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All 5 posts Subject: Jump high like a frog with ‘sapo’ Please login to post Down

Nicodem
(Hive Bee)
10-14-04 16:12
No 535828
User Picture       Jump high like a frog with ‘sapo’
(Rated as: excellent)

Certain psychoactive peptides from the Phyllomedusa frog skin act trough the opioid and adenosine receptors. They are not active orally, which is understandable for peptides, but they do pass the blood-brain barrier. I realize there are not many bees interested in ethnobotany here, but since this is not about plants, but about a nice frogy instead, I hoped some might find this interesting as I did (especially the part where adenosine receptor modulating peptides seam to cause a kind of a dissociative-like state).

Phyllomedusa bicolor

Pharmacological Studies Of 'Sapo' From The Frog Phyllomedusa Bicolor Skin: A Drug Used By The Peruvian Matses Indians In Shamanic Hunting Practices
Vlttorio Erspamer, Giuliana Falconieri Erspamer, Cinzia Severini, Rosa Luisa Potenza, Donatella Barra, Giuseppina Mignogna and Antonio Bianchi
Toxicon 31(9), (1992) 1099-1111.

Abstract: The dried skin secretion from Phyllomedusa bicolor, 'sapo' is used by the Matses Indians of the Northern Peru, in shamanic rites mainly designed to improve luck in hunting. When rubbed into burned, exposed areas of the skin, the drug causes the prompt appearance of violent peripheral gastrointestinal and cardiovascular effects soon followed by remarkable central effects (increase in physical strength, heightening of senses, resistance to hunger and thirst, exalted capacity to face stress situations). All the peripheral and most of the central effects of 'sapo' can be ascribed to the exceptionally high content of the drug (up to 7% of its weight) in potently active peptides, easily absorbed through the burned, inflamed areas of the skin. The concentration in ‘sapo’ of the single peptides (phyllocaerulein, phyllomedusin, phyllokinin, dermorphins and deltorphins) has been determined by bioassay, and peptide contents were correlated with the different symptoms of the 'sapo' intoxication.

Frog secretions and hunting magic in the upper Amazon: Identification of a peptide that interacts with an adenosine receptor.
Proc. Natl. Acad. Sci. USA 89, (1992) 10960-10963.
John W. Daly, Janet Caceres, Roger W. Moni, Fabian Gusovsky, Malcolm Moos Jr., Kenneth B. Seamon, Katharine Milton, and Charles W. Myers

Abstract: A frog used for "hunting magic" by several groups of Panoan-speaking Indians in the borderline between Brazil and Peru is identified as Phyllomedusa bicolor. This frog's skin secretion, which the Indians introduce into the body through fresh burns, is rich in peptides. These include vasoactive peptides, opioid peptides, and a peptide that we have named adenoregulin, with the sequence GLWSKIKEVGKEAAKAAAKAAGKAALGAVSEAV as determined from mass spectrometry and Edman degradation. The natural peptide may contain a D amino acid residue, since it is not identical in chromatographic properties to the synthetic peptide. Adenoregulin enhances binding of agonists to A1 adenosine receptors; it is accompanied in the skin secretion by peptides that inhibit binding. The vasoactive peptide sauvagine, the opioid peptides, and adenoregulin and related peptides affect behavior in mice and presumably contribute to the behavioral sequelae observed in humans.

“The real drug-problem is that we need more and better drugs.” – J. Ott

wimpy
(Hive Bee)
10-14-04 17:52
No 535839
      That's pretty interesting - i'd be especially...

That's pretty interesting - i'd be especially interested in the opioid like acting peptides. maybe if one could separate them to avoid at least the cardiovascular and gastrointestinal effects ...

Production or stimulation of endorphines is a thing i keep myself busy with again and again, but i did not find anything practicable yet. Most promising find yet was Anaestesia through Acupuncture (needles with electricity, practised in hospital somewhere in the 70's or 80's) ...

- Beware of the Morphail Effect! -

longimanus
(Hive Bee)
10-23-04 09:07
No 537280
User Picture       More on dermorphin

D-Alanine in the Frog Skin Peptide Dermorphin Is Derived from L-Alanine in the Precursor
Richter, Klaus, Egger, Richard, Kreil, Gunther
Science. Washington: Oct 9, 1987. Vol. 238, Iss. 4824; p. 200

Abstract:
A D-alanine-containing peptide termed dermorphin, with potent, opiate-like activity, has been isolated in the skin of the frog Phyllomedusa sauvagei. This suggests the existence of a novel post-translational reaction for the conversion of an L-amino acid to its D-isomer.
No full text.

Long time dynamics of met-enkephalin: comparison of explicit and implicit solvent models
Shen My, Freed KF
Biophysical Journal. Apr 2002. Vol. 82, Iss. 4; p. 1791

Abstract:
Met-enkephalin is one of the smallest opiate peptides. Yet, its dynamical structure and receptor docking mechanism are still not well understood. The conformational dynamics of this neuron peptide in liquid water are studied here by using all-atom molecular dynamics (MD) and implicit water Langevin dynamics (LD) simulations with AMBER potential functions and the three-site transferable intermolecular potential (TIP3P) model for water. To achieve the same simulation length in physical time, the full MD simulations require 200 times as much CPU time as the implicit water LD simulations. The solvent hydrophobicity and dielectric behavior are treated in the implicit solvent LD simulations by using a macroscopic solvation potential, a single dielectric constant, and atomic friction coefficients computed using the accessible surface area method with the TIP3P model water viscosity as determined here from MD simulations for pure TIP3P water. Both the local and the global dynamics obtained from the implicit solvent LD simulations agree very well with those from the explicit solvent MD simulations. The simulations provide insights into the conformational restrictions that are associated with the bioactivity of the opiate peptide dermorphin for the delta-receptor.

>9MB!

buz
(Hive Bee)
10-24-04 21:51
No 537525
      'fresh burns'?

are the indians burning themselves prior to intake?
if so, that's pretty radical.
i've known some 'skin-burner' people whom held burning cigaretes against their skin, claiming an endorphin rush from the pain. no frogs involved.

longimanus
(Hive Bee)
10-25-04 19:13
No 537753
User Picture       No, no, no

Buz, you`ve got it wrong. The indians burn their skins to boost the introduction of the drug. They just don`t have syringes.

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	All 5 posts		Subject: Jump high like a frog with ‘sapo’		Please login to post		Down


		Nicodem (Hive Bee) 10-14-04 16:12 No 535828				Jump high like a frog with ‘sapo’ (Rated as: excellent)
						Certain psychoactive peptides from the Phyllomedusa frog skin act trough the opioid and adenosine receptors. They are not active orally, which is understandable for peptides, but they do pass the blood-brain barrier. I realize there are not many bees interested in ethnobotany here, but since this is not about plants, but about a nice frogy instead, I hoped some might find this interesting as I did (especially the part where adenosine receptor modulating peptides seam to cause a kind of a dissociative-like state). Phyllomedusa bicolor Pharmacological Studies Of 'Sapo' From The Frog Phyllomedusa Bicolor Skin: A Drug Used By The Peruvian Matses Indians In Shamanic Hunting Practices Vlttorio Erspamer, Giuliana Falconieri Erspamer, Cinzia Severini, Rosa Luisa Potenza, Donatella Barra, Giuseppina Mignogna and Antonio Bianchi Toxicon 31(9), (1992) 1099-1111. Abstract: The dried skin secretion from Phyllomedusa bicolor, 'sapo' is used by the Matses Indians of the Northern Peru, in shamanic rites mainly designed to improve luck in hunting. When rubbed into burned, exposed areas of the skin, the drug causes the prompt appearance of violent peripheral gastrointestinal and cardiovascular effects soon followed by remarkable central effects (increase in physical strength, heightening of senses, resistance to hunger and thirst, exalted capacity to face stress situations). All the peripheral and most of the central effects of 'sapo' can be ascribed to the exceptionally high content of the drug (up to 7% of its weight) in potently active peptides, easily absorbed through the burned, inflamed areas of the skin. The concentration in ‘sapo’ of the single peptides (phyllocaerulein, phyllomedusin, phyllokinin, dermorphins and deltorphins) has been determined by bioassay, and peptide contents were correlated with the different symptoms of the 'sapo' intoxication. Frog secretions and hunting magic in the upper Amazon: Identification of a peptide that interacts with an adenosine receptor. Proc. Natl. Acad. Sci. USA 89, (1992) 10960-10963. John W. Daly, Janet Caceres, Roger W. Moni, Fabian Gusovsky, Malcolm Moos Jr., Kenneth B. Seamon, Katharine Milton, and Charles W. Myers Abstract: A frog used for "hunting magic" by several groups of Panoan-speaking Indians in the borderline between Brazil and Peru is identified as Phyllomedusa bicolor. This frog's skin secretion, which the Indians introduce into the body through fresh burns, is rich in peptides. These include vasoactive peptides, opioid peptides, and a peptide that we have named adenoregulin, with the sequence GLWSKIKEVGKEAAKAAAKAAGKAALGAVSEAV as determined from mass spectrometry and Edman degradation. The natural peptide may contain a D amino acid residue, since it is not identical in chromatographic properties to the synthetic peptide. Adenoregulin enhances binding of agonists to A1 adenosine receptors; it is accompanied in the skin secretion by peptides that inhibit binding. The vasoactive peptide sauvagine, the opioid peptides, and adenoregulin and related peptides affect behavior in mice and presumably contribute to the behavioral sequelae observed in humans. “The real drug-problem is that we need more and better drugs.” – J. Ott



		wimpy (Hive Bee) 10-14-04 17:52 No 535839				That's pretty interesting - i'd be especially...
						That's pretty interesting - i'd be especially interested in the opioid like acting peptides. maybe if one could separate them to avoid at least the cardiovascular and gastrointestinal effects ... Production or stimulation of endorphines is a thing i keep myself busy with again and again, but i did not find anything practicable yet. Most promising find yet was Anaestesia through Acupuncture (needles with electricity, practised in hospital somewhere in the 70's or 80's) ... - Beware of the Morphail Effect! -



		longimanus (Hive Bee) 10-23-04 09:07 No 537280				More on dermorphin
						D-Alanine in the Frog Skin Peptide Dermorphin Is Derived from L-Alanine in the Precursor Richter, Klaus, Egger, Richard, Kreil, Gunther Science. Washington: Oct 9, 1987. Vol. 238, Iss. 4824; p. 200 Abstract: A D-alanine-containing peptide termed dermorphin, with potent, opiate-like activity, has been isolated in the skin of the frog Phyllomedusa sauvagei. This suggests the existence of a novel post-translational reaction for the conversion of an L-amino acid to its D-isomer. No full text. Long time dynamics of met-enkephalin: comparison of explicit and implicit solvent models Shen My, Freed KF Biophysical Journal. Apr 2002. Vol. 82, Iss. 4; p. 1791 Abstract: Met-enkephalin is one of the smallest opiate peptides. Yet, its dynamical structure and receptor docking mechanism are still not well understood. The conformational dynamics of this neuron peptide in liquid water are studied here by using all-atom molecular dynamics (MD) and implicit water Langevin dynamics (LD) simulations with AMBER potential functions and the three-site transferable intermolecular potential (TIP3P) model for water. To achieve the same simulation length in physical time, the full MD simulations require 200 times as much CPU time as the implicit water LD simulations. The solvent hydrophobicity and dielectric behavior are treated in the implicit solvent LD simulations by using a macroscopic solvation potential, a single dielectric constant, and atomic friction coefficients computed using the accessible surface area method with the TIP3P model water viscosity as determined here from MD simulations for pure TIP3P water. Both the local and the global dynamics obtained from the implicit solvent LD simulations agree very well with those from the explicit solvent MD simulations. The simulations provide insights into the conformational restrictions that are associated with the bioactivity of the opiate peptide dermorphin for the delta-receptor. >9MB!



		buz (Hive Bee) 10-24-04 21:51 No 537525				'fresh burns'?
						are the indians burning themselves prior to intake? if so, that's pretty radical. i've known some 'skin-burner' people whom held burning cigaretes against their skin, claiming an endorphin rush from the pain. no frogs involved.



		longimanus (Hive Bee) 10-25-04 19:13 No 537753				No, no, no
						Buz, you`ve got it wrong. The indians burn their skins to boost the introduction of the drug. They just don`t have syringes.

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