86 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 anti-tumor drugs, and particularly relates to a flexible drug-loaded cell microparticle capable of efficiently targeting tumors and a preparation method of the flexible drug-loaded cell microparticle. Comprising tumor cell-derived drug-loaded microparticles coated with chemotherapeutic drugs, and a flexible regulator modified on the surfaces of the tumor cell-derived drug-loaded microparticles, the flexible regulator comprises a saponin compound and / or a steroid compound, and can regulate and control the hardness of the tumor cell-derived drug-loaded microparticles. The tumor cell-derived drug-loaded microparticles are modified, so that the enrichment and deep penetration of the drug-loaded microparticles in tumor tissues can be remarkably improved, and the efficient targeted delivery of the tumor tissues is realized. Meanwhile, efficient uptake of tumor stem cells to the medicine is promoted, targeted killing is achieved, the tumor stem cells are effectively removed, and tumor growth is remarkably inhibited. In addition, circulating tumor cells can be efficiently targeted, accurate delivery of tumor metastasis is achieved, and tumor metastasis is remarkably inhibited by inhibiting migration and invasion of tumor cells and reducing formation of lung metastasis.

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 invention relates to a steroidal compound as well as a preparation method and application thereof. Specifically, the invention provides a compound shown as a general formula (I), a stereoisomer or pharmaceutically acceptable salt of the compound, a preparation method of the compound, a pharmaceutical composition containing the compound and application of the compound as a GABAa receptor modulator to treatment of CNS-related diseases.

The present application relates to a kind of steroid compound Aglatestate A, its preparation method and purposes, belong to medical field.The compound is extracted from the leaves of horse kidney fruit branch, preparation separation is simple.The present application has better inhibiting effect on the release of inflammatory factor of LPS-induced RAW264.7 cell, when in non-toxic concentration, the inhibiting effect of compound on the release of inflammatory factor NO of LPS-induced RAW264.7 cell is good, and the anti-inflammatory effect IC 50 =3.41±0.05 close to positive drug PDTC (NF-κB inhibitor / antioxidant), therefore, compound Aglatestate A has good development prospects of anti-inflammatory drug, and lay a solid foundation for the preparation of anti-inflammatory drug technology development.

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.

The invention belongs to the technical field of bioengineering, and relates to a steroid C14 beta hydroxylase, an expression vector, an engineering bacterium and application thereof, the amino acid sequence of the hydroxylase is selected from a sequence shown in SEQ ID No.9 or a sequence modified on the basis of the sequence, or a sequence having at least 58% homology with the sequence. The hydroxylation of the steroid C14 beta is directly completed in one step, and the efficient and specific hydroxylation of the steroid compound C14 beta can be realized, so that the problem that the C14 beta hydroxylated steroid cannot be directly synthesized is solved.

The invention belongs to the field of medicines, and particularly relates to a pharmaceutical composition for preventing and / or treating neurodegenerative diseases, the pharmaceutical composition takes a steroid compound with a structure as shown in a formula I, a stereoisomer, a tautomer or pharmaceutically acceptable salt thereof as an active ingredient; the structure of the formula I is shown in the specification.

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 present application relates to lipid nanoparticles comprising a cationic steroid compound and to the preparation and use of such lipid nanoparticles. Such lipid nanoparticles can be used to deliver a payload, such as a nucleic acid, in vivo to a non-liver organ (e.g., lung) to treat or prevent certain diseases or disorders, particularly lung disease.

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 invention belongs to the technical field of biological enzymes, and discloses a cytochrome P450 enzyme mutant and application thereof, the mutant is subjected to any one of the following amino acid mutations on an amino acid sequence as shown in SEQ ID NO.2: L294A, L294G, L294A + T89H and L294G + T89H. The cytochrome P450 enzyme mutant provided by the invention can selectively catalyze a 7beta hydroxylation reaction of a steroid compound to generate a corresponding 7beta-hydroxylated steroid compound (such as UDCA, CA and the like), and has excellent selectivity (-96%) and / or relatively high yield (-70%), the catalytic reaction efficiency is high, and the reaction time can be shortened to be within 20 hours.

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 present invention relates to steroid compounds, uses and preparation methods thereof; it is expected that such compounds can effectively treat psychoneurological diseases and have good activity efficacy, pharmacokinetic (PK) properties, oral bioavailability, stability, safety, clearance rate and / or metabolic properties, etc.

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 a fixed-point chlorination method of a steroid compound, and belongs to the technical field of organic synthesis. The fixed-point chlorination method provided by the invention is characterized by comprising the following steps: under the conditions of electrification and illumination, enabling a steroid compound and a chlorine source to react in an electrolyte solution for 1-24 hours, so as to obtain a chlorinated steroid compound. The method has the characteristics that the chlorine source is economical and mild, the post-treatment is simple, the method can adapt to multi-site chlorination, the industrial amplification is easy, and the substrate universality is strong.

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 invention provides a preparation method and application of a high-purity steroid compound, 4, 9-diene is taken as a raw material, 5 (10), 9 (11)-diene is obtained through pyrrolidine protection and deprotection reaction, industrial pyrrolidine is pretreated and then used for reaction, peroxidation by-products in the reaction process can be obviously reduced, and the high-purity 5 (10), 9 (11)-diene compound is obtained. Compared with the prior art, the preparation method has the advantages that the purity of the 1, 9 (11)-diene is 99% or above, the content of peroxide impurities is 0.2-0.3%, the molar yield of protection and deprotection two steps reaches 85% or above, the yield is remarkably improved compared with that of pyrrolidine which is not pretreated, impurities in the product are also remarkably reduced, and the overall yield and the product quality of the gestotrienone are improved.

The application of steroid compounds in the preparation of a drug for preventing and / or treating floaters, said steroid compounds have excellent effects of treating, alleviating and preventing floaters, and can greatly reduce and / or cure floaters and improve visual clarity.

The present invention relates to a steroid compound, a use thereof and a preparation method therefor. It is expected that such compound can effectively treat mental and neurological diseases, and has good active efficacy, pharmacokinetic (PK) performance, oral bioavailability, stability, safety, clearance rate, and / or metabolic performance and the like.