简便、快速无损、准确可靠等优点。     

调脂灵治疗高脂血症的临床和实验研究

目的研究灵芝制剂调脂灵的毒理、药效、对心脑血管的保护作用及治疗高脂血症的效果.方法检测卫生指标、LD50、"三致"试验;用调脂灵对SHR-SP进行降压及卒中的疗效实验;按国家标准判定调脂灵的临床疗效.结果重金属和细菌含量符合国家标准,LD50＞10 g/kg体重,"三致"试验阴性,证明调脂灵无毒.SHR-SP实验证明,调脂灵可保护动脉内皮细胞的完整性,阻止血栓形成与出血,减少脑卒中的发生.治疗160例高脂血症患者,降TC、LDL-C和TG的总有效率分别为71.4%、71.4%和48.4%,升高HDL-C为82.5%,同时对部分患者有降血压、血糖和ALT的作用.未发现不良反应.结论调脂灵安全有效,适用于冠心病、高血压、糖尿病等伴高脂血症的治疗.     

Catalytic N-methyl amidation of carboxylic acids under cooperative conditions

Amide is a fundamental group that is present in molecular structures of all domains of organic chemistry and the construction of this motif with high atom economy is the focus of the current research. Specifically, N-methyl amides are valuable building blocks in natural products and pharmaceutical science. Due to the volatile nature of methyl amine, the generation of N-methyl amides using simple acids with high atom economy is rare. Herein, we disclose an atom economic protocol to prepare this valuable motif under DABCO/Fe₃O₄ cooperative catalysis. This protocol is operationally simple and compatible with a range of aliphatic and (hetero)aromatic acids with very good yields (60–99%). Moreover, the Fe₃O₄ can be easily recovered and high efficiency is maintained for up to ten cycles.

The generation of N-methyl amides using simple acids with high atom economy is rare owning to the volatile nature of methyl amine. Herein, an atom economic protocol was disclosed to prepare this valuable motif under DABCO/Fe₃O₄ cooperative catalysis.

Amide is a fundamental group that is present in molecular structures of all domains of organic chemistry.¹ It is widely distributed in natural products, synthetic drugs and functional polymers, and is also the key chemical connection in proteins.² It has been shown that amide bond formation alone accounts for 65% of all preliminary screening reactions in the pharmaceutical industry.³ This means the generation of amide bonds with high atom efficiency is of high practical importance. And not surprisingly, ‘amide formation avoiding poor atom economy reagents’ was voted as the top challenge for organic chemistry by the ACS Green Chemistry Institute in 2007.³From synthetic point of view, the ideal way to produce amide bonds would be the direct coupling of readily available carboxylic acids and amines, but this process is thermodynamically unfavourable due to the formation of the corresponding carboxylate-ammonium salt,⁴ therefore, stoichiometric amount of coupling reagents, such as DCC, DIC, EDCI, HATU, HBTU, HCTU, SOCl₂, BOP, acid chloride etc, are generally required to sidestep thermal conditions for amide bond formation.⁵ These reagents are highly successful, but the process generally suffers from poor atom economy and side products removal issue especially in the large-scale applications.⁵ To overcome these drawbacks, “nonclassical” amide bonds formation routes were investigated.⁶ In these processes, the catalyst takes the role of a coupling reagent in generating an active ester suitable for amidation in a waste-free manner. However, these processes have not been applied in the preparation of N-methyl amides, probably because the methyl amine was delivered in its hydrochloride salt, alcoholic or aqueous form due to its volatile nature.On a different note, N-methyl amides are extensively presented in numerous natural products and pharmaceutical molecules, as shown in Fig. 1,⁷ and the methylation of amides is a promising way to improve the pharmacological property of molecules.⁸ However, the synthesis of N-methyl amides compounds relies heavily on non-catalytic approaches.^5,9 Catalytic approaches were also investigated by Hisaeda,¹⁰ Kundu,¹¹ Li,¹² Guo,¹³ Yu,¹⁴ Maruoka,¹⁵ Wang,¹⁶ Chen,¹⁷ Lamaty¹⁸ and their co-workers starting from nitriles, primiary amides, aldoximes, aldehydes, lignin, carbamoylsilane and alcohols. Until recently, Thakur,¹⁹ Marce,²⁰ Sadeghzadeh²¹ and their co-workers developed elegant N-methyl amidation approach starting from carboxylic acids under nano-MgO, diatomite Earth@IL/ZrCl₄ and Mg(NO₃)₂·6H₂O catalysis respectively, while limitations like poor substrate scope or sophisticated tailored catalyst still persist. Mindful of all the above issues, developing an N-methyl amidation process of simple carboxylic acids, which is still of great challenge in synthesis, and establishing a broad (hetero)aryl scope with high atom economy from commercial available reagents and catalysts were critical considerations in this study. Moreover, the significance of N-methyl amides combined with our interests in the development of green synthetic approaches motivated us to explore the direct coupling of the carboxylic acids and isothiocyanates. To the best of our knowledge, this is the first successful work using isothiocyanatomethane to prepare N-methyl amides.Open in a separate windowFig. 1Marketed drugs bearing N-methyl amide group.Our initial investigation begins with phenylacetic acid and isothiocyanatomethane as model substrate for condition optimization. Using acetonitrile as solvent, only trace amount of product was detected under catalyst free or p-toluenesulfonic acid (PTSA) catalysis conditions (

Triple Therapy-Based on Tegoprazan,a New Potassium-Competitive Acid Blocker,for First-Line Treatment of Helicobacter pylori Infection: A Randomized,Double-Blind,Phase III,Clinical Trial

Background/AimsWe examined the efficacy and safety of tegoprazan as a part of first-line triple therapy for Helicobacter pylori eradication.MethodsA randomized, double-blind, controlled, multicenter study was performed to evaluate whether tegoprazan (50 mg)-based triple therapy (TPZ) was noninferior to lansoprazole (30 mg)-based triple therapy (LPZ) (with amoxicillin 1 g and clarithromycin 500 mg; all administered twice daily for 7 days) for treating H. pylori. The primary endpoint was the H. pylori eradication rate. Subgroup analyses were performed according to the cytochrome P450 (CYP) 2C19 genotype, the minimum inhibitory concentration (MIC) of amoxicillin and clarithromycin, and underlying gastric diseases.ResultsIn total, 350 H. pylori-positive patients were randomly allocated to the TPZ or LPZ group. The H. pylori eradication rates in the TPZ and LPZ groups were 62.86% (110/175) and 60.57% (106/175) in an intention-to-treat analysis and 69.33% (104/150) and 67.33% (101/150) in a per-protocol analysis (non-inferiority test, p=0.009 and p=0.013), respectively. Subgroup analyses according to MICs or CYP2C19 did not show remarkable differences in eradication rate. Both first-line triple therapies were well-tolerated with no notable differences.ConclusionsTPZ is as effective as proton pump inhibitor-based triple therapy and is as safe as first-line H. pylori eradication therapy but does not overcome the clarithromycin resistance of H. pylori in Korea (ClinicalTrials.gov identifier {"type":"clinical-trial","attrs":{"text":"NCT03317223","term_id":"NCT03317223"}}NCT03317223).     

Acute abdomen caused by torsion of the omentum: A pediatric case report

Rationale:Torsion of the omentum and infarction are rare and unusual disorders that often present as acute abdominal pain in the population. The diagnosis of omental torsion is based on clinical and imaging examinations.Patient concerns:A 7-year-old girl presented with acute right lower quadrant abdominal pain, with symptoms resembling acute appendicitis.Diagnosis:The patient was diagnosed with omental torsion based on imaging and laparoscopy.Interventions:Laparoscopic exploration was performed.Outcomes:The patient was discharged seven days after satisfactory postoperative recovery.Lessons:Omental torsion should be included in the differential diagnosis of acute abdominal pain, particularly in patients with free hemorrhagic fluid in the abdominal cavity and pelvis.