Folium Isatidis l.var.dahliae l.var.dahliae l.var.dahliae l.var.dahliae l.var.dahliae l.var.dahliae l.var.dahliae
1、       This product is the dried leaves of Isatis indigotica fort., a cruciferous plant. Harvest twice or thrice in summer and autumn, remove impurities and dry in the sun.
      [character] this product is often wrinkled and curled, and some are broken. After flattening, the intact leaves are oblong to oblong oblanceolate, 5-20cm long and 2-6cm wide; the upper surface is dark gray green, and some dark and slightly protruding dots can be seen; ; The petiole is 4 ～ 10cm long and light brown yellow. Brittle. It is slightly sour, bitter and astringent.
      [identification] (1) the powder of this product is green brown. The vertical wall of the lower epidermal cells was slightly curved and slightly Beaded thickened; . Mesophyll tissue differentiation was not obvious; The mesophyll cells contained blue fine granules and hesperidin like crystals.
      (2) Take 0.5g of this product powder, add 20ml of trichloromethane, heat and reflux for 1 hour, filter, and concentrate the filtrate to 1ml as the test solution. In addition, take indigo control and indirubin control and add chloroform to make a mixed solution containing 1mg per 1ml as the control solution. According to the test of thin-layer chromatography (general rule 0502), suck 5 μ l of each of the above two solutions, dot them on the same silica gel G thin-layer plate, develop them with cyclohexane trichloromethane acetone (5:4:2), take them out, and dry them. In the chromatogram of the test sample, the same blue spots and light purplish red spots appear at the corresponding positions of the chromatogram of the control sample.
      [inspection] the moisture content shall not exceed 13.0% (the second method of general rule 0832).
      [extract] according to the hot leaching method under the determination method of alcohol soluble extract (general rule 2201), the use of ethanol as solvent shall not be less than 16.0%.
      [content determination] determine according to HPLC (general rule 0512).
      Chromatographic conditions and system suitability test octadecylsilane bonded silica gel was used as filler; Methanol water (75:25) was used as mobile phase; The detection wavelength was 289nm. The number of theoretical plates should not be less than 4000 according to the indirubin peak.
      Preparation of reference solution take an appropriate amount of indirubin reference, weigh accurately, add methanol to make a solution containing 2 μ g per 1ml.
      Preparation of test solution take 0.25g of the fine powder of this product, weigh it accurately, put it in Soxhlet extractor, add chloroform, soak it for 15 hours, heat it to reflux and extract until the extract is colorless. Recover the solvent to dryness, add methanol to dissolve the residue and transfer it to a 100ml volumetric flask, add methanol to the scale, shake well, filter, and take the continuous filtrate.
      The determination method is to precisely suck 20 μ l of the reference solution and 20 μ l of the test solution, inject them into the liquid chromatograph, and determine.
      According to the calculation of dry product, the content of indirubin (c16hl0n2o2) shall not be less than 0.020%
      Decoction pieces
      [processing] remove impurities, wash with water, chop and dry.
      This product is irregular broken segment. ; Petiole fragments are light brownish yellow. Brittle. It is slightly sour, bitter and astringent.
      [inspection] the moisture content is the same as that of medicinal materials, and shall not exceed 10.0%.
      [identification], [extract], [content determination] are the same as those of medicinal materials.
      [nature, taste and meridian tropism] bitter, cold. Homing and stomach meridian.
      [functions and indications] it can clear away heat, detoxify, cool blood and eliminate spots. It is used for febrile diseases, high fever, dizziness, spots and rashes, gills, throat obstruction, erysipelas, carbuncle and swelling.
      [usage and setting] 9 ～ 15g.
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2、 Chemical constituents of Folium Isatidis
cycasin indigo（indigo，indigotin）， Isatin B,Indirubin（indirubin）。 . The hydrolysis of isatin can be changed intoindigoAnd d-xylo-5-hexulofuranosonic acid.

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; Dysentery bacilli, which are sensitive or resistant to doxorubicin, nitrofurazone, sulfathiazole and berberine, are very sensitive to roadside green leaves. It can also kill meningococcus. It can also kill Leptospira Pomona group, jaundice hemorrhage group Walden type and seven day fever type. The tryptamine contained in this product has a strong antibacterial effect on dermatophytes causing tinea pedis. Its Mic (ug/ml) was 3.1 for Trichophyton mentagrophyte, 3.1 for Trichophyton rubrum, 3.1 for Trichophyton catarrhalis, 3.1 for Microsporum parvum, 6.3 for Microsporum gypseum, 3.1 for dermatophyte lactis, 25 for Bacillus subtilis, and 50 for Bacillus polymyxa. It is particularly effective against bacilli and dermatophytes.
2. anticancer effect: 2.1 effect on the treatment of chronic myeloid leukemia indirubin has a higher inhibition rate on l7212 leukemia mice. According to animal experiments, indirubin is compared with other anticancer drugs.
2.1.1 effect of indirubin on cellular immune function of normal guinea pigs: normal guinea pigs (weighing 300-400g) were given daily Ig of indirubin suspension (Tween as surfactant), 100-200mg/kg, for 43-60 days. Tween and cyclophosphamide were used as controls to observe the number of lymphocytes in peripheral blood, OT skin delayed type hypersensitivity test, PHA lymphocyte transformation test and macrophage phagocytosis function test. The results showed that except that the phagocytosis function of macrophages was similar in the three groups, there was no significant difference between other indirubin groups and tween group, while the cyclophosphamide group was significantly lower than the former two groups. Pathological observation showed that there was no significant change in indirubin group and tween group, while the proliferation of cyclophosphamide group was significantly reduced, presenting with acute bone marrow failure.
2.1.2 observation of antibody production test in terms of humoral immunity each guinea pig im25% sheep red blood cells, 1ml every other day, heart blood was taken 7 days after the fourth injection, and the agglutination and hemolysis titers of anti sheep red blood cell antibodies were determined. Results: the agglutination reaction and hemolysis reaction between guinea pig serum and sheep erythrocytes were negative before immunization. After immunization, the above titers of indirubin and tween group were significantly higher than those of cyclophosphamide group, and indirubin group was slightly higher than that of Tween group.
2.1.3 effects on the kinetics of normal hematopoietic cell generation taking normal mice, rats, and guinea pigs as experimental objects, the effects of long-term and large-scale application of indirubin on hematopoietic colony forming cells, bone marrow cell proliferation ability, bone marrow volume, and peripheral hemogram were studied, and compared with malilan and cytarabine. Results: high dose indirubin (equivalent to 50 times the clinical adult dose) did not significantly inhibit the effect of hematopoietic colony forming cells (CFUs) in mice, regardless of the endogenous method or exogenous method, while the CFUs and spleen weight in the malilan group were significantly reduced. 3H deoxythymidine (3H TDR) incorporation into bone marrow cells: results after administration of large dose of indirubin for 14 days, the volume of nucleated cells in femur, 10? The CPM of bone marrow cells and femur cells were close to that of the control, while the bone marrow nucleated cell count and femur CPM were significantly decreased in the Maryland and cytarabine groups, as shown in Table 5. After long-term administration of indirubin to rats and guinea pigs, there was no difference in the histological volume of bone marrow and 3H TDR incorporation of bone marrow nucleated cells between the two groups.
2.1.4 effects on peripheral hemogram of mice, rats and guinea pigs after administration of high-dose indirubin for 14 and 30 days, the white blood cells, hematocrit and reticulocytes were not significantly changed compared with the control group, while the three indicators were significantly inhibited in the 30 day malilan administration group.
According to the clinical observation, indirubin can significantly improve the cellular rabbit epidemic function of patients with chronic myeloid leukemia, and the chromosome Ph1 positive rate, aberration rate, SCE rate and other counting results are significantly different from those before treatment. From the clinical curative effect observation, the effect is also good. Its characteristic is that indirubin has no inhibitory effect on humoral immune function and has no obvious effect on normal hematopoietic dynamics of experimental animals. Under the ultrastructure, bone marrow cells showed karyolysis, which was different from the phenomenon of withering of drugs such as harringtonine.
2.2 antitumor effect of synthetic indirubin the synthetic indirubin is a purplish red powdery crystal, mp348-353 ℃, and the purity is more than 97%. According to the conventional tumor inoculation method and curative effect evaluation standard, the curative effect of synthetic indirubin on several animal transplanted tumors was observed. Generally, 24h after inoculation, the medicinal plant oil and Arabic gum were mixed into an emulsion, and the dose of 50 or 200mg/kg per day was continuously given to animals Ig or ip8-10d. The results showed that there was no obvious therapeutic effect on mouse leukemia l7212 and P388. .
Due to the poor water solubility and fat solubility of indirubin, which affect the absorption, different dosage forms and doses were used to observe the curative effect on animal tumors.
2.3 antitumor effect of semi synthetic indirubin according to the domestic commonly used in vivo screening method, the efficacy of semi synthetic indirubin on Walker carcinosarcoma 256 in rats, sarcoma 180 in mice and lymphoid leukemia l7212 in 615 mice was observed.
2.4 antitumor activity of indirubin derivatives due to the single dosage form of indirubin, it cannot be administered in multiple ways, and some patients have gastrointestinal reactions, even hematochezia, etc. after medication. Therefore, the synthesis of indirubin derivatives was studied. Through the observation of the efficacy and toxicity of 15 derivatives on animal tumors, it was considered that the antitumor activity of four derivatives, N, n '- dimethyl indirubin, N-methyl indirubin oxime, N-methyl indirubin oxime methyl ether, and N-acetyl indirubin, on rat W256 was similar to that of indirubin, and the toxicity was not significant. Among them, N, n'- dimethyl indirubin and N-methyl indirubin oxime have stronger antitumor activity than indirubin. They are not only effective for W256 in rats, but also effective for l7212, which is not sensitive to indirubin.
. The inhibition rates of 256, IP and 200mg/kg for 6-7 days were 23-33% respectively. Sc200mg/kg twice can prolong the survival time of Walker 256 ascites type rats by 43%. It also has obvious inhibitory effect on Lewis lung cancer in mice. It is clinically used in the treatment of chronic myelogenous leukemia, and its curative effect is equivalent to that of malilan, and it has no obvious myelosuppressive effect.
3. antipyretic effect: 5-10g/kgig of Polygonum leaf decoction can significantly reduce the temperature of rabbits with fever caused by cholera and typhoid vaccine. Daqingye Decoction (100%) was added to the culture solution containing Staphylococcus aureus at a ratio of 1:10, and it had bactericidal effect after 30 minutes. Chloroform extract has anti endotoxin effect.
Polygonum leaf Decoction 5g/kgig can reduce or accelerate the regression of formaldehyde induced foot swelling in rats. Polygonum leaf Decoction (10g/kgig) can inhibit the local skin inflammatory reaction caused by xylene and reduce capillary permeability in rabbits.
4. choleretic effect: Folium Isatidis can significantly increase bile secretion in dogs; 5. anti inflammatory effect: Folium Isatidis (Isatis indigotica) decoction has obvious anti-inflammatory effect on formaldehyde induced arthritis bone by gavage in rats.
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7. effect on heart and vascular system: Polygonum leaf Decoction (equivalent to 0.125g of crude drug) has inhibitory effect on isolated toad heart, and the effect increases with the increase of dose, and even can make the heart arrest. It can dilate the blood vessels of the lower limbs of rats, especially when the blood vessels are in a contractile state.
8. effect on smooth muscle: the infusion and injection have an inhibitory effect on isolated rabbit intestinal muscle. The intestinal peristalsis is weakened, the amplitude is reduced, and the duration is long. It is not easy to recover by itself. Its inhibitory effect increases with the increase of concentration. . A small dose (0.1g) produced strong rhythmic contraction, and when the dose was increased to 0.25g, it showed tonic contraction, which lasted for a long time.
9. effect on platelet aggregation: pt-1 and PT-2 contained in this product can inhibit platelet aggregation caused by ADP (adenosinediphosphate).