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Release Date:2017/9/21 13:47:53
Epimedium
1、 Pharmacopoeia standard of Epimedium
Epimedium
Yinyanghuo
EPIMEDII FOLIUM
      This product is the dried leaves of Epimedium brevicomu maxim., Epimedium sagittatum (sieb.et zucc.) maxim., Epimedium pubescens maxim., or Epimedium koreanum Nakai, a berberine plant. Harvest in summer and autumn when the stems and leaves are luxuriant, and dry in the sun or in the shade.
      ; Three compound leaves; The leaflets are oval, 3 ~ 8cm long and 2 ~ 6cm wide; the apex is slightly pointed, the base of the terminal leaflet is heart-shaped, the leaflets on both sides are small, eccentric, and the outer side is large, in ear shape, with yellow barbed fine serrations on the edge; The upper surface is yellowish green, the lower surface is grayish green, and the main veins are 7-9. There are sparse fine hairs at the base. The thin veins are prominent on both sides, and the reticular veins are obvious; The petiole is 1 ~ 5cm long, and the leaves are nearly leathery. The breath is slight, and the taste is slightly bitter.
      Epimedium sagittatum   The leaflets are oval to ovate lanceolate, 4 ~ 12cm long and 2.5 ~ 5cm wide, with three compound leaves; the apex is gradually pointed, and the base of leaflets on both sides is obviously skewed, and the outer side is arrow shaped. The lower surface is sparsely shaggy or nearly glabrous. The leaves are leathery.
      ; The lower surface of leaves and petioles are densely covered with villous villous hairs.
      Epimedium koreanum   The leaflet is larger, 4-10cm long, 3.5-7cm wide, and the apex is long and pointed. The blade is thin.
      [identification] (1) the leaf surface of this product: Epimedium   The vertical walls of the upper and lower epidermal cells are deeply wavy, and there are different cells arranged longitudinally along the leaf veins, containing 1 ~ more calcium oxalate columnar crystals; The stomata of the lower epidermis are numerous, amorphous, and sometimes non glandular hairs can be seen.
      Epimedium sagittatum   The upper and lower epidermal cells were smaller; The pores of the lower epidermis are dense, with warty protrusions formed by the shedding of most non glandular hairs, and sometimes non glandular hairs can be seen.
      ; The stomata of the lower epidermis are sparse, with most elongated non glandular hairs.
      Epimedium koreanum   Stomata and non glandular hairs were easily seen in the lower epidermis.
      (2) . Test according to thin-layer chromatography (general rule 0502), suck 10 μ l of the test solution and 10 μ l of the control solution under icariin [content determination], respectively, dot on the same silica gel h thin-layer plate, use ethyl acetate butanone formic acid water (10:1:1) as the developing agent, develop, take out, dry, and view under the ultraviolet light (365nm). In the chromatogram of the test sample, the same dark red spots appear at the corresponding positions of the chromatogram of the control sample; Spray aluminum trichloride test solution, and then put it under the ultraviolet light (365nm) to inspect, showing the same orange red fluorescent spots.
      [check] impurities   Not more than 3.0% (general rule 2301).
      Moisture   Not more than 12.0% (the second method of general rule 0832).
      Total ash   Not more than 8.0% (general rule 2302).
      [extract] according to the cold leaching method under the determination method of alcohol soluble extract (general rule 2201), using dilute ethanol as solvent, it shall not be less than 15.0%.
      [content determination] total flavonoids   Accurately measure 0.5ml of the test solution under the determination of icariin, put it into a 50ml volumetric flask, add methanol to the scale, shake well, and use it as the test solution. In addition, take an appropriate amount of icariin reference substance, accurately weigh it, add methanol to make a solution containing 10 μ g per 1ml as the reference substance solution. .
      This product is calculated as a dry product, and the total flavonoids contained shall not be less than 5.0% based on icariin (c33h40o15).
      Icariin   Determine according to high-performance liquid chromatography (general rule 0512).
      ; Octadecylsilane bonded silica gel was used as filler; Acetonitrile water (30:70) was used as mobile phase; The detection wavelength was 270nm. The number of theoretical plates should not be less than 1500 based on icariin peak.
      Preparation of reference solution   Take an appropriate amount of icariin reference substance, weigh accurately, add methanol to make a solution containing 0.1mg per 1ml.
      Preparation of test solution   Take about 0.2g of this product powder (passing through No. 3 screen), weigh it accurately, place it in a corked conical flask, add 20ml of dilute ethanol precisely, weigh it, sonicate for 1 hour, weigh it again, make up the lost weight with dilute ethanol, shake it well, filter it, and take the filtrate.
      Assay   Precisely suck 10 μ l of the reference solution and 10 μ l of the test solution respectively, inject them into the liquid chromatograph, and determine.
      Calculated as a dry product, the content of icariin (c33h40o15) shall not be less than 0.50%.
      Decoction pieces
      [processing] Epimedium   Remove impurities, spray water, moisten slightly, shred and dry.
      This product is silk like. The upper surface is green, yellowish green or light yellow, the lower surface is grayish green, the reticulate veins are obvious, the midvein and veinlets are protruding, and the edge has yellow barbed fine serrations. . The breath is slight, and the taste is slightly bitter.
      [content determination] the content of icariin (c33h40o15) in the same medicinal material shall not be less than 0.40%.
      [identification] (except for leaf surface view) [inspection] (total ash) is the same as that of medicinal materials.
      Roasted Epimedium   Heat and melt the lanolin oil, add the epimedium, stir fry over low heat until it is even and shiny, take it out and let it cool.
      For every 100kg of epimedium, use 20kg of lanolin oil (refined).
      This product is shaped like Epimedium. The surface is light yellow and shiny. .
      ; No more than 8.0% for the same medicinal materials.
      [content determination] determine according to HPLC (general rule 0512).
      ; Octadecylsilane bonded silica gel was used as filler; With acetonitrile as mobile phase A and water as mobile phase B, perform gradient elution according to the following table; The detection wavelength was 270nm. The number of theoretical plates should not be less than 1500 based on icariin peak.
     
        Preparation of reference solution   Take an appropriate amount of icariin reference substance and pogoside Ⅰ reference substance, accurately weigh them, add methanol to make solutions containing 0.1mg per 1ml respectively.
      Preparation of test solution   Take about 0.2g of this product powder (passing through No. 3 screen), weigh it accurately, place it in a corked conical flask, add 20ml of dilute ethanol precisely, weigh it, sonicate (power 200W, frequency 40KHz) for 1 hour, cool it, weigh it again, make up the lost weight with dilute ethanol, shake it well, filter it, and take the filtrate.
      ; Precisely suck 10 μ l each of the above two reference solutions and the test solution, inject them into the liquid chromatograph, and determine.
      The total amount of icariin (c33h40o15) and pogoside Ⅰ (c27h30o10) in this product shall not be less than 0.60% according to the dry product.
      [identification] (except for leaf surface view) [inspection] (total ash) is the same as that of medicinal materials.
      [nature, taste and meridian tropism] pungent, sweet and warm. Return to liver and kidney channels.
      [functions and indications] Tonify Kidney Yang, strengthen muscles and bones, and dispel wind and dampness. It is used for kidney yang deficiency, impotence and spermatorrhea, muscle and bone flaccidity, rheumatism and arthralgia, numbness and contracture.
      [usage and dosage] 6 ~ 10g.
      .


2、 Chemical constituents of Epimedium
1. Epimedium aboveground part containsIcariin(icariin),Icariin I(icariside), It also contains inorganic elements such as potassium and calcium.
2. Epimedium sagittatum whole herb containsIcariin, soap type, bitter taste, tannin, volatile oil, ceryl alcohol, TRIACONTANE, phytosterol, oleic acid, linoeic acid, palmitic acidquercetin Quercetin and quercetin-3-o - β - D-glucoside. In addition, it contains a small amount of inorganic elements such as potassium, which has been reported in other literaturesIcariin I, icaritin-3-o-a-rhamnoside, anhy-droicaritin-3-o-a-rhamnoside,Sagittarin a(sagittatoside)、B、C,Epimedin A (epimedin)A、ZhaohuodingBepimedin c , sagittatin a, B; Icariin a(icariside)、IcariinB2、IcariinB6、IcariinB9、IcariinD3、IcariinE6、IcariinE7、IcariinH1, Icarisidinb1, icariol A1, A2, erythro - and Soviet dilignol, 5,5 '- dimethoxydilignol, erythro - and Soviet 1,2-bis-1 (4-hydroxy-3-methyl oxyphenyl) propane 1 L, 3-diol [l, 2-bis-(4-hydroxy-3-methoxyphenyl)-propane-1,3-diol], 5-methoxy - (-) - isolarixinol, 5-methoxy-9-xylosyl - (-) - isolarixinol, l-olivil, d-syringaresinol-o - β - d-glucose-glucoside, symplocosigenin-o - β - d-glucopyra-noside, dihydrodehydrocarbineol (fig dihydrodehydrodiconiferylalcohol), Phenethyl glucoside, (z) - hexyl-3-enol glucoside), blumenol C GfU coside.
3. the aerial part of Epimedium wushanense contains Epimedium flavonoid glycosides and WushanIcariin(wushanicariin),Pogoside I(baohuoside)、baohuoside baohuoside VII, rouhuoside, quercetin-3-galactoside, quercetin-3-rhamnoside,Icariin a(epimedoside),Icariin, 8-prenylkaempferol-4 '- methoxy-3 - [xylosyl (L → 4) rhamnoside] - 7-glucoside {8-prenylkaempferol-4' - methoxy-3 - [xylosyl (1 → 4) rhamnoside] - 7-glucoside} in addition, it also contains inorganic elements such as calcium.
4. the aerial part of Epimedium koreanum containsIcariinandIcariin aEpimedin a, B, C, A1, B1,quercetin , dehydrated icariin-3-rhamnoside, epimedokoreanodide I and II, n-nonacosane, nhentriacotane from the underground part,Campesterol(campesterol),β - sitosterolβ - sitosterol, β - sitosterol-3-glucoside, oleosterol-3-glucoside, 2-rhamnosylikariside a, 2-rhamnosylicariin secondary glycoside II,IcariinIcariin a, ikarisioside a i.ePogoside II(baohuoside), In addition, it also contains inorganic elements such as calcium.
5. the aboveground part of Epimedium pubescens containsIcariinIcariin I, icariin C,Pogoside IIHyperin(hyperosde) and daucosterol. In addition, it also contains inorganic elements such as calcium.
In addition, the aboveground part of the same genus of sharp leaf sheep contains inorganic elements such as calcium. . Baoxing epimedium herb containsIcariinIcariin a、C,Icariin, noricariin,Pogoside ⅠPogoside IIbaohuoside Ⅲ、baohuoside Ⅳ、baohuoside baohuoside Ⅵ、baohuoside Ⅷ, baohuosu,Triterpene(tricin), Kaempfero-3-dirhamnoside andHyperinIn addition, it also contains inorganic elements such as calcium.

3、 Pharmacological effects of Epimedium
1. effect on sexual function: This product promotes sexual function because of the hypersecretion of semen, the stimulation of sensory nerves after the seminal vesicle is filled, and the indirect excitation of sexual desire. Although Epimedium water extract by gavage in dogs could not cause tail lifting reaction, it could promote the secretion of semen, with leaves and roots having the strongest effect, followed by fruits, and stems the weakest. . After Epimedium was used in patients with chronic tracheitis, the average 24-hour urinary excretion of 17 ketosterol increased significantly, even exceeding the level of healthy people, while the 24-hour urinary excretion of 17 hydroxycorticosteroids did not improve significantly. It is suggested that Epimedium has a certain role in promoting gonadal function.
. The cough inducing method with sulfur dioxide in mice proved that both methanol and ethyl acetate extracts had antitussive effects. The former can also completely inhibit the cough caused by electrical stimulation of the superior laryngeal nerve in cats, indicating that its effect is central. The methanol extract also has a protective effect on histamine induced asthma in guinea pigs.
3. anti pathogenic microorganism effect: This product has a significant inhibitory effect on Staphylococcus albus and Staphylococcus aureus, and a mild inhibitory effect on catarrhalis Nissl, Diplococcus pneumoniae and Haemophilus influenzae. Its concentration of 1% in the test tube can inhibit the growth of Mycobacterium tuberculosis. .
4. effect on cardiovascular system: 4.1. antihypertensive effect: the decoction and ethanol extract of this product have antihypertensive effect when injected intravenously into rabbits (2.5ml / kg), cats (2ml / kg) and rats (4ml / kg), of which the effect on rabbits is the most obvious. In rats with renal hypertension, intragastric administration of 10G / kg methanol extract of this product can significantly reduce blood pressure, and the blood pressure rises after withdrawal. According to the acute blood pressure test, Epimedium can inhibit and block the pressor reflex caused by bilateral common carotid arteries in rabbits, but can not block the pressor effect of norepinephrine. After atropine injection in cats, this product still has the antihypertensive effect, and the intensity is not significantly reduced, but it can significantly inhibit the blink membrane contraction response caused by electrical stimulation of pre ganglionic fibers of sympathetic nerves in cats, but has no obvious inhibitory effect on the response of electrical stimulation of post ganglionic fibers. Therefore, it is believed that the antihypertensive effect of Epimedium is not related to adrenergic a receptor and m-choline system, but mainly related to the blockade of sympathetic ganglia.
4.2. effects on the heart: the perfusion experiment of isolated rabbit hearts proved that the icariin alcohol extract and the non amino acid fraction (no5-1-1) extracted from 200% Epimedium Aqueous Extract Tablets could significantly increase the coronary flow of isolated rabbit hearts, and the latter increased by 75.3% on average compared with that before administration. Perfusing the isolated guinea pig heart with 200% Epimedium Decoction 0.5ml increased the coronary flow by 126.6% on average. The intravenous injection of no5-1-1 1g / kg in anesthetized dogs had no obvious effect on heart rate, but the coronary flow was significantly increased and the coronary resistance was significantly reduced. . No5-1-1 also has a protective effect on acute myocardial ischemia induced by Pituitrin in rats. It can significantly shorten the duration of experimental arrhythmia produced by pilocarpine K and epinephrine, although it cannot completely combat it. .
5. effect on mice's tolerance to hypoxia under normal pressure: mice were intraperitoneally injected with 0.1-0.15ml of 100% Epimedium decoction, which had a certain protective effect on Mice 'death from hypoxia.
6. effect on blood lipids: the experimental hyperlipidemic rabbits were gavaged with 100% Epimedium decoction, 5ml each time, twice a day, for a total of 30 days. After 10, 20, 30 days of administration, b-lipoprotein and cholesterol decreased, triglyceride only decreased 10 days after administration, and slightly increased 20, 30 days later.
7. effect on blood glucose: experimental hyperglycemic rats were gavaged with Epimedium extract 10mg / kg, which had obvious hypoglycemic effect, lasting for more than 60 minutes.
8. anti inflammatory effect: subcutaneous injection of 50mg / kg methanol extract of epimedium in rats can significantly reduce the degree of egg white induced foot swelling. Intragastric administration of 15g / kg in rabbits can reduce the increase in capillary permeability caused by histamine.
9. effect on immune function: Total Flavonoids of Epimedium can restore the function of antibody forming cells and antibody titer of Yang deficiency mice, significantly promote the lymphocyte stimulation index of Yang deficiency mice, making it close to normal animals. Epimedium Flavonoids can also increase the level of serum hemolysin antibody in mice, increase the number of antibody producing cells in spleen, promote PHA stimulated lymphocyte transformation reaction, and enhance the phagocytic function of peritoneal macrophages. However, 50% methanol extract of Epimedium pubescens could strongly inhibit the proliferation response of mouse lymphocytes to ConA and LPS and the mixed lymphocyte response of mice in vitro, and its inhibition rate was positively correlated with the drug concentration; In vivo, intragastric administration to mice can partially prolong the survival of cardiac allograft in neonatal rats.
10. effects on platelet aggregation and hemorheology: Herba Epimedii decoction, polysaccharides and total flavonoids can promote ADP induced platelet aggregation in normal rats, and the intensity of action is polysaccharide > Decoction > total flavonoids, and the three themselves have no effect on inducing platelet aggregation. However, Epimedium decoction can significantly reduce ADP induced platelet aggregation rate in healthy people and promote platelet disaggregation in some subjects. After oral administration of Epimedium Decoction to healthy people, the hematocrit was significantly reduced, the erythrocyte electrophoresis time was shortened, and the erythrocyte sedimentation rate was accelerated, thus the whole blood specific viscosity was significantly reduced.
11. effect on nucleic acid metabolism: gavage of Epimedium water decoction to mice with Yang deficiency caused by hydroxyurea can significantly improve their DNA synthesis rate. In vitro test of Epimedium Polysaccharide can increase the bone marrow cell proliferation rate and DNA synthesis rate of mice with Yang deficiency caused by hydroxy porpoise by 72% and 68%.
12. other effects: the alcohol extract of Epimedium has an antagonistic effect on catecholamines, which is similar to propranolol. Mice were intraperitoneally injected with 10% Epimedium Decoction 20ml / kg, which had obvious sedative effect. Yinyanghuo can regulate the M receptor cGMP system, and its processed products can also significantly improve sexual function, increase the weight of accessory sexual organs, and increase the plasma testosterone content. It also has anti-aging effect.

[toxicity] Epimedium made in Japan can dilate the pupil of frogs, increase the voluntary movement of mice, and cause hyperreflexia, which often causes mild spasm, so that they die of respiratory arrest, and the heart continues to beat for a certain time after respiratory arrest. The median lethal dose of Epimedium extract in mice injected intraperitoneally was 36g / kg, and that of no5-1-1 mice injected intravenously was 56.8 ± 2.7g / kg. The methanol extract of this product has low toxicity. Mice were gavaged with 450g/kg and observed for 3 consecutive days. The results showed that the activity was normal and there was no toxic reaction. The Japanese produced lewd sheep can make the pupils of frogs dilate, the mice move at will and have hyperreflexia. They often have mild spasms, and then die of respiratory arrest.
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