Neuroprotection by new ligustrazine-cinnamon acid derivatives on CoCl2-induced apoptosis in differentiated PC12 cells |
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| Affiliation: | 1. School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China;2. Department of Pathology, Beijing University of Chinese Medicine, Beijing 100029, China;3. Department of Management, Beijing University of Chinese Medicine, Beijing 100029, China;1. Centre for Endocrinology and Diabetes, Institute of Human Development, Central Manchester University Hospitals NHS Foundation Trust and University of Manchester, Manchester, M13 9NT, UK;2. Weill Cornell Medical College, Doha, Qatar;1. Department of Pharmacy, “G. d’Annunzio” University, Chieti, Italy;2. Laboratory of Chemical Biology, Institute of Biochemistry, Biological Research Centre of the Hungarian Academy of Sciences, Szeged, Hungary;3. Endocannabinoid Research Group, Institute of Biomolecular Chemistry, National Research Council, Naples, Italy;1. Modern Research Center for Traditional Chinese Medicine, School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100029, China;2. State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China;1. Université de Lorraine, Institut Jean Lamour, Département CP2S (UMR CNRS 7198), Parc de Saurupt, F-54042 Nancy Cedex, France;2. Université de Lorraine, Institut Jean Lamour, Département P2M (UMR CNRS 7198), Parc de Saurupt, F-54042 Nancy Cedex, France;1. CEDECOR (UNLP-CICBA), CONICET, Departamento de Química, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, 47 y 115, 1900 La Plata, Argentina;2. Universitá degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Florence), Italy;3. Università degli Studi di Firenze, NEUROFARBA Department, Section of Pharmaceutical Chemistry, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy |
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| Abstract: | A new series of ligustrazine-cinnamon acid derivatives had been designed and synthesized as potential neuro-protective agents. Among the derivatives, 3a exhibited the promising neuroprotective activity (EC50 = 3.68 μM). Moreover, with the deep research of the drug pathway, it (the further mechanism researches) suggested compound 3a could inhibit the apoptosis of injured PC12 cells via blocking the mitochondria apoptosis pathway including up-regulation the ratio of Bcl-2/Bax, down-regulation the expression of cytochrome-c (Cyt-c) and inhibition of the activity of caspase-9 and -3. In addition, the structure-activity relationships (SARs) of novel compounds were also discussed. |
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| Keywords: | Ligustrazine-cinnamon acid derivatives Neur-protective Apoptosis pathway |
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