Screening and identification of the upregulators of ATP-binding cassette transporter A1 / 药学学报
Acta Pharmaceutica Sinica
; (12): 446-451, 2012.
Article
ي Zh
| WPRIM
| ID: wpr-323021
المكتبة المسؤولة:
WPRO
ABSTRACT
ATP-binding cassette transporter A1 (ABCA1) promotes cholesterol and phospholipid efflux from cells to lipid-poor apolipoprotein A-I (apoA-I), and plays a key role in the initial steps of the whole process of reverse cholesterol transport (RCT). Upregulation of ABCA1 is beneficial for atherosclerosis (AS) prevention and/or therapy, which indicated that ABCA1 was a target for anti-AS drug development. In the previous study, a high-throughput screening method was established using ABCA1p-LUC HepG2 cell line to find the upregulators of ABCA1. In the present study, compound 2030421B was found using this method, with EC50 of 0.50 microg x mL(-1). The compound was further identified as an upregulator of ABCA1 expression by real-time quantitative reverse transcription-polymerase chain reaction (RT-PCR) and Western blotting analysis. Studies also showed that the 2030421B could induce apoA-I-mediated cholesterol efflux and inhibit lipids uptake into mouse peritoneal macrophages RAW264.7.
النص الكامل:
1
الفهرس:
WPRIM
الموضوع الرئيسي:
Pharmacology
/
Benzaldehydes
/
Biological Transport
/
RNA, Messenger
/
Molecular Structure
/
Up-Regulation
/
Cells, Cultured
/
Chemistry
/
Cholesterol
/
Apolipoprotein A-I
نوع الدراسة:
Diagnostic_studies
/
Screening_studies
المحددات:
Animals
/
Humans
اللغة:
Zh
مجلة:
Acta Pharmaceutica Sinica
السنة:
2012
نوع:
Article