121 results about "Steroid Compound" patented technology

The invention discloses a 3-ketosteroid-delta1-dehydrogenase mutant and application of the 3-ketosteroid-delta1-dehydrogenase mutant in catalyzing dehydrogenation of a steroid compound, the mutant with high catalytic activity is obtained through screening, and the solubility of a substrate is increased by adding a cosolvent Tween-80, so that the biological catalytic efficiency is improved. Under the optimal condition, the mutant disclosed by the invention can improve the feeding amount conversion rate of 15g / L of (16 alpha)-methyl androstane-4, 9-diene-3, 17-diketone to 99.9%.

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 embodiment of the invention provides an oxadiazole-steroid compound, a pharmaceutical composition and application. The oxadiazole-steroid compound is a compound with a structure as shown in a formula I or pharmaceutically acceptable salt of the compound or a mixture of the compound and the pharmaceutically acceptable salt. The oxadiazole-steroid compound provided by the embodiment of the invention can effectively activate a metabolic regulation target FXR, and has excellent potential for preventing or treating MAFLD and related complications thereof. Meanwhile, the compound has no excitation effect on an MRGPRX4 receptor possibly causing pruritus while maintaining the FXR excitation activity, and a safer choice is provided for treatment of related diseases. Therefore, the oxadiazole-steroid compound has a more remarkable application prospect in preparation of the medicine for treating the metabolism-related fatty liver disease.

The present invention provides a method for dehalogenating 9-halogenated steroid compounds and its application, which relates to the technical field of chemical synthesis. The method for dehalogenating 9-halogenated steroid compounds includes the following steps: Compound I reacts with a thiofatty acid salt to obtain the 9-dehalogenated product Compound II of the 9-halogenated steroid compound. The method for dehalogenating 9-halogenated steroid compounds provided by the present invention reacts Compound I with a thiofatty acid salt to obtain the 9-dehalogenated product Compound II of the 9-halogenated steroid compound. Toxic reagents such as zinc powder, chromium granules or tri-n-butyltin, which are highly toxic and cause serious environmental pollution, are not used in the reaction. It is green and environmentally friendly, the synthesis process is simple and easy to operate, and the production applicability is improved.

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 discloses a radix cynanchi bungei C21 steroid compound as well as a biological fermentation method and application thereof. Fresh radix cynanchi bungei tuberous root slurry is subjected to enzymolysis treatment through a magnetic nano-composite enzyme preparation, obtained saccharified liquid is fermented through agrobacterium tumefaciens F-45, obtained fermentation liquid is freeze-dried, obtained freeze-dried powder is extracted with absolute ethyl alcohol, supernate is collected, finally, the supernate is added into a precipitation agent for treatment, and the radix cynanchi bungei tuberous root extract is obtained. And volatilizing the obtained precipitate in a water bath at 40 DEG C until no liquid is left, wherein the precipitate is the C21 steroid compound. According to the fermentation system constructed by the invention, the absolute amount of the C21 steroid compound is increased by 4.3 times compared with that of a root tuber raw material, and the C21 steroid compound is rich in variety, high in yield, short in production period and easy for large-scale industrial production; the obtained fermentation extract C21 steroid compound has a good protection effect on liver cell injury caused by oxidative stress.

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 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 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 a steroid compound and a conjugate thereof, in particular to a compound and a conjugate thereof, or a tautomer, a meso-mer, a raceme, an enantiomer, a diastereoisomer thereof, or a mixture form thereof, or a pharmaceutically acceptable salt thereof. The invention also discloses a preparation method and application of the compound and the conjugate thereof.

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.