Shikonin
1、 Pharmacopoeia standard of Arnebia euchroma       . Excavate in spring and autumn to remove sediment and dry.
      [character] Arnebia euchroma (Arnebia euchroma)   . Divergent stem residues can be seen at the top. Light, soft, easy to break, irregular section, small wood, yellowish white or yellow. Qi is special, vague, slightly bitter and astringent.
      Arnebia euchroma   It is conical or cylindrical, twisted, 6-20cm long and 0.5-4cm in diameter. The root head is slightly thick, with 1 or more residual stems at the top, and is covered with short bristles. . It is hard and brittle, easy to break, with neat section, purplish red skin, small wood, yellowish white. The gas is special and the taste is astringent.
      [identification] (1) the powder is dark purple red. The non glandular hair is a single cell with a diameter of 13-56 μ m, the base is expanded into a trumpet shape, the wall has longitudinal thin stripes, and some cell cavities contain purplish red pigment. The thrombotic cells are reddish brown in color and appear polygonal or round polygonal on the surface, containing purplish red pigment. Parenchyma cells are numerous, light brown or colorless, mostly filled with purplish red pigment. The main conduit is reticulated conduit, and few have marginal pits, with a diameter of 7-110 μ M.
      (2) Take 0.5g of this product powder, add 20ml of petroleum ether (60 ～ 90 ℃), sonicate for 20 minutes, filter, and concentrate the filtrate to 1ml as the test solution. Another 0.5g of Arnebia euchroma 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 4 μ l of each of the two solutions, dot them on the same silica gel G thin-layer plate, use cyclohexane toluene ethyl acetate formic acid (5:5:0.5:0.1) as the developing agent, develop, take out, and air dry. ; Spray 10% potassium hydroxide methanol solution again, and the spots turn blue.
      [check] moisture   .
      [content determination] hydroxynaphthoquinone total pigment   Take an appropriate amount of this product, dry it at 50 ℃ for 3 hours, smash it (through No. 3 screen), take about 0.5g, weigh it accurately, put it into a 100ml volumetric flask, add ethanol to the scale, shake it constantly within 4 hours, and filter it. . According to the ultraviolet visible spectrophotometry (general rule 0401), the absorbance is measured at the wavelength of 516nm, and the absorption coefficient (e^1%1cm) of L-shikonin (c16h16o5) is 242.
      The total pigment containing hydroxynaphthoquinone in this product shall not be less than 0.80% based on L-shikonin (c16h16o5).
      β - β′ - dimethylacrylamine   .
      ; Octadecylsilane bonded silica gel was used as filler; The mobile phase was acetonitrile water formic acid (70:30:0.05); The detection wavelength was 275nm. The number of theoretical plates should not be less than 2000 according to the peak of β - β′ - dimethylacrylamine.
      Preparation of reference solution   Take an appropriate amount of β - β′ - dimethylacrylamine reference substance, weigh it accurately, add ethanol to make a solution containing 0.1mg per 1ml.
      Preparation of test solution   Take about 0.5g of this product powder (passing through No. 4 screen), weigh it accurately, place it in a corked conical flask, add 25ml of petroleum ether (60 ～ 90 ℃), weigh it, sonicate (power 250W, frequency 33khz) for 30 minutes, cool it, weigh it again, use petroleum ether (60 ～ 90 ℃) to make up the lost weight, shake it well, and filter it. .
      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 β - β′ - Dimethylacrylate acarnine (c21h22o6) shall not be less than 0.30%.
      Decoction pieces
      [processing] Arnebia euchroma   Remove impurities and cut thick pieces or segments.
      Arnebia euchroma   Remove impurities, wash, moisten thoroughly, slice and dry.
      Xinjiang shikonin slices   It is irregular cylindrical slice or strip-shaped slice, with a diameter of 1-2.5cm. It is purplish red or purplish brown. The skin is dark purple. .
      ; They are irregular cylindrical slices or strip-shaped sheets, and some can see short bristles with a diameter of 0.5 ~ 4cm, which are hard and brittle. Purplish red or purplish brown. The skin is dark purple. Cylindrical section, smaller wood, yellowish white or yellow.
      [identification], [inspection], [content determination] are the same as those of medicinal materials.
      . Heart returning and liver meridian.
      [functions and indications] it can clear away heat and cool blood, activate blood circulation and detoxify, penetrate rash and eliminate spots. It is used for blood heat and toxin, purple and black macules, impenetrable measles, sores, eczema, and scalds.
      [usage and dosage] 5 ～ 10g. Apply appropriate amount externally, boil cream or soak with vegetable oil.
      [storage] put it in a dry place.


2、 Chemical constituents of Arnebia euchroma
Main ingredients: Arnebia Root contains pigment components and fatty acids. ① The pigment component is naphthoquinone derivative, withL-shikonin（(-)-Shikonin）、D-shikonin（(+)-Shikonin）、Acetylshikonin（Acetylshikonin）、Deoxyshikonin（Deoxyshikonin）、 Isobutyshi Konin, isovalerylshikoninβ. β - dimethyl acryloyl Shikonin（β,β-Dimethyla- crylshikonin）、β - hydroxyisovaleryl Shikonin（β-Hydroxyisovalerylshikonin）、 Alkannan, alkannin, α - methyl-n-butyrylshikonin, 3,4-dimethylpenten-3-acyl shikonin. The roots of Xinjiang pseudopurple grass contain β - hydroxyisovaleryl shikonin and 3,4-dimethylpenten-3-acyl shikonin. [2] 
② Fatty acids are mainly palmitic acid, oleic acid and linoleic acid.
2. Active ingredients: includingAcetylshikonin（acetylshikonin）、β - hydroxyisovaleryl Shikonin（β-hydro-xyisovalerylshikonin）、L-shikonin、D-shikonin、β. β - dimethyl acryloyl Shikonin(β, β -dimethylacrylshikonin) et al.


3、 Pharmacological action of Arnebia euchroma
1. anti pathogenic microorganisms: shikonin can inhibit Jingke 68-1 virus in vitro, shikonin can inhibit influenza virus in chicken embryos, and can delay the cytopathic effect of poliovirus in tissue culture, shikonin can inhibit immune response to hepatitis B antigen (HBsAg) and HAA immunoprecipitation line; Shikonin has inhibitory effect on Staphylococcus aureus, Escherichia coli, typhoid bacillus, Shigella dysenteriae and Pseudomonas aeruginosa. The decoction of crude medicine and water is 1:1, and shikonin has the strongest antibacterial ability against the above bacteria, while shikonin is poor; The 10% saline extract of Arnebia euchroma has an inhibitory effect on fungi such as dermatophyte flocculus and tinea laniformis, but it loses its antibacterial power after boiling. Shikonin decoction has certain curative effect on tuberculosis in mice.
The ether, ethanol or water extract of shikonin, shikonin, acetylshikonin and other oral or topical drugs can inhibit the hyperpermeability of capillaries (including those caused by histamine, bromelain, bradykinin and anti rat serum, rabbit serum), and can also inhibit the local edema of animals caused by carrageenan, anti rat serum, rabbit serum, formaldehyde and heat stimulation or the peritonitis of mice caused by formaldehyde. And inhibit the proliferation of subcutaneous cotton ball granuloma, indicating that it has an antagonistic effect on vascular hyperpermeability, exudation and edema in the acute exudative phase of inflammation and inflammation in the proliferative phase. Adrenalectomy in animals still has anti-inflammatory effect. The ointment prepared by Arnebia extract or its pigment components can promote the proliferation of granulation tissue and significantly accelerate wound healing.
The oral administration of shikonin decoction has a mild antipyretic effect on experimental fever in rabbits, and its extract and pigment components also have a mild antipyretic effect. Shikonin has the effect of anti herpesvirus local strains. The sensitivity test of shikonin maintenance solution with 100mg / ml to HSV-I virus was carried out, and its anti virus index was 3-5.
2. effects on gastrointestinal smooth muscle: oral administration of shikonin Decoction to rabbits can enhance the tension or contraction of the small intestine, which can be related to the efficacy of shikonin in benefiting the large intestine and smoothing the intestine. It is commonly used by people with constipation due to fever, rash and spot poison. On the other hand, shikonin and acetylshikonin at concentrations higher than 10-4g/ml It can relax the intestinal tract and antagonize acetylcholine, histamine, angiotensin, barium chloride and other intestinal contractile substances. These effects do not take effect through the autonomic nervous system or the corresponding receptors, but are the direct result of pigment component stimulation. This effect may relieve the spasm and pain of gastrointestinal smooth muscle. Shikonin is commonly used in traditional Chinese medicine to treat blood dysentery, which is not only related to its anti-inflammatory, antibacterial and other effects, but also related to the spasmolytic effect. The relationship between the above two different effects and the dosage form of drugs, the functional state of animals or organs and other reasons remains to be studied.
3. effect on blood coagulation: intraperitoneal injection of shikonin components (shikonin, acetylshikonin) does not affect blood coagulation time, but can prevent the anticoagulant effect of heparin. .
4. antitumor effect: the extract of shikonin (B, b-dimethyleneacyl shikonin, B, b-dimethylpropionyl shikonin, acetylshikonin and b-acetoxyisoacyl shikonin) has a certain inhibitory effect on the late stage of DNA synthesis (G2 phase) of HeLa cells at the concentration of 0.25mg / ml culture medium, which delays the entry into division, resulting in a decline in the division index, and a 70% decline in the division index in the first 4 hours. However, it has no inhibitory effect on 3H thymidine uptake by this cell, so it has no effect on DNA synthesis; It has a colchicine like effect on the metaphase of division, but the effect is mild. Therefore, Arnebia euchroma may also interfere with other links besides affecting the G2 phase of cells.
Further experiments showed that this part of the extract had obvious inhibitory effects on EAC, U14, S180, S39, W256, etc. When the dose is 5-10mg / kg per day, the growth of ascitic sarcoma 180 cells can be completely inhibited; 10mg / kg per day could prolong the life of tumor bearing mice by 92.5%; If the dose is too large, the patient will die of poisoning, but if the dose is too small (LMG / kg per day), it will be ineffective. Shikonin can reduce the incidence of spontaneous breast cancer.
5. contraceptive effect: the ethanol extract of grass root (made in Japan) and purple grass root can inhibit the estrous period of rats when fed to animals, while the pigment extracted from the root is ineffective. . The bioassay experiment with the change of the uterus weight of young mice as the index proved that the mice had obvious effects of anti pituitary gonadotropin and anti chorionic gonadotropin after oral administration of shikonin. In terms of the intensity of action, shikonin produced in Guangxi was better than that produced in Xinjiang. Normal mice were orally administered with Shikonin syrup 2.5G (crude drug) / (kg. day) for 2 months, and the weight of uterus and ovary were reduced, especially the weight of ovary. The mice were orally given 10% shikonin bait 5g/kg body weight. After 48 days of dissection, it was found that the follicles in the ovaries were reduced, and there were small vacuoles and steatosis in the oviduct epithelium.
6. effect on circulatory system: Arnebia euchroma from Xinjiang has obvious excitatory effect on the hearts of healthy rabbits in vivo and toads in vitro; This reaction was also observed in isolated hearts after drug inhibition. This effect may be related to the calcium salt it contains. . Under general anesthesia, intravenous or intramuscular injection of shikonin decoction can make half of the experimental animals such as rabbits, cats and dogs have a sharp drop in blood pressure, and even die, but it has no obvious effect on non anesthetized animals by injection or oral administration.
7. hypoglycemic effect: shikonin a, B, C (lithopermana) (a, B, c) obtained from Arnebia euchroma, when given a dose of 100mg / kg, intraperitoneal injection, the blood glucose reduction rates (%) of normal mice were 64, 83, 55, respectively. Among them, polysaccharide B and C could maintain for 24 hours in alloxan induced hyperglycemic mice, and only polysaccharide a had a hypoglycemic rate of 51 after 7 hours of administration.