Patent classifications
C07J53/004
Steroid derivative regulators, method for preparing the same, and uses thereof
Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound as shown in formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator of GABA .sub.A receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description. ##STR00001##
PRODUCTION METHOD OF TELOMERASE ACTIVATORS AND TELOMERASE ACTIVATORS OBTAINED BY THIS METHOD
A method for producing telomerase activators which provide to obtain new/novel molecules (metabolites) from saponin group compounds by using biotransformation with endophytic fungi and telomerase activators obtained by this method. Included is the elucidation of chemical structures and investigation of the effects of telomerase enzyme activation in cells. These molecules have the potential to be used in diseases and/or conditions that can be treated/ameliorated by telomerase activation and associated with telomere shortening (For example; HIV, degenerative diseases, acute and chronic wound healing, ex vivo cell therapies and stem cell proliferation due to increment in vitro and ex-vivo replicative capacity of cells).
SERIES OF HALOGENATED TETRACYCLIC TRITERPENE DERIVATIVES AND THEIR PREPARATION AND APPLICATION
The invention provides a series of halogenated tetracyclic triterpene derivatives and their preparation and application. It is represented by the following general structural formula:
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R.sub.1 is halogen, R.sub.2 is H, and the halogen is selected from fluorine, chlorine, bromine or iodine; or R.sub.1 and R.sub.2 are each fluorine, and R.sub.3 is an amine, alcohol, amino acid, peptide or phosphate linked to oxygen through an acyl group.
The derivatives are relatively stable in rat whole blood through pharmacokinetic studies. The absolute bioavailability after a single intragastric administration for male and female rats was 15.6% and 28.4% respectively. The mean bioavailability was 22%. The derivatives showed better in vivo activities compared with the existing standard drugs enalapril and sacubitril valsartan sodium. Meanwhile, hydrophilic prodrugs of the tetracyclic triterpenoid derivatives in the present invention were prepared. The derivatives of the present invention can be used for preparing cardiovascular medicines.
Method for Obtaining Gamma-Oryzanol
A method for obtaining γ-oryzanol comprises: (a) extracting an extract from a raw material containing γ-oryzanol by supercritical fluid extraction; (b) separating a pellet from the extract through solid-liquid separation; and (c) obtaining purified γ-oryzanol from the pellet.
Botanical Extracts and Compounds from Castanea Plants and Methods of Use
This disclosure relates to extracts from chestnut plants and compositions comprising compounds contained therein. In certain embodiments, the extracts are derived from the leaves of a Castanea plant. In certain embodiments, the disclosure relates to methods of treating or preventing bacterial infections, acne, and other related uses.
METHOD FOR EXTRACTING ASTRAGALOSIDE IV FROM FRESH RADIX ASTRAGALI
The disclosure discloses a method for extracting Astragaloside IV from fresh Radix Astragali. The method comprises the following steps: cleaning and cutting fresh Radix Astragali roots into sections, and extracting with an ethanol solution for multiple times under an ultrasonic condition; merging the extracting solutions, concentrating to remove ethanol, hydrolyzing the concentrate with sodium hydroxide-calcium hydroxide mixed alkali, filtering the precipitate; then flocculating and precipitating by using a flocculating agent chitosan, and filtering; removing impurities through a flocculation-precipitation mode and filtering with a filter screen; separating through a macroporous adsorption resin, and finally purifying through recrystallization to obtain a high-purity Astragaloside IV. The method has the advantages of easily available raw materials, low cost, high Astragaloside IV extraction efficiency, high Astragaloside IV purity and simple process, the raw materials involved in the extraction process are non-toxic and harmless, and it is suitable for large-scale industrial production.
STEROID DERIVATIVE REGULATORS, METHOD FOR PREPARING THE SAME, AND USES THEREOF
Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound as shown in formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator of GABA A receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description.
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Halogenated Cholesterol Analogues and Methods of Making and Using Same
Provided herein are halogenated cholesterol analogues, including methods of making and using the same. Also provided are methods of making radiolabeled cholesterol analogues including admixing an epoxide with a fluorine-18 source under conditions to form a radiofluorinated cholesterol analogue.
STEROID DERIVATIVE REGULATORS, METHOD FOR PREPARING THE SAME, AND USES THEREOF
Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound of formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator the of GABA.sub.A receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description.
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Method for producing microparticles from pressurized and heated starting material solution
The present invention addresses the problem of providing a method for efficiently producing uniform microparticles of curcumin and/or -oryzanol at a higher yield. The target microparticles are produced by dissolving a starting material in a solvent to give a starting material solution and then subjecting the starting material solution to crystallization by a poor solvent method to thereby deposit the starting material. To prepare the starting material solution, curcumin and/or -oryzanol are used as the starting material(s) and ethanol is used as the solvent. The starting material(s) and the solvent are stirred in a pressurized state at a temperature of 78.3-130 C. inclusive to give the starting material solution. Then, the starting material solution thus obtained is subjected to crystallization by the poor solvent method and thus the target microparticles are produced.