Tripterygium wilfordii
1、 Pharmacopoeia standard of Tripterygium wilfordii       This product is the dried stem of Erycibe obtusifolia benth. or Erycibe schmidtii Craib, a plant of Convolvulus family. It can be harvested all year round, sectioned or sliced, and dried in the sun.
      [properties] this product is a beveled segment or piece, with a diameter of 1-10cm. The outer skin is grayish yellow, grayish brown or light tan, slightly rough, with shallow grooves and irregular longitudinal cracks or turtle cracks, lenticels are punctate or warty, yellowish white, and the old cork is flaked. It is hard, has many fibers, and is not easy to break. The section is oval, yellowish brown or light yellowish brown. The heterotypic vascular bundles are flower shaped or massive, and the xylem vessels are punctate. The air is weak and the taste is light.
      [identification] take 3G of this product powder, add 40ml of ethanol, soak overnight, heat and reflux for 6 hours, filter, add 6ml of 6mol/l hydrochloric acid solution to the filtrate, heat and reflux for 3 hours, evaporate to dryness, and add 10ml of ethanol to dissolve the residue as the test solution. In addition, take scopoletin reference substance and add ethanol 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 each of the above two solutions, dot them on the same silica gel G thin-layer plate, use cyclohexane trichloromethane ethyl acetate formic acid (6:10:7:1.2) as the developing agent, develop, take out, dry, and view under the ultraviolet light (365nm). In the chromatogram of the test sample, the same bright blue fluorescent spots appear at the positions corresponding to the chromatogram of the control sample.
      [inspection] the moisture content shall not exceed 12.0% (the second method of general rule 0832).
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      [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 3.0%.
      [content determination] determine according to HPLC (general rule 0512).
      ; The mobile phase was methanol water glacial acetic acid (32:68:0.16); The detection wavelength was 298nm. The number of theoretical plates should not be less than 2000 according to scopoletin peak.
      Preparation of reference solution take an appropriate amount of scopoletin reference, weigh accurately, add methanol to make a solution containing 40 μ g per 1ml.
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      The determination method is to precisely suck 10 μ l of the reference solution and 10 μ l of the test solution, inject them into the liquid chromatograph, and determine.
      The content of scopoletin (c10h8o4) in this product shall not be less than 0.050% according to the calculation of dry product.
      Decoction pieces
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      [nature, taste and meridian tropism] pungent, warm; . .
      [functions and indications] dispel wind and dampness, reduce swelling and relieve pain. It is used for rheumatic arthralgia, hemiplegia, tumefaction and pain.
      [usage and dosage] 3-6g, used to prepare liquor, take orally or apply externally.
      ; Forbidden for pregnant women.
      [storage] put it in a dry place.


2、 Chemical constituents of Tripterygium wilfordii
Tripterygium wilfordii stem containsBaogongteng a(baorongteng a), namely 2 β - hydroxy-6 β - acetoxynortropane (2 β - hvdroxv-6 β - acetoxynortropane),Baogongteng C(baogungteng C), namely 2 β, 6 β - dihydroxynortropane, baogongtengb, namelyScopoletin Pavilion（scopoletin），Scopoletin(scopolin) and trace amounts ofcaffeic acid(caffeic acid) andchlorogenic acid（chlorogenic acid）。 Tripterygium wilfordii contains Baogongteng B andScopoletin。

3、
  . Scopoletin, an effective component extracted from Tripterygium wilfordii, was intraperitoneally injected at 25mg / kg, which had a significant protective effect on egg white and histamine induced paw swelling in rats, lasting for more than 4 h. After formaldehyde induced paw swelling in rats, scopoletin 25mg / kg · D was injected intraperitoneally for 7 days, showing obvious anti-inflammatory and detumescence effects. Intraperitoneal injection of crude extract 1g / kg or scopoletin 50mg / kg in mice significantly inhibited the increase in capillary permeability of abdominal skin caused by xylene. Intraperitoneal injection of scopoletin (11.25-15mg / (kg · d) for 7 consecutive days in rats can significantly reduce the dry weight of granuloma formed by cotton balls and inhibit the proliferation of connective tissue. 2. effect on immune function Dinggongteng injection can increase the percentage of lymphocytes positive for acid α - acetoesterase (ANAE) in peripheral blood lymphocytes of rats, and can also significantly reduce the leukocyte migration index, increase the number of specific rosette forming cells and neutrophil phagocytosis rate, indicating that Dinggongteng has a promoting effect on cellular immunity and humoral immunity.
3. pupil constriction the effective component of pupil constriction extracted from the stem of Eupatorium wilfordii is Baogongteng a, which is clinically used to treat glaucoma. It has been synthesized artificially. The synthetic strain is racemate, and the action intensity is halved. In addition, 6 β - acetoxynortropane (6 β - an), a synthetic analogue, has stronger miotic effect and can be used as a substitute for Baogongteng and pilocarpine.
(1) The optimal concentration of Baogongteng benzoate solution for miosis is 0.026%. The miosis can be maintained for 9h after dropping into rabbit eyes for 10min, and the pupil area can be reduced by 63% after 45min of medication; The synthetic with equal concentration has a slower onset and shorter maintenance time, with a pupil area of 29.9%. Equal concentration of 6 β -an has strong miotic effect, and the pupil diameter is reduced by 57% after 30min of treatment, while that of Baogongteng is 43% [4].
(2) There was no significant difference in lowering the intraocular pressure of normal rabbit eyes by 0.025% Baogongteng, 2% pilocarpine and 0.05% physostigmine.The intraocular pressure of normal rabbit eyes was reduced..the results showed that the intraocular pressure of normal rabbit eyes was decreased by 0.025% of Baogongteng, 2% of pilocarpine and 0.05% of physo; 0.003% 6 β - an had obvious hypotensive effect on normal intraocular pressure and high intraocular pressure with water load in rabbits, and the high intraocular pressure with water load decreased to normal level after 1h of treatment.
4. cardiovascular effects through the observation of rat in situ and ex vivo hearts, Baogongteng can significantly slow down heart rate, increase myocardial contractility, reduce myocardial oxygen consumption, suggesting that it has the effect of improving cardiac function [6-8]. 0.0237mg / kg of 6 β - an solution was injected intramuscularly into conscious rabbits. The heart rate slowed down from 5 to 10 minutes, and the slowest heart rate was 54% at 20 to 25 minutes. The heart rate returned to normal after 2 hours; . Under the control dose, it may be used to relieve sinus. It has moved too fast.
5. for central nervous action, the brain waves of rabbits were recorded by chronically buried electrodes. Intravenous injection of 6 β - an 12 μ g / kg or physostigmine 0.2ing / kg could antagonize scopolamine induced high amplitude diffuse waves in 20-30 min. The central m-choline tremor induced by intraperitoneal injection of Baogongteng in mice was similar to the effects of central m-choline agonists oxytremor and tremor, and the intensity was between the two. The combination of Baogongteng and tremor produced a synergistic effect, and the combination with scopolamine showed an anti-inflammatory effect, suggesting that Baogongteng and its synthetic products may become tool drugs and traditional Chinese medicine anesthetic hypnotics to replicate animal models of Parkinson's disease [6,11]. Maze and step-down tests in mice showed that intraperitoneal injection of 6 β - an at 0.08-0.12 mg / kg could promote learning and memory.
6. study on the mechanism of action there was no obvious anti cholinesterase effect and muscle fibrillation after intramuscular injection of 0.1lng / kg of Baogongteng a in rabbits; The intramuscular injection of 0.237mg / kg of 65-an had a weak inhibitory effect on the enzyme, and the lethal dose of 6 β -an did not show the phenomenon of N receptor excited muscle fibrillation. Using the cumulative dose effect curve method, the kinetics of m-choline receptor in isolated tissues (rabbit iris, guinea pig ileum longus muscle and rat jejunum) was studied. It was proved that the order of affinity and intrinsic activity for m-choline receptor was 6 β - an > Baogongteng a > pilocarpine. The three drugs showed competitive antagonism to different doses of atropine, and the anti lift parameters of the three drugs were 10-8-10-9mol / L, indicating that these drugs are specific m-choline receptor agonists [4, 6, 10, 12]. Through the radioligand [3h]qnb competition inhibition binding test, the IC50; Analysis with Hill coefficient showed that Baogongteng and pilocarpine acted on M receptor. Among the four target membrane receptors, the order of PKI (receptor affinity intensity) of 6 β -an inhibiting [3h "QNB was heart > cortex and hippocampus > intestinal longissimus > iris, suggesting that 6 β -an has the greatest affinity for cardiac membrane receptors and is a M2 receptor selective compound. 7. other effects scopoletin inhibited the contraction of isolated uterus of pregnant rats and ileum of guinea pigs induced by histamine; Levis believes that the inhibition of spontaneous uterine contraction in vitro pregnancy rats lies in the inhibition of prostate synthase and antagonism of prostaglandins. 8. toxicity the maximum tolerated dose of scopoletin in mice was 100mg/kg after intravenous injection for 72h, and no toxic reaction was found. ; The LD50 of 63-an was 6.22mg / kg. The symptoms of poisoning were parasympathetic hyperactivity, and the animals in the high-dose group had central organ tremor similar to oxytremor. Atropine and scopolamine are specific antidotes. . 0.003% - 0.004 5% concentration of 6 β -an was given to rabbit eyes twice a day for 4 months, and no abnormal changes in ocular and systemic manifestations were found.