In particular, the present invention relates to a PSMA binding ligand comprising an oligosaccharide building block which comprises a bond being cleavable by alpha-amylase.

Typically, this PSMA binding ligand further comprises a PSMA binding motif Q and a chelator residue A, wherein the PSMA binding motif Q and the chelator residue A are preferably linked via at least one linker L.sup.AQ comprising the oligosaccharide building block, the PSMA binding ligand thus preferably having the structure (I)

A-L.sup.AQ-Q

or a pharmaceutically acceptable salt or solvate thereof.

In particular, the present invention relates to a PSMA binding ligand comprising an oligosaccharide building block which comprises a bond being cleavable by alpha-amylase.

Typically, this PSMA binding ligand further comprises a PSMA binding motif Q and a chelator residue A, wherein the PSMA binding motif Q and the chelator residue A are preferably linked via at least one linker L.sup.AQ comprising the oligosaccharide building block, the PSMA binding ligand thus preferably having the structure (I)

A-L.sup.AQ-Q

or a pharmaceutically acceptable salt or solvate thereof.

The present invention relates to a method for the stereoselective preparation of apiose derivatives from allylic alcohol compounds and allene compounds using catalytic asymmetric synthesis. The method for the stereoselective preparation of apiose derivatives of the present invention is based on the catalytic asymmetric synthesis from allylic alcohol compounds and allene compounds in the presence of a metal catalyst, so that apiose derivatives can be produced stereoselectively, with high yield, with high optical purity regardless of the types of substituents of the compounds. The method of the invention can also be used for the preparation of oligosaccharides including monosaccharides, disaccharides, and polysaccharides or various compounds including apiose derivatives because the method can minimize the production of by-products without using an activating group, unlike the conventional method for the preparation of adipose derivatives.

The present invention relates to a method for the stereoselective preparation of apiose derivatives from allylic alcohol compounds and allene compounds using catalytic asymmetric synthesis. The method for the stereoselective preparation of apiose derivatives of the present invention is based on the catalytic asymmetric synthesis from allylic alcohol compounds and allene compounds in the presence of a metal catalyst, so that apiose derivatives can be produced stereoselectively, with high yield, with high optical purity regardless of the types of substituents of the compounds. The method of the invention can also be used for the preparation of oligosaccharides including monosaccharides, disaccharides, and polysaccharides or various compounds including apiose derivatives because the method can minimize the production of by-products without using an activating group, unlike the conventional method for the preparation of adipose derivatives.

Provided is a pharmaceutical composition useful for prevention and/or treatment of diseases caused by bacteria, wherein the pharmaceutical composition comprising a honeysuckle extract containing iridoid compounds and an antibiotic. Also provided is a pharmaceutical kit comprising the honeysuckle extract containing the iridoid compounds and the antibiotics which are separately placed. The honeysuckle extract is used in combination with the antibiotics, the responsiveness of multi-drug resistant bacteria to antibiotics is improved, a clinical application prospect is presented, especially the current status of the refractory bacterial infection diseases caused by the pathogenic bacteria resistant to the antibiotics can be improved. Also provided is a use of the pharmaceutical composition and pharmaceutical kit in the preparation of drugs for prevention and/or treatment a diseases caused by bacteria. In addition, also provided is a use of the honeysuckle extract in the preparation of drugs for reversing bacterial resistance.

Provided is a pharmaceutical composition useful for prevention and/or treatment of diseases caused by bacteria, wherein the pharmaceutical composition comprising a honeysuckle extract containing iridoid compounds and an antibiotic. Also provided is a pharmaceutical kit comprising the honeysuckle extract containing the iridoid compounds and the antibiotics which are separately placed. The honeysuckle extract is used in combination with the antibiotics, the responsiveness of multi-drug resistant bacteria to antibiotics is improved, a clinical application prospect is presented, especially the current status of the refractory bacterial infection diseases caused by the pathogenic bacteria resistant to the antibiotics can be improved. Also provided is a use of the pharmaceutical composition and pharmaceutical kit in the preparation of drugs for prevention and/or treatment a diseases caused by bacteria. In addition, also provided is a use of the honeysuckle extract in the preparation of drugs for reversing bacterial resistance.

The invention provides a process for enabling the production of a particulate composition containing anhydrous crystalline ascorbic acid 2-glucoside that does not significantly cake even when the production yield of ascorbic acid 2-glucoside does not reach 35% by weight. The process for producing a particulate composition containing anhydrous crystalline ascorbic acid 2-glucoside, which comprises allowing a CGTase to act on a solution containing either liquefied starch or dextrin and L-ascorbic acid and then allowing a glucoamylase to act on the resulting solution to obtain a solution with an ascorbic acid 2-glucoside production yield of at least 27%, purifying the obtained solution to increase the ascorbic acid 2-glucoside content to a level of over 86% by weight, precipitating anhydrous crystalline ascorbic acid 2-glucoside by a controlled cooling method or pseudo-controlled cooling method, collecting the precipitated anhydrous crystalline ascorbic acid 2-glucoside, and ageing and drying the collected anhydrous crystalline ascorbic acid 2-glucoside.

The invention provides a process for enabling the production of a particulate composition containing anhydrous crystalline ascorbic acid 2-glucoside that does not significantly cake even when the production yield of ascorbic acid 2-glucoside does not reach 35% by weight. The process for producing a particulate composition containing anhydrous crystalline ascorbic acid 2-glucoside, which comprises allowing a CGTase to act on a solution containing either liquefied starch or dextrin and L-ascorbic acid and then allowing a glucoamylase to act on the resulting solution to obtain a solution with an ascorbic acid 2-glucoside production yield of at least 27%, purifying the obtained solution to increase the ascorbic acid 2-glucoside content to a level of over 86% by weight, precipitating anhydrous crystalline ascorbic acid 2-glucoside by a controlled cooling method or pseudo-controlled cooling method, collecting the precipitated anhydrous crystalline ascorbic acid 2-glucoside, and ageing and drying the collected anhydrous crystalline ascorbic acid 2-glucoside.

Etoposide glycosides and methods of making etoposide glycosides are disclosed. Glycosyl transferases catalyze addition of one or more monosaccharides to etoposide to yield etoposide glycosides. Suitable monosaccharides can be in the L- or D-configuration and typically have 5, 6, or 7 carbons. Suitable monosaccharides include allose, apiose, arabinose, fructose, fucitol, fucose, galactose, glucose, glucuronic acid, mannose, A-acetylglucosamine, rhamnose, or xylose. Uridine diphosphate glycosyl transferases can catalyze formation of either an alpha or beta glycosidic bond.

Etoposide glycosides and methods of making etoposide glycosides are disclosed. Glycosyl transferases catalyze addition of one or more monosaccharides to etoposide to yield etoposide glycosides. Suitable monosaccharides can be in the L- or D-configuration and typically have 5, 6, or 7 carbons. Suitable monosaccharides include allose, apiose, arabinose, fructose, fucitol, fucose, galactose, glucose, glucuronic acid, mannose, A-acetylglucosamine, rhamnose, or xylose. Uridine diphosphate glycosyl transferases can catalyze formation of either an alpha or beta glycosidic bond.