Chemical Constituents with Proprotein Convertase Subtilisin/Kexin Type 9 mRNA Expression Inhibitory Activity from Dried Immature Morus alba Fruits

• Published in: Journal of agricultural and food chemistry Vol. 65; no. 26; pp. 5316 - 5321
• Main Authors: Pel, Pisey, Chae, Hee-Sung, Nhoek, Piseth, Kim, Young-Mi, Chin, Young-Won
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 05.07.2017; Amer Chemical Soc
• Subjects: Agriculture; Agriculture, Multidisciplinary; Chemistry; Chemistry, Applied; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - isolation & purification; Food Science & Technology; Fruit - chemistry; Hep G2 Cells; Humans; Life Sciences & Biomedicine; Molecular Structure; Morus - chemistry; Physical Sciences; Plant Extracts - chemistry; Plant Extracts - isolation & purification; Proprotein Convertase 9 - antagonists & inhibitors; Proprotein Convertase 9 - chemistry; Proprotein Convertase 9 - genetics; Proprotein Convertase 9 - metabolism; RNA, Messenger - genetics; RNA, Messenger - metabolism; Science & Technology; N-(N-phenzoyl-l-phenylalanyl)-l-phenylalanol; isomoracin D; moracin C; PCSK9 mRNA expression; Morus alba fruits; N-(N-phenzoyl-L-phenylalanyl)-L-phenylalanol; LEAVES; HEPG2 CELLS; REDUCTASE; PYRROLE ALKALOIDS; L
• ISSN: 0021-8561; 1520-5118
• DOI: 10.1021/acs.jafc.7b02088

Phytochemical investigation for a chloroform-soluble extract of dried Morus alba fruits, selected by proprotein convertase subtilisin-kexin type 9 (PCSK9) mRNA expression monitoring assay in HepG2 cells, led to the isolation of a new benzofuran, isomoracin D (1), and a naturally occurring compound, N-(N-benzoyl-l-phenylalanyl)-l-phenylalanol (2), along with 13 known compounds (3–15). All of the structures were established by NMR spectroscopic data as well as MS analysis. Of the isolates, moracin C (7) was found to inhibit PCSK9 mRNA expression with an IC50 value of 16.8 μM in the HepG2 cells.