Hypocholesteremics

A series of hypocholesteremic agents were isolated from Monascus and named monacolin J, K, and L. These polyketides were first isolated from cultures of Penicillium citrinum and they can inhibit specifically the enzyme controlling the rate of cholesterol biosynthesis. They are currently used in China in traditional and modem medicine. 

Clofibrate (91) has been in clinical use for several years as a serum triglyceride lowering agent. This drug is an important hypocholesteremic... 

Kozikowski and Li (268) also made use of this protocol for the construction of the hexahydronaphthalene portion of the hypocholesteremic agent compactin (256) (see Section 6.4.2.2). The oxime derived by from alcohol 253 (via y-lactone 252) was heated with aqueous sodium hypochlorite in the presence of triethylamine to give the tricyclic isoxazoline adduct 254 (Scheme 6.96). Reductive hydrolysis and dehydration afforded enone 255, which in several further steps led to compactin (256) (268). 

Kritchevsky D (1964) Animal techniques for evaluating hypocholesteremic drugs. In Nodine JH, Siegler PE (eds) Animal and Clinical Pharmacologic Techniques in Drug Evaluation. Year Book Medical Publishers, Inc., Chicago, pp 193-198... 

Alberts-Schonberg G, Alberts AW (1980) Hypocholesteremic fermentation products and process of preparation. US Patent 4,231,938... 

The hypocholesteremic compound 3/3-(/3-dimethylaminoethoxy)androst-5-en-17-one has been shown357 to inhibit the synthesis of the pentacyclic triterpenol tetrahymanol and of diphopterol in Tetrahymena pyriformis. 

Heterocyclic p-aryl-a-substituted propanoic acids derivatives, (V), prepared by Lohray (6) were effective in treating hypolipidemic and hypocholesteremic disorders. 

Gotteland, J.-P, Delhon, A., Junquero, D., Oms, P, Halazy, S. Design and synthesis of new hypocholesteremic organosilanes with antioxidant properties. Bioorg. Med. ChettL Lett. 1996, 6, 533-538. 

Design and synthesis of new hypocholesteremic organosilanes with antioxidant properties. Bioorg. Med. Chem. Lett. 6 533-538. 

Dextrothyroxine, the synthetic D-(+)-stereoisomer isomer of L-(-)-T4, was introduced in hypocholesteremic-hypolipidemic therapy with the premise that it would be void of calorigenic effects. The possibility of trace contamination with and metabolic conversion to T4 and congeners has restricted its use, however, especially in patients with coronary heart disease. 

Jorgensen EC, Lehman PA, Greenberg C, et al. Thyroxine analogues. VII. Antigoitrogenic, calorigenic, and hypocholesteremic activities of same aliphatic, alicyclic, and aromatic ethers of... 

QURESHI, A.A., HUANBIAO, M., PACKER, L., PETERSON, D. Isolation and identification of novel tocotrienols from rice bran with hypocholesteremic, antioxidant and antitumor properties, J. Agric. Food Chem., 2000, 48, 3130-3140. CHUNG, H.S., WOO, W.S., A quinolone alkaloid with antioxidant activity from the aleurone layer of anthocyanin-pigmented rice, J. Nat. Prod., 2001, 64, 1579-1580. 

B. B C40HJ6O24S, Mr 952.93, mp. 208-210°C. Sulfur-containing spiroketal glycosides with significant hypocholesteremic activity. They are isolated from the wood of the Taiwanese shrub Breynia officinalis (Euphorbiaceae). 

Leaf, A. Weber, P.C. 1988. AC Engl. J. Med 318 549-557. Cardiovascular effects of n-3 fatty acids. Skorve, J. Beige, R.K. 1993. Biochim. Biophys. Acta 1167 175-181. The hypocholesteremic effect of sulfur-substituted fatty acid analogues in rats fed a high carbohydrate diet. 

Probucol (DH-581, 4,4 -/rsopropylidenedlthio7bis/5,6-di-t-butylphenol7) lowers senmi cholesterol in mice, rats and monkeys without affecting serum triglycerides. Since this substance represents a new class of hypocholesteremic compounds," it would be of Interest to determine its clinical usefulness in extended studies. 

Documented effects It is an effective remedy to treat hypertension, atherosclerosis, kidney, liver, and epilepsy (Kovaleva 1971). It is a sedative for excitement of the central nervous system (Turova 1974). A decoction of the dried leaves and flowers is used to treat intestinal atonia and as an expectorant. The plant is a component of a diaphoretic tea and is added to baths. The leaves are used as a spice and in hquor production (Tsitsina 1962). The essential oil has shown antimicrobial, hypocholesteremic, and hypolipidemic activity (Nurahev and Zubaidova 1994 Takeda et al. 2008). 

Richardson, T., 1978, The hypocholesteremic effect of milk A review, /. Food Protect. 41 226. 

Limitation of cholesterol absorption either by removal of bile acids or by competitive Inhibition continued to be investigated. Cholestyramine was found to consistently reduce the LDL cholesterol with a possible offsetting of this action by a slight rise in the VLDL cholesterol . Over-all, cholestyramine had a definite hypocholesteremic action. A new copolymer of tetraethylenepentamine and epichlorohydrin, U-26597A, may be somewhat more effective than cholestyramine . The mechanism for the decreased cholesterol absorption following neomycin administration was reported to be due to the drug s ability to increase bile acid secretion as well as its known alteration of intestinal flora . The inhibition of cholesterol esterification was suggested as the mechanism for the cholesterol absorption reduction induced by cholestane-5P,5a,6p triol . 

Gordon, S., E. W. Cantrall, W. P. Cekleniak, H. J. Albers, R. Littell, and S. Bernstein The hypocholesteremic effect of 3jff-(j5-dimethyl-aminoethoxy)-androst-5-en-17-one and its mechanism of action. Biochem. biophys. Res. Commun. 6, 359 (1961). 

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