43 results about "Cholesterol biosynthesis" patented technology

Hydroxy-substituted azetidinone hypocholesterolemic agents of the formulaor a pharmaceutically acceptable salt thereof, wherein:Ar1 and Ar2 are aryl or R4-substituted aryl;Ar3 is aryl or R5-substituted aryl;X, Y and Z are -CH2-, -CH(lower alkyl)- or -C(dilower alkyl)-;R and R2 are -OR6, -O(CO)R6, -O(CO)OR9 or -O(CO)NR6R7;R1 and R3 are H or lower alkyl;q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5;R4 is selected from lower alkyl, R5, -CF3, -CN, -NO2 and halogen R5 is selected from -OR6, -O(CO)R6, -O(CO)OR9, -O(CH2)1-5OR6, -O(CO)NR6R7, -NR6R7, -NR6(CO)R7, -NR6(CO)OR9, -NR6(CO)NR7R8, -NR6SO2R9, -COOR6, -CONR6R7, -COR6, -SO2NR6R7, S(O)0-2R9, -O(CH2)1-10-COOR6, -O(CH2)1-10CONR6R7, -(lower alkylene)COOR6 and -CH=CH-COOR6;R6, R7 and R8 are H, lower alkyl or aryl-substituted IcR9 is lower alkyl, aryl or aryl-substituted lower alkyl;are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them; and a process for preparing them.

This invention discloses methods of using krill oil and compositions comprising krill oil to treat risk factors for metabolic, cardiovascular, and inflammatory disorders. The present invention also relates to methods of using compositions comprising krill oil to modulate biological processes selected from the group consisting of glucose metabolism, lipid biosynthesis, fatty acid metabolism, cholesterol biosynthesis, and the mitochondrial respiratory chain. The present invention further includes pharmaceutical and / or nutraceutical formulations made from krill oil, methods of making such formulations, and methods of administering them to treat risk factors for metabolic, cardiovascular, and inflammatory disorders.

This invention discloses methods of using krill oil and compositions comprising krill oil to treat risk factors for metabolic, cardiovascular, and inflammatory disorders. The present invention also relates to methods of using compositions comprising krill oil to modulate biological processes selected from the group consisting of glucose metabolism, lipid biosynthesis, fatty acid metabolism, cholesterol biosynthesis, and the mitochondrial respiratory chain. The present invention further includes pharmaceutical and / or nutraceutical formulations made from krill oil, methods of making such formulations, and methods of administering them to treat risk factors for metabolic, cardiovascular, and inflammatory disorders.

The invention relates to a preparation method of corn resistant starch, which uses common corn starch as raw material to produce corn resistant starch with multiple physiological functions and characteristics by combined treatment of microbial fermentation and hot pressing and cooling. The resistant starch has physiologic functions of effectively controlling body weight, preventing constipation, appendicitis, hemorrhoids and colon cancer, controlling diabetes, increasing lipid discharge, improving lipid composition, promoting absorption of zinc, calcium and magnesium ions, increasing removal of cholesterol and cholic acid, and reducing cholesterol biosynthesis, lipid absorption and fatty acid biosynthesis. The resistant starch used in food processing industry has better physicochemical properties than those of dietary fiber, low water retention capacity, good mouthfeel, no influence on food, and improve food texture. The invention solves the problems in production of resistant starch, including low yield and lack of high amylase starch in China.

The invention provides a composition and a method for lowering blood serum cholesterol levels or for preventing elevated blood serum cholesterol levels, as well as a suitable composition comprising (a) one or more phytosterols and / or phytostanols capable of reducing cholesterol absorption in the intestine and / or one or more soluble fibres capable of inhibiting ileal bile acid absorption, (b) a composition capable of inhibiting cholesterol biosynthesis, and (c) a composition capable of increasing cholesterol metabolism, wherein at least one of compositions (b) and (c) is preferably derived from plants.

A method is provided for treating, preventing or ameliorating neoplasia in a subject. This method includes administering to the subject an amount of actein or an amount of an extract of black cohosh that contains a triterpene glycoside, which amount of the actein or black cohosh is effective to treat, prevent or ameliorate the neoplasia, in combination with an amount of a statin which is effective to treat, prevent, or ameliorate the neoplasia. Related methods for treating, preventing or ameliorating breast cancer, or liver cell neoplasia are also provided. In addition, methods for modulating a cholesterol biosynthesis pathway and a stress response pathway in a subject are provided. These methods include administering to a subject a composition comprising an anti-neoplastic synergistic amount of a statin and actein. Compositions for carrying out such methods are also provided.

The present invention relates to compositions and methods for reducing cholesterolemia and its effects. More specifically, the invention is directed, in one embodiment, to methods for screening for compounds that affect cholesterol levels generally, and in particular, that affect the absorption of cholesterol. The invention also is directed to methods of screening for compounds that increase bile acid synthesis. In so doing, the inventors describe useful transgenic cells and animals which lack one or both alleles of the LXRα gene. Also provided are therapeutic methods designed to reduce cholesterol levels in suitable subjects. The reduction may be effected by decreasing cholesterol absorption, increasing bile acid synthesis, or combinations thereof. Particularly useful in decreasing cholesterol absorption are RXR agonists, for example, rexinoid compounds. Therapeutic intervention in cholesterol biosynthesis and diet are additional adjunct therapies. In addition, the present invention relates to candidate compounds that modulate the expression of ABC-1 in a cell that expresses RXR. Methods of identifying and making a modulator of ABC-1 are disclosed.

A method of promoting the generation of oligodendrocytes from oligodendrocyte precursor cells by enhancing their survival and / or maturation includes administering to the cell an effective amount of anagent that enhances and / or induces accumulation of delta8,9-unsaturated sterol intermediates of the cholesterol biosynthesis pathway in the oligodendrocyte precursor cells.

The present invention provides novel methods of reducing Flavivirus viral replication and / or infection, e.g., Dengue virus. The invention employs mevalonate decarboxylase (MVD) antagonists to inhibit the cholesterol biosynthesis pathway, thereby inhibiting viral replication / infection.

The invention provides methods for modulating, e.g., antagonizing, the activity of the Hedgehog signaling pathway, and for treating Hedgehog related disorders such as cancers (e.g., medulloblastoma). In particular, the invention provides methods for inhibiting aberrant growth states resulting from phenotypes such as Ptch loss-of-function, Hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function by administering to a mammal combinations of Smoothened inhibitors (e.g., a compound of Formula I, Formula II, or Formula III, or any of the compounds listed herein or incorporated by reference) and cholesterol biosynthesis pathway inhibitors (e.g., statins), Gli inhibitors, and / or Phosphatidylinositol 3-kinase (PI3K) inhibitors.

Belonging to the field of pharmacy, the invention relates to application of a Chinese prickly ash extract to preparation of medicaments for regulating cholesterol metabolism. In particular, the invention relates to regulation of cholesterol metabolism by a petroleum ether extract, an ethyl acetate extract and an n-butanol extract in high cholesterol and inflammation states. In vitro experiments show that in high cholesterol condition, the extracts can reduce the content of total cholesterol and secretion of an apolipoprotein B, inhibit the expression of related genes and proteins in a cholesterol biosynthesis pathway in cells, increase the expression of related genes or proteins in a reverse cholesterol transport process in cells. In vivo experiments prove that the ethyl acetate extract and n-butanol extract have anti-inflammatory activity, and improve the accumulation of inflammation-induced cholesterol in the liver by affecting expression of a liver X receptor-alpha and an ATP-binding cassette transporter gene 1. The invention further provides monomer (-)-syringaresinol-4-O-beta-D-glucoside isolated from the n-butanol extract and application thereof to regulation of cholesterol metabolism.

The invention encompasses compositions and methods for effectively treating and / or preventing diabetes and / or obesity. This is accomplished by totally addressing the multiple mechanisms that lead to such conditions. The invention includes compositions comprising a combination of agents that effectively suppress, regulate or interfere with the various biochemical processes and mechanisms that lead to diabetes and obesity. The inventive compositions used for administration to human and other mammalian subjects comprise (1) at least one agent capable of modulating expression and / or activity of one or more of peroxisome activated protein receptor gamma (PPAR-γ), CAAT / enhancer binding protein-α (C / EBPα) and Sterol Regulatory Element-Binding Protein (SREBP-1); (2) at least one agent capable of activating Wnt / β-catenin pathway; (3) at least one agent capable of activating the adenosine monophosphate-activated protein kinase (AMPK) signaling pathway; (4) at least one agent that inhibits the activity of pro-oxidants including reactive nitrogen species and reactive oxygen species (ROS); (5) at least one agent that suppresses one or more of inflammatory mediators including interleukins IL-1α, IL-1β, IL-6, NF-κB, TNF-α, matrix metalloproteinases (MMPs) and prostaglandin E2 (PGE2); (6) at least one agent capable of enhancing glucose transporter (GLUT4) and / or inhibiting glucose transporter GLUT2; (7) at least one agent that induces the expression of and / or activates adiponectin and (8) at least one agent that induces the expression of and / or activates sirtuin (SIRT1). The active agents for use herein are natural materials such as phytonutrients, vitamins and minerals. Compositions with combinations of such natural agents have the ability to prevent, reduce or treat diabetes and obesity by (a) clearing glucose and fatty acids from blood, (b) reducing the number of adipose cells and fat storage, (c) interfering with fat, glucose, and cholesterol biosynthesis, and (d) promoting fat and glucose oxidation.Since the present compositions are aimed toward normalizing metabolism and energy expenditure and managing oxidative stress and inflammation, they are also beneficial in relation to physical activity, in particular performance, endurance, fatigue and recovery during intensive and continuous exercise / exertion.

Methods of identifying agents effective as inhibitors of short heterodimer protein (SHP) and farnesoid X receptor (FXR) and promoters, cell lines and vectors used in said methods. Methods of preparing and using the agents effective as inhibitors of short heterodimer protein (SHP), including methods of using same to prevent and / or treat a condition associated with inflammatory gene activity and / or cholesterol biosynthesis in a subject. Agents effective as inhibitors of short heterodimer protein (SHP) and farnesoid X receptor (FXR) and compositions comprising same, including compositions effective in reducing inflammatory gene activity and / or cholesterol biosynthesis in a subject.

The described invention provides methods for targeting emopamil binding protein (EBP) with small molecules that induce an abnormal feedback response by lowering endogenous cholesterol biosynthesis.

The described invention provides small molecule anti-cancer compounds for treating tumors that respond to cholesterol biosynthesis inhibition. The compounds selectively inhibit the cholesterol biosynthetic pathway in tumor-derived cancer cells, but do not affect normally dividing cells.

This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.

The invention aims to prepare lozenges taking wild blueberries, wild schisandra fruits and wild acanthopanax fruits as raw materials. The lozenges have extremely high nutritional and medical values and have the effects of declining enzymes and protecting the liver, protecting the central nervous system, resisting viruses and tumors, defying ageing and inhibiting cholesterol biosynthesis. The health effect of the lozenges is irreplaceable compared with that of other products. Compared with the prior art, the lozenges disclosed by the invention have the advantages that the health function of the lozenges is higher than that of like products, and particularly, after natural pure traditional Chinese medicinal materials such as the wild acanthopanax fruits are added, the lozenges can be taken for a long time, can achieve a certain health effect on the heart, liver, eyes and the like of a human body, and overcomes the defects that the nutrition ingredients and functions of conventional lozenges are single.

Methods of identifying agents effective as inhibitors of short heterodimer protein (SHP) and farnesoid X receptor (FXR) and promoters, cell lines and vectors used in said methods. Methods of preparing and using the agents effective as inhibitors of short heterodimer protein (SHP), including methods of using same to prevent and / or treat a condition associated with inflammatory gene activity and / or cholesterol biosynthesis in a subject. Agents effective as inhibitors of short heterodimer protein (SHP) and farnesoid X receptor (FXR) and compositions comprising same, including compositions effective in reducing inflammatory gene activity and / or cholesterol biosynthesis in a subject.

Disclosed is a pharmaceutical natural composition containing both statin compounds (mevinolin and mevinolinic acid) serving as cholesterol biosynthesis inhibitors and coenzyme Q (ubiquinone-10: CoQ10 and ubiquinone-9: CoQ9) compounds which are substances that inhibit factors causing complications such as myalgia involved in long-term use of the statin, prepared using Monascus sp. and natural medicinal substances such as ginseng, mushrooms and cereals

The present invention relates to novel selection marker vectors, and methods for using these vectors to generate stable gene expression systems in eukaryotic cells utilizing any enzyme useful in the eukaryotic sterol / cholesterol biosynthetic pathway, such as a 3-ketosteroid reductase, as a metabolic selection marker to select transfected cells. In one embodiment, the method comprises transfecting cells that are auxotrophic for cholesterol with a vector encoding 3-ketosteroid reductase and at least one heterologous protein, and selecting cells that have the ability to survive in medium lacking cholesterol and / or producing the heterologous protein in these cells in chemically defined and / or serum-free media.

Water-soluble phenolics from the oil palm (Elaeis guineensis) possess significant antioxidant and health-promoting properties. This invention documents the effects of administering oil palm phenolics to mice, with the aim of identifying whether these compounds possess significant anti-obesity or anti-dyslipidemics properties for the prevention of atherosclerosis and cardiovascular disease. We first explored the gene expression changes caused by oil palm phenolics in livers of mice given a low-fat normal diet, in which fatty acid beta oxidation genes were up-regulated while five cholesterol biosynthesis genes were down-regulated. In addition, the weight gain of mice given oil palm palm phenolics was delayed, suggesting that oil palm phenolics may play a role in delaying the onset of obesity. Using Illumina microarrays, we found that the atherogenic diet caused oxidative stress, up-regulated the inflammatory response and increased the turnover of metabolites and cells in the liver, spleen and heart. In contrast, we found that oil palm phenolics showed signs of attenuating the effects of the atherogenic diet in mice. The extract increased unfolded protein response in the liver, while attenuated antigen presentation and processing in the spleen. Oil palm phenolics also increased the expression of antioxidant genes in the heart. A majority of the genes regulated by oil palm phenolics in the different organs showed a difference in direction of regulation when compared to the atherogenic diet.

Disclosed is a pharmaceutical natural composition containing both statin compounds (mevinolin and mevinolinic acid) serving as cholesterol biosynthesis inhibitors and coenzyme Q (ubiquinone-10: CoQ10 and ubiquinone-9: CoQ9) compounds which are substances that inhibit factors causing complications such as myalgia involved in long-term use of the statin, prepared using Monascus sp. and natural medicinal substances such as ginseng, mushrooms and cereals.

A purpose of the present invention is to prepare buccal tablets using wild schisandra chinensis fruit and wild acanthopanax senticosus fruit as raw materials. According to the present invention, the schisandra chinensis buccal tablets have effects of high nutrition and medicinal value, enzyme reducing, liver protection, central nervous system protection, anti-virus, anti-tumor, anti-aging, cholesterol biosynthesis inhibiting and the like, wherein the health effects cannot be replaced by other products; and compared to the buccal tablets in the prior art, the buccal tablets of the present invention have the following advantages that the health functions are superior to the similar products, and a certain health effect can be provided for heart, liver, eyes and the like of people after the long-term consumption especially by adding the natural pure Chinese herb such as the wild acanthopanax senticosus fruit so as to overcome the disadvantages of single nutrient and single function of the existing buccal tablets.

The present invention relates to compositions and methods for reducing cholesterolemia and its effects. More specifically, the invention is directed, in one embodiment, to methods for screening for compounds that affect cholesterol levels generally, and in particular, that affect the absorption of cholesterol. The invention also is directed to methods of screening for compounds that increase bile acid synthesis. In so doing, the inventors describe useful transgenic cells and animals which lack one or both alleles of the LXRα gene. Also provided are therapeutic methods designed to reduce cholesterol levels in suitable subjects. The reduction may be effected by decreasing cholesterol absorption, increasing bile acid synthesis, or combinations thereof. Particularly useful in decreasing cholesterol absorption are RXR agonists, for example, rexinoid compounds. Therapeutic intervention in cholesterol biosynthesis and diet are additional adjunct therapies. In addition, the present invention relates to candidate compounds that modulate the expression of ABC-1 in a cell that expresses RXR. Methods of identifying and making a modulator of ABC-1 are disclosed.

The present invention relates to methods for the diagnosis or prognosis of conditions caused by defects in cholesterol biosynthesis, such as Smith-Lemli-Opitz syndrome (SLOS), in particular to early diagnostic methods including in utero methods. In one aspect, the method compries detecting in a biological sample levels of delta-5 bile acid conjugated with 2-(acetylamino)-2-deoxy-D-glucose (GlcNAc) of formula (I)