Efficient Semisynthesis of (-)-Pseudoirroratin A from (-)-Flexicaulin A and Assessment of Their Antitumor Activities

CORC > 昆明植物研究所 > 中国科学院昆明植物研究所 > 植物化学与西部植物资源持续利用国家重点实验室

	Efficient Semisynthesis of (-)-Pseudoirroratin A from (-)-Flexicaulin A and Assessment of Their Antitumor Activities
	Guo, Lei 1,2,3; Tsang, Siu Wai 4; Zhang, Tong-Xin 5; Liu, Kang-Lun 4; Guan, Yi-Fu 4; Wang, Bo 6; Sun, Han-Dong7 ; Zhang, Hong-Jie 4; Wong, Man Shing 1,2
刊名	ACS MEDICINAL CHEMISTRY LETTERS
	2017-03-01
卷号	8 期号:3 页码:372-376
关键词	(-)-Pseudoirroratin A (-)-flexicaulin A apoptosis antitumor activity
英文摘要	Accumulating evidence indicates that natural ent-kaurane diterpenoids show great potential for medical treatment of different pathological conditions including cytotoxicity, antibacterial, and anti-inflammatory activity. Among a variety of diterpenoids tested, (-)-pseudoirroratin A displayed a promising antitumor property in vitro and in vivo. However, this diterpenoid could merely be isolated in a limited amount from a rare source of Isodon pseudoirrorata. To overcome such scanty source, we developed a novel, facile, and efficient semisynthetic strategy to prepare (-)-pseudoirroratin A from natural (-)-flexicaulin A, which can be expediently obtained from I. flexicaulis in a great quantity. The three-dimensional structure and the absolute configuration of our synthetic diterpenoid have been determined and confirmed with the X-ray crystallographic analysis. More importantly, we demonstrated for the first time that pseudoirroratin A exerted significant cytotoxicity against human colorectal carcinoma cells via an induction of apoptosis, as well as a remarkable suppression on tumor growth in a colon cancer xenograft mouse model.
类目[WOS]	Chemistry, Medicinal
研究领域[WOS]	Pharmacology & Pharmacy
关键词[WOS]	ENT-KAURANE DITERPENOIDS ; LEUKEMIC-CELLS ; DIFFERENTIATION ; APOPTOSIS ; DEATH
收录类别	SCI
语种	英语
WOS记录号	WOS:000396297700021
内容类型	期刊论文
源URL	[http://ir.kib.ac.cn/handle/151853/51011]
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
作者单位	1.Hong Kong Baptist Univ, Dept Chem, Kowloon Tong, Hong Kong, Peoples R China 2.Hong Kong Baptist Univ, Inst Adv Mat, Kowloon Tong, Hong Kong, Peoples R China 3.Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China 4.Hong Kong Baptist Univ, Sch Chinese Med, Kowloon Tong, Hong Kong, Peoples R China 5.Liaocheng Univ, Dept Pharm, Shandong, Peoples R China 6.BioTools Inc, 17546 Bee Line Hwy, Jupiter, FL 33458 USA 7.Chinese Acad Sci, State Key Lab Phytochem & Plant Resources West Ch, Kunming, Peoples R China
推荐引用方式 GB/T 7714	Guo, Lei,Tsang, Siu Wai,Zhang, Tong-Xin,et al. Efficient Semisynthesis of (-)-Pseudoirroratin A from (-)-Flexicaulin A and Assessment of Their Antitumor Activities[J]. ACS MEDICINAL CHEMISTRY LETTERS,2017,8(3):372-376.
APA	Guo, Lei.,Tsang, Siu Wai.,Zhang, Tong-Xin.,Liu, Kang-Lun.,Guan, Yi-Fu.,...&Wong, Man Shing.(2017).Efficient Semisynthesis of (-)-Pseudoirroratin A from (-)-Flexicaulin A and Assessment of Their Antitumor Activities.ACS MEDICINAL CHEMISTRY LETTERS,8(3),372-376.
MLA	Guo, Lei,et al."Efficient Semisynthesis of (-)-Pseudoirroratin A from (-)-Flexicaulin A and Assessment of Their Antitumor Activities".ACS MEDICINAL CHEMISTRY LETTERS 8.3(2017):372-376.