1、 Pharmacopoeia standard of Caulis Spatholobi
Caulis Spatholobi
Daxueteng
SARGENTODOXAE CAULIS
This product is the dried vine stem of Sargentodoxa cuneata (oliv.) rehd.et wils., a plant of akebiaceae. Harvest in autumn and winter, remove side branches, cut sections, and dry.Daxueteng
SARGENTODOXAE CAULIS
[properties] this product is cylindrical, slightly curved, 30-60cm long and 1-3cm in diameter. The surface is grayish brown and rough, and the outer skin is often scaly exfoliated. The exfoliated part is dark reddish brown, and some swollen nodes and slightly concave branch marks or leaf marks can be seen. It is hard, with reddish brown skin on the cross section, and several embedded wood parts. The wood parts are yellowish white, with many fine porous ducts, and the rays are arranged radially. The breath is slight and the taste is slightly astringent.
[identification] (1) cross section of this product: the cork layer is multi row cells, containing brownish red substances. . . Phloem secretory cells are often arranged tangentially and separated from the sieve tube group; A few stone cell groups were scattered. The intrafascicular cambium is obvious. Xylem vessels are mostly single scattered, quasi circular, with a diameter of about 400 μ m, surrounded by wood fibers. The rays are broad, there are many lateral stone cells, and some contain several calcium oxalate crystals. Stone cell groups can be seen in the calf. Parenchyma cells contain brown or brownish red substances.
(2) Take 5g of crude powder of the product, add 50ml of methanol, sonicate for 30 minutes, filter, evaporate the filtrate, add 10ml of 2% sodium hydroxide solution to dissolve the residue, adjust the pH value to 2 with hydrochloric acid, shake and extract three times with 10ml of ether each time, combine the ether solution, volatilize it, add 2ml of methanol to dissolve the residue, and use it as the test solution. . According to the test of thin-layer chromatography (general rule 0502), suck 2 μ l of each of the above two solutions, dot them on the same silica gel G thin-layer plate, use chloroform acetone formic acid (8:1:0.8) as the developing agent, develop, take out, dry, spray 2% ferric chloride ethanol solution, and inspect them under sunlight and ultraviolet light (365nm). In the chromatogram of the test sample, spots of the same color appear in the sunlight and fluorescent spots of the same color appear in the ultraviolet light at the corresponding position of the chromatogram of the control medicinal material..............................the color of the spots is the same under the sunlight.
[inspection] the moisture content shall not exceed 12.0% (the second method of general rule 0832).
The total ash content shall not exceed 4.0% (general rule 2302).
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Decoction pieces
[processing] remove impurities, wash, moisten, cut into thick pieces, and dry.
. The outer skin is grayish brown and rough. The cut skin is reddish brown, and several parts are embedded into the wood, which is yellow and white, with many duct holes, and the rays are arranged radially. The breath is slight and the taste is slightly astringent.
[identification] (2) [inspection] [extract] is the same as that of medicinal materials.
[nature, taste and meridian tropism] bitter, flat. It belongs to the large intestine and liver meridian.
[functions and indications] it can clear away heat, detoxify, activate blood circulation, dispel wind and relieve pain. It is used for intestinal carbuncle, abdominal pain, fever and sores, amenorrhea, dysmenorrhea, tumefaction and pain, rheumatism and arthralgia.
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2、 Chemical constituents of Caulis Spatholobi
Caulis Spatholobi containsEmodin(emodin),Emodin methyl ether(physcion),β - sitosterol(β-sitosterol),Carotene(daucsterol), ,Salidroside(salidroside), ,Chrysophanol(chrysophanol),Vanillic acid(vanillicacid),Protocatechuic acid(protocatechuic acid) and p-hydroxyhenylethylalcohol ester (p-hydroxyphenylethanol) and Hongteng polysaccharide.
3、 Pharmacological effects of Caulis Spatholobi
1. effects on cardiovascular system 1.1 effects on isolated toad heart according to the Bayi's isolated heart device, 20ml Ren's solution was perfused, and 0.1g Caulis Spatholobi was added to the perfusate (0.5%). It was found that the isolated heart was mildly inhibited, showing reduced cardiac contractility, slower heart rate (P < 0.05), and reduced cardiac output (p< 0.01).
1.2 effect on isolated rabbit aortic strips place the isolated rabbit aortic strips in the water tank of the ex vivo device (37 ± 0.5 degrees) for 1h, and add 0.2ml of extract (1g crude drug /ml) to 20ml of Krebs solution (1%). Results the blood vessels began to have obvious contractile effect, which could be blocked by phentolamine, suggesting that its contractile effect may be related to A-receptor. Then there was a lasting relaxation effect.
. However, in the contraction state caused by potassium chloride, adding drugs, the contractile effect will no longer appear, and immediately relax the blood vessels, suggesting that it is beneficial to the treatment of coronary spasm.
1.4 effects on experimental myocardial infarction in animals 1.4.1 effects of water-soluble extract of Spatholobus suberectus on experimental myocardial infarction in rabbits water soluble extract of Spatholobus suberectus (the traditional Chinese medicine is cold soaked in 95% ethanol, concentrated under reduced pressure, extracted with ether to remove ether soluble substances, syrupy precipitate is added with water until the precipitate no longer occurs, the precipitate is filtered, gelatin solution is added until the precipitate no longer occurs, the aqueous solution is concentrated into syrup under reduced pressure, extracted with methanol, methanol insoluble substances, made into water solvent, containing sugars and glycosides). Twenty four healthy rabbits were randomly divided into three groups: the control group (equal volume normal saline), the water-soluble extract group of Caulis Spatholobi (100mg/kg; equivalent to 100g of the original drug), and the propranolol group (0.05mg/kg). The patients were anesthetized with sodium pentobarbital (300mg/kg) IV for precordial multi lead ECG mapping. The chest was opened, and the root of the left anterior descending branch was ligated with 4 silk thread. Close the chest, record the chest ECG, and immediately take IV drugs, and then inject them every 6 hours for a total of 4 times. ECG mapping was performed at 4 hours and 24 hours after ligation. The heart was removed after 24-hour interval measurement, and the percentage of myocardial infarction range was calculated. Results four hours after ligation of the left anterior descending branch, the total millivolt number (∑△ st) of ST segment elevation of ECG in the Caulis Spatholobi group and propranolol group were similar, and both groups were significantly lower than that in the control group (P < 0.05). The difference was more significant at 24 hours after ligation (P < 0.01). At 24 hours after ligation, the myocardial infarction range in the Caulis Spatholobi group was reduced to 19.17%, which was similar to 19.88% in the propranolol group, and the differences were extremely significant compared with the control group (P < 0.001). At the same time, the myocardial lactic acid content of rabbits with myocardial infarction was determined: 42 rabbits were divided into four groups, namely, the normal group did not ligate the left anterior descending branch and did not give any drugs, and the other three groups ligated the left anterior descending branch. After ECG, the myocardial infarction group ivlmg/kg normal saline, the Caulis Spatholobi group ivl00mg/kg body weight, and the propranolol group IV propranolol 0.05mg/kg body weight. The lactic acid content in myocardial tissue of the four groups of rabbits was measured at the same time in each experiment. . It revealed that the degree of myocardial ischemia caused by ligation of the left anterior descending artery may be basically similar among the three groups. One hour after the animals with myocardial infarction were given normal saline or drugs, the lactic acid content of myocardial tissue in the myocardial infarction group increased significantly at one hour after myocardial infarction, while the lactic acid content of myocardial tissue in the Caulis Spatholobi group and propranolol group did not increase (similar to that in the normal group), and the difference was extremely significant (P < 0.001), indicating that the water-soluble extract of Caulis Spatholobi can improve the disorder of myocardial lactic acid metabolism.
1.4.2 effect of water-soluble extract of Caulis Spatholobi on experimental myocardial infarction in dogs nineteen mongrel dogs were randomly divided into three groups: myocardial infarction control group, without any drug treatment after ligation of the left anterior descending branch; In the Caulis Spatholobi group, while ligating the left anterior descending branch, ivl00mg/kg, After that, it was repeated every 6 hours for a total of 4 times; . The results showed that the ST segment of epicardial ECG in the Caulis Spatholobi group was significantly elevated as in the control group 5 minutes after ligation of the left anterior descending branch, with no significant difference (P < 0.05). However, the elevated ST segment recovered faster, and there was a significant difference compared with the control group at 30 minutes after ligation, P<0.05。 Compared with propranolol group, the effect of Caulis Spatholobi was slower and weaker. . The results of blood lactic acid content were consistent with the changes of lactic acid content in myocardial tissue of rabbits with myocardial infarction. The range of myocardial infarction in the Caulis Spatholobi group was narrowed, and the difference was extremely significant compared with the control group (P < 0.001). The effect of propranolol group was more obvious, but there was no significant difference compared with the Caulis Spatholobi group (P < 0.05).
1.4.3 100mg/kg of water-soluble extract of sargentodon wilfordii can significantly reduce the elevated ST segment of experimental myocardial infarction in rabbits, improve the disorder of myocardial lactate metabolism caused by ligation of the anterior descending branch of the left coronary artery, and reduce the scope of myocardial infarction.
. After IP Administration for 30-40 minutes, the limbs were anesthetized and connected to the electrocardiograph. After EKG of standard lead II of limbs was measured, iso4mg/kg (IP) was given to observe the changes of EKG at 1, 5, 10, 30 and 60 minutes. After 24 hours, repeat according to the order of administration and record of the previous day. After 48 hours of anesthesia and EKG measurement, the chest was opened for coring, sectioning, and pathological examination. Results the effect of sargentodon on the change of EKG, dlP<0.05,d2P<0.01。 To have potential therapeutic significance, pathological examination had the strongest protective effect on myocardial necrosis (P < 0.01). The effect of liriodendrin on EKG was weak and slow, and the difference did not appear until D2 (P < 0.05). Pathological examination also had a protective effect (P < 0.05). There was no statistical difference between salicin group and saline control group. . Its mechanism of action is worthy of further discussion.
1.6 effect on blood pressure of anesthetized cats four healthy cats were anesthetized. After anesthesia, the trachea was cut according to the routine, the tracheal cannula was inserted, and the carotid artery was separated to measure blood pressure. After femoral iv0.1g/kg aqueous extract of Caulis Spatholobi (1g of crude drug is equivalent to 1ml), there was a transient hypotensive effect, which could be blocked by atropine; Two vagus nerves were excised, and the hypotensive effect had no effect, suggesting that its hypotensive effect should be related to the peripheral cholinergic system.
. Results the amount of camp in plasma was significantly increased in the Caulis Spatholobi group and Salvia miltiorrhiza group, but the amount of CCMP was not significantly decreased. In addition, five mice in each group were taken, once ip3g/kg, and blood was collected from the orbit every 15, 30, 90, and 120 minutes, respectively, with normal saline control in each group. The changes of camp and cGMP in plasma at different times were observed. The results showed that the amount of camp and cGMP increased within 50 minutes after administration, and the increase of camp was more obvious. The camp/cgmp value decreased, but after 60 minutes, the amount of camp and CCMP gradually decreased, and the camp/cgmp value increased. 100mg/kg of the water-soluble extract of sargentodon wilfordii significantly increased plasma cAMP in rabbits.
3. effect on platelet aggregation in vitro, the water-soluble extract of sargentodon wilfordii can significantly inhibit and promote the disaggregation of rabbit platelet aggregation induced by ADP, with an ID50 of 14.6mg/ml. 40 and 100mg/kg of the water-soluble extract of sargentodon wilfordii could inhibit ADP induced platelet aggregation in rats. The dichloromethane extract of this product, including dihydroguaiaretic acid, can inhibit the binding of PAF (platelet activating factor) to the receptor.
4. effects on hypoxia tolerance of mice under atmospheric pressure healthy male mice weighing 17-22g were divided into three groups, with 10 mice in each group. The aqueous extract of Caulis Spatholobi was 2g (equivalent to crude drug) /kg, and the LD50 of mice IP was l1.83 ± 2.12g/kg. The control was treated with the same volume of normal saline, and the observation was carried out regularly. The respiratory arrest was taken as the death index. The results showed that it had obvious effects at different intervals.
5. the bacteriostatic effect was tested by the plate method. The 25% decoction was highly sensitive to Staphylococcus aureus and Streptococcus B, and highly sensitive to Escherichia coli, Pseudomonas aeruginosa, Streptococcus A, catarrhalis, and Staphylococcus albicans.
6. effects on gastrointestinal smooth muscle of animals the isolated intestinal segments of mice or guinea pigs were placed in 20ml of continuously ventilated Roche solution. 1% and 5% Caulis Spatholobi had obvious inhibitory effects on the intestinal segments of mice. It only needs 0.5% and 2.5% for guinea pigs to show the effect of excitation first and then inhibition, and it can also weaken the effect of acetylcholine at high doses. The experiment of intestinal peristalsis in mice showed that 5-10g/kg water extract of Caulis Spatholobi could significantly inhibit the intestinal peristalsis speed of mice.
7. other effects this product can prevent intra-abdominal adhesion of experimental animals when combined with cortex moutan. Salicin has anti fatigue effect; Liriodendrin can inhibit camp phosphodiesterase.