42 results about "Pregnenolone" patented technology

The invention discloses a method for inducing nematode-trapping fungus predatory organ formation, and belongs to the field of applied microorganisms. The method comprises the following specific steps: culturing activated nematode-trapping fungi until spores are generated; washing off the cultured spores, and diluting to obtain a spore suspension with the concentration of 30000-60000 spores / mL; coating the spore suspension into an agar culture medium paved with glass paper, uniformly coating the spore suspension, culturing for 28-36 hours at the temperature of 25-28 DEG C, adding a mixed solution of a predatory organ inducer and water, and continuously culturing for 36-60 hours at the temperature of 25-28 DEG C, so that the nematode-trapping fungi can generate a large number of predatory organs; the predatory organ inducer is one of oleic acid, linoleic acid or pregnenolone. It is found for the first time that a large number of predatory organs can be generated when pregnenolone, oleic acid or linoleic acid is used for inducing nematode-trapping fungi.

The present disclosure provides a pharmaceutical composition that includes enclomiphene and pregnenolone, and pharmaceutical combinations and uses thereof. The present disclosure also provides a pharmaceutical combination that includes a selective estrogen receptor modulator and testosterone in a form suitable for oral administration, sublingual administration, topical administration, transdermal administration, or combinations thereof and uses thereof.

The present disclosure provides a pharmaceutical composition that includes enclomiphene and pregnenolone, and pharmaceutical combinations and uses thereof. The present disclosure also provides a pharmaceutical combination that includes a selective estrogen receptor modulator and testosterone in a form suitable for oral administration, and uses thereof.

The present disclosure provides a pharmaceutical composition that includes enclomiphene and pregnenolone, and pharmaceutical combinations and uses thereof. The present disclosure also provides a pharmaceutical combination that includes a selective estrogen receptor modulator and testosterone in a form suitable for oral administration, and uses thereof.

The present disclosure provides a pharmaceutical composition that includes enclomiphene and pregnenolone, and pharmaceutical combinations and uses thereof. The present disclosure also provides a pharmaceutical combination that includes a selective estrogen receptor modulator and testosterone in a form suitable for oral administration, and uses thereof.

The present disclosure provides a pharmaceutical composition that includes enclomiphene and pregnenolone, and pharmaceutical combinations and uses thereof. The present disclosure also provides a pharmaceutical combination that includes a selective estrogen receptor modulator and testosterone in a form suitable for oral administration, and uses thereof.

The present disclosure provides a pharmaceutical composition that includes enclomiphene and pregnenolone, and pharmaceutical combinations and uses thereof. The present disclosure also provides a pharmaceutical combination that includes a selective estrogen receptor modulator and testosterone in a form suitable for oral administration, and uses thereof.

The present invention generally relates to a specific pregnenolone derivative for its use for the treatment of a Cannabinoids-Related Disorder. More particularly, the invention relates to a compound of Formula (I)for its use in the treatment of a Cannabinoids-Related Disorder. Indeed, the compound of the invention is in vivo very potent in inhibiting the effects of THC, and is able to inhibit both unconditioned and conditioned effects of THC including THC self-administration and reinstatement in THC seeking in non-human primates.

The present disclosure provides a pharmaceutical composition that includes enclomiphene and pregnenolone, and pharmaceutical combinations and uses thereof. The present disclosure also provides a pharmaceutical combination that includes a selective estrogen receptor modulator and testosterone in a form suitable for oral administration, sublingual administration, topical administration, transdermal administration, or combinations thereof and uses thereof.

The present disclosure provides a pharmaceutical composition that includes enclomiphene and pregnenolone, and pharmaceutical combinations and uses thereof. The present disclosure also provides a pharmaceutical combination that includes a selective estrogen receptor modulator and testosterone in a form suitable for oral administration, and uses thereof.

The present invention relates to the technical field of pharmaceutical compounds and specifically discloses a selenocyanine pregnenol ketamide compound having the following general structural formula: #imgabs0#. The selenocyanine pregnenol ketamide compound of the present invention exhibits strong inhibitory activity against human breast cancer cells, cervical cancer cells, ovarian cancer cells, and human liver cancer cells. Furthermore, the selenocyanine pregnenol ketamide compound of the present invention also exhibits strong inhibitory effects against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). The selenocyanine pregnenol ketamide compound of the present invention has low toxicity to humans and exhibits strong inhibitory effects against cancer cells and various drug-resistant bacteria at low concentrations. It can be used to prepare cancer treatment drugs and as an antibacterial agent against drug-resistant bacteria.

Disclosed is a method and a brexanolone containing oral composition for treating CNS disorders such as depression. An embodiment of the invention comprises orally administering a brexanolone containing composition to a subject having a CNS disorder. The composition and methods disclosed herein exhibit effective oral absorption / bioavailability and a predetermined ratio of bioavailability in a fed state administration relative to a fasted state administration.

The invention discloses a method for increasing the yield of pregnenolone in heterologous synthesis of yarrowia lipolytica. According to the method, a recombinant yarrowia lipolytica strain is constructed, and the construction method is selected from one of the following three methods: on the basis of the recombinant yarrowia lipolytica strain SyBEY12060077, CYP11A1 and an ER positioning sequence KDEL are fused; the CYP11A1 is integrated, and meanwhile, the additional Adx gene expression is increased; the CYP11A1 is integrated, and the CYB5 gene is introduced at the same time. According to the newly constructed strain, acquisition of precursor campesterol and electron transfer of P450 enzyme are improved, so that the overall steroid flux is improved, the yield of heterologous production of pregnenolone is improved, and a research thought is provided for subsequent optimization of metabolic regulation and improvement of synthesis of recombinant yarrowia lipolytica steroids.

The invention discloses a method for improving heterologous synthesis of pregnenolone and progesterone by using yarrowia lipolytica. The invention provides a method for improving the heterologous synthesis of pregnenolone by using yarrowia lipolytica, which comprises the following steps: knocking out an MHY1 gene on the basis of a recombinant yarrowia lipolytica strain SyBEY12090002, and constructing a strain Y1001; the invention relates to a method for improving heterologous synthesis of progesterone by using yarrowia lipolytica, which is characterized in that on the basis of a recombinant yarrowia lipolytica strain SyBEY12090002, 3beta-hydroxysteroid dehydrogenase is introduced, an MHY1 gene is knocked out, and a strain Y1102 is constructed. The MHY1 gene is knocked out from the strain for synthesizing the pregnenolone or the progesterone from the beginning, so that the yield of the pregnenolone or the progesterone synthesized by the recombinant lipolytic yeast strain is improved, the influence of regulating the morphological change of the yarrowia lipolytica on a heterologous synthesis pathway is explored, and a research direction is provided for subsequently improving the yield of the pregnenolone or the progesterone.

The invention discloses a 17beta-pregnenolone-amino-acid ester derivative, the chemical structure of which is as shown in the following formula: # imgabs0. The 17beta-pregnenolone-amino-acid ester derivative disclosed by the invention has an inhibiting effect on human breast cancer cells, human ovarian cancer cells, human breast duct cancer cells and human cervical cancer cells, and can be used for preparing antitumor drugs.

The application relates to the technical field of organic synthesis, and particularly discloses a synthesis process of high-purity pregnenolone, which comprises the following steps: S1, esterification reaction of progesterone and an acylation reagent to obtain product 1; S2, ketalization reaction of the product 1, diol and a dehydrating agent in the presence of a catalyst to obtain product 2; S3, reduction reaction of the product 2 and a reducing agent to obtain product 3; and hydrolysis reaction of the product 3 and an acidic compound to obtain pregnenolone. The synthesized pregnenolone has high purity and yield.

Microemulsions are described where hydrophobic liquid droplets are distributed in a continuous hydrophilic liquid phase. In relation to conventional oil-in-water (OIW) microemulsions, the described microemulsions may be thought of as modified oil-in-water (MOIW) microemulsions, where both the “oil” and “water” phases of the microemulsion are modified. The oil phase droplets of the MOIW microemulsion are modified with alcohol and can solubilize alcohol-soluble species, including nonderivatized hormones. More preferably, the modified oil phase droplets of the MOIW microemulsion directly solubilize nonderivatized hormones. The oil phase droplets of the MOIW microemulsion include DHEA, pregnenolone, and a polyphenol, where a ratio of DHEA to polyphenol is from 1:1 to 12:1 by weight. Methods of supporting and / or increasing bloodstream hormone levels in perimenopausal and postmenopausal females and improving menopausal symptoms also are disclosed.

This invention discloses sterol side-chain cleaving enzymes and 3β-hydroxysteroid dehydrogenases / Δ from different sources. 4,5 Amino acid sequences, coding sequences, and applications of isomerases. This invention, based on synthetic biology and molecular pharmacognosy, explores sterol side-chain cleaving enzymes and 3β-hydroxysteroid dehydrogenases / Δ from different plant sources. 4,5 Isomerases, which will yield sterol side-chain cleavage enzymes and 3β-hydroxysteroid dehydrogenases / Δ 4,5 The coding sequences of the isomerases were constructed into expression cassettes, and using Saccharomyces cerevisiae as the chassis strain, highly efficient pregnenolone or progesterone synthesizing strains were obtained. The pregnenolone yield of the constructed strains reached as high as 14.46±2.16 mg / L, and the progesterone yield reached as high as 32.78±1.84 mg / L. This achieved high-level synthesis of pregnenolone and progesterone by genetic engineering methods, providing an important foundation for the green synthesis of steroid hormones.

The invention provides a steroid compound containing a 3-methyl allopregnenolone mother nucleus structure as well as a preparation method, a pharmaceutical composition and application of the steroid compound, and belongs to the technical field of medicines. The invention provides a steroid compound containing a 3-methyl pregnenolone mother nucleus structure, and pharmaceutically acceptable salts, stereoisomers, tautomers, prodrugs, solvates or isotope compounds of the steroid compound. The steroid compound containing the 3-methyl pregnenolone mother nucleus structure has a structure as shown in a formula I. The invention further provides a preparation method of the steroid compound containing the 3-methyl pregnenolone mother nucleus structure. The steroid compound containing the 3-methyl allopregnenolone mother nucleus structure has a strong positive regulation effect on a GABAA receptor, and has potential application to treatment of central nervous system related diseases.

The invention relates to the technical field of organic synthesis, and particularly discloses a synthesis process of high-purity pregnenolone, which comprises the following steps: S1, carrying out esterification reaction on progesterone and an acylation reagent to obtain a product 1; s2, the product 1, diol and a dehydrating agent are subjected to a ketalation reaction in the presence of a catalyst, and a product 2 is obtained; s3, carrying out reduction reaction on the product 2 and a reducing agent to obtain a product 3; and carrying out hydrolysis reaction on the product 3 and an acidic compound to obtain pregnenolone. According to the present invention, the synthesized pregnenolone has high purity and high yield.

The present disclosure relates to the use of neuroactive steroids, including alfaxalone, alfadolone, alfadolone acetate, pregnanediol, pregnanolone, ent-pregnanolone, pregnanedione, allopregnanediol, allopregnanedione, acebrochol, ganaxolone, hydroxydione, minaxolone, renanolone, (2β,3α,5β)-21-chloro-3-hydroxy-2-morpholin-4-ylpregnan-20-one (Org-20599), 2β-(2,2-dimethyl-4-morpholinyl)-3α-hydroxy-11,20-dioxo-5α-pregnan-21-yl methanesulfonate (Org-21465), 20-(hydroxyimino)pregn-4-en-3-one (EIDD-036), posovolone (Co 134444), zuranolone (SAGE-217), 3α-hydroxy-3β- methyl-21-(pyrazolo[3',4'-c]pyridin-2'-yl)-19-nor-5β-pregnan-20-one (SGE-872), alfaxalone / alfadolone (CT1341), (3β,5β,17β)-3-hydroxyandrostane-17-carbonitrile (3β- OH), (3α,5α)-3-hydroxy-13,24-cyclo-18,21-dinorchol-22-en-24-ol (CDNC24), 3α- dihydroprogesterone (3α-DHP), ent-progesterone, dihydrodeoxycorticosterone (DHDOC), tetrahydrodeoxycorticosterone (THDOC), and betaxalone, for treating or at least partially inhibiting the development or progression of an infection caused by a neurotropic virus in a subject. This disclosure also relates to the use of neuroactive steroids for treating or at least partially inhibiting the development or progression of a condition associated with an infection caused by a neurotropic virus, such as encephalopathy or acute encephalitis.

The invention discloses a directional preparation process of B crystal form dexamethasone. The process comprises the following steps: by taking 16-dehydropregnanone propionate as a starting material, sequentially performing catalytic dehydrogenation by using steroid 1, 4-dehydrogenase from bacillus subtilis, performing catalytic dehydrogenation by using potassium methyltrifluoroborate / copper acetate / 2, 4-dihydroxyprogesterone propionate as a starting material, and performing catalytic hydrogenation by using potassium methyltrifluoroborate / The preparation method comprises the following steps: preparing dexamethasone free alkali by key steps of stereoselective methylation of a 2, 2 '-bipyridine system, catalysis of 11 beta-hydroxylation by immobilized CYP11B1 monooxygenase, epoxidation of peroxybenzoic acid, ring opening of hydrogen fluoride-ethanol and the like, and finally directionally crystallizing in a system solution consisting of 0.5% malic acid and isopropanol-water in a volume ratio of 3: 1 to obtain the high-purity B crystal form dexamethasone.

The invention relates to application of ginsenoside Rg4 as a unique active ingredient in preparation of a medicine for improving male delayed gonad hypofunction, belonging to the field of biological medicine. According to the invention, the action mechanism of the Rg4 for improving LOH is defined for the first time: the Rg4 can specifically up-regulate the mRNA expression quantity of StAR and StARD7 in a testis tissue, and promote the transport of cholesterol to the inner mitochondrial membrane of a testis Leydig cell from the transcriptional level; the Rg4 improves the mRNA expression quantity of P450scc, 3 beta-HSD in testicular tissues by promoting the efficient transport of cholesterol, enhances the conversion of cholesterol to pregnenolone and the catalytic synthesis of subsequent steroids, and improves the endogenous testosterone synthesis capability; the Rg4 can recover the negative feedback regulation function of an HPG axis, regulate secretion of pituitary LH and FSH to physiological steady state, and avoid abnormal fluctuation of hormone level. The invention fills the technical blank of Rg4 in the field of LOH gene regulation and control.

The invention relates to the technical field of cell engineering and biopharmacy, and discloses a method for promoting synthesis of steroids in forest musk gland cells, which comprises the following steps: determining the tolerance range of cholesterol concentration through a pre-experiment, setting an experimental group, culturing cells, collecting and treating a sample, and detecting by LC-MS (Liquid Chromatography-Mass Spectrometry). According to the method for promoting synthesis of the steroids in the lindel gland cells, the synthesis amount of the seven steroids in the lindel gland cells can be up-regulated by regulating the cholesterol concentration of the culture medium to 10-20 mg / L, the content of pregnenolone is up-regulated by 4.12 times (Plt, 0.05), the content of progesterone is up-regulated by 1.46 times (Plt, 0.05), and the method is remarkably superior to that of existing culture without cholesterol regulation; a complete standardized process from pre-experiment, culture, sample treatment to detection is provided, the experiment result repeatability is high, and the method can be directly applied to industrial production.

The invention provides a preparation method of pregnenolone, and relates to the technical field of biological pharmacy and biochemical engineering. Cheap and easily available steroid progesterone is used as a raw material, 3 # site esterification is carried out through a chemical method, then a catalytic reaction of hydrolase and ketoreductase is carried out, and finally a target product is obtained with the yield as high as 91%. The process has no loss except conversion, and the intermediate is relatively stable, so that the reaction product is relatively high in yield and good in quality, and is suitable for large-scale industrial production.

The invention relates to a synthesis method of stable isotope labeled 17alpha-hydroxypregnenolone 2, 3, 4-13C3, which comprises the following steps: S1, dissolving sodium cyanide in a solvent system, adding a phase transfer catalyst and dehydroepiandrosterone 2, 3, 4-13C3, stirring for catalytic reaction, and filtering to obtain a cyanohydrin intermediate I; s2, dissolving the obtained cyanohydrin intermediate I in another solvent system, adding methyl magnesium bromide under the protection of inert atmosphere, and stirring to carry out Grignard reaction; and S3, after the Grignard reaction in the S2 is finished, adding excessive sulfuric acid aqueous solution, stirring, carrying out hydrolysis reaction, and extracting, washing, drying, carrying out rotary evaporation and purifying the obtained product to obtain the 17alpha-hydroxypregnenolone 2, 3, 4-13C3 product. Compared with the prior art, the purity of the prepared 17alpha-hydroxypregnenolone-2, 3, 4-13C3 product is greater than or equal to 98%, the abundance is greater than or equal to 99atom% 13C, the abundance is not obviously diluted, and the like.

The present disclosure provides a pharmaceutical composition that includes enclomiphene and pregnenolone, and pharmaceutical combinations and uses thereof. The present disclosure also provides a pharmaceutical combination that includes a selective estrogen receptor modulator and testosterone in a form suitable for oral administration, and uses thereof.

The present invention belongs to the technical field of drug crystal forms and relates to a new crystal form of pregnenolone and a preparation method thereof. The new crystal form of pregnenolone of the present invention uses Cu-Kα radiation and, in a powder XRD ray diffraction pattern represented by 2θ, includes 7.496°, 10.449°, 10.815°, 13.484°, 14.303°, 14.983°, 15.663°, 15.917°, 16.385°, 16.798°, 17.226°, 17.495°, 18.389°, 19.115°, 20.291°, 20.861°, 21.388°, 21.948°, 22.156°, 22.443°, 23.118°, 23.727°, 24.041°, 24.46 There are diffraction peaks at positions of 1°, 24.846°, 25.649°, 25.920°, 26.189°, 27.460°, 27.768°, 28.237°, 29.129°, 30.324°, 31.385°, 31.581°, 32.905°, 34.529°, 34.89°, 37.108°, 37.300°, 38.163°, 40.271, 40.442°, 41.215°, 41.393°, 42.776°, 43.516°, 43.821°, 47.113°, and 48.092°, and the position error range of 2θ is ±0.1°.

Disclosed are: a poultry feed comprising at least one selected from the group consisting of progesterone, pregnenolone, and medroxyprogesterone; and a method for breeding poultry, the method comprising a step for causing poultry to ingest at least one selected from the group consisting of progesterone, pregnenolone, and medroxyprogesterone.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a biological oxidation preparation method of a key intermediate in a chemical synthesis medicine production process. A compound A synthesized by photocatalytic isomerization of pregnenolone is used as a raw material. Under the action of alcohol dehydrogenase, the compound A is oxidized to form a compound B, and then the compound B is shifted in a hydrogen chloride ethanol solvent to form the didrogesterone. Through the preparation technology provided by the invention, the high-purity didrogesterone bulk drug can be obtained with low cost and high efficiency.