30 results about "Hydroxycholesterols" patented technology

Provided are methods of evaluating or treating a patient, e.g., a patient having a disorder described herein, comprising: a) optionally, acquiring a patient sample; b) acquiring an evaluation of and / or evaluating the sample for an alteration in the level S24(S)-hydroxycholesterol compared to a reference standard.

Methods and compositions for the prevention and treatment of liver damage or disease in a subject in need thereof are provided. The methods involve providing the sulfated oxysterol 25-hydroxycholesterol-3-sulfate (25HC3S) to the subject e.g. by 1) administering 25HC3S to the subject; or 2) overexpressing, in the subject, the hydroxysterol sulfotransferase enzyme SULT2B1b, which catalyzes the sulfation of 25-hydroxycholesterol (25HC) to form 25HC3S.

The invention relates to the field of chemical drugs, and discloses an application of 25-hydroxycholesterol in inhibiting flaviviruses. Specifically, the invention discloses an application of the 25HC (25-hydroxycholesterol) in preparing medicines for preventing and / or treating flavivirus infection, in inhibiting the flaviviruses and in preparing medicines for preventing and / or treating microcephaly caused by Zika virus infection. The invention also discloses a pharmaceutical composition, wherein the pharmaceutical composition consists of the 25HC, at least one adjuvant agent conductive to inhibition of the flaviviruses and at least one pharmaceutically acceptable vector. With the application of the 25HC, the flaviviruses can be inhibited, so that a protecting effect is taken on a host; and specifically, the 25HC can be used for inhibiting the flavivirus infection in human cell, mouse and rhesus monkey models, and can be used for preventing and / or treating the microcephaly caused by Zika viruses.

The present invention relates to a synthesis method for 25-hydroxy-7-ketocholesterol. The method comprises: using a 25-hydroxycholesterol derivative as a raw material in an organic solvent, initiating by an initiator in the presence of an N-hydroxy catalyst; reacting 1-40 hours at a temperature of 0 DEG C-150 DEG C with air or oxygen; performing dehydration reaction for 1-20 hours by adding a dehydrant at a temperature of -20 DEG C-100 DEG C after completion of the reaction; then performing hydrolysis reaction for 1-2 hours at a temperature of 50 DEG C-80 DEG C; and obtaining 25-hydroxy-7-ketocholesterol after separation treatment of the reaction solution. The raw materials and reagents used in the present invention are readily available and environmentally-friendly. The synthesis method for 25-hydroxy-7-ketocholesterol provided by the present invention avoids the use of the metal Cr, the oxidant PCC and the like that pollute the environment seriously, and is good in reaction sclectivity, high in yield, low in cost, simple in treatment thereafter, less in three wastes, easy in product separation and high in purity.

PCT No. PCT / JP96 / 02369 Sec. 371 Date Feb. 26, 1998 Sec. 102(e) Date Feb. 26, 1998 PCT Filed Aug. 26, 1996 PCT Pub. No. WO97 / 08336 PCT Pub. Date Mar. 6, 1997A method for preparing at least one hydroxycholesterol chosen from the group consisting of 25-hydroxycholesterol, 17,25-dihydroxycholesterol and 25,26-dihydroxycholesterol by biological hydroxylation of cholesterol, and the aforementioned dihydroxycholesterols. In the above biological hydroxylation, a microorganism is used which has the abovementioned hydroxylation capacity and which belongs to the genus Amycolata and the genus Sphingomonas.

The invention discloses a production method of 25-hydroxycholesterol. The production method comprises the following steps: 1) protecting 3-hydroxyl of 24-dehydrocholesterol to obtain acylated 24-dehydrocholesterol; 2) reacting the acylated 24-dehydrocholesterol with deionized water and a halogenating reagent in a solvent at a temperature ranging from -20 DEG C to -1 DEG C for 2-4 hours to obtain a hydroxyhalogenated product; and 3) reacting the hydroxyhalogenated product with hydrogen in an organic solvent under the catalysis of an alkali and a Lindlar catalyst to obtain the 25-hydroxycholesterol. The production method of the 25-hydroxycholesterol, which is disclosed by the invention, is relatively mild in conditions, relatively short in reaction time and reliable in results because the Lindlar catalyst is used for reaction; as the hydrogen is used as a hydrogen source, the production cost of the production method is reduced and the production method is green and clean.

Disclosed are methods for determining efficacy of a cyclodextrin therapy in a subject afflicted with a disorder involving oxysterol accumulation. These methods comprise: obtaining a first body fluid sample from the subject prior to cyclodextrin administration; administering cyclodextrin; obtaining at least one second body fluid sample after the cyclodextrin administration; subjecting the body fluid samples to chromatography-mass spectroscopy analysis to determine concentration of 24-hydroxycholesterol and / or cholestane-3β,5α,6β-triol; and determining magnitude of difference between the 24-hydroxycholesterol and / or cholestane-3β,5α,6β-triol concentration of the body fluid samples, whereby an increase or stabilization of 24-hydroxycholesterol concentration, or a reduction of cholestane-3β,5α,6β-triol concentration in the at least one second sample compared to the first sample, indicates efficacy of the cyclodextrin therapy.

The present invention relates to a method for in vitro maturation of oocytes comprising the steps of:(a) culturing one or more GV oocytes in a culture medium, the culture medium comprising a nuclear maturation inhibiting substance and comprising one or more gonadotropins and / or one or more growth factors, the culturing taking place for a time period sufficient for cytoplasmatic maturation to occur;(b) washing the GV oocytes of step (a) to remove the nuclear maturation inhibiting substance;(c) culturing the washed oocytes of step (b) in a culture medium comprising one or more gonadotropins and / or one or more growth factors and / or MAS for a time period sufficient for nuclear maturation.The invention also relates to an oocyte culture medium comprising a nuclear maturation inhibiting substance and comprising one or more gonadotropins and / or one or more growth factors. The nuclear maturation inhibiting substance may be a MAS antagonist or an FF-MAS synthesis inhibitor, preferably a cytochrome P450 lanosterol 14α-demethylase (P45014DM) inhibitor e.g. ketoconazole or 22-hydroxycholesterol. The one or more gonadotropins and / or one or more growth factors are preferably a combination of EGF and FSH and / or LH.The invention also relates to the use of a nuclear maturation inhibiting substance and one or more gonadotropins and / or one or more growth factors as described above for the preparation of a cell culture medium for in vitro maturation of oocytes.

The invention discloses a synthetic method of 25-hydroxycholesterol. The synthetic method comprises the following steps: (1) protecting 3-hydroxy of 24-dehydrocholesterol so a to obtain acylated 24-dehydrocholesterol; (2) carrying out hydroxyhalogenation reaction on double bonds on the 24th site of the product obtained in the step (1), namely reacting the acylated 24-dehydrocholesterol with deionized water and a halogenated agent for 2-4 hours in a solvent at the temperature of -20 DEG C to -1 DEG C; and carrying out aftertreatment on reaction liquid so as to obtain a hydroxyhalogenation product; and (3) reacting the hydroxyhalogenation product with an aluminium hydrogenation reagent for 3-8 hours in the solvent at the temperature of 20-70 DEG C, wherein the molar ratio of the aluminium hydrogenation reagent to the hydroxyhalogenation product is (2-6): 1, and carrying out aftertreatment on reaction liquid, thus obtaining the 25-hydroxycholesterol. The synthetic method of the 25-hydroxycholesterol has the characteristics of simple process, environmental protection, few side reactions and high yield.

The present invention relates to a synthesis method for 25-hydroxy-7-ketocholesterol. The method comprises: using a 25-hydroxycholesterol derivative as a raw material in an organic solvent, initiating by an initiator in the presence of an N-hydroxy catalyst; reacting 1-40 hours at a temperature of 0 DEG C-150 DEG C with air or oxygen; performing dehydration reaction for 1-20 hours by adding a dehydrant at a temperature of -20 DEG C-100 DEG C after completion of the reaction; then performing hydrolysis reaction for 1-2 hours at a temperature of 50 DEG C-80 DEG C; and obtaining 25-hydroxy-7-ketocholesterol after separation treatment of the reaction solution. The raw materials and reagents used in the present invention are readily available and environmentally-friendly. The synthesis method for 25-hydroxy-7-ketocholesterol provided by the present invention avoids the use of the metal Cr, the oxidant PCC and the like that pollute the environment seriously, and is good in reaction sclectivity, high in yield, low in cost, simple in treatment thereafter, less in three wastes, easy in product separation and high in purity.

The present invention relates to a pharmaceutical composition comprising (a) 7β-hydroxycholesterol, (b) a water soluble organic solvent, preferably propylene glycol and / or DMSO, and (c) a solubilizing agent, preferably PEG hydrated castor oil, and to a method for preparing the same. This composition is suitable for preparing an intravenously administered preparation and comprises the pharmaceutically active substance β-hydroxycholesterol, which is poorly soluble in water.

The invention discloses a 20-hydroxycholesterol-Biotin molecular probe and a preparation method and application thereof. 20-hydroxycholesterol is used as a raw material and performs condensation reaction with Biotin-OSu to obtain the 20-hydroxycholesterol-Biotin molecular probe shown as a formula (1). The preparation method has the advantages of mild reaction conditions, simple and easy operation and high yield. The invention further discloses application of the 20-hydroxycholesterol-Biotin molecular probe in identification of 20-hydroxycholesterol binding proteins.

The invention relates to an application of 22 (R)-hydroxycholesterol as 1-type poly (ADP-ribose) synthetase inhibitor. 22 (R)-hydroxycholesterol as a cholesterol analogue does not have the cytotoxic effects of common anti-tumor drugs or other 1-type poly (ADP-ribose) synthetase inhibitors, and the safety of the 22 (R)-hydroxycholesterol can be predicated. The 22 (R)-hydroxycholesterol can be widely applied as the medicine for treating cholesterol related diseases, including cardiovascular diseases, tumour and the like.

The invention discloses the application of 25-hydroxycholesterol in promoting the proliferation of chicken primordial germ cells. The inventor has studied in depth the impact of 25-hydroxycholesterol on the proliferation of chicken primordial germ cells. The results showed that adding 25‑hydroxycholesterol to the existing culture medium of chicken primordial germ cells could promote the proliferation of chicken primordial germ cells. According to the difference of adding 25-hydroxycholesterol concentration, its promotion degree to chicken primordial germ cell proliferation is different, and when 25-hydroxycholesterol concentration is 1 μ M, its action effect is the most remarkable, can effectively promote chicken primordial germ cell proliferation in vitro Proliferate, and chicken primordial germ cells can well maintain their biological characteristics in the culture medium containing this concentration of 25-hydroxycholesterol.

The invention relates to an application of 22 (R)-hydroxycholesterol as 1-type poly (ADP-ribose) synthetase inhibitor. 22 (R)-hydroxycholesterol as a cholesterol analogue does not have the cytotoxic effects of common anti-tumor drugs or other 1-type poly (ADP-ribose) synthetase inhibitors, and the safety of the 22 (R)-hydroxycholesterol can be predicated. The 22 (R)-hydroxycholesterol can be widely applied as the medicine for treating cholesterol related diseases, including cardiovascular diseases, tumour and the like.

This invention relates, e.g., to a method for inhibiting the growth and / or proliferation and / or infectivity of a virus in a cell, such as a mammalian cell (e.g. for inhibiting entry of the virus into the cell), comprising administering, or causing to be administered, to the cell, 25-hydroxycholesterol (25HC) in an amount sufficient to inhibit the growth and / or proliferation and / or infectivity of the vines in the cell. The method can be carried out in vivo or in vitro. Among the viruses that can be inhibited are, e.g., VSV, HSV, MHV68, HCV, HIV, EBOV, RVFV, RSSEV and Nipah virus. In one embodiment of the invention, the 25HC is administered topically, e.g. to a mucosal surface.

The invention discloses a 20-hydroxycholesterol-Biotin molecular probe and a preparation method and application thereof. 20-hydroxycholesterol is used as a raw material and performs condensation reaction with Biotin-OSu to obtain the 20-hydroxycholesterol-Biotin molecular probe shown as a formula (1). The preparation method has the advantages of mild reaction conditions, simple and easy operation and high yield. The invention further discloses application of the 20-hydroxycholesterol-Biotin molecular probe in identification of 20-hydroxycholesterol binding proteins.

A method for preparing at least one hydroxycholesterol chosen from the group consisting of 25-hydroxycholesterol, 17,25-dihydroxycholesterol and 25,26-dihydroxycholesterol by biological hydroxylation of cholesterol, and the aforementioned dihydroxycholesterols. In the above biological hydroxylation, a microorganism is used which has the abovementioned hydroxylation capacity and which belongs to the genus Amycolata and the genus Sphingomonas.

The invention discloses a synthetic method of 25-hydroxycholesterol. The synthetic method comprises the following steps: (1) protecting 3-hydroxy of 24-dehydrocholesterol so as to obtain acylated 24-dehydrocholesterol; (2) carrying out epoxidation reaction on double bonds on the 24th site of the product obtained in the step (1), namely carrying out epoxidation reaction on the acylated 24-dehydrocholesterol and an epoxidation reagent in a solvent II under the catalytic action of manganese salt so as to obtain an epoxidation product; and (3) carrying out reduction ring opening on the epoxidation product obtained in the step (2), namely carrying out reduction ring opening on the epoxidation product obtained in the step (2) and a reduction reagent in a solvent III so as to obtain the 25-hydroxycholesterol. The synthetic method of the 25-hydroxycholesterol has the advantages that peroxyacetic acid and meta-chloroperoxybenzoic acid which are non-toxic and low in cost are used as the epoxidation reagents and environmentally-friendly, the reaction is carried out at a low temperature, and the manganese salt is used as a catalyst and is high in selectivity.