Asiatic Moonseed Root Extract
Dauricine
CAS: 524-17-4
Molecular Formula: C38H44N2O6
Asiatic Moonseed Root Extract - Names and Identifiers
Asiatic Moonseed Root Extract - Physico-chemical Properties
| Molecular Formula | C38H44N2O6 |
| Molar Mass | 624.77 |
| Density | 1.185±0.06 g/cm3(Predicted) |
| Melting Point | 115° |
| Boling Point | 712.3±60.0 °C(Predicted) |
| Specific Rotation(α) | D11 -139° in methanol |
| Flash Point | 384.6°C |
| Solubility | Soluble in ethanol, acetone and benzene, slightly soluble in ether |
| Vapor Presure | 5.76E-21mmHg at 25°C |
| Appearance | Slightly yellow amorphous body |
| Color | Pale Beige |
| pKa | 9.31±0.45(Predicted) |
| Storage Condition | -20°C Freezer, Under inert atmosphere |
| Refractive Index | 1.601 |
| MDL | MFCD26960929 |
| Physical and Chemical Properties | The rhizome derived from the tetrandrae plant, dahuricae (Sophora tonkinensis) |
Asiatic Moonseed Root Extract - Reference
| Reference Show more | 1. He Wanwan and Zhang Jianwei Li Yunjing Kang Tingguo. Correlation between microscopic characteristic index and chemical composition of root of bean [J]. Chinese Journal of Experimental prescriptions, 2017, 23(01):42-46. 2. He Wanwan and Zhang Jianwei Li Yunjing Kang Tingguo. Correlation between powder color and effective components of radix sophorae tonkinensis [J]. Chinese Journal of Experimental prescriptions, 2017, 23(05):57-62. 3. Qiao, Baoru, et al. "Dauricine negativellely lipopolysaccharide-or cecal ligation and puncture-induced flammatory response via NF-Δb inactivation." Archives of biochemistry and biology 666 (2019): 99-106.https:// doi.org/10.1016/j. Abb.3/01, 9/2019 4. [IF = 3.559] Baoru Qiao et al."Dauricine negatively regulates lipopolysaccharide- or cecal ligation and puncture-induced inflammatory response via NF-κB inactivation."Arch Biochem Biophys. 2019 May;666:99 5. [IF=5.81] Ji Hu et al."Dauricine Attenuates Vascular Endothelial Inflammation Through Inhibiting NF-κB Pathway."Front Pharmacol. 2021; 12: 758962 |
Asiatic Moonseed Root Extract - Nature
Open Data Verified Data
is an alkaloid obtained from the rhizome of the Tetrandrine plant Pueraria dahuricae (cynomolgus), belonging to the group of benzyltetrahydroisoquinolines. As a broad-spectrum anti-arrhythmic drug, K ,Na and Caz transmembrane ion flow inhibition, but no anti-vagal effect. In addition, there are antihypertensive, local anesthesia, analgesic and diuretic effect. Commonly used for its sulfate, white fine needle-like crystals, odorless, bitter taste, light in case of gradual discoloration, aqueous solution was right optical rotation. Soluble in boiling water or ethanol, dissolved in chloroform, slightly soluble in water, almost insoluble in ether.
Last Update：2024-01-02 23:10:35
Asiatic Moonseed Root Extract - Preparation Method
Open Data Verified Data
The rhizome of D. Bat was extracted with 95% ethanol for 3 times, and the extract was concentrated to obtain the extract. The extract was extracted with 2%H2 S04, and the H2 S04 extract was extracted with chloroform to remove fat-soluble impurities, after extraction, the acid solution was adjusted to pH 9-10 with ammonia water, extracted with chloroform, concentrated, washed with 3% KOH, washed with water until neutral, dried and dehydrated with anhydrous Na2 S04, distilled chloroform to dryness; The residue was dissolved in sulfuric acid, and the dissolved solution was adjusted to pH 9~10 with ammonia water; Then extracted with ether, the ether extract was extracted repeatedly with 3% KOH, and the alkali solution was combined, add excess NH4 Cl to pH 9~10 to generate turbid liquid, the turbid liquid is extracted with ether, the extract is concentrated, and the product can be obtained by crystallization.
Last Update：2022-01-01 11:15:21
Asiatic Moonseed Root Extract - Use
Open Data Verified Data
dauricine has antipyretic, analgesic, spasmolytic, hypotensive and diuretic functions. Mainly used for tonsillitis, rheumatic pain and asthma treatment, the dosage of 30~40mg/times.
Last Update：2022-01-01 11:15:21
Asiatic Moonseed Root Extract - Reference Information
| Alkaloids | Dauricine, also known as nordaurine, is extracted and separated from the rhizome of the Fanghexiaceae plant Budzu (Sophora chinensis) to obtain a dibenzyl tetrahydroisoquinoline alkaloid, which is a toxic drug. Pharmacological studies have shown that, dauricine has antibacterial, antiarrhythmic, protective effects on myocardial ischemia, protective effects on cerebral ischemia and anti-tumor effects. The effect is similar to quinidine and has no anticholinergic effect. It can inhibit the transmembrane ion flow of potassium, sodium and calcium, which can reduce the maximum rise rate and amplitude of the action potential 0 phase, and prolong the time course of the action potential of the atrial and ventricular muscles. Reduce autonomy and myocardial excitability, slow heart rate, inhibit myocardial contractility. It has the characteristics of fast onset and slow recovery. Dauricine is a broad-spectrum antiarrhythmic drug with high curative effect and low side effects. It has been produced and used in clinical practice. It is suitable for the treatment of tachyarrhythmia, especially for atrial, borderline and ventricular premature beats. Better; good effect on preexcitation syndrome with ventricular tachycardia; poor effect on atrial flutter and fibrillation. |
| bean root | bean root, also known as bat vine and bat kudzu, is the Menispermum dauricum DC of bat kudzu. The dry root. Perennial twining herb, several meters long, the whole plant is nearly glabrous. The rhizome is long, thicker and yellowish brown. Born on hillsides, roadsides, bushes. Distributed in Liaoning and other places. Dig in spring and autumn to remove sediment and impurities and dry in the sun. North bean root is bitter and cold, has small poison, and has the effects of clearing away heat and detoxification, treating qi and dampness, dispelling wind and relieving pain. It is often used clinically to treat heat, poison, diarrhea, sore throat, rheumatism, arthralgia and other diseases. The content of total alkaloids in bean root is about 1.7% ~ 2.5%, of which bat dauricine is the highest. Its content accounts for about 50% of the total alkaloids and has strong pharmacological activity. Antibacterial effect: It has inhibitory effect on Staphylococcus aureus, Epidermophyton flocculus and Candida albicans. Budzuvine root produced in Northeast China and Japan contains alkaloids such as kudzu root, tetrandrine, dauricine and magnolia root. The leaves contain sinomenine, disinomenine, disinomenine, light steganine, and dehydroxyl dianhexine. Sophorine has a hypotensive effect on anesthetized animals, the pulse wave increases, and the breathing has a short excitement. The principle of its antihypertensive effect is central, and it also has a direct expansion effect on blood vessels (10-6~10-5 concentration can expand isolated rabbit ear blood vessels). In addition, blocking the ganglion (5~10 mg/kg can block the impulse transmission of the cat's superior cervical ganglion) is undoubtedly a cause of blood pressure reduction. Clinically, it is effective for patients with mild hypertension and improves glomerular filtration function, but it is ineffective for severe patients. It can inhibit the contraction of rabbit isolated small intestine and reduce intestinal tension, and has antispasmodic effect. And can reduce blood cholesterol. The toxicity is very small. Dauricine is a quaternary ammonium compound, which has a good muscle relaxation effect, and its properties are the same as those of arrow poison. It can increase the tension of isolated rabbit intestine. Figure 1 is a picture of the plant bat kudzu. |
| analysis method | 1. neutralization method: take about 0.3g of this product, weigh it accurately, add 5 ml of anhydrous ethanol, dissolve it, add 1 drop of methyl red indicator solution, add 25.00 ml of N/10 sulfuric acid solution precisely, and titrate with N/10 sodium hydroxide solution. 2. non-aqueous alkaline measurement method: take about 0.8 mEq of this product, accurately weigh and add 10ml of anhydrous glacial acetic acid, add 5ml of acetic anhydride after dissolution, and 5 drops of crystal violet indicator solution. titrate with N/10 perchloric acid bath until the solution is blue. (The end point is compared with the electrical potential method), and the results are corrected with a blank test. 3. ultraviolet spectrophotometry: take appropriate amount of standard substance, weigh it accurately, and use N/1O hydrochloric acid as solvent to prepare a solution containing 100 μg of standard substance per lml. Accurately measure 1.0, 2.0, 3.0, 4.0 and 5.0ml, place them in 10ml, dilute to scale with N/10 hydrochloric acid, shake well, measure absorbance at 279±1nm wavelength with N/10 hydrochloric acid as blank by spectrophotometry. Draw standard curves with absorbance as longitudinal coordinates and concentration as horizontal coordinates. Take a proper amount of the sample, weigh it accurately, use N/10 hydrochloric acid to make a solution containing about 30 μg of this product per 1ml, use N/10 hydrochloric acid as blank, measure the absorbance at 279±1nm, find out the equivalent concentration from the standard curve, and calculate the content. 4. high performance liquid chromatography: Hypersil ODS2-C18 chromatographic column (4.6mm × 150mm,5 μm), mobile phase buffer (0.68 mL of phosphoric acid and 0.71 mL of triethylamine mixed solution is added with water to 500mL, and the 0.45 μm water microporous filter membrane is passed)-acetonitrile (76: 24 ) , detection wavelength is 281 nm, column temperature is 40 ℃, flow rate is 1.0 mL?min -1, injection volume is 10 μL. The phenolic total alkali (45g) of Dendron dauricum is dissolved in 5 times of CHCl3 solution, 3% NaOH is extracted for 4 times (CHCl3 -NaOH volume ratio is 1: 3), CHCl3 layer is washed with pure water once, 1% HCL is extracted for 3 times (CHCl3 -HCL volume ratio is 1: 3), 3% NaOH is taken from acid water layer to adjust pH9, the precipitate is placed for precipitation, filtered, the precipitate is washed with water to neutral, and dried at room temperature, the crude dauricine was obtained and determined by HPLC with an average mass fraction of 85.08%. |
| method for extracting dauricine from bean root | refer to the warm soaking method. bean root is directly cut off (0.5~1cm) without soaking in water, and acid water percolation is extracted. Take 1kg of the original medicinal material of bean root and soak it with 1% sulfuric acid aqueous solution for 12 h at a percolation rate of 3.5 mL? Min -1 (calculated by percolating 10 times of acid water solution for 24 hours), collecting 16 times of acid water solution, adding 40% sodium hydroxide solution to adjust pH 9 after filtration (stirring evenly at the same time), resting for 24 hours, precipitating precipitate, discarding supernatant, precipitating to near-dry precipitate, washing to pH 7-8, naturally drying the precipitate to obtain total phenolic alkaloids of baguris, and the content is determined by HPLC, the total alkali mass fraction is 73.63% ~ 80.72%. the phenolic total alkali of kudzu is dissolved in CHCl3 solution, 0. 5% NaOH is extracted 4 times, the residual alkali of CHCl3 layer is washed with purified water, the CHCl3 layer is extracted 3 times with 1% HCL, the acid water layer is collected, the pH is adjusted by 0.5% NaOH, the precipitate is precipitated, filtered, and dried at room temperature to obtain kudzu alkali. |
| pharmacological activity | the pharmacological effect of dauricine is similar to that of quinidine, which has the effects of reducing myocardial contractility, inhibiting self-discipline, prolonging functional refractory period, reducing excitability, reducing right heart frequency, reducing the amplitude and rate of zero phase rise of action potential, prolonging the time course of action potential, and anti-choline acetate shortening the time course of atrial muscle action potential. This product has no selective effect on the transmembrane ion transport of myocardial cells, but has the dual effect of anti-calcium and sodium resistance. |
| pharmacological action | 1. bacteriostatic effect: it has been confirmed by in vitro bacteriostatic test that total dauricula, dauricula and dauricula have bacteriostatic effects on various respiratory and intestinal bacteria. Among them, dauricine has the strongest antibacterial effect, and the antibacterial rate is as high as 83.33%. Dauricine has the most obvious inhibitory effect on pneumococcus. 2. antiarrhythmic effect: dauricine can inhibit arrhythmia caused by early and later depolarization. Related tests have also confirmed that dauricine is effective for a variety of experimental arrhythmias. 3. Protective effect on myocardial ischemia: bat daurine, as the main active component of bat dauricum, can effectively improve myocardial metabolism and coronary circulation blood flow, and play a protective role on myocardial ischemia. 4. Protective effect on cerebral ischemia: dauricine can inhibit the formation of thrombus and the release of platelet activating factor, thus inhibiting the formation of arterial thrombus. It can improve cerebral ischemia, reduce the scope of cerebral infarction of cerebral ischemia, and further improve neuromotor function. Dauricine can promote the expression of Bcl-2 protein in rat brain tissue, inhibit the expression of Bax protein, increase the ratio of Bcl-2/Bax, reduce the apoptosis of body neurons, and protect brain tissue from cerebral ischemia and ischemia reperfusion injury. 5. Anti-tumor effect: dauricine has inhibitory effect on various tumor cells. Dauricine can effectively inhibit human promyelocytic leukemia and human erythroleukemia cell lines. Dauricine has cytotoxic effect on nasopharyngeal carcinoma cell lines and can effectively inhibit highly differentiated nasopharyngeal carcinoma cells. Dauricine has significant inhibitory effect on lung cancer cell line QG-56 cultured in vitro, has significant anti-tumor effect, induces apoptosis of tumor cells, and plays a role in protecting body tissue cells. 6. antihypertensive effect: using a syringe to inject epinephrine from the femoral vein, it is pointed out that in a very short period of time, different dose groups of dauricine have a significant antihypertensive effect on rats, lasting more than 1h, and pointed out that with the increase of dauricine dose, the better the antihypertensive effect. |
| toxicology | mice oral LD50 of this product is 1180±130 mg/kg, safety index is 8.6, far safer than quinidine 4.6. Subacute toxicity test shows that rats drink this product slowly for a long time, although the dose is large, there is no obvious toxicity, and there is no change in the heart, liver, kidney and other organs and tissues. Special toxicological tests showed no mutagenic, teratogenic and carcinogenic effects of this product. MTT assay was used to detect the activity of dauricine on liver cells and kidney cells and to observe the cell morphology. The results showed that after administration, liver and kidney cells shrank, decreased and died to varying degrees, and the number of cells with poor state increased significantly with the increase of drug concentration. |
| metabolism | this product is absorbed from the gastrointestinal tract after oral administration, and is widely distributed in various organs of the body. it reaches the highest concentration in the heart, liver, lung, kidney and brain at 1-2h, while the plasma concentration is lower. It is excreted in the body through feces and urine. The pharmacokinetics of dauricine injected intravenously in rats is a two-compartment open model, which conforms to the first-order kinetic linear elimination process. After intragastric administration, the blood drug concentration of rats was low, and the peak concentration was less than lrng?L-1, and the blood drug concentration-time curve showed obvious bimodal phenomenon. Its absolute bioavailability is about 16.6%. After two routes of administration, the drug is distributed in all tissues and organs, and the content of each tissue is significantly higher than that of blood drug concentration at the same time. The content of lung tissue was the highest after intravenous injection, while the content of stomach, intestine and liver was the highest after intragastric administration. Urine and feces accumulated and excreted 31.22% at 48h. The results of the study of the residual amount of drugs in various segments of the gastrointestinal tract at different time points after administration suggest the existence of gastrointestinal circulation. |
| adverse reactions | after taking this product, the general reactions include loss of appetite and lethargy. a few patients have abdominal distension, abdominal pain, increased stool frequency, and some have constipation. |
| precautions | (l) be used with caution for patients with high years, serious illness and myocardial damage;(2) regularly check liver function during medication, and this product is not suitable for patients with original liver diseases. |
| storage method | sealed and stored in a dark place. |
| use | used for content determination/identification/pharmacological experiments, etc. Pharmacological effects: reduce autonomy and myocardial excitability, and can slow down heart rate and inhibit myocardial contractility. It has the characteristics of fast onset and slow recovery. It is absorbed by the gastrointestinal tract, reaches the peak blood concentration for 1-2h, and is excreted through feces and urine. This product is a broad-spectrum antiarrhythmic drug, suitable for tachyarrhythmias, especially for atrial, borderline and ventricular premature beats; for pre-excitation syndrome with ventricular tachycardia The effect is good; but the effect on atrial flutter and atrial fibrillation is poor. |
Last Update：2024-04-09 20:52:54
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