Abstract: A plasticization device includes: a rotor rotated by a drive motor and having a groove forming surface in which a first groove portion is formed along a rotation direction; a rotor case configured to accommodate the rotor; a barrel facing the groove forming surface and having a through hole; a first heating unit configured to heat the rotor or the barrel; and a cooling mechanism configured to cool a side surface of the rotor. In the plasticization device, a material supplied between the first groove portion and the barrel is plasticized by rotation of the rotor and heating by the first heating unit to flow out from the through hole, and the side surface of the rotor has a material guiding port configured to guide the material to the first groove portion, and a second groove portion configured to feed the material supplied between the rotor and the rotor case to the material guiding port.

Abstract: Recombinant DNA techniques are used to produce oleaginous recombinant cells that produce triglyceride oils having desired fatty acid profiles and regiospecific or stereospecific profiles. Genes manipulated include those encoding stearoyl-ACP desturase, delta 12 fatty acid desaturase, acyl-ACP thioesterase, ketoacyl-ACP synthase, and lysophosphatidic acid acyltransferase. The oil produced can have enhanced oxidative or thermal stability, or can be useful as a frying oil, shortening, roll-in shortening, tempering fat, cocoa butter replacement, as a lubricant, or as a feedstock for various chemical processes. The fatty acid profile can be enriched in midchain profiles or the oil can be enriched in triglycerides of the saturated-unsatturated-saturated type.

Abstract: The present invention relates to steroidal ligands for use in nuclear receptor-based inducible gene expression systems. The invention further relates to methods of modulating the expression of genes of interest with a system containing one or more nuclear receptor complexes and one or more steroidal ligands. Further aspects include ligand compositions including therapeutic compositions.

Abstract: Disclosed are the isolation, purification and analysis of the triterpenoid compositions (including ergostane and lanostane) in the fruiting body of Antrodia cinnamomea using HPLC and NMR, as well as the stereo structures and the amounts of the triterpenoid compositions. The cytotoxicity of triterpenoids is also revealed. Based on the aforementioned techniques, the presence and amounts of ergostane and lanostane in the drugs, healthcare food or other goods are able to be detected.

Abstract: [Problem to be Solved] An immunostimulant highly safe and administrable for a long period of time as well as a pharmaceutical composition containing the immunostimulant as an active ingredient and drink or food products for immunostimulation are developed and provided. [Solution] An immunostimulant containing a compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient is provided. R1 is a hydrogen atom or a substituted or unsubstituted alkyl group having 1 to 6 carbon atoms, R2 to R5 are independently a hydrogen atom, or a substituted or unsubstituted lower alkyl or lower acyl group, X is —(CH2)2—, —(CH2)3—, —(CH2)4—, —CO—CH2—, —CO—(CH2)2—, —CO—(CH2)3—, —CH2—CO—CH2—, —CO—O—CH2—, —CO—O—(CH2)2—, —O—CO—CH2—, —O—CO—(CH2)2—, —CH2—O—CH2—, —CH2—O—(CH2)2—, —O—CH2—, —O—(CH2)2—, —O—(CH2)3—, —NHY—CO—CH2—, —NHYCO—(CH2)2—, —CO—NHY—CH2— or —CO—NHY—(CH2)2—, Y herein is a hydrogen atom or a lower alkyl group.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: There is disclosed a method for isolation and purification of phytosterols from tall oil pitch comprising the steps of: a) contacting the tall oil pitch with a solvent to form a tall oil solvent mixture; b) separating the tall oil pitch solvent mixture in at least two separate streams wherein one process stream is enriched in acidic pitch components and a second stream enriched in free- and bound sterols in the form of steryl esters; c) subjecting the stream enriched in free- and steryl esters to treatment with an alcohol under transesterification conditions wherein a reaction mixture is formed and sterols comprising the steryl esters are liberated as free sterols; and d) separating the free sterols from the reaction mixture of step c) by crystallization and extraction with one or more solvents. There are disclosed free fatty acids and resin acids separated from the tall oil pitch. Moreover, there is disclosed a manufacture and separation of fatty acid alkyl esters by the method.

Abstract: Salt sensitivity is measured as a function of the urinary 25-OHD binding activity, which may be evaluated by measuring 25-hydroxyvitamin D binding activity using radiolabeled 25-hydroxyvitamin D3. High binding activity is indicative of salt sensitivity and is an important predictor for development of salt-sensitivity related hypertension.

Abstract: For reducing the negative effects of the metabolic syndrome on mammal organisms, it is proposed to use phytoecdysones for diminishing the fat body mass in individuals, notably with a weight excess. Phytoecdysones are advantageously incorporated into a food composition. The phytoecdysones can come from food plants, such as quinoa.

Abstract: The subject application provides an aqueous composition suitable for use as an artificial tear solution comprising one or more lipids produced by an enzyme of the diacylglycerol acyltransferase 2 (DGAT2) family and/or the acyl-CoA cholesterol acytransferase (ACAT) family. This invention also provides related methods.

Abstract: The present invention relates to natural brassinosteroids of general formula (I), wherein R is CH2 or O—CH2 group, R2 is hydrogen or hydroxyl, R3 is hydroxyl, R24 is alkyl or alkenyl, which are selected from the group consisting of methyl, ethyl, propyl, isopropyl, methylen, ethylen and propylen, and R25 is alkyl selected from the group consisting of methyl and ethyl, and a pharmaceutically acceptable salt thereof, for use for treating hyperproliferation, treating proliferative diseases and reducing adverse effects of steroid dysfunction in mammals. The present invention also provides methods capable to arrest of the cell cycle by natural brassinosteroids resulting in apoptotic changes in cancer cells. More specifically, the present invention relates to use for treatment of the adverse effects of hyperproliferation on mammalian cells in vitro and in vivo, especially treatment of hyperproliferative diseases in mammals by administering compositions containing natural brassinosteroids.

Abstract: A method for producing dihydrocucurbitacin F-25-0-acetate consisting of the steps as followed: percolating radix hemsleyae using acetone as solvents to obtain extract; eluting the extract in silica gel column using chloroform: methanol as eluting agent (gradient) to obtain the crude; recrystallizating the crude using methanol or ethanol to obtain di-hydrocucurbitacin F-25-O-acetate (purity:>98%). And the use of dihydrocucurbitacin F-25-O-acetate in the manufacture of medicaments for treating cancers of liver, lung, stomach, larynx, prostate and leukemia.

Abstract: The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof wherein R is a corticosteroid residue selected from: The compounds are useful in the treatment of respiratory diseases.

Abstract: The present invention provides crystals of the compound represented by formula (I): crystals of a vitamin D derivative which are obtained by purifying a crude or preliminarily purified product of the vitamin D derivative through a reverse phase chromatography and then crystallizing the purified derivative from an organic solvent; novel compounds which are formed during the synthesis of a vitamin D derivative as by-product; and a method for purifying a vitamin D derivative or the precursor thereof. The method of the present invention makes it possible to supply a highly purified vitamin D derivative, especially ED-71, in bulk and steadily.

Abstract: The present invention is a di-steroidal prodrug of estradiol having the following formula:

Abstract: The present invention is a di-steroidal prodrug of ethinyl estradiol according to formula I:

Abstract: Compounds of formula (I) in which: R1 represents a hydrogen atom or an O-protecting group; R2 represents a hydroxyl, lower alkoxy, carboxaldehyde, lower alk-1-enyl or hydroxy- or lower alkoxy-substituted lower alkyl group; R3 represents a methyl group having ?- or ?-configuration; X represents a C1-3 alkylene group or a valence bond; Y represents a carboxaldehyde group or a group of formula —C(R4)(R5)OR1 where R1 is as defined above and R4 and R5, which may be the same or different, are each selected from hydrogen atoms, alkyl, alkenyl and alkynyl groups such that the total carbon content of R4 and R5 does not exceed three atoms, with the proviso that X is a valence bond when both R4 and R5 are other than hydrogen; and the dotted line signifies that a double bond may optionally be present at the 16(17)-position exhibit potent cell modulating activity, including antiproliferative and antiangiogenic effects.

Abstract: Compounds of Formula (I) in which: R1 and R2, which may be the same or different, each represents a lower alkyl, alkenyl or alkynyl group; R3 represents a methyl group having ?- or ?-configuration; R4 represents a hydrogen atom or an etherifying or esterifying group; R5 represents a hydrogen atom, a hydroxyl group or a lower alkoxy group; X represents a group OR4, wherein R4 is as defined above, or a group NR6R7 wherein R6 represents a hydrogen atom, an aliphatic or araliphatic organic group, or an acyl group comprising an aliphatic, araliphatic or aryl organic group linked to the nitrogen atom by way of a carbonyl group; and R7 is a hydrogen atom or a lower alkyl group; Y represents a lower alkylene, alkenylene or alkynylene group optionally substituted by a hydroxyl, etherified hydroxyl or esterified hydroxyl group; and the dotted lines signify that double bonds may be present at the 16(17)-position and/or either at the 6(7)- and 8(9)-positions or at the 7(8)-position exhibit potent effects on modulation of

Abstract: A liver-targeting active compound has the general formula (I):- wherein A is &agr;-OH or &bgr;-OH, B is &agr;-H or &bgr;-H, C is —H, &agr;-OH or &bgr;-OH, or B and C together form a double bond, D is —H, &agr;-OH or &bgr;-OH, E is —H, &agr;-OH or &bgr;-OH, —G-is a side chain moiety, —NH—J is selected from (i) a residue of an amino group-containing active compound wherein said —NH— group is provided by said amino group of the active compound, and (ii) a residue of an active compound to which an amino group has been added wherein said —NH— group is provided by said added amino group; each of X and Y independently represents a single bond, —(CH2)z— (where z is 1 to 8), —O— or —S—; n is 0 or 1; m is 0 or 1; and p is 0 or 1; provided that, when —NH—J is (i), m is 1. A method of producing such as compound is also disclosed.

Abstract: Analysis of full-blood glucose, serum insulin, serum triglycerides and total serum cholesterol were performed. Glucose levels in blood samples from the oral glucose tolerance test were used for calculation of the incremental Area Under the Curve (AUC0-120 min−baseline). All data are expressed as percentage change of vehicle treated animals (cf. FIGS. 1 and 2).

Abstract: The present invention provides crystals of the compound represented by formula (I): 1

Abstract: Certain novel sterol derivatives having no hydroxy group in the 3-position can be used to regulate the meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives.

Abstract: Compound of formula I: wherein the R groups are as defined by the specification. The compounds are useful in the inhibition of HIV integrase, the treatment of infection of HIV and treatment of AIDS.

Abstract: Disclosed are compositions and methods for promoting plant growth. The compounds are cyclopropyl-, cyclobutyl-, and cyclopentyl-substituted brassinosteroids having high growth promoting ability. They may be used alone or in combination with other plant growth regulating agents.

Abstract: Disclosed are compositions and methods for promoting plant growth. The compounds are cyclopropyl- and cyclobutyl-substituted brassinosteroids having high growth promoting ability. They may be used alone or in combination with other plant growth regulating agents.

Abstract: A process for the production of a compound of formula (II), which comprises reacting an epoxy compound of formula (I) with an alcohol, wherein the reaction is carried out under a basic condition. ##STR1## R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are as defined in the specification. The compounds are useful intermediates for the production of vitamin D.sub.3 derivatives.

Abstract: A compound of the formula ##STR1## having progestomimetic activity, wherein the substituents are as defined in the specification and compositions of a compound of formula I and an estrogen compound.

Abstract: The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.

Abstract: Steroid compounds of the contignasterol family, including stereoisomers and pharmaceutically acceptable salts, as well as compositions containing these materials and a pharmaceutically acceptable carrier, are disclosed. The steroid compounds have a 3.alpha.-hydroxyl, a 4.beta.-hydroxyl, a 6.alpha.-hydroxyl, a 7.beta.-hydroxyl, a 15-ketone, a trans A/B ring juncture and a cis or trans C/D ring juncture. The compounds and compositions may be used, for example, for the prevention of inflammatory or allergic reactions, or the treatment of cardiovascular or haemodynamic disorders.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.

Abstract: A method is provided for isolating 5,7-diene-containing steroids, particularly 3.beta.-ols and esters of 3.beta.-ols, from a sterol mixture. The method involves (1) treating the mixture with a dienophile or with an oxidizable dienophile precursor in combination with an oxidizing agent so as to provide a Diels-Alder adduct of the 5,7-diene to be isolated, followed by (2) removal of the adduct from the mixture and (3) regeneration of the 5,7-diene with a suitable reducing agent. The invention also encompasses subsequent purification steps and intermediate modification of the Diels-Alder intermediate, e.g., wherein chemical conversion of the Diels-Alder adduct is effected prior to regeneration of the 5,7-diene. Novel compounds which are Diels-Alder adducts of 5,7-diene-containing steroids are provided as well.

Abstract: There are provided pregnane derivatives represented by formula ##STR1## wherein A.sup.1 represents a hydrogen atom or a hydroxyl group, A.sup.2 represents a substituent such as a hydroxyl group when A.sup.1 represents a hydrogen atom, or A.sup.2 represents a hydrogen atom when A.sup.1 represents a hydroxyl group, or A.sup.1 and A.sup.2 are combined together to form an oxo group; D.sup.1 represents a substituent such as a hydroxyl group, and D.sup.2 represents a hydrogen atom, or D.sup.1 and D.sup.2 are combined together to form an epoxy group or a single bond; D.sup.3, D.sup.5 and D.sup.7 each represents a hydrogen atom, D.sup.4 represents a hydroxyl group, and D.sup.6 represents a substituent such as a hydroxyl group, or D.sup.3 and D.sup.4 may be combined together to form an epoxy group or a single bond, or D.sup.4 and D.sup.5 may be combined together to form a single bond, or D.sup.5 and D.sup.6 may be combined together to form an epoxy group or a single bond, or D.sup.6 and D.sup.

Abstract: The process of the invention comprises reacting a C-22-halo-23,24-bisnorsteroid or C-22-halo-23,24-bisnor-9,10-secosteroid with a nickel complex of an electron withdrawing alkene of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxycarbonyl, lower alkoxycarbonyl, lower alkylcarbonyl or unsubstituted or substituted lower alkyl, and R.sub.2 is hydroxyl, lower alkoxy, or unsubstituted or substituted lower alkyl, to yield a C-25 or C-26 precursor of the formula ##STR2## which is appropriately functionalized for conversion into the corresponding steroid or secosteroid by treatment as hereinafter described.

Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.A, R.sub.A.sup.1, R.sub.B R.sub.B.sup.1 are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms or R.sub.A and R.sub.A.sup.1 or R.sub.B and R.sub.B.sup.1 together with the nitrogen atom to which they are attached form a 5- to 6-member heterocycle optionally substituted with alkyl of 1 to 3 carbon atoms and Y is hydrogen or ##STR2## wherein R.sub.6 is selected from the group consisting of hydrogen, --CH.sub.3, --F and --Cl, R.sub.9 and R.sub.11 form a second bond at 9(11) or R.sub.9 is hydrogen or --F and R.sub.11 is hydrogen, --OH or .dbd.0, R.sub.16 is --CH.sub.3 or hydrogen, R.sub.17 is hydrogen, --OH or acyloxy, the dotted lines indicate the possible presence of a second bond at 1(2) and 6(7)-positions and the wavy line indicates the .alpha.- and .beta.

Abstract: New 11.beta.-phenyl-14.beta.H-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N.about.OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an .alpha.-permanent hydroxy group and either A and B together are a second compound and D is a hydrogen atom, where R.sup.1 is a five or six-part heteroalkyl residue or a cycloalkyl, cycloalkenyl or aryl residue or A is a hydrogen atom and B and D together are a methylene bridge, where R.sup.1 besides the aforementioned residues may be a possibly substituted hydrocarbon residue with up to 10 C atoms, a possibly substituted amino group, a hydroxy or C.sub.1-8 alkoxy, mercapto or thioalkyl group, R.sup.2 is a methyl or ethyl residue, and R.sup.3 /R.sup.4 represents the usual combination of substituents on the C17 atom in steroid chemistry, having antigestagenic and other properties.

Abstract: Vitamin D.sub.2 analogs in which a cyclopropane ring is introduced onto the 24-carbon of the side chain of 1.alpha.,25-dihydroxyvitamin D.sub.2 and 1.alpha.-hydroxyvitamin D.sub.2. The compounds are characterized by a marked intestinal calcium transport activity while exhibiting much lower activity than 1.alpha.,25-dihydroxy-vitamin D.sub.3 in their ability to mobilize calcium from bone. Because of their preferential calcemic activity, these compounds would be useful for the treatment of diseases where bone formation is desirbed, such as osteoporosis.

Abstract: The process of the invention comprises reacting a C-22-halo-23,24-bisnorsteroid or C-22-halo-23,24-bisnor-9,10-secosteroid with a nickel complex of an electron withdrawing alkene of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxycarbonyl, lower alkoxycarbonyl, lower alkylcarbonyl or unsubstituted or substituted lower alkyl, and R.sub.2 is hydroxyl, lower alkoxy, or unsubstituted or substituted lower alkyl,to yield a C-25 or C-26 precursor of the formula ##STR2## which is appropriately functionalized for conversion into the corresponding steroid or secosteroid by treatment as hereinafter described.

Abstract: A process for producing a 1.alpha.,3.beta.,24-trihydroxy-.DELTA..sup.5 -steroid represented by the formula (II): ##STR1## wherein R.sub.1 and R.sub.2, independently, represent a hyrogen atom, or R.sub.1 and R.sub.2 together form a single bond, R.sub.3 represents an unsubstituted or halogen-substituted lower alkyl, and R.sub.4 represents a hydrogen atom, hydroxy or a protected hydroxy, comprising reducing a 1.alpha.,2.alpha.-epoxy-.DELTA..sup.4,6 -3,24-dioxosteroid represented by the formula (I) ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the same meanings as defined in formula (II), using an alkaline metal or alkaline earth metal and a proton donor in a solvent comprising ammonia or amine characterized in that at an early stage of the reaction, the 1.alpha.,2.alpha.-epoxy-.DELTA..sup.

Abstract: (22E)-5,7,22-Ergostatriene-1.alpha.,3.beta.,25-triol and the 24-epimer thereof which are new intermediates for the synthesis of 1.alpha.,25-dihydroxyvitamin D.sub.2 and the 24-epimer thereof. A new process for the preparation of 1.alpha.,25-dihydroxyvitamin D.sub.2 and the 24-epimer thereof is also described which comprises irradiation of (22E)-5,7,22-ergostatriene-1.alpha.,3.beta.,25-triol or the 24-epimer thereof followed by isomerization.

Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.

Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.