Coptis chinensis
1、 Pharmacopoeia standard of Coptis chinensis       This product is the dried rhizome of Coptis chinensis franch., Coptis deltoidea c.y.cheng et Hsiao or Coptis teeta wall. The above three are commonly known as "Wei Lian", "Ya Lian" and "Yun Lian". .
      [character] Weilian   . Brown scaly leaves are mostly left on the upper part, and residual stems or petioles are often left on the top. It is hard, with irregular section, orange red or dark brown skin, bright yellow or orange yellow wood, arranged radially, and hollow pulp. The breath is slight and the taste is extremely bitter.
      Yalian   . The "bridge crossing" is long. There are a few residual stems at the top.
      Yunlian   The bending is hook like, mostly single branches, and relatively small.
      . The cortex is wide, and stone cells are scattered individually or in groups. The fibers in the middle column sheath are in bundles or accompanied by a few stone cells, all of which are yellow. Vascular bundle outer tough, circular. The xylem is yellow, all lignified, and the wood fiber is relatively developed. The medulla was all parenchymal cells without stone cells.
      Yalian   There are stone cells in the pulp.
      Yunlian   There were no stone cells in cortex, columella and medulla.
      (2) . Another 0.25g of Coptis reference medicinal material was taken and prepared into the reference medicinal material solution by the same method. Then take berberine hydrochloride reference substance and add methanol to make a solution containing 0.5mg per 1ml as the reference substance solution. According to the test of thin-layer chromatography (general rule 0502), suck 1 μ l of each of the above three solutions, dot them on the same high-performance silica gel G thin-layer plate, use cyclohexane ethyl acetate isopropanol methanol water triethylamine (3:3.5:1:1.5:0.5:1) as the developing agent, put them in the developing cylinder pre saturated with concentrated ammonia test solution for 20 minutes, develop, take out, dry them, and view them under UV light (365nm). In the chromatogram of the test sample, there are more than 4 fluorescent spots of the same color at the position corresponding to the chromatogram of the control medicinal material; Fluorescent spots of the same color are displayed on the corresponding position of the control chromatography.
      [check] moisture   Not more than 14.0% (the second method of general rule 0832).
      Total ash   .
      [extract] according to the hot leaching method under the alcohol soluble extract determination method (general rule 2201), using dilute ethanol as solvent, it shall not be less than 15.0%.
      [content determination] Weilian   Determine according to high-performance liquid chromatography (general rule 0512).
      ; Octadecylsilane bonded silica gel was used as filler; The mobile phase was acetonitrile-0.05mol/l potassium dihydrogen phosphate solution (50:50) (add 0.4g sodium dodecyl sulfate per 100ml, and adjust the pH value to 4.0 with phosphoric acid); The detection wavelength was 345nm. The number of theoretical plates should not be less than 5000 according to the peak of berberine hydrochloride.
      Preparation of reference solution   Take an appropriate amount of berberine hydrochloride reference substance, accurately weigh it, add methanol to make a solution containing 90.5 μ g per 1ml.
      Preparation of test solution   Take about 0.2g of this product powder (through No. 2 screen), weigh it accurately, place it in a corked conical flask, add 50ml of methanol hydrochloric acid (100:1) mixed solution precisely, close the stopper, weigh it, sonicate it (power 250W, frequency 40KHz) for 30 minutes, cool it, weigh it again, use methanol to make up the lost weight, shake it well, filter it, accurately measure 2ml of the continued filtrate, place it in a 10ml measuring flask, add methanol to the scale, shake it well, filter it, and take the continued filtrate.
      Assay   Accurately 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 them. Taking the peak area of berberine hydrochloride reference as the control, calculate the content of berberine, epiberberine, berberine and bamatine respectively, and determine the relative retention time of the chromatographic peak of the component to be tested and the chromatographic peak of berberine hydrochloride.
      The relative retention time of berberine, berberine, palmatine and berberine should be within ± 5% of the specified value. The relative retention time is shown in the table below:
   
        According to the calculation of dry product, the content of berberine hydrochloride (c20h18clno4) shall not be less than 5.5%, epiberberine (c20h17no4) shall not be less than 0.80%, berberine (c19h13no4) shall not be less than 1.6%, palmatine (c21h21no4) shall not be less than 1.5%.
      Yalian shall be calculated as a dry product, and the content of berberine (c20h17no4) shall not be less than 4.5% based on berberine hydrochloride (c20h18clno4).
      The content of berberine (c20h17no4) in Yunlian shall not be less than 7.0% based on berberine hydrochloride (c20h18clno4) calculated according to the dried product.
      Decoction pieces (Weilian)
      [processing] Coptis chinensis tablets   Remove impurities, cut into thin pieces after being moistened, air dry, or mash when used.
      The product is in irregular flakes. The outer skin is grayish yellow or yellowish brown, rough, and has fine fibrous roots. The cut surface or broken section is bright yellow or red yellow, with radial texture, slight air, and extremely bitter taste.
      [check] moisture   No more than 12.0% for the same medicinal materials.
      Total ash   No more than 3.5% of the same medicinal materials.
      [content determination] according to berberine hydrochloride, the content of berberine (c20h17no4) shall not be less than 5.0%, and the total content of epiberberine (c20h17no4), berberine (c19h13no4) and palmatine (c21h21no4) shall not be less than 3.3%.
      [identification] (except for the transverse section) [extract] is the same as that of medicinal materials.
      ; Take the Rhizoma Coptidis and fry it according to the wine roasting method (general rule 0213).
      For every 100kg of Rhizoma Coptidis, 12.5kg of rice wine was used.
      This product is shaped like Coptis chinensis tablets, and its color is deepened. .
      [identification], [inspection], [extract], [content determination] tonghuanglian tablets.
      Rhizoma Coptidis   Take Rhizoma Coptidis and stir fry it according to the ginger juice roasting method (general rule 0213).
      Ginger 12.5kg per 100kg of Rhizoma Coptidis.
      . It has a pungent taste of ginger.
      [identification], [inspection], [extract], [content determination] tonghuanglian tablets.
      Coptis chinensis   Take Evodia rutaecarpa and add proper amount of water to decoct, mix the decoction with Rhizoma Coptidis, soak up the solution, and fry it dry.
      For every 100kg of Coptis chinensis, use 10kg of Evodia rutaecarpa.
      . .
      [identification] take 2G of this product powder, add 20ml of trichloromethane, sonicate for 30 minutes, filter, treat the filter residue twice in the same way, combine the filtrate, recover the solvent to dryness under reduced pressure, add 1ml of trichloromethane to dissolve, and use it as the test solution. Another 0.5g of Evodia rutaecarpa reference medicinal material was prepared into the reference medicinal material solution by the same method. Then take the limonin reference substance and add chloroform to make a solution containing 1mg per 1ml as the reference substance solution. . In the chromatogram of the test sample, the main spots with the same color appear at the corresponding position of the chromatogram of the control medicinal material; On the position corresponding to the chromatogram of the reference substance, the spots with the same color appear.
      [inspection], [extract], [content determination] tonghuanglian tablets.
      [nature, taste and meridian tropism] bitter, cold. .
      [functions and indications] clearing heat and dampness, purging fire and detoxifying. For damp heat fullness, vomiting and acid swallowing, diarrhea, jaundice, high fever and dizziness, hyperactivity of heart fire, restlessness, palpitation, blood heat vomiting, red eyes, toothache, diabetes, carbuncle, swelling and sores; External treatment of eczema, wet sores, ear canal suppuration. . For red eyes and mouth sores. Rhizoma Curcumae can clear stomach and stop vomiting. It is used for the combination of cold and heat, damp and heat resistance, fullness and vomiting. Yuhuanglian soothes the liver and stomach to stop vomiting. For disharmony between liver and stomach, vomiting and acid swallowing.
      [usage and dosage] 2 ～ 5g. Suitable for external use.
      .


2、 Chemical constituents of Coptis chinensis
1. rhizome of Coptis chinensis containsberberine（berberine）5. 56％-7.25％，Berberine（coptisine），Epiberberine（epiberberine），Berberine（berberrubine），Palmatine（palmatine），Tetrandrine（columbamine），Jatrorrhizine（jatrorrhizine），Methyl Berberine（worenine），Magnoliane（magnoflorine），Ferulic acid（ferulic acid），Berberine（obakunone）， Obakulactone.
2. rhizome of Coptis deltoides containsEpiberberine，berberine，Berberine，Palmatine，Methyl Berberine，Jatrorrhizine，Magnoliane。
3. rhizome of Coptis yunnanensis containsberberine，Palmatine，Jatrorrhizine，Methyl Berberine，Magnoliane，Berberine。

3、 Pharmacological action of Coptis chinensis
. The test tube dilution test of Coptis Decoction showed that 1:160 against sonnei, 1:1280 against Freund, 1:2560 against Shigella, 1:5120 against Shigella dysenteriae, 1:160 against typhoid bacillus, 1:128 against Yersinia pestis, 1:160 and 1:1280 against a- and B-hemolytic Streptococcus, 1:640 against diphtheria bacillus, pneumococcus, Vibrio cholerae, and 1:2560 against human Mycobacterium tuberculosis (H37). Rhizoma Coptidis decoction has inhibitory effects on Bacillus anthracis at 1:640, Staphylococcus aureus and erysipelas at 1:320, and Pseudomonas aeruginosa at 1:20. Coptis Decoction 100%, tincture 20%, using plate filter paper method or penetration test on Shigella, Shigella, flexneri dysentery bacilli and Staphylococcus aureus, Streptococcus have significant inhibitory effect. Rhizoma Coptidis Decoction with 100% concentration and plate drilling test showed that it had antibacterial effect on Shigella, Freund, sonnei and Shigella. Huanglian decoction has bacteriostatic effect on pertussis bacilli at the concentration of 1:1-1:128. Berberine at a concentration of 1:4000 has inhibitory effect on Mycobacterium tuberculosis. 1.5, 2.5g/kg by gavage for 21, 28 days can delay the development of experimental tuberculosis in mice. ; 1: 16000 has inhibitory effect on Staphylococcus aureus and Staphylococcus albus; 1: 8000 has inhibitory effect on Staphylococcus citri, Streptococcus viridans, Diphtheria Bacillus, Bacillus subtilis, Shigella dysenteriae, Shigella flexneri; 1: 4000 has inhibitory effect on pneumoniae and Proteus; 1: ; It was found that seven amino acids (aspartic acid and its amide, histidine, glycine, methionine, threonine, tryptophan), three vitamins (nicotinic acid and nicotinamide, p-aminobenzoic acid, vitamin B6), adenylic acid and uracil could resist the antibacterial effect of berberine, so the antibacterial effect of berberine may be realized by affecting the metabolic process of bacteria. Rhizoma Coptidis Decoction and alcohol extract 1g/ml, the plate drilling test showed that it had inhibitory effect on meningococcus, the test tube dilution method Decoction 1:1280, alcohol extract 1:320 had inhibitory effect on meningococcus. Berberine promoted the incorporation of 3H thymidine and 3H uridine into Staphylococcus aureus and Escherichia coli at low concentration (10 μ g/ml) and inhibited it at high concentration (100, 500 mg / ml).
. Rhizoma Coptidis aqueous extract at a concentration of 1:3 has antibacterial effect on Trichophyton violaceum, Trichophyton concentric, Trichophyton gypsioides, Xanthomonas schrenckii, Micrococcus audouane, Micrococcus ferrugosus, Micrococcus laniformis, dermatophyton inguinal, dermatophyton rubrum, Kaufman Wolff epidermis, Candida albicans, blastophytes compactly pigmented, and Nocardia stauroides.
3. antiviral effect: the 50% concentration of Coptis decoction is 0.1ml/ egg. The chicken embryo test shows that it has inhibitory effect on influenza virus PR8 strain, influenza A virus 56-s8 strain, subtype A virus FML strain, influenza B virus Lee strain, and endotype influenza virus 1233 strain. Huanglian decoction has inhibitory effect on hepatitis B virus DNA at 25-100% concentration. Berberine 0.5mg/ egg can effectively reduce the mortality of trachoma virus infected chicken embryos and inhibit the production of virus protosomes.
4. anti amebic effect: Coptis Decoction at 1:20-1:80 concentration and berberine at 1:5000-1:10000 concentration have anti amebic effect in vitro; Coptis Decoction 1.3g/kg and berberine 50mg/kg were intragastrically administered to kill amoeba histolytica inoculated in the cecum of rats.
5. anti inflammatory and anti diarrhea effects: the methanol extract of Rhizoma Coptidis 400 μ g/ chicken fertilized egg test showed that it had the effect of inhibiting the proliferation of granulation tissue. Berberine hydrochloride 50mg/kg gavage also had anti-inflammatory effects on croton oil capsule method and cotton ball method in rats. Berberine at a concentration of 1 × 10 (-4) inhibited leukotriene B4 production by human polymorphonuclear leukocytes in vitro, with an inhibition rate of 43.7 ± 5.6%. Berberine 40.80mg/kg by gavage could antagonize diarrhea in mice caused by castor oil or senna leaf; After 30.60mg/kg gavage, the increase of abdominal exudation induced by acetic acid in mice was inhibited; Subcutaneous injection of 20.50mg/kg inhibited the increase of skin capillary permeability induced by histamine in rats; . Berberine 0.06-20mg/kg gavage can delay, reduce and alleviate the diarrhea of dogs caused by Ipomoea turpeth μ m root, but it has no effect on the diarrhea of rats caused by MgSO4 gavage. 10mg/kg gavage or intraperitoneal injection can reduce the intestinal motility of normal mice. Because it has no precipitation effect on serum protein or egg albumin, its anti diarrhea is not due to convergence effect. . Berberine 10mg/kg by gavage can delay, reduce and reduce diarrhea caused by cholera toxin in rats, and also reduce intestinal water and dielectric levels in rats. For rats injected with cholera toxin into the small intestine, berberine 1mm injected into the intestine can promote na+cl- absorption. Berberine 5mg injected into the intestine of guinea pigs at a concentration of 2.7 × 10 (-3) m can reduce the secretion of water and dielectric caused by Escherichia coli toxin, and its anti secretory effect is similar to that of A-receptor agonists, opiates and antihistamines.
6. cardiovascular effects: Berberine 3-5mg/kg intravenously can reduce the blood pressure of anesthetized dogs. If the animals are treated with ergot poison in advance, the antihypertensive effect of berberine can be reversed. Berberine sulfate 0.1-6.0mg/kg intravenously can reduce the blood pressure of anesthetized dogs, cats and rats. Berberine 2-10 μ g/ml could inhibit the contraction of rabbit pulmonary artery strips induced by norepinephrine. . Berberine and coptisine have inhibitory effects on acetylcholinesterase in rat brain in vitro, with IC50 of 9.8 × 10 (-7) for berberine and 5.8 × 10 (-6) for berberine. Berberine can block the contraction effect of phenylephrine on isolated rabbit aortic strips with an IC50 of 30 μ m, but it has no effect on the contraction of superior arterial strips caused by histamine, serotonin and KCl, nor does it affect the basic tension of vascular strips, indicating that berberine has a selective blocking effect on A-receptor. Berberine (0.3, 1.3 μ mol/l) caused a parallel right shift in the first effect curve of the cumulative amount of phenylephrine in rat anococcygeal muscle and rabbit aorta specimens, without depressing the maximum response, indicating that berberine has a competitive blocking effect on A-receptor.
Berberine (10 μ mol / L) and yuxiangbin (1mol / L) significantly attenuated the inhibitory effect of clonidine on the excitation induced by electrical stimulation of the prostate end of the vas deferens in rats, shifted the cumulative dose-response curve of clonidine to the right, and the maximum response remained unchanged, with pA2 values of 5.3 and 7.8, respectively; Berberine 1 μ mol/l and pazosin 10 μ mol/l in rat anococcygeal muscle specimens can make the phenylephrine dose-response curve parallel to the right, and the maximum effect remains unchanged, with pA2 values of 6.4 and 8.5, respectively, indicating that berberine has a blocking effect on A1 and A2 receptors, and the selective ratio of blocking effect (a1/a2) is 8. Berberine 5.5 μ mol / L shifted the dose-response curve of acetylcholine on rat anococcygeal muscle contraction to the right, and the maximum response was reduced by 83.5 and 38.4%. Berberine 5 μ mol / l could antagonize the contraction of rat anococcygeal muscle caused by serotonin 10 μ mol / L, also antagonize the contraction of rat anococcygeal muscle caused by histamine 1mmol / L, and also inhibit the contraction of rat anococcygeal muscle caused by isoproterenol, indicating that berberine has a blocking effect on a variety of receptors in rat anococcygeal muscle.
Berberine intraperitoneal injection had a protective effect on ventricular fibrillation induced by CHCl3 in mice, and its half effective dose was 14.91 ± 0.0104mg/kg; Berberine 15mg/kg intravenously also had a protective effect on aconitine induced ventricular fibrillation in rats, but had no effect on ouabain induced ventricular arrhythmia. Berberine 1mg/kg intravenously can cause the decrease of blood pressure, left ventricular pressure and left ventricular end diastolic pressure in awake rats. The degree of decline is diastolic blood pressure > systolic blood pressure > left ventricular pressure. The heart rate reflex accelerates, and then slowly and persistently decreases. While the afterload and heart rate decrease, it is not accompanied by the decrease of the maximum rate of left ventricular pressure change (± dp/dt) max, the decrease of the left ventricular pressure rise velocity pressure change ratio (dp/dt) P-1, or the reduction of the left ventricular force velocity vector loop LVP ((dp/dt) p-1) and its slope, and even slightly increases, indicating the enhancing effect of berberine on myocardial contractility, so the blood pressure is reduced.The main effect was to reduce heart rate and peripheral vascular resistance? Mg/kg intravenously can increase the threshold of electric induced ventricular fibrillation in anesthetized cats. 6-120 μ mol/l can prolong APD and ERP in isolated papillary muscles of guinea pigs. Positive inotropic effect appears when asked, which may be related to promoting Ca2 + transmembrane influx.
Berberine at a concentration of 10 (-4) mol/l could significantly enhance the contractility of isolated left atrium of guinea pigs, prolong the functional refractory period (FRP), reduce the concentration of epinephrine induced spontaneous threshold, and also enhance the contractility of right atrium, slow down the spontaneous beat frequency, antagonize the positive frequency of epinephrine without affecting its positive inotropic effect. Berberine was injected intravenously at a loading dose of 1mg/kg in dogs, and then input at a constant speed of 0.2mg/kg per minute, which could prolong the ERP and FRP of the ventricle and atrium, and increase the threshold of ventricular fibrillation induced by electrical stimulation. Berberine at a concentration of 0.1-30 μ mol/l can dose dependently reduce APA, Vmax, maximum depolarization potential (MDP) and spontaneous beat frequency of rabbit sinoatrial node and atrioventricular node cells, and prolong apd50, apd95 and ERP, while inhibiting sinus node function, that is, prolonging sinus cycle and sinus recovery time and correcting sinus recovery time. The inhibitory effect of berberine on sinus node is not antagonized by atropine. The A2 receptor antagonist bht-920 or A1 receptor agonist phenylephrine can not reverse the effect of berberine; Its effect of inhibiting the sinus cycle, APA and Vmax can be reversed by norepinephrine. In calcium free solution, the inhibitory effect of berberine on the sinus node still exists, but in the atrium, except for apd50 and apd95, other indicators disappear. Therefore, berberine may act on B receptor and Ca2 + influx, and its antiarrhythmic effect may be related to myocardial slow response cells.
; In the overall test, berberine 10mg/kg intravenous injection can shorten the A-H (atrium to his bundle conduction time) and H-V (His bundle to ventricular conduction time) intervals of rabbit heart, and prolong the atrial effective refractory period (AERP) and atrioventricular node functional refractory period (avnfrp), indicating that berberine accelerates the intra atrial and indoor conduction, but 15mg/kg intravenous injection can cause severe cardiac depression. Berberine 5-100 μ mol / L decreased the action potential Vmax and prolonged apd90 in isolated guinea pig right ventricular papillary muscles; After 4mg/kg intravenous injection, the blood pressure of rats decreased, the maximum rate of change of left ventricular pressure (dp/dtmax) and the peak value of left ventricular pressure (LVSP) decreased slightly, and the interval between the beginning of ventricular contraction and the maximum rate of pressure rise (t-dp / dt max) and the left ventricular end diastolic pressure (LVEDP) increased mildly, indicating that the left ventricular myocardial contractility was inhibited. After 5 minutes, the cardiac contractility gradually strengthened, LVSP, dp/dtmax and -dp/dtmax increased, and the left ventricular diastolic pressure (lvop), LVEDP and t-dp/dtmax decreased. Berberine (0.1-300 μ mol / L) had a positive inotropic effect on isolated right atrial and papillary muscles of guinea pigs, and could also prolong the refractory period (FRP) of myocardial function and inhibit the abnormal automaticity induced by epinephrine. Berberine 5mg/kg intravenously can prolong the QTc interval of electrocardiogram in dogs with chronic myocardial infarction, prolong the right ventricular effective refractory period (rERP), the left ventricular normal refractory period (NERP) and the left ventricular infarct refractory period (IERP), narrow the difference of IERP and the dispersion of the left ventricular effective refractory period, and inhibit the ventricular tachycardia and ventricular fibrillation induced by programmed stimuli.
. Berberine hydrochloride at a concentration of 1% was given intravenously to dogs at a constant rate of 10ml/kg every 1 hour. With the increase of the dose in vivo, the peak left ventricular pressure (LVSP) increased, the maximum rate of change of left ventricular pressure (dp/dtmax) accelerated, and the interval between the onset of left ventricular contraction and the occurrence of dp/dtmax (r-dp/ dtmax) shortened; After continuous infusion, the dose in the body continued to increase. At 60 minutes after infusion, LVSP decreased, DP / dtmax slowed down, and r-dp / dt Max prolonged. Finally, the heart contracted weakly, and the blood pressure fell to death, indicating that berberine at a small dose excited the heart, while at a large dose inhibited it. Berberine had a biphasic effect on the slow ionic current of guinea pig ventricular papillary muscle. Berberine 72365 μ mol / L significantly promoted the extracellular Ca2 + influx and increased the amplitude of the slow ionic current at the initial stage of treatment. With the extension of the action time, berberine blocked the calcium channel, so that the Ca2 + influx decreased, the amplitude of the slow ionic current gradually decreased, or even disappeared, and the myocardial contractility decreased. This may be the cause of myocardial depression and even death caused by intravenous infusion of berberine in clinical patients.
.
8. hypoglycemic effect: Rhizoma Coptidis Decoction 1.0-10.0g/kg by gavage can reduce the blood glucose level of normal mice; . Berberine 50mg/kg by gavage does not affect insulin secretion in mice, nor does it affect the number and affinity of hepatic thin membrane insulin receptors. The effect of berberine can be a post receptor effect. Berberine can resist the increase of blood glucose caused by glucose injection, inhibit gluconeogenesis with alanine as substrate, and the hypoglycemic effect of Berberine is closely related to the increase of blood lactate. Therefore, berberine may have hypoglycemic effect by inhibiting gluconeogenesis or promoting glycolysis.
9. hypolipidemic effect: 2ml of Rhizoma Coptidis aqueous extract was given by gavage for 7 weeks. For rabbits fed with cholesterol, the content of serum cholesterol could be reduced. Berberine 50mg/kg gavage for 7 consecutive days can reduce the serum cholesterol content of mice fed with high cholesterol emulsion.
10. antioxidant effect: 0.5ml of 5% Coptis chinensis Decoction and 5% 0.6ml of rat brain homogenate can reduce the production of malondialdehyde (MDA) in brain homogenate; The content of MDA in pancreas and liver of alloxan treated rats was decreased by intragastric administration of 10% Coptis chinensis Decoction (4-5ml / rat), twice a day.
11. effects on the blood system: berberine sulfate 1-3mg/ml in vitro test can reduce the anticoagulant effect of heparin (50u/ml) on human and canine blood, but berberine 10mg/ml alone has anticoagulant effect. Berberine 40-200 μ g/ml in vitro has inhibitory effect on ADP induced platelet aggregation in rabbits, with an IC50 of 120 μ g/ml and a dose-response relationship. Berberine can inhibit platelet aggregation and release of ATP in rabbits. The IC50 of inhibiting ADP induced platelet aggregation and release are 0.19 and 0.6mmol/l, 0.12 and 0.08mmol/l, 0.76 and 0.43mmol/l, respectively. The IC50 of inhibiting A23187 induced platelet aggregation and release are 2.36 and 0.85mmol/l, respectively. The mechanism of action may be related to the inhibition of arachidonic acid metabolism and the increase of intracellular ca2+ and / or camp.The. Berberine (0.5mol/l) significantly inhibited the proliferation of collagen ADP、 The release of thromboxane A2 (TXA2) from rabbit platelets induced by arachidonic acid showed a dose-dependent relationship. After intravenous injection of 25mg/kg in rabbits, the content of prostacyclin (PGI2) in plasma decreased 60min later. The experimental results proved that berberine could inhibit the release and metabolism of arachidonic acid from platelet membrane phospholipids.
12. other effects: Berberine at a concentration of 1 × 10 (-4) inhibited leukotriene B4 production by human polymorphonuclear leukocytes stimulated by calcium ionophore A23187 in vitro. Berberine hydrochloride 4.40 μ g/ml in vitro can inhibit the synthesis of DNA, RNA, protein and fat in mouse sarcoma 180 (S180 cells), and also inhibit the oxidation of glucose to CO2. However, when administered in vivo, 10mg/kg intraperitoneal injection has little inhibitory effect on tumor DNA and protein synthesis in mice, and 2.5-20mg/ kg intraperitoneal injection has no inhibitory effect on S180 in mice. This difference may be due to the problem of blood glucose concentration. Adding glucose concentration of 0.01-2.68mg/ml to the tumor cell culture medium can hinder the inhibitory effect of berberine on protein synthesis, indicating that glucose and berberine have an antagonistic effect on S180 cell uptake. Berberine 30, 60mg/kg subcutaneous injection can prolong the survival time of atmospheric pressure closed hypoxia mice, and can resist isoproterenol or phentolamine to shorten the hypoxia tolerance time. Berberine 30, 60mg/kg gavage or 4.8mg/kg subcutaneous injection can prolong the duration of mouth opening action of decapitated mice, and also prolong the survival time of kcn4mg/kg intravenous injection and NaNO2 800mg/kg intraperitoneal injection poisoning mice. 40, 80mg/kg gavage can prolong the survival time of lidocaine 150mg/kg intraperitoneal injection poisoning mice. Berberine hydrochloride 1.5mg/kg has cholagogic effect on dogs. It also has anti ulcer effect.