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Peer-reviewedCC BYInternational journal of molecular sciences

A First Insight into the Biological Activity Profile of Individual Compounds of Valeriana officinalis L.

2 more authors
9 affiliations
  1. 1Laboratory of Analytical Biochemistry and Biotechnology, K.A. Timiryazev Institute of Plant Physiology, Russian Academy of Sciences, 127276 Moscow, Russia
  2. 2Laboratory of Bioanalytical Chemistry, Institute of Natural Sciences, Immanuel Kant Baltic Federal University, Universitetskaya 2, 236040 Kaliningrad, Russia
  3. 3Department of Pharmacognosy, Saint Petersburg State Chemical and Pharmaceutical University, 197376 St. Petersburg, Russia
  4. 4Laboratory of Cellular Mechanisms of Blood Homeostasis, Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, 194223 St. Petersburg, Russia
  5. 5Interdisciplinary Laboratory of Neurobiology, Sechenov Institute of Evolutional Physiology and Biochemistry, 194223 St. Petersburg, Russia
  6. 6Resource Center of Magnetic Resonance Research Methods, Saint Petersburg State University, 198504 St. Petersburg, Russia
  7. 7Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, 117997 Moscow, Russia
  8. 8Department of Bioorganic Chemistry, Leibniz-Institute of Plant Biochemistry, 06120 Halle, Germany
  9. 9Institute of Living Systems, Immanuel Kant Baltic Federal University, A. Nevskogo Street 14, 236016 Kaliningrad, Russia

Abstract

Valeriana officinalis L. is a widely spread representative of the Eurasian flora. Preparations based on valerian extracts are recognized as sedatives, antidepressants, and anxiolytics by both traditional and modern medicine. Despite the extremely high interest in the biological and pharmacological properties of valerian extracts, the composition of biologically active substances and specific activities of their components are still not completely studied. Therefore, here we address the metabolic profiles of the valerian plants with a special emphasis on their major root constituents with pronounced neuroprotective activity. The following phytochemical analysis of the V. officinalis roots led to isolation of nine compounds, including two previously undescribed iridoids—isovaltrate isovaleroyloxyisohydrin (1) and isovaltrate α-(isovaleroxy)isovaleroxyhydrin (2)—together with one previously undescribed valerenic acid derivative—2-oxovalerenic acid (3). Three previously described iridoids—iridoidvol A (4), isovaltrate isovaleroyloxyhydrin (5), and valtrate hydrine B1 (6)—along with valerenic acid (7) and its metabolites—hydroxyvalerenic (8) and acetoxyvalerenic acids (9)—were isolated. Functional assays accomplished with the isolated compounds revealed moderate antioxidant activity characteristic for all of them. Moreover, a distinct neuroprotective potential was observed for the compound 3 (and, to a lesser extent, compound 8). This potential was manifested by a preliminary antineurodegenerative effect in the model of Aβ25–35 induced cytotoxicity. In respect of thrombin-induced platelet aggregation, compounds 1, 4, and 7 demonstrated pronounced inhibitory activity, whereas compounds 2, 5, and 6 showed distinct potentiating activity. Valerenic acid showed activity on TRPV1 ion channels, manifested by both channel activation and potentiation of the capsaicin response in CHO cells expressing TRPV1. Moderate antioxidant activity was characteristic of all compounds.

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BibTeX
@article{orlova2026first,
  title = {{A First Insight into the Biological Activity Profile of Individual Compounds of Valeriana officinalis L.}},
  author = {Anastasia Orlova and Alena Soboleva and Anastasiia O. Whaley and Andrei K. Whaley and Darya Meshalkina and Stepan Gambaryan and Sergey N. Smirnov and Margarita M. Shamatova and Yuliya V. Korolkova and Sergey A. Kozlov and Eugene A. Rogozhin and Toni Ditfe and Stanislav Sukhikh and Andrej Frolov},
  journal = {International journal of molecular sciences},
  year = {2026},
  month = sep,
  doi = {10.3390/ijms27198756},
  url = {https://europepmc.org/article/PMC/PMC13664934},
  note = {CC BY},
}
RIS
TY  - JOUR
TI  - A First Insight into the Biological Activity Profile of Individual Compounds of Valeriana officinalis L.
AU  - Anastasia Orlova
AU  - Alena Soboleva
AU  - Anastasiia O. Whaley
AU  - Andrei K. Whaley
AU  - Darya Meshalkina
AU  - Stepan Gambaryan
AU  - Sergey N. Smirnov
AU  - Margarita M. Shamatova
AU  - Yuliya V. Korolkova
AU  - Sergey A. Kozlov
AU  - Eugene A. Rogozhin
AU  - Toni Ditfe
AU  - Stanislav Sukhikh
AU  - Andrej Frolov
PY  - 2026
DA  - 2026/09/30
JO  - International journal of molecular sciences
DO  - 10.3390/ijms27198756
UR  - https://europepmc.org/article/PMC/PMC13664934
AB  - Valeriana officinalis L. is a widely spread representative of the Eurasian flora. Preparations based on valerian extracts are recognized as sedatives, antidepressants, and anxiolytics by both traditional and modern medicine. Despite the extremely high interest in the biological and pharmacological properties of valerian extracts, the composition of biologically active substances and specific activities of their components are still not completely studied. Therefore, here we address the metabolic profiles of the valerian plants with a special emphasis on their major root constituents with pronounced neuroprotective activity. The following phytochemical analysis of the V. officinalis roots led to isolation of nine compounds, including two previously undescribed iridoids—isovaltrate isovaleroyloxyisohydrin (1) and isovaltrate α-(isovaleroxy)isovaleroxyhydrin (2)—together with one previously undescribed valerenic acid derivative—2-oxovalerenic acid (3). Three previously described iridoids—iridoidvol A (4), isovaltrate isovaleroyloxyhydrin (5), and valtrate hydrine B1 (6)—along with valerenic acid (7) and its metabolites—hydroxyvalerenic (8) and acetoxyvalerenic acids (9)—were isolated. Functional assays accomplished with the isolated compounds revealed moderate antioxidant activity characteristic for all of them. Moreover, a distinct neuroprotective potential was observed for the compound 3 (and, to a lesser extent, compound 8). This potential was manifested by a preliminary antineurodegenerative effect in the model of Aβ25–35 induced cytotoxicity. In respect of thrombin-induced platelet aggregation, compounds 1, 4, and 7 demonstrated pronounced inhibitory activity, whereas compounds 2, 5, and 6 showed distinct potentiating activity. Valerenic acid showed activity on TRPV1 ion channels, manifested by both channel activation and potentiation of the capsaicin response in CHO cells expressing TRPV1. Moderate antioxidant activity was characteristic of all compounds.
SN  - 1422-0067
ER  -