Forsythia suspensa
1、 Pharmacopoeia standard of Forsythia suspensa       This product is the dried fruit of Forsythia suspensa (thunb.) Vahl, a plant of Oleaceae. When the fruit is green at the first ripening in autumn, it is harvested to remove impurities, steamed, and dried in the sun. It is commonly known as "green Forsythia"; When the fruit is ripe, it is harvested, dried in the sun, and impurities are removed. It is commonly known as "old warping".
      [character]   This product is long ovoid to ovoid, slightly flat, 1.5-2.5cm long, 0.5-1.3cm in diameter. There are irregular longitudinal wrinkles and most protruding small spots on the surface, and there is an obvious longitudinal groove on both sides. The top is sharp, and the base has small fruit peduncles or has fallen off. Most of the green warps do not crack, and the surface is greenish brown, with few gray white spots raised; Hard quality; The seeds are mostly yellowish green, slender, with wings on one side. The old Forsythia crazes or splits into two petals from the top, the surface is yellowish brown or reddish brown, and the inner surface is mostly light yellowish brown, smooth, with a mediastinum; ; The seeds are brown, and most of them have fallen off. It smells slightly fragrant and tastes bitter.
      [identification]   (1) Cross section of the peel of this product: the exocarp is a row of flat cells, the outer wall and side wall are thickened and covered with cuticle. Vascular bundles were scattered in the lateral parenchyma of mesocarp; The inner side of mesocarp is multilayered stone cells, which are strip-shaped, quasi circular or oblong, with different wall thicknesses and multi tangential mosaic arrangement. The endocarp is a row of parenchyma cells.
      (2) Take 1g of this product powder, add 20ml of petroleum ether (30 ～ 60 ℃), close the plug, sonicate for 15 minutes, filter, discard the petroleum ether liquid, volatilize the petroleum ether from the residue, add 20ml of methanol, close the plug, sonicate for 20 minutes, filter, evaporate the filtrate, add 5ml of methanol to dissolve the residue, and use it as the test solution. Another 1g of Forsythia suspensa reference medicinal material was prepared into the reference medicinal material solution by the same method. Then take phillyrin reference substance and add methanol to make a solution containing 0.25mg per 1ml as the reference solution. According to the test of thin-layer chromatography (general rule 0502), suck 3 μ l of each of the above three solutions, respectively dot on the same silica gel G thin-layer plate, use chloroform methanol (8:1) as the developing agent, develop, take out, dry, spray 10% sulfuric acid ethanol solution, and heat at 105 ℃ until the spots are clear. .
      [check]   Impurities shall not exceed 3%; No more than 9% of the elderly (general rule 2301).
      The moisture content shall not exceed 10.0% (the fourth method of general rule 0832).
      The total ash content shall not exceed 4.0% (general rule 2302).
      ; Old warpage shall not be less than 16.0%.
      [content determination]   Forsythin was determined by HPLC (general rule 0512).
      Chromatographic conditions and system suitability test   Octadecylsilane bonded silica gel was used as filler; Acetonitrile water (25:75) was used as mobile phase; .
      Preparation of reference solution   Take an appropriate amount of phillyrin reference substance, weigh it accurately, add methanol to make a solution containing 0.2mg per 1ml.
      Preparation of test solution   Take about 1g of this product powder (passing through No. 5 screen), weigh it accurately, place it in a corked conical flask, add 15ml of methanol precisely, weigh it, soak it overnight, sonicate it (power 250W, frequency 40KHz) for 25 minutes, cool it, weigh it again, use methanol to make up for the lost weight, shake it well, filter it, accurately measure 5ml of continuous filtrate, evaporate it to near dryness, add 0.5g of neutral alumina, mix it well, add it on a neutral alumina column (100-120 mesh, 1g, inner diameter 1-1.5cm), elute with 80ml of 70% ethanol, collect the eluent, concentrate it to dryness, dissolve the residue with 50% methanol, and transfer it to 5ml L in a measuring flask, dilute to the scale, shake well, filter, and take the continued 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.
      According to the calculation of dry product, the content of phillyrin (c27h34o11) shall not be less than 0.15%.
      Forsythiaside a  Determine according to high-performance liquid chromatography (general rule 0512).
      ; Octadecylsilane bonded silica gel was used as filler; The mobile phase was acetonitrile-0.4% glacial acetic acid solution (15:85); The detection wavelength was 330nm. The theoretical plate number should not be less than 5000 according to forsythiaside a peak.
      Preparation of reference solution   Take an appropriate amount of forsythiaside a reference substance, accurately weigh it, add methanol to make a solution containing 0.1mg per 1ml, and then get it (prepared for clinical use).
      Preparation of test solution   Take about 0.5g of this product powder (passing through No. 5 screen), weigh it precisely, place it in a corked conical flask, add 15ml of 70% methanol precisely, close the stopper, weigh it, sonicate (power 250W, frequency 40KHz) for 30 minutes, cool it, weigh it again, make up the weight lost with 70% methanol, shake it well, filter it, and take the filtrate.
        ; 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.
      According to the calculation of dry product, the content of forsythiaside a (c29h36o15) shall not be less than 0.25%.
      [nature, taste and meridian tropism]   Bitter, slightly cold. .
      ; It can clear away heat and toxin, dissipate swelling and nodules, and evacuate wind heat. It is used for carbuncle and gangrene, scrofula, breast carbuncle, erysipelas, wind heat and cold, febrile disease at the beginning, warm fever entering the camp, high fever and thirst, dizziness and spots, hot shower and pain.
      [usage and dosage]   6～15g。
      [storage]   Place in a dry place.


2、 Chemical constituents of Forsythia suspensa
Fruit contains lignans:Forsythin（forsythin，phillyrin）[1]，Forsythin（phillygenin）， Pinoresin ol [2,3], pinoresinol - β - D-glucoside [3,4]; Flavonoids:rutin（rutin）[2,4]； Phenylethane derivatives:Forsythin a（forsythoside）、ForsythinC、ForsythinD、ForsythinE[5]， Forsythiaside [6],Salidroside（salidroside）[5]； ,Forsythia cyclohexanol（rengyol）， Isorengyol, rengyoxide, rengyolone, rengyoside a, B, c[5]; Triterpenoids:Betulinic acid（betulinic acid），oleanolic acid （oleanolic acid）［2］，Ursolic acid（ursolic acid）［3］，β - Caryophyllin ethyl ester（β-amyrin acetate）， Isobauerenyl acetate, 20 (s) - dammar-24-ene-3 β, 20-diol-3-acetate [7], etc.

3、 Pharmacological effects of Forsythia suspensa
1. antibacterial and antiviral effects 1.1. antibacterial effect: the volatile oil emulsion of Forsythia suspensa seeds was tested by tube dilution method. The results showed that the drug had strong antibacterial effect on 10 strains of gram positive and negative bacteria except for Pseudomonas aeruginosa. Among them, the effect on Staphylococcus aureus was the strongest (the antibacterial titer was 1 / 1.024); ; Streptococcus A and B; Catarrhalis; Shigella flexneri; Paratyphoid A; (the antibacterial titer was 1 / 512) and Escherichia coli (the antibacterial titer was 1 / 256), and the antibacterial titers against pneumoniae and Proteus vulgaris were 1 / 28. The test solution with antibacterial effect on the tested bacteria was selected for subculture test. The results showed that the antibacterial effect of Forsythia suspensa seed volatile oil on the tested bacteria was thorough and stable. The concentrated decoction of Forsythia suspensa has antibacterial effect in vitro, and can inhibit typhoid bacillus, paratyphoid bacillus, Escherichia coli, dysentery bacillus, Diphtheria Bacillus, Vibrio cholerae, Staphylococcus, Streptococcus, etc. ; It is the main antibacterial component in yinqiao powder. The inhibitory effect of honeysuckle on Salmonella spp., especially typhoid bacillus and hemolytic streptococcus seems to exceed Forsythia suspensa, while Forsythia suspensa seems to be better for dysentery bacillus and Staphylococcus aureus. The combination of the two has no synergistic effect in the test tube. The compound with Coptis chinensis and Scutellaria baicalensis has stronger antibacterial effect in vitro than Forsythia suspensa alone. There are few studies on the antibacterial active ingredients in Forsythia suspensa. The antibacterial concentration of forsythiol against Staphylococcus aureus in the trial camp is 1:5120; 1:1280 for Shigella; It is 1:640 against diphtheria bacilli and paratyphoid (a) bacilli, and can be used as an antibacterial active ingredient. Flower has certain curative effect on experimental tuberculosis in mice, but has no effect on guinea pigs. In addition, its anti tuberculosis effect in vitro and in clinic has also been reported. . Forsythia suspensa water extract (1:5) has some inhibitory effect on Nocardia staphyloma in the test tube.
1.2. antifungal effect: the volatile oil emulsion of Forsythia suspensa seeds was tested against Candida albicans and Candida tropicalis by tube dilution method. The results showed that the drug had obvious antibacterial effect on the two strains tested, and its antibacterial titers were 1 / 1.024 and 1 / 512, respectively.
1.3. antiviral effect the volatile oil emulsion of Forsythia suspensa seeds was tested for its effect against Asian influenza A virus and type I parainfluenza virus by the in embryo method (drug concentration of 1 / 32) and the in embryo method. . It can be seen that the volatile oil emulsion of Forsythia suspensa seeds has significant antiviral effect on Jingke 68-1 strain and Sendai strain virus outside the chicken embryo. The antiviral titer of the two viruses tested was 1 / 65536. By dot blot hybridization test, Forsythia suspensa Decoction at a concentration of 25% - 100% can reduce the content of hepatitis B virus deoxyribonucleic acid (HBVDNA).
2. effects on cardiovascular system 2.1. effects of Forsythia suspensa injection on the heart of cats in vivo during toxic shock: three cats were used in the experiment. They were anesthetized intraperitoneally, blood pressure was measured by carotid intubation, endotracheal intubation was performed, and an electric artificial ventilator was connected. The chest and pericardium were opened to expose the heart. The heart tip was connected to a micro tension sensor with silk thread, and the cardiac relaxation and contraction curves were recorded with a three pen recorder. Before the experiment, first trace a section of myocardial relaxation and contraction and blood pressure curve as a normal control, and then intravenously inject typhoid vaccine 0.8-2.5ml / kg to wait for more obvious damage to the myocardial curve (the height of myocardial relaxation and contraction wave is uneven, the rhythm is irregular), and the blood pressure drops. After intravenous injection of Forsythia suspensa injection 8g / kg, the heart rhythm became homogeneous, and the amplitude of myocardial systolic and diastolic waves increased in two cats, and the blood pressure increased about 40mmhg after 30 minutes. It suggests that it has cardiotonic and pressor effects.
2.2. effects on capillary permeability healthy mice of either sex weighing 18-22g were selected and divided into experimental group and control group. Seven animals in the experimental group were injected with Forsythia suspensa injection (60g/kg) via tail vein or subcutaneous injection, and nine animals in the control group were injected with normal saline instead of drugs (0.4ml / mouse). After 10 minutes, 0.2ml of 0.5% Evans blue solution was injected into the tail vein. After 30 minutes, 0.4ml of 0.4% acetic acid was injected intraperitoneally. After another 30 minutes, the mice were sacrificed by exsanguination. The abdominal cavity was opened and the peritoneal exudate was rinsed with normal saline. The washout was placed in a 5ml graduated tube to the scale, and the heart was separated at 2000 rpm for 10 minutes. The supernatant was taken to determine the concentration of Evans blue. Results the concentration of Evans blue (μ g%) in the peritoneal exudate of the control group was 368.47 ± 28.55 (mean ± standard deviation, the same below), while that of the experimental group was 160.12 ± 28.37 (P < 0.01). .
3. the inhibitory effect on isolated small intestine of guinea pigs was tested, and the isolated intestinal specimens were made according to the magnur method. . The contraction amplitude was weakened 8 times and unchanged 2 times. Equal volume normal saline had no effect on isolated intestine. It is suggested that Forsythia suspensa has inhibitory effect on isolated small intestine of guinea pigs.
4. inhibition of elastase activity: Forsythia suspensa et al. Diluted into three concentrations of 1.5g, 0.75g and 0.375g per 1ml. Porcine pancreatic elastase (PPE) was diluted into two concentrations of 19U / 0.5mg · ml and 9.5u / 0.25mg · ml. After mixing the 19U / 0.5mg · ml enzyme solution with the above drugs of different concentrations in equal amounts, take 10 μ l each and drop them into the agar plate wells. Leave two wells in each dish with 10 μ L and 9.5u / 0.25mg · ml enzyme solution as the parallel control for enzyme dissolution. Measure the diameter of the dissolution loop after incubation at 37 ℃ for 24 hours. . The effect of Forsythia suspensa on elastase activity is shown in Table 5. It can be seen that Forsythia suspensa at three concentrations can significantly inhibit the enzyme activity of 0.095u of PPE (P < 0.001), and the enzyme activity of PPE is completely inhibited at the concentration of 7.5mg. .
5. radiation damage resistance. The methanol extract of Forsythia suspensa (1g/kg) was injected intraperitoneally and administered 5 minutes before X-ray irradiation, which had a protective effect on skin damage in mice.