77 results about "Leonurine" patented technology

A leonurin salt is soluble salt which is prepared by reaction of leonurin on the acidic salt of inorganic, organic, or polybasic acid. It can be used to prepare tablet, capsule, softgel, particle, oral liquid, injection, syrup, etc.

A process for synthesizing the leonurine from syringic acid as initial raw material includes such steps as carbonylation reaction, acylchlorination reaction, esterification reaction, ammonification reaction to obtain leonuriamine, and reacting with methylisothiourea. Its advantages are simple operation, easy control, high output rate, and high purity (99.8%).

A process for extracting leonurine from fresh motherwort includes such steps as extracting juice, depositing in alcohol, filtering, column exchanging, eluting, concentrating and drying. Said leonurine can be made into capsule, tablet, or injection for treating gynopathy with hige curative effect.

The invention belongs to the field of pharmacy, and relates to applications of leonurine in preparation of medicines used for treating atherosclerosis. Leonurine possesses a structure represented by formula (I). It is shown by results of experiments on a rabbit model with high fat diet induced atherosclerosis that, leonurine possesses anti-inflammatory activity and antioxidant activity, so that leonurine is capable of increasing the content of high-density lipoprotein, reducing the content of total cholesterol, reducing mean blood flow velocity of arteries, improving blood flowing states, protecting the integrity of blood vessel endothelium, and reducing deposition of lipid in blood vessels and generation of macrophage, and can be used for treating atherosclerosis.

The invention belongs to the field of traditional Chinese medicine manufacturing, and relates to application of leonurine to preparation of a medicament for treating 2-type diabetes. Animal experiments prove that the fasting blood glucose of a 2-type diabetes mouse, i.e., a db/db mouse, can be lowered by the leonurine, and the tolerance of oral glucose is improved; and meanwhile, fasting plasma insulin is increased, the plasma triglyceride is reduced and the content of the plasma high-density lipoprotein is increased. Experiment results also show that the expression of liver glucose metabolic enzymes such as glucokinase, glucose-6-phosphatase and phosphoenolpyruvate carboxyl enzyme is adjusted by the leonurine in an Akt dependent mode; and the biological response of an inflammatory mediator, such as generation of TNF (Tumor Necrosis Factor)-alpha, degradation of IkB-alpha and subsequent phosphorylation of NF-kBp65, is suppressed. Through the leonurine, the inflammatory state of the 2-type diabetes can be corrected, and the symptoms of the 2-type diabetes can be improved; and the leonurine can be used as a treatment medicament to be applied to the treatment of the 2-type diabetes.

The invention relates to medicinal use of leonurine for menopause disease, and in particular provides the medicinal use of the leonurine or pharmaceutical salts thereof for preventing or treating menopause syndrome and menopause syndrome related diseases.

The invention belongs to the field of medicinal chemistry, and relates to a synthesizing method of leonurine and aspirin conjugate. The method comprises the steps that syringic acid, S-methylisothiourea and aspirin serve as starting materials, reactions of acetylation, BOC protection, amidation, deacetylation and the like are conducted, and corresponding structure segments are obtained; dilauryl hydrogen phosphite, 4-dimethylaminopyridine and 4-toluenesulfonic acid are used together to serve as a condensation catalyst to connect the three segments, de-BOC protection is conducted on trifluoroacetic acid, and a target compound is obtained. The synthesizing method of the leonurine and aspirin conjugate is easy and convenient to operate, mild in condition, simple in post treatment and capable of increasing the yield of the intermediate leonurine product; the total yield of the prepared leonurine and aspirin conjugate is 25.27%, a pharmacological activity test is conducted, it is shown through the result that very good antioxidant and anti-apoptosis effects at a cellular level are achieved, and the effect on protecting myocardial cells is exact.

The invention belongs to the traditional Chinese medicine pharmacy field, and relates to an application of leonurine SCM198 in preparation of medicines used for preventing and treating parkinson disease. According to the invention, neurotoxin 6-OHDA induces damage of nerve cells in rats, the result shows that leonurine SCM198 is capable of improving behavior changes of PD model rats, increasing the survival rate of damaged nerve cells, raising antioxidant enzyme superoxide dismutase activity, minimizing excessive generation of active oxygen species, stabilizing mitochondrial membrane potential, minimizing apoptotic cells and regulating the change level of Bax and Bcl2 gene and protein. The result proves that the leonurine SCM198 has protection effect on a PD model, and can be used for preparing medicines for preventing and treating PD.

The invention discloses alkaloid fuming particles for low-temperature heating non-combustible products. The alkaloid fuming particles comprise the following components in parts by weight: 0.1-15 partsof alkaloid, 30-60 parts of Chinese herbal medicines and 10-30 parts of a smoke agent, wherein the alkaloid is any one of cytisine, leonurine, sophocarpidine, notoginsenoside and lobeline. The invention also discloses a preparation method of the alkaloid fuming particles. According to the invention, the fuming particles adopt alkaloid and natural Chinese herbal medicine formulas and can replace nicotine-containing tobacco, so that addiction and health hazards are reduced, and meanwhile, the effects of refreshing, decompressing and medicine health care are achieved.

The invention relates to the technical field of organic chemistry, in particular to a synthetic method for leonurine. Gamma-butyrolactone is used as a starting material to be subjected to ammonolysis to obtain gamma-hydroxybutyric acid amide; the gamma-hydroxybutyric acid amide and acetyl syringic acid are subjected to a condensation reaction; a dehydration reaction and a reduction reaction are carried out to obtain leonurus amine; and the leonurus amine and S-methyl isothiourea sulfate are subjected to a reaction to obtain the leonurine. The target product leonurine is synthetized from the cheap industrial raw materials of the gamma-butyrolactone and the syringic acid used as the starting materials through reactions of ammonolysis, esterification, dehydration, reduction and the like. The reaction conditions are mild and easy to control; the yield is up to 65%; the product purity is 98% or above; and the synthetic method for leonutine provides the production with an excellent synthetic route and is suitable for large-scale production.

The invention discloses a Chinese herbal preparation for treating uterine bleeding after drug abortion, which is made from following raw materials in weight proportion: 2 to 6 parts of astragalus root, 1.5 to 4 parts of agrimony, 0.9 to 2 parts of Chinese angelica, 2 to 4 parts of leonurine, 0.3 to 0.9 part of powdered notoginseng root, 1.5 to 3 parts of portulaca, 1 to 3 parts of redroot gromwell root, 0.8 to 2 parts of aspidium, 0.6 to 2 parts of bitter orange and 0.6 to 2 parts of dried rehmannia root. The invention integrates the functions of Qi supporting and blood enriching, muscle regeneration and hemostasis and heat clearing and blood cooling and cures uterine bleeding after drug abortion with safety, reliability and without pain and can obviously increase complete abortion rate and reduce bleeding quantity of the uterine to shorten bleeding time and avoid twice curettage.

The invention discloses a method for synthesizing leonurine. The method is characterized in that raw material 2,3-dihydrofuran undergoes the alkoxy oxime synthesis reaction, obtained product 4-hydroxyl butyl-O-methyl oxime and carbalkoxy syringic acid undergo the esterification and oxime reduction reaction to obtain herba leonuri amine, and the herba leonuri amine reacts with S-methylisothiourea to obtain leonurine. The reaction process atom economy is good, the excessive use of a reagent is avoided, the environmental pollution is reduced, and the method is high in yield and easy to operate.

The invention provides a leonurine derivative and application of the leonurine derivative in preparation of a medicine for preventing or treating ischemic cerebrovascular diseases. The leonurine derivative has a structure as shown in a general formula (I), wherein X is selected from O or NH; Y is selected from any one of natural amino acid, substituted amino acid or amino alcohol; Z is selected from H, proline and any substituted proline. Pharmacological experiments prove that the leonurine derivative provided by the invention has the effects of neuroprotection, cerebral infarction area reduction and animal neurobehavioral scoring, and is good in safety, so that the leonurine derivative has important significance for developing novel medicines for preventing or treating ischemic cerebrovascular diseases.

The invention discloses a leonurine derivative as well as a preparation method and application thereof. In a compound and pharmaceutically acceptable salt or prodrug thereof as shown in a formula (I),R1, R2 and R3 are the same or different and are independently selected from hydrogen, C1-C10 linear chain or branched alkyl carbonyl or C1-C10 linear chain or branched alkoxyl carbonyl. Relative to the leonurine in the prior art, the leonurine derivative as shown in the formula (I) has the following advantages: the bioavailability of the leonurine derivative in the animal body is greatly improved; furthermore, the leonurine derivative in blood is hydrolyzed into leonurine rapidly, and the condition of low exposed quantity caused by the fact that the leonurine is absorbed insufficiently in theliving body is improved. (The formula is as shown in the description).

The invention discloses a beta crystal form of leonurine hydrochloride as well as a preparation method and application of the beta crystal form. Stronger diffraction peaks displayed in a powder X-raydiffraction pattern expressed by diffraction angles 2theta are 11.630 (54 percent), 11.990 (21 percent), 14.420 (18 percent), 22.430 (21 percent), 23.330 (19 percent), 24.710 (16 percent) and 25.670 (100 percent). The beta crystal form of the leonurine hydrochloride, which is prepared with the preparation method disclosed by the invention, has the characteristic of high stability, can keep stableunder conditions of high illumination, high temperature, high humidity and long-time storage, and can be used for preparing a drug composition.

The invention provides an extracting method of a green tea extracting solution. The extracting method comprises the steps that fresh green tea is taken, cleaned and triturated, water 10 times by weight of the tea is added, soaking is performed for 0.5 hour, decoction is performed for 1 hour, filtering is performed, water 8 times by weight of medicinal materials is added to decoction dregs, decoction is performed for 1 hour, medicinal liquid is filtered out, two times of decoction liquid are mixed, concentration is performed to obtain 60 DEG C liquid with the relative density of 1.05, ethanol is added to make the volume percentage of alcohol content up to 75%, stirring, standing and filtration are performed, filtrate is concentrated to obtain 65 DEG C liquid with the relative density of 1.25, the ethanol is recovered to obtain concentrate, the green tea extracting solution is obtained through microwave extraction, the tea polyphenol content is high, and the green tea extracting solution is compatible with leonurine and forsythin to make a tea beverage.

The invention belongs to the field of pharmacy, relates to application of leonurine to preparation of a medicine for treating dementia and in particular relates to application of the leonurine to preparation of a medicine for treating vascular dementia. A rat VD model is successfully copied and an experiment result shows that the leonurine can remarkably improve cognitive impairment caused by the VD and alleviate impairment of long-term postsynaptic inhibition; the content of hydrogen peroxide (H2O2) and glutamate is reduced, the specific value of NR2A/2B is improved and the expression of LC3II/LC3I and Beclin-1 is regulated down, so that autophagic flux is inhibited. The leonurine can be used as a treatment medicine for treating the dementia, especially brain injury diseases caused by the VD.

The invention belongs to the technical field of medicine detection and relates to a method for quantitatively detecting the content of leonurine in blood plasma. The method is characterized by adopting the high performance liquid chromatography-mass spectrometry technology, using benzoyl arginine ethyl ester as an internal standard of a detected substance, using a method of precipitating the proteins with perchloric acid to pretreat the blood plasma sample and calculating the blood concentration of leonurine in the blood plasma by using the peak area according to an internal standard method, wherein liquid chromatography adopts Agilent ZorbaxSB-C18 column as the stationary phase, the acetonitrile/ammonium acetate buffer solution mixed solution is used as the mobile phase and gradient elution is carried out; mass spectrometry adopts an electrospray ionization source; leonurine is quantified by adopting multiple reaction monitoring; and the lowest limit of quantification of leonurine in the method reaches 4ng/mL. The method has the following beneficial effects: the method has strong sample detection specificity and high sensitivity and is simple and convenient to operate; all the textual research indexes of methodology can meet relevant technical requirements of Chinese pharmacopoeia; and the method can be used for pharmacokinetics research after oral administration of leonurine.

The invention belongs to the field of medicine synthesis, and particularly relates to a leonurine main metabolite and a preparation method thereof. The main metabolite which has a structure shown in the formula (I) (please see the formula in the description) and combines leonurine with glucuronic acid is synthesized by taking glucuronic acid lactone, 4-aminobutanol and syringic acid as starting raw materials through multi steps of reactions. The prepared leonurine main metabolite compound which has the novel chemical structure and combines leonurine with glucuronic acid has a good pharmacological activity prospect and can be used for further pharmacological activity evaluation. The method has the advantages that the synthetic route is simple, control is easy, the raw materials are cheap and easy to obtain, and the product stability is good.

The invention discloses a virus immunized inducer and application thereof, and belongs to the technical field of plant virus immunized induction. The inducer is prepared by the following steps: uniformly mixing the following components in percentage by weight: 32 percent of astragalus polysaccharide, 26 percent of chlorogenic acid, 26 percent of total tanshinones and 16 percent of leonurine; and adding 8.5 percent of the mixture in a root medium for strawberry virus-free seedling tissue culture. The immunized inducer has the advantages of effectively improving the resistance of strawberry virus-free seedlings on viruses, has excellent immunity on strawberry mottle virus, crinkle virus and vein banding virus in the natural planting process, and has minor immunity on strawberry mild yellow edge virus.

The invention discloses a leonurine hydrochloride tablet and a preparation method thereof, and belongs to the technical field of medicines. The tablet prepared by the invention mainly comprises the following components in parts by weight: 500 mg of leonurine hydrochloride, 8750 mg of a filler, 500 mg of a disintegrating agent, 200 mg of an adhesive and 50 mg of a lubricant. In the preparation process, the leonurine hydrochloride, the filling agent and the disintegrating agent are firstly mixed, then the adhesive aqueous solution is added to prepare a soft material, then granulation is performed, and finally tabletting and coating are performed on the soft material, the lubricant and the adhesive dry powder. The preparation process comprises the steps of mixing of raw materials and auxiliary materials, wet granulation, drying, size stabilization, total mixing and tabletting. The leonurine hydrochloride raw material medicine is prepared into tablets for the first time; organic solvents such as ethanol are not used in the preparation method, so that organic solvent residues are avoided; the dissolution rates of the leonurine hydrochloride tablets prepared by the invention in water dissolution media with the pH values of 1.2, 4.5 and 6.8 respectively reach about 85% within 30 minutes. The preparation process is cheap and easily available in raw materials, stable in quality and suitable for large-scale industrial production.

The invention belongs to the field of modern pharmacy of traditional Chinese medicines, and relates to application of a specific monomer leonurine in preparation of a medicine for improving infertility pregnancy outcome. The leonurine is injected into the abdominal cavity during an EMS (acute renal syndrome) modeling period, so that the volume and weight of an ectopic focus can be remarkably reduced, local fibrosis, invasion and transfer are inhibited, and the pregnancy rate of an EMS model mouse can be remarkably increased. The leonurine inhibits proliferation and invasion of endometrium stromal cells by inducing apoptosis of the endometrium stromal cells, adjusts expression balance of a local estrogen-progestin receptor of the ectopic focus, activates EMS model pelvic and abdominal immune cells, enhances phagocytic and killing functions of the cells, reverses poor ecdysis of the EMS model mouse, has similar effects on growth and invasion of ectopic focus ESC of a human EMS patient and expression of the estrogen-progestin receptor, does not affect growth and activity of the endometrium ESC of a normal child-bearing female, hormone receptor expression, ecdysis process and proliferation, apoptosis and cell activity of human early-pregnancy embryo trophoblast, and can be used for preparing an effective prevention and treatment medicine for EMS combined infertility patients.

The invention discloses pressure reduction medicinal granules and a preparation method thereof. The pressure reduction medicinal granules comprise herba taxilli, concha haliotidis, radix puerariae lobatae, flos chrysanthemi indici, spica prunellae, carrots, folium nelumbinis, water chestnut, broadbean flower, cortex eucommiae, scutellariae radix and herba leonuri. The pressure reduction medicinalgranules have the beneficial effects that leonurine is added to improve the urine volume discharging of the human body so as to perform a function of pressure reduction, and in addition, the pressurereduction medicinal granules can tonify spleen, clear dampness, calm the liver, lighten complications caused by high blood pressure and regulate the mechanism of the human body. In a formula, a traditional Chinese medicine formula is adopted, side effects are avoided, relapse is reduced, and in addition, the pressure reduction medicinal granules have a good taste and are suitable to be widely popularized.