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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