66 results about "Motilin" patented technology

A complex is provided for the treatment of neurogenic conditions having the formula:

where R¹ is

M is a metal ion Ca(II), Mg(II), Cu(II) or Ni(II); n is an integer 1 or 2; R is BBB peptide, transferrin, membrane transporter peptide, TAT peptide, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidegluconate, L-lactate, L-leucine, L-tryptophan, and L-glutamate; and R is coupled to M through a carboxylate moiety. Magnesium (II) represents the preferred metal ion as magnesium is known to have neuroprotective effects. The metal ion is in part chelated by a non-steroidal anti-inflammatory drug that does not inhibit platelet activity and includes salicylate and ibuprofenate. The complex also includes a ligand operative in transport across the blood brain barrier. A process for making an inventive complex includes the stoichiometric addition of ligands containing carboxylate groups to a solution of the metal ion. In instances where the metal ion is magnesium (II), a stoichiometric ratio of 1:1:1 is found between the non-steroidal anti-inflammatory ligand:magnesium (II):transporter ligand.

A compound is provided that has the formula

NH₂CH₂CH₂CH₂C(O)N—R   (I)

where R is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine blood brain barrier (BBB) peptide, membrane translocating protein, TAT peptides, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptidetransferrin, glucosylamnine, amino saccharin, lactylamine, leucine, tryptophan, glutamate and amino cholines.

Stable, pharmaceutical compositions including a synthetic motilin-like peptide in a buffered solution are disclosed. The composition provides for a peptide that remains stable and substantially retains its initial potency during extended storage and after steam sterilization.

A compound is provided that has the formula

NH₂CH₂CH₂CHR¹C(O)N—R  (I)

where R¹ is p-chlorophenyl, R is a moiety capable of crossing the blood brain barrier and is as a free compound serotonin, dopamine blood brain barrier (BBB) peptide, membrane translocating protein, TAT peptides, bradykinin, beta-endorphin, bombesin, calcitonin, cholecystokinin, an enkephalin, dynorphin, insulin, gastrin, substance P, neurotensin, glucagon, secretin, somatostatin, motilin, vasopressin, oxytocin, prolactin, thyrotropin, an angiotensin, galanin, neuropeptide Y, thyrotropin-releasing hormone, gonadotropnin-releasing hormone, growth hormone-releasing hormone, luteinizing hormone, vasoactive intestinal peptide transferrin, glucosylamine, amino saccharin, lactylamine, leucine, tryptophan, glutamate and amino cholines.

The present invention discloses stable pharmaceutical compositions containing synthetic motilin-like polypeptides in buffer. The composition provides a peptide that remains stable and substantially retains its starting potency after prolonged storage and steam sterilization.

The present invention relates to novel conformationally-defined macrocyclic compounds that bind to and/or are functional modulators of the motilin receptor including subtypes, isoforms and/or variants thereof. These macrocyclic compounds are useful as therapeutics for a range of gastrointestinal disorders, in particular those in which suppression or inhibition of the migrating motor complex (MMC) is effective or malfunction of gastric motility or increased motilin secretion is observed, such as hypermotilinemia, imitable bowel syndrome, dyspepsia, including gallbladder dyspepsia, diarrhea, cancer treatment-related diarrhea, cancer-induced diarrhea, chemotherapy-induced diarrhea, radiation enteritis, radiation-induced diarrhea, stress-induced diarrhea, chronic diarrhea, AIDS-related diarrhea, C. difficile associated diarrhea, traveller's diarrhea, acute infectious diarrhea, diarrhea induced by graph versus host disease, other types of diarrhea, functional gastrointestinal disorders, chemotherapy-induced nausea and vomiting (emesis), post-operative nausea and vomiting, cyclic vomiting syndrome and functional vomiting. Accordingly, methods of treating such disorders with such macrocyclic compounds and pharmaceutical compositions thereof are also provided in addition to methods of modulating the migrating motor complex.

The invention discloses a Lactobacillus fermentum suo strain capable of preventing gastrohelcoma and a health-care application thereof. The collection number of the strain is CCTCC NO:M2013511. The strain has high acid resistance, and the survival rate in the simulated gastric fluid with the pH value of 3.0 after 3 hours is up to 92.46+/-4.06%; the strain can slowly grow in a bile salt with the concentration of 1.0%, and the growth efficiency reaches 17.36+/-1.19% of the bile-salt-free culture; the hydrophobicity of the Lactobacillus fermentum suo cells is up to 68.44+/-2.48%; and the strain can normally grow in the human intestinal tract. The Lactobacillus fermentum suo is capable of reducing the gastrohelcoma area, lowering the gastrohelcoma degree, lowering the motilin (MOT) and substance-P (SP) to different degrees, increasing the somatostatin (SS) and vasoactive intestinal peptide (VIP) and lowering the tumor necrosis factor-alpha (TNF-alpha), leucocyte interleukin-6 (IL-6), leucocyte interleukin-12 (IL-12) and interferon-gamma (IFN-gamma), has favorable gastrohelcoma inhibitubg function, and achieves the effects approximate to the drug omeprazole.

The invention discloses an extracting method of cordyceps militaris polysaccharide. The extracting method comprises the steps of decocting cordyceps militaris in water, filtering, adding absolute ethyl alcohol into filtrate until the ethyl alcohol concentration is 70+/-5V%, standing and separating solid from liquid. The obtained sediment is the cordyceps militaris polysaccharide. The invention further discloses application of the cordyceps militaris polysaccharide in an aspect of preparing functional constipation treating medicine. Experiments show that the cordyceps militaris polysaccharide disclosed by the invention can obviously improve the content of motilin (MTL), gastrin (GAS), somatostation (SS) and P substance in serum and improve functional constipation. Therefore, the cordyceps militaris polysaccharide is ideal medicine for treating the functional constipation.

The invention relates to conformation-constrained entirely-synthetic macrocyclic compounds. A conformation-constrained, space-defined 12-30-member macrocyclic system (I) which is as shown in the description comprises three different constitution units: an aromatic template a, a confor1ation regulator b and a spaced part c, which are illustrated in the description and the claims. The macrocyclic compounds (I) can be easily prepared according to a parallel synthesis method or a combinatorial chemistry method, and are designed for realizing interaction with a specific biological target. Particularly, the compounds show agonistic or antagonistic activity to the following matters: a motilin receptor (MR), a 5-hydroxytryptamine receptor (5-HT2B receptor) of a subtype 5-HT2B, and a prostaglandin F2alpha receptor (FP receptor). Thus, the compounds are effectively used for treating gastrointestinal tract hypomotility disorder such as diabetic gastroparesis and constipation-predominant irritable bowel syndrome, CNS-related diseases such as migraine, schizophrenia, psychosis and depression, ocular hypertension such as glaucoma-related ocular hypertension, and premature delivery.

The invention discloses a bifidobacterium bifidum for relieving constipation and regulating intestinal flora disorder and application thereof, and belongs to the field of microorganisms. The bifidobacterium bifidum provided by the invention can obviously improve the water content of excrement and the intestinal propulsive rate and reduce the first black excrement time of constipation mice, and has the effect of obviously improving apparent pathological indexes of constipation; in the detection of physiological indexes, the bifidobacterium bifidum can also improve the content of motilin and reduce the content of somatostatin, so that the intestinal tract movement is fundamentally influenced; the bifidobacterium bifidum can regulate the abundance of important microorganisms in the intestinal tract and maintain the steady state of the intestinal tract. Compared with GDMCC NO: 60940, the bifidobacterium bifidum CCFM1166 has the advantages that the content of MTL in serum is better increased, the content of SS in the serum is reduced, and the promotion effect on intestinal peristalsis is more remarkable, so that a more personalized treatment scheme can be adopted for constipation patients in the future, and the application prospect is very considerable.

The invention discloses new application of a medicament composition composed of coptis chinensis and fructus evodiae in preparation of a medicament for treating functional dyspepsia. The medicament composition is composed of the following components by weight: 1-30 parts of the coptis chinensis and 10-40 parts of the fructus evodiae. Efficacy experiment verification of the medicament composition shows that the capacity of gastric emptying and intestine propulsion of atropine gastrointestinal motility obstacle model mouse can be obviously improved, the content of motilin and gastrin of rat plasma can be obviously increased, and objective indicators of serum acetyl choline, acetylcholinesterase, choline acetyltransferase, and the like can be effectively enhanced after coptis chinensis and fructus evodiae are mixed and matched in a certain proportion. The medicament composition has good treatment effect on a functional dyspepsia patient.

The invention provides a natural composition for improving functions of stomach and intestine and preventing osteoporosis. The natural composition consists of a radix codonopsis extract, a radix astragali extract, a bighead atractylodes rhizome extract, a Chinese yam extract, a maca extract and a licorice root extract, and the effective ingredients of the components are in interaction, so that gastrin secretion and motilin secretion can be increased, the vasoactive intestinal peptide level of blood vessels is reduced, the functions of the stomach and the intestine are improved, the bone density can be increased, the content of bone minerals of bone calcium, bone phosphorus and the like can be increased, and the effect of relieving osteoporosis can be achieved.

The invention relates to a method for extracting malus halliana flower polysaccharide, and is characterized in that the method comprises the steps: carrying out heating reflux of dried malus hallianaflowers with petroleum ether, then taking a residue, and soaking with ethanol; after the end of soaking, taking out the residue, adding water and decocting; and after the end of decoction, filtering,adding 95% ethanol to the filtrate until the final concentration is 70-85%, allowing to stand, taking a precipitate, and leaching with anhydrous ethanol, acetone and petroleum ether respectively, wherein the obtained precipitate after leaching is the malus halliana flower polysaccharide. The invention also discloses an application of the malus halliana flower polysaccharide in preparation of drugsfor treating functional constipation. Tests find that the malus halliana flower polysaccharide can significantly increase the content of motilin (MTL), gastrin (GAS) and P substances in serum, reduces the content of somatostatin (SS) and improves functional constipation. The malus halliana flower polysaccharide is indicated to be an ideal drug for treating functional constipation.

The compounds of formula (I) are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor disorders. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.