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

doi:10.1055/a-0598-4866

	In Vitro Human Dihydroorotate Dehydrogenase Inhibitory, Anti-inflammatory and Cytotoxic Activities of Alkaloids from the Seeds of Nigella glandulifera
	Gao, Jun-Bo 1,6; Zhang, Xing-Jie 2,3; Zhang, Rui-Han 2,3; Zhu, Li-Li ; Pu, De-Bing2,3 ; Li, Xiao-Li 2,3; Li, Hong-Lin 5; Xu, Min 4; Xiao, Wei-Lie 1,2,3
	2018-09-01
发表期刊	PLANTA MEDICA
ISSN	0032-0943
卷号	84 期号:14 页码:1013-1021
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.
关键词	dolabellane-type diterpene alkaloids Ranunculaceae Nigella glandulifera human dihydroorotate dehydrogenase lipopolysaccharide nitric oxide production cytotoxic activity
DOI	10.1055/a-0598-4866
语种	英语
WOS记录号	WOS:000444454300003
引用统计	被引频次：13[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/62430
专题	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.