RESUMO
This review is the first attempt at systematization and analysis of the literature data (covering the last decade) on the chemical structures and specific activities of cholesterol-regulating agents. Six of thirty currently known biological targets for treating hyperlipidemia were selected and considered. All of the chemical structures under study are divided into two classes with different mechanisms of their activity: cholesterol biosynthesis blockers (HMG-CoA reductase and squalene 2,3-oxide-lanosterol cyclase inhibitors) and regulators of cholesterol transformations in the organism (PPARα and PPARα/γ agonists, inhibitors of intestinal absorption of cholesterol, cholesteryl ester transfer protein (CETP) inhibitors, and regulators of low-density-lipoprotein receptor (LDLR) expression).
Assuntos
Colesterol/metabolismo , Inibidores de Hidroximetilglutaril-CoA Redutases/farmacologia , Hipercolesterolemia/tratamento farmacológico , Receptores Ativados por Proliferador de Peroxissomo/agonistas , Colesterol/biossíntese , Humanos , Inibidores de Hidroximetilglutaril-CoA Redutases/química , Inibidores de Hidroximetilglutaril-CoA Redutases/metabolismo , Inibidores de Hidroximetilglutaril-CoA Redutases/uso terapêutico , Hipercolesterolemia/metabolismo , Hipercolesterolemia/fisiopatologia , Receptores Ativados por Proliferador de Peroxissomo/químicaRESUMO
Information on the structure and biological activity of animal alkaloids, polymethyleneamine components of spider and wasp venoms, is considered and systematized. These natural compounds are used for the development and modification of medicines for treating the functional disturbances in the central nervous system of humans.
Assuntos
Alcaloides/química , Neurotoxinas/química , Venenos de Aranha/química , Aranhas/química , Venenos de Vespas/química , Vespas/química , Alcaloides/metabolismo , Alcaloides/uso terapêutico , Animais , Doenças do Sistema Nervoso Central/tratamento farmacológico , Humanos , Neurotoxinas/metabolismo , Neurotoxinas/uso terapêutico , Venenos de Aranha/metabolismo , Venenos de Aranha/uso terapêutico , Aranhas/metabolismo , Venenos de Vespas/metabolismo , Venenos de Vespas/uso terapêutico , Vespas/metabolismoRESUMO
This review, issued in two parts, describes the information on the structure and biological activity of animal alkaloids derived from polymethyleneamines and produced by marine organisms, wasps, spiders, and microorganisms. Animal alkaloids are outstanding models for developing methods and drugs for the treatment of many human diseases. In the first part, we consider compounds produced by marine and microbial organisms. Some promising synthetic analogues of these alkaloids are used in developing modem preparations for the chelate therapy of excessive blood iron content and antituberculosis, antiproliferative, and immunosuppressive drugs. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2005, vol. 31, no. 6; see also http://www.maik.ru.
