title: Cytotoxic activity of lignans from Justicia procumbens.
abstract: Three new lignans, Pronaphthalide A (1), Procumbiene (2), and Procumbenoside J (3), along with a novel natural product Juspurpudin (4), and twelve other known lignans were isolated from Justicia procumbens. The structures of the new compounds were elucidated by extensive spectroscopic analyses and the data of 3 provided insight into the conformational equilibria existing in it. All compounds were evaluated for their in vitro cytotoxic activity against Human LoVo and BGC-823 cell lines except for compound 2, and eight of them were found to possess potent cytotoxicity. The structure-activity relationship (SAR) analysis revealed that (i) the parent structure of 2-carbonyl arylnaphthalide lactone attached with 6 and 7-OMe was the essential element; (ii) the polarity of substituents on C-4 might significantly affect the activity; (iii) a proper cyclic lipophilic group at the C-3″ and C-5″ of apiofuranose on C-4 might enhance the activity, which could optimize the application of 3 similar to VP-16.
authors: Beijing Institute of Radiation Medicine, Beijing 100850, China.
authors: Hong
authors: H
authors: Jin
authors: Beijing University of Technology, Beijing 100124, China.
authors: Hai-Long
authors: HL
authors: Yin
authors: Beijing Institute of Radiation Medicine, Beijing 100850, China.
authors: Shi-Jun
authors: SJ
authors: Liu
authors: Beijing Institute of Radiation Medicine, Beijing 100850, China.
authors: Li
authors: L
authors: Chen
authors: Beijing Institute of Radiation Medicine, Beijing 100850, China.
authors: Ying
authors: Y
authors: Tian
authors: Beijing Institute of Radiation Medicine, Beijing 100850, China.
authors: Bin
authors: B
authors: Li
authors: Beijing Institute of Radiation Medicine, Beijing 100850, China.
authors: Qiong
authors: Q
authors: Wang
authors: Beijing Institute of Radiation Medicine, Beijing 100850, China. Electronic address: djx931314@163.com.
authors: Jun-Xing
authors: JX
authors: Dong
mesh_terms: D027901:Acanthaceae / Q000737:chemistry*; D000970:Antineoplastic Agents; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004365:Drugs, Chinese Herbal / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D017705:Lignans / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D010946:Plants, Medicinal; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D004365:Drugs, Chinese Herbal; D017705:Lignans
keywords: Cytotoxic activity; Justicia procumbens; Lignans; Structure–activity relationship