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Release Date:2017/9/8 11:08:56
Ophiopogon japonicus
1、 Pharmacopoeia standard of Ophiopogon japonicus
Ophiopogon japonicus
Maidong
OPHIOPOGONIS RADIX
      This product is the dried root of Ophiopogon japonicus (L.f) Ker Gawl, a lily plant. Excavate in summer, wash, repeatedly expose to the sun, pile up, and dry to 70% or 80%, remove fibrous roots, and dry.
      [character]   This product is spindle shaped, slightly pointed at both ends, 1.5 ~ 3cm long, 0.3 ~ 0.6cm in diameter. The surface is light yellow or grayish yellow, with fine longitudinal lines. It is flexible, with yellowish white section, translucent, and small central column. It is slightly fragrant and tastes sweet and bitter.
      [identification] (1) cross section of this product: 1 column of epidermal cells or exfoliation, and 3-5 columns of lignified cells in the root coat. The cortex was broad, with scattered mucus cells containing calcium oxalate needle crystal bundles, and some needle crystals were up to 10 μ m in diameter;the diameter of the needle crystal was 0.5 μ M.The diameter of the needle crystal was 0.5 μ M.The diameter of the needle crystal was 0.5 μ M.The diameter of the needle crystal; The cell wall of the endothelial layer is uniformly thickened, lignified, with channel cells, and a row of stone cells on the outside. Its inner wall and side wall are thickened, and the pits are fine and dense. The stele is smaller, with 16-22 phloem bundles, and the xylem is connected into a ring layer by vessels, tracheids, wood fibers, and inner lignified cells. The pulp is small, and the thin walled cells are round.
      (2) . Another 2G of Ophiopogon japonicus reference medicinal material was prepared into the reference medicinal material solution by the same method. According to the test of thin-layer chromatography (general rule 0502), suck 6 μ l of each of the above two solutions, dot them on the same silica gel gf254 laminate respectively, use toluene methanol glacial acetic acid (80:5:0.1) as the developing agent, develop, take out, dry, and view under the UV light (254mn). In the chromatogram of the test sample, spots of the same color appear on the corresponding position of the chromatogram of the control medicinal material.
      [check]   The moisture content shall not exceed 18.0% (the second method of general rule 0832).
      The total ash content shall not exceed 5.0% (general rule 2302),
      [extract]   It shall be determined according to the cold leaching method under the determination method of water-soluble extract (general rule 2201), and shall not be less than 60.0%.
      [content determination]   Preparation of reference solution take an appropriate amount of Ruscogenin reference substance, weigh accurately, add methanol to make a solution containing 50 μ g per 1ml.
      Preparation of standard curve   Accurately measure 0.5ml, 1ml, 2ml, 3ml, 4ml, 5ml, 6ml of the reference solution, respectively, put it into a stoppered test tube, volatilize the solvent in a water bath, precisely add 10ml of perchloric acid, shake it well, keep it in hot water for 15 minutes, take it out, cool it with ice water, take the corresponding reagent as blank, measure the absorbance at the wavelength of 397nm by UV visible spectrophotometry (general rule 0401), and draw a standard curve with absorbance as the ordinate and concentration as the abscissa.
      ; Take about 3G of fine powder of this product, accurately weigh it, place it in a corked conical flask, accurately add 50ml of methanol, weigh it, heat and reflux for 2 hours, cool it, weigh it again, use methanol to make up for the weight lost, shake it well, filter it, accurately measure 25ml of the continuous filtrate, recover the solvent to dryness, add 10ml of water to dissolve the residue, shake and extract with saturated n-butanol for 5 times, 10ml each time, combine the n-butanol solution, wash it twice with ammonia test solution, 5ml each time, discard the ammonia solution, and evaporate the n-butanol solution to dryness. Dissolve the residue with 80% methanol, transfer to a 50ml volumetric flask, add 80% methanol to the scale, and shake well. Accurately measure 2 ~ 5ml of the test solution, put it into 10ml plugged test tube, according to the method under the preparation of the standard curve, measure the absorbance according to the law from "volatilizing the solvent in the water bath", read the weight of Ruscogenin in the test solution from the standard curve, and calculate.
      The total saponin content of Ophiopogon japonicus should not be less than 0.12% based on Ruscogenin (c27h42o4) calculated as dry product.
      Decoction pieces
      [processing]   Remove impurities, wash, moisten, flatten and dry.
      This product is shaped like Ophiopogon japonicus, or a flattened spindle shaped piece. The surface is light yellow or grayish yellow, with fine longitudinal lines. . It is slightly fragrant and tastes sweet and bitter.
      [character], [identification], [inspection], [content determination], [1]  Same as medicinal materials.
      [nature, taste and meridian tropism]   Sweet, slightly bitter, slightly cold. .
      ; Nourish yin and generate fluid, moisten lung and clear heart. It is used for lung dry cough, yin deficiency tuberculosis cough, throat obstruction and sore throat, fluid injury and thirst, internal heat and thirst, upset and insomnia, intestinal dryness and constipation.
        [usage and dosage]   6~12g。
      [storage]   Store in a cool and dry place and keep away from moisture.


2、 Chemical constituents of Ophiopogon japonicus
The root tubers of Ophiopogon japonicus contain a variety of glucosides: aglycones areRuscogenin(Ruscogenin) has ophiopogonin B and D; The aglycones are (22s, 24s, 25s) - 23-24-dihydroxyroscoegenin [(23S, 24s, 25s) - 23, 24 dihydroxyroscoegenin] (23S, 24s, 25s) - 23, 24 dihydroxyroscoegenin-1-o - [α - l-rhamnopyranosyl (1 → 2)] [β - d-xylopyranosyl (1 → 3)] - α - l-arabinopyranoside-24-o - β - d-fucopyranoside {(23S, 24s, 25s) -23,the, 24-dihydroxyruscogenin-1-o - [α - l-rhamnopyranosyl (1 → 2)] [β - d-xylopyranosyl (1 → 3)]- α-L-arabinopyranoside-24-O-β-D-fucopyranoside},(23S,24S,25S)-23, 24-dihydroxyroscoene-1-o - [α - L-2, 3, 4-tri-o-acetylrhamnopyranosyl (1 → 2)] [β - d-xylopyranosyl (1 → 3)] - α - l-arabinopyranoside-24-o - β - d-fucopyranoside {(23S, 24s, 25s) -23, 24-dihydroxyruscogenin-1-o-[α - L-2, 3, 4-tri-o-acetylrhamnopyranosyl (1 → 2)] [β - d-xylopyranosyl (1 → 3)] - α - l-arabinopyranoside-24-o - β - d-fucopyranoside}, (23S, 24s, 25s) - 23,24-dihydroxyroscoegenin-1-o - [α - l-4-o-acetylrhamnopyranosyl (1 → 2)] [β - d-xylopyranosyl (1 → 3)] - α - l-arabinopyranoside-24-o- β - d-fucopyranoside {(23S, 24s, 25s) -23, 24-dihydroxyruscogenin-1-O-[α-L-4-O-acetylrhamnopyranosyl(1→2)][β-D-xylopyranosyl(1→3)]-α-L-arabinopyranoside-24-O-β-D-fucopyranoside}; Diosgenin has Ophiopogon saponin d', diosgenin-3-o - [α - l-rhamnopyranosyl (1 → 2)] - (3-o-acetyl) - β - d-xylopyranosyl (1 → 3) - β - D-glucopyranosyl {diosgenin-3-o - [α - l-rhamnopyranosyl (1 → 2)] - (3-o-acetyl) - β - d-xylopyranosyl (1 → 3) - β - d-glucopyranoside.Side}, Diosgenin-3-o - [(2-o-acetyl) - α - l-rhamnopyranosyl (1 → 2)] [β - d-xylopyranosyl (1 → 3)] - β - d-glucopyranoside {diosgenin-3-o - [(2-o-acetyl) - α - l-rhamnopyranosyl (1 → 2)] - β - d-xylopyranosyl (1 → 3) - β - d-glucopyranoside}; ; Www.med126.com aglycones are borneol-2-o - β - d-glucopyranoside, l-borneol-2-o - β - d-apiofuranosyl (1 → 6) - β - d-glucopyranoside [borneol-2-o - β - d-apiofuranosyl (1 → 6) - β - d-glucopyranoside], borneol-2-o - α - l-furanoarabinosyl (1 → 6) - β - d-glucopyranoside,β - d-glucopyranoside [borneol-2-o - α - l-arabinofuranosyl- (1 → 6) - β - d-glucopyranoside]. It also contains high homoisoflavonoid components:Methyl Ophiopogon flavanone a(methylophiopogonanone)、Methyl Ophiopogon flavanoneB, ophiopogonanone aOphiopogon flavanoneB,6-aldehyde isoophiopogon flavanone a(6-aldehydo-7-O-methylisoophiopogonanone)、B, 6-aldehydoisoophiopogonone a, B, Ophiopogon a, desmethylisoophiopogonone B, 5,7,2 '- trihydroxy-6-methyl-3 - (3', 4 '- methylenedioxybenzyl) chromone [5,7,2' - trihydroxy-6-methyl-3 - (3 ', 4' - methylenedioxybenzyl) chromone], 5,7,2 '- trihydroxy-8-methyl-3 - (3', 4 '- methylenedioxybenzyl) chromone,3', 4'- methylenedioxybenzyl) chromone [5, 7, 2'-trihydroxy-8-methyl-3-(3',4'-methylenedioxybenzyl)chromone], Racemic 5-hydroxy-7,8-dimethoxy-6-methyl-3 (3', 4'- dihydroxybenzyl) chromanone [5-hydroxy-7,8-dimethyl-6-methyl-3- (3', 4'-dihydroxybenzyl) chromanone]. It also contains ruscogenin-1-o-sulfate, calcium Bornyl sulfate, Ophiopogon aglycone,Glycerol(glycerol), n-[β - hydroxy - β - (4-hydroxy) benzene) ethyl-4-hydroxycinnamamide]{n-[β - hydroxy - β - (4-hydroxy) phenyl]ethyl-4-hydroxycinnamide} andβ - sitosterol(β-sitosterol),StigmasterolStigmasterol, β - sitosterol-3-o - β - d-glucopyranoside, etc. It also contains volatile oil, from which Longifolene, α - and β - patchoulene, cyperene,Guaiacol(guaiol), α - humulene,camphor(camphor),Linalool(linalool), Terpinen-4-ol, jasmolone and other components. It also contains 28 inorganic elements such as potassium, sodium, calcium, magnesium, iron, copper, cobalt, manganese, chromium, lead, nickel, barium, zinc, etc. , (25s) - roscoegenin 1-O - β - d-xylopyranose-3-o - α - l-rhamnopyranoside [(25s) - Ruscogenin 1-O - β - d-xylopyranoside-3-o - α - l-rhamnopyranoside], (25s) - roscoegenin 1-O - [(2-o-acetyl) - α - l-rhamnopyranosyl (1 → 2)] [β - d-xylopyranosyl (1 → 3)] - β - d-fucopyranoside {(25s) -ruscogenin cogenin 1-o-[(2-o-acetyl) - α - l-rhamnopyranosyl (1 → 2)] [β - d-xylopyranosyl (1 → 3)] - β - d-fucopyranoside}, (25s) - roscoegenin 1-o-[(3-o-acetyl) - α - l-rhamnopyranosyl (1 → 2)] [β - d-xylopyranosyl (1 → 3)] - β - d-fucopyranoside {(25s) -rucosgenin 1-o-[(3-o-acetyl) - α - l-rhamnopyranosyl (1 → 2)] [β - d-xylopyranosyl (1 → 3)] - β - d-glucopyranoside}, Yamogenin-3-o - [α - l-rhamnopyranosyl (1 → 2)] [β - d-xylopyranosyl (1 → 3)] - β - d-glucopyranoside {yamogenin3-o - [α - l-rhamnopyranosyl (1 → 2)] [β - d-xylopyranosyl (1 → 3)] - β - d-glucopyranoside}, (25s) - roscoegenin 1-O - α - l-rhamnopyranosyl (1 → 2) - β - d-xylopyranoside glucoside [(25s) - Ruscogenin 1-O - α - l-rhamnopyranosyl (1 → 2) - β - d-xylopyranoside]. The root contains 1-n-butyl - β - d-fructopyranoside, L-pyroglutamic acid and adenosine.

3、
1. effects on the central nervous system: after intraperitoneal injection of 0.5ml/10g total amino acids of Ophiopogon japonicus into mice for 30 minutes, intraperitoneal injection of 30mg / kg sodium pentobarbital was used to observe the number of animals whose righting reflex disappeared. Results the total amino acids of Ophiopogon japonicus had obvious synergistic central inhibitory effect (P < 0.05), while the total saponins and total sugars of Ophiopogon japonicus had no obvious effect on the effect of pentobarbital sodium at subthreshold hypnotic dose. 15% Ophiopogon japonicus preparation 10ml / kg gavage could inhibit the fever of rabbits injected with turpentine 2.0ml / kg (P < 0.01), but the drug had no inhibitory effect after fever. Ophiopogon japonicus decoction has sedative effect, can also strengthen the sedative effect of chlorpromazine, enhance the hypnotic effect of pentobarbital sodium, antagonize the excitatory effect of caffeine, and can delay the time of convulsion, tonic convulsion and death caused by huisuling, but it can not prevent the animal from death.
2. impact on cardiovascular system:.
2.1. effects on the cardiac function of isolated toad hearts: demonstrated by perfusion of isolated toad hearts using the Yagi Hartung method; Total saponin I (crude extract) of Ophiopogon japonicus has the strongest effect on enhancing myocardial contractility, while total saponin II (purer extract) has less effect than total saponin I. generally, the enhancement of myocardial contractility is accompanied by the increase of cardiac output. Large doses of total saponins Ⅰ, Ⅱ and total sugar can inhibit the heart, which can weaken myocardial contractility, reduce cardiac output, atrioventricular block, or even arrest. Total saponins Ⅰ, Ⅱ, total sugar and total amino acids generally have no obvious effect on heart rate, which is slightly slower or unchanged.
2.2. effects on the amplitude of myocardial contraction in isolated guinea pig hearts: perfusion of isolated guinea pig hearts with Langendorff method showed that low doses of total saponins and total amino acids of Ophiopogon japonicus could enhance myocardial contractility and increase coronary flow, while high doses inhibited myocardium and reduced coronary flow, but both had no effect on heart rate.
2.3. antiarrhythmic effect and its electrophysiological characteristics: Total Saponins of Ophiopogon japonicus 10mg / kg intravenously can effectively prevent or combat arrhythmias induced by CHCl3 ADR, BaCl2, ACO, and reduce the incidence of ventricular arrhythmias from 87 ± 8 to 57 ± 7% after 24 hours of coronary artery ligation in dogs. Electrophysiological experiments showed that total saponins of Ophiopogon japonicus 15mg / kg could significantly reduce the Vmax of monophasic action potential and shorten its apd10 and apd50 in rabbits; Total saponins of Ophiopogon japonicus (50 μ g / ml) could also significantly reduce APA, Vmax, apd10, apd50 of transmembrane action potential in guinea pig papillary muscle cells; At the same time, ERP / APD increased significantly. . The experimental dogs with myocardial infarction were treated with magnesium sulfate 2.5G, Ophiopogon 20g diluted in 500ml glucose normal saline by intravenous infusion. The frequency of premature beats in 6h and 24h after the treatment was compared with that in the control group. The results showed that Ophiopogon contract with low-dose magnesium sulfate had a certain preventive effect on arrhythmia after myocardial infarction. Medical Online www.med126.com
. Results at 15 minutes after operation, camp and cGMP in the control group continued to increase, while those in the Ophiopogon group showed a downward trend (P < 0.05). At 30 minutes after operation, those in the Ophiopogon group were still lower than those in the control group (P < 0.02), and returned to the preoperative level at 60 minutes after operation. Changes of plasma cAMP / cGMP ratio: there was no significant difference between the two groups before operation, but the ratio decreased in both groups immediately after operation; In the control group, the continuous decline was 4.6 ± 1.61 at 15 and 30 minutes after operation, respectively; 4.57 ± 2.01; However, the level of Ophiopogon japonicus group was close to the preoperative level, which was 6.46 ± 2.12 and 6.48 ± 2.39 respectively (P < 0.05). 60 minutes after operation, the level of Ophiopogon japonicus group still maintained the preoperative level, while the control group had an upward trend, and there was no significant difference between the two groups. After acute myocardial infarction, the plasma cAMP and cGMP levels were significantly higher than normal. It may be a stress response. A large number of cardiomyocytes are necrotizing and dissolving, releasing camp and cGMP, increasing the level in plasma, reflecting the degree of myocardial injury. Because the increase of cGMP is more obvious than that of camp during myocardial ischemia, the ratio of cAMP / cGMP decreased significantly after myocardial infarction. Ophiopogon japonicus may increase myocardial nutrient blood flow after infarction, repair and protect ischemic and hypoxic cardiomyocytes quickly, reduce the release of myocardial cGMP and camp, thereby reducing the content in plasma, and restore the balance of the ratio of the two.
3. effect on animal immune activity:.
3.1. effect on hypoxia tolerance of mice under normal pressure: take 30 ICR mice of 18-20g, and inject Ophiopogon japonicus polysaccharide and total saponins of ginseng (20mg / kg) intraperitoneally respectively. The control uses the same amount of normal saline. After 30 minutes, place them in a closed wide mouth bottle containing sodium lime, and record the time of death of the mice. Results the survival time of mice in Ophiopogon japonicus polysaccharide group was significantly longer than that in the control group (P < 0.01).
3.2. effect on the weight of immune organs: ICR mice were injected with Ophiopogon japonicus polysaccharide and total ginsenoside (dose 10mg / kg) intraperitoneally, and the control was given the same amount of normal saline. After 7 days of continuous administration, the animals were sacrificed by exsanguination. The body weight and the weight of thymus and spleen were weighed, and the thymus index and spleen index were calculated. Results Ophiopogon japonicus polysaccharide could significantly increase the spleen weight of mice (P < 0.01), but had no obvious effect on thymus.
3.3. effect on carbon clearance in mice: ICR mice were injected with Ophiopogon japonicus polysaccharide, total ginsenosides of ginseng (10mg / kg) and normal saline intraperitoneally for 7 consecutive days. After the last administration, 0.1ml / 10g diluted 3 times of Chinese carbon ink was given by tail vein, and the clearance index was calculated respectively. Results Ophiopogon japonicus polysaccharide group could significantly enhance the carbon clearance of mice (P < 0.01 =. Www.med126.com
3.4. effect on the decrease of white blood cell number in mice caused by cyclophosphamide and 60cor irradiation: Ophiopogon japonicus polysaccharide 10mg / kg had a very significant antagonistic effect on the decrease of white blood cell caused by intraperitoneal injection of 0.4ml cyclophosphamide (5mg / ml) in mice (P < 0.01). The same dose of Ophiopogon japonicus polysaccharide was injected intraperitoneally for 8 days. The mice were placed 60cm away from the irradiation source (60cor) for irradiation at a total dose of 20.64c/kg on the 8th day after administration. The mice were given the same dose for 3 days after irradiation. On the 7th day after irradiation, the blood was taken from the orbit and the number of white blood cells was calculated. Results Ophiopogon japonicus polysaccharide could significantly resist the white blood cell decline caused by 60cor radiation (P < 0.01 =).
3.5. Ophiopogon japonicus polysaccharide can significantly promote the formation of hemolysin in mouse serum, and has lectin like effect on rabbit red blood cells.
3.6.ophiopogon japonicus Decoction injected intraperitoneally into mice at a dose equivalent to 12.5g crude drug / kg can significantly increase the spleen weight of mice; ; It can significantly resist the leukopenia caused by cyclophosphamide.
3.7. effects on humoral immunity and cellular immunity: BALB / C young mice were paired into experimental group and control group. After feeding for 1 month, each mouse was injected with 400million sheep cells (0.2ml). After injection, blood was taken regularly, antibodies were measured, and HC50 was calculated. The results showed that Ophiopogon japonicus whiskers could promote antibody production and delay antibody regression (P < 0.05). The spleen cell suspensions of BALB / c mice in two groups were used, two with pha60 μ g/ml and one without schizogen. After 72h of culture, the lymphocyte transformation stimulation index was measured by scintillation instrument after 3H thymidine incorporation. The results showed that Ophiopogon japonicus fibrous root extract had the effect of improving cellular immunity.
3.8. effect on immune function of tumor bearing mice: Ophiopogon japonicus whisker aqueous solution significantly increased the white blood cells and T cells of NIH pure line inoculated with S180 and EAC cancer cells (P < 0.01 or P < 0.05). .
. The inhibition rate of monoamine oxidase (MAO-B) in the brain of male mice was 38.6%. SOD activity in the liver of male mice increased by 45.5%. The life span test of Drosophila melanogaster also showed that Ophiopogon japonicus root whisker feed significantly prolonged the life span of Drosophila melanogaster, suggesting a trend of delaying aging. Swimming test showed that saponins, polysaccharides and amino acids contained in Ophiopogon japonicus had obvious anti fatigue effect.
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