BACE1 (beta-secretase) inhibitory phenolic acids and a novel sesquiterpenoid from Homalomena occulta.
Four phenolic acids, namely 2-[(Z)-heptadec-11-enyl]-6-hydroxybenzoic acid (1), 2-[(6Z,9Z,12Z)-heptadeca-6,9,12-trienyl]-6-hydroxybenzoic acid (2), 2-[(9Z,12Z)-heptadeca-9,12-dienyl]-6-hydroxybenzoic acid (3), and 2-hydroxy-6-(12-phenyldodecyl)benzoic acid (4), and one sesquiterpene, asperpenoid (5), were isolated from the 95% EtOH extract of the roots of Homalomena occulta, among which 1, 2, and 5 represent new compounds. Further, the phenolic acids 1-4 exhibited BACE1 (beta-secretase) inhibitory activity with IC(50) values of 6.23+/-0.94, 6.28+/-0.63, 7.93+/-0.38, and 7.65+/-0.62 microM, respectively.
Tian
Xiao-Yan
XY
Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine (Peking Union Medical College), Ministry of Education, Beijing 100050, P. R. China.
Zhao
Ying
Y
Yu
Shi-Shan
SS
Fang
Wei-Shuo
WS
D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D029064:Araceae / Q000737:chemistry*; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D062385:Hydroxybenzoates / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008968:Molecular Conformation; D018696:Neuroprotective Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D018517:Plant Roots / Q000737:chemistry; D012459:Salicylates / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology
D062385:Hydroxybenzoates; D018696:Neuroprotective Agents; D012459:Salicylates; D053829:Amyloid Precursor Protein Secretases; D016282:Aspartic Acid Endopeptidases; C509280:BACE1 protein, human; C017616:phenolic acid