Oligomeric phloroglucinols with hAChE inhibitory and antibacterial activities from tropic Rhodomyrtus tomentosa

doi:10.1016/j.bioorg.2023.106836

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	Oligomeric phloroglucinols with hAChE inhibitory and antibacterial activities from tropic Rhodomyrtus tomentosa
	Luo,E-E; Liu,Si-Na; Wang,Zhao-Jie; Chen,Ling-Yun; Liang,Cheng-Qin; Yu,Mu-Yuan; Qin,Xu-Jie
	2023
发表期刊	BIOORGANIC CHEMISTRY
ISSN	1090-2120
卷号	141 页码:106836
摘要	Alzheimer's diseases (AD) and other infectious diseases caused by drug-resistance bacteria have posed a serious threat to human lives and global health. With the aim to search for human acetylcholinesterase (hAChE) inhibitors and antibacterial agents from medicinal plants, 16 phloroglucinol oligomers, including two new phloroglucinol monomers (1a and 1b), four new phloroglucinol dimers (3a, 3b, 4b, and 5a), six new phloroglucinol trimers (6a, 6b, 7a, 7b, 8a, and 8b), and two naturally occurring phloroglucinol monomers (2a and 2b), along with two known congeners (4a and 5b), were purified from the leaves of tropic Rhodomyrtus tomentosa. The structures and absolute configurations of these new isolates were unequivocally established by comprehensive analyses of their spectroscopic data (NMR and HRESIMS), ECD calculation, and single crystal Xray diffraction. Structurally, 3a/3b shared a rare C-5 ' formyl group, whereas 6a/6b possessed a unique C-7 ' aromatic ring. In addition, 7a/7b and 8a/8b were rare phloroglucinol trimers with a bis-furan and a C-6 ' hemiketal group. Pharmacologically, the mixture of 3a and 3b showed the most potent human acetylcholinesterase (hAChE) inhibitory activity with an IC50 value of 1.21 +/- 0.16 mu M. The molecular docking studies of 3a and 3b in the hAChE binding sites were performed, displaying good agreement with the in vitro inhibitory effects. In addition, the mixture of 3a and 3b displayed the most significant anti-MRSA (methicillin-resistant Staphylococcus aureus) with MIC and MBC values of both 0.50 mu g/mL, and scanning electron microscope (SEM) studies revealed that they could destroy the biofilm structures of MRSA. The findings provide potential candidates for the further development of anti-AD and anti-bacterial agents.
关键词	Rhodomyrtus tomentosa Oligomeric phloroglucinols h AChE inhibitors Molecular docking Antibacterial effects MYRTUCOMMULONE DERIVATIVES ACYLPHLOROGLUCINOLS MYRTUCOMMUACETALONE LEAVES
DOI	10.1016/j.bioorg.2023.106836
收录类别	SCI
WOS记录号	WOS:001084335300001
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/75472
专题	中国科学院昆明植物研究所
推荐引用方式 GB/T 7714	Luo,E-E,Liu,Si-Na,Wang,Zhao-Jie,et al. Oligomeric phloroglucinols with hAChE inhibitory and antibacterial activities from tropic Rhodomyrtus tomentosa[J]. BIOORGANIC CHEMISTRY,2023,141:106836.
APA	Luo,E-E.,Liu,Si-Na.,Wang,Zhao-Jie.,Chen,Ling-Yun.,Liang,Cheng-Qin.,...&Qin,Xu-Jie.(2023).Oligomeric phloroglucinols with hAChE inhibitory and antibacterial activities from tropic Rhodomyrtus tomentosa.BIOORGANIC CHEMISTRY,141,106836.
MLA	Luo,E-E,et al."Oligomeric phloroglucinols with hAChE inhibitory and antibacterial activities from tropic Rhodomyrtus tomentosa".BIOORGANIC CHEMISTRY 141(2023):106836.

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