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

doi:10.1007/s13659-025-00557-0

Natural Products and Bioprospecting ›› 2026, Vol. 16 ›› Issue (1): 4-4.DOI: 10.1007/s13659-025-00557-0

• Original Article • Previous Articles Next Articles

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

Ling-Yun Chen^1,2, Mu-Yuan Yu², E-E Luo^2,3, Wen-Ying Zong^2,3, Shu-Mei Lei^2,3, Yu Pan^2,3, Ai-Chun Lu^2,3, Cheng-Qin Liang¹, Xu-Jie Qin^2,3

1. College of Pharmacy, Guilin Medical University, Guilin 541199, 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;
3. University of Chinese Academy of Sciences, Beijing 100049, People's Republic of China

Received:2025-05-28 Online:2026-03-25 Published:2026-02-14
Contact: Cheng-Qin Liang,E-mail:cqliang@glmc.edu.cn;Xu-Jie Qin,E-mail:qinxujie@mail.kib.ac.cn
Supported by:
This study was financially supported by the National Natural Science Foundation of China (32270425 and 31970377), the Yunnan Fundamental Research Projects (202501AS070093, 202201AT070181, and 202401AT070191), the Top Young Talent of Ten Thousand Talents Program of Yunnan Province (YNWR-QNBJ-2020-253), the Reserve Talents of Young and Middle-Aged Academic and Technical Leaders of Yunnan Province (202105AC160023), and CAS Light of West China Program. We are grateful to Analysis and Testing Centre (Kunming Institute of Botany, Chinese Academy of Sciences) for NMR, HRESIMS, CD, and bioactive measurement.

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

Ling-Yun Chen^1,2, Mu-Yuan Yu², E-E Luo^2,3, Wen-Ying Zong^2,3, Shu-Mei Lei^2,3, Yu Pan^2,3, Ai-Chun Lu^2,3, Cheng-Qin Liang¹, Xu-Jie Qin^2,3

1. College of Pharmacy, Guilin Medical University, Guilin 541199, 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;
3. University of Chinese Academy of Sciences, Beijing 100049, People's Republic of China

通讯作者: Cheng-Qin Liang,E-mail:cqliang@glmc.edu.cn;Xu-Jie Qin,E-mail:qinxujie@mail.kib.ac.cn
基金资助:
This study was financially supported by the National Natural Science Foundation of China (32270425 and 31970377), the Yunnan Fundamental Research Projects (202501AS070093, 202201AT070181, and 202401AT070191), the Top Young Talent of Ten Thousand Talents Program of Yunnan Province (YNWR-QNBJ-2020-253), the Reserve Talents of Young and Middle-Aged Academic and Technical Leaders of Yunnan Province (202105AC160023), and CAS Light of West China Program. We are grateful to Analysis and Testing Centre (Kunming Institute of Botany, Chinese Academy of Sciences) for NMR, HRESIMS, CD, and bioactive measurement.

Abstract

Abstract: Rhodomyrtus tomentosa fruits serve as both functional food and medicinal resources due to their rich bioactive 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 rhodotomentodimers H-N (2-8), along with six previously described congeners (9-14). Based on the detailed inspection 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. Heterodimeric 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.

Key words: Rhodomyrtus tomentosa fruits, Phloroglucinols, hAChE inhibitory activity, Anti-VRE activity, Molecular docking

摘要： Rhodomyrtus tomentosa fruits serve as both functional food and medicinal resources due to their rich bioactive 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 rhodotomentodimers H-N (2-8), along with six previously described congeners (9-14). Based on the detailed inspection 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. Heterodimeric 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.

关键词: Rhodomyrtus tomentosa fruits, Phloroglucinols, hAChE inhibitory activity, Anti-VRE activity, Molecular docking

Ling-Yun Chen, Mu-Yuan Yu, E-E Luo, Wen-Ying Zong, Shu-Mei Lei, Yu Pan, Ai-Chun Lu, Cheng-Qin Liang, Xu-Jie Qin. Diverse phloroglucinols with hAChE inhibitory and anti-VRE effects from Rhodomyrtus tomentosa fruits[J]. Natural Products and Bioprospecting, 2026, 16(1): 4-4.

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

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

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