Antihypertensive activity of indole and indazole analogues: A review

Heterocyclic compounds occupy an important position in chemistry because of their wide range of uses in drug design, photochemistry, agrochemicals, and other fields. Indole and indazole scaffolds are available from natural and synthetic sources, and molecules containing these scaffolds have been shown to have various biological effects, including anti-inflammatory, antibacterial, antiviral, antifungal, analgesic, anticancer, antioxidant, anticonvulsant, antidepressant, and antihypertensive activities. Indole and indazole molecules bind to receptors with high affinity, and thus are useful for the study of bioactive compounds involved in multiple pathways. In this review, we highlight the antihypertensive activity and the mechanisms of action of indole and indazole derivatives. In addition, structure–activity relationship studies of the antihypertensive effect are presented.     

Histochemical and ultrastructural changes of sternomastoid muscle in aged wistar rats

The aim of this study was to evaluate histochemically and ultrastructurally the sternomastoid muscle (SM) of adults and aged rats, employing histochemic (NADH-TR reaction) and transmission electron microscopic methods. It was used 20 rats, divided into two groups: adults (n = 10), animals with 4 months of age, and aged group (n = 10), animals with 24 months of age. Five animals from each group were anesthetized with an overdose of urethane (3 g/kg i.p.), and the muscles dissected after the samples processing for histochemical reaction (NADH-TR). Three types of fibers were identified by their metabolic characteristics: fibers with high oxidative capacity (O), intermediate oxidative capacity (OG) and low oxidative capacity (G). For transmission electron microscopic method, the animals were anesthetized and perfused by modified Karnovsky solution and the tissues were postfixed in 1% osmium tetroxide solution, dehydrated and embedded in Spurr resin. It was performed ultra-thin sections for transmission electron microscopic analysis. The SM showed heterogeneity in their composition according to the fiber types, with significant difference (p < 0.05) when comparing the fibers types between the superficial and deep regions and between the adult and aged groups. It was observe a decrease between the comparison of the total fibers density and GO fiber, and an increase of the O fiber in aged group. Ultrastructural characteristics of muscle cells in aged group showed typical morphological changes, characterizing muscular atrophy. We conclude based on physiological ageing process, changes in muscle fibers classification, and ultrastructuraly, morphological alterations on muscle cells, characterizing a muscular atrophy.     

单个大鼠胎肝干细胞的激光光镊喇曼光谱

激光光镊喇曼光谱系统是将激光光镊与喇曼光谱相结合的一项光学技术,可以在接近自然的生理状态下研究单个生物细胞的识别及其构成成分的检测.本文采用胶原酶消化法,分离10~21天不同孕期大鼠的胎肝干细胞和成体大鼠的肝实质细胞,应用激光光镊喇曼光谱技术检测分离到单个胎肝干细胞和肝实质细胞,以及WB-F344大鼠肝干细胞系细胞,并比较了胎肝干细胞和肝实质细胞的喇曼光谱.结果发现,13天以前孕大鼠胎肝干细胞在1 336cm-1(代表多聚核苷酸链(嘌呤))和1 446cm-1(代表蛋白的弯曲模型)处的峰依次增高,13天孕大鼠胎肝干细胞在1 336cm-1和1 446cm-1处的平均峰值最高,14天以后逐渐降低.结果表明激光光镊喇曼光谱系统可以鉴别不同孕期的胎肝细胞和成体肝实质细胞,分析胎肝干细胞的分化机理,为临床应用肝干细胞治疗奠立基础.     

硝酸镧对大鼠肝脏的亚慢性毒性实验研究

以大鼠为对象,连续用生理盐水和20,10,2,0．2,0．1mg.kg^-1La(NO3)3灌胃6个月后,观察了体重,肝体比变化;检测了血清中谷草转氨酶,谷丙转氨酶,碱性磷酸酶和δ－谷氨酰转移酶含量的变化,应用组织化学及透射电镜技术观察了不同剂量La(NO3)3对大鼠肝脏形态结构的影响。20mg/kg^-1La(NO3)3组动物体重增长缓慢,0．1mg.kg^-1La(NO3)3组动物体重增加较快;20mg/kg^-1La(NO3)3组肝脏汇管区有炎细胞浸润,有些肝细胞内有少量的脂滴,糖原减少,线粒体基质密度增高,有电子密度高的致密体,肝细胞核形态正常或轻度变形。     

实验性醋酸铅诱发鼠肾脏病理超微结构改变

观察了实验性醋酸铅诱发鼠肾病理超微结构改变。用不同剂量醋酸铅拔掺入饮水中自由钦用染毒,于染毒后第30、60、90天分别随机抽取动物处死并取其肾脏进行电镜观察。结果表明,5ppm剂量组染毒90天后可见肾小管上皮细胞、肉质网、基底膜、细胞器等发生形态或数量改变,随剂量增大,其改变亦甚。表明醋酸铅可诱发鼠肾病理超微结构的改变。     

噪声应激对大鼠免疫功能的影响

以SD大鼠为材料,分别给予80dB和100dB的噪声刺激,在第1、5、10、15、20d检测大鼠的免疫功能的变化,实验结果表明：机体由于噪声应激产生免疫抑制因子,导致T淋巴细胞转化和T淋巴细胞ANAE＋率显著下降;巨噬细胞的FC受体阳性百分率和对抗原的吞噬能力下降;B淋巴细胞的抗体形成及抗体效价降低,表明机体的细胞免疫、体液免疫和非特异性免疫功能下降。