31 results about "Prostaglandin synthesis" patented technology

The invention relates to the gene encoding the mammalian prostaglandin H synthase-2 and its product. More specifically, the invention relates to the diagnosis of aberrant PGHS-2 gene or gene product; the identification, production, and use of compounds which modulate PGHS-2 gene expression or the activity of the PGHS-2 gene product including but not limited to nucleic acid encoding PGHS-12 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules; and pharmaceutical formulations and routes of administration for such compounds.

Topically applied transdermally quick penetrating (best targeting the epidermis and subsequently remaining there for a prolonged period of time) systemic independent acting, combinations and formulations which employ, combine, or incorporate a therapeutically effective non-toxic (to the patient) amount of a drug which inhibits prostaglandin synthesis together with an amount of hyaluronic acid and / or salts thereof (for example the sodium salt) and / or homologues, analogues, derivatives, complexes, esters, fragments, and / or sub units of hyaluronic acid to treat a disease and condition of the skin and exposed tissue for example, basal cell carcinoma, the precancerous, often recurrent, actinic keratoses lesions, fungal lesions, "liver" spots and like lesions (found for the most part in the epidermis), squamous cell tumours, metastatic cancer of the breast to the skin, primary and metastatic melanoma in the skin, genital warts cervical cancer, and HPV (Human Papilloma Virus) including HPV of the cervix, psoriasis (both plaque-type psoriasis and nail bed psoriasis), corns on the feet and hair loss on the head of pregnant women and remain in the skin for a prolonged period of time.

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A:wherein R represents an aryl group such as p-methoxyphenyl.This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required a-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A:wherein R represents an aryl group such as p-methoxyphenyl.This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

One embodiment of the present invention provides a composition, comprising, in amounts effective to treat sulfur mustard or half sulfur mustard induced toxicity or skin damage: an agent that inhibits alkylation of —SH and >NH protein groups; an agent that reduces —SS— to SH; a scavenger of reactive oxygen species; a substrate that maintains tissue reduction-oxidation status; an agent that protects against invading inflammatory cells and associated oxidative stress; an antagonist of prostaglandin synthesis; and an agent that induces tissue regeneration. Methods of using the composition are also provided.

Methods for the detection of active lupus nephritis (LN) and worsening renal disease activity and / or active LN in patients diagnosed with systemic lupus erythematosus, using a panel of biomarkers including transferrin (Tf), ceruloplasmin (Cp), alpha-1-acid glycoprotein (AGP1), lipocalin-like prostaglandin D synthetase (L-PGDS), and urinary neutrophil gelatinase associated lipocalin (UNGAL).

The present invention discloses recombinant escherichia coli. The recombinant escherichia coli over-expresses an encoding gene of prostaglandin H synthase and an encoding gene of prostaglandin E synthase. The present invention also discloses an application of the recombinant escherichia coli in production of prostaglandin E2. The present invention also discloses a method for producing the prostaglandin E2. Arachidonic acid is used as a substrate and the recombinant escherichia coli is used to produce the prostaglandin E2. The escherichia coli strain capable of expressing the prostaglandin H synthase and the prostaglandin E2 synthetase is constructed and the expressed enzymes can directly catalyze conversion of the arachidonic acid into the prostaglandin E2.

Fused cyclopentane—4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A:wherein R represents an aryl group such as p-methoxyphenyl.This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required α-side chain and then the required ω-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

A method of treating an individual with a condition which condition is one wherein the individual with the condition benefits from the administration of GnRH and / or a GnRH analogue, the method comprising administering to the individual GnRH and / or a GnRH analogue and an inhibitor of prostaglandin synthesis and / or a prostaglandin receptor antagonist. The methods of the invention also include combating a sex-hormone dependent disease in an individual, and regulating fertility in an individual.

The present invention provides a novel DNA microarray chip that can be used for simultaneous testing of transcriptional responses to cutaneous stressors in the context of neuro-endocrine-immune functions of the skin. The transcriptional responses to ultraviolet radiation in epidermal keratinocytes were tested using such microarray chip containing more than 700 neuro-endocrine-immune related genes. The gene expression pattern was non-random and time dependent; it included increased expression of genes involved in water and salt balance, prostaglandin synthesis, keratinocyte differentiation as well as genes coding for stress effectors, cytokines and metalloproteinases. In contrast, expression was decreased for genes coding for growth factors and their receptors, and for elements of extracellular matrix. This stochastic pattern suggests that transcriptional responses are coordinated and aimed at preservation of epidermal barrier function, prevention of early carcinogenic events and remodeling of extracellular matrix.

The invention discloses a method for preparing prostaglandin E1 by using gene engineering cyclooxygenase-1 and gene engineering prostaglandin E synthetase-1, and belongs to the field of bioengineering. The method comprises the following steps: expressing related enzymes required by prostaglandin E1 synthesis by a prokaryotic expression means, namely cyclooxygenase-1 (COX-1) and prostaglandin E synthetase-1 (mPGES-1); and reacting the enzymes with a substrate to synthesize the prostaglandin E1. By the method, a large amount of prostaglandin synthetase can be expressed, the prostaglandin E1 is synthesized, and the problem that tissue enzymes taken from living bodies are easy to pollute in industrial production can be solved. Meanwhile, the enzyme type expressed by a prokaryotic expression issingle, the concentration of the expressed enzyme is high, organic impurities in an escherichia coli system are few, and the impurities of a product after enzymatic reaction are few, so that the purification and utilization of the prostaglandin E1 are facilitated, and a new path is opened up for the artificial synthesis of the prostaglandin E1.

This invention described various formula composite of Scutellaria baicalensis for various diseases and conditions. The formula takes the advantage of our recent discovery of Scutellaria baicalensis can inhibit cyclooxygenase-2 (COX-2) activity and expression, resulting in decrease of prostaglandin synthesis. COX-2 is involved in many biological processes, such as inflammation, pain, carcinogenesis, etc. Combination of Scutellaria baicalensis with lycopene can be used for cancer prevention, especially smoking induced. Combination of Scutellaria baicalensis with glucosamine and chondroitin can be used for arthritis. Finally, this invention disclosed various method to prepare this formula and composition.

The invention belongs to the technical field of biological medicine and relates to application of CD4+ T cell-derived BACE1 and / or prostaglandin E2 receptor EP2 and / or EP4 as a therapeutic target of Alzheimer's disease. It is found for the first time that CD4 + T cell-derived BACE1 can specifically shear prostaglandin synthetase precursor protein mPGES2, so that the maturation of mPGES2 is promoted, synthesis of prostaglandin PGE2 is promoted through mature mPGES2, and therefore, abnormal activation of CD4 + T cells is caused; meanwhile, the CD4 + T cells are abnormally activated and the expression of BACE1 is increased in AD patient and AD mouse models; meanwhile, the PGE2 receptor EP2 / EP4 antagonist can improve the pathological phenotype of the Alzheimer's disease. Therefore, the CD4 + T cell-derived BACE1 and / or EP2 and / or EP4 can be used as a target for treating the Alzheimer's disease, and a new target is provided for researching a novel medicine for treating the Alzheimer's disease.

The invention relates to a pharmaceutical composition, and relates to inhibitors Aspirin and Flufenamic acid of a key enzyme AKR1C3 in a prostaglandin synthesis pathway, wherein the inhibitors can reverse the resistance of hepatoma carcinoma cells to sorafenib at low concentration in cooperation with sorafenib. An adopted specific method is an effective method that the AKR1C3 inhibitors Aspirin and Flufenamic acid and low-concentration sorafenib act together on sorafenib-resistant HepG2 hepatoma cell lines and can significantly inhibit the growth of sorafenib-resistant HepG2 cells, so as to overcome the sorafenib resistance.

The invention discloses an application of an miR-509-3p expression inhibitor in the preparation of polycystic ovary syndrome treatment drugs. The invention also provides the polycystic ovary syndrome treatment drugs containing the miR-509-3p expression inhibitor. After the inhibition of the expression of miR-509-3p in granular cells, the mRNA level of prostaglandin-endoperoxide synthase 1 (PTGS1) rises, the prostaglandin synthesis increases, and the activity of tissue-type plasminogen activation factors in ovary increases, so the ovulation is promoted. The miR-509-3p expression inhibitor can regulate the expression of PTGS1 gene to influence the prostaglandin synthesis and ovulation in order to treat the PCOS ovulation abnormity.

The present invention provides new methods for inhibiting the activity of the enzyme cycloxygenase-2 (or COX-2). Inhibitors of COX-2 are known to be useful anti-inflammatory, analgesic and anti-angiogenic agents. The compounds in the present case are heterocyclic substituted 4-aminoglutarimides. Methods of using the compounds to inhibit prostaglandin synthesis are claimed.

The invention discloses a method for preparing prostaglandin E1 by using genetic engineering cyclooxygenase-1 and genetic engineering prostaglandin E synthetase-1, belonging to the field of bioengineering. The method expresses the relevant enzymes required for the synthesis of prostaglandin E1 by means of prokaryotic expression, that is, cyclooxygenase-1 (COX-1) and prostaglandin E synthase-1 (mPGES-1), and utilizes enzymes and substrates reaction to synthesize prostaglandin E1. Through this method, prostaglandin synthase can be expressed in large quantities and prostaglandin E1 can be synthesized, which can avoid the problem of easy contamination of tissue enzymes taken from living bodies in industrial production. At the same time, the types of enzymes expressed by the prokaryotic are relatively single, and the concentration of the expressed enzymes is relatively high, and the organic matter impurities in the E. coli system are relatively small, and the product impurities after the enzymatic reaction are relatively small, which is conducive to the purification and utilization of prostaglandin E1. Synthetic prostaglandin E1 has opened up a new path.

The invention discloses a urea derivative and application thereof to prevention and treatment of inflammation. The formula I is shown in the description, wherein R1, R2 and R3 are independently selected from H, F or CH3 respectively. An in-vitro activity determination result shows that a compound provided by the invention has 5-lipoxygenase inhibition activity and prostaglandin E synthetase inhibition activity, and can be used as a medicine for treating the inflammation for deeper and wider researches; the inflammation can be gynecological inflammation, hepatitis, myocarditis, encephalitis, nephritis, pneumonia, trachitis, pharyngitis, periodontitis, gastritis, enteritis and the like.

The invention provides an optically active cyclopentanone compound shown as a formula (I) and a preparation method thereof. The optically active cyclopentanone compound can be used for preparing key intermediates and derivatives thereof in prostaglandin synthesis. The invention also provides a method for synthesizing prostaglandin by using the optically active cyclopentanone compound. When the optically active cyclopentanone compound is used for synthesizing prostaglandin, the synthesis steps of prostaglandin can be remarkably shortened, the synthesis efficiency is improved, and the production cost is reduced.

The invention discloses a recombinant Escherichia coli, which overexpresses the encoding gene of prostaglandin H synthetase and the encoding gene of prostaglandin E synthetase. The invention also discloses the application of the above-mentioned recombinant Escherichia coli in producing prostaglandin E2. The invention also discloses a method for producing prostaglandin E2, which uses arachidonic acid as a substrate to produce prostaglandin E2 by using the recombinant Escherichia coli. The invention constructs an Escherichia coli strain capable of expressing the prostaglandin H synthetase and the prostaglandin E2 synthetase, and the expressed enzyme can directly catalyze the transformation of arachidonic acid into the prostaglandin E2.

This invention relates to treating an inflammatory disease by administering a phosphodiesterase 4 inhibitor in combination with an inhibitor of prostaglandin synthesis, NSAIDs being exemplary.

The present invention provides new methods for inhibiting the activity of the enzyme cycloxygenase-2 (or COX-2). Inhibitors of COX-2 are known to be useful anti-inflammatory, analgesic and anti-angiogenic agents. The compounds in the present case are heterocyclic substituted 4-aminoglutarimides. Methods of using the compounds to inhibit prostaglandin synthesis are claimed.

The invention relates to the technical field of embryo transplantation, in particular to a medicine for improving a pregnancy rate and / or an embryo survival rate during embryo transplantation and application of the medicine. The effective component of the medicine comprises an epoxidase inhibitor. According to the medicine provided by the invention, an epoxidase inhibitor (tolfenamic acid and / or flunixin meglumine) is utilized to inhibit the activity of epoxidase (COX) and influence the synthesis of prostaglandin (PGF2alpha), so the function of corpus luteum is favorably maintained, and the pregnancy rate of transplanted embryos and the survival rate of the embryos are further improved. According to embodiments in the invention, compared with a control group, the medicine has the advantages that the pregnancy rate of of transplanted embryos is increased by 14.6%-33.0%, and the survival rate of the embryo is increased by 42.3%-86.2%.

Therapies effective for the treatment and prevention of cancer and other diseases are disclosed herein. These methods include the administration of therapeutically effective amounts of agents that increase the local production of effector cell-attracting chemokines within tumor lesions, with concommittant suppression of local production of undesirable chemokines that attract regulatory T(reg) cells. These methods include administering to the subject therapeutically effective amounts of a Toll-like receptor (TLR) agonist or other activator of NF-kB pathway in combination with a blocker of prostaglandin synthesis or a blocker of prostaglandin signaling, in combination with a type-1 interferon, or in combination with both a blocker of prostaglandin synthesis or signaling and with a type-1 interferon, thereby treating or preventing cancer or an infectious disease, or preventing their recurrence in the subject. Alternatively, the methods derived from the same paradigms, but aimed to treat or prevent autoimmune disease, chronic inflammatory disease, transplant rejection or GvH, include the combination of a Toll-like receptor (TLR) agonist in combination with a prostaglandin or other cAMP-activator.

The invention provides a preparation method of spirulina walnut milk. The preparation method comprises the following steps: selecting, removing impurities, soaking, decoloring, grinding into thick liquid, separating, extracting spirulina, burdening, blending, homogenizing, deodorizing and carrying out high-temperature instantaneous sterilization to obtain the spirulina walnut milk beverage. The spirulina walnut milk beverage has the functions of tonifying brain, improving intelligence, resisting ageing, preventing constipation, reducing blood sugar, helping sleep, preventing cardiovascular andcerebrovascular diseases, maintaining beauty, keeping young and being delicious of walnuts, and has multiple medicinal and health functions of reducing cholesterol, detoxifying kidney toxin, improving the immune function of a human body, promoting prostaglandin synthesis, inhibiting and preventing cancers, accelerating wound healing and the like of the spirulina; through homogenizing treatment and vacuum treatment in the homogenizing treatment, the fishy smell and other peculiar smells which are difficult to accept by people are effectively removed; the beverage is fine and smooth in taste; the nutritional and health requirements of people are met.

The invention provides a mesalazine enteric-coated tablet composition with a four-layer coating system and a preparation method of the mesalazine enteric-coated tablet composition, and belongs to thefield of medicines. The composition is formed by combining a mesalazine tablet core and four layers of coatings, wherein the coatings sequentially comprise a first layer, a second layer, a third layerand a fourth layer from inside to outside, wherein the first layer is an isolation layer; the second layer is a slow-release casing layer; the third layer is a positioning acid-resistant layer; and the fourth layer is a moisture-proof layer. A second method for determining the dissolution rate by adopting the appendix of the Chinese pharmacopoeia is adopted, the release rate of the product is determined at 50rpm, and the release behavior should be as follows: the release rate is less than 10% in a dissolution medium with the pH value of 1.0 for 2h, then the product is transferred into a 7.4 medium, the release rate is 10-30% in 45min, the release rate is 50-75% in 75min and the release rate is 85% or above in 105min. The product is slowly released in intestines, most of the medicines canreach colons and act on inflammatory mucous membranes, prostaglandin synthesis causing inflammation and formation of inflammatory mediator leukotriene are inhibited, and the product has a remarkable anti-inflammatory effect on intestinal wall inflammation and particularly has a good effect on inflammatory intestinal wall connective tissues.

The invention relates to a preparation method of cyclopentenone and cyclopentenone used for synthesizing benzindene prostaglandins. The present invention provides novel processes for the preparation of racemic and optically active cyclopentenones of formula I: The present invention also provides novel cyclopentenones of formula I in racemic or optically active form.