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DR ANTHONY MELVIN CRASTO, WORLDDRUGTRACKER

Could “Magic” Mushrooms be used to treat anxiety and depression?

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Jun 252013
 

Emerging research indicates that low doses of the active chemical psilocybin can have positive psychiatric effects. Image via Wikimedia Commons/Dohduhdah Read more: http://blogs.smithsonianmag.com/science/2013/06/could-magic-mushrooms-be-used-to-treat-anxiety-and-depression/#ixzz2VpZRRGE2  Follow us: @SmithsonianMag on Twitter

Emerging research indicates that low doses of the active chemical psilocybin can have positive psychiatric effects. Image via Wikimedia Commons/Dohduhdah

The latest study, published last week in Experimental Brain Research, showed that dosing mice with a purified form of psilocybin reduced their outward signs of fear. The rodents in the study had been conditioned to associate a particular noise with the feeling of being electrically shocked, and all the mice in the experiment kept freezing in fear when the sound was played even after the shocking apparatus was turned off. Mice who were given low doses of the drug, though, stopped freezing much earlier on, indicating that they were able to disassociate the stimuli and the negative experience of pain more easily.

http://myscienceacademy.org/2013/06/12/could-magic-mushrooms-be-used-to-treat-anxiety-and-depression/

File:Psilocybn.svg

Psilocybin is a naturally occurring psychedeliccompound produced by more than 200 species of mushrooms, collectively known aspsilocybin mushrooms. The most potent are members of the genus Psilocybe, such asP. azurescensP. semilanceata, and P. cyanescens, but psilocybin has also been isolated from about a dozen other genera. As a prodrug, psilocybin is quickly converted by the body to psilocin, which has mind-altering effects similar to those of LSDmescaline, and DMT. The effects generally include euphoria, visual and mental hallucinations, changes in perception, a distorted sense of time, and spiritual experiences, and can include possible adverse reactions such as nausea and panic attacks.

 

Psilocybin (O-phosphoryl-4-hydroxy-N,N-dimethyltryptamine or 4-PO-DMT) is a prodrug that is converted into the pharmacologicallyactive compound psilocin in the body by a dephosphorylation reaction. This chemical reaction takes place under strongly acidicconditions, or under physiological conditions in the body, through the action of enzymes called phosphatases.

Psilocybin is a tryptamine compound with a chemical structure containing an indole ring linked to an ethylamine substituent. It is chemically related to the amino acid tryptophan, and is structurally similar to the neurotransmitter serotonin. Psilocybin is a member of the general class of tryptophan-based compounds that originally functioned as antioxidants in earlier life forms before assuming more complex functions in multicellular organisms, including humans. Other related indole-containing psychedelic compounds includedimethyltryptamine, found in many plant species and in trace amounts in some mammals, and bufotenine, found in the skin ofpsychoactive toads. Biosynthetically, the biochemical transformation from tryptophan to psilocybin involves several enzyme reactions: decarboxylation, methylation at the N9 position, 4-hydroxylation, and O-phosphorylation. Isotopic labeling experiments suggest that tryptophan decarboxylation is the initial biosynthetic step and that O-phosphorylation is the final step. The precise sequence of the intermediate enzymatic steps is not known with certainty, and the biosynthetic pathway may differ between species.

A possible biosynthetic route to psilocybin. Although the order of the first (decarboxylation) and last (phosphorylation) steps are known with some certainty, the sequence of the two intermediate steps is speculative.

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New aspects of natural products in drug discovery

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Jun 252013
 

 

 

Full-size image (66 K)

Structures of compounds of microbial origin that are in development as anti-infective agents. Key to compounds: 1, arylomycin; 2, ECO-0501; 3, GE23077; 4, GE81112; 5, LBM415; 6, AC98–6446.

During the past 15 years, most large pharmaceutical companies have decreased the screening of natural products for drug discovery in favor of synthetic compound libraries. Main reasons for this include the incompatibility of natural product libraries with high-throughput screening and the marginal improvement in core technologies for natural product screening in the late 1980s and early 1990s. Recently, the development of new technologies has revolutionized the screening of natural products. Applying these technologies compensates for the inherent limitations of natural products and offers a unique opportunity to re-establish natural products as a major source for drug discovery. Examples of these new advances and technologies are described in this review.

http://www.sciencedirect.com/science/article/pii/S0966842X07000686

New aspects of natural products in drug discovery

  • Nereus Pharmaceuticals Inc., 10480 Wateridge Circle, San Diego, CA 92121, USA

Available online 11 April 2007

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