Synthesis,neuroprotective and antioxidant capacity of PBN-related indanonitrones |
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| Institution: | 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China;2. Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, Guangzhou 510405, PR China;3. Key Laboratory of Uighur Medicine of Xinjiang Uygur Autonomous Region, Xinjiang Institute of Materia Medica, Urumqi 830004, PR China;4. College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow G12 8QQ, Scotland, UK |
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| Abstract: | In this work six PBN-related indanonitrones 1–6 have been designed, synthesized, and their neuroprotection capacity tested in vitro, under OGD conditions, in SH-SY5Y human neuroblastoma cell cultures. As a result, we have identified indanonitrones 1, 3 and 4 (EC50 = 6.64 ± 0.28 μM) as the most neuroprotective agents, and in particular, among them, indanonitrone 4 was also the most potent and balanced nitrone, showing antioxidant activity in three experiments LOX (100 μM), APPH (51%), DPPH (36.5%)], being clearly more potent antioxidant agent than nitrone PBN. Consequently, we have identified (Z)-5-hydroxy-N-methyl-2,3-dihydro-1H-inden-1-imine oxide (4) as a hit-molecule for further investigation. |
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| Keywords: | Antioxidant Indanonitrones Lipid peroxidation Lipoxygenase inhibitors Neuroprotection PBN Synthesis AAPH"} {"#name":"keyword" "$":{"id":"k0045"} "$$":[{"#name":"text" "_":"2 2′-azobis(2-amidinopropane) dihydrochloride DPPH"} {"#name":"keyword" "$":{"id":"k0055"} "$$":[{"#name":"text" "_":"1 1-diphenyl-2-picrylhyrazyl LP"} {"#name":"keyword" "$":{"id":"k0065"} "$$":[{"#name":"text" "_":"lipid LOX"} {"#name":"keyword" "$":{"id":"k0075"} "$$":[{"#name":"text" "_":"lipoxygenase |
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