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Release Date:2018/3/22 9:37:40
1、 Pharmacopoeia standard of Herba Artemisiae Scopariae
Herba Artemisiae Scopariae
Yinchen
ARTEMISIAE SCOPARIAE HERBA

This product is the dry aboveground part of Artemisia scoparia waldst. et kit. or Artemisia capillaris thunb., a composite plant. The seedlings are harvested when they are 6-10cm high in spring or when the flower buds grow to the beginning of flower opening in autumn. Impurities and old stems are removed and dried in the sun. .
[character] Herba Artemisiae capillaris is mostly curled into a mass, gray white or gray green, and all are densely covered with white fluffy hair, which is as soft as velvet. The stem is small, long, 1.5 ~ 2.5cm, 0.1 ~ 0.2cm in diameter, and obvious longitudinal lines can be seen after removing the white hairs on the surface; . ; After flattening, the leaves show one to three pinnate divisions, and the leaves are 1-3cm long and 1cm wide; the small lobes are oval or slightly oblanceolate and strip-shaped, and the apex is acute. It smells light and bitter.
; It is light, brittle, and white in cross section. The leaves are dense, or more shedding; The lower leaves have two to three pinnately deep lobes, and the lobes are strip-shaped or thin strip-shaped, and both sides are densely covered with white pilose; Cauline leaves are pinnately divided in one to two loops, with stem hugging at the base, and the lobes are filiform. The capitulum is ovate, most of which are cone-shaped, 1.2-1.5mm long and 1-1.2mm in diameter, with short stems; Involucral bracts 3-4 layers, ovate, bracts 3-lobed; There are 6-10 female flowers in the outer layer, up to 15, and 2-10 androgynous flowers in the inner layer. Achenes oblong, yellowish brown. It smells fragrant and tastes slightly bitter.
[identification] Herba Artemisiae Scopariae (1) the powder of this product is grayish green. The non glandular hairs are "t" shaped, 600-1700 μ m long, slightly folded into a "V" shape in the middle, with unequal arms, extremely thick cell walls, slit like cavities, and 1-2 cells in the stalk.
(2) Take 0.5g of this product powder, add 20ml of 50% methanol, sonicate for 30 minutes, centrifuge, and take the supernatant as the test solution. Take chlorogenic acid reference substance and add methanol to make a solution containing 0.1mg per 1ml as the reference solution. . In the chromatogram of the test sample, fluorescent spots of the same color appear at the corresponding positions of the chromatogram of the control sample.
Herba Artemisiae Scopariae take 0.4g of this product powder, add 10ml of methanol, sonicate for 30 minutes, filter, evaporate the filtrate, add 2ml of methanol to dissolve the residue, and use it as the test solution. In addition, take the reference substance of Scoparone and add methanol to make a solution containing 0.4mg per 1ml as the reference solution. According to the test of thin-layer chromatography (general rule 0502), suck 5 μ l of each of the above two solutions, dot them on the same silica gel G thin-layer plate respectively, use petroleum ether (60 ~ 90 ℃) - ethyl acetate acetone (6:3:0.5) as the developing agent, develop, take out, dry, and view under the ultraviolet light (365nm). In the chromatogram of the test sample, fluorescent spots of the same color appear at the corresponding positions of the chromatogram of the control sample.
[inspection] the moisture content shall not exceed 12.0% (the second method of general rule 0832).
[extract] the content of water-soluble extract of Herba Artemisiae Scopariae determined by hot leaching method (general rule 2201) shall not be less than 25.0%.
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Chromatographic conditions and system suitability test octadecylsilane bonded silica gel was used as filler; ; The detection wavelength is 327nm. The number of theoretical plates should not be less than 5000 according to the chlorogenic acid peak.
Preparation of reference solution take an appropriate amount of chlorogenic acid reference substance, accurately weigh it, place it in a brown volumetric flask, add 50% methanol to make a solution containing 40 μ g per 1ml.
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The determination method is to precisely suck 10 μ l of the reference solution and 5 ~ 20 μ l of the test solution, inject them into the liquid chromatograph, and determine.
According to the calculation of dry product, the content of chlorogenic acid (c16h18o9) shall not be less than 0.50%.
Herba Artemisiae capillaris was determined by HPLC (general rule 0512).
Chromatographic conditions and system suitability test octadecylsilane bonded silica gel was used as filler; ; The detection wavelength was 345nm. The number of theoretical plates should not be less than 2000 according to the peak of Scoparone.
Preparation of reference solution take appropriate amount of Scoparone reference, weigh accurately, and add methanol to make a solution containing 20 μ g per 1ml.
Preparation of the test solution take about 0.2g of the powder (passing the second sieve), accurately weigh it, place it in a corked conical flask, precisely add 50ml of methanol, weigh it, heat and reflux for 40 minutes, cool it, weigh it again, make up the lost weight with methanol, shake it well, centrifuge it, and take the supernatant.
The determination method is to precisely suck 10 μ l of the reference solution and 10 μ l of the test solution, inject them into the liquid chromatograph, and determine.
According to the calculation of dry product, the content of Scoparone (c11h10o4) shall not be less than 0.20%.
Decoction pieces
[processing] remove residual roots and impurities, and crush or chop them. .
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[functions and indications] clear away dampness and heat, benefit gallbladder and eliminate jaundice. It is used for jaundice with little urine, damp temperature and heat dampness, wet sores and itching.
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[storage] store in a cool and dry place and keep away from moisture.

2、 Chemical constituents of Herba Artemisiae Scopariae

Artemisia capillaris contains Artemisia coumarin, an effective ingredient with choleretic effect,
That is, the content of 6,7-dimethoxycoumarin varies according to the season, and the flowering period is the highest, reaching 1.98%, andchlorogenic acidandcaffeic acidThe whole grass contains about 0.27% of essential oil; There are many essential oils in the ear, with a content of 1%. Its ingredients are: β - pinene, herbacetin, echinone, herbacetin. It also contains fatty oil, of which the fatty acid is stearic acid,palmitic acid, oleic acid, linoleic acid, arachidic acid, lignitic acid. The ash contains potassium chloride. The seeds also contain Artemisia coumarin and potassium chloride.

3、 Pharmacological effects of Herba Artemisiae Scopariae Scopariae Scopariae Scopariae Scopariae Scopariae Scopariae Scopariae Scopariae Scopariae Scopariae Scopariae Scopariae Scopariae Scopariae scoparia

1. Choleretic effect
[6,7 dimethoxycoumarin structural formula] 6,7 dimethoxycoumarin structural formula decoction, water extract, volatile oil
Water extract, volatile oil, alcohol extract, 6,7-dimethoxycoumarin, chlorogenic acid, etc. all have the effects of promoting bile secretion and choleretic. This product is 0.25g/kg of water extract, or 1g/kg of refined extract (with or without volatile oil removed) intravenously injected into dogs with acute gallbladder intubation, or 1g/kg of refined extract is gavaged into dogs with chronic gallbladder flaccidity. It has cholagogic effect on healthy dogs or dogs with liver damage caused by carbon tetrachloride. When the bile secretion increases, its dry weight also increases. When 6,7-dimethoxycoumarin 0.2g/kg or 0.3g/kg was injected into the duodenum of anesthetized rats, the bile secretion increased by 50% or 180% on average after 30 minutes. In dogs with chronic cholecystostomy, bile increased by 73.86% on average within 3 hours after gavage of 0.3g/kg. . P-hydroxyacetophenone has obvious choleretic effect on rats, can increase bile secretion, can also increase the excretion of solids, cholic acid and bilirubin in bile, and has the same effect on liver injury caused by carbon tetrachloride. It was also reported that the choleretic effect intensity of Herba Artemisiae Scopariae components was in the order of Herba Artemisiae a, Herba Artemisiae B, 6,7-dimethoxycoumarin, Herba Artemisiae chromogen ketone.
injection
Yinchen decoction can also reduce the tension of sphincter of Oddi in anesthetized dogs. Herba Artemisiae diyne, Herba Artemisiae diketone and Herba Artemisiae lactone can also promote bile secretion and excretion.

2. Effects on liver
The rats with liver damage caused by carbon tetrachloride were subcutaneously injected with Yinchen Decoction 0.61g every day, and histological examination was performed on the 8th day. It can be seen that the swelling, ballooning, steatosis and necrosis of hepatocytes in the treatment group were alleviated to varying degrees compared with those in the control group.
oral liquid
The content of prokaryotic and ribonucleic acid recovered or was close to normal, and the activity of serum alanine aminotransferase decreased significantly, indicating that it still has a certain liver protective effect. Yinchenhao Decoction 0.25ml/10g was given to mice by gavage, twice a day for 4 days, and the liver P450 content was determined. The results showed that Herba Artemisiae Scopariae decoction could increase the liver P450 content, increase the liver / body weight ratio, and shorten the sleep time induced by sodium isopentabarbital in mice, which preliminarily showed that Herba Artemisiae Scopariae decoction could induce liver enzymes in mice. As liver enzymes are involved in the metabolism of bile acids, bilirubin, esters and some poisons in addition to drug metabolism, the induction of liver enzymes may be related to the functions of Herba Artemisiae Scopariae, such as cholagogic and anti jaundice.
Some flavonoids and coumarins in Herba Artemisiae Scopariae have anti-ccl4 or galactose induced cytotoxicity in rat hepatocytes, and their intensity is in the order of Herba Artemisiae chromogen ketone, scopoletin, 6,7-dimethoxycoumarin, Herba Artemisiae flavone, quercetin, isorhamnetin. The effective ingredients in Yinchenhao Decoction can significantly reduce the serum levels of glutamic pyruvic transaminase (SGPT) and glutamic oxaloacetic transaminase (SGOT) in acute jaundice rats, but have a slight effect on serum bilirubin (sb). In addition, 6,7-dimethoxycoumarin has a strong inhibitory effect on hepatocyte damage.

3. Antipyretic action
Effect on normal temperature of mice: mice were injected with 40 and 80mg/kg of artemisinin water suspension by intraperitoneal injection, and the control was treated with normal saline. The normal temperature of each group before administration was 37.7 ± 0.06, 37.8 ± 0.07 and 37.7 ± 0.08 ℃ (x ± SE), and the average temperature was 36.3 ± 0.05, 35.5 ± 0.04 and 37.6 ± 0.08 ℃ measured 30 minutes after administration. The body temperature of the administration group was lower than that before administration, and the difference was very significant (p< 0.01), but there was no change in the control group. In addition, according to the dose of 40 and 20mg/kg, the mice in the two groups were injected intraperitoneally, and the body temperature was continuously measured. The temperature in the 40mg/kg dose group lasted for 6 hours, and the body temperature in the 20mg/kg group gradually recovered in about 3 hours.
Effect on normal temperature of rats: Rats weighing 40-60g were given artemisinin orally or intraperitoneally, and divided into five dose groups (125, 250, 500mg/kg and 5, 20, 40mg/kg), and chlorpromazine positive control and normal control groups were set. Anal temperature was measured once at 0.5, 1, 2, 3, 4 and 8 hours after administration. Results the normal body temperature of rats in the treatment group was significantly decreased, and the effect was positively correlated with the dose. The cooling amplitude increased with the increase of dose, and the action time extended with the increase of dose. Generally, the body temperature will drop 0.5 hours after administration, reaching the peak in 1-2 hours, and maintaining for about 4 hours.
Antipyretic effect on rats induced by Saccharomyces cerevisiae: oral Yinchen (1% Astragalus membranaceus gum suspension) 250mg/kg, oral compound analgin (aminopyrine 400mg/kg, analgin 600mg/kg) and oral equivalent volume of 1% Astragalus membranaceus gum solution were used as controls. Results both yinchensu and compound analgin had a good antipyretic effect on the rats with fresh beer yeast induced fever. Both of them had antipyretic effect from 0.5 hours after administration, and the body temperature could be reduced by about 3 ℃ in about 2 hours, and the maintenance time could be up to about 4 hours.
Antipyretic and preventive effects on 2,4-dinitrophenol-induced fever in rats: compared with the positive control aminopyrine 80mg/kg and normal saline control group, the body temperature drop rate of the medication group was significantly different from that of the normal saline control group 3 hours after administration (p< 0.05), and the preventive effect of artemisinin on fever was higher than that of aminopyrine (p< 0.05).
The intraperitoneal injection of 20 mg / kg of inchenin had a good antipyretic effect on rabbits with fever caused by expired typhoid bacteria and 2,4-dinitrophenol.

4.
The experimental hypercholesterolemic rabbits were gavaged with Herba Artemisiae Scopariae Decoction 3g/kg. After 2-3 weeks of treatment, the serum cholesterol of the treatment group decreased by 19.2mg% and 30mg%, β - lipoprotein also decreased significantly, the atherosclerosis of the arterial wall was lighter than that of the control group, and the cholesterol content of the rabbit aortic wall was also significantly lower than that of the control group, indicating that Herba Artemisiae Scopariae has certain anti atherosclerotic effect. Both Yinchen injection and 6,7-dimethoxycoumarin can increase the coronary flow of isolated rabbit hearts. The determination of summer calcium time, the observation of antithrombin effect, protein electrophoresis, fibrinolysis test, Staphylococcus aureus aggregation test, and the determination of fibrin (original) cleavage products proved that the bacteria had the effect of anticoagulation and promoting fibrinolysis. 6,7-dimethoxycoumarin can inhibit the contractile effects of NE, 5-HT, his and at - Ⅱ on vascular smooth muscle, and its mode of action is very similar to that of nitroglycerin.

5. Hypotensive effect
The water extract, ethanol, water extract, volatile oil and 6,7-dimethoxycoumarin of Yinchen have the effect of reducing blood pressure. The latter, 0.4-10mg/kg intravenously or duodenally, can significantly reduce blood pressure in rats, cats and rabbits under general or local anesthesia. . When 1/50-1/10 intravenous dose was injected into vertebral artery, the intensity of blood pressure reduction was approximately equal to the total dose, suggesting that its blood pressure lowering effect may be central. 6,7-dimethoxycoumarin can enhance the contractility of eutopic rabbit heart and cat heart. Scoparone has significant antihypertensive and tranquilizing effects. The hypotensive effect was stronger than that of methyl dopa. Intravenous injection of 10mg/kg in dogs could reduce blood pressure by 58.6% for 160 minutes. At the same dose, methyl DOPA decreased blood pressure by 12.4% for 120 minutes. Scoparone also has diuretic effect.

6. Antibacterial and anti-inflammatory effects
In vitro tests showed that Yinchen decoction had different degrees of inhibition on Staphylococcus aureus, Diphtheria Bacillus, anthrax bacillus, typhoid bacillus, paratyphoid a bacillus, Pseudomonas aeruginosa, Escherichia coli, dysentery flexneri, Shigella dysentery bacillus, meningococcus, Bacillus subtilis, etc. 10% decoction can completely inhibit the growth of human tuberculosis. 1: The concentration of 100 had inhibitory effect on both human and bovine Mycobacterium tuberculosis. The in vitro test of Herba Artemisiae chromone has antagonistic effect on the antibacterial effect of chloramphenicol. Herba Artemisiae diynone has a high anti Herba Artemisiae effect, especially a strong effect on skin pathogenic filamentous bacteria, showing bactericidal effect. After a long time of high temperature treatment above 100 ℃, its antibacterial effect is still not reduced. At the concentration of 0.25 μ g/ml, the growth and reproduction of Trichophyton scarlet could be completely prevented. . .

7. Effect on smooth muscle
Herba Artemisiae Scopariae Decoction and alcohol extract had a slight excitatory effect on isolated rabbit intestine. The water extract can inhibit the activity of intestinal muscle in dogs and rabbits in vitro. . The refined extract has an excitatory effect on the uterus of nonpregnant rabbits and postpartum guinea pigs. The excitatory effect on the uterus of nonpregnant guinea pigs can be antagonized by diphenhydramine.

8. Effect on aflatoxin
Artemisia capillaris water decoction induces TA98 frameshift type TA100  Base substitution mutagenesis reversion mutation inhibition experiment showed that Artemisia capillaris water decoction had a significant inhibitory effect on the mutagenic effect of AFB1 in a dose-dependent manner. It is suggested that it may be of significance in the prevention of liver cancer.

9. Effect on immune function
Herba Artemisiae Scopariae can promote the division of white blood cells, increase the number of white blood cells, improve the immune activity of T cells, participate in the immune regulation of the body and induce interferon, so it can improve the immune function of the body in many ways. . Oral administration of Herba Artemisiae Scopariae at 250mg/kg could significantly enhance the delayed type hypersensitivity of transplanted tumor mice.

10. Other roles
The product and its components also have anti Leptospira, anti Ascaris lumbricoides, antiasthmatic, anti killing mouse Ehrlich ascites cancer cells, metha cells.
 
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