Inhibitory effects of hydroxylated cinnamoyl esters on lipid absorption and accumulation

被引：9

作者：

Imai, Masahiko ^{[1
]}

Kumaoka, Takaya ^{[1
]}

Hosaka, Makiko ^{[1
]}

Sato, Yui ^{[1
]}

Li, Chuan ^{[1
]}

Sudoh, Masashi ^{[2
]}

Tamada, Yoshiko ^{[2
]}

Yokoe, Hiromasa ^{[2
]}

Saito, Setsu ^{[2
]}

Tsubuki, Masayoshi ^{[2
]}

Takahashi, Noriko ^{[1
]}

机构：

[1] Hoshi Univ, Inst Med Chem, Physiol Chem Lab, Shinagawa, Tokyo 1428501, Japan

[2] Hoshi Univ, Inst Med Chem, Bioorgan Chem Lab, Shinagawa, Tokyo 1428501, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2015年 / 23卷 / 13期

关键词：

Lipase; Lipid absorption; Lipid accumulation; Anti-obesity; Caffeic acid phenylethyl ester; ACID PHENETHYL ESTER; FACTOR-KAPPA-B; PANCREATIC LIPASE; ANTIOXIDANT PROPERTIES; METABOLIC SYNDROME; GENE-EXPRESSION; IN-VITRO; OBESITY; CELLS; ADIPOCYTES;

D O I：

10.1016/j.bmc.2015.03.086

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Obesity is a risk factor associated with several lifestyle-related diseases, for example, diabetes, high blood pressure, hyperlipidemia and cancer. Caffeic acid 2-phenylethyl ester (CAPE, 1), a naturally-occurring compound found in various plants and propolis, which exhibits anti-inflammatory, immunomodulatory and cytotoxic activities and inhibits 3T3-L1 differentiation to adipocytes. As part of our efforts to moderate lifestyle-related diseases, we synthesized analogs of 1 and studied their effects on pancreatic lipase activities, lipid absorption, and 3T3-L1 differentiation. We found that catechols 1-4 show inhibitory activities against pancreatic lipase in a dose-dependent manner in vitro. Compounds 1-3 proved to be more potent inhibitors of pancreatic lipase than 5, 6, 8, and 9, which have one hydroxyl group, respectively. Compound 7 has three aromatic hydroxyl groups and restrains greater lipase inhibitory activity than the other compounds. In addition, 7 and 3 significantly suppress a rise in blood triglyceride (TG) levels in mice given corn oil orally. Furthermore, 2 and 3 are more potent at preventing 3T3-L1 differentiation (lipid accumulation) than 1, while 7 is more potent than 3, 8, and 9 in these assays. Compounds 2, 3, and 7 inhibit lipid absorption and accumulation, with new compound 7 being the most potent. These results indicate that 7 may have potential benefits as a health agent with anti-obesity properties. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：3788 / 3795

页数：8

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