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Insomnia
Published in Ethan Russo, Handbook of Psychotropic Herbs, 2015
The authors posited“a positive interaction of valerian at the barbiturate binding site of the GABAA-benzodiazepine receptor complex.” They further stated,“One may conclude that valerenic acid contributes to the pharmacological efficacy of our valerian extracts” (Hiller and Zetler, 1996, p. 149).
Therapeutic modulation of retinoid X receptors – SAR and therapeutic potential of RXR ligands and recent patents
Published in Expert Opinion on Therapeutic Patents, 2019
Further natural RXR modulators were discovered in a computer-assisted screening for RXR ligands where isopimaric acid (15), dehydroabietic acid (16) and valerenic acid (1) were identified as natural RXR agonists (Figure 6). Isopimaric acid (15) and dehydroabietic acid (16) showed micromolar potency on all three subtypes with moderate transactivation efficacy in a Gal4 hybrid reporter gene assays. Valerenic acid (1, Figure 1), in contrast to 15 and 16, revealed remarkable selectivity for RXRβ (RXRα: EC50 = 27 µM, ninefold activation; RXRβ: EC50 = 5 µM, 69-fold activation; RXRγ: EC50 = 43 µM, fourfold activation) without activating other nuclear receptors like RARs, PPARs, LXRs and FXR [10].
Sleep-promoting activity of lotus (Nelumbo nucifera) rhizome water extract via GABAA receptors
Published in Pharmaceutical Biology, 2022
Yejin Ahn, Singeun Kim, Chunwoong Park, Jung Eun Kim, Hyung Joo Suh, Kyungae Jo
It was earlier documented that the oral administration of lotus leaf alkaloids significantly increases cortical GABA concentration in a dose-dependent manner (Kim et al. 2021). Similarly, the oral administration of LE increased the GABA concentration (Figure 3). GABA is a representative inhibitory neurotransmitter in the central nervous system with a sleep-promoting function. Many antianxiety and sleeping pills, including alprazolam and diazepam, function by increasing the concentration of GABA in the brain (Griffin et al. 2013). Some sleep-promoting substances including valerenic acid, baicalein and alkaloids, are also known to increase the concentration of GABA (Shi et al. 2014).
The impact of sesquiterpenes β-caryophyllene oxide and trans-nerolidol on xenobiotic-metabolizing enzymes in mice in vivo
Published in Xenobiotica, 2018
Kateřina Lněničková, Hana Svobodová, Lenka Skálová, Martin Ambrož, Filip Novák, Petra Matoušková
Activation of phase II xenobiotic-metabolizing enzymes by natural substances may result in improved detoxification of carcinogens and represents one mechanism of their anticarcinogenic effects (Moon et al., 2006). However, as only SULT activity was elevated in liver after a single dose of NER, it seems that this mechanism is not the case for tested sesquiterpenes. Although modulation of phase II enzymes, especially UGT and GST, by various fruit, vegetable and bioactive compounds have been examined both in vitro and in vivo (reviewed e.g. by Hodges & Minich, 2015; Moon et al., 2006), there is much scarcer evidence on the influence of terpenes on these enzymes. Jodynis-Liebert et al. (2000) found that several sesquiterpenes lactones isolated from Helenium aromaticum lowered the activity of GST in rat liver and kidney in vivo by 30–50% (Jodynis-Liebert et al., 2000), which is in accordance with our results. However, in vitro zerumbone (sesquiterpene occurring in tropical ginger Zingiber zerumbet Smith) caused significant induction of GST in rat normal epithelial cell line, which has been put into context with activation of Nrf2/ARE-dependent detoxification pathway. As reduced analogs did not show any inducing effect, electrophilic property is probably related to induction of phase II enzymes (Nakamura et al., 2004). In vitro study focusing on UGT revealed that valerenic acid, a sesquiterpenoid constituent of the essential oil of Valerian plant, inhibited glucuronidation of acetaminophen, estradiol, and morphine in human liver microsomes and expressed UGTs (Alkharfy & Frye, 2007). No effect on GST, UGT and SULT was documented by farnesol, trans- and cis-nerolidol in human and rat liver subcellular fractions (Spicakova et al., 2017). As far as we are aware, only this study has dealt with the impact of sesquiterpenes on SULT.