Selective Inhibitors of Pancreatic Cholesterol Esterase

胰腺胆固醇酯酶的选择性抑制剂

• 批准号: 6337793
• 负责人: John E. Heidrich
• 金额: $ 7.03万
• 依托单位: ALBUQUERQUE AVIAN EXOTIC/SM ANIMAL CLINC
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-06-01 至 2001-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6337793
• 关键词: acetylcholinesterase; antihypercholesterolemic agent; clinical chemistry; dietary lipid; dosage; drug adverse effect; drug design /synthesis /production; enzyme inhibitors; gastrointestinal absorption /transport; hamsters; histopathology; lipid metabolism; nonhuman therapy evaluation; nutrition related tag; pancreas enzyme; serology /serodiagnosis; urinalysis

DESCRIPTION (Scanned from the Applicant's Abstract): The specific aim of this esterase (CE) inhibitor in an acute cholesterol absorption assay. Hamsters will be gavage fed 3H-labeled cholesterol with CE-inhibitor ranging from 20-200 umoles. Twenty-four hours later, hepatic and serum cholesterol absorption will be assayed. Hepatic and serum cholesterol levels will be determined in a subchronic hamster assay. CE-inhibitor from 20-200 umoles will be fed in chow supplemented with 0.2 percent cholesterol and 0.1 percent cholic acid for 4 days. Hepatic and serum cholesterol will be determined. In a third study, toxicity will be determined following a 30 day feeding trial of CE inhibitor. The optimum dose of CE-inhibitor determined in the previous two experiments and 200 umoles will be added to chow supplemented with 1 percent cholesterol and 0.5 percent cholic acid. Clinical chemistry, hepatic and serum cholesterol, urinalysis and histopathology will be obtained.

描述（从申请人的摘要扫描）：本申请的具体目的是 酯酶（CE）抑制剂在急性胆固醇吸收试验。仓鼠会 用20-200倍CE抑制剂灌胃3 H标记胆固醇 umoles。24小时后，肝脏和血清胆固醇吸收将 进行分析。肝脏和血清胆固醇水平将在 亚慢性仓鼠试验。将在食物中饲喂20-200 umole的CE抑制剂 补充0.2%胆固醇和0.1%胆酸， 天将测定肝脏和血清胆固醇。在第三项研究中， 在CE抑制剂的30天喂养试验后测定毒性。 在前两个实验中确定的CE抑制剂的最佳剂量和 200微摩尔将被添加到补充有1%胆固醇和0.5%胆固醇的食物中。 %胆酸。临床生化、肝脏和血清胆固醇， 将获得尿液分析和组织病理学结果。

项目成果

Inhibition of pancreatic cholesterol esterase reduces cholesterol absorption in the hamster.

• DOI: 10.1186/1471-2210-4-5
• 发表时间: 2004-04-19
• 期刊: BMC pharmacology
• 作者: Heidrich JE;Contos LM;Hunsaker LA;Deck LM;Vander Jagt DL
• 通讯作者: Vander Jagt DL