Screening of anti-experimental epilepsy of Stellera chamaejasme L. extract

Screening of anti-experimental epilepsy of Stellera chamaejasme L. extract

Screening of anti-experimental epilepsy of Stellera chamaejasme L. extract
【Abstract】 Objective To compare the pharmacodynamics and toxicity of six extracts of Stellera chamaejasme L. (in turn, Stellera chamaejasme, exudates, acetone, petroleum ether, B, and ethanol extracts). Low-toxic anti-epileptic compounds for easy preclinical mechanisms. Methods Three kinds of convulsion models of animals were used to determine the half effective dose (ED50) of six extracts of Stellera chamaejasme L. against experimental epilepsy. Calculate its median lethal dose (LD50). Results The extracts of Stellera chamaejasme L. Ë ~ Î, namely acetone, petroleum ether, B, and ethanol extracts on mice with maximum electroshock attack (M ES), pentylenetetrazol convulsion (M ET) and electrical stimulation The rat cortical convulsion threshold (TL S) model has a strong antagonistic effect. Among them, acetone extract is less toxic and the therapeutic index is as high as 1419. Conclusion The acetone extract of Stellera chamaejasme L. is a promising anti-epileptic compound with strong anticonvulsant effect and low toxicity.
【Key words】 Epilepsy, Stellera chamaejasme, extract, screening
Since the discovery of the alkaline extract of Stellera chamaejasme L. has strong anticonvulsant and antiepileptic effects, it has further carried out Stellera cham aejasm e L. (for the medicinal root radix stellerae). A large number of basic studies have found that Stellera chamaejasme has stronger anticonvulsant and antiepileptic activity, but so far, no reports of anticonvulsant and antiepileptic have been reported. In this paper, the anti-experimental epilepsy effect (ED50) and the LD50 of six extracts of Stellera chamaejasme L. were used to screen the high-efficiency and low-toxicity acetone extract, which facilitated further preclinical mechanism research.
1 material
111 Animals: 660 Kunming mice, 6-8 weeks old, weighing (22±4) g, both male and female. Seventy-two female rats, 3 to 4 months old, weighing (180 ± 20) g, were provided by the Experimental Animal Center of the school.
112 Drugs and preparation: Six extracts of Stellera chamaejasme, virgin, acetone, petroleum ether, B, and ethanol (extract: É~ Î) were provided by Shenyang Pharmaceutical University. Before the experiment, the water extract, the raw material and the acetone extract were prepared with distilled water; the petroleum ether, the B, and the ethanol extract were mixed with distilled water and 2% Tween 013 mL to prepare different concentration suspensions. Tetrazolium was purchased from the Dutch Epilepsy Research Center and formulated with distilled water to the desired concentration before the experiment.
113 instruments: maximum electrical shock convulsion experimental electrical convulsion instrument; electrical stimulation rat cortical convulsion threshold measurement
Use the convulsion threshold automatic meter.
2 methods
211 anti-experimental epilepsy
21111 maximal elect ro shock seiz2ure test (M ES): slightly improved by the Sw inyard method. Two ear electrodes were used to clamp the tip of both ears of the animal, and then 013 s was stimulated by 8 Hz, 110 V alternating current, and the limb rigidity was observed or not [1]. Animals were screened 24 h before the experiment, and no irritation of hind limbs or insignificant response was observed. The qualified mice were divided into 5 groups, 10 rats in each group, respectively, and different doses of the same extract suspension were injected intraperitoneally. The anti-M ES effect was determined after 2 h, and the six extracts of Stellera chamaejasme L. were calculated by B liss method. Anti-M ES ED50 value and 95% confidence limit.
21112 rt tetrazol seizure test (M ET ): qualified mice were divided into 6 groups, 10 in each group, 5 of which were intraperitoneally injected with different doses of the same extract suspension, normal control The group was intraperitoneally injected with equal volume of distilled water plus 2% Tween. After 2 hours, pentylenetetrazol 100 mgökg was injected intraperitoneally to determine whether the extract could prevent pentylenetetrazol-induced systemic convulsions as an indicator, and observe 5 min. All normal mice in the normal control group developed clonic convulsions within 50 s after pentylenetetrazol injection. The six extracts were calculated for anti-M ET ED50 and 95% confidence limits.
21113 Electrostimulation of rat cortical convulsion threshold (th resho ld fo rlocalized seizure, TL S): The experimental rat urethane 5 mLö kg was anesthetized by intraperitoneal injection and fixed on the animal brain stereotaxic instrument for aseptic surgery. According to the method of Vo skuyl et al [2], two 112 mm diameter stainless steel electrodes were implanted into the frontal cortex motor area on both sides of the brain, and the cement was fixed by the cement. Rat convulsion threshold was measured by electrical stimulation convulsion threshold automatic tester 1 week after operation. Stimulation parameters: one-way ramp trapezoidal bipolar pulse; wave width 2 ms; intensity from 15 to 1 000 LA within 15 s, daily stimulation 2 times, so that the forelimb paralysis or facial fibrillation and half body sputum Stimulation is stopped, and the stimulus intensity (LA) is used as the threshold for convulsions. After 1 week of continuous stimulation, the convulsion threshold was stabilized and used for the experiment. The experiment was divided into 3 groups, 6 in each group, all stimulated 3 times, and the mean value was taken as the pre-drug convulsion threshold. Then, different doses (the same amount of the original drug) were injected intraperitoneally with the same extract of the test substance Ë~ Î, and the same threshold parameters were stimulated 2 hours after the drug, and the elevated threshold was recorded.
212 LD50 determination
Healthy mice were divided into 5 groups, 10 rats in each group, and different doses of the same extract suspension were intraperitoneally injected to observe the number of deaths in 24 h mice. The B liss method calculates the extract of Stellera chamaejasme Ë~ Î LD50.
213 statistical methods
The results were expressed as xq±s, and the experimental data were analyzed by u test and factorial analysis.
3 results
311 Anti-M ES effect (ED50): See Table 1. The four extracts of acetone, petroleum ether, B, and ethanol in the six extracts of Stellera chamaejasme L. were effective against mouse M ES and had a dose-dependent antagonistic effect on M ES.
312 Anti-M ET effect (ED50): See Table 1. The four extracts of acetone, petroleum ether, B, and ethanol in the six extracts of Stellera chamaejasme have different degrees of antagonistic effects on M ET, and have a dose-dependent effect on M ET.
313 Anti-TL S effect: The extraction threshold of extracts 60, doses of 60, 90, 120 mg were 141±49, 256±83, 305±81, respectively; extract Ì, doses of 500, 750, 1 000 mg The thresholds for elevation were 141±49, 198±70, 244±62, respectively. The thresholds for extract Í, doses of 160, 240, 320 mg were 168±79, 305±90, 277±119, respectively; extract Î The elevated thresholds for doses of 400, 600, and 800 mg were 152 ± 45, 136 ± 89, and 261 ± 94, respectively. The middle dose group of the four extracts was compared with the low dose group P < 0101, and the high dose group was compared with the low dose group P < 01001. Four extracts also increased rat TL S, and the same extract was positively correlated.
314 LD50 determination: See Table 1. Among the four extracts, acetone extract was less toxic, and its LD50 was significantly different from petroleum ether, B, and ethanol extracts (P < 0101), and the therapeutic index was as high as 1419.
4 Discussion
This experiment was the first to find that Stellera chamaejasme has anti-epileptic activity. The results of pharmacodynamic experiments showed that the four extracts of Stellera chamaejasme L., acetone, petroleum ether, B, and ethanol extracts were effective against the maximum electroconvulsive seizures in mice, and there were different degrees of pentylenetetrazol convulsions. The antagonistic effect. The four extracts also improved the threshold of convulsions induced by electrical stimulation in the cortical motor area of ​​rats, and the positive extract of the same extract was positively correlated, further affirming its anticonvulsant effect. The toxicity test (Table 1) showed that the acetone extracts were less toxic in the four extracts, and the LD50 was significantly different from that of petroleum ether, B, and ethanol extracts (P < 0101). The therapeutic index is as high as 1419.
The above results fully indicate that Stellera chamaejasme L. is a promising Chinese herbal medicine, and it is expected that the acetone extract of the anti-epileptic component of the drug can be further separated and extracted by high-tech means, and its chemical structure is analyzed to lay a material foundation for the targeted semi-synthetic antiepileptic drug. And provide a theoretical basis.

Hydrazine Compound Series

Carbohydrazide can act as an oxygen scavenger to prevent corrosion, especially in boiler feedwater systems, rocket propellant assemblies, color image and soap stabilizers, antioxidant rubber, boiler water deoxidizers and metal passivators. Carbohydrazide can also be used as an anticorrosive agent. Organic synthesis of intermediates.

CAS No. 497-18-7 EINECS 207-837-2

Molecular Formula CH6N4O Molecular Weight 90.08

Attributes:

Carbohydrazide is a white crystalline powder or granule. The effective content of carbohydrazide is from 98.0 to 100.0%.

Specifications:

Items

Index

Appearance

White crystal line powder or pellets

Active Content (%)

98.0-100.9%

PH (12% Solution, @ 25 ℃)

8.45±1.25

Free Hydrazine

≤250ppm

Chloride (Cl)

≤10ppm

Sulfate (SO4)

≤20ppm

Silica (SiO2)

≤10ppm

Copper (Cu)

≤1ppm

Iron (Fe)

≤4ppm

Sodium (Na)

≤4ppm

Lead (Pb)

≤4ppm

Moisture

≤0.2%

Packaging and storage:

Pack 25 kg or 50 kg with woven bags or fiber drums.

Store in a cool, dry, well-ventilated area away from incompatible materials. Please close the container when not in use.

Tert-Butyl Carbazate,Ethyl Carbazate,Benzyl Carbazate,Carbohydrazide,Acetyl Hydrazine

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