Achyranthes Pharmacology Application
Pharmacological applications;
Assimilation of proteins
The quercetin contained in Achyranthes has a strong protein synthesis promoting effect. Two hours after intragastric administration or intracavernous injection of ecdysterone to the mice for 2 hours, the incorporation of amino acid precursors in the liver nuclei, mitochondria and microsomes of mice was increased, and the effect was stronger after 4 hours. At the same time, protein synthesis was also observed in the kidney, but it returned to its original level after 4 hours. The centrifugation analysis of the sucrose density sample showed that the administration of blood RNA had twice as much cast activity as the control blood, suggesting that the protein synthesis effect of ecdysterone is accompanied by at least the role of promoting m-RNA synthesis. When male deciduous male mice were continuously given ecdysteroids for 60 days, their body weight increased rapidly, and the protein synthesis of liver and kidney was also increased. Liver tissue examination showed hepatocellular hyperfunction.
Anti-inflammatory and analgesic effects:
Effect on croton oil ear swelling mice:
Thirty mice were randomly divided into three groups. The experimental group was injected with 0.5 ml/20 g of Achyranthes bidentata. Normal saline was injected into the control group. The results showed that the Achyranthes bidentata had significant inhibitory effect on oily ear swelling of Croton, and the effect increased with increasing dose.
Effects on formaldehyde-induced rat paw edema:
Twenty healthy rats were randomly divided into two groups, which were injected with 2.5% formaldehyde 0.1ml into the right and left iliac crest to induce inflammation. The left and right feet were their own controls. Intraperitoneal injection of Achyranthes 16.6 ml/(kg. days), the results showed significant differences between the experimental group and the control group (P <0.05).
The role of mice in the acetic acid-responsive mice Mice oral administration of Achyranthes bidentata decoction has a very significant analgesic effect.
Effects on the cardiovascular system
Effects on the heart: Achyranthes alcohol extract has certain inhibitory effects on isolated frog hearts and anesthetized cats. The effect of water decoction on anesthetized dogs' myocardium is more obvious.
Effects on blood pressure in animals: Achyranthes decoction has a temporary antihypertensive effect on anesthetized cats and dogs, and respiratory depression is associated with a decrease in blood pressure, and there is no rapid tolerance to hypotensive effect. It is speculated that the mechanism may be related to histamine. The release, cardiac inhibition and expansion of peripheral blood vessels are related.
Effect on the bowel
Rabbits were selected, and both males and females were used. The duodenum, jejunum, and ileum were selected. Each segment was 3-4 cm in length and was subjected to a smooth muscle routine experiment. Using 16 rabbits and 56 intestines and giving an alcohol extract, the intestine can be excited, the tone increased, the contraction force increased, and the change can be resumed soon after the change.
The role of the uterus
Effects on isolated rat uterus and smooth muscle:
Twenty-eight virgin rats (unpermanent cycle smears) were randomly selected and the body weight was 230±SDI 7.3g. The isolated uterine specimens were prepared according to the conventional method. The uterine muscle segment length was 1.5 cm and placed in a thermostatic trough containing DeJaoln solution I. Internally (20 ml), the baseline tension was adjusted to 1.5 g, and the experiment was started after equilibrating for 30-60 minutes with continuous 95% O2+5% CO2 (32±0.5° C., pH=7.4-7.6). The muscle force transducer was connected during the experiment and the uterine contraction activity was traced by a bench-top auto-balance recorder. The area under the uterine contraction curve (abbreviated as the uterine contraction area, UCA) was calculated as the index by a planimeter. Observed the effects of 4 different doses of A. saponins on the uterus of isolated pregnant rats. Achyranthes bidentata has obvious stimulatory effect on rat uterine smooth muscle. The amplitude of uterine contractions increased after administration, and the frequency increased and the tension increased. The main is the regular rhythmic contraction, and there is rarely spastic contraction. UCA was significantly increased (P<0.001) before administration. From the UCA within 10 minutes after administration, UCA increased correspondingly with dose. The peak of UCA in each group also gradually advanced, and the latency of uterine contraction shortened accordingly. Ten samples were randomly selected from each dose group of the above experiment, and light was administered once. After 3 minutes of action, the liquid was flushed three times. After the specimens were recovered, they were administered again one time. Repeated administration to the uterus smooth muscle was observed. effect. The results showed that with the increase of administration dose, the effect of total saponin from Achyranthes bidentata on excitability of uterine smooth muscle was remarkably weakened when the dose was repeatedly administered. When the dose was increased above 0.5 mg/ml, re-administration did not cause significant uterine smooth muscle excitability.
Effects of drugs on the uterus under different physiological conditions:
28 female rats were used, 4 of them were young rats (within 7 weeks of age), weighing 104±SD 2.8g, and the rest were mature non-pregnant or B-pregnant rats, weighing 226.8±SD 15.5g. The pregnancies of mature rats before vaginal smears, deterministic cycle, according to the Turner CD's method of partial cycles, select estrus, intercourse rats. Pregnant rats are divided into 3 types of pregnancy according to pregnancy: within 7 days for early pregnancy, 8 to 14 days for the pregnancy, and 15 days for the late pregnancy. Another 4 rats were consecutively subcutaneously injected daily. Diethylstilbestrol 0.1 mg/kg for 2 days resulted in an artificial estrus period for the experiment. The experimental methods were the same as before. Each group of experiments used 8 to 10 specimens to compare the effects of 0.5 mg/ml total alfalfa on the uterine smooth muscle under different physiological conditions. The results are shown in Table 5. Within 10 minutes before administration, UCA was significantly higher in each pregnancy group than in the non-pregnant group (P<0.05). UCA increased after administration in each group. The increase was ranked in order of size: late pregnancy group> early pregnancy group> intercourse group> middle pregnancy group, diethylstilbestrol group, estrous group> young group. The youngest group was the lowest, and the youngest group was the highest.
Comparison of the effects of Achyranthes total saponin on cervix and uterine horn of unpregnant rats: 12 cervix and cervix specimens of non-pregnant rats were used in the experiment, and the length of the specimen was 1-1.5cm. The experiment was performed according to the above method. Achyranthes total saponin 4.5 mg/ml was used to compare the effects of drugs on the cervix and uterine horn. The results are shown in Table 6. Achyranthes saponin 0.5 mg/ml had no obvious stimulant effect on rat cervix. After administration, the rat cervix had no significant increase in tension and frequency except for a certain increase in tension; it had a significant effect on the rat uterine horn, increased tension, increased amplitude of contraction, and accelerated frequency.
The role of rabbits in the uterus: 3 rabbits weighing 2 to 2.51 g without pregnancy and 10 to 20 days pregnant were used for surgery under intravenous anesthesia with pentobarbital sodium 25 mg/kg. A uterine suspension was used to record uterine contractions. The lower end of the uterine cannula and the abdominal wall incision were punctured so that the uterus was immersed in a low-calcium solution (38% of normal calcium) heated at 38°C. Resting load was 3-5g, and after 30-60 minutes of stabilization, the experiment was started when the uterine activity described was constant. With topical administration, the liquid in the cannula was firstly aspirated, and then 0.5 mg/ml of Achyranthes total saponin (prepared with low-calcium solution) was added and observed for 30 minutes. After the first administration of 4 animals (not pregnant, half in half pregnant), the fluid was changed several times and repeated once more.
The results showed that, within 1-4 minutes after administration, unhybrid and mid-pregnancy rabbits may have strong contractions in the uterus. The performance is increased tension, the amplitude of contraction increases, the frequency increases, and the excitement generally continues to weaken for about 25 minutes. Repeated administration was still poorly stimulatory, but the effect was less than when it was administered for the first time. Zhu He et al. used the rat uterine contraction area (UCA) as an index, and used indomethacin and chlorpromazine as blocking agents to analyze the mechanism of the effect of Achyranthes bidentata saponin (ABS) on rat uterus excitability. The experimental results show that before the experiment, rats with indomethacin (75mg / gavage only or indomethacin 20ug / ml), can significantly reduce the ABS on rat excitability of isolated uterus. Prostaglandin E2200mg/ml can significantly enhance the uterus effect of ABS excited rats. Chlorpromazine 0.5mg/ml can also significantly reduce the stimulatory effect of ABS on uterus of pregnant and non-pregnant rats, while atropine 10ug/ml has no significant effect on uterine excitability induced by ABS. The uterus excitement induced by ABS has no significant effect. It is suggested that the uterus of ABS excited rats may be related to the promotion of prostaglandin and 5-HT release.
Anti-fertility effect
Anti-birth and abortion effects of Achyranthes bidentata saponins (ABS) on rats:
Thirty-eight female virgin rats weighing 200-250 g and 18 mature male rats weighing 250 g or more were selected and kept in cage for more than two weeks. Female rats were randomly divided into three groups (12 in each group) for experimentation according to the literature method. Females were sacrificed after drug treatment and the uterus was examined by necropsy to calculate the percentage of pregnancy in each group, average live births, abortions, and implantation points. Compared with the control group, there was no significant difference in the indicators between the administration group. Abortion test Healthy female rats (230-260g) and male rats (>750g) were bred in a 2:1 cage. The pregnant rats were examined on the d10 of pregnancy under ether anesthesia and the implantation points and sutures of the bilateral uterine horns were observed. Dl4-dl9 was administered to ABS aqueous solution and all animals were sacrificed during pregnancy d20. The results of laparotomy showed no significant effect on the rate of fetal loss compared with the control group. The average body weight of the litter was significantly lower than that of the control group (P<0.01). There are output situations.
Anti-fertility and anti-implantation effects of ABS on mice:
Healthy adult mice were selected, female mice were weighed 26-35g, males were weighed 30-45g, and mated to cages in a 2:1 ratio. Pregnant rats were randomly assigned to the administration group and the control group. The dl-d10 in the administration group and the thrombus was administered once a day by gavage, and the control group was given distilled water. When dl3 was present in the vaginal suppository, animals were sacrificed and the uterus was necropsied. The test indicators were the same as those of rats. The results showed that S250mg/kg gavage for 10 days showed a certain anti-fertility effect. The average number of stillbirths in this group and the number of live fetuses were similar. The number of bed points was significantly different from that of the control group (P<0.05, when the dose was increased by 500 mg/kg or more, the rate of pregnant mice was zero, showing 100% anti-fertility effect, and the half effective amount of ABS antifertility effect was calculated according to the literature method. 218 ± 48 mg/kg (P = 0.95) Anti-implantation test was performed on the dl-5 of vaginal suppository, administered once daily by gavage, and animals were sacrificed after 6 days of discontinuation, and fetuses were necropsied.Results: S 500 mg/kg The number of pregnant mice in the post-gastric administration group was significantly less than that in the control group (P<0.05)
Other effects
Promoting ecdysterone can improve liver function and reduce plasma cholesterol. Achyranthes decoction or alcohol extract has mild diuresis and shorten the role of silkworm age.
The in vivo process of ecdysterone:
Experiments in mice with 3H-ecdysterone showed that after 10 minutes of intraperitoneal injection, the radioactivity intensity reached the highest level in all organs and rapidly decreased. When administered orally, it is slow, and the amount of liver, blood, kidney and other organs is lower than when injected intraperitoneally. Regardless of intragastric administration or intraperitoneal injection, the liver was high in all organs. At the time of intraperitoneal injection, radioactive activity can rapidly occur in feces or in urine, but it occurs slowly when taken orally. Both routes of administration can be seen in feces in this urine, suggesting that the absorption of promoted ecdysterone mainly through hepatobiliary secretion Enter the intestine to excrete.
[Pharmaceuticals] The median lethal dose of quercetin was 6.4 g/kg for ecdysterone-injected mice and 7.8 g/kg for achyranthes. Both were >9 g/kg when gavage. The above sample decoction was administered at 60g/kg/day for 30 consecutive days. There were no abnormalities in the blood (animal), kidney function, major internal organs, body weight, and activities of the animal (mouse) compared with the normal control group.
Chemical composition of traditional Chinese medicine root contains triterpene saponin: oleanolic acid α-L-rhamnopyrrolidone-β-D-galactopyranose (oleanolic acid a-L-hamnopyranosyl-β-D-galac- Topyranoside). It also contains a variety of polysaccharides: one is an anti-tumor active polysaccharide precipitated from acetone in the aqueous extract of the root; the other is a water-soluble oligosaccharide composed of 6 glucose residues and 3 mannose residues. AbS, has a significant activity to enhance immune function; the other is the immune activity of the peptidoglycan ABAB, is from glucuronic acid (galcurose acid, galactose), galacturonic acid (galacturonic acid), arabinose (arabinose) and rhamnose are composed of a molar ratio of 12:2:1:1:1, and the content of peptide is 24.7%, which is mainly composed of glycine, glutamic acid and aspartic acid. (Aspartic acid) and Serine, with a relative molecular weight of 23,000. Also contains ecdysterone, inokosterone, rubro-sterone and arginine, glycine, serine, aspartic acid, glutamic acid, threonine (threonine), proline, tyrosine, TCMLIByptophan, valine, phenylalanine, leucine and alkaloids And coumarin compounds.
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