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Uncaria rhynchophylla
Gouteng
UNCARIAE RAMULUS CUM UNCIS
This product is the dried hooked stem branches of Uncaria rhynchophylla (miq.) miq.ex havil., Uncaria macrophylla wall., Uncaria hirsuta havil., Uncaria sinensis (oliv.) havil., or Uncaria sessilifructus roxb., which belong to the Rubiaceae family. Harvested in autumn and winter, defoliated, segmented, and dried in the sun.Gouteng
UNCARIAE RAMULUS CUM UNCIS
[properties] the stems and branches of this product are cylindrical or square columnar, 2-3cm long and 0.2-0.5cm in diameter. The surface is reddish brown to purplish red with fine longitudinal lines, smooth and hairless; Some yellowish green to grayish brown ones can see white punctate lenticels, which are covered with yellowish brown pubescence. Most branches have two opposite downward curved hooks (sterile peduncle), or only one side has hooks, and the other side is a protruding scar; The hook is slightly flat or round, the apex is thin and pointed, and the base is relatively broad; On the branches at the base of the hook, there are dens like traces and ring-shaped stipule traces after the petiole falls off. It has tough texture, yellowish brown section, fibrous skin, yellowish white or hollow pulp. The air is weak and the taste is light.
[identification] (1) Uncaria rhynchophylla powder is yellowish brown to reddish brown. Phloem parenchyma cells are in sheets, the cells are elongated, the boundary is not obvious, and the secondary wall is often separated from the primary wall, in a spiral or irregular twisted shape. The fibers are in bundles or scattered individually, with many fractures, with a diameter of 10-26 μ m and a wall thickness of 3-11 μ M. . The epidermal cells are brownish yellow, polygonal or slightly elongated on the surface, with a diameter of 11 ~ 34 μ M. Calcium oxalate sand crystals exist in the oblong parenchyma cells, which are dense, and some sand crystal containing cells are connected in rows.
Uncaria sinensis is similar to Uncaria.
Single cell non glandular hairs were more common in Uncaria grossedentata, and multicellular non glandular hairs were 2-15 cells.
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Non glandular hairs are rare in Uncaria sessiliflora, with 1-7 cells. Sclerenchymal cells, oblong like, 41-121 μ m long and 17-32 μ m in diameter can be seen.
(2) Take 2G of this product powder, add 2ml of concentrated ammonia test solution, soak for 30 minutes, add 50ml of chloroform, heat and reflux for 2 hours, cool, filter, take 10ml of filtrate, volatilize, add 1ml of methanol to dissolve the residue, and use it as the test solution. In addition, take isorhynchophylline reference substance and add methanol to make a solution containing 0.5mg per 1ml as the reference substance solution. According to the thin-layer chromatography (general rule 0502), suck 10 ~ 20 μ l of the test solution and 5 μ l of the control solution, respectively dot on the same silica gel G thin-layer plate, use petroleum ether (60 ~ 90 ℃) - acetone (6:4) as the developing agent, develop, take out, dry, and spray with improved bismuth potassium iodide test 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 10.0% (the second method of general rule 0832).
The total ash content shall not exceed 3.0% (general rule 2302).
[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 6.0%.
[nature, taste and meridian tropism] sweet and cool. Return to liver and pericardial meridian.
[functions and indications] it can calm the wind, calm the shock, clear away heat and calm the liver. It is used for internal movement of liver wind, convulsion, febrile convulsion, cold shock, crying of children, eclampsia during pregnancy, headache and dizziness.
[usage and dosage] 3 ~ 12g, rear lower.
[storage] put it in a dry place.
2、 Chemical constituents of Uncaria rhynchophylla
1. the stems and leaves of Uncaria rhynchophylla contain 2-oxoindole alkaloids;Isorhynchophylline(isocorynoxeine), Isorhynchophylline, isorhynchophyllic acid methyl ester,Rhynchophylline(corynoxeine), Rhynchophylline (rhynchophyllic acid methyl ester), indole alkaloidsRhynchophylline dehydrogenate(hirsuteine), Hirsutine, corynantheine, dihydrocorynantheine andTrace akumidine(akuammigine)。 The leaves also contain indole alkaloids glucoside: 6 ′ - feruloyl vinculin lactam, vincoside lactam, strictosamide, isovincoside lactam, indole alkaloids: vallesiachotamine and phenolic compounds: l-epicatechin,Hyperin(hyperin),Trifolin(trifolin)。 . Uncaria also contains β - (yohimbine) and GEIs soschizine methyl ether.
2. the stems of Uncaria sinensis contain 2-oxoindole alkaloids: isopteropodic acid, ptcropodic acid, MI traphylic acid, indole alkaloids:Tetrahydropalmatine(tetrahydroalstonine),Rhynchophylline e(isopteropodine),Isorhynchophylline。Rhynchophylline C(pteropodine), Rhynchophylline a (7-isormosanine),CapparineThat is, mitraphylline, mitraphyllic acid methyl ester.Rhynchophylline, isorhynchophylline N-oxide, pteropodine N-oxide, rhynchophylline N-oxide, and mitraphylline N-oxide. containScopoletin Pavilion(scopoletin) 3. the leaves of Uncaria macrophylla contain 2-oxoindole alkaloids:Isorhynchophylline,Rhynchophylline, corynoxine, corynoxine B.
3、 Pharmacological action of Uncaria rhynchophylla
1. effect on cardiovascular system: 1.1. antihypertensive effect: Uncaria Decoction, ethanol extract, Uncaria alkaloids and Uncaria alkaloids have antihypertensive effect on anesthetized animals or non anesthetized animals, normal animals or hypertensive animals, as well as intravenous or gastric administration. And no rapid tolerance. Intravenous injection of Uncaria Decoction 2-3g/kg in anesthetized rabbits or 0.05g/kg in anesthetized dogs can reduce blood pressure by 30-40% compared with the original level, lasting for more than 3-4 hours. Anesthetized cats were intravenously injected with 6.25g/kg Junteng decoction, 20mg/kg rhynchophylline hydrochloride, and 20mg/kg rhynchophylline hydrochloride. Blood pressure showed three-phase changes: first, blood pressure decreased, then rose quickly, and then decreased. The blood pressure decreased by 30-70%, 13.9-23.2%, and 11.7-41.7%, respectively, for 3-4 hours. However, the antihypertensive effect of Gouteng Decoction is weakened if it is decocted for a long time, and it is appropriate to decoct it within 20 minutes. The hypotensive degree of Junteng ethanol extract 3g/kg was similar to that of Decoction 2g/kg. Both rhynchophylline 20mg/kg and rhynchophylline 20mg/kg intravenously had antihypertensive effects in cats; . The renal hypertensive rats were treated with intragastric administration of Junteng Decoction 8g/kg, rhynchophylline 50mg/kg and rhynchophylline 50mg/kg, once a day for 15-20 days. The blood pressure started to drop on the 3rd-5th day, and fell to the lowest on the 7th-15th day. The average blood pressure reduction was 16.9mmhg, 12mmhg and 18mmhg, respectively; Rhynchophylline 20mg/kg, intraperitoneal injection, can make the blood pressure of rats drop on the same day. After 8 days of medication, the average blood pressure drop is 24mmhg. In 12 anesthetized dogs, blood pressure decreased after intravenous infusion of rhynchophylline 20mg/kg at a constant rate; ; The total peripheral vascular resistance decreased significantly at the initial stage of hypotension; The heart rate slowed significantly; Stroke volume increased significantly. Rhynchophylline causes hypotension by reducing peripheral resistance (early stage) and cardiac output (late stage).
In terms of the effect of juntengine on myocardial mechanics in anesthetized dogs and cats, dp/dt was used as a multi index comprehensive analysis. At the same time of measuring dp/dt, the left ventricular wall muscle tension was measured with a stressmeter arch, which was used as an index of myocardial contractility. Combined with the VCE index, which was sensitive to the acute change of contractile performance level and had a small load dependence, the inotropic effect of juntengine on the heart was observed. After intravenous injection of rhynchophylline 20mg/kg, myocardial contractility indexes such as LVP, dp/dtmax, lvmt, VPM, and Vmax were significantly reduced; Rhynchophylline can reduce the intraventricular pressure, so the reduction of TTI indicates the reduction of myocardial energy and O2 consumption, which may have protective significance when the myocardial supply is insufficient. Although rhynchophylline has obvious negative inotropic effect and can reduce O2, all indicators tend to recover after 15 minutes, indicating that its effect of inhibiting myocardial contractility is reversible. In addition to vasodilation and reduced peripheral resistance, the antihypertensive effect of the drug is partly related to the inhibition of myocardial contractility. Using isolated rabbit thoracic aorta strips, the mechanism of rhynchophylline vasodilation was explored and compared with verapamil. Both drugs can reduce the contraction tension caused by k+ and norepinephrine, and the effect of k+ contraction is significantly greater than that of norepinephrine. The two drugs significantly attenuate the release of internal ca+ in the contraction reaction of norepinephrine, and shift the dose-response curve of k+, norepinephrine and ca2+ to the right, and the maximum response is depressed, suggesting that juntengine blocks the influx of external ca2+ and the release of internal ca2+, and its characteristics are similar to verapamil. The methanol extract of Junteng also had a strong and lasting antihypertensive effect after intravenous injection of 0.1mg/kg to rats.
1.2. effect on hemodynamics: the hemodynamic effect of rhynchophylline on awake rats showed that: LVSP, Vmax, dp/dtmax immediately decreased significantly, with the decrease ranges of - 7.8%, 15.9% and - 23.2%, respectively, which were maintained for 5, 10 and 20 minutes, and then gradually returned to the pre drug level, while LVSP was significantly higher than that before administration at 90 minutes. Sap, DAP and map also immediately decreased significantly. The duration of SAP decline was shorter than the latter two items, and recovered at 30 minutes. DAP also rose slightly at 30 minutes, but it was lower than normal at 60 minutes, and map was always lower than normal during the observation. . LVEDP increased significantly just after administration, and then decreased to a level lower than that before administration. The HR immediately decreased significantly, and its maximum change value was - 35.3%, which was significantly lower than the pre drug level within 90 minutes of observation. Lvp- (dp/dtmax) P-1 loop was significantly narrowed, especially at 1 minute after treatment, and then gradually returned to normal.
. When the dose was increased to 5-10g/kg, the righting reflex of animals could not disappear. The 1g/kg intraperitoneal injection of the decoction of juntenggou and stem can reduce the excitability of the cerebral cortex of rats, weaken the impulse summation ability, affect the positive conditioned reflex of some rats, and prolong the reflex time. However, it has no obvious effect on differentiation inhibition and unconditioned reflex.
. At the same time, it can also prevent the explosion caused by hair cutting in the epileptic area of guinea pigs.
3. effect on contractile response of uterine smooth muscle: the contractile response of smooth muscle cells must be achieved by stimulating the activity of contractile proteins with the participation of ca2+. The uterine smooth muscle was depolarized with high k+ solution, and the potential dependent ca2+ channel (PDC) on the cell membrane was opened, prompting ca2+ influx to induce uterine contraction for a longer time. . Juntengine also had the same effect, indicating that it may also inhibit PDC. Rhynchophylline could also inhibit oxytocin induced contraction of rat uterus in vitro, which was enhanced with the increase of dose, and was antagonized by the addition of excessive CaCl2 (2mm).
4. other effects: juntengine can inhibit frog heart and rabbit heart in vitro and in vivo. It can also inhibit the respiration of frogs and mice and reduce the pupil. . Rhynchophylline could inhibit the contraction of colonic band induced by acetylcholine or high potassium depolarization in a dose-dependent manner. The dose-response curve showed that rhynchophylline antagonized CaCl2 non competitively. Juntengine has significant inhibitory effect on platelet aggregation and antithrombotic effect on myocardial electrophysiology, which increases with the dose.