Abstract

The pharmacological activities and acute toxicity of the psilocin (PC) and dried residues of the crude extracts of psychotropic mushrooms were investigated in mice. The hallucinogenic substances were effectively isolated, by using methanol, from the species of Psilocybe semilanceata and Pholiotina cyanopus, that were collected in the north-east region of Poland. The chemical analysis of these extracts, which was performed by liquid chromatography with mass spectrometry detection (LC-MS), indicated the presence of psilocin and other hallucinogenic substances, including indolealkylamines and their phosphorylated analogues. When the pure psilocin or fungal extracts were used, slight differences in determined LD50 values were observed. However, the application of PC evoked the highest level of toxicity (293.07 mg/kg) compared to the activity of extracts from Ph. cyanopus and P. semilanceata, where the level of LD50 was 316.87 mg/kg and 324.37 mg/kg, respectively. Furthermore, the behavioral test, which considered the head-twitching response (HTR), was used to assess the effects of the studied psychotropic factors on the serotonergic system. Both, the fungal extracts and psilocin evoked characteristic serotoninergic effects depending on the dose administered to mice, acting as an agonist/partial agonist on the serotonergic system. A dose of 200 mg/kg 5-hydroxytryptophan (5-HTP) induced spontaneous head-twitching in mice (100% effect), as a result of the formation of 5-hydroxytryptamine (5-HT) in the brain. Compared to the activity of 5-HTP, the intraperitoneal administration of 1mg/kg of psilocin or hallucinogenic extracts of studied mushrooms (Ph. cyanopus and P. semilanceata) reduced the number of head-twitch responses of about 46% and 30%, respectively. In contrast, the administration of PC exhibited a reduction of about 60% in HTR numbers.

Highlights

  • IntroductionThe research carried out on the determination of chemical content of psychedelic mushroom species such as Galerina, Gymnopilus, Inocybe, Panaeolus, Pholiotina and Psilocybe showed that they mainly contained psilocybin and its dephosphorylated metabolite—psilocin—as well as the minor amounts of other indoleamine derivatives such as baeocystin, norbaeocystin and aeruginascin, may have occurred [1,2,3,4,5,6,7,8,9,10,11,12]

  • One of the sources of psychotropic substances is hallucinogenic mushrooms

  • The LD50 values were calculated by means of the Kerber’s method [31], whereas the substance acute toxicity was evaluated by the Litchfield and Wilcoxon method

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Summary

Introduction

The research carried out on the determination of chemical content of psychedelic mushroom species such as Galerina, Gymnopilus, Inocybe, Panaeolus, Pholiotina and Psilocybe showed that they mainly contained psilocybin and its dephosphorylated metabolite—psilocin—as well as the minor amounts of other indoleamine derivatives such as baeocystin, norbaeocystin and aeruginascin, may have occurred [1,2,3,4,5,6,7,8,9,10,11,12]. Hallucinogens cause extensive changes in the process of perception, thinking and mood of a human being, as well as depersonalisation [13]. These substances mainly belong to two chemical classes: indoleamines and phenylalkylamines. Studies, described in the literature, have demonstrated that these substances behave as non-specific serotonin receptor (5-HT) agonists (partial agonists), that bind with 5-HT1A, 5-HT2A and

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