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Release Date:2017/6/26 16:54:19
Nux vomica
1、 Pharmacopoeia standard of nux vomica
Nux vomica
Maqianzi
STRYCHNI SEMEN
      This product is the dried mature seed of Strychnos nux vomica L., a plant in the family of loganaceae. Harvest the mature fruits in winter, take out the seeds, and dry them in the sun.
      [properties] this product is button shaped, round and plate-shaped. It is often raised on one side and slightly concave on the other side. It is 1.5 ~ 3cm in diameter and 0.3 ~ 0.6cm thick. Its surface is densely covered with gray brown or gray green silky hairs, which are arranged radially from the middle to the four sides, with silk like luster. The edge is slightly raised, thicker, with raised micropyle, and a raised dot shaped navel in the center of the bottom. . The breath is slight and the taste is extremely bitter.
      [identification] (1) the powder of this product is grayish yellow. The non glandular hairs are single-cell, the base is expanded like stone cells, the wall is extremely thick, broken and lignified. Endosperm cells are polygonal, thick walled, and contain fatty oil and aleurone grains.
      (2) Take 0.5g of this product powder, add 5ml of trichloromethane ethanol (10:1) mixed solution and 0.5ml of concentrated ammonia test solution, tightly plug, shake for 5 minutes, place for 2 hours, filter, and take the filtrate as the test solution. In addition, take strychnine reference substance and brucine reference substance, add chloroform to make a mixed solution containing 2mg per 1ml as the reference solution. . In the chromatogram of the test sample, spots with the same color appear at the corresponding position of the chromatogram of the control sample.
      [inspection] the moisture content shall not exceed 13.0% (the second method of general rule 0832).
      The total ash content shall not exceed 2.0% (general rule 2302).
      [content determination] determine according to HPLC (general rule 0512).
      Chromatographic conditions and system suitability test octadecylsilane bonded silica gel was used as filler; The mobile phase was acetonitrile-0.01mol/l sodium heptanesulfonate and 0.02mol/l potassium dihydrogen phosphate (pH adjusted to 2.8 with 10% phosphoric acid) (21:79); .
      Preparation of reference solution take 6mg of strychnine reference and 5mg of brucine reference, weigh them accurately, put them into 10ml volumetric flasks respectively, add appropriate amount of chloroform to dissolve and dilute to the scale, and shake them well. Accurately measure 2ml respectively, put it into the same 10ml measuring flask, dilute it with methanol to the scale, shake well, and get it (containing 0.12mg strychnine and 0.1mg brucine per 1ml).
      Preparation of test solution take about 0.6g of powder (passing through No. 3 screen), weigh accurately, place in a corked conical flask, add 3ml of sodium hydroxide test solution, mix well, place for 30 minutes, add 20ml of trichloromethane precisely, close the stopper, weigh, put in a water bath for reflux extraction for 2 hours, cool, weigh again, make up the lost weight with trichloromethane, shake well, take trichloromethane solution, filter with a small amount of anhydrous sodium sulfate, discard the primary filtrate, accurately measure 3ml of the secondary filtrate, place in a measuring bottle, add methanol to the scale, shake well, and get it.
      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.
      According to the calculation of dry product, the content of strychnine (c21h22n2o2) should be 1.20% - 2.20%, and brucine (C23H26N2O4) should not be less than 0.80%.
      Decoction pieces
      [processing] remove impurities from raw nux vomica.
      [character], [identification], [inspection], [content determination] are the same as those of medicinal materials.
      .
      This product is shaped like nux vomica, with both sides bulging and thick edges. The surface is brown or dark brown, hard and brittle, and the brown or dark brown endosperm can be seen in the parallel section. It has slight aroma and bitter taste.
      [identification] (1) the powder of this product is brown or dark brown. Non glandular hairs are single-cell, brownish yellow, swollen like stone cells at the base, extremely thick wall, broken and lignified. Endosperm cells are polygonal, thick walled, and contain brown matter.
      [inspection] the moisture content is the same as that of medicinal materials, and shall not exceed 12.0%.
      [identification] (2) [inspection] (total ash) [content determination] is the same as that of medicinal materials.
      [nature, taste and meridian tropism] bitter, warm; It is highly toxic. Return to the liver and spleen meridians.
      [functions and indications] dredging collaterals and relieving pain, dispersing nodules and detumescence. It is used for traumatic injuries, bone fracture swelling and pain, rheumatism obstinate arthralgia, numbness and paralysis, carbuncle, gangrene and sore poison, sore throat swelling and pain.
      .
      [note] it is forbidden for pregnant women; It is not suitable to take more than once and for health use; Athletes should use it with caution; The toxic ingredients can be absorbed through the skin, and it is not suitable to apply them on a large area for external use.
      [storage] put it in a dry place.
 

2、 Chemical constituents of semen Strychni
    Muscarine(strychnine),Brucine(brucine), Isostrychnine, isobrucine, strychnine oxide, brucinen oxide, β - colubrine, 16 hydroxy - β - colubrine, 16 hydroxy - α - colubrine. ② Pseudoseries alkaloids: pseudostrychnine, pseudobrucine. ③ "N-methylpseudoseries" alkaloids: n-methyl-off-pseudomuscarine,Muscovite hypocrine(vomicine), n-methyl-off-pseudobrucine. The alkaloids contained in seeds are mainly of the "positive" series [1-3]. The seeds were heated at high temperature (220 ~ 260 ℃, 3min), and highly toxic componentsMuscarineBrucineThe content of isobrucine, isobrucine, N-oxide of brucine and N-oxide of brucine increased [3] The root bark and root xylem mainly contain "positive" series alkaloids, the stem bark mainly contains "pseudo" and "N-methyl pseudo" series alkaloids, and the leaves mainly contain "N-methyl pseudo" series alkaloids [1]. . The pulp also contains iridoid compounds: loganin, lo ganicacid, deoxyloganin, ketolo Ganin, secologanin [4].

There are many alkaloids in the seeds of Strychnos longicosa, which can be divided into three types: ① the "positive" series alkaloids: 4-hydroxy-3-methoxy-strychnine, strychnine, Brucine, 4-hydroxy-strychnine, strychnine N-oxide, α - krueline. ② "Pseudo" series alkaloids: pseudo strychnine, pseudo brucine. ③ "N-methyl-pseudo" series alkaloids: n-methyl-duan-pseudo-strychnine, strychnine, n-methyl-duan-pseudo-brucine and 4-hydroxy-3-methoxy-n-methyl-duan-pseudo-strychnine [5,6]. The alkaloids contained in seeds are mainly of the "positive" series [5]. The root bark and root xylem mainly contain "Zheng" series alkaloids, and the stem bark contains 1. effects on the central nervous system the muscarine contained in this product has an excitatory effect on the entire central nervous system. First, it excites the reflex function of the spinal cord, second, it excites the respiratory center and vasomotor center of the medulla oblongata, and can improve the sensory center function of the cerebral cortex.

1.1. action on the spinal cord the spinal cord is highly sensitive to strychnine. When 0.02% strychnine nitrate solution 0.5ml is injected subcutaneously into the frog, it can be seen that the reflex excitation increases, and the animal tremor can be caused by gently touching the skin surface; The increased reflexes were also observed in cats with brain amputation after intravenous injection of 0.01% muscarine nitrate 0.2mg/kg. Tonic convulsions may occur when the dose increases. The therapeutic dose of Genistein can make the nerve impulse transmit easily in the spinal cord, and can improve the excitability of spinal cord reflex, so it can shorten the spinal cord reflex time, increase the reflex intensity, and do not destroy the interactive inhibition process of spinal cord center, but the toxic dose of Genistein can destroy the interactive inhibition process. Tonic convulsions occurred. In the test tube, chitin can inhibit the decomposition of acetylcholine by cholinesterase. Therefore, it was once believed that this is the principle of the excitatory effect of chitin. . At the same time, it can also block the inhibitory effect of renshawcell on motor neurons in the spinal cord, which weakens or eliminates the interactive inhibition between antagonistic muscles (extensors and flexors), so large doses can cause tonic seizures.

1.2. effect on medulla oblongata according to the data, when 2mg/kg of muscarine nitrate was intravenously injected into the curare paralyzed dog, the blood pressure immediately increased (10-20mmhg) and continued at a high level for a long time. However, if the medulla oblongata of animals is destroyed, the blood pressure will drop immediately, and the dose of paxiletine will be increased, and the blood pressure will no longer increase, indicating that paxiletine can improve the excitability of vasomotor center and enhance blood circulation. Muscarine also has the effect of exciting the vagus nerve center, and can appear bradycardia. . In addition, it can also excite the cough center.

1.3. effects on cerebral cortex a small dose of muscarine can strengthen the excitatory process of the cortex and promote the recovery of patients in an inhibited state. It can also improve the functions of sensory organs such as taste, touch, hearing and vision. The therapeutic dose of muscarine has a good effect on experimental neurosis in dogs and monkeys, and can promote the recovery of the normal relationship between excitation and inhibition processes. .

2. effects on human lymphocytes it has been reported in clinic that the treatment of chronic aplastic anemia with paxiletine nitrate is effective. Liudexiang and others observed the effect of different doses of nux vomica sub Decoction on the mitotic index of human lymphocytes cultured in vitro. The results showed that when the concentration of the decoction was 0.3-0.7mg/ml, the mitotic index was basically the same, when the concentration was 0.2mg/ml, the mitotic index was basically the same, when the concentration was 0.1mg/ml, the mitotic index reached 9.975%, sharply increased to 1, more than the control group.

3. effects on digestive system the alkaloid has a strong bitter taste, which can stimulate the reflex of taste receptors, increase the secretion of gastric juice, and promote digestive function and appetite. The intestinal flaccidity test of patients has proved that the alkaloid has no excitatory effect on human gastrointestinal smooth muscle.

4. effects on respiratory system according to the report of the Xinjiang Uygur Autonomous Region pharmacology cooperation group for the prevention and treatment of chronic tracheitis in the elderly, the cough inducing test with sulfur dioxide or ammonia fog proved that brucine 50mg/kg gavage had obvious antitussive effect on mice, and its effect intensity exceeded that of codeine. The phenol red excretion method in mice proved that brucine 40mg/kg had obvious expectorant effect, and the intensity was not significantly different from that of ammonia chloride. The antiasthmatic effect is weak. However, animal experiments have found that the anti histamine effect of rabbits can be strengthened when the medication time is prolonged and the dosage is increased.

5. antibacterial effect: the water decoction (1:2) of nux vomica has different degrees of inhibitory effect on tinea schrenckii and tinea odonioides in the test tube. In vitro test showed that 0.1% brucine could completely inhibit the growth of Haemophilus influenzae, Diplococcus pneumoniae, Streptococcus A and catarrhalis.

6. other effects sollmanta reported that brucine has a paralyzing effect on sensory nerve endings. 5-10% brucine solution can anesthetize the oral mucosa. Brucine and strychnine can block neuromuscular transmission at a maximum dose, presenting an arrow like effect. This effect is covered by generalized convulsion on the whole animal, and can only be shown on the isolated neuromuscular specimens. Pseudo "and" N-methyl pseudo "series alkaloids are dominant, while leaves contain" N-methyl pseudo "series alkaloids [5]. In addition, leaves also contain n-cyano-sec-pseudostrychnine and n-cyano-sec-pseudobrucine [7,8].

3、 Pharmacological effects of nux vomica
 
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