牛磺酸对心血管系统保护作用及发生机制研究综述

牛磺酸的生物学功能非常广泛,不仅具有抗心肌纤维化、促进神经系统发育、抑制细胞凋亡、减轻细胞钙超载、促进脑部神经细胞增殖分化、修复血管内皮功能以及抑制血管平滑肌细胞增殖等作用,而且还能够促进胆固醇的排泌和代谢。同时,牛磺酸对防止血管疾病介入治疗后再发生狭窄以及防治心血管疾病亦有重要作用。现将牛磺酸对心血管系统保护作用及其发生机制进行综述。     

牛磺酸对大鼠高血压的影响

在大鼠腹主动脉狭窄和高盐摄入引起的高血压模型上,观察到口服牛磺酸治疗可显著降低动物血压,(20.8±4.0kPa VS非治疗组27.3±3.2 kPa.P<0.01)抑制高血压动物血浆CGRP的减少.改善动物血管条的舒张反应。实验结果提示,牛磺酸可能具有临床上抗高血压作用。     

牛磺酸镁抗心律失常的实验研究

牛磺酸(Taurinc)和镁离子(Mg~(2 ))分别具有多种心血管药理作用,业已证明两药合用抗心律失常作用得到加强。中国科学院新药研究基地对两药结构进行改造,合成新型化合物——牛磺酸镁,此类化合物及其作用的研究尚少见报道。研究表明牛磺酸镁具有明显的心血管药理作用,对实验性心律失常显示良好治疗学效果。     

牛磺酸对心血管的药理作用

<正> 牛磺酸(Taurine)是动物体内的一种含硫氨基酸,分子量125u。它是牛胆汁成份之一,因此得名。以后发现牛磺酸广泛分布于脊椎动物某些器官,其作用不限于合成胆酸而具有较广泛的生物活性。牛磺酸对中枢神经系统和心血管系统均有明显作用,已用于解热抗炎、抗癫痫、治疗心力衰竭。牛磺酸几无毒性,但过量时可引起心律失常。     

牛磺酸镁对家兔离体心房不应期和兴奋性的作用

目的:研究牛磺酸镁对家兔抗心律失常作用的机制.方法:制备家兔离体心房,以电生理学方法观察牛磺酸镁对其不应期和兴奋性的影响.结果:牛磺酸镁可显著延长离体心房的不应期,且呈剂量依赖性;而对其兴奋性作用很小,无统计学差异.结论:牛磺酸镁可通过延长心房不应期而发挥抗心律失常作用.     

高浓度牛磺酸滴眼液的制备

牛磺酸是一种具有多种生理功能的β-氨基酸,化学名称为氨基乙磺酸,临床上具有解热、解毒、镇静、抗炎和加强免疫功能等作用。曾有报道,其在视皮质内的正常含量,对神经细胞的健康发育起重要作用,动物实验结果表明,缺乏牛磺酸可引起严重的视网膜及脉络膜退化。眼科临床近年来使用5％牛磺酸滴眼液治疗各种结膜炎症,有着较好的疗效。作者自1989年以来,提高其浓度,     

牛磺酸抗藜芦碱实验性心律失常作用

大白鼠静脉注射藜芦碱(Veratrine)1mg/kg 可诱发实验性心律失常,并能被阿托品部分对抗,表明心律失常的发生与迷走神经活动增强相关。本实验结果证明,牛磺酸(Ta-urine)可以预防藜芦碱引起的心律失常,使其发生率减少,持续时间缩短,机制尚不清楚。曾有报道;牛磺酸具有抗中枢胆碱能神经作用,故其抗心律失常作用也可能与其减弱迷走神经的活动有关。牛磺酸是体内重要的氨基酸,中枢神经系统含量较多,心肌组织亦较丰富,约占心肌所含氨基酸的1/2。有报道牛磺酸治疗地高辛、肾上腺素所致实验性心律失常有效。本实验观察不同剂量牛磺酸防治藜芦碱心律失常的作用,并对其作用机制进行初步探讨。     

牛磺酸增强渐增再灌注心肌保护作用的实验研究

目的研究牛磺酸对渐增再灌注处理的离体大鼠缺血/再灌注损伤心肌的保护作用。方法采用Langendorff离体心脏灌流法制备离体大鼠心肌缺血/再灌注模型。SD大鼠随机分为7组:正常对照组(Nor)、缺血/再灌注组(I/R)、渐增再灌注组(GR)、牛磺酸低浓度组(T20)、牛磺酸高浓度组(T40)、渐增再灌注联合牛磺酸低浓度组(GT20)、渐增再灌注联合牛磺酸高浓度组(GT40)。记录平衡末及再灌注90min心功能,TTC染色法测定心肌梗死面积,检测冠脉流出液中乳酸脱氢酶(LDH)活性及心肌组织中Caspase-3活性,TUNEL法检测心肌细胞凋亡。结果与缺血/再灌注组比较,GR、牛磺酸能够改善心功能,减少心肌梗死面积,减少LDH漏出,降低心肌Caspase-3活性并减少心肌细胞凋亡;相比单纯应用GR及牛磺酸,渐增再灌注联合牛磺酸的保护作用更强,且GT40组保护作用最强。结论 GR和牛磺酸均能减轻大鼠离体缺血/再灌注心肌的损伤,牛磺酸,特别是高浓度牛磺酸能够增强渐增再灌注对心肌的保护作用,抗凋亡可能是二者发挥心肌保护作用的机制之一。     

牛磺酸的降压作用

牛磺酸Taurine(Z-aminaethane Sulfonie acid)是含硫氨基酸的一种,广泛分布于自然界,在机体内牛磺酸与胆汁酸结合成牛磺胆酸而存在于胆汁中,在心肌,骨骼肌,中枢神经系统中也大量存在。关于牛磺酸的生理作用,还有许多不明之处,在心血管系统方面,它具有使心肌细胞膜安定化作用及正性肌力和抗心律失常等作用。而且近年来有报告:对大白鼠自发的高血压症有抑制血压升高的作用;对原发性高血压患者有降压作用。本文就牛磺酸对循环系统特别是对血压作用论述如下。     

牛磺酸的多种临床用途

牛磺酸系动物体内存在的含硫氨基酸,80年代我国开始用于临床。由于本品的药理作用广泛,也无毒性,临床上已用以治疗支气管炎、扁桃体炎及眼炎等感染性疾病。因它具有解热和镇静作用,故可治疗感冒、乙醇戒断症状、癫痫与肌强直等症。牛磺酸还有利胆作用,故有用以治疗肝胆疾病、动脉粥样硬化、心衰与降低血糖。此外,牛磺酸对幼儿发育期的营养作用已引起普遍关注。     

Effect of taurine on calcium levels and contractility in guinea-pig ventricular strips

Taurine increases the calcium levels in guinea-pig ventricular strips at external calcium concentrations of 0.45, 0.9 and 1.8 mM. At 2.7 mM calcium, however, a decrease is observed. Analogous changes occur in contractile force. It is also seen that the superfusion of ventricular strips with taurine-free medium produces a decrease in taurine content at the end of 120 min superfusion. Taurine levels can be restored by superfusion with 10 mM taurine; a linear relationship exists between external taurine and internal taurine levels.     

牛磺酸对大鼠心肌Ca~(2+)调节作用的研究

研究了牛磺酸对大鼠离体左心室肌~(45)Ca内流的影响。对照组~(45)Ca内流与KH液中Ca_-~(2+)浓度有关。当Ca~(2+)浓度分别为0.62(低Ca~(2+)),1.25(正常Ca_-~(2+))和1.87(高Ca_-~(2+))mmol/L时,~(45)Ca内流相应为1.02±0.25,1.37±0.14,和1.45±0.14μmol/g。加入牛磺酸后,上述情况显著改变。低Ca_-~(2+),Tau 10、20、40mmol/L能分别使~(45)Ca内流增加为1.11±0.11,1.45±0.12和1.48±0.09μmol/g:正常Ca~(2+)时,Tau 10、20、40mmol/L能分别使~(45)Ca内流减少为1.19±0.07,1.14±0.23和0.97±0.24μmol/g:高Ca~(2+)时、Tau 10、20、40mmol/L能使~(45)Ca内流显著降低为1.12±0.05,0.58±0.18和0.53±0.10μmol/g。结果表明不同Ca~(2+)浓度能影响心肌~(45)Ca内流,牛磺酸对心肌~(45)Ca内流有双向调节作用,这可能在其抗心律失常机制中起重要作用。     

牛磺酸对肾病综合征大鼠血脂的影响

目的：研究牛磺酸对肾病综合征（ＮＳ）大鼠高脂血症的影响。方法：采用多柔比星加单肾切除的ＮＳ模型，观察牛磺酸对高脂血症的影响。结果：在持续６周后结束时，给予牛磺酸治疗的大鼠尿蛋白减轻（Ｐ〈０．０５），血尿素氮、血胆固醇、甘油三酯、低密度脂蛋白、极低密度脂蛋白较对照组（Ｐ〈０．０５）。结论：牛磺酸不仅可改善肾病综合征的高脂血症，并且具有保护肾功能作用。     

Studies on protein and taurine in normal, senile and diabetic cataractous human lenses

An attempt has been made to explore the possible role of Taurine in cataractogenesis. Normal lenses were obtained from eye bank donors and cataractous lenses from patients who had undergone surgery for cataract extraction. Lenses were weighed and homogenised. Extraction, isolation and estimation of protein and taurine were carried out. It has been found that the lens wet weight increased progressively with the stage of maturation of cataract, i.e., from mature to hypermature which was significant and also with increase in age. Diabetic cataract group also showed an increase similar to that of senile cataract. Taurine and total protein decreases with different stages of maturation of cataract but not with age. It may be suggested that in the process of development of human senile cataract, there is (a) alteration in the structural integrity and permeability of lens membrane to protein and amino acids including taurine, (b) changes in the lens function including possible inhibition of proteins and amino acids (taurine) synthesis and transport across the cell membrane.     

PITC柱前衍生化法测定保健食品中牛磺酸的含量

目的 建立液相色谱法测定保健食品中牛磺酸含量的方法.方法 采用C18色谱柱,以异硫氰酸苯酯(PITC)做为柱前衍生化试剂,以醋酸钠缓冲液-乙腈-水体系为流动相,流速为1.0mL·min-1,在254nm波长处检测.结果 牛磺酸在0.28～0.95μg范围内与峰面积呈良好线性关系(r=0.9998),液体、固体保健食品的平均回收率均为95.6％,RSD分别为1.5％和0.8％(n=6).结论 该方法结果准确,稳定可靠,重复性好.     

Taurine: a particular aminoacid with multiple functions

Taurine has multiple biological and metabolic functions: this particular B-amino acid is an antioxidant, it conjugates biliary acids, detoxifies some xenobiotics and modulates intracellular calcium levels. Moreover, taurine plays an important part in osmoregulation, neuromodulation and stabilization of the membranes. Taurine is looked upon as an "essential amino acid" in some particular situations associating inadequate intake or synthesis and major loss of biliary salts. Clinically, taurine has been used with varying degrees of success in the treatment of several pathologies (cardiovascular diseases, cystic fibrosis, alcoholism, retinal degeneration, hepatic disorders). Being found in the secretions of the mammalian reproductive tract, it preserves the motility of the spermatozoa, supports their capacitation, improves the chances of success of fertilization and the early embryonic development. This is why it can be found in some culture media for in vitro fertilization.     

Taurine analogues; a new class of therapeutics: retrospect and prospects

Taurine was discovered more than two hundred years ago from animal sources. It is distributed in both mammals and non-mammals and its content is high in several tissues. For more than a century-and-a-half, taurine was regarded just as an end product of sulfur metabolism. Recently, taurine has been rediscovered and its beneficial effects in processes like epilepsy, hypertension, congestive heart failure and diabetes have been well-documented. It was patented and found some clinical utility, but being an amino acid, therapeutic use confronts limitations like restricted permeability and more. This necessitates the development of pro-drugs (analogues) mainly derivatives of taurine. A large number of taurine derivatives have been reported in the literature with partial to marked activity. Taurine derivatives like taltrimide, acamprosate and tauromustine, are already in the market as anti-convulsant, anti-alcoholic and anti-cancer agents. Many other analogues are effective in experimental models. The in depth analysis of these analogues and their biological actions can provide certain clues for further consideration. In the present review, attempts have been made to provide synopsis, synthesis and symbiosis of chemical and biological actions, which may provide future guidance and facilitate further research in this area. The successful journey of these analogues to clinical utility is a healthy and happy sign and an index of bright future, and we hope that this review will provide enough input to ignite the minds.     

牛磺酸对皮质神经元急性氧糖缺失所致损伤的保护作用(英文)

目的已证实牛磺酸对在体脑缺血有保护作用,本研究观察其对缺失氧糖的离体神经元是否有直接的保护作用及可能的作用机制。方法制备离体大鼠脑皮质神经元的氧糖缺失模型。在氧糖缺失前20 h及氧糖缺失4 h过程中,分别给予牛磺酸5,10和20 mmol·L-1。MTT法和流式细胞术检测神经元的死亡率;Fura-2/AM负载检测神经元内游离钙离子水平([Ca2 +]i);高效液相色谱法检测培养基中谷氨酸水平。结果氧糖缺失可致神经元死亡增加,[Ca2 +]i和培养基中谷氨酸水平异常升高;牛磺酸处理可使氧糖缺失引起的神经元死亡率明显降低,抑制氧糖缺失引起的神经元[Ca2 +]i和胞外谷氨酸浓度的异常升高。结论牛磺酸可以减轻氧糖缺失引起的大鼠皮质神经元损伤,其机制可能与其抑制胞内钙超载和抑制谷氨酸释放或漏出有关。     

牛磺酸对急性局部脑缺血大鼠脑血流和脑梗死体积的影响

目的 :研究牛磺酸对脑缺血再灌注模型大鼠的局部脑血流和脑梗死体积的影响。方法 :用大脑中动脉栓塞 (MCAO)法制作大鼠急性局部脑缺血再灌注模型 ,分别用 10 ,4 0和 80mg·kg- 1牛磺酸经腹腔注射给药 ,检测缺血 1h和灌注 30min内脑血流 ,再灌注 2 4h后进行神经功能缺损评分并计算脑梗死体积的大小。结果 :MCAO引起大脑中动脉供血区脑血流显著下降 ,牛磺酸可减少脑血流量下降的幅度 ;缺血 1h再灌注 2 4h后 ,模型组脑梗死体积为 (33±s 9) % ,而牛磺酸治疗组脑梗死体积明显缩小 ,各组分别为 (17± 5 ) % ,(12± 5 ) %和 (11± 3) % ;牛磺酸治疗组神经缺损评分比模型组小。结论 :牛磺酸可以增加缺血局部的脑血流量 ,缩小脑梗死体积 ,对急性脑缺血具有脑保护作用。     

Review of Some Actions of Taurine on Ion Channels of Cardiac Muscle Cells and Others

• 1.Taurine has recently been known to protect against ischemia and heart failure. Taurine possesses plenty of actions on the ion channels and transports, but is very non-specific.
• 2.Taurine may directly and indirectly help to regulate the [Ca]_i level by modulating the activity of the voltage-dependent Ca²⁺ channels (also dependent on [Ca]_i/[Ca]_o), by regulation of Na⁺ channels, and secondly via Na-Ca exchange and Na⁺-taurine cotransport.
• 3.Taurine can prevent the Ca²⁺ ([Ca]_o or [Ca]_i)-induced cardiac functions.
• 4.Therefore, it seems possible that taurine could exert the potent cardioprotective actions even under the condition of low [Ca]_i level as well as under the Ca²⁺ overload condition.
• 5.The electrophysiological actions of taurine on cardiomyocytes, smooth muscle cells, and neurons from recent studies are summarized.