Chemistry & Biodiversity
May 1, 2009
Daniel Trachsel, David E. Nichols, Stephanie Kidd et al.
15 citations
A series of novel 2-phenylethylamine compounds with a 4'-aryl substituent was synthesized and tested for binding affinity at the serotonin 5-HT(2A) receptor. Most compounds acted as antagonists with generally low affinity, except for a few with substituents at the 4''-position. The 4''-butyl, 4''-phenyl, and 4'-naphthyl derivatives showed relatively high affinity, with K(i) values of 32, 33, and 41 nM, respectively, indicating tolerance for bulky groups at this location. The 4'-aryl moiety was introduced via a palladium-catalyzed Suzuki reaction.
Chemistry & Biodiversity
September 26, 2022
Albert Katchborian‐neto, Mário F. C. Santos, Diego Fernandes Vilas Boas et al.
9 citations
Ayahuasca, a psychoactive beverage made from Banisteriopsis caapi and Psychotria viridis, showed moderate activity against Trypanosoma cruzi trypomastigotes in vitro (IC50 95.78 μg/mL), compared to the reference drug benznidazole (IC50 2.03 μg/mL). The β-carboline alkaloid harmine, isolated from B. caapi, was active (IC50 6.37 μg/mL), while the tryptamine DMT from P. viridis was moderately active (IC50 21.02 μg/mL). In vivo, harmine alone reduced parasitemia in a dose-responsive manner (10 and 100 mg/kg) without toxic effects. Ayahuasca and the harmine-DMT combination worsened parasitemia, suggesting immune modulation via increased IgG and IgG1 antibodies. Molecular docking indicated harmine binds to trypanothione reductase, a promising drug target absent in humans. The findings support ayahuasca's potential against Chagas disease and internal parasites.
Chemistry & Biodiversity
September 23, 2025
Nathália Andrezza Carvalho de Souza, Pedro Guilherme Sousa de Sá, Tarcísio Cícero de Lima Araújo et al.
2 citations
The chemical composition of Mimosa tenuiflora (Jurema-preta), a plant used in traditional medicine, varies with seasons. Over two years of bimonthly collections in northeastern Brazil, phenolic compounds (especially flavonoids) increased with water stress, radiation, and temperature. Production of the psychoactive compound N,N-dimethyltryptamine (DMT) decreased with higher radiation and temperature but was unaffected by rainfall. Total alkaloids and overall yield showed little connection to climate. These findings highlight the importance of considering season when harvesting the plant for pharmacological use.