RESUMO
Although several studies have been conducted to elucidate the relationship between psychedelic consumption and cognition, few have focused on understanding the long-term use influence of these substances on these variables, especially in ritualistic contexts. To verify the influence of ritualistic ayahuasca consumption on the cognition of experienced ayahuasca religious users (> 20 years) and beginners (< 3 years), which participated in rituals of the Centro Luz Divina (CLD), a Santo Daime church in Brazil. Observational, descriptive, and cross-sectional study was carried out in which 48 people participated divided into three groups: (a) experienced ayahuasca users (n = 16), (b) beginner ayahuasca users (n = 16) and (c) control group (n = 16). All groups were matched by sex, age, and education and contained 8 women and 8 men. Cognition was assessed with the WASI (intelligence quotient), Digit Span (verbal working memory), Corsi Block-Tapping Task (visuospatial-related and working memory), Rey-Osterrieth Complex Figure test (visual perception, immediate memory), and Wisconsin Card Sorting and Five Digit Test (executive functions). Groups were homogenous in terms of sociodemographic characteristics, with participants presenting average intellectual performance. There was no evidence of cognitive decline amongst ayahuasca users. The experienced group showed higher scores compared to the less experienced group in the Digit Span and Corsi Block-Tapping tasks, which assess working verbal and visuospatial memories respectively. We confirmed the botanical identities of Psychotria viridis and Banisteriopsis caapi and the presence of the alkaloids both in the plants and in the brew. Short and long-term ayahuasca consumption does not seem to alter human cognition, while long-term use seems to be associated with improvements in aspects of working memory when compared with short-term use.
RESUMO
Ayahuasca is a psychoactive and psychedelic decoct composed mainly of Banisteriopsis caapi and Psychotria viridis plant species. The beverage is rich in alkaloids and it is ritualistically used by several indigenous communities of South America as a natural medicine. There are also reports in the literature indicating the prophylaxis potential of Ayahuasca alkaloids against internal parasites. In the present study, Ayahuasca exhibited moderate inâ vitro activity against Trypanosoma cruzi trypomastigotes (IC50 95.78â µg/mL) compared to the reference drug benznidazole (IC50 2.03â µg/mL). The ß-carboline alkaloid harmine (HRE), isolated from B.â caapi, was considered active against the trypomastigotes forms (IC50 6.37), and the tryptamine N, N-dimethyltryptamine (DMT), isolated from P.â viridis was also moderately active with IC50 of 21.02â µg/mL. Regarding the inâ vivo evaluations, no collateral effects were observed. The HRE alone demonstrated the highest trypanocidal activity in a dose-responsive manner (10 and 100â mg/kg). The Ayahuasca and the association between HRE and DMT worsened the parasitaemia, suggesting a modulation of the immunological response during the T.â cruzi infection, especially by increasing total Immunoglobulin (IgG) and IgG1 antibody levels. The inâ silico molecular docking revealed HRE binding with low energy at two sites of the Trypanothione reductase enzyme (TR), which are absent in humans, and thus considered a promissory target for drug discovery. In conclusion, Ayahuasca compounds seem to not be toxic at the concentrations of the inâ vivo evaluations and can promote trypanocidal effect in multi targets, including control of parasitaemia, immunological modulation and TR enzymatic inhibition, which might benefit the treatments of patients with Chagas' disease. Moreover, the present study also provides scientific information to support the prophylactic potential of Ayahuasca against internal parasites.
Assuntos
Alcaloides , Banisteriopsis , Doença de Chagas , Alucinógenos , Humanos , Banisteriopsis/química , Alucinógenos/farmacologia , Harmina/farmacologia , Simulação de Acoplamento Molecular , N,N-Dimetiltriptamina/farmacologia , Carbolinas , Triptaminas , Doença de Chagas/tratamento farmacológico , Imunoglobulina G , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêuticoRESUMO
Banisteriopsis caapi is used to prepare the psychoactive beverage ayahuasca, and both have therapeutic potential for the treatment of many central nervous system (CNS) conditions. This study aimed to isolate new bioactive compounds from B. caapi extract and evaluate their biological activity, and that of the known ß-carboline components of the plant (harmine, harmaline, and tetrahydroharmine), in BV-2 microglial cells, the in vivo activation of which is implicated in the physiopathology of CNS disorders. B. caapi extract was fractionated using semipreparative liquid chromatography (HPLC-DAD) and the exact masses ([M + H]+m/z) of the compounds in the 5 isolated fractions were determined by high-resolution LC-MS/MS: F1 (174.0918 and 233.1289), F2 (353.1722), F3 (304.3001), F4 (188.1081), and F5 (205.0785). Harmine (75.5-302 µM) significantly decreased cell viability after 2 h of treatment and increased the number of necrotic cells and production of reactive oxygen species at equal or lower concentrations after 24 h. F4 did not impact viability but was also cytotoxic after 24 h. Most treatments reduced proinflammatory cytokine production (IL-2, IL-6, IL-17, and/or TNF), especially harmaline and F5 at 2.5 µM and higher concentrations, tetrahydroharmine (9.3 µM and higher), and F5 (10.7 µM and higher). The results suggest that the compounds found in B. caapi extract have anti-inflammatory potential that could be explored for the development of treatments for neurodegenerative diseases.
Assuntos
Banisteriopsis , Banisteriopsis/química , Cromatografia Líquida , Harmalina , Harmina/farmacologia , Microglia , Extratos Vegetais/farmacologia , Plantas , Espectrometria de Massas em TandemRESUMO
Takiwasi is a therapeutic community for the treatment of Substance Use Disorders (SUDs) that combines traditional Amazonian medicine (TAM) with modern psychotherapy. One of the plant medicines from TAM used in this protocol is purgahuasca. It is a decoction of the vine Banisteriopsis caapi alone, whose use is traditional among the Awajún and other ethnic groups in Peru. The research began with a field trip to Awajún territory to explore the indigenous use of purgahuasca as an initiation rite. Then, analysis of its application was conducted in the clinical context of Takiwasi. Open-ended and semi-structured interviews with Awajún informants and Takiwasi's therapeutic staff were performed and analyzed following the narrative methodological approach. Further clinical data on the ingestion of purgahuasca by Takiwasi's SUD patients were obtained from the internal repository. These indicate that 359 (92.1%) patients reported having had the so-called mareación (dizziness), 299 (76.7%) experienced physical sensations, and 208 (53.3%) had visions. These effects can be related to the psychoactivity of ß-Carbolines alkaloids from B. caapi, a medicinal plant that seems to have potential benefits also for SUD, especially giving a key contribution to the patients' therapeutic process of becoming aware of the personal reasons behind addictive behaviors.
Assuntos
Alcaloides , Banisteriopsis , Plantas Medicinais , Transtornos Relacionados ao Uso de Substâncias , Humanos , Medicina Tradicional , Extratos Vegetais , Transtornos Relacionados ao Uso de Substâncias/terapiaRESUMO
Ayahuasca is a psychoactive infusion with a large pharmacological application normally prepared with Banisteriopsis caapi, which contains the monoamine oxidase inhibitors ß-carbolines, and Psichotria virids, which contains the serotonin receptor agonist N,N dimethyltryptamine (DMT). The objectives of this study were to investigate the chemical profile of B. caapi and of ayahuasca collected in various Brazilian regions. In total, 176 plant lianas, of which 159 B. caapi and 33 ayahuasca samples were analyzed. Dried liana samples were powdered, extracted with methanol, diluted, and analyzed by LC-MS/MS. Ayahuasca samples were diluted and analyzed. Mean concentrations in B. caapi were 4.79 mg/g harmine, 0.451 mg/g harmaline, and 2.18 mg/g tetrahydroharmine (THH), with a high variability among the samples (RSD from 78.9 to 170%). Native B. caapi samples showed significantly higher harmine concentrations than cultivated ones, and samples from the Federal District/Goiás had higher THH content than those collected in the State of Acre. The other Malpighiaceae samples did not contain ß-carbolines, except for one D. pubipetala sample. Concentrations in ayahuasca samples ranged from 0.109 to 7.11 mg/mL harmine, 0.012 to 0.945 mg/mL harmaline, 0.09 to 3.05 mg/mL THH, and 0.10 to 3.12 mg/mL DMT. The analysis of paired ayahuasca/B. caapi confirmed that harmine is reduced to harmaline and to THH during the brew preparation. This is the largest study conducted with Malpighiaceae samples and showed a large variability in the main ß-carbolines present in B. caapi. This biodiversity is a challenge for standardization of the material used in ethnopharmacological studies of B. caapi and ayahuasca.
RESUMO
Ayahuasca (caapi, yajé), is a psychoactive brew from the Amazon Basin region of South America traditionally considered a "master plant." It is prepared as a decoction from Banisteriopsis caapi and Psychotria viridis, which it is thought that it stimulates creative thinking and visual creativity. Native healers of the Orinoco and Amazon basins have used traditionally ayahuasca as a healing tool for multiple purposes, particularly to treat psychological disorders in the patients, with some beneficial effects experimentally and clinically validated. Recently, several syncretic religions, as the "União de Vegetal" (UDV) group in Brazil, have been spread around the world. The use of ayahuasca has been popularized by internet and smart-shops, bringing the psychoactive substance to new highs, emerging new "ayahuasqueros." Ayahuasca has alkaloids as ß-carbolines and dimethyltryptamines, which inhibit the monoamine oxidase and active the 5-HT2A (5-hydroxytryptamine) receptor, respectively, resulting in hallucinations in the users. Ayahuasca induces a psychedelic change in the anteroposterior coupling of the electrophysiological brain oscillations in humans. Traditional ayahuasca beverage is generating pharmacological, commercial and spiritual interest among the scientific community, government people, and different populations worldwide. The goal of this article is to report about the uses, chemistry and biological activities of ayahuasca.
RESUMO
Ayahuasca is a beverage used in religious rituals of indigenous and nonindigenous groups, and its therapeutic potential has been investigated. Ayahuasca is obtained by decoction of the Banisteriopsis caapi that contains ß-carbolines (harmine, harmaline, and tetrahydroharmine) plus Psychotria viridis that contains N,N-dimethyltryptamine. Although plants used in folk medicine are recognized as safe, many of them have genotoxic potential. The Salmonella/microsome assay is usually the first line of the mutagenicity evaluation of products intended for therapeutic use. Our objective was to evaluate the mutagenicity of ayahuasca beverage and their constituents using the Salmonella/microsome assay with TA98 and TA100. We analyzed two ayahuasca samples, and also beverage samples prepared each individual plant P. viridis and B. caapi. Harmine and harmaline were also tested. All beverage samples were chemically characterized and both ayahuasca samples could be considered representative of the beverages consumed in religious rituals. Both ayahuasca samples were mutagenic for TA98 and TA100 with and without S9, with similar potencies. The beverage obtained from P. viridis was not mutagenic, and beverage obtained from B. caapi was mutagenic for TA98 with and without S9. Harmine was nonmutagenic and harmaline was mutagenic only for TA98 without S9. Harmaline fully explain the mutagenicity observed with TA98 without S9 of both ayahuasca samples and the B. caapi beverage samples. We conclude that the ayahuasca samples are mutagenic and this effect is partially explained by harmaline, one of the ß-carbolines present in the beverage. Other mutagenic compounds seem to be present and need to be further investigated. Environ. Mol. Mutagen. 60:269-276, 2019. © 2018 Wiley Periodicals, Inc.
Assuntos
Banisteriopsis/química , Harmina/análogos & derivados , Mutagênicos/farmacologia , N,N-Dimetiltriptamina/farmacologia , Preparações de Plantas/farmacologia , Psychotria/química , Bebidas , Harmina/farmacologia , Medicina Tradicional , Microssomos/efeitos dos fármacos , Monoaminoxidase/metabolismo , Testes de Mutagenicidade , Salmonella/efeitos dos fármacosRESUMO
Rats were treated orally with ayahuasca (AYA) on gestation days (GD) 6-20 at doses corresponding to one-(1X) to eight-fold (8X) the average dose taken by a human adult in a religious ritual, and the pregnancy outcome evaluated on GD21. Rats treated with 4X and 8X doses died during the treatment period (44 and 52%), and those that survived showed kidney injury. Rats surviving the 8X dose showed neuronal loss in hippocampal regions and in the raphe nuclei, and those from the 2X dose neuronal loss in CA1. Delayed intrauterine growth, induced embryo deaths and increased occurrence of foetal anomalies were observed at the 8X dose. At non-lethal doses, AYA enhanced embryolethality and the incidence of foetal soft-tissue and skeleton anomalies. This study suggested that AYA is developmentally toxic and that its daily use by pregnant women may pose risks for the conceptus.
Assuntos
Banisteriopsis , Bebidas/toxicidade , Alucinógenos/toxicidade , Preparações de Plantas/toxicidade , Teratogênicos/toxicidade , Anormalidades Induzidas por Medicamentos , Anormalidades Múltiplas/induzido quimicamente , Animais , Encéfalo/anormalidades , Encéfalo/efeitos dos fármacos , Encéfalo/patologia , Embrião de Mamíferos/efeitos dos fármacos , Feminino , Retardo do Crescimento Fetal , Rim/anormalidades , Rim/efeitos dos fármacos , Fígado/anormalidades , Fígado/efeitos dos fármacos , Masculino , Troca Materno-Fetal , Neurônios/efeitos dos fármacos , Gravidez , Ratos Wistar , Esqueleto/anormalidades , Esqueleto/efeitos dos fármacos , Testículo/anormalidades , Testículo/efeitos dos fármacos , Ureter/anormalidades , Ureter/efeitos dos fármacos , Útero/anormalidades , Útero/efeitos dos fármacosRESUMO
Objetivo: Evaluar el efecto de la ingestión de Banisteriopsis caapi y Psychotria viridis 'Binomio ayahuasca' en el hipocampo de cerebro de ratas. Diseño: Estudio experimental, descriptivo, analítico, transversal. Institución: Instituto de Investigación en Ciencias Farmacéuticas y Recursos Naturales, Facultad de Farmacia y Bioquímica, Universidad Nacional Mayor de San Marcos, Lima, Perú. Material biológico: Ratas. Intervenciones: Administración del binomio ayahuasca por vía orogástrica a ratas albinas adultas de la especie Rattus novergicus y de cepa Holtzman. A siete grupos de cinco con un peso promedio de 240 ± 30 g se les administró (GI) blanco, (GII) 2,5 mL diazepam, (GIII) 0,7 mL solución de Banisteriopsis caapi, (GIV) 0,7 mL Psychotria viridis, y a los grupos (GV), (GVI) y (GVII) se administró 0,7 mL, 3,5 mL y 7,0 mL de solución del binomio ayahuasca, respectivamente. Principales medidas de resultados: Macroscópicos: comportamiento de reflejos y actividad motora. Microscópicos: número de células piramidales y granulosas, y desorganización celular. Resultados: En el tamizaje fitoquímico del extracto se caracterizó presencia de alcaloides, antraquinonas, triterpenoides y esteroides, fenoles, flavonoides y saponinas. Los volúmenes de droga administradas a los grupos de intervención con el binomio en la dosis de 0,7 mL manifestaron significativo aumento en el número de células granulosas sobre las células piramidales; a dosis de 3,5 mL el número de células granulosas fue menor con presencia de células piramidales grandes y pequeñas; y a dosis de 7,0 mL se manifestó desorganización celular, presencia de células piramidales grandes y pequeñas, y aumento de células granulosas. Conclusiones: El extracto alcohólico del binomio ayahuasca presenta efecto neuropatológico en el hipocampo del cerebro de ratas. (AU)