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Ayahuasca

Ayahuasca Modifies Amphetamine Self Ingestion and Modifies Anxiety and Locomotor Activity in Adolescent Rats

May 9, 2017 / Ayahuasca, Papers, Psychology, Substance Use Disorder / By / , ,

Abstract

Several reports indicate that the hallucinogen beverage better known as Ayahuasca (AYA) may be utilized for the recuperation of drug abusers. However, there is a lack of scientific evidence for this idea, which led us to use laboratory animals to test it. Amphetamine (AMPH), a substance globally abused principally amongst adolescents, is known to have a high potential to lead to addiction, anxiety, and increases in locomotor activity. The objective of the present work was to experimentally evaluate whether AYA is capable of modifying the self ingestion and behavioral effects caused by AMPH. Adolescent rats were trained to ingest water or AMPH solution (0.6 mg/ml) during a 13 days period, in the absence or presence of AYA treatment (2 ml/kg, gavage). 24 h after the last day of treatment, the rats’ locomotor activity and anxiety behaviors were evaluated using an open field arena (OF) and an elevated plus maze (EPM) apparatus. We observed that the animals have a preference for drinking AMPH, and that AYA prevents this preference. In the EPM tasks, AYA treatment significantly decreased the rise in the percentage of closed arm entries caused by AMPH treatment. In the OF tasks, AYA normalized the hyper-locomotor effect of AMPH, as well as the higher latency to cross the central part of arena and the lower number of center crossings in the arena. Taken together, our findings together indicate that AYA is able to modify AMPH ingestion and its effects. In conclusion, this work presents scientific evidence that ayahuasca can be beneficial for drug abuse users. 

Godinho, A. F., Silva, M. C., & Kawashima, J. D. Ayahuasca Modifies Amphetamine Self Ingestion and Modifies Anxiety and Locomotor Activity in Adolescent Rats. Electronic J Biol, 13(2).
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A review on traditional uses, phytochemistry, pharmacology, pharmacokinetics and toxicology of the genus Peganum

May 5, 2017 / Ayahuasca, Biology & Ethnobotany, Papers, Psychiatry & Medicine / By / , ,

Abstract

Ethnopharmacological relevance

The plants of the genus Peganum have a long history as a Chinese traditional medicine for the treatment of cough, hypertension, diabetes, asthma, jaundice, colic, lumbago, and many other human ailments. Additionally, the plants can be used as an amulet against evil-eye, dye and so on, which have become increasingly popular in Asia, Iran, Northwest India, and North Africa.

Aim of the review

The present paper reviewed the ethnopharmacology, phytochemistry, analytical methods, biological activities, metabolism, pharmacokinetics, toxicology, and drug interaction of the genus Peganum in order to assess the ethnopharmacological use and to explore therapeutic potentials and future opportunities for research.

Materials and methods

Information on studies of the genus Peganum was gathered via the Internet (using Google Scholar, Baidu Scholar, Elsevier, ACS, Pudmed, Web of Science, CNKI and EMBASE) and libraries. Additionally, information was also obtained from some local books, PhD and MS’s dissertations.

Results

The genus Peganum has played an important role in traditional Chinese medicine. The main bioactive metabolites of the genus include alkaloids, flavonoids, volatile oils, etc. Scientific studies on extracts and formulations revealed a wide range of pharmacological activities, such as cholinesterase and monoamine oxidase inhibitory activities, antitumor, anti-hypertension, anticoagulant, antidiabetic, antimicrobial, insecticidal, antiparasidal, anti-leishmaniasis, antioxidant, and anti-inflammatory.

Conclusions

Based on this review, there is some evidence for extracts’ pharmacological effects on Alzheimer’s and Parkinson’s diseases, cancer, diabetes, hypertension. Some indications from ethnomedicine have been confirmed by pharmacological effects, such as the cholinesterase, monoamine oxidase and DNA topoisomerase inhibitory activities, hypoglycemic and vasodilation effects of this genus. The available literature showed that most of the activities of the genus Peganum can be attributed to the active alkaloids. Data regarding many aspects of the genus such as mechanisms of actions, metabolism, pharmacokinetics, toxicology, potential drug interactions with standard-of-care medications is still limited which call for additional studies particularly in humans. Further assessments and clinical trials should be performed before it can be integrated into medicinal practices.

Li, S., Cheng, X., & Wang, C. (2017). A review on traditional uses, phytochemistry, pharmacology, pharmacokinetics and toxicology of the genus Peganum. Journal of Ethnopharmacology. 10.1016/j.jep.2017.03.049
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Monoamine Oxidase Inhibitors—Revisiting a Therapeutic Principle

May 1, 2017 / Anxiety Disorders / PTSD, Ayahuasca, Depressive Disorders, Neuroscience, Papers, Psychology / By / ,

Abstract

Over more than 60 years, monoamine oxidase (MAO) inhibitors are available for therapy of central nervous diseases. Although they have shown to be efficacious specifically in the treatment of major depressive disorders and treatment-resistant depression, they became less a therapeutic choice for the physicians mostly due to severe side effects, such as liver failure and hypertensive crisis associated specifically with the first generation of inhibitors. Nevertheless, this class of drugs is still being used for treatment specifically as more selective and reversible inhibitors became available and will provide clinicians with additional treatment options. The current review revisits monoamine oxidase inhibitors and their potential in the treatment of human diseases, such as anxiety, depression, mood and personality disorders, and pain and introduces current ideas and developments.
Entzeroth, M., & Ratty, A. K. (2017). Monoamine Oxidase Inhibitors—Revisiting a Therapeutic Principle. Open Journal of Depression, 6(02), 31. 10.4236/ojd.2017.62004
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Anxiety, panic, and hopelessness during and after ritual ayahuasca intake in a woman with generalized anxiety disorder: A case report

April 24, 2017 / Anxiety Disorders / PTSD, Ayahuasca, Papers, Psychology / By / , , ,

Abstract

Background and aims

Ayahuasca is a dimethyltryptamine- and β-carboline-rich hallucinogenic beverage traditionally used by indigenous groups of Northwest Amazonian for ritual and therapeutic purposes. Animal and human studies suggest that ayahuasca has antidepressant and anxiolytic potentials and has a good safety profile. However, anxiety-like reactions may also occur after ayahuasca intake, although they are rare.

Methods

Case report.

Results

Here, we describe a case of a non-medicated, symptom-free young female with generalized anxiety disorder, who experienced intense anxiety, panic, and hopelessness during and for 3 days after participating in an ayahuasca ritual. The symptoms appeared in the first hours after ayahuasca intake and were gradually reducing in the following hours/days, but were intense enough to cause significant suffering to her, who needed to seek psychiatric help and restarted pharmacological treatment.

Conclusions

Although “bad/horror trips” with anxiety features may occur during the acute effects of ayahuasca and other hallucinogens, to the best of our knowledge, this is the first report of a subacute/prolonged anxiety-like reaction to this substance. Ayahuasca should be used with caution in people with a history of anxiety disorders.

dos Santos, R. G., Osório, F. L., Crippa, J. A. S., & C. Hallak, J. E. (2017). Anxiety, panic, and hopelessness during and after ritual ayahuasca intake in a woman with generalized anxiety disorder: A case report. Journal of Psychedelic Studies, 1(1), 35-39. 10.1556/2054.01.2017.004
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Psychotria viridis: Chemical constituents from leaves and biological properties

April 1, 2017 / Ayahuasca, Biology & Ethnobotany, Papers, Pharmacology & Chemistry, Publications / By / , , , , , ,

Abstract

The phytochemical study of hexane, chloroform and methanol extracts from leaves of Psychotria viridis resulted in the identification of: the pentacyclic triterpenes, ursolic and oleanolic acid; the steroids, 24-methylene-cycloartanol, stigmasterol and β-sitosterol; the glycosylated steroids 3-O-β-D-glucosyl-β-sitosterol and 3-O-β-D-glucosyl-stigmasterol; a polyunsaturated triterpene, squalene; the esters of glycerol, 1-palmitoylglycerol and triacylglycerol; a mixture of long chain hydrocarbons; the aldehyde nonacosanal; the long chain fat acids hentriacontanoic, hexadecanoic and heptadenoic acid; the ester methyl heptadecanoate; the 4-methyl-epi-quinate and two indole alkaloids, N,N-dimethyltryptamine (DMT) and N-methyltryptamine. The chemical structures were determined by means of spectroscopic (IR, 1H and 13C NMR, HSQC, HMBC and NOESY) and spectrometric (CG-MS and LCMS-ESI-ITTOF) methods. The study of biologic properties of P. viridis consisted in the evaluation of the acetylcholinesterase inhibition and cytotoxic activities. The hexane, chloroform, ethyl acetate and methanol extracts, the substances 24-methylene-cycloartanol, DMT and a mixture of 3-O-β-D-glucosyl-β-sitosterol and 3-O-β-D-glucosyl-stigmasterol showed cholinesterase inhibiting activity. This activity induced by chloroform and ethyl acetate extracts was higher than 90%. The methanol and ethyl acetate extracts inhibit the growth and/or induce the death of the tumor cells strains B16F10 and 4T1, without damaging the integrity of the normal cells BHK and CHO. DMT also demonstrated a marked activity against tumor cell strains B16F10 and 4T1.
SOARES, D., DUARTE, L. P., CAVALCANTI, A. D., SILVA, F. C., BRAGA, A. D., LOPES, M. T., … & VIEIRA-FILHO, S. A. (2017). Psychotria viridis: Chemical constituents from leaves and biological properties. Anais da Academia Brasileira de Ciências, 89(2), 927-938. 10.1590/0001-3765201720160411
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Type A monoamine oxidase and serotonin are coordinately involved in depressive disorders: from neurotransmitter imbalance to impaired neurogenesis

March 14, 2017 / Ayahuasca, Depressive Disorders, Neuroscience, Papers / By / , ,

Abstract

Type A monoamine oxidase (MAOA) catabolizes monoamine transmitters, serotonin, norepinephrine and dopamine, and plays a major role in the onset, progression and therapy of neuropsychiatric disorders. In depressive disorders, increase in MAOA expression and decrease in brain levels of serotonin and norepinephrine are proposed as the major pathogenic factors. The functional polymorphism of MAOA gene and genes in serotonin signal pathway are associated with depression. This review presents recent advance in studies on the role of MAOA in major depressive disorder and related emotional disorders. MAOA and serotonin regulate the prenatal development and postnatal maintenance of brain architecture and neurocircuit, as shown by MAOA-deficient humans and MAO knockout animal models. Impaired neurogenesis in the mature hippocampus has been proposed as “adult neurogenesis” hypothesis of depression. MAOA modulates the sensitivity to stress in the stages of brain development and maturation, and the interaction of gene–environmental factors in the early stage regulates the onset of depressive behaviors in adulthood. Vice versa environmental factors affect MAOAexpression by epigenetic regulation. MAO inhibitors not only restore compromised neurotransmitters, but also protect neurons from cell death in depression through induction of anti-apoptotic Bcl-2 and prosurvival neurotrophic factors, especially brain-derived neurotrophic factor, the deficiency of which is detected in depression. This review discusses novel role of MAOA and serotonin in the pathogenesis and therapy of depressive disorders.

Naoi, M., Maruyama, W., & Shamoto-Nagai, M. (2017). Type A monoamine oxidase and serotonin are coordinately involved in depressive disorders: from neurotransmitter imbalance to impaired neurogenesis. Journal of Neural Transmission, 1-14. 10.1007/s0070
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Is Ayahuasca a Potential Ethnic Plant for the Treatment of Parkinson’s Disease?

March 14, 2017 / Ayahuasca, Neuroscience, Papers, Publications / By / , , , ,

Abstract

Objective: Investigate the MAO inhibitory properties, toxicity, behavioral and neuroprotective properties of ayahuasca in mice and dopamine rich neuroblastoma cells in order to assess its potential effects on PD. 

Methods: This study examined the effects of the soluble extract of Banisteriopsis caapi on the activity MAO in mouse brain, the MAO inhibitory activity using HPLC with electrochemical detection and the animal´s behavior in an open field and marble burying test. In vitro cell-based assays in neuroblastoma NB69 cells were employed for evaluation of the antioxidant property of ayahuasca by measuring the auto-oxidation to quinones upon dopamine exposure and its neuroprotective effects against cytotoxicity induced by DA and rotenone. The neuroprotective activity was determined by MTT, LDH and trypan blue or propidium iodide (PI) staining. 

Results: Intraperitoneal injection in mice of ayahuasca extract produced a significant striatal inhibitory effect on MAO A and MAO B activity. In mice striatum of ayahuasca treated mice there is an elevation of dopamine and reduction of the levels of di-hydroxy-phenyl acetic acid (DOPAC), homovanillic acid (HVA) and 5-hydroxy-indole acetic acid (5-HIAA). After ayahuasca administration, the mice display less anxiogenic behavior in marble burying test and less exploratory activities in the open field tests. Results demonstrated no significant antioxidative and neuroprotective effects of ayahuasca on dopamine and rotenone toxicity. 

Conclusion: Ayahuasca extract due its strong inhibitory effect on MAO A activity and more powerful inhibition of MAO B, and absence of toxicity could be used as an alternative or complementary therapy for the treatment of Parkinson´s disease.

Perucho, J., Alarcón, F., Mena, M. Á., de Yebenes, J. G., & Casarejos, M. J. Is Ayahuasca a Potential Ethnic Plant for the Treatment of Parkinson’s Disease?.
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Reproductive effects of the psychoactive beverage ayahuasca in male Wistar rats after chronic exposure

March 9, 2017 / Ayahuasca, Papers, Psychiatry & Medicine, Publications / By / , , ,

Abstract

Ayahuasca is a psychoactive beverage used ancestrally by indigenous Amazonian tribes and, more recently, by Christian religions in Brazil and other countries. This study aimed to investigate the reproductive effects of this beverage in male Wistar rats after chronic exposure. The rats were treated by gavage every other day for 70 days at 0 (control), 1×, 2×, 4× and 8× the dose used in a religious ritual (12 animals per group), and animals euthanized on the 71st day. Compared to controls, there was a significant decrease in food consumption and body weight gain in rats from the 4× and 8× groups, and a significant increase in the brain and stomach relative weight at the 8× group. There was a significant increase in total serum testosterone, and a decrease in spermatic transit time and spermatic reserves in the epididymis caudae in the 4× group, but not in the highest dose group. No significant changes were found in the other reproductive endpoints (spermatozoid motility and morphology, total spermatozoid count and daily sperm production), and histology of testis and epididymis. This study identified a no-observed-adverse-effect-level for chronic and reproductive effects of ayahuasca in male Wistar rats at 2× the ritualistic dose, which corresponds in this study to 0.62 mg/kg bw N,N-dimethyltryptamine, 6.6 mg/kg bw harmine and 0.52 mg/kg bw harmaline. A potential toxic effect of ayahuasca in male rats was observed at the 4× dose, with a non-monotonic dose–response. Studies investigating the role of ayahuasca components in regulating testosterone levels are needed to better understand this action.

Santos, A. D. F. A., Vieira, A. L. S., Pic-Taylor, A., & Caldas, E. D. (2017). Reproductive effects of the psychoactive beverage ayahuasca in male Wistar rats after chronic exposure. Revista Brasileira de Farmacognosia. 10.1016/j.bjp.2017.01.006
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Synthesis of New Harmine Isoxazoles and Evaluation of their Potential Anti-Alzheimer, Anti-inflammatory, and Anticancer Activities

March 1, 2017 / Ayahuasca, Neuroscience, Papers, Pharmacology & Chemistry, Publications / By / , , , ,

Abstract

Harmine 1 was extracted from the seeds of Peganum harmala. From this natural molecule, a new series of isoxazole derivatives with complete regiospecificity were prepared using 1,3-dipolar cycloaddition reactions with various arylnitrile oxides. Harmine and its derivatives were characterized by (1)H NMR, (13)C NMR and HRMS. The evaluation of their anti-acetylcholinesterase (AChE), anti-5-lipoxygenase (5-LOX), anti-xanthine oxidase (XOD) and anticancer activities were studied in vitro against AChE, 5-LOX and XOD enzymes, respectively, and in HTC-116, MCF7 and OVCAR-3 cancer cell lines. The prepared derivatives were shown to be inactive against the XOD enzyme (0-38.3 ± 1.9% at 100 µM). Compound 2 exhibited the best anti-AChE activity (IC50=1.9 ± 1.5 µM). Derivatives 3a, 3b and 3d had moderate cytotoxic activities (IC50=5.0 ± 0.3 µM (3a) and IC50=6.3 ± 0.4 µM (3b) against HCT 116 cells, IC50=5.0 ± 1.0 µM (3d) against MCF7 cells).

Filali, I., Romdhane, A., Znati, M., B Jannet, H., & Bouajila, J. (2016). Synthesis of New Harmine Isoxazoles and Evaluation of their Potential Anti-Alzheimer, Anti-inflammatory, and Anticancer Activities. Medicinal Chemistry, 12(2), 184-190. 10.2174/157340641202160209104115
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Indole Alkaloids from Plants as Potential Leads for Antidepressant Drugs: A Mini Review

February 28, 2017 / Ayahuasca, Biology & Ethnobotany, Depressive Disorders, Neuroscience, Papers, Psychology, Publications / By / , ,

Abstract

Depression is the most common illness observed in the elderly, adults, and children. Antidepressants prescribed are usually synthetic drugs and these can sometimes cause a wide range of unpleasant side effects. Current research is focussed on natural products from plants as they are a rich source of potent new drug leads. Besides Hypericum perforatum (St. John’s wort), the plants studied include Passiflora incarnata L. (passion flower), Mitragyna speciosa (kratom), Piper methysticum G. Forst (kava) and Valeriana officinalis L. Harman, harmol, harmine, harmalol and harmaline are indole alkaloids isolated from P. incarnata, while mitragynine is isolated from M. speciosa. The structure of isolated compounds from P. methysticum G. Forst and V. officinalis L. contains an indole moiety. The indole moiety is related to the neurotransmitter serotonin which is widely implicated for brain function and cognition as the endogenous receptor agonist. An imbalance in serotonin levels may influence mood in a way that leads to depression. The moiety is present in a number of antidepressants already on the market. Hence, the objective of this review is to discuss bioactive compounds containing the indole moiety from plants that can serve as potent antidepressants.

Hamid, H. A., Ramli, A. N., & Yusoff, M. M. (2017). Indole Alkaloids from Plants as Potential Leads for Antidepressant Drugs: A Mini Review. Frontiers in Pharmacology, 8, 96. 10.3389/fphar.2017.00096
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