Gastrodin [English name]
[alias]
[Chemical Name] B-D- glucopyranoside, 4- (hydroxymethyl) phenyl-
[Fraction formula]
[Molecular weight] 286.27
[Physical properties] White prismatic clusters with double melting points of 96 ~ 98℃/ 145 ~ 148℃, (a) 160D-66.4 (c = 0.65, water). White needle crystal, melting point 154 ~ 156℃, (a)28D-59 (c = 1.97, methanol).
[Component Classification]
[pharmacological action] 1. Sedative and anticonvulsant effects: intraperitoneal injection of gastrodin can inhibit spontaneous activity of mice, resist the excitatory effect of caffeine, and prolong the sleep time of pentobarbital sodium, cyclohexylbarbital sodium and thiopental sodium, indicating that it has obvious synergistic effect with central depressants. Healthy people take gastrodin orally. According to the analysis of brain waves, it was found that the A wave index decreased and there was a sleepy wave pattern. Synthetic gastrodin can prolong the sleep time of mice induced by chloral hydrate, but has no obvious effect on passive activities of mice. Intraperitoneal injection of gastrodin in mice can antagonize clonic convulsion caused by pentylenetetrazol, prolong the latent period of convulsion, reduce or increase the mortality by half, and improve the tolerance of mice to convulsion threshold voltage. 2. Effect on cardiovascular system: Intravenous gastrodin can slightly lower the blood pressure of cats and slow down the heart rate of rabbits. Gastrodia elata injection can significantly enhance the nutritional blood flow of myocardium in mice and improve the hypoxia tolerance of mice. Synthetic gastrodin can accelerate the beating frequency, enhance the contractility and regulate the rhythm of myocardial cells. There was no significant difference between different dosage groups, and there was no effect on the general morphology of myocardial cells. However, the intracellular glycogen, ribonucleic acid, deoxyribonucleic acid, adenosine triphosphate, succinate dehydrogenase and lactate dehydrogenase were significantly increased in each experimental group. Gastrodin may have the effect of promoting energy metabolism of myocardial cells, especially obtaining energy under hypoxia. Using the cytopathological model of myocardial injury induced by MMC, it was observed that synthetic gastrodin could reduce the degeneration and necrosis of myocardial cells induced by MMC and significantly enhance the activities of SDH and LDH. This may be closely related to gastrodin promoting energy metabolism of myocardial cells and enhancing its anti-injury effect. 3. Antiepileptic effect: Gastrodin 1000mg/kg and 2000 mg/kg were injected intraperitoneally in lh, and then coriaria lactone 3 mg/kg was injected intramuscularly; 3000 mg/kg was injected into the ear vein half an hour ago. The results show that there is a tendency to prolong the latent period of epilepsy, reduce the degree of grand mal, shorten the course of grand mal, speed up its recovery process and reduce the mortality rate. The dosage of 2000 mg/kg or 3000 mg/kg can not only fight against small attacks, but also fight against serious attacks. 4. Other effects: Gastrodin and thiopental sodium have synergistic effect, which can prolong anesthesia time. In vivo rabbit intestinal experiments show that most animals have increased intestinal tension and increased intestinal peristalsis contraction, suggesting that it can slightly strengthen intestinal peristalsis. Gastrodin and gastrodin have the same pharmacological effects. From the analysis of pharmacological experiment results, it is considered that gastrodin is absorbed into the blood and then decomposed into gastrodin to play its role. 5. In vivo process: After taking gastrodin for 3 hours, only 5.2% dose of gastrointestinal radioactivity remained for 2 hours. The radioactivity in the blood increased rapidly, and T 1/2A only lasted for 6 minutes. The radioactivity in blood is maintained at a high level around1h. The elimination half-life of intravenous injection is 4.44 hours, and that of oral administration is 7.47 hours. Radioactivity is distributed in kidney, followed by liver, lung, heart, spleen and brain. Radioactivity can penetrate the blood-brain barrier, but the changes in the brain are inconsistent with blood. Radioactivity is mainly excreted from urine. The total radioactivity discharged from urine, feces and bile 24 hours after oral administration was 76.8% of the dose, of which 97% was discharged from urine. Mice were given the drug via tail vein, with three doses of 50, 100 and 200 mg/kg. Blood was taken from the tail at 2, 5, 10, 15, 30 minutes, 1, 4, 8 hours after administration, and radioactivity was measured. Results Radioactivity distributed rapidly in the body, but the dose was inconsistent with the distribution speed. The radioactive elimination rate increases with the increase of dose; It shows that when the dose is large, the excretion is accelerated and gastrodin is not easy to accumulate in the body. In the experimental dose range, the pharmacokinetic behavior of gastrodin 3H is nonlinear. The experiment also showed that 100 mg/kg was suitable for intravenous injection in mice. The pharmacokinetics of gastrodin in rats were different after 3 hours administration. The peak time (Tp) is after 8: 00 at the latest, the absorption rate constant (Ka) is after 20: 00, and the area under the blood radioactivity-time curve (ADC) is the smallest after 2: 00. [Toxicity] Gastrodin was given to mice by gavage, and no poisoning or death was found when the dose was 5000 mg/kg. Dogs took gastrodin 75 mg/kg, 1 time every day for 1 4 days, while mice took gastrodin 250 mg/kg, 375 mg/kg,1time every day for 60 days, which had no effect on the total number of red blood cells, white blood cells, platelets, liver, renal function and blood lipids.
[Toxicity]
[Adverse reaction]
[use]
[Source] The tuber of Gastrodia elata. An orchid plant, and the whole grass of Vanilla. ..