Patent classifications
C07H17/04
STABLE VACCINE AGAINST CLOSTRIDIUM DIFFICILE
The present invention relates to a synthetic saccharide of general formulate (I) that is related to Clostridium difficile PS-II cell-surface polysaccharide and conjugate thereof. Said synthetic saccharide, said conjugate and pharmaceutical composition containing said synthetic saccharide or said conjugate are useful for prevention and/or treatment of diseases associated with Clostridium difficile. Furthermore, the synthetic saccharide of general formula (I) is useful as marker in immunological assays for detection of antibodies against Clostridium difficile bacteria.
STABLE VACCINE AGAINST CLOSTRIDIUM DIFFICILE
The present invention relates to a synthetic saccharide of general formulate (I) that is related to Clostridium difficile PS-II cell-surface polysaccharide and conjugate thereof. Said synthetic saccharide, said conjugate and pharmaceutical composition containing said synthetic saccharide or said conjugate are useful for prevention and/or treatment of diseases associated with Clostridium difficile. Furthermore, the synthetic saccharide of general formula (I) is useful as marker in immunological assays for detection of antibodies against Clostridium difficile bacteria.
Method for separating eight components in Chinese traditional medicine composition
The solution provides a method for separating a Chinese traditional medicine composition. To explain a pharmacological effect mechanism of a medicine made of two or more components and scientific content in rules of compatibility among components of a compound medicine, systematic researches on the material basis is very necessary. Accordingly, deep researches are done on chemical components of the pharmaceutical composition in the solution, and eight compounds are separated, which are 10-O-(p-hydroxycinnamoyl)-adoxosidic acid, aloe-emodin-8-O-β-D-glucopyranoside, quercitrin, matairesinol-4′-O-glucoside, liquiritin apioside, epi-vogeloside, vogeloside and ethyl caffeate, which provides a new quality control method for the composition in the solution.
CONJUGATE OF GalNAc-OLIGONUCLEOTIDE FOR DELIVERY TO LIVER AND MANUFACTURING METHOD THEREOF
The present invention provides a conjugate of an oligonucleotide having a nucleic acid sequence expected to have a pharmacological effect in hepatic parenchymal cells with a biantennary GalNAc unit, or a pharmaceutically acceptable salt thereof, and a medicament or the like containing the same as an active component.
CONJUGATE OF GalNAc-OLIGONUCLEOTIDE FOR DELIVERY TO LIVER AND MANUFACTURING METHOD THEREOF
The present invention provides a conjugate of an oligonucleotide having a nucleic acid sequence expected to have a pharmacological effect in hepatic parenchymal cells with a biantennary GalNAc unit, or a pharmaceutically acceptable salt thereof, and a medicament or the like containing the same as an active component.
MANGIFERIN AND PREPARATION METHOD THEREOF
The present disclosure belongs to the technical field of plant extraction, and particularly relates to mangiferin and a preparation method thereof. The present disclosure includes activated carbon treatment and extraction of raw materials successively to obtain the mangiferin; the raw materials are mango leaves and/or almond leaves; the extraction is absolute methanol extraction, and the extraction is conducted at 60-65° C. Results of examples indicate that mangiferin obtained by the preparation method of mangiferin provided by the present disclosure has a purity of 98% to 99.5%, and mangiferin yield is as high as 66.7% of total mangiferin content in the mango leaves or almond leaves. The preparation method of mangiferin provided by the present disclosure is simple to operate, which obtains high-yield and highly pure mangiferin while reducing production costs of the mangiferin, and realizes the industrial production of the mangiferin.
MANGIFERIN AND PREPARATION METHOD THEREOF
The present disclosure belongs to the technical field of plant extraction, and particularly relates to mangiferin and a preparation method thereof. The present disclosure includes activated carbon treatment and extraction of raw materials successively to obtain the mangiferin; the raw materials are mango leaves and/or almond leaves; the extraction is absolute methanol extraction, and the extraction is conducted at 60-65° C. Results of examples indicate that mangiferin obtained by the preparation method of mangiferin provided by the present disclosure has a purity of 98% to 99.5%, and mangiferin yield is as high as 66.7% of total mangiferin content in the mango leaves or almond leaves. The preparation method of mangiferin provided by the present disclosure is simple to operate, which obtains high-yield and highly pure mangiferin while reducing production costs of the mangiferin, and realizes the industrial production of the mangiferin.
Enzyme-specific intracellularly-retained red fluorescent probe
It is an object of the present invention to provide a fluorescence imaging probe capable of selectively visualizing target cells such as cells expressing β-galactosidase (lacZ expressing cells) at a single-cell level in a red fluorescence region, and of performing co-staining together with GFP. An intracellularly-retainable red fluorescent probe comprising a compound represented by the following formula (I) or a salt thereof: ##STR00001## wherein: A represents a monovalent group cleaved by an enzyme; R.sup.1 represents a hydrogen atom, or one to four of the same or different substituents bonded to a benzene ring; R.sup.3, R.sup.4, R.sup.5, and R.sup.6 each independently represent —CFR.sup.10R.sup.11, —CF.sub.2R.sup.12, a hydrogen atom, a hydroxyl group, an alkyl group, or a halogen atom, wherein at least one of R.sup.3, R.sup.4, R.sup.5, and R.sup.6 is —CFR.sup.10R.sup.11 or —CF.sub.2R.sup.12; R.sup.2 and R.sup.7 each independently represent a hydrogen atom, a hydroxyl group, an alkyl group, or a halogen atom; R.sup.8 and R.sup.9 each independently represent a hydrogen atom or an alkyl group; R.sup.10, R.sup.11, and R.sup.12 each independently represent a hydrogen atom, an alkyl group, or an alkenyl group; X represents Si(R.sup.a) (R.sup.b), wherein R.sup.a and R.sup.b each independently represent a hydrogen atom or an alkyl group; and Y is —C(═O)— or —R.sup.cC(═O)—, wherein R.sup.c is an alkylene group having 1-3 carbon atoms.
Enzyme-specific intracellularly-retained red fluorescent probe
It is an object of the present invention to provide a fluorescence imaging probe capable of selectively visualizing target cells such as cells expressing β-galactosidase (lacZ expressing cells) at a single-cell level in a red fluorescence region, and of performing co-staining together with GFP. An intracellularly-retainable red fluorescent probe comprising a compound represented by the following formula (I) or a salt thereof: ##STR00001## wherein: A represents a monovalent group cleaved by an enzyme; R.sup.1 represents a hydrogen atom, or one to four of the same or different substituents bonded to a benzene ring; R.sup.3, R.sup.4, R.sup.5, and R.sup.6 each independently represent —CFR.sup.10R.sup.11, —CF.sub.2R.sup.12, a hydrogen atom, a hydroxyl group, an alkyl group, or a halogen atom, wherein at least one of R.sup.3, R.sup.4, R.sup.5, and R.sup.6 is —CFR.sup.10R.sup.11 or —CF.sub.2R.sup.12; R.sup.2 and R.sup.7 each independently represent a hydrogen atom, a hydroxyl group, an alkyl group, or a halogen atom; R.sup.8 and R.sup.9 each independently represent a hydrogen atom or an alkyl group; R.sup.10, R.sup.11, and R.sup.12 each independently represent a hydrogen atom, an alkyl group, or an alkenyl group; X represents Si(R.sup.a) (R.sup.b), wherein R.sup.a and R.sup.b each independently represent a hydrogen atom or an alkyl group; and Y is —C(═O)— or —R.sup.cC(═O)—, wherein R.sup.c is an alkylene group having 1-3 carbon atoms.
Lactuloside compounds and preparation and use thereof
The present disclosure relates to the field of pharmaceutical chemistry, and particularly to a compound represented by Formula (I), a preparation method and medical use thereof. In the compound represented by Formula (I), a lactulosyl group is connected to a heteroatom of genin (G) via a glycosidic bond, wherein the genin (G) is a group formed by removing one hydrogen atom from a heteroatom of an active pharmaceutical molecule, and “” indicates that the lactulosyl group is connected to the heteroatom of the genin (G) via an α-glycosidic bond or a β-glycosidic bond. Pharmacokinetic experiments prove that the lactuloside compound according to the present disclosure can pass through the gastrointestinal tract of a mammal without being absorbed significantly by the gastrointestinal tract and hydrolyzed significantly by endogenous enzymes of a mammal host. Therefore, the lactuloside compound can arrive at the colon site of the mammal, and release an active drug in the colon under the action of colon flora. The lactuloside compound has a function of colon-localized drug release, and can be used for preventing or treating an intestinal disease. ##STR00001##