Structure activity relationship study of curcumin analogues toward the amyloid-beta aggregation inhibitor |
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| Institution: | 1. Department of Chemistry, Pondicherry University, Pondicherry 605 014, India;2. Department of Organic Chemistry, University of Madras, Guindy Campus, Chennai 600025, Tamil Nadu, India;1. Pharmaceutical Research Center and Jiangsu Province Hi-Tech Key Laboratory for Bio-medical Research, School of Chemistry and Chemical Engineering, Southeast University, Nanjing 211189, China;2. State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China;1. Natsol Laboratories Private Limited, II Floor, Research & Development Building, Ramky Commercial Hub, J. N. Pharmacity, Visakhapatnam, India;2. Department of Biomedical Sciences, CVMNAH, Tuskegee University, Tuskegee, AL, USA;3. Department of Chemical Engineering, Tuskegee University, Tuskegee, AL, USA;4. Biopharmatech Consulting, Inc., Leesburg, VA, USA;5. Department of Chemical Engineering, University of Mississippi, MS, USA;6. Department of Pharmacology and Experimental Therapeutics, College of Pharmacy & Pharmaceutical Sciences, University of Toledo, OH 43614, USA;1. Department of Chemistry, Acharya Nagarjuna University, Guntur, AP, India;2. Natsol Laboratories Private Limited, II Floor, Research & Development Building, Ramky Commercial Hub, J.N. Pharmacity, Visakhapatnam, India;3. Medicinal Chemistry Research Labs, College of Pharmaceutical Sciences, Andhra University, Visakhapatnam 530 003, India |
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| Abstract: | Inhibition of the amyloid β aggregation process could possibly prevent the onset of Alzheimer’s disease. In this article, we report a structure–activity relationship study of curcumin analogues for anti amyloid β aggregation activity. Compound 7, the ideal amyloid β aggregation inhibitor in vitro among synthesized curcumin analogues, has not only potent anti amyloid β aggregation effects, but also water solubility more than 160 times that of curcumin. In addition, new approaches to improve water solubility of curcumin-type compounds are proposed. |
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| Keywords: | Curcumin Alzheimer’s disease Amyloid-beta Aggregation inhibitor Water solubility |
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