title: ÐÐ¾Ð»ÐµÐºÑÐ»ÑÑÐ½ÑÐµ Ð¼ÐµÑ Ð°Ð½Ð¸Ð·Ð¼Ñ Ð´ÐµÐ¹ÑÑÐ²Ð¸Ñ ÑÐ¸ÐºÐ»Ð¾Ð³ÐµÐºÑÐ¸Ð»-Ð¿ÑÐ¾Ð¸Ð·Ð²Ð¾Ð´Ð½ÑÑ O-Ð¸Ð¼Ð¸Ð½Ð¾-Ð¸Ð·Ð¾Ð¼Ð¾ÑÐµÐ²Ð¸Ð½Ñ Ð½Ð° Ð¼Ð¾Ð´ÐµÐ»ÑÐ½ÑÐµ Ð»Ð¸Ð¿Ð¸Ð´Ð½ÑÐµ Ð¼ÐµÐ¼Ð±ÑÐ°Ð½Ñ
title: Ð²ÑÐ¿ÑÑÐºÐ½Ð°Ñ ÐºÐ²Ð°Ð»Ð¸ÑÐ¸ÐºÐ°ÑÐ¸Ð¾Ð½Ð½Ð°Ñ ÑÐ°Ð±Ð¾ÑÐ° Ð±Ð°ÐºÐ°Ð»Ð°Ð²ÑÐ°
titleType: Subtitle
title: Molecular mechanisms of action of cyclohexyl derivatives of O-imino-isourea on model lipid membranes
Creators: name: Ð§ÐµÑÐ½ÑÑÐ¾Ð²Ð°, ÐÐ°ÑÐ½Ð°
Publisher: name: Ð¡Ð°Ð½ÐºÑ-ÐÐµÑÐµÑÐ±ÑÑÐ³ÑÐºÐ¸Ð¹ Ð¿Ð¾Ð»Ð¸ÑÐµÑÐ½Ð¸ÑÐµÑÐºÐ¸Ð¹ ÑÐ½Ð¸Ð²ÐµÑÑÐ¸ÑÐµÑ ÐÐµÑÑÐ° ÐÐµÐ»Ð¸ÐºÐ¾Ð³Ð¾
Year: 2020
Subjects: ÑÐ¸ÐºÐ»Ð¾Ð³ÐµÐºÑÐ¸Ð»-Ð¿ÑÐ¾Ð¸Ð·Ð²Ð¾Ð´Ð½ÑÐµ Ð¾-Ð¸Ð¼Ð¸Ð½Ð¾-Ð¸Ð·Ð¾Ð¼Ð¾ÑÐµÐ²Ð¸Ð½Ñ
ÐºÑÐµÐ½Ð¾Ð±Ð¸Ð¾ÑÐ¸ÐºÐ¸
Ð¼Ð¾Ð´ÐµÐ»ÑÐ½ÑÐµ Ð»Ð¸Ð¿Ð¸Ð´Ð½ÑÐµ Ð¼ÐµÐ¼Ð±ÑÐ°Ð½Ñ
Ð»Ð¸Ð¿Ð¾ÑÐ¾Ð¼Ñ
cyclohexyl derivatives of o-imino-isourea
xenobiotics
model lipid membranes
liposomes

description: Ð¦Ð¸ÐºÐ»Ð¾Ð³ÐµÐºÑÐ¸Ð»-Ð¿ÑÐ¾Ð¸Ð·Ð²Ð¾Ð´Ð½ÑÐµ Ð¾-Ð¸Ð¼Ð¸Ð½Ð¾-Ð¸Ð·Ð¾Ð¼Ð¾ÑÐµÐ²Ð¸Ð½Ñ â ÐºÑÐµÐ½Ð¾Ð±Ð¸Ð¾ÑÐ¸ÐºÐ¸, Ð¾Ð±Ð»Ð°Ð´Ð°ÑÑÐ¸Ðµ Ð°Ð½ÑÐ¸ÐºÐ°Ð½ÑÐµÑÐ¾Ð³ÐµÐ½Ð½Ð¾Ð¹ Ð°ÐºÑÐ¸Ð²Ð½Ð¾ÑÑÑÑ. ÐÑÐ¸Ð¼ÐµÐ½ÐµÐ½Ð¸Ðµ Ð² ÑÐ¾Ð²ÑÐµÐ¼ÐµÐ½Ð½Ð¾Ð¹ ÑÐ°ÑÐ¼Ð°ÐºÐ¾ÑÐ¸Ð¼Ð¸Ð¸ Ð¿ÑÐµÐ¿Ð°ÑÐ°ÑÐ¾Ð² Ð½Ð° Ð¾ÑÐ½Ð¾Ð²Ðµ ÐºÑÐµÐ½Ð¾Ð±Ð¸Ð¾ÑÐ¸ÐºÐ¾Ð² Ð¸Ð¼ÐµÐµÑ ÑÑÐ´ ÑÐµÑÑÐµÐ·Ð½ÑÑ Ð¿Ð¾Ð±Ð¾ÑÐ½ÑÑ ÑÑÑÐµÐºÑÐ¾Ð². ÐÐ¾ÑÑÐ¾Ð¼Ñ Ð¸Ð·ÑÑÐµÐ½Ð¸Ðµ Ð¼ÐµÑÐ°Ð½Ð¸Ð·Ð¼Ð¾Ð² Ð´ÐµÐ¹ÑÑÐ²Ð¸Ñ ÐºÑÐµÐ½Ð¾Ð±Ð¸Ð¾ÑÐ¸ÐºÐ¾Ð² Ð½Ð° Ð±Ð¸Ð¾Ð»Ð¾Ð³Ð¸ÑÐµÑÐºÐ¸Ðµ Ð¼ÐµÐ¼Ð±ÑÐ°Ð½Ñ ÑÐ²Ð»ÑÐµÑÑÑ Ð°ÐºÑÑÐ°Ð»ÑÐ½Ð¾Ð¹ Ð·Ð°Ð´Ð°ÑÐµÐ¹ ÑÐ°ÑÐ¼Ð°ÐºÐ¾Ð»Ð¾Ð³Ð¸Ð¸ Ð¸ ÑÑÐµÐ±ÑÐµÑ Ð¸ÑÑÐ»ÐµÐ´Ð¾Ð²Ð°Ð½Ð¸Ð¹ Ñ Ð¿ÑÐ¸Ð²Ð»ÐµÑÐµÐ½Ð¸ÐµÐ¼ Ð¼Ð¾Ð´ÐµÐ»ÑÐ½ÑÑ ÑÐ¸ÑÑÐµÐ¼. Ð¦ÐµÐ»Ñ ÑÐ°Ð±Ð¾ÑÑ - ÑÑÑÐ°Ð½Ð¾Ð²Ð»ÐµÐ½Ð¸Ðµ Ð¼Ð¾Ð»ÐµÐºÑÐ»ÑÑÐ½ÑÑ Ð¼ÐµÑÐ°Ð½Ð¸Ð·Ð¼Ð¾Ð² Ð´ÐµÐ¹ÑÑÐ²Ð¸Ñ ÐºÑÐµÐ½Ð¾Ð±Ð¸Ð¾ÑÐ¸ÐºÐ¾Ð² Ð½Ð° Ð¾ÑÐ½Ð¾Ð²Ðµ Ð¾-Ð¸Ð¼Ð¸Ð½Ð¾-Ð¸Ð·Ð¾Ð¼Ð¾ÑÐµÐ²Ð¸Ð½Ñ Ð½Ð° Ð¼Ð¾Ð´ÐµÐ»ÑÐ½ÑÐµ Ð»Ð¸Ð¿Ð¸Ð´Ð½ÑÐµ Ð¼ÐµÐ¼Ð±ÑÐ°Ð½Ñ. ÐÑÐ¾Ð²ÐµÐ´ÐµÐ½Ñ ÑÐ»ÐµÐºÑÑÐ¾ÑÐ¸Ð·Ð¸Ð¾Ð»Ð¾Ð³Ð¸ÑÐµÑÐºÐ¸Ðµ Ð¸ ÑÐ»ÑÐ¾ÑÐ¸Ð¼ÐµÑÑÐ¸ÑÐµÑÐºÐ¸Ðµ Ð¸Ð·Ð¼ÐµÑÐµÐ½Ð¸Ñ Ð¸Ð·Ð¼ÐµÐ½ÐµÐ½Ð¸Ð¹ Ð³ÑÐ°Ð½Ð¸ÑÐ½Ð¾Ð³Ð¾ Ð¸ Ð´Ð¸Ð¿Ð¾Ð»ÑÐ½Ð¾Ð³Ð¾ Ð¿Ð¾ÑÐµÐ½ÑÐ¸Ð°Ð»Ð° Ð¼ÐµÐ¼Ð±ÑÐ°Ð½, Ð¾ÑÐµÐ½ÐµÐ½Ð° Ð¿ÑÐ¾Ð½Ð¸ÑÐ°ÐµÐ¼Ð¾ÑÑÑ Ð»Ð¸Ð¿Ð¸Ð´Ð½Ð¾Ð³Ð¾ Ð±Ð¸ÑÐ»Ð¾Ñ Ð¿ÑÑÐµÐ¼ Ð¸Ð·Ð¼ÐµÑÐµÐ½Ð¸Ñ ÑÑÐµÑÐºÐ¸ ÑÐ»ÑÐ¾ÑÐµÑÑÐµÐ½ÑÐ½Ð¾Ð³Ð¾ Ð¼Ð°ÑÐºÐµÑÐ° Ð¸Ð· Ð»Ð¸Ð¿Ð¸Ð´Ð½ÑÑ Ð²ÐµÐ·Ð¸ÐºÑÐ», Ð° ÑÐ°ÐºÐ¶Ðµ Ð´Ð¸ÑÑÐµÑÐµÐ½ÑÐ¸Ð°Ð»ÑÐ½Ð°Ñ ÑÐºÐ°Ð½Ð¸ÑÑÑÑÐ°Ñ Ð¼Ð¸ÐºÑÐ¾ÐºÐ°Ð»Ð¾ÑÐ¸Ð¼ÐµÑÑÐ¸Ñ ÑÑÑÐ¿ÐµÐ½Ð·Ð¸Ð¸ Ð»Ð¸Ð¿Ð¸Ð´Ð½ÑÑ Ð²ÐµÐ·Ð¸ÐºÑÐ». Ð ÑÐ°Ð±Ð¾ÑÐµ ÑÑÑÐ°Ð½Ð¾Ð²Ð»ÐµÐ½Ð¾, ÑÑÐ¾ ÑÐ¸ÐºÐ»Ð¾Ð³ÐµÐºÑÐ¸Ð»-Ð¿ÑÐ¾Ð¸Ð·Ð²Ð¾Ð´Ð½ÑÐµ Ð¾-Ð¸Ð¼Ð¸Ð½Ð¾-Ð¸Ð·Ð¾Ð¼Ð¾ÑÐµÐ²Ð¸Ð½Ñ, ZS-04, ZS-17 Ð¸ ZS-26, Ð²ÐºÐ»ÑÑÐ°ÑÑÐ¸Ðµ ÑÐ¸ÐºÐ»Ð¾Ð³ÐµÐºÑÐ¸Ð»Ð¾Ð²ÑÐ¹, Ð¿Ð¸ÑÐ¸Ð´Ð¸Ð½Ð¸Ð»Ð¾Ð²ÑÐ¹ Ð¸ Ð¸Ð·Ð¾Ð¿ÑÐ¾Ð¿Ð¸Ð»Ð¾Ð²ÑÐ¹ ÑÐ°Ð´Ð¸ÐºÐ°Ð»Ñ, ÑÐ¾Ð¾ÑÐ²ÐµÑÑÑÐ²ÐµÐ½Ð½Ð¾, Ð½Ðµ Ð¸Ð·Ð¼ÐµÐ½ÑÑÑ ÑÐ»ÐµÐºÑÑÐ¸ÑÐµÑÐºÐ¸Ñ Ð¿Ð°ÑÐ°Ð¼ÐµÑÑÐ¾Ð² Ð¼ÐµÐ¼Ð±ÑÐ°Ð½Ñ. ÐÐ¾ÐºÐ°Ð·Ð°Ð½Ð¾, ÑÑÐ¾ ÑÐ¿Ð¾ÑÐ¾Ð±Ð½Ð¾ÑÑÑ Ð¸Ð½Ð´ÑÑÐ¸ÑÐ¾Ð²Ð°ÑÑ ÑÑÐµÑÐºÑ ÑÐ»ÑÐ¾ÑÐµÑÑÐµÐ½ÑÐ½Ð¾Ð³Ð¾ Ð¼Ð°ÑÐºÐµÑÐ° Ð¸Ð· Ð»Ð¸Ð¿Ð¾ÑÐ¾Ð¼, Ð²ÐºÐ»ÑÑÐ°ÑÑÐ¸Ñ Ð¸ Ð½Ðµ ÑÐ¾Ð´ÐµÑÐ¶Ð°ÑÐ¸Ñ ÑÑÐµÑÐ¸Ð½Ñ, ÑÐ¼ÐµÐ½ÑÑÐ°ÐµÑÑÑ Ð² ÑÑÐ´Ñ: ZS-26 (Ð½Ðµ Ð±Ð¾Ð»ÐµÐµ 20%) &gt; ZS-17 â ZS-04 (Ð½Ðµ Ð±Ð¾Ð»ÐµÐµ 15 %). Ð¦Ð¸ÐºÐ»Ð¾Ð³ÐµÐºÑÐ¸Ð»-Ð¿ÑÐ¾Ð¸Ð·Ð²Ð¾Ð´Ð½ÑÐµ Ð¾-Ð¸Ð¼Ð¸Ð½Ð¾-Ð¸Ð·Ð¾Ð¼Ð¾ÑÐµÐ²Ð¸Ð½Ñ Ð½Ðµ ÑÐ°ÑÐ°ÐºÑÐµÑÐ¸Ð·ÑÑÑÑÑ Ð²ÑÑÐ°Ð¶ÐµÐ½Ð½ÑÐ¼Ð¸ ÑÑÑÐµÐºÑÐ°Ð¼Ð¸ Ð² Ð¾ÑÐ½Ð¾ÑÐµÐ½Ð¸Ð¸ ÑÐµÑÐ¼Ð¾ÑÑÐ¾Ð¿Ð½Ð¾Ð³Ð¾ Ð¿Ð¾Ð²ÐµÐ´ÐµÐ½Ð¸Ñ Ð¼ÐµÐ¼Ð±ÑÐ°Ð½Ð¾Ð¾Ð±ÑÐ°Ð·ÑÑÑÐ¸Ñ Ð»Ð¸Ð¿Ð¸Ð´Ð¾Ð²: Ð¿ÑÐ¸ ÑÐºÐ²Ð¸Ð¼Ð¾Ð»ÑÑÐ½Ð¾Ð¼ ÑÐ¾Ð¾ÑÐ½Ð¾ÑÐµÐ½Ð¸Ð¸ Ðº Ð»Ð¸Ð¿Ð¸Ð´Ñ ZS-26 ÑÐ¼ÐµÐ½ÑÑÐ°ÐµÑ ÑÐµÐ¼Ð¿ÐµÑÐ°ÑÑÑÑ Ð³Ð»Ð°Ð²Ð½Ð¾Ð³Ð¾ ÑÐ°Ð·Ð¾Ð²Ð¾Ð³Ð¾ Ð¿ÐµÑÐµÑÐ¾Ð´Ð° Ð´Ð¸Ð¿Ð°Ð»ÑÐ¼Ð¸ÑÐ¾Ð¸Ð»ÑÐ¾ÑÑÐ¾ÑÐ¾Ð»Ð¸Ð½Ð° Ð½Ð° 1 ËC, Ð° ZS-04 Ð¸ ZS-17 Ð½Ð° ÑÑÑ Ð²ÐµÐ»Ð¸ÑÐ¸Ð½Ñ Ð½Ðµ Ð²Ð»Ð¸ÑÑÑ.
description: The Cyclohexyl derivatives of o-imino-isourea are xenobiotics characterized by anticancer activity. The use of xenobiotic-based drugs in modern pharmacochemistry has a number of serious side effects. Therefore, the study of the mechanisms of action of xenobiotics on the biological membranes is an urgent task of modern pharmacology which requires the using the model systems. The purpose of the work is to establish the molecular mechanisms of action of xenobiotics based on o-imino-isourea on the model membranes. Electrophysiological and fluorimetric methods for measuring the boundary and dipole potential of the membranes, the fluorimetry of marker leakage from lipid vesicles, and the differential scanning microcalorimetry of liposome suspension have been performed. It was found that cyclohexyl derivatives of o-imino-isourea, ZS-04, ZS-17, and ZS-26, including cyclohexyl, pyridinyl and isopropyl radicals, respectively, did not change the electrical parameters of the model membranes. It was shown that the ability to induce the leakage of the fluorescence marker from liposomes, with or without sterols, decreased in the row: ZS-26 (15-20%) &gt; ZS-17 â ZS-04 (less than 15%). Cyclohexyl derivatives of o-imino-isourea did not practically change the thermotropic behavior of lipids: at equimolar ratio to lipid, ZS-26 reduced the temperature of the main phase transition of dipalmitoylphosphocholine on 1Â°C, while ZS-04 and ZS-17 did not change this parameter.