OPEN Foundation

Author name: OPEN Foundation

Screening of Hallucinogenic Compounds and Genomic Characterisation of 40 Anatolian Salvia Species

Abstract

Introduction
Salvia, an important and widely available member of Lamiaceae family. Although comparative analysis on secondary metabolites in several Salvia species from Turkey has been reported, their hallucinogenic chemicals have not been screened thoroughly.
Objective
This study provides LC–MS/MS analysis of 40 Salvia species for screening their psychoactive constituents of salvinorin A and salvinorin B. 5S–rRNA gene non-coding region of Salvia plants was sequenced, aligned and compared with that sequence of Salvia divinorum plant.
Methodology
Targeted molecules of salvinorin A and salvinorin B were quantified, using LC–MS/MS, from all aerial parts of 40 Salvia species, collected from different parts of Turkey. Regions of 5S–rRNA gene from different species were amplified by polymerase chain reaction and DNA sequences were aligned with Salvia divinorum DNA sequences.
Results
Very few of the Salvia species (S. recognita, S. cryptantha and S. glutinosa) contained relatively high levels of salvinorin A (212.86 ± 20.46 μg/g, 51.50 ± 4.95 μg/g and 38.92 ± 3.74 μg/g, respectively). Salvinorin B was also found in Salvia species of S. potentillifolia, S. adenocaulon and S. cryptantha as 2351.99 ± 232.22 μg/g, 768.78 ± 75.90 μg/g and 402.24 ± 39.71 μg/g, respectively. The sequences of 5S–rRNA gene of 40 different Salvia species were presented and it was found that none of the Salvia species in Turkey had similar DNA sequence to Salvia divinorum plant.
Conclusion
This is the first report of screening 40 Salvia species in Turkey according to their psychoactive constituents, salvinorin A and salvinorin B and their genomic structures. It is possible that some of these Salvia species may exhibit some psycho activity. Thus, they need to be screened further.
Hatipoglu, S. D., Yalcinkaya, B., Akgoz, M., Ozturk, T., Goren, A. C., & Topcu, G. (2017). Screening of Hallucinogenic Compounds and Genomic Characterisation of 40 Anatolian Salvia Species. Phytochemical Analysis. 10.1002/pca.2703
Link to full text

Screening of Hallucinogenic Compounds and Genomic Characterisation of 40 Anatolian Salvia Species Read More »

Mushroom-Derived Indole Alkaloids

Abstract

Mushrooms are known to produce over 140 natural products bearing an indole heterocycle. In this review, the isolation of these mushroom-derived indole alkaloids is discussed, along with their associated biological activities.
Homer, J. A., & Sperry, J. (2017). Mushroom-Derived Indole Alkaloids. Journal of Natural Products80(7), 2178-2187. 10.1021/acs.jnatprod.7b00390
Link to full text

Mushroom-Derived Indole Alkaloids Read More »

First time view on human metabolome changes after a single intake of 3,4 methylenedioxymethamphetamine (MDMA) in healthy placebo-controlled subjects

Abstract

3,4-Methylenedioxymethamphetamine (MDMA; “ecstasy”) is widely consumed recreationally. Little is known about its effects on the human metabolome. Mapping biochemical changes after drug exposure can complement traditional approaches by revealing potential biomarkers of organ toxicity or discovering new metabolomic features in a time- and dose-dependent manner. We aimed to analyze for the first time plasma samples from a randomized, double-blind, placebo-controlled crossover study in healthy adults to explore changes in endogenous plasma metabolites following a single intake of MDMA. Plasma samples from 15 subjects taken at four different time points were analyzed with the commercially available AbsoluteIDQ kit (Biocrates). Time series analysis revealed a total of nine metabolites, which showed a significant concentration change after MDMA administration compared with placebo. Paired t tests of the single time points showed statistically significant concentration changes mainly of glycerophospholipids and the metabolic ratio of methionine-sulfoxide over methionine. Changes of this metabolic ratio may be indicative for changes in systemic oxidative stress levels, and the increased amount of glycerophospholipids could be interpreted as an upregulation of energy production. Baseline samples within the experimental study design were crucial for evaluation of metabolomics data as interday individuality within subjects was high otherwise resulting in overestimations of the findings.
Boxler, M. I., Liechti, M. E., Schmid, Y., Kraemer, T., & Steuer, A. E. (2017). First Time View on Human Metabolome Changes after a Single Intake of 3, 4-Methylenedioxymethamphetamine in Healthy Placebo-Controlled Subjects. Journal of Proteome Research16(9), 3310-3320. 10.1021/acs.jproteome.7b00294
Link to full text

First time view on human metabolome changes after a single intake of 3,4 methylenedioxymethamphetamine (MDMA) in healthy placebo-controlled subjects Read More »

Screening of Hallucinogenic Compounds and Genomic Characterisation of 40 Anatolian Salvia Species

Abstract

INTRODUCTION:
Salvia, an important and widely available member of Lamiaceae family. Although comparative analysis on secondary metabolites in several Salvia species from Turkey has been reported, their hallucinogenic chemicals have not been screened thoroughly.
OBJECTIVE:
This study provides LC-MS/MS analysis of 40 Salvia species for screening their psychoactive constituents of salvinorin A and salvinorin B. 5S-rRNA gene non-coding region of Salvia plants was sequenced, aligned and compared with that sequence of Salvia divinorum plant.
METHODOLOGY:
Targeted molecules of salvinorin A and salvinorin B were quantified, using LC-MS/MS, from all aerial parts of 40 Salvia species, collected from different parts of Turkey. Regions of 5S-rRNA gene from different species were amplified by polymerase chain reaction and DNA sequences were aligned with Salvia divinorum DNA sequences.
RESULTS:
Very few of the Salvia species (S. recognita, S. cryptantha and S. glutinosa) contained relatively high levels of salvinorin A (212.86 ± 20.46 μg/g, 51.50 ± 4.95 μg/g and 38.92 ± 3.74 μg/g, respectively). Salvinorin B was also found in Salvia species of S. potentillifolia, S. adenocaulon and S. cryptantha as 2351.99 ± 232.22 μg/g, 768.78 ± 75.90 μg/g and 402.24 ± 39.71 μg/g, respectively. The sequences of 5S-rRNA gene of 40 different Salvia species were presented and it was found that none of the Salvia species in Turkey had similar DNA sequence to Salvia divinorum plant.
CONCLUSION:
This is the first report of screening 40 Salvia species in Turkey according to their psychoactive constituents, salvinorin A and salvinorin B and their genomic structures. It is possible that some of these Salvia species may exhibit some psycho activity. Thus, they need to be screened further.
Hatipoglu, S. D., Yalcinkaya, B., Akgoz, M., Ozturk, T., Goren, A. C., & Topcu, G. (2017). Screening of Hallucinogenic Compounds and Genomic Characterisation of 40 Anatolian Salvia Species. Phytochemical Analysis. 10.1002/pca.2703
Link to full text

Screening of Hallucinogenic Compounds and Genomic Characterisation of 40 Anatolian Salvia Species Read More »

From rau to sacred plants: Transfigurations of shamanic agency among the Siona Indians of Colombia

Abstract

Translations of the native notion of shamanic agency of the Siona Indians of Colombia is explored throughout different historical and social contexts. The polysemic concept rau is central to the shaman’s capacity for establishing relations of exchange and negotiation with humans and non-humans. As the embodiment of his power, it fits within a semantic field that conveys the waxing and waning of life cycles. Sharing a series of qualities with the Melanesian concept of mana, rau should be understood as a social phenomenon whose use and meaning has transfigured through time and space. However, unlike the globalization of new mana, the important notion of Siona shamanic agency has been substituted by representations of the ritual substance of yajé as key symbol for power and knowledge as Siona rituals have been revitalized in their dialogue with the ethnic identity movement and the neo-shamanic network that associates sacred plants with primordial knowledge and agency.
Langdon, E. J. (2017). From rau to sacred plants: Transfigurations of shamanic agency among the Siona Indians of Colombia. Social Compass64(3), 343-359. 10.1177/0037768617713654
Link to full text

From rau to sacred plants: Transfigurations of shamanic agency among the Siona Indians of Colombia Read More »

Posttraumatic Stress Disorder: An Integrated Overview of the Neurobiological Rationale for Pharmacology

Abstract

Thirty years of research on the biology of posttraumatic stress disorder now provides a foundation for hypotheses related to the mechanisms underlying the pharmacotherapy of this disorder. Only two medications, sertraline and paroxetine, are approved by the U.S. Food and Drug Administration for the treatment of PTSD. Although these medications are somewhat effective, other treatment mechanisms must be explored to address the unmet need for effective treatment. This article provides a concise summary of advances in our understanding of the neurobiology of PTSD and novel approaches to pharmacotherapy.
Kelmendi, B., Adams, T. G., Southwick, S., Abdallah, C. G., & Krystal, J. H. (2017). Posttraumatic stress disorder: An integrated overview of the neurobiological rationale for pharmacology. Clinical Psychology: Science and Practice. 10.1111/cpsp.12202
Link to full text

Posttraumatic Stress Disorder: An Integrated Overview of the Neurobiological Rationale for Pharmacology Read More »

European Psilocybin Seminar at Tyringham Hall

Tyringham Hall In June 2017, a two-day seminar on psilocybin for European therapists and researchers took place at Tyringham Hall, in the UK. The event was organised by OPEN in collaboration with UK mental health company Compass Pathways.
During a wonderful weekend at Tyringham Hall, near Oxford in the UK, attendees were invited to learn from leading experts in psychedelic-assisted psychotherapy, to discuss necessary competencies and other requirements for clinical applications of psilocybin, and to better understand pathways towards regulatory approval and patient access.
Facilitated by leading experts in the field of psilocybin research and therapy from the US, Switzerland and the UK, the participants discussed competencies for (new) therapists aiming to conduct research into psilocybin for various clinical indications. Attendees could learn from both patients and therapists on the importance of preparing, and supporting people in psilocybin-facilitated treatment at NYU, Imperial College and in Switzerland.
This small meeting consisted of a great mixture of academic researchers, clinicians and therapists from all over Europe: Denmark, Sweden, Norway, Portugal, Switzerland, Germany, Czech Republic, the Netherlands, Israel and the United Kingdom. With serious discussions, plenty of time for everyone to connect and share experiences, in a breath-taking setting, this was an inspiring first meeting of like-minded researchers and clinicians.

European Psilocybin Seminar at Tyringham Hall Read More »

Monoamine receptor interaction profiles of 4-thio-substituted phenethylamines (2C-T drugs)

Abstract

BACKGROUND:
4-Thio-substituted phenethylamines (2C-T drugs) are potent psychedelics with poorly defined pharmacological properties. Because of their psychedelic effects, 2C-T drugs are sometimes sold as new psychoactive substances (NPSs). The aim of the present study was to characterize the monoamine receptor and transporter interaction profiles of a series of 2C-T drugs.
METHODS:
We determined the binding affinities of 2C-T drugs at monoamine receptors and transporters in human cells that were transfected with the respective receptors or transporters. We also investigated the functional activation of serotonergic 5-hydroxytryptamine 2A (5-HT2A) and 5-HT2B receptors, activation of human trace amine-associated receptor 1 (TAAR1), and inhibition of monoamine uptake transporters.
RESULTS:
2C-T drugs had high affinity for 5-HT2A and 5-HT2C receptors (1-54 nM and 40-350 nM, respectively). With activation potencies of 1-53 nM and 44-370 nM, the drugs were potent 5-HT2A receptor and 5-HT2B receptor, respectively, partial agonists. An exception to this were the benzylthiophenethylamines, which did not potently activate the 5-HT2B receptor (EC50 > 3000 nM). Furthermore, the compounds bound to serotonergic 5-HT1A and adrenergic receptors. The compounds had high affinity for the rat TAAR1 (5-68 nM) and interacted with the mouse but not human TAAR1. The 2C-T drugs did not potently interact with monoamine transporters (Ki > 4000 nM).
CONCLUSION:
The receptor binding profile of 2C-T drugs predicts psychedelic effects that are mediated by potent 5-HT2 receptor interactions.
Luethi, D., Trachsel, D., Hoener, M. C., & Liechti, M. E. (2017). Monoamine receptor interaction profiles of 4-thio-substituted phenethylamines (2C-T drugs). Neuropharmacology. 10.1016/j.neuropharm.2017.07.012
Link to full text

Monoamine receptor interaction profiles of 4-thio-substituted phenethylamines (2C-T drugs) Read More »

The alkaloids of Banisteriopsis caapi, the plant source of the Amazonian hallucinogen Ayahuasca, stimulate adult neurogenesis in vitro

Abstract

Banisteriopsis caapi is the basic ingredient of ayahuasca, a psychotropic plant tea used in the Amazon for ritual and medicinal purposes, and by interested individuals worldwide. Animal studies and recent clinical research suggests that Bcaapi preparations show antidepressant activity, a therapeutic effect that has been linked to hippocampal neurogenesis. Here we report that harmine, tetrahydroharmine and harmaline, the three main alkaloids present in Bcaapi, and the harmine metabolite harmol, stimulate adult neurogenesis in vitro. In neurospheres prepared from progenitor cells obtained from the subventricular and the subgranular zones of adult mice brains, all compounds stimulated neural stem cell proliferation, migration, and differentiation into adult neurons. These findings suggest that modulation of brain plasticity could be a major contribution to the antidepressant effects of ayahuasca. They also expand the potential application of Bcaapi alkaloids to other brain disorders that may benefit from stimulation of endogenous neural precursor niches.
Morales-García, J. A., de la Fuente Revenga, M., Alonso-Gil, S., Rodríguez-Franco, M. I., Feilding, A., Perez-Castillo, A., & Riba, J. (2017). The alkaloids of Banisteriopsis caapi, the plant source of the Amazonian hallucinogen Ayahuasca, stimulate adult neurogenesis in vitro. Scientific reports7, 5309. 10.1038%2Fs41598-017-05407-9
Link to full text

The alkaloids of Banisteriopsis caapi, the plant source of the Amazonian hallucinogen Ayahuasca, stimulate adult neurogenesis in vitro Read More »

The alkaloids of Banisteriopsis caapi, the plant source of the Amazonian hallucinogen Ayahuasca, stimulate adult neurogenesis in vitro

Abstract

Banisteriopsis caapi is the basic ingredient of ayahuasca, a psychotropic plant tea used in the Amazon for ritual and medicinal purposes, and by interested individuals worldwide. Animal studies and recent clinical research suggests that Bcaapi preparations show antidepressant activity, a therapeutic effect that has been linked to hippocampal neurogenesis. Here we report that harmine, tetrahydroharmine and harmaline, the three main alkaloids present in Bcaapi, and the harmine metabolite harmol, stimulate adult neurogenesis in vitro. In neurospheres prepared from progenitor cells obtained from the subventricular and the subgranular zones of adult mice brains, all compounds stimulated neural stem cell proliferation, migration, and differentiation into adult neurons. These findings suggest that modulation of brain plasticity could be a major contribution to the antidepressant effects of ayahuasca. They also expand the potential application of Bcaapi alkaloids to other brain disorders that may benefit from stimulation of endogenous neural precursor niches.
Morales-García, J. A., de la Fuente Revenga, M., Alonso-Gil, S., Rodríguez-Franco, M. I., Feilding, A., Perez-Castillo, A., & Riba, J. (2017). The alkaloids of Banisteriopsis caapi, the plant source of the Amazonian hallucinogen Ayahuasca, stimulate adult neurogenesis in vitro. Scientific Reports7. 10.1038%2Fs41598-017-05407-9
Link to full text

The alkaloids of Banisteriopsis caapi, the plant source of the Amazonian hallucinogen Ayahuasca, stimulate adult neurogenesis in vitro Read More »

Local Community Meet-up (Amsterdam) - In-Person Event - July 23