Ensuiko Sugar Refining Co., Ltd.

Other

Kaken Pharmaceutical Company, Ltd.

Osaka Research Institute of Industrial Science and Technology

Bio Research Corporation of Yokohama

Okayama University

Hiroki Hamada

Yoshio Shimizu

Ensuiko Sugar Regining Co., Ltd.

Tadakatsu Mandai

Director of National Food Research Institute, Minstry of Agriculture,

Osaka Municipal Technical Research Institute

Hamada, Hiroki

Shimizu, Yoshio

Katsuhiko Mikuni

Kozo Hara

Koji Hara

Hiroshi Okumoto

Katsuyoshi Nakanishi

Tetsuya Ito

Hisaharu Masaki

Hiroki Tadokoro

Takaaki Kiryu

Teruhiko Umetsu

Taro Kiso

Hiromi Murakami

Nobuhiro Kuwahara

Hideki Takahashi

Shoichi Kobayashi

Hitoshi Hashimoto

Masaharu Seno

Mitsuru Monma

Toshiya Takano

Tomonari Kasai

Kyoko Saito

Yoshinori Tsuchiya

Kosho Nakamura

Ichiro Fujiwara

Masaharu Murakami

Tsukasa Shigehiro

The present invention provides a D-glucaric acid-producing bacterium and a method for producing D-glucaric acid. The present invention is characterized in that D-glucaric acid or a salt thereof is produced from one or more saccharides selected from the group consisting of D-glucose, D-gluconic acid and D-glucuronic acid with catalytic action of a specific alcohol dehydrogenase PQQ-ADH (1) and a specific aldehyde dehydrogenase PQQ-ALDH (2), and that D-glucaric acid or a salt thereof is produced by using a microorganism having the PQQ-ADH (1) and the PQQ-ALDH (2) or a processed product thereof in the presence of the one or more saccharides. The present invention can provide a microorganism having improved productivity of D-glucaric acid to be used for production of D-glucaric acid and a method for efficiently producing D-glucaric acid.

D-glucaric acid producing bacterium, and method for manufacturing D-glucaric acid

In order to reduce the side effects of paclitaxel derivatives having excellent anti-cancer effects, an attempt was made to produce a liposome encapsulating paclitaxel derivatives such as paclitaxel monoglycosides and docetaxel monoglycosides. However, the introduction efficiency of paclitaxel derivatives, etc., into a liposome was poor, and this technique was not developed to a practical level. The present invention provides a method for producing a liposome encapsulating a paclitaxel monoglycoside and/or a docetaxel monoglycoside, and having an antibody specifically recognizing a cancer cell, the method comprising a step of bringing a liposome encapsulating a polyoxyethylene ester derivative, a lower alcohol, and a buffer or water into contact with a solution in which a paclitaxel monoglycoside and/or a docetaxel monoglycoside is dissolved in an alkylene glycol-containing buffer or water.

Method for producing liposome encapsulating paclitaxel monoglycoside and/or docetaxel monoglycoside

The object of the invention is to develop baccatin derivatives useful for preparing taxoid compounds such as paclitaxel and a process for the producing the same. The invention provides baccatin derivatives represented by the general formula (I) as well as a process for producing baccatin derivatives represented by the general formula (I) above, which comprises allowing a baccatin represented by the general formula (II) to react with a &bgr;-ketoester in the absence of a catalyst or in the presence of a tin compound or an amine base, preferably under reduced pressure.

Baccatin derivatives and a process for producing the same

Taxoid derivatives and process for producing the same

A taxoid compound represented by general formula (I) ##STR1## where the symbols R.sup.1, R.sup.2, R.sup.3, R.sup.4, Bz, and Ac have specified meanings. Also, a method for producing the taxoid derivative from a baccatin derivative having a .beta.-ketoester group at the 13-position by transesterification and a method for producing taxoid compound such as paclitaxel from the taxoid derivative under mild condition are disclosed.

Taxoid compound and method for producing the same

Disclosed are ursodeoxycholic acid derivatives having an increased solubility in water, and methods for producing the derivatives. To produce the derivatives, ursodeoxycholic acid is protected at its carboxyl group with a benzyl group, then reacted with tetrabenzyl-acetic acid-oxyglucoside of the following formula (1), and de-benzylated; or ursodeoxycholic acid is protected at its hydroxyl group with a t-butyldimethylsilyl group, then reacted with tetrabenzyl-2-hydroxyethyloxyglucoside of the following formula (2), and de-t-butyldimethylsilylated and de-benzylated. ##STR1##

Ursodeoxycholic acid derivatives and methods for producing them

A sugar derivative wherein a hydroxy-carboxylic acid is combined to a position 1 of a sugar via ether linkage, and other hydroxyl groups are protected with a protective groups. A method of producing the sugar derivative, comprises allowing glycolic ester to react with a compound so as to combine said glycolic ester at the position 1 of the sugar skeleton, and then saponifying, said compound has on the position 1 any of hydroxyl group, halogen atom and sulfur atom with a substitutent group, and has other hydroxyl groups being protected with a protective groups.

Process for acylating the 1-position of saccharides

A taxoid derivative wherein sugar is combined with any one of paclitaxel, docetaxel and 10-deacetyl-bacatin III via a spacer. A method of producing the taxoid derivative comprises protecting hydroxyl groups at specific position of paclitaxel or docetaxel by protective compound followed by reacting with tetrabenzyl acetyloxyglucoside, and then carrying out debenzyl and detriethylsilyl reactions. A method of producing the taxoid derivative comprises reacting paclitaxel or docetaxel with tetrabenzyl acetyloxyglucoside, and then carrying out debenzyl reaction.

Taxoid derivative and method of producing thereof

There is provided an unbranched cyclodextrin or a branched cyclodextrin inclusion complex of taxol. The complex is produced by adding an unbranched cyclodextrin of a branched cyclodextrin to taxol at a molar ratio of 1-20 times with respect to taxol. A method is provided for the improvement of the solubility of taxol in water by adding an unbranched cyclodextrin or a branched cyclodextrin thereto at a molar ratio of 1-20 times with respect to taxol. The solubility of taxol in water is improved by the present invention. A cyclodextrin inclusion complex of taxol according to the present invention serves to make taxol more easily absorbed when administered to a cancer patient, which is beneficial to cancer patients and the physiological effects of taxol may therefore be more effectively induced.

Cyclodextrin inclusion complex of taxol, and method for its production

In a method for preparing multiple glucosyl branched-cyclodextrins, a debranching enzyme is contacted to a mixture of maltose or a substance containing maltooligosaccharide such as maltose with a cyclodextrin to obtain a reaction product from which a branched-cyclodextrin is then separated; said branched-cyclodextrin is converted to glycosyl-cyclodextrin under the action of glucoamylase, which is thereafter mixed with maltose or a substance containing maltooligosaccharide such as maltose; and the resulting mixture is successively acted on by a debranching enzyme and glucoamylase.

Method for the preparation of multiple glucosyl branched-cyclodextrins

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Yokohama, Japan

Katsuhiko Mikuni