Abstract. Flos albiziae (FA) is reportedly used for treatment of insomnia and anxiety in traditional medicine. The hypnotic effect of an extract of FA (FAE) and its constituent quercetin [2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one, QR] was examined in mice. QR is a widely distributed natural flavonoid abundant in FA flowers and other tissues. The possible mechanisms underlying the hypnotic effects of FAE and QR were investigated using behavioral pharmacology. FAE and QR significantly potentiated pentobarbital-induced [50 mg/kg, intraperitoneal (ip)] sleep (prolonged sleeping time; shortened sleep latency) in a dose-dependent manner, and these effects were augmented by administration of 5-hydroxytryptophan (5-HTP), a precursor of 5-hydroxytryptamine. With a sub-hypnotic dose of pentobarbital (28 mg/kg, ip), FAE and QR significantly increased the rate of sleep onset and were synergistic with 5-HTP (2.5 mg/kg, ip). Pretreatment with p-chlorophenylalanine, an inhibitor of tryptophan hydroxylase, significantly decreased sleeping time and prolonged sleep latency in pentobarbital-treated mice, whereas FAE and QR significantly reversed this effect. Data show that FAE and QR have hypnotic activity, possibly mediated by the serotonergic system. The present study offers a rationale for the use of FA in treating sleep disorders associated with serotonin system dysfunction.
IntroductionBenzodiazepines are extensively used to treat insomnia; however, their uses are limited by concerns regarding long-term efficacy and the potential for abuse, dependence and adverse effects.Thus, complementary and alternative medicine is often a source for treating insomnia. Chinese herbal medicine (CHM), a form of complementary and alternative medicine, is often explored for treating insomnia, either with single herbs or with herbal formulas. Recently, >200 studies of CHM for insomnia from a systematic review indicated that CHM was similar to Western medication for treating insomnia, and that the frequency of adverse events associated with CHM were similar to that of the placebo; however, they were less frequent than that of Western medication (1). Therefore, identifying a single herb or herbal formula from CHM to treat insomnia is advantageous.Albizia julibrissin Durazz is a small tree with smooth, gray-brown bark and doubly pinnate leaves. Clusters of pink flower heads are borne in summer (2) and the tree is widely distributed throughout Korea, China, Japan and Africa. The main active ingredients of the flowers include triterpenoids and their glycosides, flavonoids, alkaloids, organic acids, sterols, lignans and tannin. Quercetin [2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one, QR] is a major constituent of the flowers of Flos albiziae (FA) and QR is identified in vegetables, fruits, red wine and other herbal preparations. Pharmacological research on aqueous extracts of FA (FAE) and QR indicate that they have broad bioactivity, such as antithrombotic and anti-inflammatory effects, anti-infectious and immunomodulator...