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Diverse phloroglucinols with hAChE inhibitory and anti-VRE effects from Rhodomyrtus tomentosa fruits

摘要Rhodomyrtus tomentosa fruits serve as both functional food and medicinal resources due to their rich bioac-tive constituents and manifold pharmacological effects.Phytochemical exploration of the R.tomentosa fruits led to the identification of eight new polymethylated phloroglucinols,designated as rhodotomentodione F(1)and rho-dotomentodimers H-N(2-8),along with six previously described congeners(9-14).Based on the detailed inspec-tion of comprehensive spectroscopic data,electronic circular dichroism(ECD)simulations,and nuclear magnetic resonance(NMR)calculations,and DP4+analyses,the structures of phloroglucinols 1-8 were determined.Heterodi-meric phloroglucinols 3-14 exhibited human acetylcholinesterase(hAChE)inhibitory activities,with 13 exhibiting the highest potency(IC50=1.04 μM).Moreover,molecular docking analysis clarified the potential binding interactions between the most active phloroglucinol 13 with hAChE.In addition,phloroglucinols 11 and 12 displayed significant anti-VRE(vancomycin-resistant Enterococci)activities,with MIC values reaching as low as 1 μg/mL.

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作者 Ling-Yun Chen [1] Mu-Yuan Yu [2] E-E Luo [3] Wen-Ying Zong [3] Shu-Mei Lei [3] Yu Pan [3] Ai-Chun Lu [3] Cheng-Qin Liang [4] Xu-Jie Qin [3] 学术成果认领
作者单位 College of Pharmacy,Guilin Medical University,Guilin 541199,People's Republic of China;State Key Laboratory of Phytochemistry and Natural Medicines,Kunming Institute of Botany,Chinese Academy of Sciences,Kunming 650201,People's Republic of China [1] State Key Laboratory of Phytochemistry and Natural Medicines,Kunming Institute of Botany,Chinese Academy of Sciences,Kunming 650201,People's Republic of China [2] State Key Laboratory of Phytochemistry and Natural Medicines,Kunming Institute of Botany,Chinese Academy of Sciences,Kunming 650201,People's Republic of China;University of Chinese Academy of Sciences,Beijing 100049,People's Republic of China [3] College of Pharmacy,Guilin Medical University,Guilin 541199,People's Republic of China [4]
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DOI 10.1007/s13659-025-00557-0
发布时间 2026-05-09(万方平台首次上网日期,不代表论文的发表时间)
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