1、 Pharmacopoeia standard of Sinomenium sinense
This product is the dried vine stems of Sinomenium acutum (thunb.) rehd. et wils. and Sinomenium acutum (thnnh.) rehd.et wils. var. Cinereum rehd. et wils. Harvest and cut in late autumn and early winter, tie or cut long sections, and dry them in the sun.
[properties] the product is long cylindrical, often slightly curved, 20-70 cm long or longer, and 0.5-2cm in diameter. The surface is greenish brown to tan, some grayish brown, with fine longitudinal lines and lenticels. The nodes are slightly swollen and branched. It is light, hard and brittle, easy to break, with uneven section, grayish yellow or grayish brown, narrow skin, radial arrangement of wood rays, and yellowish white or yellowish brown pulp. The breath is slight and the taste is bitter.
[identification] (1) cross section of this product: the outermost layer is epidermis, covered with thick cuticle, or cork layer. . The fiber bundle of the middle column sheath is crescent shaped, and its inner side is often 2-5 rows of stone cells, and extends tangentially to connect with the stone cell population in the ray to form a ring. . The phloem ray widens outward, and cone-shaped or branched stone cells can be seen; Most phloem cells were decadent, and some scattered 1-3 fibers. Xylem vessels are singly scattered or several tangential connections. The pulp cell wall is slightly thicker and the pits are obvious. Parenchyma cells contained starch granules and calcium oxalate crystals.
Powder yellowish brown or grayish brown. The epidermal cells are yellow or yellowish brown, round or rectangular in cross-section, with a diameter of 24-78 μ m, and are covered with cuticle. The stone cells are light yellow or yellow, square, spindle, oval or irregular, with thick walls and obvious pore grooves. The cortical fibers are yellowish or yellow, with a diameter of 27-70 μ m, extremely thick walls and narrow cell cavities. Calcium oxalate needle crystals are fine and exist in parenchyma cells.
(2) Take 2G of this product powder, add 25ml of ethanol, heat and reflux for 1 hour, filter, evaporate the filtrate, add 1ml of ethanol to dissolve the residue, and use it as the test solution. In addition, take sinomenine reference substance and add ethanol to make a solution containing 1mg per 1ml as the reference substance 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).
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[content determination] determine according to high performance liquid chromatography (general rule 0512).
Chromatographic conditions and system suitability test octadecylsilane bonded silica gel was used as filler; The mobile phase was methanol phosphate buffer (0.005mol/l sodium dihydrogen phosphate solution, 0.005mol/l sodium dihydrogen phosphate to adjust the pH value to 8.0, and 1% triethylamine to adjust the pH value to 9.0) (55:45); .
Preparation of reference solution take an appropriate amount of sinomenine reference, weigh accurately, add methanol to make a solution containing 0.5mg per 1ml.
Preparation of test solution take about 0.5g of the powder (passing through No. 3 screen), accurately weigh it, place it in a corked conical flask, precisely add 20ml of 70% ethanol, close the stopper, weigh it, sonicate (power 250W, frequency 20KHz) for 20 minutes, cool it, weigh it again, use 70% ethanol to make up the lost weight, shake it well, filter it, and take the filtrate.
The determination method is to precisely suck 5 μ l each of the reference solution and the test solution, inject them into the liquid chromatograph, and determine.
The content of sinomenine (c19h23no4) in this product shall not be less than 0.50% according to the calculation of dry product.
Decoction pieces
[processing] remove impurities, slightly bubble, moisten thoroughly, cut thick pieces, and dry.
This product is a thick round piece. The outer surface is greenish brown to tan, some are grayish brown, with longitudinal lines, and some can see lenticels. The cut surface is grayish yellow to grayish yellow, the skin is narrow, the wood has obvious radial texture, with many small holes, and the pulp is yellowish white to brownish yellow. The breath is slight and the taste is bitter.
[inspection] the moisture content is the same as that of medicinal materials, and shall not exceed 9.0%.
[identification] (except the cross-sectional surface) [inspection] (total ash) [content determination] is the same as that of medicinal materials.
[nature, taste and meridian tropism] bitter, pungent and peaceful. Return to the liver and spleen meridians.
. For rheumatism, arthralgia, joint swelling, paralysis and itching.
[usage and dosage] 6 ～ 12g.
[storage] put it in a dry place.

2、 Sinomenine A and other alkaloids are contained in the stems of sinomenine.

3、

① Effects on the nervous system
I. analgesic effect: sinomenine has been proved to have definite analgesic effect in the tests of electric stimulation in mice, hot plate method and photothermal stimulation in rabbits. The dose needed for intracerebral injection to produce analgesic effect is equivalent to 1 / 2000 of that of intraperitoneal injection, indicating that the analgesic effect is located in the central nervous system; When combined with allyl morphine, it does not antagonize, but synergize, indicating that its analgesic principle is different from morphine analgesics. The dose needed to produce analgesia is about 10 times that of morphine, and the duration is short. Continuous application can also produce tolerance, but it is slower than morphine, and there is no cross tolerance with morphine. When combined with promethazine, the effect is enhanced, which is mainly due to the synergy of the central effects of the two drugs, and partly due to promethazine antagonizing the release of histamine from sinomenine. When combined, it has no effect on the generation of tolerance and toxicity of sinomenine. Second, sedative effect: sinomenine significantly reduced the spontaneous and passive activities of mice, and had no obvious effect on barbiturate sleep time; It has some antagonistic effects on strychnine (reducing the convulsion threshold of strychnine in mice), but it cannot antagonize pentamethene tetrazolium. Sinomenine 45 ～ 95 mg / kg orally also has significant sedative effect in dogs and monkeys. A small dose (5-10 mg / kg) can prolong the latency of defensive motor conditioning in mice and cats, and some of the conditioned reflex disappears, followed by a small part of the unconditioned reflex, indicating that it first has an inhibitory effect on the excitation process of higher neural activities. Sinomenine can also eliminate the irritating reaction caused by electrical stimulation in mice, which seems to have a stabilizing effect. 3. Other effects: sinomenine has antitussive effect, and its antitussive potency in mice and cats is similar to that of codeine; For guinea pigs, its potency is only 1 / 4 that of codeine. . In addition, it has a slight emetic effect and has no effect on vomiting caused by morphine injection. It has a certain cooling effect on rats when a large dose is injected intraperitoneally. When rabbits are injected with toxic dose, the body temperature also decreases, but if given repeatedly, tolerance can be produced and the body temperature will not drop. It is reported that it has a local anesthetic effect on rabbit cornea and can be used as a local infiltration anesthetic, but it can also produce tolerance. If continuous injection, the effect will be weakened.

② Hypotensive effect
Sinomenine has a certain acute antihypertensive effect on anesthetized or non anesthetized experimental animals (dogs, cats, rabbits, rats), whether injected intravenously or by gavage. The effect is rapid, significant and lasting, but it can produce rapid tolerance when administered continuously for many times. The hypotensive effect is not related to M-cholinergic nerve or acetylcholine, nor is it caused by histamine release, which may be related to its anti epinephrine and nerve reflex effects. Due to the above antihypertensive properties, it has no significant therapeutic effect on chronic experimental hypertension in dogs. The acidic extract of Sinomenium sinense did not affect blood pressure in the acute test of rabbits.

③ Effect on gastrointestinal activity
Sinomenine often has mild gastrointestinal adverse reactions when administered orally to dogs and monkeys; It has inhibitory effect on isolated rabbit intestine and guinea pig intestine, and can resist the spasmodic effect caused by pilocarpine, histamine, acetylcholine and barium chloride, but for the eutopic dog and rabbit intestine, intravenous injection of sinomenine causes temporary excitation of the small intestine, which can be completely blocked by diphenhydramine and hexahydrocarbon quaternary ammonium, and completely or partially blocked by atropine, but cutting off the bilateral vagus nerve cannot block it. Injection of sinomenine could increase the secretion and acidity of gastric juice, and the pepsin activity had no obvious change. The excitatory effect on gastrointestinal tract is mainly related to histamine release. . The acidic extract of Sinomenium sinense can excite the isolated rabbit intestine.

④
Sinomenine has a significant regressive effect on formaldehyde induced and egg white arthritis in rats, but it has no effect after adrenalectomy or pituitary gland resection. For normal rats, it can reduce the content of vitamin C in the adrenal gland, and it will lose this effect after pentobarbital (which can inhibit the hypothalamus) anesthesia. Therefore, the anti-inflammatory mechanism of sinomenine may be caused by the influence of the hypothalamus on the pituitary adrenal system, and has nothing to do with the release of histamine. It can prevent active anaphylactic shock in guinea pigs, but it is relatively poor in dogs. When applied simultaneously with antigen, it can inhibit the release of histamine from antigen. It also has inhibitory effect on Trichomonas and Plasmodium.