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In Vitro Human Dihydroorotate Dehydrogenase Inhibitory, Anti-inflammatory and Cytotoxic Activities of Alkaloids from the Seeds of Nigella glandulifera

文献类型：期刊论文

作者Gao, Jun-Bo1,6; Zhang, Xing-Jie2,3; Zhang, Rui-Han2,3; Zhu, Li-Li; Pu, De-Bing2,3; Li, Xiao-Li2,3; Li, Hong-Lin5; Xu, Min4; Xiao, Wei-Lie1,2,3
刊名PLANTA MEDICA
出版日期2018-09-01
卷号84期号:14页码:1013-1021
ISSN号0032-0943
关键词dolabellane-type diterpene alkaloids Ranunculaceae Nigella glandulifera human dihydroorotate dehydrogenase lipopolysaccharide nitric oxide production cytotoxic activity
DOI10.1055/a-0598-4866
英文摘要Four new dolabellane-type diterpene alkaloids, glandulamines A-D (1-4), together with twelve known compounds (5-16), were isolated from the seeds of Nigella glandulifera using repeated column chromatography and semipreparative HPLC. The structures of 1-16 were elucidated based on NMR data analysis, HRMS experiments and other spectroscopic interpretations. The absolute configuration of 5 was determined by single-crystal X-ray diffraction data for the first time. Compounds 10 and 12 showed human dihydroorotate dehydrogenase inhibitory activity with IC50 values of 61.1 +/- 5.3 and 45.9 +/- 3.0 mu M, respectively. Molecular docking of the active compound 12 and positive control teriflunomide on the inhibitor-binding site of human dihydroorotate dehydrogenase was subsequently performed to visualize the interaction pattern. In addition, compounds 8 and 10 exhibited inhibitory effects against lipopolysaccharide-induced nitric oxide production with inhibition rates of 61 and 41%, respectively, at the concentration of 10 mu M. Compounds 9 and 12 showed cytotoxic activities with cell viability varying from 29 +/- 57% at 100 mu M against T98G, U87, U251, and GL261 glioma cancer cell lines. These data provide new insights on the pharmacologically active compounds of this plant widely used in folk medicine.
资助项目Natural Science Foundation of China[81422046] ; Natural Science Foundation of China[21762048] ; Program for Changjiang Scholars and Innovative Research Team in University[IRT_17R94]
WOS研究方向Plant Sciences ; Pharmacology & Pharmacy ; Integrative & Complementary Medicine
语种英语
出版者GEORG THIEME VERLAG KG
WOS记录号WOS:000444454300003
资助机构Natural Science Foundation of China ; Program for Changjiang Scholars and Innovative Research Team in University
源URL[http://ir.kib.ac.cn/handle/151853/62430]  
专题昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室
通讯作者Xu, Min; Xiao, Wei-Lie
作者单位1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming, Yunnan, Peoples R China
2.Yunnan Univ, Key Lab Med Chem Nat Resource, Minist Educ, Sch Chem Sci & Technol, 2 North Cuihu Rd, Kunming 650091, Yunnan, Peoples R China
3.Yunnan Univ, State Key Lab Conservat & Utilizat Bioresources Y, Kunming, Yunnan, Peoples R China
4.Southeast Univ, Sch Med, Dept Pharmacol, 87 Dingjiaqiao Rd, Nanjing 210096, Jiangsu, Peoples R China
5.East China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Sch Pharm, State Key Lab Bioreactor Engn, Shanghai, Peoples R China
6.Univ Chinese Acad Sci, Beijing, Peoples R China
推荐引用方式
GB/T 7714		 Gao, Jun-Bo,Zhang, Xing-Jie,Zhang, Rui-Han,et al. In Vitro Human Dihydroorotate Dehydrogenase Inhibitory, Anti-inflammatory and Cytotoxic Activities of Alkaloids from the Seeds of Nigella glandulifera[J]. PLANTA MEDICA,2018,84(14):1013-1021.
APA Gao, Jun-Bo.,Zhang, Xing-Jie.,Zhang, Rui-Han.,Zhu, Li-Li.,Pu, De-Bing.,...&Xiao, Wei-Lie.(2018).In Vitro Human Dihydroorotate Dehydrogenase Inhibitory, Anti-inflammatory and Cytotoxic Activities of Alkaloids from the Seeds of Nigella glandulifera.PLANTA MEDICA,84(14),1013-1021.
MLA Gao, Jun-Bo,et al."In Vitro Human Dihydroorotate Dehydrogenase Inhibitory, Anti-inflammatory and Cytotoxic Activities of Alkaloids from the Seeds of Nigella glandulifera".PLANTA MEDICA 84.14(2018):1013-1021.

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来源：昆明植物研究所

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