Ayahuasca: a toxicological approach of the ritualistic use

The Ayahuasca tea has been used for more than a thousand years by the Indians of South America, as a spiritual and ritualistic instrument, for religious purposes. Non-Indians sects have arose in the last century, and started to use the tea. This utilization is increasing since the legalization of the Ayahuasca for religious use in Brazil. The effect of the tea is caused by the presence of alkaloids in the plants used in its preparation: the Banisteriopsis caapi liana, and the leaves of Psycotria viridis shrub. The effects observed are: hallucination, hypertension, tachycardia, nausea, vomiting and diarrhea. These actions may cause more serious damage to the organism, and therefore deserve more attention from the health professionals, because even for strickly religious use the tea may cause higher biological damage and therefore, the users should be made aware of the possible toxic effects of these substances.O chá da Ayahuasca vem sendo utilizado milenarmente por índios da América do Sul,como instrumento espiritual e ritual, com extrema religiosidade. No século passado surgiram seitas não-indígenas, que passaram a fazer uso do chá. Essa utilização vem aumentando desde a liberação do uso da Ayahuasca para fins religiosos no Brasil. A ação do chá deve-se à presença de alcalóides nas plantas utilizadas na sua preparação: o cipó Banisteriopsis caapi e as folhas do arbusto Psycotria viridis. Os efeitos observados são: alucinações, hipertensão, taquicardia, náuseas, vômitos e diarréia. Estas ações podem causar efeitos mais sérios ao organismo e, portanto, merecem maior atenção dos profissionais da saúde, no sentido de que se promovam estudos que possam permitir a utilização religiosa do chá sem maiores danos biológicos e para a conscientização dos usuários sobre os possíveis efeitos tóxicos destas substâncias.31031

Ayahuasca: uma abordagem toxicológica do uso ritualístico

The Ayahuasca tea has been used for more than a thousand years by the Indians of South America, as a spiritual and ritualistic instrument, for religious purposes. Non-Indians sects have arose in the last century, and started to use the tea. This utilization is increasing since the legalization of the Ayahuasca for religious use in Brazil. The effect of the tea is caused by the presence of alkaloids in the plants used in its preparation: the Banisteriopsis caapi liana, and the leaves of Psycotria viridis shrub. The effects observed are: hallucination, hypertension, tachycardia, nausea, vomiting and diarrhea. These actions may cause more serious damage to the organism, and therefore deserve more attention from the health professionals, because even for strickly religious use the tea may cause higher biological damage and therefore, the users should be made aware of the possible toxic effects of these substances.O chá da Ayahuasca vem sendo utilizado milenarmente por índios da América do Sul,como instrumento espiritual e ritual, com extrema religiosidade. No século passado surgiram seitas não-indígenas, que passaram a fazer uso do chá. Essa utilização vem aumentando desde a liberação do uso da Ayahuasca para fins religiosos no Brasil. A ação do chá deve-se à presença de alcalóides nas plantas utilizadas na sua preparação: o cipó Banisteriopsis caapi e as folhas do arbusto Psycotria viridis. Os efeitos observados são: alucinações, hipertensão, taquicardia, náuseas, vômitos e diarréia. Estas ações podem causar efeitos mais sérios ao organismo e, portanto, merecem maior atenção dos profissionais da saúde, no sentido de que se promovam estudos que possam permitir a utilização religiosa do chá sem maiores danos biológicos e para a conscientização dos usuários sobre os possíveis efeitos tóxicos destas substâncias

Pharmacological screening of ayahuasca in tumor cells culture, nociception and anxiety (Banisteriopsis caapi and Psychotria viridis)

Orientador: João Ernesto de CarvalhoDissertação (mestrado) - Universidade Estadual de Campinas, Faculdade de Ciências MédicasResumo: Este trabalho teve como objetivo realizar uma triagem inicial da ayahuasca em cultura de células e em modelos de nocicepção e ansiedade. A ayahuasca é uma decocção de duas plantas (Banisteriopsis caapi e Psychotria viridis) com ação alucinógena, utilizada por diversas religiões no Brasil. As principais substâncias relacionadas com as atividades no sistema nervoso central são a DMT(dimetiltriptamina), agonista serotoninérgico dos receptores 5HT1A, 2A/2C e as ?-carbolinas, inibidoras da monoaminoxidase-A (MAO), encontradas na P. viridis e B. caapi, respectivamente. Nos últimos anos, a ayahuasca se espalhou pela Europa e Estados Unidos, chamando a atenção dos pesquisadores quanto aos seus efeitos. Desta forma, o presente trabalho revelou que a ayahuasca possui atividade sobre a nocicepção em modelos de contorção abdominal e placa quente, atividade ansiolítica em ratos submetidos aos testes de labirinto em cruz elevado (LCE) e efeito citostático leve em cultura de células tumorais humanas de mama (MCF-7), rim (786-0), pulmão (NCI-H460), próstata (PC-3), ovário (OVCAR-3), cólon (HT-29), mama resitente a múltiplas drogas (NCI-ADR)Abstract: This study aimed to perform an initial screening of ayahuasca in cultured cells and in models of nociception and anxiety. Ayahuasca is a decoction of two plants (Banisteriopsis caapi and Psyvhotria viridis) with hallucinogenic action, used by various religions in Brazil. The main activities related substances in the central nervous system are DMT ( dimethyltryptamine ) , serotonin 5HT1A receptor agonist, 2A/2C and ? - carbolines , inhibiting monoamine oxidase -A ( MAO ) , found in P. viridis and B. caapi , respectively. In recent years, ayahuasca has spread to Europe and the United States, calling the attention of researchers for their effects. Thus , the present study showed that ayahuasca has activity on nociception in models writhing and hot plate , anxiolytic activity in rats submitted to the elevated maze tests (EPM ) and light cytostatic effect on cultured human tumor cells breast ( MCF -7) , kidney ( 786-0 ) , lung ( NCI- H460 ) , prostate (PC -3), ovarian ( OVCAR -3) , colon ( HT -29) , breast , multidrug resistente ( NCI- ADR )MestradoEnsino em SaúdeMestra em Clínica Médic

New 3-tetrazolyl-beta-carbolines and beta-carboline-3-carboxylates with anti-cancer activity

The synthesis and in vitro anticancer activity of novel beta-carbolines is reported. New tryptamines have been prepared via hetero-Diels-Alder reaction of nitrosoalkenes with indoles and used to prepare functionalized beta-carbolines by the Pictet-Spengler approach. These included 6-substituted-beta-carboline-3-carboxylates and 3-(1H-tetrazol-5-yl)-beta-carbolines, whose synthesis is reported for the first time. Carboline-3-carboxylates derived from L-tryptophan methyl ester were also prepared. The structural diversity that was achieved allowed the discovery of impressive activities against a range cancer cell lines with the selectivity depending on the type of substitution pattern of the beta-carboline core. We have identified at least one beta-carboline derivative with GI(50) < 1 mu M for each of the following human tumor cell lines: glioblastoma (U251), melanona (UACC-61), breast (MCF-7), ovarian expressing multiple-drug-resistance phenotype 4 (NCI-ADR/RES), renal (786-0), lung (NCI-H460), ovarian cancer (OVCAR-3), leukemia (K-562) and colon (HT29). These results demonstrated that the new 3-carboline derivatives are very promising anticancer agents179123132CNPQ - Conselho Nacional de Desenvolvimento Científico e Tecnológico201583/2014-

Evaluation of in vitro solar protection factor (SPF), antioxidant activity, and cell viability of mixed vegetable extracts from Dirmophandra mollis benth, Ginkgo biloba L., Ruta graveolens L., and Vitis viní­fera L.

The aim of this study was to validate a HPLC method for the assay of flavonoids in extracts obtained from natural sources, i.e., from Dirmophandra mollis Benth, Ginkgo biloba L., Ruta graveolens L., and Vitis vinífera L. The potential sun protecting effect, antioxidant activity, and cell viability of the extracts were also determined. Individual extracts (obtained from each individual species) and a mixed extract (containing the four extracts) were analyzed by the validated HPLC method for the identification of flavonoids and quantification of rutin and quercetin. An in vitro cell viability study was carried out using the neutral red method. The in vitro sun protection factor was determined by spectral transmittance and in vitro antioxidant efficacy was evaluated against DPPH, ABTS, and AAPH radicals. The HPLC method used for the identification and quantification of flavonoids in extracts exhibited linearity, precision, accuracy, and robustness. Detection and quantification limits were, respectively, 2.881 ± 0.9 g·mL1 and 0.864 ± 0.9 g·mL1 for quercetin, and 30.09 ± 1 g·mL1 and 9.027 ± 1.1 g·mL1 for rutin. All extracts did not affect cell viability at the evaluated concentration range and exhibited a sun protection effect and antioxidant activity. Among the evaluated extracts, Ginkgo biloba L. and the mixed extract depicted the most expressive antioxidant activity. The mixed extract exhibited sunscreen protection against ultraviolet A (UVA) and ultraviolet B (UVB) and a critical wavelength of 372.7 ± 0.1. Our results translate the enhanced flavonoids composition of the mixed extract, which may be a potential alternative over sunscreens and antioxidants in pharmaceutic/cosmetic formulations.This research was funded by FAPESP (grant numbers 2015/25533-7 and 2017/14757-7), CAPES and CNPq. The authors also received support from the Portuguese Science and Technology Foundation (FCT/MCT) and from European Funds (PRODER/COMPETE) under the project reference M-ERA-NET/0004/2015-PAIRED, co-financed by FEDER, under the Partnership Agreement PT2020, and PhD scholarship (SFRH/BD/130555/2017).info:eu-repo/semantics/publishedVersio

Silver Nimesulide Complex in Bacterial Cellulose Membranes as an Innovative Therapeutic Method for Topical Treatment of Skin Squamous Cell Carcinoma

Oxidative stress and inflammation act on skin squamous cell carcinoma (SSCC) development and progression. Curative therapy for SSCC patients is mainly based on surgical resection, which can cause various sequelae. Silver ions have in vitro activities over tumor cells, while nimesulide has antioxidant and anti-inflammatory activities. This study aimed to evaluate the effects of a silver(I) complex with nimesulide (AgNMS) incorporated in a sustained release device based on bacterial cellulose membrane, named AgNMS@BCM, on topic SSCC treatment. The antiproliferative effect of AgNMS complex was evaluated in the SCC4, SCC15 and FaDu SCC lines. AgNMS complex activity on exposure of phosphatidylserine (PS) residues and multicaspase activation were evaluated on FaDu cells by flow cytometry. The AgNMS@BCM effects were evaluated in a SSCC model induced by 7,12-dimethylbenzanthracene/12-o-tetradecanoyl-phorbol-13-acetate (DMBA/TPA) in mice. Toxicity and tumor size were evaluated throughout the study. AgNMS complex showed antiproliferative activity in SCC15 and FaDu lines in low to moderate concentrations (67.3 &micro;M and 107.3 &micro;M, respectively), and induced multicaspase activation on FaDu cells. The AgNMS@BCM did not induce toxicity and reduced tumor size up to 100%. Thus, the application of AgNMS@BCM was effective and safe in SSCC treatment in mice, and can be seen as a potential and safe agent for topic treatment of SSCC in humans