40 results about "Platelet-activating factor" patented technology

A composition comprising a biologically active agent and a permeation enhancing lipid wherein the permeation enhancing lipid is a platelet activating factor antagonist or a biologically inactive a platelet activating factor, and increases permeability of the biologically active agent across a tissue layer. Also disclosed is a process of increasing the permeability of a biological agent across a layer tissue comprising contacting the tissue layer with a composition comprising the biological agent and a permeation enhancing lipid wherein the permeation enhancing lipid is a platelet activating factor antagonist or a biologically inactive platelet activating factor.

The invention relates to a ginkgolide K, which is ginkgolide compound, is a receptor antagonist for strengthening platelet activating factors (PAF), and has very wide application prospect in pharmacy; Lou Fengchang et al. prepares trace amount of ginkgolide K by means of preparing liquid phases and the like, but the content of the ginkgolide K in natural product is extremely rare, the preparation method is lack of practical application value due to overhigh cost, and the preparation method prepares the ginkgolide K by synthesis. The preparation method has simple technique and low cost and provides possibility for further developing the compound.

The invention discloses application of parthenolide as a platelet-activating factor (PAF) inhibitor. The parthenolide can be used as a safe PAF antagonist to be applied to treatment, auxiliary treatment and prevention of diseases such as thrombus, atherosclerosis, ischemic cardio-vascular disease, cerebral ischemia, acute pancreatitis, endotoxic shock, asthma, hepatic fibrosis and hepatocirrhosis, injury of nerve, gastrointestinal ulcer and necrosis, psoriasis, systemic lupus erythematosus and acquired immune deficiency syndrome related to platelet-activating factor.

The invention provides a rupatadine fumarate compound which has dual effects of antihistamine and antagonistic platelet activating factor (PAF). According to the research, allergy and inflammatory diseases are multi-factor complex processes caused by generation and release of various different media; histamine is the most inflammatory medium appearing in allergy early symptom, and the disease symptoms including sneezing, rhinocnesmus, tearing, running nose, skin itch, wheal and the like are mostly caused by histamine H1 receptor. And PAF also can cause bronchial constriction and increased permeability of the vessel, so that running nose, nasal congestion, wheal and itch are caused; meanwhile, the PAF is also a main cause of asthma. The antiallergic drug which is clinically used only has an antihistamine activity effect, but does not have a PAF antagonistic effect.

A ginkgolide type compound which serves as a powerful antagonist of platelet activating factors (PAF) has very good protective effects on focal cerebral ischemia and diffuse total cerebral ischemia. Ginkgolide is divided into ginkgolide A, ginkgolide B, ginkgolide C, bilobalide, ginkgolide K, ginkgolide L and the like. The content of ginkgolide L in ginkgo leaves is extremely low, so that ginkgolide L is difficult to obtain, and research report on ginkgolide L is nearly zero. The invention relates to a preparation method of ginkgolide L. Ginkgolide L is extracted from commercially available ginkgo total lactone or ginkgo total lactone obtained based on a known method. The preparation method is simple to operate, the raw materials are low in cost, a plenty of ginkgolide L can be obtained rapidly, and basis is provided for research on ginkgolide L.

The present invention discloses a kind of medicine compound antaonizing platelet activating factor. The medicine compound is bilobalide B with nitrogen-containing radical connected to the hydroxyl radial in the site 10 and has the structure as shown. The medicine compound of the present invention has high water solubility, high bioavailability and high curative effect, and its salt has greatly raised water solubility, bioavailability and curative effect.

The invention relates to the field of pharmaceutical chemistry, in particular to a benzoheterocycle compound and a preparation method, a pharmaceutical preparation comprising same as well as medical application thereof. Pharmacological experiments prove that the compound has a strong antagonistic effect on H1 receptors; and a part of compounds have certain antagonistic activity to the PAF (Platelet Activating Factor) receptors. The type of compounds and the medical preparations thereof can be used for preparing medicaments for treating a series of diseases caused by allergy, such as allergic asthma, allergic rhinitis, allergic pharyngitis, urticaria or eczema.

The invention discloses a detection kit and a detection method for the activity and the total amount of lipoprotein-associated phospholipase Lp-PLA2. The detection kit is prepared from a solid-phase carrier, a zymolytic substrate, a buffer solution, an enzyme labeled antibody reagent, a cleaning solution, a chromogenic substrate, a stop solution, an enzymatic activity calibration substance and an enzymatic calibration-free substance, wherein the enzyme-linked immunosorbent assay plate is coated with an anti-Lp-PLA2 specific N-terminal non-inhibiting antibody; the zymolytic substrate is a platelet activating factor, a platelet activating factor analogue or phosphatidylcholine modified by the platelet activating factor analogue in an oxidative manner; the enzyme labeled antibody reagent is horseradish peroxidase or alkaline phosphatase or a biotin labeled anti-Lp-PLA2 inhibiting antibody; the enzymatic activity calibration substance comprises multiple concentrations of paranitrophenol standard substances; the enzymatic calibration-free substance comprises multiple reference calibration substances containing Lp-PLA2 antigens. By using the detection kit, the inference of other matter in a sample can be avoided; the in-vivo condition of the Lp-PLA2 can be more accurately reflected; the more accurate judgment basis is provided for clinic.

The present invention relates to directed differentiation and maturation of mammalian hepatocytes, such as human hepatocytes. The hepatocyte obtained in accordance with the present invention show a phenotype which is more similar to that of primary hepatocytes than previously shown. In particular, the present invention relates to exposure of mammalian hepatocytes, such as human hepatocytes, to at least one maturation factor selected from the group consisting of Src kinase inhibitors, vitamin D including precursors, metabolites and analogs thereof, hypoxia inducing compounds, sphingosine and sphingosine derivatives, activators of peroxisome proliferator-activated receptors (PPARs), platelet-activating factor (PAF), PKC inhibitors, and combinations thereof.

The invention relates to the technical field of medicines and in particular relates to application of a triterpenoid saponins compound. The invention provides application of the triterpenoid saponins compound with a structure formula I to preparation of a medicine for treating asthma. An experiment testifies that the triterpenoid saponins compound with the structure formula I has an obvious inhibition effect on a platelet activating factor receptor and can be used for alleviating tachypnea and accelerated frequency, caused by the asthma, and remarkably reducing the amount of Eos (Eosinophile granulocyte) in rat blood and reducing infiltration on trachea by the Eos; meanwhile, the secretion of GM-CSF (Granulocyte-Macrophage Colony-Stimulating Factor) in BALF (Bronchoalveolar Lavage Fluid) of guinea pigs can be inhibited and a PAF (Platelet-Activating Factor) level of blood serum of the guinea pigs is remarkably reduced, and the activation of inflammatory cells and the releasing of inflammatory transmitters are stopped, so that inflammation of the trachea is alleviated and smooth muscles of bronchus are relaxed; the high responsiveness of the trachea is reduced to treat the asthma, so that the triterpenoid saponins compound has the effect of treating the asthma and application value.

The invention belongs to the technical field of medicine and relates to a derivative of ginkgolide B structure, shown as the formula 1 and formula 2, having a carboxylic group introduced to a hydroxylgroup 10, an ester derivative with the carboxylic group, and an organic or inorganic salt pharmaceutically acceptable. By applying chemical structural modifications to ginkgolide B as a matrix, so that solubility is improved, bioavailability is improved, and therapeutic effect is enhanced; the prepared compound and its carboxylate have evident antagonistic action upon the platelet activating factor, evident anticoagulant action and evident resistance to acute cerebral ischemia, and are applicable to the preparation of drugs to prevent and treat ischemic stroke, thrombosis, angina, cardiopulmonary infarct, inflammations, asthma, and other diseases associated with the platelet activating factor.

The invention belongs to the field of medicines and relates to new use of hydroxyl carthamin yellow A in treatment of pyaemia through inhibiting occurrence and development of the pyaemia. The invention particularly relates to application of the hydroxyl carthamin yellow A in treatment of the pyaemia through lowering expression of high-mobility group protein B1 (HMGB1) of late stage inflammatory factor, lowering release of tissue factor (TF) and platelet activating factor (PAF) and lowering expression levels of cytotoxin T lymphocyte related antigen 4 (CTLA-4) and fork head box protein transcription factor P3 (Foxp3) of regulatory T cells (Treg).

The invention discloses application of glabridin in preparation of drugs to treat thrombotic diseases and belongs to the technical field of medicine. Experiments show that glabridin can significantlyinhibit platelet activating factor receptors, and can significantly reduce, in vivo, p-selectin, vWF, GPIIb/IIIa and TXB2 levels in serum of a thrombosis model rat due to external application of FeCl3solution. venous injection of glabridin can significantly inhibit the rise of whole blood PAF (platelet activating factor) concentration induced by artery thrombosis and can significantly reduce IP3content in platelets and the expression of platelet IP3 receptors; it is indicated that glabridin can inhibit platelet PAF-IP3-IP3R-[Ca2+]i signal transduction pathway, and the inhibition is one of mechanisms of glabridin to inhibit platelet activating and gathering. Glabridin can inhibit thrombosis via multiple targets and multiple pathways, and is functional in and worthy of treating thromboticdiseases.

The invention provides a method, composition and kit for treating T-cell mediated diseases, degenerative joint diseases or diseases mediated by platelet activating factor (PAF) comprising administering to an animal in need thereof, an effective amount a pharmaceutical composition containing N-acetyl-kynurenine (NAK) or pharmaceutically acceptable salts thereof as the active ingredient.

The invention belongs to the technical field of chemical synthesis and discloses platelet activating factor derivatives with the structure of formula (I), wherein the substituent R represents an acyl group. Its synthetic route uses the acetonide of the chiral source S configuration as the initial reactant. After 9 steps of reaction, the present invention adopts this method for the first time to synthesize 2-thioplatelet activating factor and its derivatives, with high yield and easy advantages of separation. The invention realizes the low-cost and large-scale synthesis of 2-S-PAF and its derivatives, and is of great significance to the activity research, biological experiment, clinical application and disease treatment of 2-S-PAF and its derivatives.