Pharmacological effects
1, the role of the cardiovascular system:
Antihypertensive effects: Uncaria decoction, ethanol extract, Rhynchophylline and rhynchophylline, whether for anesthetized animals or non-anesthetized animals, normal animals or hypertensive animals, regardless of intravenous injection or intragastric administration Antihypertensive effect. There is no rapid tolerance. Anesthetized rabbit intravenous injection of Uncaria decoction 2-3g/kg or anesthetized intravenous injection of the decoction 0.05g/kg, can make the blood pressure lower than the original level by 30-40% for more than 3-4 hours. Anesthetized cats were intravenously injected with 6.25 g/kg of civet decoction, total alkaloid hydrochloride was 20 mg/kg, and rhynchophylline hydrochloride was 20 mg/kg. Blood pressure showed three-phase changes: first, blood pressure decreased, and then quickly recovered. , and then fell again, the blood pressure reduction rate of 30-70%, 13.9-23.2% and 11.7-41.7%, respectively, to maintain 3-4 hours. However, decoction of Uncaria decoction for a long time will reduce the antihypertensive effect, and it is advisable to fry within 20 minutes. The degree of decompression of 3 g/kg of ethanol extract of Moring was similar to 2 g/kg of decoction. Intravenous injection of rhynchophylline 20mg/kg or rhynchophylline 20mg/kg all have antihypertensive effect; Rats fed rat rhynchophylla total alkali 50mg/kg. days 20 days or rhynchophylline 50mg/kg. days 15 days, All have significant antihypertensive effect. Kidney-type hypertensive rats were given intragastrical decoction of 8g/kg, rhynchophylline 50mg/kg and rhynchophylline 50mg/kg once daily for 15-20 days. 5 days began to decline, the 7th to 15th days to a minimum, the average blood pressure were 16.9mmHg, 12mmHg and 18mmHg; rhynchophylline 20mg/kg, intraperitoneal injection, can make the blood pressure on the day of the rats, medication for 8 days, the average drop Press 24mmHg. Twelve dogs were anesthetized and their blood pressure decreased after constant intravenous infusion of rhynchophylline total base 20 mg/kg; cardiac output increased first and then decreased slightly; total peripheral vascular resistance decreased significantly in the early stage of blood pressure reduction; heart rate significantly decreased; heart rate The amount has increased significantly. Rhynchophylline reduces blood pressure by decreasing peripheral resistance (early) and reducing cardiac output (later).
From the effects of Sinomenine on myocardiac mechanics in anesthetized dogs and cats, dp/dt was used as a multi-indicator comprehensive analysis. In the determination of dp/dt, the left ventricular wall muscle tension was measured with a strain gauge arch as a myocardial contraction. The force index, combined with a small load-dependent response, reflects the acute change in the level of contraction performance of sensitive VcE-type indicators, and observes the muscle strength effects of A. gondii. Intravenous injection of rhynchophylline 20mg/kg, significantly reduce the myocardial contractility index such as LVP, dp/dtmax, LVMT, Vpm, and Vmax; rhynchophylline can reduce intraventricular pressure, so TTI decreases, indicating myocardial energy and O2 Reduced consumption may have protective implications when the supply of the heart muscle is insufficient. Although Rhynchophylline has a significant negative inotropic effect and can reduce O2, however, the indicators tend to recover about 15 minutes after the drug, indicating that the effect of inhibiting myocardial contractility is reversible. The antihypertensive effect of the drug is related to the contraction of the myocardial contractility, in addition to the expansion of the blood vessels and the decrease of peripheral resistance. The isolated rabbit thoracic aortic strips were used to investigate the mechanism of rhynchophylline dilating blood vessels and compared with verapamil. Both can decrease the contractile tension caused by K+ and norepinephrine, and the effect of K+ contraction is significantly greater than that of norepinephrine. The two drugs significantly attenuate the intracellular Ca+ release portion of the norepinephrine contractile response, and cause K+ to go to The effect of adrenaline and Ca2+ was shifted to the right, and the maximum response pressure was low, indicating that Sinomenine blocks extracellular Ca2+ influx and intracellular Ca2+ release, and its characteristics are similar to that of verapamil. The rat vinegar extract of methanol gives intravenous injection of 0.1 mg/kg to rats, which also has strong and long-lasting antihypertensive effect.
Effects on hemodynamics: The hemodynamic effects of rhynchophylline on conscious rats showed that LVSP, Vmax, and dp/dtmax immediately decreased significantly, with decreases of -7.8%, -15.9%, and -23.2%, respectively. After 5, 10, and 20 minutes of maintenance, it gradually returned to pre-dose levels, with the LVSP being significantly higher than the pre-dose at 90 minutes. SAP, DAP, and MAP all also dropped immediately. The decrease in SAP's maintenance time was shorter than the last two items and recovered at 30 minutes. Although DAP also recovered slightly at 30 minutes, it was below normal at 60 minutes. MAP is always below normal during observation. From the absolute value and percentage of SAP and DAP decline, DAP is greater than SAP. The LVEDP increased significantly immediately after the drug was given, and fell to below the pre-drug level after 1 minute. HR immediately decreased significantly with a maximum change of 35.3%, which was consistently lower than pre-drug levels during the 90-minute observation period. The LVP-(dp/dtmax) P-1 LOOP was significantly reduced, most markedly at 1 minute after drug administration, and gradually returned to normal.
2, sedative and anticonvulsant effects: <unribble or ethanol extract 0.1g/kg intraperitoneal injection, can inhibit spontaneous activity of mice, maintain 3-4 hours, and can increase the activity of animals caused by caffeine, but even if Increasing the dose to 2.5 g/kg does not enhance the hypnotic effect of pentobarbital sodium, but it can delay the animal death time caused by large doses of pentobarbital sodium. The increase in dose to 5-10 g/kg still did not allow the animals to correct their righting reflexes. Intraperitoneal injection of 1g/kg of decoction of hook rattan and stem can reduce the excitability of rat cerebral cortex and impair the impulsive total ability. The positive condition reflex of some rats is affected and the reflex time is prolonged. There was no significant effect on inhibition of differentiation and non-conditioned reflexes.
Radix Astragali alcohol infusion 2g/kg subcutaneous injection, the guinea pig experimental epilepsy prevention and control, can prevent epilepsy occurred, but the relapse will be 3 days. At the same time, it can also prevent guinea pigs from causing irritability due to shearing in the epileptic area.
3, the impact of uterine smooth muscle contraction response: smooth muscle cell contraction response must be involved in the activation of contractile protein in the participation of Ca2+ can be achieved. The high K+ solution depolarizes the uterine smooth muscle and opens the potential-dependent Ca2+ channel (PDC) on the cell membrane, which induces the Ca2+ influx to induce a longer time contraction of the uterus. Verapamil relaxes this contractile response in a time and dose-dependent manner, suggesting that it inhibits PDC and blocks Ca2+ influx. Sinomenine also has the same effect, indicating that it may also inhibit PDC. Rhynchophylline also inhibited oxytocin-induced contraction of isolated uteri in rats and increased with increasing doses, and was counteracted by the addition of excess CaCl2 (2 mM).
4. Other effects: Alkaloids can inhibit ex vivo and in-flight frog hearts and rabbit hearts. And can inhibit the frog and mouse breathing and reduce the role of the pupil. Capillary alkaloids and dehydroabietin caprine ia anesthetize dogs at 3–1000 μg/dose, with dose-dependent diastolic hind limb blood vessels, similar in intensity to papaverine. Rhynchophylline exerted a dose-dependent inhibitory effect on the contraction of the colonic band after Ca2+ depolarization induced by acetylcholine or hyperkalemia. The dose-response curve showed that rhynchophylline antagonized CaCl2 in a non-competitive manner. Castanospermine has significant inhibition of platelet aggregation and antithrombotic effects on the electrophysiological effects of the myocardium as the dose increases.
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