张琪以加味甘露饮治疗慢性肾功能衰竭的经验分析

张琪教授是全国著名中医临床学家,精于仲景学说,对金元四大家、明清各家学派及温病学术理论有高深造诣。临证善治多种疑难病症,如肾病、心病、神志病、肝病、风湿病、糖尿病等,但尤对慢性肾脏病有较深造诣,治疗方法独具特色。     

活血化瘀强度与气血双亏型胃癌转移率相关性机理探讨

本文回顾研究了益气生血方剂中活血化瘀强度与气血双亏型胃癌转移率之间的相关性,显示两者有较强的正相关,提示气血双亏型胃癌转移率随活血化瘀作用加强而增高。推测可能与本型胃癌血小板数量及聚集性下降、血浆纤维蛋白含量低及凝血抑制、纤溶增强易于肿瘤转移有关,且大多数活血化瘀方药具有抑制血小板聚集,抗血凝和增加纤溶的现代药理机制。进而建议气血双亏型胃癌,在血小板数量及聚集率明显下降、凝血时间明显延长及FDP高时,尽量降低方剂中活血化瘀强度,以避免促进肿瘤转移。     

不同产地金银花挥发油GC-MS的比较分析

金银花为忍冬科植物忍冬 Lonicera japonicaThunb.的干燥花蕾 ,具有清热解毒、凉散风热的功效。金银花分布广泛 ,山东和河南是我国传统的道地产区 ,而产地不同 ,其有效成分含量存在着较大差异 [1,2 ] 。有关挥发油的成分研究曾有报道[3～ 5] ,为全面了解其挥发油成分的差异及变化 ,提高金银花的质量 ,我们采用 GC- MS首次对山东、河南及江苏等地金银花的挥发油成分做了比较分析。1　实验部分1 .1　样品及挥发油的提取 :样品分别采自山东平邑、日照 ,河南封丘、新密 ,江苏南京等地 ,经鉴定为L.japonica Thunb.。称取新鲜的花蕾 1 0 0 g,…     

大蒜素对T细胞激活的影响

大蒜素在高浓度(50μg／ml)时对T细胞激活有抑制作用。但在适当浓度(3．125～12．5μg／ml)时则对T细胞激活有促进作用，这种促进作用与大蒜素抑制巨噬细胞产生NO的能力有关。大蒜素能够对抗S180细胞和艾氏暖水癌细胞产生的肿瘤免疫抑制因子对T细胞激活的抑制作用。提示大蒜素在肿瘤治疗中可能有较大的应用价值。     

老年慢性阻塞性肺病治验一得

本文秉承姚培发老中医"肾精虚衰是人体衰老和老年病的主要因素"之学术观点.认为老年慢性阻塞性肺病中多见脾肾两虚,痰瘀内阻,尤其阳气不足,三焦气化不利.更易痰饮停聚,为咳为喘.总结剖析老年慢性阻塞性肺病医案二则.提出三条主张:1.补肾健睥为治本之重点;2.注重扶阳.阴阳平衡;3.久病宜益气活血祛瘀.     

Study on modified shengmai yin injection for prevention and treatment of brain impairment in endotoxin shock rats

Objective:To examine the effects of modified Shenmai Yin on invigorating vital energy, promoting blood flow, and protection against neural impairment in an endotoxin-induced shock rat model. Methods: Ninety-six SD rats were randomly divided into four groups: sham operation (saline 20 ml/kg), shock model (lipopolysaccharide, LPS, 8 mg/kg), Reformed Shengmai Yin (加味生脉饮 Pulse-activating Decoction) (LPS 8 mg/kg + reformed Shengmai Yin Injection 10 ml/kg), and dexamethasone (LPS 8 mg/kg + dexamethasone 5 mg/kg) groups. Each group was subdivided into 1 h, 2 h, 3 h, and 6 h time points for observation. The carotid artery was separated and connected with a biological functional system to monitor mean arterial pressure (MAP). Brain water levels, malonaldehyde (MDA) content, and superoxide dismutase (SOD) activity were also determined. Results: In the shock model group, MAP was progressively decreased after injection of LPS, brain water and MDA contents were increased, brain SOD activity was decreased, and capillary vessel edema in brain tissue was also observed. All these parameters were improved significantly in both treatment groups, although the effects were more marked with Shengmai Yin than with dexamethasone. Conclusion: Modified Shengmai Yin exhibits strong anti-shock and neuroprotective effects against Endotoxininduced shock.     

舒肺贴不同贴敷时间对慢性阻塞性肺疾病稳定期生存质量的影响

目的：分析舒肺贴不同贴敷时间对慢性阻塞性肺疾病稳定期生存质量的影响,确定最佳贴敷时间。方法：采用多中心、随机、对照的临床试验设计,将164例慢性阻塞性肺疾病稳定期患者随机分为A组和B组,其中A组82例（贴敷6-8 h）;B 组82例（贴敷8-12 h）。于夏季“三伏天”前的第10天、“三伏天”内的第1、10、20天,“三伏天”后的第10天各贴敷1次。研究结束后,脱落或剔除18例,本研究对符合研究要求的共146例（A组71例、B组75例）进行统计分析。结果：两组治疗后均能提高慢性阻塞性肺疾病稳定期患者的生存质量,但组间差异无统计学意义,患者贴敷6-8 h和贴敷8-12 h在治疗上均无统计学差异,但贴敷6-8 h严重大泡发生率低,安全性更好,选择6-8 h为最佳贴敷时间。结论：患者贴敷6-8 h和贴敷8-12 h在治疗上均无统计学差异,而贴敷8-12 h发生严重大泡率高,安全性较差,故舒肺贴最佳贴敷时间为6-8 h。     

部分和全天遮盖治疗儿童单眼弱视首剂效应的疗效分析

目的:探讨单眼弱视患者每日部分或全天遮盖优势眼后首次复诊的疗效,评估不同遮盖量所产生的最大效能。方法:回顾性临床研究。连续收集我院2020-01/2021-12本院门诊治愈的单眼弱视患者135例。根据遮盖时间分为2h/d遮盖组、6h/d遮盖组和全天遮盖组,配合弱视眼精细目力训练,记录首剂效应(基线视力-首次复查视力)、治愈视力、首次复诊时立体视觉以及弱视眼治愈时间。并分析影响单眼弱视患者首剂效应的因素。结果:所有患者基线视力为0.4(0.22, 0.52),首次复诊视力为0.22(0.15, 0.3),首剂效应为0.1(0.08, 0.18),弱视达治愈时视力为0(-0.08, 0.05)。2h/d遮盖组患者首剂效应为0.08(0.07, 0.12),6h/d遮盖组为0.18(0.08, 0.3),全天遮盖组为0.10(0.08, 0.18),6h/d遮盖组首剂效应最显著(P<0.05);不同影响因素分析显示3～6岁组、7～12岁组、女性组、斜视性弱视组、轻中度弱视组的6h/d遮盖首剂效应值最高(P<0.05);同时,6h/d遮盖首剂效应与弱视眼治愈时间呈正相关(r     

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 (