Alternative Extraction Methods of Essential Oil From the Flowers of Citrus aurantium L. Var Daidai Tanaka: Evaluation of Oil Quality and Sedative-Hypnotic Activity

The aim of this study was to analyze the content of hypnotic components in the essential oil from Citrus aurantium flowers (EDD), extracted by different methods, and to characterize its sedative-hypnotic effects. The sedative-hypnotic capacity of EDD was evaluated using pentobarbital-induced sleeping assays, locomotor activity tests and GABAA receptor antagonists. The results showed that EDD extracted by steam and water distillation (SWD), hydrodistillation (HD), and ultrasound-assisted hydrodistillation (UHD) had as their main components linalool, linalyl acetate, and limonene, comprising more than 55% of the total peak area. Compared with EDD extracted by HD and UHD, the total content of linalool and linalyl acetate in EDD obtained by SWD was highest, whereas the content of limonene in EDD extracted by the 3 different methods was not different. Oral and intraperitoneal administration of EDD resulted in reduced sleep latency and increased sleep duration of mice, as well as reduced locomotor activity, which was proven by decreases in the total distance travelled, average velocity, number of activities, and central distance. Interestingly, intraperitoneal injection of EDD had better sedative and hypnotic effects than oral ingestion. In vitro assays using SH-SY5Y cells showed that EDD dose-dependently increased Cl− influx, which could be blocked by the GABAA receptor antagonists, picrotoxin, bicuculline, and flumazenil, suggesting that EDD promoted sedative-hypnotic activity by potentiating GABAA receptor-mediated Cl− current responses. Altogether, these results suggest that the important hypnotic-sedative activity of EDD appears to be due to the effects of limonene, and particularly the high contents of linalool and linalyl acetate, which were effectively extracted by SWD.

ANTIOXIDANT, SEDATIVE AND HYPNOTIC POTENTIAL OF MILK EXTRACT OF MYRISTICA FRAGRANS: A COMPLIMENTARY MEDICINE FOR THE MANAGEMENT OF INSOMNIA

The Myristica fragrans (MF) is well known in Ayurveda for many therapeutic uses. The present research work was carried out to investigate the antioxidant (in vitro), sedative and hypnotic effects of the MFmilk extracts in Wistar rats. The extraction was carried out by hot percolation and cold maceration methods. The phytochemical, HPLC and pharmacological evaluations were done. The overall sedative and hypnotic effects of the different extracts were evaluated using the parameters locomotor activity, muscle strength and thiopental induced sleeping time. The milk extracts shown the presence of quercetin. It was confirmed using HPLC analysis, which might be responsible for its in-vitro antioxidant activity. The extract also showed the significant (P<0.05) sedative and hypnotic effect at 50 mg/kg, 100 mg/kg and 200 mg/kg on oral administration. Consequently, the treated groups have shown a significant increase in thiopental induced sleeping time. The study concluded that the milk extracts possess antioxidant, sedative and hypnotic activity. further research is needed to develop suitable formulation and to establish the mechanism of action of milk extract of MF.

Comprehensive phytochemical analysis and sedative-hypnotic activity of two Acanthopanax species leaves

Acanthopanax senticosus leaves (SCL) and Acanthopanax sessiliflorus leaves (SFL), which are usually made into functional teas, possess similar pharmacological activities.

Medicinal Potential and Scientific Validations of Mallotus philippinensis (Lam.) Muell. Arg. ( Kampillaka ): A Review

Mallotus philippinensis (Lam.) M Arg is one of the endangered plants in the central ecoregion. It belongs to the Euphorbiaceae family. Mallotus philippinensis (Lam.) Muell. Arg. (Family: Euphorbiaceae) is a medicinally important common perennial shrub used in indigenous medicine. It is distributed mainly in the tropical and subtropical regions of the world. Though it is a drug of herbal origin, it has been grouped into one of the eight Sadharana rasa groups [Glands and hairs of Mallotus philippinensis (Kampillaka), Arsenic (Somala), Ammonium Chloride (Navasagara), Cowri (Kaparda), Amber (Agnijaara), Red Oxide of Mercury (Girisindoora), Cinnabar (Hingula), Litharge (Muddaarashringa)] in Rasa - shastra (Ayurveda study of minerals and metals) of Ayurvedic pharmacopoeia. M. philippinensis is included in Virecana ghana (group of medicinal plants or products use to purgation therapy) of Ayurveda medicine. Especially roots, fruits (also as fruit powder) and the leaves are used for medicinal purposes. Leaves are bitter and have a cooling and appetizing nature. The glands/hairs of the fruit and the leaves are recommended for dermal problems. So far, scientific studies have been carried out to prove and look-into the pharmacological activities of M. philippinensis. Here, an attempt is taken to summarize the distribution, morphology, Ayurveda and traditional uses, and scientific investigations on M. philippinensis . Researchers have scientifically proven the Antimicrobial activity, Hepatoprotective activity, Anti-Leukemic activity, Anti-HIV activity, Anti-inflammatory activity, Anti-filarial activity, Analgesic and hypnotic activity, Antiproliferative activity, Antifertility activity, Purgative activity and Anthelmintic activity and Antiallergic activity against different parts of the M. philippinensis.

Hypnotic activity of Capparis spinosa hydro-alcoholic extract in mice

Background: Sleep disorders are among the most common psychiatric and medical conditions. Objective: The present study aimed at investigating the hypnotic activity of the hydro-alcoholic extract of Capparis spinosa (HAE) in mice. Method: Three doses of HAE (30, 60 and 120 mg/kg) and three fractions of it, namely n-hexane fraction (NHF), water fraction (WF), and ethyl acetate fraction (EAF), were given in comparison with diazepam (3mg/kg body weight i.p.) as positive control and saline as negative control. After 30 min, pentobarbital (30 mg/kg body weight i.p.) was administrated. In addition, LD50 of HAE was examined and the cytotoxicity of HAE was assessed in l929 cells using the MTT assay. Moreover, for motor-coordination ability 30 mins after administration of HAE rota-rod test was performed. Results: The results exhibited that the HAE and all the fractions significantly augmented pentobarbital induced sleeping time which was comparable to that of induced by diazepam. The LD50 value was 2.4 g/kg. The extract did not induce any cytotoxic effects in L929 fibroblast cells. HAE did not affect the animals’ performance on the rota-rod test. Conclusion: Our finding suggests that hydro-alcoholic extract of C. spinosa possesses hypnotic potential that may require further scientific investigations.

Preparation and characterization of vetiver oil encapsulated polymeric microcapsules for sedative and hypnotic activity

In the present work, in view of the medicinal properties of vetiver oil (extracted from the roots of Vetiveria zizanioides L.), we made an attempt to encapsulate vetiver oil in a biocompatible polymeric system made of sodium alginate with gellan gum or karaya gum. Sodium alginate and gellan gum or karaya gum were ionotropically cross-linked to encapsulate vetiver oil. Vetiver oil encapsulations in these microcapsules were 35.92 ± 3.18 % to 78.55 ± 3.35%. Vetiver oil encapsulated microcapsules were of spherically shaped with 656-769 µm mean diameter. This vetiver oil encapsulated microcapsules made of alginate-gellan gum blends were found capable of providing a long release of encapsulated oil, showing the potential for the sustained release application. These microcapsules were analyzed by FTIR, DSC, and SEM, etc. In addition, sedative and hypnotic activities of vetiver oil encapsulated polymeric microcapsules in the male Swiss albino mice were evaluated. The sedative-hypnotic activity of vetiver oil encapsulated polymeric microcapsules in rats was observing the number of crossing and motilities. The results proves that vetiver oil encapsulated polymeric microcapsules decreased motility when compared to the control group.

Progress on the Biological Activities of Helicid and its Derivatives

Helicid is a specific Chinese natural drug. Helicid, its congeners, and its derivatives exhibit pronounced biological activities, among which its hypnotic effects stand out. The well-documented sedation and analgesic activity and low side effects of helicid have drawn more and more attention from scientists. Moreover, its clinical success and intriguing mechanism of action have stimulated great interest in further modification of helicid for improving its hypnotic activity. The 4-formyl group has been a major target for structural derivatization aimed at either producing more potent compounds or overcoming drug disadvantages. Accordingly, numerous helicid derivatives have been prepared via molecular docking and hemisynthesis. Although neither systematic nor comprehensive, there are two excellent reviews on the distribution, sources, applications, synthesis, and pharmacological activity of helicid that have been published in Chinese. In the present review, we attempt to compile and discuss the key data available in the literature on the multiple biological activities of helicid derivatives. This compilation of 102 references may be helpful in understanding the diverse biological properties of helicid while providing insights into its mechanism of action. This may direct future research in the synthesis of new derivatives and the exploration of other biological activities.

Antidepressant and Sedative-hypnotic Activities of Methanolic Extract of Grewia asiatica Linn. Leaves in Mice

Grewia asiatica (Family-Malvaceae), known as Phalsa in Bangladesh, is also native to India, Nepal, Pakistan, Cambodia and Thailand. The plant has a long history of traditional uses. The present investigation was designed to evaluate acute toxicity test, antidepressant and sedative-hypnotic activities of the methanolic extract of the leaves of G. asiatica. In acute toxicity test, methanolic soluble fraction of the plant extract of G. asiatica showed no significant changes in the body weight between the control and treated group at the doses of 1000, 2000 and 3000 mg/kg body weight. The extract could not significantly reduce immobility time in comparison with control group and standard drug (Nortriptyline) treated group in forced swimming and tail suspension tests. Sedative-hypnotic activity was evident at the doses of 100 and 200 mg/kg body weight after observing in hole board test. Sedative-hypnotic activity of short duration of action was also evident in hole cross and open field test. Bangladesh Pharmaceutical Journal 22(2): 185-191, 2019