53 results about "Antithrombin Activity" patented technology

The invention discloses a Fuc3S4S substituted oligo-glycosaminoglycan with the weight-average molecular weight of about 4.5-9kD, a medicine composition containing the Fuc3S4S substituted oligo-glycosaminoglycan, preparation methods thereof and an application thereof in preparing medicines for preventing or treating thrombotic diseases. The oligo-glycosaminoglycan has a structure shown as the formula (I); in the formula (I), a substituent group is defined as the specification. The Fuc3S4S substituted oligo-glycosaminoglycan and the medicine composition thereof have strong-effect factor X enzyme inhibition activity and HC-II depended antithrombase activity, and can be used for preparing antithrombus medicines.

The invention discloses a reagent for detecting antithrombin activity, including reagent 1 and reagent 2, wherein: reagent 1 is a chromogenic substrate of FXa, and reagent 2 is a diluent containing FXa and heparin; wherein the chromogenic substrate of FXa is selected from From the following: CH 3 SO 2 ‑D‑Leu‑Gly‑Arg‑p‑nitroanilide·AcOH; CH 3 OCO‑D‑CHG‑Gly‑Arg‑p‑nitroanilide·AcOH; CH 3 OCO‑D‑CHA‑Gly‑Arg‑p‑nitroanilide AcOH; Benzoyl‑Ile‑Glu‑Gly‑Arg‑p‑nitroanilide HCl; Suc‑Ile‑Glu(γ‑Piperidyl)‑Gly‑Arg‑p‑nitroanilide HCl; N-α-Z-D-Arg-Gly-Arg-p-nitroanilide 2HCl; Boc-D-Arg-Gly-Arg-p-nitroanilide 2HCl; Acetyl-D-Arg-Gly-Arg-p ‑nitroanilide·2HCl; 4‑Nz‑D‑Arg‑Gly‑Arg‑p‑nitroanilide·2HCl; 4‑Mbs‑D‑Arg‑Gly‑Arg‑p‑nitroanilide·2HCl. The invention has good detection stability and repeatability, high sensitivity and accuracy, can accurately reflect the activity of antithrombin, and can find patients with abnormal antithrombin activity in the body, thereby providing a basis for treatment.

The invention discloses a leech culture method and belongs to the technical field of aquaculture. The method specifically comprises the following steps: (1) building an aquaculture cage; (2) arranging a culture pond; (3) putting in young leeches; (4) performing feeding management; and (5) performing water quality management. According to the method disclosed by the invention, the yield and quality of leeches can be effectively improved, the yield can be improved by about 30%, the activity of antithrombin in the leeches is well enhanced, and the application value is high.

The invention relates to a method for extracting hirudin by stimulating a living leech with electricity. By utilizing the simulating effect of current on organism glands, a way for simulating a living leech to extract high-purity hirudin at mass by direct weak current is directly used, and the living character of the leech is maintained, therefore, the production process of hirudin is simplified,the product purity is improved, the wild leech resources are recycled, the production cost is reduced and the problem of seasonal disorder of production is solved. The hirudin extracted by using the method is subjected to nanofiltration water removal and decompression spray drying to be made into powdery hirudin with the antithrombin activity of 800AT-U / g and liquid hirudin with the antithrombin activity of 1,000AT-U / g when protective agents are added in the liquid hirudin.

The invention discloses a breeding method for fast increasing the activity of antithrombase of leeches. The breeding method comprises the following steps of 1 young leech collection, 2 weight-increasing breeding, 3 temperature control and feed deprivation and 4 harvesting. The breeding method for fast increasing the activity of the antithrombase of the leeches is short in breeding period, the activity of the antithrombase with unit mass of the leeches can be fast improved in the short term, the activity of the antithrombase with unit mass of the leeches can be improved by 35.28% to 116.61% within one month, the medicinal value of the leeches is effectively improved, the temporary keeping time is shortened, production management cost is reduced, breeding risks are reduced, and therefore the economic benefits of breeding can be increased.

The invention provides a hirulog as well as a preparation method and application thereof and belongs to the field of polypeptides and preparation methods thereof. A metabolic product of a recombined hirulog provided by the invention in urine of a rat has stronger antithrombin activity, which is found in the process that the recombined hirulog metabolizes in the body of the rat. Through extraction, separation and structural evaluation, the metabolic product is found to be a hirulog which is formed by retaining the N ends of a group of recombined hirulogs and removing 17-12 amino acids on the C ends of the group of recombined hirulogs, namely a hirulog rH1-51, a hirulog rH1-52 and a mixture of the hirulog rH1-51 and the hirulog rH1-52. The preparation method mainly comprises the following steps of: carrying out intravenous administration on the rat, collecting urine, extracting and purifying by using a gel filtration high performance liquid chromatography (GF-HPLC) and combining a reverse phase high performance liquid chromatography (RP-HPLC) to obtain the hirulog. The immunogenicity of the hirulog provided by the invention is remarkably reduced, and therefore, the hirulog is expected to become a new-generation antithrombus drug and is favorable in development prospect and high in clinical application value.

The invention relates to a process for preparing high activity thrombin inhibitors, which comprises subjecting hirudin, the natural specific inhibitor of thrombin to DNA family restructuring, carrying out restructuring to hirudin HV1, HV2, HV3 genes, constructing reorganization library for hirudin bacteriophage display, using thrombin as coating antigen, subjecting bacteriophage reorganization library to three rounds of enriched elutriation including adsorption, elution and expansion, obtaining a plurality of bacteriophage monoclons with high affinity with thrombin through ELISA screening, carrying out pronucleus induced expression to these clones, finally detecting the antithrombogenic activity of the purification expression product.

The invention discloses a preparation method of an enteric coated tablet with leech as a raw material, belonging to the technical field of traditional Chinese medicine. In the invention, research is carried out on the freezing temperature, the number of days of freezing, a mashing process, a low-temperature drying process and a sterilizing process, and the antithrombin activity is used an indicator to optimize a new process method. The process method is organic combination of different process parameters, i.e. the process method avoids high mechanical force and high temperature to achieve the effect of maintaining the activity of leech. By the process method provided by the invention, the enteric coated tablet prepared by using complete fresh live leech as medicine has higher antithrombin activity.

The invention pertains to the field of medical technology, relating to an oxazine compound and a medical application thereof; the oxazine compound and an oxazine salt obtained from an addition reaction of pharmaceutically-applicable oxazine acid can be used as a platelet aggregation inhibitor; the oxazine compound has a structural formula shown as above; in a structural formula I and a structural formula II, X can be independently chosen from CH2 and C=0, R1 can be independently chosen from H and a substituted or un-substituted aromatic base, R2 can be independently chosen from H or a substituted or un-substituted aromatic base, and R3 can be independently chosen from H, alkyl group with one to four carbon atoms, benzyl or substituted or un-substituted aromatic base. The oxazine compound has simple synthetic method, adapts to industrialized production and is more stable when compared with natural analogues. Shown by biological activity assay, the oxazine compound has the functions of analgesia, anti-inflammatory and antithrombin activity and is a platelet aggregation inhibiting medicament.

The invention belongs to the technical field of traditional Chinese medicines, and discloses a method for preparing enteric capsules by taking leech as a raw material. A novel process method is selected preferably by study on freezing temperature, number of freezing days, a crushing process, a low-temperature drying process and a sterilizing process to research and by taking antithrombin activity as an index. The process method organically combines different process parameters, namely, the process method avoids high mechanical force and high temperature as much as possible to achieve the effect of keeping the activity of the leech. The enteric capsules in which the fresh leech is used as a medicament wholly and which is prepared by using the process method have higher antithrombin activity.

The invention discloses a maixuekang capsule detection method. A maixuekang capsule is obtained through filling crushed fresh leech to a capsule. The detection method comprises methods for determining the contents of amino acids and polysaccharides in the maixuekang capsule, and makes up the single antithrombase activity determination and content determination methods in the prior art. The detection method has the advantages of accuracy, high sensitivity, good repeatability, and effective control of the quality of the maixuekang capsule.

The invention discloses a method for increasing hirudin extraction yield. The method includes: supplementary feeding 12-54 hours before fishing; or fishing 12-54 hours after normal feeding; extracting live leeches to a storage tank under room temperature, rinsing with deionized water, filtering water, immersing into normal saline for rising, adding electrolyte for covering, applying direct currents for stimulation, collecting liquid secreted by the leeches, and returning the live leeches to a cultivation tank from a filtering tank; performing 800-micrometer nano-filtration film subsequent processing on the collected secretion to remove part of moisture, adding stabilizer, and performing spraying drying to obtain antithrombase-active hirudin dry powder. The method has the advantages that leech feeding time is changed to improve the hirudin contents in the leeches, electricity is used to stimulate the live leeches so as to extract the hirudin, the production process of the hirudin is simplified, the live leeches can be kept, and high-purity hirudin can be extracted for many times.

The invention pertains to the field of medical technology and relates to a furo [2, 3-h] chromene compound and an application thereof for inhibiting platelet aggregation; the furo [2, 3-h] chromene compound, pharmaceutically-acceptable salt, or stereo-isomers and pre-drugs of the furo [2, 3-h] chromene compound, as well as pharmaceutical compatibility acceptable carriers or diluents of the furo [2, 3-h] chromene compound can be used as platelet aggregation inhibitors. The structural formula of the furo [2, 3-h] chromene compound is as shown above, wherein, X can be chosen from CH2 or C=O, R1 can be independently chosen from H or a substituted or un-substituted aromatic base, R2 can be independently chosen from H or a substituted or un-substituted aromatic base, and R can be independently chosen from H, alkyl group with one to four carbon atoms, chlorine, bromine, fluorin, methoxyl, nitryl or hydroxyl. The furo [2, 3-h] chromene compound has simple synthetic method, adapts to industrialized production and is more stable compared with natural analogues. Shown by biological activity assay, the furo [2, 3-h] chromene compound has antithrombin activity and is a platelet aggregation inhibiting drug.

The present invention provides compositions and methods for preventing blood-sucking infection in livestock, isolated protein with antithrombin activity and nucleotide sequence encoding the protein. A protein named thrombostatin was isolated from the salivary gland of horn fly western horn fly. The composition can be used as a veterinary vaccine to prevent infective horn flies from sucking blood on domestic animals. The proteins of the invention are also useful in the treatment of thrombosis.

The invention provides an antithrombin activity assay method of an injection for promoting blood circulation to remove blood stasis. The antithrombin activity assay method is characterized in that a ceramic whiteware spot plate is taken as a reaction carrier; thrombin titration interval time, thrombin concentration and stirring frequency of a tool pin are controlled to ensure that the determination results are stable. The antithrombin activity assay method provides a biological quality control method for the injection for promoting blood circulation to remove blood stasis, and facilitates evaluation to reliability and controllability of the quality.

The invention belongs to the field of biotechnology and relates to DTI (Direct thrombin inhibitor) peptides and the application thereof. According to the invention, the molecule of RGD-Hirudin is truncated on the basis of the structure of the RGD-Hirudin, so as to obtain micro-molecule DTI Peptide 1 and micro-molecule DTI Peptide 2. A test and an animal experiment show that the Peptide 1 and the Peptide 2 are DTIs, have antithrombin activity, have definite action target points, have no impact on other blood coagulation factors, can be further used for preparing oral anticoagulant drugs or subcutaneous sustained-release anticoagulant drugs, and particularly suitable for thrombotic disease prevention. The DTI peptides can be taken as candidate drugs for DTIs to be studied intensively, and lay the foundation for developing novel DTIs.

The present invention relates to preparation process of leech medicine granule. The preparation process includes preparing scalded leech piece, decoction, filtering, decompression concentrating the filtrate to obtain extractum, spray drying to obtain powder, mixing with magnesium stearate and one of dextrin, lactose and maltodextrin in certain weight proportion, and pelletizing with roller to form 18-40 mesh granule. The leech medicine granule contains amino nitrogen not less than 10 mg / g, active antitrombase not less than 16.0 U / g and sarkin not less than 2 mg / g.

The invention discloses a test box for rapidly detecting the activity of antithrombin of leeches. The test box comprises a 0.9 percent sodium chloride solution, a trihydroxymethyl aminomethane hydrochloric acid buffering solution containing 0.5 percent fibrinogen and a prepared thrombin solution. The invention further discloses a detection method for rapidly detecting the activity of the antithrombin of the leeches; the detection method comprises the following steps: 1) weighing and chopping the leaches and putting the leaches into the sodium chloride solution; 2) extracting and centrifuging;3) adding the trihydroxymethyl aminomethane hydrochloric acid buffering solution; 4) dropwise adding the prepared thrombin solution; 5) calculating; 6) calibrating according to environment temperature. The test box and the detection method can be used for rapidly detecting the activity of the antithrombin in the leeches, have the advantages of accurate detection result, low equipment requirementsand rapid detection, and can be suitable for outdoor on-site operation.

The invention relates to a preparation method of a clinical detection reagent and in particular relates to a preparation method of an antithrombase III activity determination kit. The preparation method of the antithrombase III activity determination kit comprises the following steps: dissolving lyophilized antithrombase powder and sodium heparin with Tris-HCl to form an S1 reagent, dissolving antithrombase chromogenic substrate S-2238 or Sar-Pro-Arg-P-nitroanilide with Tris-HCl to form an S2 reagent, lyophilizing the reagents S1 and S2 to form an S1 lyophilized product and an S2 lyophilized product; redissolving the S1 lyophilized product with Tris-HCl containing sodium azide solution to form an S1 lyophilized and redissolved reagent; dissolving the S2 lyophilized product with ultrapure water to form an S2 lyophilized and redissolved reagent; lyophilizing multi-person mixed plasma to prepare an ATIII calibrator; valuing the ATIII calibrator in the range of 90-110%; drawing a standard curve by adopting the valued ATIII calibrator, the S1 hyophilized and redissolved reagent and the S2 hyophilized and redissolved reagent, wherein linear correlation coefficient is larger than 0.99; and adding the S1 hyophilized and redissolved reagent and the S2 hyophilized and redissolved reagent into a to-be-detected plasma sample, and carrying out chromogenic reaction. The antithrombase III activity determination kit obtained by adopting the preparation method provided by the invention is low in cost, wide in linear range, good in stability and easy to use.

The invention pertains to the filed of medical technology, relating to an oxazine compound and a medical application thereof; the oxazine compound and an oxazine salt obtained from an addition reaction of pharmaceutically-applicable oxazine acid can be used as a platelet aggregation inhibitor with a structural formula shown as follow; in structural formulas I-VI, R3 can be independently chosen from H, alkyl group with one to four carbon atoms, benzyl or substituted or un-substituted aromatic base. The oxazine compound has simple synthetic method, adapts to industrialized production and is more stable when compared with natural analogues. Shown by biological activity assay, the oxazine compound has the functions of analgesia, anti-inflammatory and antithrombin activity and is a platelet aggregation inhibiting medicament.

The invention discloses a making method of rice-processed leech, comprising soaking, segmenting and stir frying and characterized in that the soaking step is rice milk soaking, including: crushing glutinous rice and polished round-grained rice into powder, adding drinking water, boiling, cooling, and soaking leech; the stir frying step includes: stirring the soaked leech with glutinous rice and polished round-grained rice, and removing the two types of rice. The leech making method is modified; viscous fluid on the surface of leech is effectively removed; fishy smell of the leech is significantly relieved; stimulation to human stomach and intestine is significantly relieved; antithrombin activity of leech is improved.

It is an object of the present invention to provide a therapeutically effective agent for therapy and / or improvement of DIC, or a method for treating and / or improving DIC. The present invention provides an agent for therapy and / or improvement of disseminated intravascular coagulation comprising thrombomodulin as an active ingredient, which is administered to antithrombin-reduced patients having a low plasma antithrombin activity of less than 50%.

The invention discloses a preparation method of an active extract gel product taking Hirudinaria Manillensis freeze-dried powder as a raw material. The method includes cleaning all fresh living Hirudinaria Manillensis, homogenizing, and freeze-drying to obtain freeze-dried powder; adding appropriate amount of pure water into the freeze-dried powder, stirring for extraction, filtering, collecting a filtrate, adding appropriate amount of pure water into residues, stirring for extraction, filtering, collecting the filtrate, and mixing the filtrate; adding appropriate amount of anhydrous ethanol into the filtrate, centrifuging, and collecting a supernatant as an active extractive solution for later use; and preparing carbopol gel matrix, adding sodium hydroxide to adjust pH value, slowly adding the active extractive solution into the prepared gel matrix, and stirring to obtain 20-40 antithrombin active units / g gel. The freeze-dried powder extract of Hirudinaria manillensis has very high activity, so that the extract can be made into cosmetics with high activity to ensure good effect; in addition, the extract is configured into cosmetics with different active units; and the gel product is convenient to manufacture, use and carry, and can further be applied locally and on the whole face as required.

The invention provides a method for determining the antithrombin activity of a Shuxuetong injection. The method is characterized in that a white porcelain spot plate is adopted as a reaction carrier, and the thrombin titration interval time, thrombin concentration and the stirring frequency of a stirring needle are controlled to ensure the stability of a determination result. The method is a biological quality control method for the Shuxuetong injection and facilitates the assessment on the quality reliability and controllability of the Shuxuetong injection.

Compositions and methods for preventing hematophagous infestation of cattle are provided, directed at isolated proteins with antithrombin activity and nucleotide sequences encoding the proteins. The proteins named thrombostasin is isolated from the salivary glands of Haematobia irritans. The compositions are useful as veterinary vaccines in prevention of blood-feeding in cattle by the infesting horn fly. The proteins of the invention are also useful in treatment of thrombosis.

The invention relates to the technical field of hirudo nipponia culture, in particular to a culture method for rapidly increasing antithrombin activity of hirudo nipponia. The culture method comprisesthe following steps that S1, a breeding water tank is arranged, wherein the length of the breeding water tank ranges from 100 cm to 200 cm, the width of the breeding water tank ranges from 40 cm to 60 cm, the height of the breeding water tank ranges from 30 cm to 40 cm, the water temperature in the water tank is controlled to range from 17 DEG C to 20 DEG C, and the water level in the water tankis controlled to range from 1 cm to 3 cm; S2, breeding seedlings of the hirudo nipponia; S3, conducting feed preparation; S4, feeding feed; and S5, conducting water quality management. The invention aims to provide the culture method for rapidly increasing the antithrombin activity of the hirudo nipponia. The culture method is used for solving the problems of low survival rate and low antithrombinactivity efficiency of the hirudo nipponia in the prior art.

The invention pertains to the field of medical technology and relates to a furo [2, 3-h] chromene compound and an application thereof for inhibiting platelet aggregation; the furo [2, 3-h] chromene compound, pharmaceutically-acceptable salt, or stereo-isomers and pre-drugs of the furo [2, 3-h] chromene compound, as well as pharmaceutical compatibility acceptable carriers or diluents of the furo [2, 3-h] chromene compound can be used as platelet aggregation inhibitors. The structural formula of the furo [2, 3-h] chromene compound is as shown above, wherein, X can be chosen from CH2 or C=O, R1 can be independently chosen from H or a substituted or un-substituted aromatic base, R2 can be independently chosen from H or a substituted or un-substituted aromatic base, and R can be independently chosen from H, alkyl group with one to four carbon atoms, chlorine, bromine, fluorin, methoxyl, nitryl or hydroxyl. The furo [2, 3-h] chromene compound has simple synthetic method, adapts to industrialized production and is more stable compared with natural analogues. Shown by biological activity assay, the furo [2, 3-h] chromene compound has antithrombin activity and is a platelet aggregation inhibiting drug.