Polymethylated acylphloroglucinols from Rhodomyrtus tomentosa exert acetylcholinesterase inhibitory effects

doi:10.1016/j.bioorg.2020.104519

KIB OpenIR

	Polymethylated acylphloroglucinols from Rhodomyrtus tomentosa exert acetylcholinesterase inhibitory effects
	Qin,Xu-Jie ; Liu,Hui ; Li,Pan-Pan ; Ni,Wei ; He,Li ; Khan,Afsar ; Hao,Xiao-Jiang; Liu,Hai-Yang
	2021
发表期刊	BIOORGANIC CHEMISTRY
ISSN	0045-2068
卷号	107 页码:104519
摘要	Chemical investigation of the twigs and leaves of Rhodomyrtus tomentosa led to the isolation and structural identification of a novel polymethylated phloroglucinol meroterpenoid (PPM) featuring a 6/6/6/6 tetracyclic system, rhotomentodione F (1), five new polymethylated polycyclic phloroglucinols (PPPs) with a rare bis-furan framework, rhotomentosones A-E (2-6), and one new adduct composed of an acylphloroglucinol and two beta-triketone units, rhotomentosone F (7), as well as five known analogues (8-12). Their structures and absolute configurations were unambiguously determined by comprehensive spectroscopic data and electronic circular dichroism (ECD) calculations. All isolates were evaluated for their anti-inflammatory and acetylcholinesterase (AChE) inhibitory activities. Compound 6 displayed significant AChE inhibitory effect with an IC50 value of 8.68 mu M. Further molecular docking studies of 6 revealed that the interactions with AChE residues Ser125, Glu202, and Tyr133 are crucial for AChE inhibitory activity. The current study not only enriches the chemical diversity of phloroglucinols in Myrtaceae species, but also provides potential lead compounds for the further design and development of new AChE inhibitors to treat Alzheimer's disease.
关键词	Rhodomyrtus tomentosa Polymethylated acyphloroglucinols AChE inhibitory effect Molecular docking PHLOROGLUCINOL MEROTERPENOIDS LEAVES DERIVATIVES TWIGS BETA
DOI	10.1016/j.bioorg.2020.104519
WOS记录号	WOS:000618105400005
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/73469
专题	中国科学院昆明植物研究所
作者单位	1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Kunming Med Univ, Affiliated Hosp 1, Dept Dermatol, Kunming 650032, Yunnan, Peoples R China 4.COMSATS Univ Islamabad, Dept Chem, Abbottabad Campus, Abbottabad 22060, Pakistan
推荐引用方式 GB/T 7714	Qin,Xu-Jie,Liu,Hui,Li,Pan-Pan,et al. Polymethylated acylphloroglucinols from Rhodomyrtus tomentosa exert acetylcholinesterase inhibitory effects[J]. BIOORGANIC CHEMISTRY,2021,107:104519.
APA	Qin,Xu-Jie.,Liu,Hui.,Li,Pan-Pan.,Ni,Wei.,He,Li.,...&Liu,Hai-Yang.(2021).Polymethylated acylphloroglucinols from Rhodomyrtus tomentosa exert acetylcholinesterase inhibitory effects.BIOORGANIC CHEMISTRY,107,104519.
MLA	Qin,Xu-Jie,et al."Polymethylated acylphloroglucinols from Rhodomyrtus tomentosa exert acetylcholinesterase inhibitory effects".BIOORGANIC CHEMISTRY 107(2021):104519.

条目包含的文件		下载所有文件
文件名称/大小	文献类型	版本类型	开放类型	使用许可
044-D05-104.pdf（2105KB）	期刊论文	出版稿	开放获取	CC BY-NC-SA	浏览下载