Abstract: A new method of producing metabolites of tibolone comprising fermenting tibolone with Rhizopus stolonifer (ATCC 12938) resulting in the formation of ?4-Tibolone (C21H28O2), 6?-Hydroxytibolone, and 15?-Hydroxytibolone (C21H28O3) is reported.

Abstract: Method of producing ?5-Tibolone (C21H28O2), 6?-Hydroxy-?4-tibolone (C21H28O3), 6?-Hydroxy-?4-tibolone (C21H28O3), 15?-Hydroxy-?4-tibolone (C21H28O3), 6?-Hydroxy-?1,4-tibolone (C21H28O3) and 6?-Methoxy-?4-tibolone (C22H30O3) contacting tibolone with Gibberella fujikuroi (ATCC 10704) is reported.

Abstract: The present invention relates to novel yeast strains, methods and genetic constructs for their preparation, and their use for the synthesis or modification of steroidal compounds. More particularly, the invention describes strains having a reduced 20?HSD type activity, in particular by modifying the GCY1 and/or YPR1 genes. The yeast strains of the invention make it possible to improve the efficiency of the synthesis or to increase the selectivity or the yields of the method, as well as the quality of the final product. The strains, methods and compounds of the invention are useful in the search for, the development and the production of products with therapeutic or prophylactic activity, in humans or animals, in particular of steroidal derivatives.

Abstract: The present invention provides a method for preparing 20-O-?-D-glucopyranosyl-20(S)-protopanaxadiol (Ginsenoside M1) by using Sanqis leaves and stems. The method of the invention includes the steps of: (a) provides powder of Sanqi leaves and stems; (b) provides a fungus for fermenting the Sanqi leaves and stems, wherein the fermentation temperature is ranged from 20-50° C., the fermentation humidity is ranged from 70-100%, the pH value is ranged from 4.0-6.0, and the fermentation period is ranged from 5-15 days; (c) extracts and collects the fermentation products; and (d) isolates 20-O-?-D-glucopyranosyl-20(S)-protopanaxadiol from the fermentation products.

Abstract: The present invention refers to a new enzymatic process for obtaining 17?-monoesters of cortexolone and/or its 9,11-dehydroderivatives starting from the corresponding 17?,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone 17?-propionate and 9,11-dehydro-cortexolone 17?-butanoate.

Abstract: The present invention relates to a method for preparing 2-alkoxy and 2-aryloxyestrogen compounds, and the intermediate compounds prepared during the use of this method, which intermediate compounds are useful intermediates in the preparation of certain physiologically active compounds.

Abstract: The present invention provides methods for production of one or more sterol compounds. Further provided are methods and systems for producing engineered oleaginous yeast or fungi that are capable of production of one or more sterol compounds, and compositions which utilize the produced sterol compound(s).

Abstract: The present invention provides a method for producing antcin K, zhankuic acid A, zhankuic acid B or zhankuic acid C from the mycelium of the fungus Antrodia cinnamomea by culturing the fungus on a gel medium, harvesting the mycelium and isolating the products by HPLC.

Abstract: The invention relates to ginsenoside glycosidases which hydrolyzes ginsenosides having higher contents in ginsengs so as to prepare rare ginsenosides with high physioloigical activity. Said ginsenoside glycosidases are derived from microorganism cultures, ginseng plants, almonds, wheat brans, malts and animal livers etc., and are categoried to four types depending on their capability of hydrolyzing the sugar moieties of ginsenosides, namely, ginsenoside glycosidase I, ginsenoside glycosidase II, ginsenoside glycosidase III and ginsenoside-?-rhamnosidase. The invention also relates to the uses of the ginsenoside glycosidases in preparing rare ginsenosides.

Abstract: The present invention relates to genetically modified yeast strains autonomously producing, from a simple carbon source, steroids. The invention also relates to a method for producing steroids from such yeast strains.

Abstract: The present invention relates to a method for preparing 2-alkoxy and 2-aryloxyestrogen compounds, and the intermediate compounds prepared during the use of this method, which intermediate compounds are useful intermediates in the preparation of certain physiologically active compounds.

Abstract: The present invention relates to genetically modified yeast strains autonomously producing, from a simple carbon source, steroids. The invention also relates to a method for producing steroids from such yeast strains.

Abstract: The present invention relates to a method for preparing 7-dehydrocholesterol and/or the biosynthetic intermediates and/or secondary products thereof by culturing organisms, in particular yeasts. Furthermore, the invention relates to the preparation of the nucleic acid constructs required for preparing the genetically modified organisms and to said genetically modified organisms, in particular yeasts, themselves.

Abstract: The present invention relates to a method for the production of ergosta-5,7-dienol and/or its biosynthetic intermediates and/or metabolites by culturing genetically modified organisms, and to the genetically modified organisms, in particular yeasts, themselves.

Abstract: Seven new and one known metabolites of tibolone were obtained by incubation of tibolone with various fungi. Their structures were elucidated by means of a homo and heteronuclear 2D NMR and by HREI-MS techniques. The relative stereochemistry was deduced by 2D NOESY experiment. These metabolites of tibolone were strong inhibitors of tyrosine enzyme and thus useful in producing skin lightning and preserving fruits and vegetables.

Abstract: Sixteen new and one known metabolites were obtained by incubation of tibolone and hydroxytibolones with various fungi. Their structures were elucidated by means of a homo and heteronuclear 2D NMR and by HREI-MS techniques. The relative stereochemistry was deduced by 2D NOESY experiment. These metabolites have shown promising inhibitory activities against ?-glucosidase enzyme. Seven metabolites exhibited potent inhibitory activity against the ?-glucosidase enzyme and were thus found useful in the treatment of diabetes mellitus and other diseases related to the activity of ?-glucosidase enzyme.

Abstract: The invention relates to an isolated polynucleotide sequence comprising a nucleic acid sequence encoding the amino acid sequence of KshA protein or of KshB protein, encoded by nucleotides 499-1695 of SEQ ID NO:1 or by nucleotides 387-1427 of SEQ ID NO:2, respectively, and functional homologues thereof. The polynucleotides of the invention can be used to construct genetically modified microorganisms blocked in 3-ketosteroid 9?-hydroxylase activity, which are useful in the microbial degradation of steroids to accumulate certain steroid products.

Abstract: To control the differentiation of mesenchymal stem cells into steroid hormone producing cells. Mesenchymal stem cells can be differentiated into steroid hormone-producing cells by being stimulated by a transcriptional factor (SF-1), preferably by the transcriptional factor (SF-1) and cAMP. The present invention is a method for differentiating mesenchymal stem cells into steroid hormone producing cells, comprising stimulating the mesenchymal stem cells by the transcriptional factor (SF-1). The mesenchymal stem cells may be further stimulated by cAMP.

Abstract: An object of the present invention is to provide a process according to which 5-ene-3-one or 3,6-dione derivatives of sterols can be synthesized with a better yield, as well as a process for production of lipid metabolism improvers, foods, drinks, and animal feeds containing the 5-ene-3-one or 3,6-dione derivatives of sterols. The process for production of 5-ene-3-one or 3,6-dione derivatives of sterols of the present invention involves preparing a culturing solution containing an Arthrobacter bacterium, which is a microorganism exhibiting a cholesterol oxidase activity, and then, adding to the culturing solution an equivalent amount of hexane so as to prepare a bilayer solution consisting of an aqueous layer and a hydrocarbon-based solvent layer. Thereafter, sterol, or a derivative thereof, is made as a substrate contained therein, a reaction performed with cholesterol oxidase at 30° C. for 2 days, and, ethanol then added to separate a hydrocarbon-based solvent layer.

Abstract: The invention relates to an isolated polynucleotide sequence comprising a nucleic acid sequence encoding the amino acid sequence of KshA protein or of KshB protein, encoded by nucleotides 499-1695 of SEQ ID NO:1 or by nucleotides 387-1427 of SEQ ID NO:2, respectively, and functional homologues thereof. The polynucleotides of the invention can be used to construct genetically modified microorganisms blocked in 3-ketosteroid 9?-hydroxylase activity, which are useful in the microbial degradation of steroids to accumulate certain steroid products.

Abstract: A process to produce 19-nor-10?-carboxylic acids by fungal oxidation of 6-substituted-?6-pregnanes is disclosed.

Abstract: The present invention can be a method to prepare a glycosylated natural product or pharmaceutical from either a BocO-pyranone or a BocO-enone. The identical methods of production utilize catalytic palladium and catalytic amounts of phosphine ligand to place the desired group stereospecifically at the C-1 position. The natural product can be the compound digitoxin. Post-glycosylation reactions can add H, OH, F, Cl, Br, I, NH2, NHAc, CN, or N3 on C-2, C-3, or C-4 and C-6 can be any alkyl, aryl, heteroalkyl, hydroxyalkyl groups with any amino, halo or hydroxyl substitution. A further aspect of the present invention can be a method to prepare either BocO-pyranone or BocO-enone.

Abstract: In a preferred embodiment, a pipettor head, including: a body; one or more solenoid valves disposed in the body; each one or more solenoid valves having an outlet at a lower end and an inlet at an upper end; each one or more solenoid valves having an outlet attached to a dispensing passageway; each one or more solenoid valves having its inlet attached to a standpipe; and the standpipe having an open top communicating with an interior of a closed vacuum/pressure chamber defined in the pipettor head, the closed vacuum/pressure chamber being arranged such that vacuum or pressure may be selectively applied to the closed vacuum/pressure chamber. A method of using the pipettor head is also provided.

Abstract: Disclosed is a microorganism having an excellent ability to convert sterol into and rost-4-ene-3,17-dione (AD) and androsta-1,4-diene-3,17-dione (ADD), a method for preparation of the microorganism and use thereof, and more particularly, a mutant strain of Mycobacterium fortuitum ATCC 29472, Mycobacterium fortuitum EUG-119, a method for preparation of the mutant and use thereof in preparing AD and ADD. The mutant of the present invention has an excellent ability to convent sterol into AD and ADD which are steroid hormone precursors, compared with the known microorganisms and accordingly, is very useful for mass production of steroid hormones.

Abstract: The present invention relates to a method for preparation of androst-4-ene-3,17-dione (AD) and androsta-1,4-diene-3,17-dione (ADD). More particularly, the present invention relates to a method for preparing AD/ADD, comprising the steps of: (a) heating sterols and emulsifier respectively, to dissolve completely and mixing to prepare a mixture; (b) placing the mixture in a water bath at 70˜90° C. and stirring to obtain emulsified sterols; and (c) adding the emulsified sterols to culture media of microorganism as a component. And the present invention relates to a method for preparing AD/ADD, comprising the addition of cyclodextrin-sterol complexes extracted from milk to culture media of microorganism as a component. The emulsified sterols and cyclodextrin-sterol complexes adopted in the present invention can be easily prepared and be effectively used for obtaining AD/ADD at a high yield.

Abstract: The present invention provides a protein having saponin-decomposing activity, more specifically a protein which can decompose a glycoside having soyasapogenol B as an aglycone to produce soyasapogenol B, a polynucleotide encoding such a protein, and a method of producing soyasapogenol B on a large scale using the same. A protein according to the present invention are concerned with (a), (b) or (c), namely (a) a protein comprising an amino acid sequence selected from the group consisting of the amino acid sequences shown in SEQ ID NOs: 2, 4, and 6; (b) a protein that has at least 50% homology to the protein comprising the amino acid sequence of the sequence described in (a) and having saponin-decomposing activity; or (c) a protein comprising a modified amino acid sequence of the sequence described in (a) that has one or more amino acid residues deleted, substituted, inserted, or added and having saponin-decomposing activity.

Abstract: The present invention is related to a process for selectively transesterifying stanols in mixtures comprising sterols and stanols, and a process for separating sterols from said mixtures. The process of selective transesterification comprises the forming of a reacting mixture by contacting a selective lipase with a reactant mixture comprising sterols and stanols and an ester selected from the group consisting of esters of an organic acid with a short chain aliphatic alcohol. The transetrifying is carried out agitated reactors at pressures below atmospheric pressure and temperatures from 30 to 90° C.

Abstract: A process for producing steryl or stanyl esters, comprises the steps of: a) forming a reacting mixture by contacting a lipase with a reactant mixture wherein the reactant mixture comprise sterols or stanols and one or more esters selected from the group consisting of esters of a fatty acid with a short chain aliphatic alcohol; b) separating the lipase from the reacting mixture to form a reacted mixture; and c) separating steryl or stanyl esters from the reacted mixture. The reaction is carried out in stirred reactors at pressures below atmospheric pressure and temperatures from 30 to 90° C. The separation of esters from the reacted mixtures is carried out by distillation at low pressures. A process for esterifying sterols or stanols comprise forming a reacting mixture by contacting a lipase with a reactant mixture wherein the reactant mixture comprise sterols or stanols and one or more esters selected from the group consisting of esters of a fatty acid with a short chain aliphatic alcohol.

Abstract: The present invention provides a protein having saponin-decomposing activity, more specifically a protein which can decompose a glycoside having soyasapogenol B as an aglycone to produce soyasapogenol B, a polynucleotide encoding such a protein, and a method of producing soyasapogenol B on a large scale using the same. A protein according to the present invention are concerned with (a), (b) or (c), namely (a) a protein comprising an amino acid sequence selected from the group consisting of the amino acid sequences shown in SEQ ID NOs: 2, 4, and 6; (b) a protein that has at least 50% homology to the protein comprising the amino acid sequence of the sequence described in (a) and having saponin-decomposing activity; or (c) a protein comprising a modified amino acid sequence of the sequence described in (a) that has one or more amino acid residues deleted, substituted, inserted, or added and having saponin-decomposing activity.

Abstract: An objective of the present invention is to provide a method of producing soyasapogenol B and to provide novel microorganisms. The present invention provides a method of producing soyasapogenol B comprising the steps of culturing microorganisms that belong to genus Neocosmospora or genus Eupenicillium, in a medium containing a glycoside having soyasapogenol B as an aglycone, and then collecting soyasapogenol B from the resulting culture.

Abstract: The present invention is a novel process for the transformation of 17&agr;-hydroxy-6&agr;-methylpregn-4-ene-3,20-dione 17-acetate (I) to 11&bgr;,17&agr;,21-trihydroxy-6&agr;-methylpregna-1,4-diene-3,20-dione 21-acetate (VI)

Abstract: A process for the production of ergosterol and its intermediate products using recombinant yeasts and plasmids for transformation of yeasts is described.

Abstract: 7&agr;-Hydroxy-pregn-4-en-3-one-20-carbaldehyde, a production method thereof and a method for producing 7&agr;,21-dihydroxy-20-methyl-pregn-4-en-3-one, which is useful as a synthetic intermediate for pharmaceuticals such as squalamine and the like, efficiently at high purity from the carbaldehyde.

Abstract: A process to produce 19-nor-10&bgr;-carboxylic acids by fungal oxidation of 6-substituted-&Dgr;6-pregnanes is disclosed.

Abstract: The present invention provides a protein having saponin-decomposing activity, more specifically a protein which can decompose a glycoside having soyasapogenol B as an aglycone to produce soyasapogenol B, a polynucleotide encoding such a protein, and a method of producing soyasapogenol B on a large scale using the same. A protein according to the present invention are concerned with (a), (b) or (c), namely (a) a protein comprising an amino acid sequence selected from the group consisting of the amino acid sequences shown in SEQ ID NOs: 2, 4, and 6; (b) a protein that has at least 50% homology to the protein comprising the amino acid sequence of the sequence described in (a) and having saponin-decomposing activity; or (c) a protein comprising a modified amino acid sequence of the sequence described in (a) that has one or more amino acid residues deleted, substituted, inserted, or added and having saponin-decomposing activity.

Abstract: The present invention relates to a method for preparation of androst-4-ene-3,17-dione (AD) and androsta-1,4-diene-3,17-dione (ADD). More particularly, the present invention relates to a method for preparing AD/ADD, comprising the steps of: (a) heating sterols and emulsifier respectively, to dissolve completely and mixing to prepare a mixture; (b) placing the mixture in a water bath at 70˜90° C. and stirring to obtain emulsified sterols; and (c) adding the emulsified sterols to culture media of microorganism as a component. And the present invention relates to a method for preparing AD/ADD, comprising the addition of cyclodextrin-sterol complexes extracted from milk to culture media of microorganism as a component. The emulsified sterols and cyclodextrin-sterol complexes adopted in the present invention can be easily prepared and be effectively used for obtaining AD/ADD at a high yield.

Abstract: The present invention relates to novel yeast strains, methods and genetic constructs for their preparation, and their use for the synthesis or modification of steroidal compounds. More particularly, the invention describes strains having a reduced 20&agr;HSD type activity, in particular by modifying the GCY1 and/or YPR1 genes. The yeast strains of the invention make it possible to improve the efficiency of the synthesis or to increase the selectivity or the yields of the method, as well as the quality of the final product. The strains, methods and compounds of the invention are useful in the search for, the development and the production of products with therapeutic or prophylactic activity, in humans or animals, in particular of steroidal derivatives.

Abstract: The invention relates to a process for the production of 4-(17&agr;-methyl-substituted 3-oxoestra-4,9-dien-11&bgr;-yl)benzaldehyde-(1E or 1Z)-oximes of general formula (I), in which R1 is a hydrogen atom, a C1-6-alkyl radical or a CnF2n+1 radical, whereby n is 1, 2 or 3, R2 is a C1-4-alkyl radical, X is an OH group in E- or Z-position, and Y is an OC1-6-alkyl group, an SC1-6-alkyl group or an OCH2CnF2+1 group, whereby n is 1, 2 or 3, which provides the target compounds of formula (I) with a high yield and good selectivity.

Abstract: An objective of the present invention is to provide a method of producing soyasapogenol B and to provide novel microorganisms. The present invention provides a method of producing soyasapogenol B comprising the steps of culturing microorganisms that belong to genus Neocosmospora or genus Eupenicillium, in a medium containing a glycoside having soyasapogenol B as an aglycone, and then collecting soyasapogenol B from the resulting culture.

Abstract: Methods for modulating amyloid deposition in a subject are described. An effective amount of at least one ATP binding cassette (ABC) transporter blocker is administered to a subject, such that modulation of amyloid deposition occurs. Methods also include administering and effective amount of at least one ABC transporter blocker, or a pharmaceutically acceptable salt thereof, to a subject such that a disease state associated with amyloidosis is treated. Packaged pharmaceutical compositions for treating amyloidosis are described. The package includes a container for holding an effective amount of a pharmaceutical composition and instructions for using the pharmaceutical composition for treatment of amyloidosis. The pharmaceutical composition includes at least one ABC blocker for modulating amyloid deposition in a subject. Methods for identifying agents which modulate amyloid deposition in a subject are also described.

Abstract: An expression cassette, operable in a recombinant host, comprising a heterologous DNA coding sequence encoding a protein, which is functional, alone or in cooperation with one or more additional proteins of catalyzing an oxidation step in the biological pathway, for conversion of cholesterol into hydrocortisone, which step is selected from the group consisting of: the conversion of cholesterol to pregnenolone; the conversion of pregnenolone to progesterone; the conversion of progesterone to 17&agr;-hydroxyprogesterone; the conversion of 17&agr;-hydroxyprogesterone to cortexolone; the conversion of cortexolone to hydrocortisone, and the corresponding control sequences effective in that host.

Abstract: The invention relates to a new synthesis intermediate product of formula I 1

Abstract: A novel cholesterol oxidase is disclosed. The enzyme according to the present invention has the following properties: acts on cholesterol to convert it to cholest-5-en-3-one; acts 3&bgr;-sterols but not on 3&agr;-hydroxysteroids; optimum pH: 5.0-8.5; and stable pH: 4 to 11. This enzyme carries out the oxidation reaction at high velocity at low substrate concentrations, reacts in a broad pH range, is heat resistant, and reacts at high reaction velocity even in the presence of an organic solvent. The enzyme according to the present invention is useful as a reagent for measuring cholesterol concentration, as a composition for the extermination of harmful insects, and as a bleaching agent.

Abstract: A method of chromatographic isolation for non-glyceride components (squalenes, carotenes, vitamin E, sterols and/or the like) from a non-glyceride components-comprising compound by the steps of a. introducing the non-glyceride components-comprising compound onto a selective adsorbent to allow an adsorption of the non-glyceride components, and subsequently b. desorbing the non-glyceride components from the adsorbent, wherein the adsorption and/or desorption of the non-glyceride components is carried out under a supercritical fluid environment.

Abstract: The present invention is related to a process for selectively transesterifying stanols in mixtures comprising sterols and stanols, and a process for separating sterols from said mixtures.

Abstract: A process for producing steryl or stanyl esters, comprises the steps of:

Abstract: The present invention is a novel process for the transformation of 17&agr;-hydroxy-6&agr;-methylpregn-4-ene-3,20-dione 17-acetate (I) 1

Abstract: A process for the preparation of desglucodesrhamnoruscin which comprises the hydrolysis of Ruscus Aculeatus steroid glycosides (ruscosaponins) through fermentation of a substrate containing said glycosides by means of fungi of the aspergillus niger species.

Abstract: The present invention provides a new bioactive compound of formula (I), which has an antimicrobial activity against pathogenic microorganisms, and a process for production thereof. Also provided are a pharmaceutical composition comprising the compound and pharmaceutically acceptable carrier, a use of the WF002 as a medicament and use of the compound for manufacture of the medicament for treatment of infectious disease.

Abstract: A method for restoring immunoreactivity of a tissue, particularly decalcified tissue, fixed width an aldehyde fixative agent and embedded in an embedding medium, usually comprising celloidin, the method comprising the steps of contacting the tissue with an aldehyde releasing reagent solution comprising a solvent and an aldehyde releasing reagent and removing aldehyde released by the aldehyde releasing reagent from contact with the tissue by reacting the aldehyde in a substantially irreversible manner to form a non-aldehyde derivative, and removing excess base from the tissue. A preferred solution for celloidin-embedded decalcified tissue comprises methanolic sodium hydroxide at about one-third saturation.