周围静脉压测定法监测硝酸酯静脉扩张效应

将周围静脉压测定法稍加改良后用于监测硝酸酯静脉扩张效应60例次，结果舌下含服硝酸甘油(NTG)后1～2min静脉压开始下降，4～6min显下降，9-12min下降到最大值，平均下降比率53.61±7．83％。认为周围静脉压测定法监测NTG扩血管效应方法简单，操作方便，过程稳定，数据可靠。     

Molecular mechanism of Chuanxiong Rhizoma in treating coronary artery diseases

ObjectiveMost of the studies on the herb Chuanxiong Rhizoma (CR) have focused on the l-arginine-nitric oxide (NO) pathway, but the nitrate-nitrite-NO (NO₃⁻–NO₂⁻–NO) pathway was rarely investigated. Therefore, the aim of this study was to evaluate the effects and mechanisms of action of CR in coronary artery disease (CAD).MethodsThe NO₃⁻, NO₂⁻ and NO levels were examined in the NO₃⁻–NO₂⁻–NO pathway. High-performance ion chromatography was used to quantify NO₃⁻ and NO₂⁻ levels. Then, NO was quantified using a multifunctional enzyme marker with a fluorescent probe. The tension of aortic rings was measured using a multi myograph system.ResultsHigh content of NO₃⁻ and low content of NO₂⁻ was found in CR, and which could potently convert NO₃⁻ to NO₂⁻ in the presence of endogenous reductase enzyme. Incubating human coronary artery endothelial cells (HCAECs) with CR-containing serum showed that CR significantly decreased the NO₃⁻ content and increased the levels of NO₂⁻ and NO in the cells under hypoxic conditions. In addition, CR significantly relaxed isolated aortic rings when the l-arginine –NO pathway was blocked. The optimal concentration of CR for relaxation was 200 mg/mL.ConclusionCR supplements large amounts of NO in cells and vessels to achieve relaxation via the NO₃⁻–NO₂⁻–NO pathway, thereby making up for the deficiency caused by the lack of NO after the l-arginine-NO pathway is suppressed. This study also supports the potential use of a traditional Chinese herb for future drug development.     

Mechanisms underlying blood pressure reduction by dietary inorganic nitrate

Nitric oxide (NO) importantly contributes to cardiovascular homeostasis by regulating blood flow and maintaining endothelial integrity. Conversely, reduced NO bioavailability is a central feature during natural ageing and in many cardiovascular disorders, including hypertension. The inorganic anions nitrate and nitrite are endogenously formed after oxidation of NO synthase (NOS)‐derived NO and are also present in our daily diet. Knowledge accumulated over the past two decades has demonstrated that these anions can be recycled back to NO and other bioactive nitrogen oxides via serial reductions that involve oral commensal bacteria and various enzymatic systems. Intake of inorganic nitrate, which is predominantly found in green leafy vegetables and beets, has a variety of favourable cardiovascular effects. As hypertension is a major risk factor of morbidity and mortality worldwide, much attention has been paid to the blood pressure reducing effect of inorganic nitrate. Here, we describe how dietary nitrate, via stimulation of the nitrate‐nitrite‐NO pathway, affects various organ systems and discuss underlying mechanisms that may contribute to the observed blood pressure‐lowering effect.     

硝酸羟胺急性中毒组织病理学观察

目的　探讨硝酸羟胺急性中毒病理变化特点 ,为硝酸羟胺急性中毒的临床救治提供理论依据。方法　ICR雄性小鼠 ,体重 18～ 2 2g ,一次性腹腔注射 12 0mg/kg体重的硝酸羟胺 ,制作硝酸羟胺急性中毒小鼠模型 ,染毒 7d后处死 ,取主要脏器进行病理学检查。结果　以肺、肝脏损伤较重 ,表现为肺泡及其间质广泛出血 ,肝细胞严重变性、弥漫性水肿和气球样变。结论　肝脏和肺是硝酸羟胺急性中毒作用的靶器官     

茶多酚对硝酸羟胺染毒小鼠血常规和血清生化值的影响

目的　观察绿茶提取物茶多酚对硝酸羟胺染毒小鼠血常规、血清生化值的影响。方法　采用腹腔注射硝酸羟胺建立中毒模型。雄性ICR小鼠随机分为正常组、硝酸羟胺染毒组、茶多酚预防组、茶多酚治疗组 ,常规测量各组外周血细胞和生化指标。结果　经过统计学分析 ,茶多酚可明显促进硝酸羟胺中毒导致的小鼠血常规的WBC、RBC、HGB、PLT计数改变的恢复 ,部分血清生化值AST/ALT、ChE、ALB、LDH、UA、Fe病理性改变的恢复。结论　茶多酚灌胃给药对硝酸羟胺中毒引起的氧化损伤具有一定的保护作用     

How to use nitrates

Nitrates are old drugs, available in many formulations, that are effective in relieving symptoms in various CAD syndromes as well as congestive heart failure. Nitrate tolerance is the major problem limiting nitrate efficacy and use by physicians. Currently, an intermittent dosing strategy is the only practical way to limit the development of tolerance or attenuation of nitrate actions.     

硝酸咪康唑脂质体的制备工艺研究

目的:探讨硝酸咪康唑脂质体的制备工艺.方法:以包封率和载药量为指标,应用正交试验法优选最佳制备工艺.结果:最佳工艺处方为乙醇注入法,药脂比3%(w/w),磷脂与胆同醇的摩尔比为80:20,缓冲液pH7.4.制备的脂质体包封率为75.54%,平均粒径为222.3 nm,zeta电位为-0.31mV.结论:乙醇注入法制备硝酸咪康唑脂质体包封率高.制备工艺合理、可行.     

硝酸舍他康唑栓治疗外阴阴道假丝酵母菌病28例

［摘要］目的评价硝酸舍他康唑栓治疗外阴阴道假丝酵母菌病的疗效及安全性。方法采用随机双盲对照试验。治疗组及对照组各30例,分别外用硝酸舍他康唑栓300 mg和克霉唑栓500 mg,用药1或2次。停药后（7±1） d及28～35 d时进行观察。结果治疗组28例、对照组30例纳入分析,治疗组和对照组停药后（7±1） d临床有效率分别为89.29%,86.67%（P＞0.05）;用药结束后28～35 d时的临床有效率分别为81.48%,66.67%（P＞0.05）;均未发生与药物相关的不良反应。结论硝酸舍他康唑栓治疗外阴阴道假丝酵母菌病有效,安全。     

壳聚糖包覆的硝酸毛果芸香碱眼用亚微乳的研究

本文设计了一种壳聚糖包覆的硝酸毛果芸香碱眼用亚微乳(chitosan-coated pilocarpine nitrate submicroemulsion,CS-PN/SE),旨在开发一种新型的具有黏膜黏附性的亚微乳眼部给药系统,以延长药物在眼表滞留时间,促进药物的眼部吸收。以中长链甘油三酯(medium chain triglycerides,MCT)为油相,Tween 80为主乳化剂,采用高速剪切工艺制备硝酸毛果芸香碱亚微乳(pilocarpine nitrate submicro emulsion,PN/SE),进一步采用孵育法制备CS-PN/SE,并利用星点设计-效应面优化法进行处方优化。对其粒径、zeta电位、包封率和微观形态进行表征,以新西兰白兔为动物模型,评价了CS-PN/SE在兔眼表滞留特性以及缩瞳作用。眼表滞留特性评价结果显示,与硝酸毛果芸香碱溶液剂组(pilocarpine nitrate solution,PNs)和PN/SE组相比,CS-PN/SE组在眼表的清除率下降,KCS-PN/SE为(0.006 4±0.000 3)min-1,平均驻留时间(mean residence tim...     

硝酸酯类NO供体型齐墩果酸衍生物的合成及抗肿瘤活性

以齐墩果酸为先导物,将其3位OH通过各种类型的连接基团与硝酸酯类NO供体偶联,合成了10个目标化合物（2,4,8a～8c,10,12,15a～15c）。结构均经IR,MS及¹H NMR确证,并采用MTT法测定了偶联物的细胞毒性。结果显示,化合物8c对人肺癌细胞A549、人结肠癌细胞HT-29及人肝癌细胞SMMC-7721均具有较强的抗肿瘤活性,值得进一步研究。