46 results about "Steroid Compound" patented technology

The present application provides a kind of application of the steroid compound in preparation prevention or treatment skin pigmentation related condition or anti-aging related product, the steroid compound is as shown in formula I, and has treatment, lightening and / or alleviating effect on senile plaques, freckles, chloasma and the like caused by pigmentation on the skin of mammal.(I).

The application discloses a kind of steroid compounds and preparation method and purposes, and the structure of the steroid compound is as shown in formula I, wherein the definition of each substituent group is described in the specification and claims.The steroid compound of the application is a steroid compound with excellent AR antagonistic and AR degradation activity dual function, with good drug properties, good safety characteristics, and can be used for the treatment of diseases related to AR signal pathway.

The application of a steroid compound in the preparation of a medicine for preventing and / or treating floaters. The steroid compound can have a good treatment, alleviation and prevention effect on floaters, can greatly alleviate and / or cure floaters, and improve visual clarity.

The invention belongs to the technical field of biology, and relates to a method for producing a steroid compound by utilizing saccharomyces cerevisiae. The method comprises the following steps: replacing a YPL062w gene of the saccharomyces cerevisiae with an expression cassette of a PptHMGR gene, replacing a DPP1 gene of the saccharomyces cerevisiae with an expression cassette of ERG10, ERG13 and tHMG1 genes, replacing an LPP1 gene of the saccharomyces cerevisiae with an expression cassette of ERG12, ERG8, ERG19 and IDI1 genes, replacing an ROX1 gene of the saccharomyces cerevisiae with an expression cassette of ERG20, ERG9 and ERG1 genes, and replacing an ARO10 gene of the saccharomyces cerevisiae with an expression cassette of ERG11, ERG2 and ERG3 genes. An expression cassette of ERG1, DrDHCR7, GgDHCR24 and LEU2 genes is inserted into a delta DNA multi-copy site, and a first recombinant strain capable of synthesizing cholesterol is obtained; introducing a coding gene of an enzyme required for synthesizing a target steroid compound by taking cholesterol as a precursor into the genome of the first recombinant strain to obtain a second recombinant strain; and culturing the second recombinant strain and extracting the target steroid compound. The method has a wide application prospect in steroid compound production.

The present application relates to the field of compounds, discloses a kind of steroid compound with general formula I structure and its purposes, preparation method and the pharmaceutical composition comprising the steroid compound, to GABA A Receptor has strong positive regulation, can be used for preparing oral anti-severe depression and postpartum depression drug, with the characteristics of high efficiency.

This invention belongs to the technical field of steroid compound preparation, specifically relating to a safe post-processing technology for 11α,17α-dihydroxyprogesterone fermentation broth, comprising four processing steps: 1) extraction; 2) saponification; 3) secondary dissolution for impurity removal; and 4) decolorization. This invention employs a four-step post-processing procedure of extraction-saponification-secondary dissolution for impurity removal-decolorization, which not only improves the yield and purity of 11α,17α-dihydroxyprogesterone, achieving a purity of over 99%, but also solves the problem of high-yield extraction of 11α,17α-dihydroxyprogesterone from fermentation broth. Furthermore, it makes the reaction conditions milder, the operation simpler, safer, and more reliable, making it more suitable for large-scale production.

The application discloses a kind of steroidal compounds with anti-parkinson disease activity and its preparation method and application.The steroidal compound has the structure as shown in formula (I) or formula (II), or stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug of the structure shown in formula (I) or formula (II).The application is fermented by fungal co-cultivation to alternaria brassicae and penicillium granatum, and the expression of silent gene of strain is promoted by adopting co-cultivation and optimizing medium condition strategy, novel secondary metabolite is obtained, and new steroidal compound with treatment parkinson disease value and application prospect is extracted and separated from co-cultivation ferment, which provides great prospect for the research and development of parkinson disease treatment drugs.

This invention provides a soft material, container, liquid calibrator, and test kit sealed with a sealing agent. The sealing agent in the soft material is a steroid compound. This invention solves the problem in existing technologies where steroid hormones are easily adsorbed by the soft material of the container during storage, and is applicable to the field of soft materials.

The invention relates to the technical field of organic synthesis of steroid compounds, in particular to a preparation method of androstane-4-ene-3, 6, 17-triketone. Dehydroepiandrosterone acetate is used as an initial raw material to prepare androstane-4-ene-3, 6, 17-triketone through four steps of reactions including chlorohydrination, hydrolysis, oxidation and elimination, the yield and purity of androstane-4-ene-3, 6, 17-triketone are improved, 4-AD impurities are not generated, the total yield of a route reaches 80%, and the purity is larger than or equal to 98.0%; and the preparation process does not involve the use of dangerous chemicals and environment-polluting chromium oxidants, and is suitable for industrial production.

The application discloses a steroid C14 alpha hydroxylase CLCYP14 mutant, relates to the field of proteins, and applies a site-directed saturation mutation technology and a combination mutation strategy to screen and obtain CLCYP14 mutants I111L-M115K and I111L-V124W with high hydroxylation specificity. Compared with CLCYP14, the hydroxylation selectivity and conversion rate of I111L-M115K and I111L-V124W for steroid compounds progesterone, 21-hydroxyprogesterone, 5beta-hydroxyprogesterone, 1-dehydroprogesterone, 21-hydroxypregna-1,4-diene-3,20-dione and deoxycortisone are obviously improved.

The invention discloses application of fungal cytochrome P450 enzyme, and belongs to the technical field of biological enzyme catalysis. The fungal cytochrome P450 enzyme is derived from Gibberella fujikuroi, and the amino acid of the fungal cytochrome P450 enzyme is as shown in SEQ ID NO. 1 or has at least 80% similarity with the sequence as shown in SEQ ID NO. 1; the fungal cytochrome P450 enzyme at least can catalyze 7beta hydroxylation of five steroids L1, L2, L3, L4 and L5, and has excellent selectivity and high yield, and corresponding hydroxylation products can directly or indirectly generate ursodesoxycholic acid. The invention provides a good prospect for synthesizing ursodesoxycholic acid more environmentally and efficiently by using a biological enzyme method.

The present invention provides use of a steroid compound in preparing drugs for preventing and / or treating presbyopia. The steroid compound provided by the present invention is represented by formula (I). The steroid compound has the effect of treating, alleviating and preventing presbyopia, and can greatly alleviate and / or cure presbyopia to improve vision.

The invention belongs to the technical field of biological medicines, and discloses a deep sea steroid compound, a preparation method thereof and application of the deep sea steroid compound in preparation of medicines for preventing or treating renal fibrosis. The steroid compound is a class of highly oxidized and modified ergoketone compounds, and in some embodiments, the compound has an unusual malonyl substitution at the C-12 position of an ergoketone skeleton. The steroidal compound disclosed by the invention can achieve the effect of inhibiting renal fibrosis by regulating and controlling expression down-regulation of key fibrosis markers, namely alpha-smooth muscle actin (alpha-SMA) and I-type collagen (COL1A1), and has an inhibiting effect on proliferation of TGF-beta1-induced mouse renal fibroblasts; therefore, the compound has a great application prospect in preparation of drugs for preventing or treating renal fibrosis.

The invention relates to the technical field of medicine synthesis, in particular to C3 and C20 N-containing pregnane type steroid alkaloid derivatives as well as a preparation method and application thereof. A pregnane type steroid alkaloid skeleton in Miao medicine tri-silver is used as a template, a steroid compound epiandrosterone is used as a raw material, C3-site and C20-site keto compounds are obtained through Wittig alkylenation reaction and oxidation, and the C3-site and C20-site keto compounds are subjected to continuous reductive amination reaction to obtain a series of pregnane type steroid alkaloid derivatives containing N at C3 site and C20 site simultaneously. The C3 and C20 N-containing pregnane type steroid alkaloid derivatives provided by the invention have remarkable anti-inflammatory and anti-gastric ulcer activity, and a scientific basis is provided for searching novel anti-inflammatory and anti-gastric ulcer lead compounds with high selectivity and safety and developing novel anti-inflammatory and anti-gastric ulcer medicines.

The application discloses a 4-azasteroid compound, wherein the C-10 position methyl is in alpha configuration, and the 4-azasteroid compound has strong inhibiting effect on prostate cancer and colon cancer cells in addition to the drug activity of finasteride / dutasteride. The preparation method of the 4-azasteroid compound is simple in operation, high in efficiency, low in cost, environment-friendly, high in product purity, free of toxic by-products, and high in yield, and is suitable for large-scale industrial production. The application further discloses the use of the 4-azasteroid compound in the preparation of a drug for inhibiting cancer cells, and a pharmaceutical composition composed of the 4-azasteroid compound, which is verified by pharmacological experiments to have strong inhibiting effect on prostate cancer and colon cancer cells, and has a good application prospect in the preparation of the drug for inhibiting cancer cells.

The invention provides a steroid compound 11 alpha-hydroxylase and application of the steroid compound 11 alpha-hydroxylase. The coexpression vector provided by the invention can simultaneously express the steroid compound 11alpha-hydroxylase and cytochrome P450 reductase in escherichia coli or mycobacteria, a genetic engineering strain containing the coexpression vector can be suitable for 11alpha-hydroxyl conversion of various steroid substrates, the specificity is relatively strong, the highest conversion rate can reach 90.39%, and the coexpression vector can be applied to the conversion of 11alpha-hydroxyl of various steroid substrates. And the production technology is simple, efficient and controllable, and has important industrial application value.

The invention relates to the technical field of biocatalysis manufacturing of steroidal compounds, and discloses a method for converting a steroidal compound by ketoreductase and glucose dehydrogenase, which adopts a single liquid phase reaction medium composed of a water-miscible ionic liquid and a specific content of water; the medium spontaneously forms a hydration microcell on the microcosmic level, and the hydration microcell is used for jointly enriching free ketoreductase, free glucose dehydrogenase, coenzyme NADP (H) and a microcell affinity buffering agent; the main body non-aqueous phase of the medium is used for dissolving a steroid compound substrate at a high concentration, co-localization of a catalytic unit and in-situ regeneration of coenzyme are realized through the microstructure, and the problem of local pH instability during high-speed catalysis is solved through the in-situ buffer action of an interface catalytic conversion substrate and a buffer agent.

The invention relates to the technical field of enzyme engineering and gene engineering, in particular to a monooxygenase P450BM3 multi-site mutant and application of the monooxygenase P450BM3 multi-site mutant in catalyzing a steroid compound to generate a product C7beta. The mutant is a mutation of one or more of amino acid residues 87, 88, 188 and 330 in an amino acid sequence SEQ ID NO.7 of a wild type P450BM3-LG-23; the mutant is a mutant of one or more of amino acid residues 87, 88, 188 and 330 in the amino acid sequence SEQ ID NO.7; the amino acid residues at each site can be mutated into L, T or A in a same or different manner. According to the invention, LG-23 is taken as an initial template, protein engineering and a directed evolution strategy are combined, and a series of novel combined mutants with relatively high C7beta hydroxylation selectivity and conversion rate on steroid substrates such as testosterone (TES), nandrolone (NAL), 4-androstenedione (4AD), 1, 4-androstenedione (ADD) and the like are successfully obtained through multiple rounds of site-directed saturation mutagenesis. Compared with LG-23, the substrate spectrum of the obtained mutant expands 1, 4-androstenedione, the steroid substrate selectivity is improved to 77%-93%, and the conversion rate is improved to 94.7% or above.

The application belongs to the technical field of mother liquor recycling, and particularly relates to a treatment method of fluticasone propionate mother liquor. The treatment method of fluticasone propionate mother liquor provided by the application first mixes the fluticasone propionate mother liquor and amine compounds to perform a Hofmann alkylation reaction, quenches fluorohalomethane under mild conditions by using the Hofmann alkylation reaction of the amine compounds, reduces the impurity of fluticasone propionate, and recovers fluticasone propionate with high purity and high recovery rate, so that the material is fully utilized, and the pollution of fluorohalomethane and steroid compounds (fluticasone propionate) to the environment is reduced.

A lipid nanoparticle, comprising an ionizable lipid, a steroid compound and a polyethylene glycol-lipid, and not comprising a helper lipid. The ionizable lipid is selected from a compound having a structure represented by formula (I) and / or a pharmaceutically acceptable salt thereof. The three-component lipid nanoparticle not comprising a helper lipid reduces the complexity of the formulation and the difficulty of large-scale production, and further improves the nucleic acid encapsulation efficiency.

This invention discloses an enzyme for preparing C7-hydroxylated steroidal compounds, its gene, recombinant vector, engineered bacteria, and applications, belonging to the field of synthetic biotechnology. It addresses the problems of low expression levels and low conversion rates in the enzymatic conversion of BA to 7-OH-DBA. The amino acid sequence of the enzyme is shown in SEQ ID NO: 2. This invention also provides the gene sequence of this enzyme and a recombinant genetically engineered bacterium expressing the C7-hydroxylase. The enzyme of this invention is modified from an α-ketoglutarate-dependent dioxygenase. Compared with the wild type, the modified enzyme obtained in this invention can be successfully applied to the conversion of BA, achieving a conversion rate of 75% to produce 7-OH-DBA. This invention achieves enzymatic catalytic C7-hydroxylation of BA, which, compared with traditional chemical synthesis methods, is simpler, greener, and more economical. The synthesis of 7-OH-DBA will provide strong support for the development of new processes for steroidal drug production.

The present invention provides an estetrol synthesis process, and relates to the technical field of steroid compound synthesis processes, and the method comprises the following steps: taking estrone as an initial raw material, firstly carrying out 3-site hydroxyl protection, and then carrying out an oxidative dehydrogenation reaction in the presence of a metal catalyst and in an oxygen atmosphere to prepare a key intermediate ketene, then 17-site carbonyl reduction, 17-site hydroxyl protection, 15, 16-site double bond dihydroxylation, 3-site protecting group removal and hydrolysis reaction are sequentially carried out, and finally the target product estetrol is obtained. The method adopts metal catalysis to directly oxidize to construct cycloenone, effectively avoids the problem of poor stability of partial intermediates in the prior art, has the advantages of simple process, short reaction steps, greenness, environmental protection and the like, and is suitable for industrial production.

According to the chick embryo fermentation product and the preparation method and application thereof provided by the invention, the bioactive component content and functionality of the chick embryo fermentation product are remarkably improved through optimal incubation conditions, compound microbial fermentation and synergistic addition of various active components. The composition prepared by the method is rich in sialic acid, small molecule peptide, unsaturated fatty acid, nucleotide, steroids and hormone substances, has various physiological functions of enhancing immunity, regulating intestinal flora, preventing metabolic diseases and the like, and is especially suitable for physical recovery and endurance improvement of sports people; wide application prospects and market potentials are realized.

The invention relates to the technical field of medicine synthesis, in particular to a C3-site oxime ester steroid alkaloid derivative as well as a synthesis method and application thereof. A steroid compound epiandrosterone is used as an initial raw material, a C3-position keto compound is obtained through Wittig alkylenation reaction and oxidation, the C3-position keto compound reacts with hydroxylamine hydrochloride to obtain a hydroxylamine compound, and the hydroxylamine compound reacts with acyl chloride to obtain a series of oxime ester derivatives. The C3-site oxime ester steroid alkaloid derivative provided by the invention has remarkable anti-inflammatory and anti-gastric ulcer activity, and provides a scientific basis for searching novel anti-inflammatory and anti-gastric ulcer lead compounds with high selectivity and safety and developing novel anti-inflammatory and anti-gastric ulcer medicines.

The present application relates to a kind of steroid compound and its application in treating neurodegenerative diseases, the steroid compound has the structure shown in formula I: The steroid compound of structure I is isolated from the whole grass of Solanum nigrum by yeast fermentation for the first time, it shows better neurotrophic factor (NGF) activity and acetylcholinesterase inhibitory activity, is expected to be developed as the drug or functional food of neurotrophic and neuroprotective function, for treating neurodegenerative diseases (such as senile dementia).

Methods for stereoselectively crystallizing 3-keto-5β-cholanic acid (“3-KCA”) and 3-ketoursodeoxycholic acid (“3-KUDCA”) of extremely high purity, salts for carrying out such methods, particularly tert-butylamine and cyclohexylamine salts of 3-KCA, tert-butylamine salts of 3-KUDCA, and crystalline forms of these salts, as well as methods for preparing commercial steroid compounds from these purified materials.

The invention relates to a steroidal compound as well as application and a preparation method thereof. The compound is expected to be capable of effectively treating psychiatric and neurological diseases, and has good active efficacy, pharmacokinetic (PK) performance, oral bioavailability, stability, safety, clearance rate and / or metabolic performance and the like.

The application discloses a 3-steroid ketone-delta 1-dehydrogenase mutant and application thereof in catalyzing dehydrogenation of a steroid compound, and the mutant with high catalytic activity is screened, and a cosolvent Tween-80 is added to increase solubility of a substrate and then improve biological catalytic efficiency.Under optimal conditions, the mutant can increase the conversion rate of (16alpha)-methyl androst-4,9-diene-3,17-dione 15g / L to 99.9%.

Disclosed in the present invention are a steroid compound, and a preparation method therefor and the use thereof. The structure of the steroid compound is as shown in formula I, and the definition of each substituent in the formula are as described in the description and claims. The steroid compound of the present invention is a steroid compound having the dual functions of excellent AR antagonistic activity and AR degradative activity, has the characteristics of good druggability and safety, and can be used for treating diseases related to an AR signaling pathway.

The present application provides a cytochrome P450 enzyme mutant and use thereof. The mutant has any one of the following amino acid mutations in the amino acid sequence shown in SEQ ID NO. 2: G294A, G294A+E89G, G294A+N236H, G294A+F321W, G294A+N236H+F321W, G294A+N236H+F321W+V297A, and G294A+N236H+F321W+I397V. The present application takes the amino acid sequence shown in SEQ ID NO. 2 as a template, mutates and modifies key active sites of the template, constructs a mutant library, and screens a series of mutants with significantly improved catalytic activity and / or selectivity. The mutant can selectively catalyze 7β-hydroxylation of a steroid compound to generate a corresponding 7β-hydroxylated steroid compound, and has excellent selectivity and / or high yield, indicating that the mutant has a good application prospect in catalyzing the steroid compound to generate a 7β-hydroxylated steroid compound.