Xanthium sibiricum
1、 Pharmacopoeia standard of Xanthium sibiricum       This product is the dry and mature fruit with involucre of Xanthium sibiricum patr., a composite plant. The fruits are harvested when they are ripe in autumn, dried, and the impurities such as stems and leaves are removed.
      [character]   The product is spindle shaped or oval, 1-1.5cm long and 0.4-0.7cm in diameter. The surface is yellowish brown or yellowish green, and all have barbs. There are two thicker barbs at the top, separated or connected, and there are fruit stem marks at the base. It is hard and tough, with a longitudinal septum in the center of the transverse section, 2 chambers, and 1 achene each. Achene is slightly spindle shaped, one side is relatively flat, the top has a raised stylar base, and the pericarp is thin, gray black, with longitudinal lines. . The breath is slight, and the taste is slightly bitter.
      [identification] (1) the powder of this product is yellowish brown to yellowish green. The involucral bracts are fibrous and often arranged vertically and horizontally. Pericarp epidermal cells are brown, oblong like, and often connected with the underlying fibers. The pericarp fibers are in bundles or scattered individually, elongated fusiform, and the pits and pore grooves are obvious or not obvious. The seed coat cells are pale yellow, the outer cells are polygonal, and the wall is slightly thick; . Wood parenchyma cells are oblong like and have pits. The cotyledon cells were vaguely powdered and oil droplets.
      (2) . Another 2G of Xanthium sibiricum L. reference medicinal material was prepared by the same method. According to the test of thin-layer chromatography (general rule 0502), suck 4 μ l of each of the above two solutions, dot them on the same silica gel G thin-layer plate, use the upper solution of n-butanol glacial acetic acid water (4:1:5) as the developing agent, develop, take out, air dry, and smoke in ammonia vapor until the spots are clear. 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]   Moisture   Not more than 12.0% (the second method of general rule 0832).
      The total ash content shall not exceed 5.0% (general rule 2302).
      Carboxy Atractyloside   Determine according to high-performance liquid chromatography (general rule 0512).
      ; ; The mobile phase was acetonitrile-0.01mol/l sodium dihydrogen phosphate solution (pH adjusted to 5.4 with 4% sodium hydroxide solution) (10:90). The detection wavelength was 203nm. The number of theoretical plates should not be less than 5000 according to the peak of carboxyl Atractyloside.
      Preparation of reference solution   Take an appropriate amount of carboxyatractyloside Tripotassium salt reference substance, accurately weigh it, add water to make a solution containing 0.1mg per 1ml, and get it (weight of carboxyatractyloside = weight of carboxyatractyloside Tripotassium salt /1.1482).
      Preparation of test solution   Take about 1g of this product powder (passing through No. 3 screen), weigh it precisely, place it in a conical flask with a stopper, add 20ml of water precisely, weigh it, sonicate (power 300W, frequency 40KHz) for 40 minutes, cool it, weigh it again, make up the lost weight with water, shake it well, centrifuge (rotating speed 12000 rpm, 5 minutes), take the supernatant, filter it, take the filtrate, and get it.
      Assay   Precisely suck 5 μ l of the reference solution and 5 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 carboxyatractyloside (c31h46o18s2) should not exceed 0.35%.
      [content determination]     Determine according to high-performance liquid chromatography (general rule 0512).
      Chromatographic conditions and system suitability test octadecylsilane bonded silica gel was used as filler; The mobile phase was acetonitrile-0.4% phosphoric acid solution (10:90); The detection wavelength is 327nm. The number of theoretical plates should not be less than 3000 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 50 μ g per 1ml, and then get it (stored under 10 ℃).
      .
      The determination method is to precisely suck 5 μ l each of the reference solution and 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 0.25%.
      Decoction pieces
      [processing]   Xanthium sibiricum seeds remove impurities.
      [character], [identification], [inspection], [content determination] are the same as those of medicinal materials.
      Stir fry Xanthium sibiricum, take out the Xanthium sibiricum, stir fry until it is yellowish brown according to the clear stir fry method (general rule 0213), remove the thorn, and screen it.
      This product is shaped like cocklebur, with yellowish brown surface and prickle marks. Slightly fragrant.
      [check]   Moisture   No more than 10.0% for the same medicinal materials.
      .
      ; ; The mobile phase was acetonitrile-0.01mol/l sodium dihydrogen phosphate solution (pH adjusted to 5.4 with 4% sodium hydroxide solution) (20:80); .
      Preparation of reference solution   Take an appropriate amount of Atractyloside dipotassium salt reference substance, accurately weigh it, add 20% methanol to make a solution containing 0.1mg per 1ml, and get it (Atractyloside weight - Atractyloside dipotassium salt weight /1.1048).
      Preparation of test solution   Take about 1g of this product powder (passing through No. 3 screen), weigh it precisely, place it in a conical flask with a stopper, add 20ml of water precisely, weigh it, sonicate (power 300W, frequency 40KHz) for 40 minutes, cool it, weigh it again, make up the lost weight with water, shake it well, centrifuge (rotating speed 12000 rpm, 5 minutes), take the supernatant, filter it, take the filtrate, and get it.
      Assay   Precisely suck 5 μ l of the reference solution and 5 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 Atractyloside (c30h46o16s2) should be 0.10% - 0.30%.
      ; Same as medicinal materials.
      [nature, taste and meridian tropism]   Bitter, bitter, warm; . Return to lung meridian.
      ; . For wind cold headache, nasal congestion and runny nose, epistaxis, nasal pits, rubella itching, dampness arthralgia contracture.
      [usage and setting]   3～10g。
      [storage]   Place in a dry place.


2、 Chemical constituents of Fructus Xanthii
1. Xanthium sibiricum fruit produces 9.2% fatty oil, including fatty acids:palmitic acid（palmitic acid）5.32%， Stearic acid 3.68%, oleic acid 26.8%, linoleic acid 64.20%. Unsaponifiable matter contains ceryl alcohol,β-Sitosterol，γ-SitosterolAnd ξ - sitosterol. . It also contains stromaroside, namely β - sitos terol - β - D-glucoside; Glucose, fructose, sucrose; Tartaric acid,Succinic acid（succinic acid），Fumarate（fumaric acid）， Malic acid,l-leucine （L-leucine），L-phenylalanine（L-phenylalnine），glycine（glycine），L-aspartic acid （L-aspartic acid），L-asparagine（L-asparagine）。 It also contains protein, including amino acids:glycine，l-serine （serine），L-aspartic acid , glutamic acid,L-alanine（L-alanine），L-valine （valine），l-leucine ，L-lysine（lysibne），L-asparagine，l-tyrosine （tyro-sine），L-threonine（threonine），L-Proline （proline）， Arginine,L-phenylalanineRecently, I got from the fruit1,3,5-tricaffeoylquinic acid（1,3,5-Tricaffeoylquinic acid），Isochlorogenic acid A（3,5-Dicaffeoylquinic acid）。
The seed kernel contains 40% fatty oil, including fatty acids:palmitic acid.
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2. the kernel of Xanthium mongolicum contains Atractyloside.

3、 Pharmacological effects of Fructus Xanthii
1. hypoglycemic: 1mg/kg of white crystalline glycoside (c31h-48o24s2) can reduce blood glucose in normal rabbits.
2. effect on respiratory system: Xanthium sibiricum 100% Decoction 0.3ml/ mouse by gavage has antitussive effect on mice; 15ml/kg had no expectorant effect on rabbits. Tincture injection has respiratory excitatory effect on frogs, while large dose has inhibitory effect.
3. cardiovascular effects: Xanthium sibiricum injection has a short-term antihypertensive effect on rabbits and dogs................................the injection of Xanthium sibiricum l.s.l.is injected intraveno.
4. anti inflammatory effect: the diterpenoid hydroxy acid Atractyloside contained in this product has anti-inflammatory effect according to the carrageenan edema test in rats. The LD50 of intraperitoneal injection, subcutaneous injection and oral administration were 2.9, 5.3 and 350mg / kg, respectively.
4. Xanthium sibiricum decoction has some antibacterial effect on Staphylococcus aureus in vitro, and its acetone or ethanol extract also has antibacterial effect on Trichophyton rubrum in vitro.
5. toxicity: according to the analysis, Xanthium sibiricum oil (heated to 120 ℃) and its protein (insoluble in water and denatured in the extraction process) have no obvious toxicity, while the water extract prepared from the defatted part is very toxic. A glycoside was isolated from the water extract, which may be the main toxic component of Xanthium sibiricum. The residue after water immersion is less toxic or non-toxic. After high heat treatment, its toxicity can be destroyed if it is charred. The median lethal dose of one intraperitoneal injection in mice is 0.93g / kg. Rats, mice, guinea pigs and rabbits have basically the same poisoning manifestations to different routes of administration, such as reduced activity, sluggish response to external stimuli, irregular breathing, extreme difficulty in breathing before death, accompanied by paroxysmal seizures. Histopathological examination revealed that the main organs damaged after poisoning in various animals were basically the same except for the difference in degree. ; The renal convoluted duct epithelium is turbid and swollen, and there are protein tubules in the lumen; The lungs and brain are congested and edematous, and the heart is slightly cloudy and swollen. Among them, liver damage is the most serious, which is similar to carbon tetrachloride damage. Therefore, it is believed that the main cause of seed seed extract poisoning is liver necrosis, and the secondary convulsion caused by brain tissue edema may be the direct cause of death. Promethazine has preventive and therapeutic effects on poisoned rabbits and guinea pigs. Phospholipids, DL Methionine, cystine, vitamin C, vitamin K3, vitamin B12, diphenhydramine, aminophylline or glucose also have certain effects. . Atropine, Coramine, chlorpromazine, barbital and norepinephrine were ineffective. It is also believed that the strong paroxysmal convulsion after animal poisoning is related to the significant reduction of blood glucose caused by the glycosides contained in Xanthium sibiricum. Injection of a large amount of glucose can alleviate the convulsion and prolong life. The tincture made of Xanthium sibiricum can enhance the respiratory movement of frogs, which can inhibit respiration in a large amount.