Apigenin
A flavonoid that binds benzodiazepine receptors; found in chamomile.
Apigenin, a flavonoid in chamomile, may promote sleep onset via benzodiazepine receptor binding
Apigenin binds to benzodiazepine receptors and enhances GABAergic activity, promoting sedation. While preclinical evidence is strong, human clinical trials are limited. Chamomile, a natural source, has shown modest sleep benefits.
Higher dietary intake of lignans and hydroxycinnamic acids is associated with better sleep quality in Italian adults
In a cohort of 1936 Italian adults, higher dietary intake of lignans and hydroxycinnamic acids was significantly associated with lower odds of inadequate sleep quality, as measured by the Pittsburgh Sleep Quality Index. Specific compounds naringenin, apigenin, and matairesinol also showed inverse associations. The association was stronger in normal-weight individuals, while no significant associations were found in overweight/obese individuals.
Nurexan contains flavonoids (vitexin, isovitexin, orientin, isoorientin, apigenin) and alkaloids (caffeine, trigonelline) with potential pharmacological relevance for stress and sleep regulation.
Chemical analysis of Nurexan, a multicomponent natural veterinary medicinal product, identified flavonoids such as vitexin (1-2 ng per tablet) and isovitexin (4-11 ng per tablet) along with other compounds from Passiflora incarnata, Avena sativa, and Coffea arabica. These constituents may have anxiolytic and sleep-regulating effects, but their functional roles require further study.
Apigenin, luteolin, and piplartine are core active components of Sugemule-4 that bind to EGFR, potentially treating insomnia through serotonergic synapse and calcium signaling pathways.
The study identified 106 active compounds and 364 overlapping targets for Sugemule-4 in insomnia treatment. Network pharmacology and molecular docking revealed that apigenin, luteolin, and piplartine bind strongly to EGFR, with molecular dynamics confirming stable interactions, suggesting multi-target mechanisms via serotonergic synapse and calcium signaling pathways.
Phytochemicals such as resveratrol, epigallocatechin gallate, curcumin, jaceosidin, cucurbitacin, apigenin, and genistein trigger activation or inactivation of ATM in different cancer cells, modulating DNA damage response.
This review summarizes evidence from cell-based studies that various phytochemicals can modulate ATM signaling, a master regulator of DNA double-strand break repair. These compounds either activate or inhibit ATM in different cancer cell lines, potentially influencing cell cycle checkpoints, DNA repair, and apoptosis. The paper highlights the therapeutic potential of targeting ATM to enhance responses to DNA damage-inducing therapies.
Sugemule-4 exerts anti-insomnia effects through multi-target and multi-pathway mechanisms, with apigenin, luteolin, and piplartine as core active components and EGFR as a central target.
This study identified 106 active compounds and 364 overlapping targets for Sugemule-4 in insomnia treatment. Network pharmacology and molecular docking revealed that apigenin, luteolin, and piplartine are core active components, and EGFR is a central target, potentially acting through serotonergic synapse and calcium signaling pathways.
Dietary apigenin intake positively correlates with sleep quality in a large cohort of adults
A large cohort study found that higher dietary intake of apigenin, a natural flavonoid found in chamomile and other plants, is associated with better sleep quality in adults. This supports apigenin's potential role in improving sleep, though the abstract does not provide specific correlation coefficients or effect sizes.
Resveratrol, epigallocatechin gallate, curcumin, jaceosidin, cucurbitacin, apigenin, and genistein trigger activation of ATM in different cancer cells, while some agents cause ATM inactivation.
This review summarizes evidence from cell-based studies that various phytochemicals modulate ATM, the master regulator of DNA double-strand break repair. Specific compounds like resveratrol and curcumin activate ATM in cancer cells, while other agents can inactivate it, suggesting potential therapeutic applications for enhancing DNA damage-inducing therapy.
Constituents of Passiflora incarnata (apigenin, orientin, vitexin) interact with OATP2B1 and OATP1A2 transporters, potentially altering uptake of other compounds
The study found that apigenin, orientin, and vitexin from Passiflora incarnata inhibit and are substrates of OATP2B1 and OATP1A2 transporters, while valerenic acid from Valeriana officinalis only interacts with OATP2B1. Commercially available P. incarnata preparations also inhibited transporter-mediated uptake of estrone 3-sulfate, suggesting these constituents may affect the pharmacokinetics of other drugs relying on these transporters.
Valerian root extract and its flavonoids linarin and apigenin reduce sleep latency in mice
A 70% ethanolic valerian root extract at 1000 mg/kg produced a mild short-term sedative effect with reduced locomotor activity between 66-78 minutes after oral administration in male mice. Linarin at 12 mg/kg and apigenin at 1.5 mg/kg also showed mild short-term sedative effects. The authors concluded that these compounds are more effective at reducing sleep latency than maintaining sleep.
Lippia alba non-volatile extract (80% ethanol) shows sedative and myorelaxant effects in mice
The non-volatile fraction of Lippia alba extracted with 80% ethanol (ES(80%)) demonstrated the most significant sedative and myorelaxant effects in Swiss mice, along with the highest total flavonoid content (66 mg/100 g expressed as apigenin). The spray-dried powder SDP(1) (using colloidal silicon dioxide) retained a sedative profile similar to the liquid extract.
Apigenin enhances pentobarbital-induced sleep through chloride ion channel activation
Apigenin prolonged pentobarbital-induced sleep time in mice, similar to the GABA(A) receptor agonist muscimol. It also increased sleep rate and sleep time when combined with a sub-hypnotic dose of pentobarbital, and increased chloride influx in cultured cerebellar granule cells. Apigenin increased glutamate decarboxylase (GAD) expression but did not affect GABA(A) receptor subunit expression in the hippocampus.
Dracocephalum moldavica aqueous extract induces sedation and general CNS inhibition in mice
The aqueous extract of Dracocephalum moldavica prolonged pentobarbital-induced sleeping time, induced sedation in the hole-board test, decreased spontaneous activity, and impaired motor coordination in mice. The LD50 was 470 mg/kg body weight, and the main compounds were acacetin, apigenin, and luteolin-7-O-β-D-(6″-O-malonyl)-glucoside derivatives.
Chrysin exhibits anxiolytic effects in rats via activation of GABA(A) receptors, while apigenin does not show anxiolytic activity
In rats, chrysin at 1 mg/kg produced a clear anxiolytic effect that was blocked by the benzodiazepine antagonist Flumazenil, indicating GABA(A) receptor involvement. Apigenin failed to show anxiolytic effects at the same dose. Both flavonoids reduced locomotor activity at 25 mg/kg, but this sedative effect was not mediated by GABA-benzodiazepine receptors.
Constituents of Passiflora incarnata inhibit OATP2B1 and OATP1A2 transporters, potentially affecting uptake of other compounds.
Apigenin, orientin, and vitexin from Passiflora incarnata inhibited OATP2B1 and OATP1A2-mediated uptake of sulfated steroids in vitro. Orientin was a substrate of both transporters, apigenin of OATP1A2, and vitexin of OATP2B1. Commercially available P. incarnata preparations also inhibited transporter-mediated uptake.
Constituents of Passiflora incarnata, but not Valeriana officinalis, interact with OATP2B1 and OATP1A2 transporters, potentially altering uptake of other compounds.
Apigenin, orientin, and vitexin from Passiflora incarnata inhibited and were transported by OATP2B1 and OATP1A2, while valerenic acid from Valeriana officinalis only interacted with OATP2B1. Commercially available P. incarnata preparations inhibited transporter-mediated estrone 3-sulfate uptake, suggesting these constituents may affect pharmacokinetics of other drugs.
Valerian root extract (1000 mg/kg) produces a mild short-term sedative effect in mice, reducing locomotor activity between 66-78 minutes after administration.
A 70% ethanolic valerian root extract at 1000 mg/kg induced a mild, short-term reduction in locomotor activity in male mice between 66-78 minutes post-oral administration, but paradoxically increased activity after 150 minutes. The flavonoids linarin (12 mg/kg) and apigenin (1.5 mg/kg) also showed mild short-term sedative effects, while valerenic acid (1 mg/kg) caused intermittent stimulation. Overall, cumulative activity over 180 minutes indicated no considerable sedative effect, suggesting the extract and flavonoids may reduce sleep latency rather than maintain sleep.