title: Synthesis and SAR study of novel sarsasapogenin derivatives as potent neuroprotective agents and NO production inhibitors.
abstract: Sarsasapogenin, isolated from rhizomes of Anemarrhena asphodeloides, was found to be able to enhance memory. On the basis of the structure of Sarsasapogenin, a series of derivatives were synthesized and evaluated for their neuroprotective activity in PC12 cells and NO production inhibitory activity in RAW264.7 cell lines. The preliminary structure-activity relationship of them indicated that introduction of carbamate groups at the 3-hydroxyl position of sarsasapogenin might improve neuroprotective activity. Some synthesized derivatives such as AA3, AA4, AA9 and AA13 exhibited both notably neuroprotective activity and NO production inhibitory activity.
authors.affiliation: Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, PR China.
authors.forename: Hui
authors.initials: H
authors.lastname: Pan
authors.affiliation: Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, PR China.
authors.forename: Pham
authors.initials: P
authors.lastname: Van Khang
authors.affiliation: Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, PR China.
authors.forename: Dong
authors.initials: D
authors.lastname: Dong
authors.affiliation: Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, PR China. Electronic address: ruiwang@ecust.edu.cn.
authors.forename: Rui
authors.initials: R
authors.lastname: Wang
authors.affiliation: Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, PR China. Electronic address: malei@ecust.edu.cn.
authors.forename: Lei
authors.initials: L
authors.lastname: Ma
mesh_terms: D031403:Anemarrhena / Q000737:chemistry / Q000378:metabolism; D000818:Animals; D008264:Macrophages / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D018696:Neuroprotective Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D009569:Nitric Oxide / Q000378:metabolism; D016716:PC12 Cells; D000067996:RAW 264.7 Cells; D051381:Rats; D027343:Rhizome / Q000378:metabolism; D013150:Spirostans / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D018696:Neuroprotective Agents; D013150:Spirostans; D009569:Nitric Oxide; C046297:sarsasapogenin
keywords: Natural product; Neuroprotective activity; SAR study; Sarsasapogenin