Sesquiterpenes and a monoterpenoid with acetylcholinesterase (AchE) inhibitory activity from Valeriana officinalis var. latiofolia in vitro and in vivo
Abstract
Acetylcholinesterase Inhibitor (AchEI) is the most extensive in all anti-dementia drugs. The extracts and isolated compounds from the Valeriana genus have shown anti-dementia bioactivity. Four new sesquiterpenoids (1-4) and a new monoterpenoid (5) were isolated from the root of Valeriana officinalis var. latiofolia. The acetylcholinesterase (AchE) inhibitory activity of isolates was evaluated by modified Ellman method in vitro. Learning and memory ability of compound 4 on mice was evaluated by the Morris water maze. The contents of acetylcholine (Ach), acetylcholine transferase (ChAT) and AchE in mice brains were determined by colorimetry. The results showed IC50 of compound 4 was 0.161 μM in vitro. Compared with the normal group, the learning and memory ability of mice and the contents of Ach and ChAT decreased in model group mice (P<0.01), while the AchE increased (P<0.01). Compared with the model group, Ach and ChAT in the positive control group, the high-dose group and the medium-dose group increased (P<0.01), while the AchE decreased (P<0.01). Compound 4 can improve the learning and memory abilities of APPswe/PSΔE9 double-transgenic mice, and the mechanism may be related to the regulation of the relative enzyme in the cholinergic system.
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Valeriana officinalis extracts, particularly volvalerenic acid K, inhibited AChE activity in a dose-dependent manner and improved learning and memory in APPswe/PS1E9 double-transgenic mice.
“Valeriana officinalis extracts, particularly volvalerenic acid K, inhibited AChE activity in a dose-dependent manner and improved learning and memory in APPswe/PS1E9 double-transgenic mice [86].”
From Cholinesterase Inhibitors from Plants and Their Potential in Alzheimer’s Treatment: Systematic Review (2025) · cites this paper as [86]
Volvalerenic acid K from Valeriana officinalis var. latifolia improved learning and memory abilities of mice, with in vitro IC50 = 0.16 μM.
“It was observed that the Volvalerenic acid K (8) improved the learning and memory abilities of mice, with IC50 = 0.16 µM in vitro.”
From Acetylcholinesterase Inhibitory Potential of Various Sesquiterpene Analogues for Alzheimer’s Disease Therapy (2021) · cites this paper as [88]
In APPswe/PS1E9 double-transgenic mice, middle and high dose groups of Volvalerenic acid K had improved AChT activity in brain tissues and significantly decreased AChE activity, causing increased learning memory.
“The results of the study showed that, in mice (APPswe/PS1E9 double-transgenic mouse) from middle and high dose groups, the AChT (acetylcholine transferase) activity had been improved in the brain tissues, while the AChE activity was significantly decreased causing an increase in the learning memory.”
From Acetylcholinesterase Inhibitory Potential of Various Sesquiterpene Analogues for Alzheimer’s Disease Therapy (2021) · cites this paper as [88]
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- Authors
- Chen, H.-W., He, X.-H., Yuan, R., Wei, B.-J., Chen, Z., Dong, J.-X., & Wang, J.
- Affiliations
- China Academy of Chinese Medical Sciences (CN)
- Corresponding author
- Dong, Jun-Xing
- Wang, Jie
- Venue
- Fitoterapia
- Publisher
- Elsevier BV
- Published
- 2016-04
- Volume
- 110
- Pages
- 142-149
- ISSN
- 0367-326X (ISSN-L)
- OpenAlex
- W2302270970
- Cited by
- 41
- References
- 42
- Citations by year
- 2026: 3 · 2025: 4 · 2024: 5 · 2023: 4 · 2022: 2 · 2021: 5 · 2020: 4 · 2019: 5 · 2018: 8 · 2017: 1
- FWCI
- 3.77
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Fitoterapia (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Major Scientific and Technological Special Project (2013ZX09301307)
- National Natural Science Foundation of China (81503421)
- Topics
- Health Sciences › Medicine › Pharmacology › Cholinesterase and Neurodegenerative Diseases
- Health Sciences › Medicine › Complementary and alternative medicine › Medicinal Plants and Neuroprotection
- Health Sciences › Medicine › Complementary and alternative medicine › Medicinal Plant Extracts Effects
- Keywords
- sesquiterpenes, monoterpenoids, acetylcholinesterase inhibition, learning and memory, cholinergic system, acetylcholine, acetylcholinesterase, root extract, natural product isolation
- MeSH terms
- Animals, Brain, Cholinesterase Inhibitors, Male, Memory, Mice, Transgenic, Sesquiterpenes, Valerian, Molecular Structure, Plant Roots, Maze Learning, Monoterpenes, Mice
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
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