36 results about "Complement activity" patented technology

The present invention relates to novel Fc variants that comprise at least one novel amino acid residue which may provide for enhanced effector function. More specifically, this invention provides Fc variants that have modified binding affinity to one or more Fc receptor or ligand (e.g., Fc gamma R, C1q). Additionally, the Fc variants have altered complement dependent cytotoxicity (CDC) activity and / or antibody-dependent cell-mediated cytotoxicity (ADCC). The invention further provides methods and protocols for the application of said Fc variants, particularly for therapeutic purposes.

The present invention provides modulators of complement activity. Also provided are methods of utilizing such modulators as therapeutics.

The present invention encompasses methods for inhibiting cancer, but in particular for inhibiting metastasis, by administering to a cancer patient an inhibitor of the complement cascade.

The present invention relates to peptide, polynucleotide and fusion proteins for use as inhibitors in hemostasis. These inhibitors are members of the family of proteins bearing a collagen-like domain and a globular domain. The inhibitors are useful for promoting blood flow in the vasculature by reducing thrombogenic and complement activity. The inhibitors are also useful for pacify collagenous surfaces and modulating wound healing.

The present invention provides polypeptide modulators of complement activity, including cyclic polypeptide modulators. Also provided are methods of utilizing such modulators as therapeutics.

The present invention provides modulators of complement activity. Also provided are methods of utilizing such modulators as therapeutics.

The dosages and methods described herein provide desirable pharmacokinetic (PK) and pharmacodynamics (PD) characteristics which inhibit alternative pathway complement activity, for example at least 85% or more inhibition of AP activity in vivo at dosages from about 120 mg to 200 mg BID that provides a plasma level Ctrough at least about 65 ng / ml, which provides sufficient AP inhibition to reduce the risk of complement breakthrough. In addition, the dosage form described herein provides a significantly low Cmax, providing additional safety margin and better dosing flexibility.

The invention belongs to the field of pharmacy, and relates to a novel application of a flavan compound in preparing anti-complement medicines. According to the invention, a modern pharmacological screening method is applied, and researches are carried out upon anti-complement active substances in plant medicines. According to the invention, the flavan compound is obtained by separation from an n-butanol extract of a commelinaceae plant commelina and an n-butanol extract of a polygonum plant fagopyrum. With an in-vitro complement activity evaluation test, it is verified that the compound has high inhibition effect upon classical pathway and alternative pathway of a complement system. The CH50 of the inhibition effect of the compound upon the classical pathway of the complement system is 0.13 (plus or minus 0.03)-0.78 (plus or minus 0.06) mM, and the AP50 of the inhibition effect of the compound upon the alternative pathway of the complement system is 0.12 (plus or minus 0.01)-1.00 (plus or minus 0.15) mM. The compound can be used for preparing anti-complement medicines.

The invention provides application of codiaceae polysaccharide to an anti-complement drug. The codiaceae polysaccharide has complement activity, and the application of the codiaceae polysaccharide refers to the application of the codiaceae polysaccharide with the complement activity to the preparation of the anti-complement drug or / and an anti-complement health-care product. The invention discovers the remarkable inhibiting function of the codiaceae polysaccharide on the classical pathway complement activity and the alternative pathway complement activity for the first time and discloses the application of the codiaceae polysaccharide to the preparation of the anti-complement drug and the anti-complement health-care product, so that the excessive activation of a complement system can be inhibited and further the certain preventive and therapeutic effects on various diseases such as systemic lupus erythematosus, rheumatoid arthritis and acute respiratory distress syndrome caused by the excessive activation of the complement system are achieved.

The invention belongs to the field of pharmacy, and relates to a new application of toluylene compounds in preparation of anticomplement medicaments. According to the invention, toluylene compounds are prepared from ethyl acetate extraction positions of roots of polygonum cuspidatum Sieb. et Zucc., and are confirmed to have strong inhibition effect on the classical pathway and the alternative pathway of the complement system by in-vitro anticomplement activity evaluation tests. The CH50 of the compounds for the inhibition effect on the classical pathway of the complement system is 110+ / - 12, 250+ / -20 [mu]g / ml, and the AP50 for the inhibition effect on the alternative pathway of the complement system is 800+ / -25, 440+ / -15 [mu]g / ml. The compounds can be used for preparation of anticomplement medicaments.

The invention belongs to the field of pharmacy, and relates to a boraginaceae phenol compound and a purpose thereof in preparing anticomplement medicines. According to the invention, a boraginaceae phenol compound is extracted from an ethyl acetate part of an ethanol extract of a boraginaceae plant arnebia euchroma (Royle) Johnst. With an in-vitro complement activity evaluation test, it is verified that the compound has high inhibition effect upon classical pathway and alternative pathway of a complement system. The CH50 of the compound is 0.53 +- 0.10mM, and AP50 is 0.36 +-0.02mM. The compound can be used for preparing anti-complement medicines.

The present invention relates to polypeptide modulators of complement activity, including cyclic polypeptide modulators. Included are methods of utilizing such modulators as therapeutics.

The present disclosure relates to polypeptide modulators of complement activity, including cyclic polypeptide modulators. Included are methods of utilizing such modulators as therapeutics. Also provided are methods of measuring C5 and related complexes using C5 binding agents.

The present disclosure provides methods of treating paroxysmal nocturnal hemoglobinuria (PNH) in subjects with varying exposure to eculizumab by administering R5000. The methods include methods of switching subjects from treatment with eculizumab to R5000.

The present invention relates to polypeptide modulators of complement activity, including cyclic polypeptide modulators. Included are methods of utilizing such modulators as therapeutics.

The invention belongs to the field of pharmacy, and relates to a purpose of a shikonin tetramer compound in preparing medicines. According to the invention, the shikonin tetramer compound is extracted from an ethyl acetate extract of a boraginaceae plant arnebia euchroma (Royle) Johnst. With an in-vitro complement activity evaluation test, it is verified that the compound has high inhibition effect and cytotoxic effect upon classical pathway and alternative pathway of a complement system. The compound provided by the invention has both inhibition effects upon classical pathway and alternative pathway of a complement system. The CH50 of the compound is 0.14 (plus or minus 0.01)-0.57 (plus or minus 0.11)mM, and AP50 is 0.06 (plus or minus 0.01)-0.16 (plus or minus 0.02)mM. The novel shikonin E in the compound has substantial inhibition effects against lung cancer cells (A549), prostate cancer cells (DU145), nasopharynx cancer cells (KB), and KB resistant strains (KBvin), wherein ED50 are respectively 5.00mM, 5.42mM, 3.71mM and 4.57mM. The compound can be used for preparing anti-complement or antitumor medicines.

The invention discloses a formula and a preparation method of large yellow croaker lactobacillus plantarum feed. The formula of the large yellow croaker lactobacillus plantarum feed comprises feeding feed and basal feed, wherein the feeding feed comprises 1*10<6> cfu / kg of lactobacillus plantarum, 0.1g / kg of thallus, 9.999g / kg of milk, 540g / kg fish meal, 183g / kg of starch, 37g / kg of fish paste, 20g / kg of gluten, 20g / kg of fish oil, 64g / kg of shrimp shell powder, 94g / kg of defatted soybean meal, 35g / kg of mineral mixture and 7g / kg of vitamin mixture, the percentage by mass of the feeding feed is 25.2%, and the basal feed comprises 47.3% of crude protein, 8.9% of crude fat, 10.2% of ash content and 8.4% of moisture content in percentage by mass. The preparation method comprises the following steps: carrying out separation culture, collecting the lactobacillus plantarum, mixing the defatted milk, adding the basal feed, mixing and preparing. The large yellow croaker lactobacillus plantarum feed can be used for increasing growth rate of body mass of large yellow croakers and feeding rate of the large yellow croakers, improving non-specific immunity performances such as complement activity, lysozyme activity, phagocytic activity and respiration of leukocytes in head and kidney of the large yellow croakers and enhancing pathogenic bacteria resistance and facilitates development of large yellow croaker breeding industries.

The invention belongs to the field of pharmacy, and relates to a novel application of a flavan compound in preparing anti-complement medicines. According to the invention, a modern pharmacological screening method is applied, and researches are carried out upon anti-complement active substances in plant medicines. According to the invention, the flavan compound is obtained by separation from an n-butanol extract of a commelinaceae plant commelina and an n-butanol extract of a polygonum plant fagopyrum. With an in-vitro complement activity evaluation test, it is verified that the compound has high inhibition effect upon classical pathway and alternative pathway of a complement system. The CH50 of the inhibition effect of the compound upon the classical pathway of the complement system is 0.13 (plus or minus 0.03)-0.78 (plus or minus 0.06) mM, and the AP50 of the inhibition effect of the compound upon the alternative pathway of the complement system is 0.12 (plus or minus 0.01)-1.00 (plus or minus 0.15) mM. The compound can be used for preparing anti-complement medicines.

The invention belongs to the field of pharmacy, and relates to a purpose of a shikonin compound in preparing anticomplement medicines. According to the invention, the shikonin compound is extracted from an ethyl acetate extract of a boraginaceae plant arnebia euchroma (Royle) Johnst. With an in-vitro complement activity evaluation test, it is verified that the compound has high inhibition effect upon classical pathway and alternative pathway of a complement system. The CH50 of the inhibition effect of the compound upon the classical pathway of the complement system is 0.16 (plus or minus 0.02)-0.63 (plus or minus 0.09)mM, and AP50 of the inhibition effect of the compound upon the alternative pathway of the complement system is 0.24 (plus or minus 0.04)-0.41 (plus or minus 0.04)mM. The compound can be used for preparing anti-complement medicines.

The invention discloses a strain of marine streptomyces DUT11 and its anti-complement activity application; the marine streptomyces is marine streptomyces (Streptomyces sp.) DUT11 CGMCC No.14581. For the marine Streptomyces of the present invention, the complement hemolysis test shows that its fermentation liquid has significant anti-complement activity. The invention also discloses the fermentation condition for the preparation of the marine streptomyces anti-complement active substance and its metabolites tunicamycin I, V and VII all have anti-complement activity.

The present invention provides polypeptide modulators of complement activity, including cyclic polypeptide modulators. Also provided are methods of utilizing such modulators as therapeutics.

The present invention relates to a transgenic cloned pig for xenotransplantation in which porcine endogenous retrovirus (RUN) EnvC is negative, α1,3-galactosyltransferase (GGTA1), CMP-N-acetylneuraminic acid hydroxylase (CMAH), isoglobotrihexosylceramide synthase (iGb3s), and beta-I,4-N-acetyl-galactosaminyl transferase2 (β4GalNT2) are knocked out, and human CD46 and thrombomodulin (TBM) genes are expressed, and to a method of preparing the transgenic cloned pig. The transgenic cloned pig according to the present invention may overcome hyperacute and antigen-antibody mediated immune rejection reaction, immune rejection reaction due to blood coagulation, and immune rejection reaction due to complement activity, without causing transfer of porcine endogenous retrovirus that occurs in xenotransplantation. Therefore, the transgenic cloned pig according to the present invention may be usefully utilized as a donor animal for xenotransplantation of organs and cells.

The present invention relates to the field of traditional Chinese medicine pharmacy, particularly to uses of aryl-substituted phenylpropanoid-based compounds in preparation of anti-complement drugs. According to the present invention, the aryl-substituted phenylpropanoid-based compounds 1-3 are extracted from the root of an Aquifoliaceae plant Ilexasprella by using an activity guide separation method, and the results of the classical pathway anti-complement activity evaluation test and the alternative pathway anti-complement activity evaluation test show that the compounds provide strong inhibition effects for the classical pathway and the alternative pathway of the complement system, wherein the inhibition effect on the classical pathway (CH50) is 0.032-0.059 mg / ml, and the inhibition effect on the alternative pathway (AP50) is 0.061-0.275 mg / ml; and the compounds can be used for preparing anti-complement drugs and further preparing drugs for treatment of complement-related diseases.

The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to phenol compounds represented by a formula I and novel purposes of the compounds in the preparations of anti-complement medicines. According to the invention, phenol active substances are separated from n-butyl alcohol site of ethanol extract of commelinaceae commelina commelina communis Linn., ethyl acetate site of ethanol extract of boraginaceae arnebia arnebia euchroma (Royal) Johnst dried root, and n-butyl alcohol site of ethanol extract of polygonaceae fagopyrum fagopyrum dibotrys (D. Don) Hara dried rhizome. As a result of in vitro anti-complement activity selection experiments, the compounds have substantial inhibitive effects against classical pathways and alternative pathways of complement systems. CH50 of the inhibitive effects of the compounds against classical pathways of complement systems are 41+-8mug / ml to 278+-11mug / ml. AP 50 of the inhibitive effects of the compounds against alternative pathways of complement systems are 39+-5mug / ml to 761+-110mug / ml. The compounds can be applied in the preparation of anti-complement medicines.

The invention discloses a strain of marine streptomyces S063 and its anti-complement activity application; the marine streptomyces is marine streptomyces (Streptomyces sp.) S063 CGMCC No.14582. For the marine Streptomyces of the present invention, the complement hemolysis test shows that its fermentation liquid has significant anti-complement activity. The invention also discloses the fermentation conditions for preparing the anti-complement active substance of the marine streptomyces.

The invention belongs to the field of pharmacy, and relates to a purpose of a shikonin tetramer compound in preparing medicines. According to the invention, the shikonin tetramer compound is extracted from an ethyl acetate extract of a boraginaceae plant arnebia euchroma (Royle) Johnst. With an in-vitro complement activity evaluation test, it is verified that the compound has high inhibition effect and cytotoxic effect upon classical pathway and alternative pathway of a complement system. The compound provided by the invention has both inhibition effects upon classical pathway and alternative pathway of a complement system. The CH50 of the compound is 0.14 (plus or minus 0.01)-0.57 (plus or minus 0.11)mM, and AP50 is 0.06 (plus or minus 0.01)-0.16 (plus or minus 0.02)mM. The novel shikonin E in the compound has substantial inhibition effects against lung cancer cells (A549), prostate cancer cells (DU145), nasopharynx cancer cells (KB), and KB resistant strains (KBvin), wherein ED50 are respectively 5.00mM, 5.42mM, 3.71mM and 4.57mM. The compound can be used for preparing anti-complement or antitumor medicines.

The invention belongs to the field of preparation of traditional Chinese medicines, and relates to an application of an alkaloid compound namely 5-hydroxypyrrolidine-2-ketone in preparation of an anticomplement drug. According to the invention, the alkaloid compound namely 5-hydroxypyrrolidine-2-ketone is separated from the n-butanol extraction part of an ethanol extract of a dried whole Borraginaceae plant namely Anchusaitalica Retz.; meanwhile, in-vitro anticomplement activity evaluation experiment results verify that the alkaloid compound namely 5-hydroxypyrrolidine-2-ketone has strong inhibitory effects on the classical pathway and the alternative pathway of a complement system. The alkaloid compound namely 5-hydroxypyrrolidine-2-ketone has a CH50 value of 83 [mu]g / ml and an AP50 valueof 77 [mu]g / ml, and can be used as an active ingredient for preparation of the anticomplement drug.

The invention belongs to the technical field of traditional Chinese medicine pharmacy, and in particular relates to phenyl bis-lactone compounds and their application in the preparation of anti-complement drugs. The present invention adopts the activity-oriented separation method to separate and extract the phenyl lactone compounds maysedilactone C and maysedilactone D from the whole herb of Polygonaceae (Polygonaceae) plant Polygonum chinensis Linn, and through the anti-complement activity evaluation test, the results show that, The compound has a strong inhibitory effect on the classical and alternative pathways of the complement system, wherein the inhibitory effect on the classical pathway (CH 50 ) is 0.72 ~ 0.94mM, the inhibitory effect on the alternative pathway (AP 50 ) is 0.98 to 1.20 mM. The compounds of the present invention can be used to prepare anti-complement drugs and further prepare drugs for treating complement-related diseases.