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Molecules 2017, 22(10), 1638; doi:10.3390/molecules22101638

Bioassay-Guided Isolated Compounds from Morinda officinalis Inhibit Alzheimer’s Disease Pathologies

Pharmaceutical Botany Laboratory, College of Pharmacy, Chung-Ang University, Heukseok-dong, Dongjak-gu, Seoul 151-756, Korea
Author to whom correspondence should be addressed.
Received: 20 September 2017 / Revised: 28 September 2017 / Accepted: 28 September 2017 / Published: 29 September 2017
(This article belongs to the Collection Bioactive Compounds)
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Due to the side effects of synthetic drugs, the therapeutic potential of natural products for Alzheimer’s disease (AD) has gained interest. Morinda officinalis has demonstrated inhibitory effects on geriatric diseases, such as bone loss and osteoporosis. However, although AD is a geriatric disease, M. officinalis has not been evaluated in an AD bioassay. Therefore, M. officinalis extracts and fractions were tested for AD-related activity, including inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), β-site amyloid precursor protein cleaving enzyme 1 (BACE1), and advanced glycation end-product (AGE) formation. A bioassay-guided approach led to isolation of 10 active compounds, eight anthraquinones (18), one coumarin (9), and one phytosterol (10), from n-hexane and ethyl acetate fractions of M. officinalis. The five anthraquinones (48) were stronger inhibitors of AChE than were other compounds. Compounds 3 and 9 were good inhibitors of BChE, and compounds 3 and 8 were good inhibitors of BACE1. Compounds 15 and 79 were more active than the positive control in inhibiting AGE formation. In addition, we first suggested a structure-activity relationship by which anthraquinones inhibit AChE and BACE1. Our findings demonstrate the preventive and therapeutic efficacy of M. officinalis for AD and its potential use as a natural alternative medicine. View Full-Text
Keywords: Morinda officinalis; bioassay-guided isolation; Anthraquinone; Alzheimer’s diseases; structure-activity relationship Morinda officinalis; bioassay-guided isolation; Anthraquinone; Alzheimer’s diseases; structure-activity relationship

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Lee, Y.K.; Bang, H.J.; Oh, J.B.; Whang, W.K. Bioassay-Guided Isolated Compounds from Morinda officinalis Inhibit Alzheimer’s Disease Pathologies. Molecules 2017, 22, 1638.

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