39results about How to "Strong analgesic activity" patented technology

The invention belongs to the fields of biochemistry and molecular biology, relates to an alpha-conotoxin peptide, and a medical composition, a preparation method and a purpose thereof, also relates to a propeptide of the conotoxin peptide, a nucleic acid construct, an expression vector, a transformed cell and a fusion protein, and also relates to a method for blocking acetylcholine receptors and a pharmaceutical purpose of the conotoxin peptide. The alpha-conotoxin peptide can specifically block the acetylcholine receptors (nAChRs) (such as alpha3beta2 nAChR), has high analgesic activity and addiction withdrawal activity and has a good application prospect in the aspects of preparing analgesics, smoking cessation or drug treatment medicines and the like.

The invention discloses an alpha conus polypeptide derivative, amino acid residues of which are shown in sequence 1 in a sequence table. To effectively resist the degradation digestion of partial protease in a human body, and improve the bioavailability and the drug metabolism performance, an N end of the alpha conus polypeptide derivative can be connected with a benzoyl group. The alpha conus polypeptide derivative can also be subjected to cyclization, fattening or PEG modification to strengthen the treatment effect of the alpha conus polypeptide derivative. A big mouse experiment shows that the alpha conus polypeptide derivative shows strong analgesic activity in a neuropathic pain model of a big mouse, and the analgesic activity is remarkably higher than that of control peptide Vc1.1 and shows dose-dependent relation.

The invention provides a benzoyl fluorobenzene salicylamide compound and a preparation method and an application thereof. The benzoyl fluorobenzene salicylamide compound with a structure shown in a formula (I) is formed by the substitution reaction of benzoyl fluorobenzene salicyloylchloride as shown in a formula (III) and R1R2NH in an organic solvent at a temperature of between 0 and 160 DEG C. Derivatives of the benzoyl fluorobenzene salicylamide compound and the preparation method and the application thereof of the invention have the advantages of: (1) providing a novel anti-inflammatory and analgesic drug with remarkable anti-inflammatory and analgesic activities, and providing a research basis for selecting novel drugs; (2) simple preparation process and applicability industrialized production.

The invention discloses alpha-type conus polypeptides and application thereof. The invention provides seven polypeptides: in the polypeptide I, an amino acid sequence is disclosed by a sequence 7 in a sequence table, and the last amino acid residue is amidated; in the polypeptide II, an amino acid sequence is disclosed by a sequence 8 in the sequence table, and the last amino acid residue is amidated; in the polypeptide III, an amino acid sequence is disclosed by a sequence 9 in the sequence table, and the last amino acid residue is amidated; in the polypeptide IV, an amino acid sequence is disclosed by a sequence 10 in the sequence table, and the last amino acid residue is amidated; in the polypeptide V, an amino acid sequence is disclosed by a sequence 11 in the sequence table, and the last amino acid residue is amidated; in the polypeptide VI, an amino acid sequence is disclosed by a sequence 12 in the sequence table, and the last amino acid residue is amidated; and in the polypeptide VII, an amino acid sequence is disclosed by a sequence 13 in the sequence table. By the determination of activity, the seven polypeptides of a general formula I have abirritation, wherein the alpha-type conus polypeptides T-1, T-2, T-3 and T-4 have obvious analgesic activity, T5-T7 also have obvious analgesic activity, and the alpha-type conus polypeptides have application value in an analgesic aspect.

The invention relates to haemadipsa sylvestris analgesic peptide mh2620 and a gene and application thereof and belongs to the technical field of biomedicine.The haemadipsa sylvestris analgesic peptide mh2620 is single-link polypeptide subjected to haemadipsa sylvestris analgesic peptide gene coding, the molecular weight is 2620.13 Dalton, and the isoelectric point is 5.26.The haemadipsa sylvestris analgesic peptide mh2620 is composed of an amino acid sequence shown as SEQ ID NO: 1.The gene for encoding the haemadipsa sylvestris analgesic peptide mh2620 is composed of a nucleotide sequence shown as SEQ ID NO: 2.The haemadipsa sylvestris analgesic peptide mh2620 is applied to preparation of a sodium ion channel inhibitor and an analgesic drug.The haemadipsa sylvestris analgesic peptide mh2620 has the advantages of being capable of inhibiting a sodium ion channel, having a remarkable analgesic effect, and being simple in structure, convenient to synthesize artificially, high in analgesic activity and capable of being applied to preparation of the sodium ion channel inhibitor and the analgesic drug.

The invention belongs to the fields of biochemistry and molecular biology, and relates to alpha-conotoxin TxIC, a medicinal composition thereof, a preparation method thereof and an application. The invention further relates to a propeptide of conotoxin, a nucleic acid construct thereof, an expression vector thereof and a transformed cell, and a fused protein thereof. The invention further relates to a method for blocking an acetylcholine receptor and a pharmaceutical use of the conotoxin. The alpha-conotoxin disclosed by the invention can be used for specifically blocking the acetylcholine receptor (nAChRs) (such as alpha3beta2nAChR), has high analgesic activity and addiction withdrawal activity, and has a good application prospect on the aspect of preparation of analgesics, smoking addiction withdrawal medicaments or drug addiction withdrawal medicaments and the like.

The invention belongs to the technical field of medicines, and discloses an amide derivative containing a benzoheterocycle structure, and a composition and an application thereof. The amide derivativecontaining the benzoheterocycle structure is a compound represented by structural formula I and a nontoxic pharmaceutically acceptable salt thereof, or the amide derivative containing the benzoheterocycle structure is a compound represented by structural formula II or a nontoxic pharmaceutically acceptable salt thereof. The amide derivative containing the benzoheterocycle structure has good analgesic activity and good inhibition effect on a target sodium ion channel Nav1.7.

The invention relates to preparation of a Scolopendra mutilans analgesic peptide precursor protein Ssm-A and products thereof (Ssm-A1 and Ssm-A2). The Scolopendra mutilans analgesic peptides (Ssm-A1 and Ssm-A2) have the beneficial characteristics of simple structure and special activity. The Scolopendra mutilans analgesic peptides (Ssm-A1 and Ssm-A2) can be separated and purified from Scolopendra mutilans venom. The invention also relates to application of the Scolopendra mutilans analgesic peptides (Ssm-A1 and Ssm-A2); and the Scolopendra mutilans analgesic peptides (Ssm-A1 and Ssm-A2) have analgesic effect on pains caused by multiple factors, and can be used for preparing analgesic drugs.

The invention discloses alpha-conus polypeptides and use thereof. The invention provides seven polypeptides: a polypeptide I of which the amino acid sequence is represented by a sequence 7 in a sequence table and in which the last amino acid residue is amidated; a polypeptide II of which the amino acid sequence is represented by a sequence 8 in the sequence table and in which the last amino acid residue is amidated; a polypeptide III of which the amino acid sequence is represented by a sequence 9 in the sequence table and in which the last amino acid residue is amidated; a polypeptide IV of which the amino acid sequence is represented by a sequence 10 in the sequence table and in which the last amino acid residue is amidated; a polypeptide V of which the amino acid sequence is representedby a sequence 11 in the sequence table and in which the last amino acid residue is amidated; a polypeptide vI of which the amino acid sequence is represented by a sequence 12in the sequence table andin which the last amino acid residue is amidated; and a polypeptide VII of which the amino acid sequence is represented by a sequence 13 in the sequence table and in which the last amino acid residueis amidated. The result of activity tests, the seven polypeptides of the general formula (I) have pain relieving effect, alpha-conus polypeptides T-1, T-2, T-3 and T-4 have obvious pain-relieving activity, and the alpha-conus polypeptides T-5, T-6 and T-7 also have obvious pain-relieving effect, and the alpha-conus polypeptides have application values in pain-reliving aspect.

The invention discloses seven alpha type conotoxin peptides and applications thereof. The peptide I has an amino acid sequence shown as the sequence 7 in a sequence table, and the last amino acid residue is amidated; the peptide II has an amino acid sequence shown as the sequence 8 in the sequence table, and the last amino acid residue is amidated; the peptide III has an amino acid sequence shownas the sequence 9 in the sequence table, and the last amino acid residue is amidated; the peptide IV has an amino acid sequence shown as the sequence 10 in the sequence table, and the last amino acidresidue is amidated; the peptide V has an amino acid sequence shown as the sequence 11 in the sequence table, and the last amino acid residue is amidated; the peptide VI has an amino acid sequence shown as the sequence 12 in the sequence table, and the last amino acid residue is amidated; and the peptide VII has an amino acid sequence shown as the sequence 13 in the sequence table. Proved by determination of activity, the seven peptides shown as a general formula I have an analgesic effect, wherein alpha type conotoxin peptides T-1, T-2, T-3 and T-4 have remarkable analgesic activity, and thealpha type conotoxin peptides T5-T7 also have remarkable analgesic activity, and the application value on the aspect of analgesia is achieved.

The invention belongs to the field of traditional Chinese medicines, and particularly relates to a traditional Chinese medicine composition for treating hemorrhagic haemorrhoids as well as a preparation method and an application of the traditional Chinese medicine composition. The traditional Chinese medicine composition for treating hemorrhagic haemorrhoids provided by the invention comprises the following components in parts by weight: 10 parts of mint, 15 parts of coptis chinensis, 6 parts of asarum, 10 parts of radix angelicae dahuricae, 10 parts of rhubarb, 6 parts of fructus arctii, 20 parts of scrophularia ningpoensis, 17 parts of flos carthami, 10 parts of fructus forsythia, 13 parts of dandelion, 15 parts of honeysuckle, 30 parts of rhizoma atractylodis macrocephalae, 6 parts of clove and 10 parts of fructus cnidii. The traditional Chinese medicine composition has a good treatment effect on hemorrhagic haemorrhoids, and has significant clinical promotional value.

The present invention belongs to the field of biomedicine technology. Chinese hard tick neuropeptide is a kind of single-stranded small peptide obtained from the ganglion of Chinese hard tick and with molecular weight of 1005.22 dalton, isoelectric point of 8.59, and the first order whole sequence structure of NH2-LVVYPWTK-COOH. It is prepared through adhering Chinese hard tick to the bottom of watch glass and on ice for 20 min, cutting along back side to eliminate ganglion, homogenizing, centrifuging and eliminate precipitate, filtering with membrane, and twice reverse high efficiency liquid phase chromatographic separation and purification. The Chinese hard tick neuropeptide has powerful analgetic activity, and may be used as analgetic medicine.

The invention relates to the fields of natural medicaments and medical health care, and in particular relates to medical application of 1,2,3,4,6-O-pentagalloylglucose (PGG) in preparation of demulcent medicaments. Animal experiments prove that the PGG has obvious demulcent activity for visceral pain, central pain and peripheral pain, and has low effective dose. The invention also discloses a composition of the PGG and ligustilide A (SA) in a specific ratio. The composition has a strong demulcent effect on the visceral pain, and has a broad application prospect.

The invention discloses a traditional Chinese medicine composition for treating nephritis, and belongs to the technical field of medicines. The medicine composition is prepared from the following components: corn silk, cherokee rose fruit, herba houttuyniae, spreading hedyotis herb, lily, Chinese wolfberry, Chinese-date, peach kernel, eucommia, lalang grass rhizome, shizandra berry, white mulberry root-bark, black soybean, and liquorice. The traditional Chinese medicine composition has an excellent curative effect on treating or preventing the acute nephritis, and the medicine side effect is low, so that the traditional Chinese medicine composition has a remarkable clinical promotional value.

The invention belongs to the field of traditional Chinese medicines, and particularly relates to a traditional Chinese medicine composition for treating hemorrhagic haemorrhoids as well as a preparation method and an application of the traditional Chinese medicine composition. The traditional Chinese medicine composition for treating hemorrhagic haemorrhoids provided by the invention comprises the following components in parts by weight: 10 parts of mint, 15 parts of coptis chinensis, 6 parts of asarum, 10 parts of radix angelicae dahuricae, 10 parts of rhubarb, 6 parts of fructus arctii, 20 parts of scrophularia ningpoensis, 17 parts of flos carthami, 10 parts of fructus forsythia, 13 parts of dandelion, 15 parts of honeysuckle, 30 parts of rhizoma atractylodis macrocephalae, 6 parts of clove and 10 parts of fructus cnidii. The traditional Chinese medicine composition has a good treatment effect on hemorrhagic haemorrhoids, and has significant clinical promotional value.

The invention provides application of a triterpenoid saponin compound to preparation of analgesics, and particularly relates to application of a triterpenoid saponin compound shown in a formula I fortreatment of neuralgia, bone pain, muscle pain, pain caused by traumatic injury, headache, stomach pain, intestinal colic, biliary colic, renal colic and cancer pain. (Please see the specification forthe formula I). In the formula I, R1=H, glu, R2=H, OH. The invention further discloses application of a salt of the compound of the formula I to the preparation of the analgesics. The triterpenoid saponin compound can be a naturally existing organic compound or a synthetic organic compound, has strong analgesic activity, and is used as an active ingredient for preparing the analgesics or a pharmaceutical composition together with pharmaceutically acceptable carriers or excipients.

The invention belongs to the field of pharmaceutical chemicals, and relates to a 3-(1-aryl-piperidin-4-yl)-2-aryl-thiazole-4-ketone compound, medicinal salt thereof, a preparation method thereof and use thereof, in particular to a compound shown in the formula I or medicinal salt thereof. The 3-(1-aryl-piperidin-4-yl)-2-aryl-thiazole-4-ketone compound or the medicinal salt thereof has obvious N-type calcium channel blocking-up activity and good pharmacokinetics properties, can prevent and cure or relieve pain effectively, and has potential used as novel medicine for preventing and / or treating pain, apoplexy and cerebral ischemia, alcohol addiction and intoxication, acute and chronic renal failure, or renal insufficiency.

The invention discloses a method for preparing analgesic polypeptide from silkworms and belongs to the field of gene engineering. The preparation method comprises steps as follows: a conotoxin omega-MVIIA gene sequence is optimized according to BmNPV (Bombyx mori Nucleopolyhedrovirus) codon usage frequency, genes obtained after chemical synthesis are linked to a donor plasmid pFastBacDual and introduced to EGFP (enhanced green fluorescent protein) genes, and a recombinant donor plasmid pFBD-MVIIA / EGFP is established. MVIIA / EGFP is transposed to BmNPV with a Bac-to-Bac method, and a recombinant virus vBmMVIIA / EGFP is formed. DNA of the recombinant virus is transfected to cells of the silkworms, BV particles are obtained and injected into the silkworms at 200 pfu after the titer of the BV particles is tested by the aid of green fluorescence, and blood of the silkworms is collected after five days of transfection. Acetic-acid-induced mouse writhing experiments show that the blood of the silkworms infected with expressed conotoxin omega-MVIIA has remarkable analgesic activity, and the number of the average writhing times is only 3.55 and is remarkably higher than 37.30 in a control group of mice injected with normal saline. A new method is provided for expression of conotoxin omega-MVIIA with analgesic activity, and has potential application value.

The invention belongs to the fields of biochemistry and molecular biology, and relates to alpha-conotoxin TxIC, a medicinal composition thereof, a preparation method thereof and an application. The invention further relates to a propeptide of conotoxin, a nucleic acid construct thereof, an expression vector thereof and a transformed cell, and a fused protein thereof. The invention further relates to a method for blocking an acetylcholine receptor and a pharmaceutical use of the conotoxin. The alpha-conotoxin disclosed by the invention can be used for specifically blocking the acetylcholine receptor (nAChRs) (such as alpha3beta2nAChR), has high analgesic activity and addiction withdrawal activity, and has a good application prospect on the aspect of preparation of analgesics, smoking addiction withdrawal medicaments or drug addiction withdrawal medicaments and the like.

The invention discloses a medical use of (S)-3-fluoro-2-(4-isobutyl phenyl) propionic acid. Further, the (S)-3-fluoro-2-(4-isobutyl phenyl) propionic acid can be used for preparing analgesic and anti-inflammatory or anti-tumor medicaments containing the (S)-3-fluoro-2-(4-isobutyl phenyl) propionic acid or pharmaceutical acceptable salts thereof.

The invention relates to a multi-hydrogen isoquinoline derivative as well as a preparation method and medical application thereof, the multi-hydrogen isoquinoline derivative is a compound as shown ina formula (I) or cis / trans isomers, enantiomers, diastereoisomers, racemates, solvates, hydrates or pharmaceutically acceptable salts thereof, and Z, R1, R2, G, n, W and Y are defined in the specification. The novel molecular polyhydroisoquinoline derivative is novel in structure, higher in safety, small in side effect and better in patent medicine property, has the analgesic activity equal to oreven higher than that of morphine, is simple in synthesis operation, provides a feasible method for realizing large-scale preparation in a laboratory, can be used for preparing medicines for preventing, treating and improving pain, and has wide application prospects. The pain such as acute pain, chronic pain such as inflammatory pain and peripheral mediated neuropathic pain, preferably migraine, is treated, the effect is remarkable, and the derivative is worthy of popularization.

The invention discloses alpha-conus polypeptides and use thereof. The invention provides seven polypeptides: a polypeptide I of which the amino acid sequence is represented by a sequence 7 in a sequence table and in which the last amino acid residue is amidated; a polypeptide II of which the amino acid sequence is represented by a sequence 8 in the sequence table and in which the last amino acid residue is amidated; a polypeptide III of which the amino acid sequence is represented by a sequence 9 in the sequence table and in which the last amino acid residue is amidated; a polypeptide IV of which the amino acid sequence is represented by a sequence 10 in the sequence table and in which the last amino acid residue is amidated; a polypeptide V of which the amino acid sequence is representedby a sequence 11 in the sequence table and in which the last amino acid residue is amidated; a polypeptide vI of which the amino acid sequence is represented by a sequence 12in the sequence table andin which the last amino acid residue is amidated; and a polypeptide VII of which the amino acid sequence is represented by a sequence 13 in the sequence table and in which the last amino acid residueis amidated. The result of activity tests, the seven polypeptides of the general formula (I) have pain relieving effect, alpha-conus polypeptides T-1, T-2, T-3 and T-4 have obvious pain-relieving activity, and the alpha-conus polypeptides T-5, T-6 and T-7 also have obvious pain-relieving effect, and the alpha-conus polypeptides have application values in pain-reliving aspect.

The invention relates to a goosegrass extract and a preparation method thereof. The extract is widely used in medicines and health products for analgesia, improvement of learning and memory functions, prevention or treatment of Alzheimer's disease. The extract used in the invention has extensive and cheap plant resources, and its preparation process is simple and easy for large-scale production.

The invention discloses a medical use of (S)-3-fluoro-2-(4-isobutyl phenyl) propionic acid. Further, the (S)-3-fluoro-2-(4-isobutyl phenyl) propionic acid can be used for preparing analgesic and anti-inflammatory or anti-tumor medicaments containing the (S)-3-fluoro-2-(4-isobutyl phenyl) propionic acid or pharmaceutical acceptable salts thereof.

The invention discloses an alpha conus polypeptide derivative, amino acid residues of which are shown in sequence 1 in a sequence table. To effectively resist the degradation digestion of partial protease in a human body, and improve the bioavailability and the drug metabolism performance, an N end of the alpha conus polypeptide derivative can be connected with a benzoyl group. The alpha conus polypeptide derivative can also be subjected to cyclization, fattening or PEG modification to strengthen the treatment effect of the alpha conus polypeptide derivative. A big mouse experiment shows thatthe alpha conus polypeptide derivative shows strong analgesic activity in a neuropathic pain model of a big mouse, and the analgesic activity is remarkably higher than that of control peptide Vc1.1 and shows dose-dependent relation.

The invention discloses a preparation method of an antalgic active polypeptide and belongs to the genetic engineering field. The preparation method comprises the following steps: optimizing the gene sequence of the pokeweed antibacterial peptide PaAMP1 according to the frequency of use of the escherichia coli codon, linking the gene sequence to a prokaryotic expression vector pET-32a by virtue of chemical synthesis; next, importing the recombinant plasmid to an escherichia coli Origami (DE3) strain and realizing high-efficiency solution expression of recombinant PaAMP1 after IPTG induction; separating and purifying the recombinant PaAMP1 by use of nickel ion affinity chromatography; according to the preparation method, a mouse acetic acid body torsion test is performed to prove that the recombinant PaAMP1 has remarkable analgesic activity and has potential application value in the analgesia field for the first time; as the PaAMP1 is from the plant pokeweed which is easy to plant at a large scale and is far abundant than maritime cone shell resources, natural antalgic polypeptides are expected to be industrially extracted from the large-scale planted pokeweeds to meet the requirements for medicine research and development and clinic use.