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天然存在的菲并吲哚里西啶生物碱安托芬通过直接抑制PPARγ表达发挥抗脂肪生成活性。

Anti-adipogenic activity of the naturally occurring phenanthroindolizidine alkaloid antofine via direct suppression of PPARγ expression.

作者信息

Jang Eun Jung, Kim Hyo Kyeong, Jeong Hana, Lee Ye Seul, Jeong Mi Gyeong, Bae Su Jung, Kim Sanghee, Lee Sang Kook, Hwang Eun Sook

机构信息

College of Pharmacy and Graduate school of Pharmaceutical Sciences, Global Top5 Research Program, Ewha Womans University, 52 Ewhayeodae-gil, Seodaemun-gu, Seoul 120-750, Korea, (phone: +82-2-32774369; fax: +82-2-32773760).

出版信息

Chem Biodivers. 2014 Jun;11(6):962-9. doi: 10.1002/cbdv.201300365.

DOI:10.1002/cbdv.201300365
PMID:24934681
Abstract

Antofine (ANTF) is a phenanthroindolizidine alkaloid isolated from the root of Cynanchum paniculatum Kitagawa (Asclepiadaceae), which is used as an herbal remedy for pain and inflammation. ANTF also possesses antiviral and antitumorigenic activities. In this study, we investigated the role of ANTF in adipogenesis. Chronic ABTF administration suppressed adipocyte differentiation and marker expression in a dose-dependent manner. Furthermore, acute administration of ANTF at early stages of differentiation process inhibited lipid droplet formation and adipogenic gene expression. ANTF Treatment decreased expression of PPARγ protein, a master transcription factor in the regulation of adipocyte differentiation, leading to a suppression of aP2 promoter activity. These results suggest that ANTF exerts potent anti-adipogenic effects via direct suppression of PPARγ protein expression, with consequent downregulation of adipogenic gene expression.

摘要

安托非宁(ANTF)是一种从北沙参(萝藦科)根部分离出的菲并吲哚里西啶生物碱,它被用作治疗疼痛和炎症的草药。ANTF还具有抗病毒和抗肿瘤活性。在本研究中,我们研究了ANTF在脂肪生成中的作用。长期给予ABTF以剂量依赖性方式抑制脂肪细胞分化和标志物表达。此外,在分化过程的早期急性给予ANTF可抑制脂滴形成和脂肪生成基因表达。ANTF处理降低了PPARγ蛋白的表达,PPARγ蛋白是调节脂肪细胞分化的主要转录因子,导致aP2启动子活性受到抑制。这些结果表明,ANTF通过直接抑制PPARγ蛋白表达发挥强大的抗脂肪生成作用,从而导致脂肪生成基因表达下调。

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Possible pharmaceutical applications can be developed from naturally occurring phenanthroindolizidine and phenanthroquinolizidine alkaloids.
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Phytochem Rev. 2021;20(4):845-868. doi: 10.1007/s11101-020-09723-3. Epub 2020 Sep 25.
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Antofine suppresses endotoxin-induced inflammation and metabolic disorder via AMP-activated protein kinase.安托芬通过AMP活化蛋白激酶抑制内毒素诱导的炎症和代谢紊乱。
Pharmacol Res Perspect. 2017 Aug;5(4). doi: 10.1002/prp2.337.