Institute of Applied Biochemistry

Kabushiki Kaisha Vitamin Kenkyusyo

Kabushiki Kaisha Vitamin Kenkyuso

Other

Kabushiki Kaisha Vitamin Kenkyusho

Kabushiki Kaisha Vitamin Kenkyusya

Institute of Applied Biochemistry Gifu-ken

Kunio Yagi

Nobuko Ohishi

Masayasu Kurono

Takehiko Suzuki

Tomio Ogasawara

Takafumi Iida

Hitoshi Noda

Sadaaki Komura

Naoko Ishida

Takuya Koshizaka

Jun Yoshida

Katsuhiro Hayashi

Hideshi Ideno

Hidehumi Yamakawa

Takehiko Susuki

Eiichi Kato

Mariko Kitoh

Hidefumi Yamakawa

Keizo Sakuda

Makoto Takano

Nakao Kojma

Hiroaki Kodama

Haruyoshi Yajima

Yasuyuki Shimohigashi

It provides a gene-entrapping liposome preparation which can be preserved over a long period of time, and a process for the preparation of the same. The preparation can be prepared by adding an aqueous solution of disaccharide to gene-entrapping liposomes. The frozen preparation can be preserved for 6 months or more at preservation temperature of &minus;20&deg; C., and the preparation shows excellent restoration ability in water and does not show reduction in biological activity. In the case of the lyophilized preparation, it can be preserved for longer time of about 1 year, shows excellent restoration ability in water, and does not show reduction in biological activity.

Gene-entrapped liposomes preparation and process for the preparation thereof

There are disclosed a composition containing 9-cis .beta.-carotene in high-purity and an industrially applicable method of obtaining the same from an alga. The composition can be obtained through steps of washing with ethanol dry powder of the alga belonging to Dunaliella, adding hexane to the washed algal powder, stirring the same, subjecting the same to filtration to obtain a filtrate, concentrating the filtrate to obtain a semi-solidic concentrate, adding hexane to the semi-solidic concentrate in an amount of 10-18 ml of hexane to 1 g of the semi-solidic concentrate, stirring the same, subjecting the same to filtration to obtain a filtrate, concentrating the filtrate to obtain an oily concentrate, adding hexane to the oily concentrate in an amount of 2-4.5 ml of hexane to 1 g of the oily concentrate to dissolve the same, and leaving the solution, as it is, under lower temperature condition to cause a separation of the composition. The composition is a rubiginous powder or crystals and contains 9-cis .beta.-carotene in an amount of 75% or more to total amount of the composition.

Method of obtaining a composition containing 9-cis .beta.-carotene in

A plasmid entrapping multilamellar liposome for introducing a gene into cells, which liposome has constitutive lipids of N-(.alpha.-trimethylammonioacetyl)-didodecyl-D-glutamate chloride (TMAG); dioctanoylphosphatidyl choline (DOPC) or didecanoylphosphatidyl choline (DDPC); and dioleoylphosphatidyl ethanolamine (DOPE) or dilauroylphosphatidyl ethanolamine (DLPE) and in a molar ratio of 1:2-3:2-1 in case of lipid combination of TMAG, DOPC and DOPE, or 1:2:2 in case of lipid combination of TMAG, DDPC or DOPC and DLPE.

Plasmid entrapping multilamellar liposomes

There are described novel glycosides of catechol estrogen, a method of preparing the same, and a medicament comprising one of the glycosides as an active ingredient. The glycosides are shown by the formula of ##STR1## wherein X is carbonyl group or ##STR2## R.sub.10 is hydroxyl group or glycosyloxy group, and R.sub.2 is a hydrogen atom or ethynyl group; R.sub.11 is a hydrogen atom, hydroxyl group, or glycosyloxy group; R.sub.12 is hydroxyl group or glycosyloxy group; and R.sub.13 is hydroxyl group or glycosyloxy group, in which glycosyloxy group is selected from the group consisting of glycosyloxy, galactosyloxy, mannosyloxy, arabinosyloxy, ribosyloxy, xylosyloxy, fructosyloxy, rhamnosyloxy, fucosyloxy, maltosyloxy, cellobiosyloxy, lactosyloxy, sucrosyloxy, maltotriosyloxy, maltotetraosyloxy, maltopentaosyloxy, maltohexaosyloxy, maltoheptaosyloxy, and sialosyloxy, and in this case, at least one of R.sub.10, R.sub.11, R.sub.12, and R.sub.13 is glycosyloxy group as defined above.

Manufacture and use of novel glycosides of catechol estrogens

For increasing gene entrapping efficiency, it is preferable that liposome membrane to be formed is positively charged. For this purpose, a lipid with quaternary amine has been employed as one of constitutional lipids, but the such lipid may show toxicity to cells to be transformed with the gene for expression. The invention selects, as constitutional lipids for liposomes, N-(.alpha.-trimethylammonioacetyl)-didodecyl-D-glutamate chloride (TMAG), dilauroylphosphatidylcholine (DLPC), and dioleoylphosphatidylethanolamine (DOPE) with molar ratio of 1:2:2, and vortex treatment for preparing the liposomes with multi-layers to entrap the gene therein.

Liposome for entrapping gene, liposomal preparation and process for the

There are described novel glycosides of catechol estrogen, a method of preparing the same, and a medicament comprising one of the glycosides as an active ingredient. The glycosides are shown by the formula of ##STR1## wherein X is carbonyl group or ##STR2## R.sub.10 is hydroxyl group or glycosyloxy group, and R.sub.2 is a hydrogen atom or ethynyl group; R.sub.11 is a hydrogen atom, hydroxyl group, or glycosyloxy group; R.sub.12 is hydroxyl group or glycosyloxy group; and R.sub.13 is hydroxyl group or glycosyloxy group,

Glycosides of catechol estrogens

The invention relates to enkephalin analogs of the formula ##STR1## wherein in case of X is D-Val, D-Phe, Pro, D-Met, D-Met(O), D-Leu, D-Glu, D-Glu(Obzl), D-Lys, D-Lys(Z), or D-Arg,

Enkephalin analogs

The present invention relates to intermediates for synthesizing BH.sub.4 and derivatives thereof. The intermediates are shown as follows; ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl, aralkyl, or aryl group; R.sub.2 is an alkyl, hydroxyalkyl, or polyhydroxyalkyl group; R.sub.3 and R.sub.4 are the same or different and represent alkyl, aralkyl, or aryl group; R.sub.5, R.sub.6, R.sub.7, and R.sub.8 are the same or different and represent a hydrogen atom or acyl group; R.sub.9 is an alkyl, aralkyl, or aryl group; R.sub.10 and R.sub.11 are the same or different and represent a hydrogen atom or acyl group; n is an integer of 5 or less; and HX is an acid. The invention also relates to a process for the preparation of L-biopterin.

Intermediates for synthesizing BH.sub.4 and its derivatives

An agent for inhibiting the binding of 5.alpha.-dihydrotestosterone with androgen receptor, which comprises at least one extract from herbs or one of specific xanthone compounds, and a process for obtaining the agent.

Agent for inhibiting binding of 5-dihydro-testosterone with androgen

The present invention relates to intermediates for synthesizing BH.sub.4 and derivatives thereof. The intermediates are shown as follows: ##STR1## wherein R.sub.1 is a hydrogen atom, alkyl, aralkyl, or aryl group; R.sub.2 is an alkyl, hydroxyalkyl, or polyhydroxyalkyl group; R.sub.3 and R.sub.4 are the same or different and represent alkyl, aralkyl, or aryl group; R.sub.5, R.sub.6, R.sub.7, and R.sub.8 are the same or different and represent a hydrogen atom or acyl group; R.sub.9 is an alkyl, aralkyl, or aryl group; R.sub.10 and R.sub.11 are the same or different and represent a hydrogen atom or acyl group; n is an integer of 5 or less; and HX is an acid. The invention also relates to a process for the preparation of L-biopterin.

Some of antineoplastic agents, for instance, adriamycin and daunorubicin, have a positive charge at physiological pH. Such drugs possess high affinity for binding to steroidal sulfate by means of electrostatic force. The invention utilizes this property to prepare steroidal sulfate liposomes having a net negative charge and encapsulating the antineoplastic agent.

Antineoplastic agent-entrapping liposomes

A liposome preparation entrapping adriamycin as the effective component, whose constitutional lipids are phosphatidylcholine, cholesterol, and sulfatide in a specific molar ratio.

Adriamycin-entrapping liposome preparation

A novel resolution method of a racemic mixture, wherein four kinds of salts are dissolved in a resolving solvent to fractionally crystallize a desired optically active isomer through an exchange reaction between counter ions.

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Nagoya, Japan

Kunio Yagi