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Preliminary chemical profile and in vitro pharmacological evaluation of the hallucinogenic plant Diplopterys cabrerana

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For the last few years, Ayahuasca ceremonies have been gaining popularity in recreational settings in Europe and North America [1]. Similar to Psychotria viridis, Diplopterys cabreranais also suggested to contain the psychoactive compound N,N-dimethyltryptamine, and is therefore used in Aya-huasca rituals for its ability to induce hallucinations, euphoria and entheogenic effects [1-3]. However, while information on the toxic profile of D. cabreranaremains very limited, its acquisition is easily ac-complished by consumers. We aimed to characterize the aqueous extracts of D. cabreranaleaves, mimicking those typically consumed, to identify bioactives that underlie the psychoactive or toxic effects, and evaluate their impact on neuronal function, neurotransmission and radical stress. Chemical characterization was attained by HPLC-DAD. Impact upon neuronal viability was assessed by the MTT assay (up to 1000 μg/mL) in SH-SY5Y neuroblastoma cells. Impact on neuromodulation and neuroinflammation was evaluated through acetylcholinesterase and 5-lipoxygenase inhibition, while an-tiradical properties were assessed by evaluating nitric oxide (•NO) and xanthine oxidase (XO) activity. Inhibition of the α-glucosidase enzyme was also evaluated. Statistical comparisons among groups per-formed by one-way ANOVA followed by Dunnett post hoc test. Preliminary characterization results revealed the presence of several catechin derivates, alongside two apigenin derivates and one tryp-tamine derivate. Cytotoxicity was not verified up to the highest concentration tested. Acetylcholinesterase inhibition was recorded starting at 250 μg/mL, and a concentration-dependent inhibition of 5-lipoxygen-ase was found (IC50=79.77 μg/mL). Concentration-dependent scavenging effects upon •NO and XO inhi-bition were verified at concentrations higher than 1.953 μg/mL and 31.25 μg/mL, respectively. At last, inhibition of α-glucosidase occurred with concentration-dependency and an IC50of 4.78 μg/mL. Conclu-sions:Although antiradical, anti-inflammatory and antidiabetic properties were verified, with no in vitrocytotoxicity being detected, further research is needed to elucidate the underlying mechanisms that might be involved in our preliminary results.

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New psychoactive substances Ayahuasca Hallucinogenic plants Recreational setting Neuro-toxicity

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Garcia, M. R., Dutka, M., Guimarães, S., Andrade, P. B., Seabra, V., & Dias-da-Silva, D. (2024). Preliminary chemical profile and in vitro pharmacological evaluation of the hallucinogenic plant Diplopterys cabrerana. Scientific Letters, 1(Sup 1). https://doi.org/10.48797/sl.2024.221

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