Fruttamed Clinical studies
Bio-assay-Guided Isolated Compounds from Morinda Citrifolia Inhibit Alzheimer’s Disease (AD) Pathologies
Due to the serious and multiple side effects of synthetic or chemical drugs, the therapeutic potential of natural products especially medicinal mushrooms for Alzheimer’s disease (AD) has gained interest. Morinda Citrifolia has demonstrated and also clearly exhibited inhibitory effects on geriatric diseases, such as bone loss and osteoporosis. However, although AD is a geriatric disease, Morinda Citrifolia has not been evaluated in an AD bioassay. Therefore, Morinda Citrifolia 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 bio-assay-guided approach led to isolation of 10 active compounds, eight anthraquinones (1–8), one coumarin (9), and one phytosterol (10), from n-hexane and ethyl acetate fractions of M. officinalis. The five anthraquinones (4–8) were stronger inhibitors of AChE than the other compounds. Compounds 3 and 9 were good inhibitors of BChE, and compounds 3 and 8 were good inhibitors of BACE1. Compounds 1–5 and 7–9 were more active than the positive control in inhibiting AGE formation. Additionally, we first suggested a structure-activity relationship by which anthraquinones inhibit AChE and BACE1. Our findings demonstrate the preventive and therapeutic efficacy of Morinda Citrifolia for AD and its potential use as a natural alternative medicine.