金丝桃甙(hyperin)药理作用研究进展

金丝桃甙系锦葵科植物黄蜀葵中提取的有效单体，属黄酮醇甙化合物，临床上对很多疾病有很好疗效。具有镇痛，保护脑缺血损伤等作用，并对钙离子内流有影响。本文综述近年来金丝桃甙的临床应用及药理研究的概况。     

金丝桃甙镇痛作用的机制

用小鼠光热辐射甩尾模型证明,低钙和高钙分别能增强和拮抗Hyp的镇痛作用。在痛介质诱发传入神经放电的模型上,同样证明低钙或高钙能显著加强或拮抗Hyp对组胺和氯化钾诱发神经放电的抑制作用。促进Ca²⁺内流的A₂₃₁₈₇几乎完全拮抗Hyp的末梢镇痛作用,并且在蛙坐骨神经标本上,Hyp可抑制KCl诱发的Ca²⁺内流。提示Hyp的镇痛作用与减少感觉神经末梢Ca²⁺内流有密切关系。     

金丝桃甙中枢镇痛作用及其机制的研究

金丝桃甙5μg/只(20g)侧脑室注射,经小鼠甩尾试验,热板法测痛,证实其有显著的中枢镇痛作用,其作用效价强度约等吗啡的1/20;相当于外周给药(腹腔给药)的100倍。用放射免疫法测得各脑区亮氨酸脑啡肽与金丝桃甙镇痛作用无关,纳络酮亦未能拮抗金丝桃甙的镇痛作用,但侧脑室注射CaCl_2和EGTA可分别拮抗和增强金丝桃甙的镇痛作用,并用原子吸收光谱法测得金丝桃甙产生镇痛作用时,小鼠脑内Ca~(2+)含量显著地减少。提示金丝桃甙中枢镇痛作用可能与降低脑内Ca~(2+)含量有密切关系。     

金丝桃甙的合成研究

金丝桃甙的合成研究蒋忠良，朱胄远，伍越环，王钟，周维善（中国科技大学化学系，合肥２３００２６；中国科学院上海有机化学研究所，上海２０００３２）金丝桃甙（Ⅰ）有抗过敏、解痉、抗胃溃疡和利尿等作用，且有显著止咳，降血压，降低胆固醇效果，无副作用（１～３）...     

广寄生叶中金丝桃甙的分离鉴定

从广寄生叶的乙酸乙酯萃取部分获得一种黄酮类化合物,由理化性质及光谱分析证明为金丝桃甙(hyperin)     

金丝桃甙对心肌脂质过氧化的影响

用ＴＢＡ法测定丙二醛（ＭＤＡ）含量，观察金丝桃甙（Ｈｙｐ）对阿霉素以及缺氧／再灌注所致心肌脂质过氧化的影响。结果表明：Ｈｙｇ１００ｍｇ·ｋｇ－１和ＥＧＴＡ４００μｍｏｌ·ｋｇ－１ｉｐ可明显抑制阿霉素所致小鼠心肌ＭＤＡ含量的升高，ＨＰＰ可增强ＥＧＴＡ的作用，Ａ２３１８７拮抗Ｈｙｐ的作用。ＨｙＰ１０、１００μｍｏｌ·Ｌ－１可显著减少缺氧；再灌注离体大鼠心脏ＭＤＡ的产生。提示Ｈｙｐ具有抗心肌脂质过氧化的作用，此作用可能与其阻滞钙内流有关。     

金丝桃甙诱变性研究

金丝桃甙诱变性研究余素贞，王家骥，宋必卫，马传庚，徐叔云（安徽医科大学，合肥２３００３２）ＭＵＴＡＧＥＮＩＣＩＴＹＴＥＳＴＳＯＦＨＹＰＥＲＩＮ￥ＳＨＥＳｕ－Ｚｈｅｎ；ＷＡＮＧＪｉａ－Ｊｉ；ＳＯＮＧＢｉ－Ｗｅｉ；ＭＡＣｈｕａｎＧｅｎｇ；ＸＵＳｈｕ－Ｙｕ...     

罗布麻中金丝桃甙的脉冲极谱测定

本文报道了罗布麻中金丝桃甙的提取、分离和脉冲极谱测定条件。罗布麻中含有较大量的金丝桃甙,生药用甲醇提取后用聚酰胺板分离,展开剂为氯仿—甲醇—水(4:1.5:0.1),用5 ml混合溶剂浸泡、洗脱,金丝桃甙在0.1 M硫酸铵底液中于—1.45V(vs SCE)有很好的峰形。     

秦岭三种金丝桃属植物药中金丝桃甙的含量测定

用薄层一紫外分光光度法测定了秦岭地区三种金丝桃属植物药贯叶连翘、红旱莲、大对经草中金丝桃甙的含量。结果以红旱莲含金丝桃甙为最高，达１．１７２％。     

八厘麻毒素对豚鼠心乳头肌膜电位及收缩力的影响

用固定频率起搏的离体豚鼠心乳头肌标本,研究了RTX对心肌膜电位及收缩力的影响。结果表明:RTX增加心肌Fc,降低RP和APA,缩短APD₂₀和APD₅₀,其降低RP的作用与其增加Fc的作用相平行。RTX的全部效应均是时间和浓度依赖性的。在给RTx前和后加用TTX能分别减弱和逆转RTX的作用,并能迅速抵消RTX所诱发的自动节律活动。本实验结果提示:RTX能选择性地作用于心肌快Na⁺通道,与TTX有拮抗作用,似可作为研究心肌离子转运的工具药之一。     

THE EFFECT OF VASOPRESSIN ON HEPATIC ARTERY FLOW IN THE RAT

The effects of vasopressin infusion on hepatic artery flow was studied in rats. Hepatic artery ligation followed by the infusion of vasopressin (0.08 microU/g body weight per min) decreases portal venous flow and liver blood flow. Vasopressin infusion results in an increase in hepatic artery flow and liver blood flow both of which are abolished by subsequent hepatic artery ligation. The increase in hepatic artery flow and the decrease in portal venous flow following the infusion of vasopressin is discussed in relation to the management of patients presenting with bleeding oesophageal varices.     

THE EFFECT OF THE CALCIUM ION ANTAGONIST 8-(N,N-DIETHYLAMINO)-OCTYL-3,4,5-TRIMETHOXYBENZOATEON MALIGNANT HYPERPYREXIA-SUSCEPTIBLE PORCINE SKELETAL MUSCLE

In malignant hyperpyrexia susceptible (MHS) porcine skeletal muscle, a low concentration (100 mumol/l) of the calcium ion antagonist 8-(N,N-diethylamino)-octyl-3,4,5-trimethoxybenzoate (TMB-8) inhibited KCl-induced contractures, but potentiated contractures induced by halothane, caffeine and succinylcholine. Higher concentrations of TMB-8 (333 mumol/l to 1 mmol/l) contracted MHS muscle, but had little effect on muscle tension in control preparations. Treatments which inhibit excitation-contraction coupling abolished TMB-8-induced hyper-reactivity in MHS muscle. TMB-8 (50 mumol/l and 1 mmol/l) did not alter 45Ca2+ levels in actively loaded microsomal preparations from MHS swine. These results suggest that in malignant hyperpyrexia the primary abnormality occurs proximal to the release of calcium from the sarcoplasmic reticulum, probably at the level of excitation-contraction coupling.     

THE EFFECT OF ETHANOL ON THE RESPONSE OF HAND BLOOD FLOW TO DISTANT ICE APPLICATION

SUMMARY 1. The effect of orally administered ethanol on the vasoconstrictor response of hand resistance vessels to application of ice to the neck has been studied in normal subjects.
2. Ethanol significantly reduced the ice response.
3. The mechanism of this blocking action is obscure, but a central inhibitory action, possibly at the ponto-medullary vasomotor centre level, is postulated.     

EFFECT OF NG-M0N0METHYL-L-ARGININE ON THE MICROCIRCULATION OF RAT SKIN

1. The effects of N^G-monomethyl-L-arginine (L-NMMA), a nitric oxide (NO) synthase inhibitor, on the microcirculation of rat dorsal skin were studied to examine the role of NO in the regulation of regional haemodynamics. 2. The blood volume in the skin microcirculation, which was continuously measured by reflectance spectrophotometry, was significantly decreased in response to L-NMMA (10 mg/kg bodyweight, i.v.), suggesting vasoconstriction, and the response continued for more than 20 min. In contrast, the increase in systemic blood pressure (BP) disappeared soon after administration of L-NMMA. 3. These results show that L-NMMA elicits long-lasting responses in the skin microcirculation, whereas the systemic BP rapidly recovers, suggesting a large contribution of the NO system to the regulation of rat skin microcirculation.     

CHLORIDE ION INGESTED WITH SODIUM AFFECTS THE DEVELOPMENT OF CEREBRAL LESIONS IN STROKE-PRONE SPONTANEOUSLY HYPERTENSIVE RATS

1. To determine the effect of chloride ion on the development of hypertension and the incidence of cerebral lesions in stroke-prone spontaneously hypertensive rats (SHRSP), groups of 10 rats were administered chronically with either 171 mmol/L sodium chloride or equimolar sodium provided as sodium citrate in the drinking water from the age of 12 weeks. 2. The life span was significantly extended in SHRSP given sodium citrate (336 +/- 28 vs 246 +/- 26 days, mean +/- s.e.m., P less than 0.05) but their development of hypertension was not different from SHRSP given sodium chloride. 3. In order to determine the role of calcium homeostasis, calcium in urine was collected. Urinary calcium in SHRSP given sodium citrate was significantly decreased (1.0 +/- 0.12 vs 1.8 +/- 0.18 mg/24 h urine, P less than 0.05). 4. If the normal life span is 320 +/- 35 days, this suggests that chloride ion ingested with sodium accelerates the development of cerebrovascular diseases, and that increased urinary calcium excretion may be related to this adverse chloride effect on the development of hypertension in SHRSP.     

4'-甲基立可定对冠脉血流和家兔实验性心肌梗塞的影响

实验表明4′-甲基立可定具有增加家免冠脉血流量和小白鼠心肌营养性血流量的作用,但对家兔心肌收缩力和心率无明显影响。通过对家兔实验性心肌梗塞疗效的观察,证明4′-甲基立可定可改善结扎冠脉后引起的心电图变化,表现为∑ST明显降低,NST和TO显著减少,NBT染色法也证明用药后梗塞心肌的重量明显减轻。与立可定进行对比研究指出,二者作用基本相似,唯后者增加心肌营养性血流的作用不够明显。     

THE EFFECT OF PHENOXYBENZAMINE AND SARALASIN ON THE ALTERED RENAL BLOOD FLOW DISTRIBUTION IN BABOONS WITH OBSTRUCTIVE JAUNDICE

1. Using the ¹³³xenon (¹³³Xe) washout technique, renal cortical perfusion was measured in fourteen baboons before and 1 and 2 weeks after ligation of the common bile duct. 2. In the 1-week group (seven animals), ligation of the common bile duct caused no significant changes in cortical perfusion in comparison with preligation values. 3. Intrarenal infusion of the angiotensin II blocking agent, saralasin, at a rate of 0.1 mmol/min caused no change in cortical perfusion in the 1-week group. However, an infusion of 0.3 mmol/min of the α-adrenoreceptor blocking agent, phenoxybenzamine, caused significant increases in outer cortical flow over control (P < 0.05) and 1-week values (P < 0.05). 4. In the 2-week group (seven animals), ligation of the common bile duct caused a non-significant decrease in outer cortical flow and a significant decrease in the percentage distribution of radioactivity distributed to the outer cortex (P < 0.001). 5. A 0.1 mmol/min intrarenal infusion of saralasin had no effect on outer cortical flow in the 2 week group, but significantly raised the percentage distribution of flow to the outer cortex (P < 0.001) over the 2-week value. An intrarenal infusion of 0.3 mmol/min phenoxybenzamine in the 2-week group significantly increased outer cortical flow levels over the 2-week (P < 0.001) and control (P < 0.05) values. The percentage distribution to the outer cortex was also significantly raised (P < 0.001) over the 2-week values. 6. There was a significant correlation between the changes in outer cortical blood flow induced by phenoxybenzamine at 1 and 2 weeks and the percentage increases in total serum bilirubin (r= 0.802, P < 0.001) and cholesterol (r= 0.668, P < 0.01) plasma levels over baseline values. 7. These results demonstrate that in baboons with experimentally-induced obstructive jaundice there is increased activity of the renal a-adrenoreceptors, and when renal cortical vasoconstruction is present, the renin-angiotensin system may also be activated and contributes to the cortical vasoconstriction.