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Valerenic acid is a sesquiterpenoid that has been found in V. officinalis and has diverse biological activities.1,2,3,4,5 It selectively transactivates retinoid X receptor β (RXRβ) over RXRα and RXRγ in reporter assays using HEK293T cells (EC50s = 5.2, 27, and 43 µM, respectively), as well as the retinoic acid receptors (RARs), peroxisome proliferator-activated receptors (PPARs), liver X receptors (LXRs), farnesoid X receptor (FXR), constitutive androstane receptor (CAR), vitamin D receptor (VDR), and pregnane X receptor (PXR) at 30 µM.2 Valerenic acid also enhances GABA-induced activation of α1β2γ2-subunit containing GABA receptors in CHO cells (EC50 = 12.6 µM).3 It is cytotoxic to GLC-4 lung and COLO 320 colon cancer cells (IC50s = 127 and 124 µM, respectively).1 Valerenic acid (100 mg/kg, i.p.) decreases motor performance in the rotarod test and increases pentobarbital-induced sleeping time in mice.4 It increases the number of entries into and percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity, when administered at a dose of 12 mg/kg.5
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1. Cytotoxic potential of valerian constituents and valerian tinctures. Phytomedicine 5(3), 219-225 (1998).
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3. Clerodane diterpenes from Casearia corymbosa as allosteric GABAA receptor modulators. J. Nat. Prod. 85(5), 1201-1210 (2022).
4. Central nervous depressant activity of valerenic acid in the mouse. Planta Med. 51(1), 28-31 (1985).
5. Valerenic acid reduces anxiety-