Paregoric Kid
02-15-2010, 03:48 PM
I've been reading about Erinacine E which is a kappa opioid agonist from the mushroom Hericium ramosum. there was also a report that suggests that the mushroom Pleurotus ostreatus may have opioid effects. anyone know of any other opioids from mushrooms/fungi?
Erinacine E as a kappa opioid receptor agonist and its new analogs from a basidiomycete, Hericium ramosum.
Saito T (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Saito%20T%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Aoki F (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Aoki%20F%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Hirai H (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Hirai%20H%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Inagaki T (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Inagaki%20T%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Matsunaga Y (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Matsunaga%20Y%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Sakakibara T (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Sakakibara%20T%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Sakemi S (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Sakemi%20S%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Suzuki Y (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Suzuki%20Y%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Watanabe S (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Watanabe%20S%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Suga O (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Suga%20O%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Sujaku T (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Sujaku%20T%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Smogowicz AA (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Smogowicz%20AA%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Truesdell SJ (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Truesdell%20SJ%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Wong JW (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Wong%20JW%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Nagahisa A (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Nagahisa%20A%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Kojima Y (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Kojima%20Y%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Kojima N (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Kojima%20N%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract).
Natural Product & Lead Discovery Laboratory, Central Research Division, Pfizer Pharmaceuticals Inc., Taketoyo, Aichi, Japan.
A kappa opioid receptor binding inhibitor was isolated from the fermentation broth of a basidiomycete, Hericium ramosum CL24240 and identified as erinacine E (1). Three analogs of 1 were produced by fermentation in other media and by microbial biotransformation. Of these compounds, 1 was shown to be the most potent binding inhibitor. Preliminary SAR studies of these compounds indicated that all functional groups and side chains were required for the activity. Compound 1 was a highly-selective binding inhibitor for the kappa opioid receptor: 0.8 microM (IC50) for kappa, >200 microM for mu, and >200 microM for delta opioid receptor. Compound 1 suppressed electrically-stimulated twitch responses of rabbit vas deferens with an ED50 of 14 microM. The suppression was recovered by adding a selective kappa opioid receptor antagonist nor-binaltorphimine, indicating that 1 is a kappa opioid receptor agonist.
Antinociceptive Activity of Pleurotus ostreatus., an Edible Mushroom, in Rats
N.S. Vasudewahttp://informahealthcare.com/entityImage/?code=200B*, D.T.U. Abeytungahttp://informahealthcare.com/entityImage/?code=200B* and W.D. Ratnasooriyahttp://informahealthcare.com/entityImage/?code=200B*Department of Chemistry, University of Colombo, Colombo, Sri Lanka
Department of Zoology, University of Colombo, Colombo, Sri Lanka
Department of Chemistry, University of Colombo, Colombo 3, Sri Lanka thusitha@chem.cmb.ac.lk (http://informahealthcare.com/doi/abs/10.1080/thusitha@chem.cmb.ac.lk)
Abstract
The antinociceptive potential of Pleurotus ostreatus. (Jacquin: Fries) P. Kummer (Tricholomataceae) was investigated in rats (doses used: 125, 500, and 1000 mg/kg). Male rats and female rats in proestrous, estrous, and diestrous stages were orally administered 1000 mg/kg of freeze-dried P. ostreatus. and the reaction times on hot-plate and tail-flick tests were recorded. In the hot-plate test, the reaction time was significantly prolonged in male rats and diestrous female rats. Marked and significant prolongation in the reaction time at 1 h in males (28% mid and 32% high dose) and up to 2 h in diestrous females (57% mid and 79% high dose after 1 h) were observed on the hot-plate test. This effect was dose-dependent. In contrast, none of the rats showed increases in reaction time in the tail-flick test. In the formalin test, in rats administered a 1000 mg/kg dose of P. ostreatus., pain was significantly suppressed in both phases (females: licking time, 23%, 48%; licking frequency, 28%, 28%; males: licking time, 32%, 43%; licking frequency, no significant change). P. ostreatus. possessed antihistamine activity (histamine wheal test). Naloxone blocked the antinociceptive activity in the hot-plate test; however, metochlopramide did not abolish the activity. P. ostreatus. also showed mild antioxidant activity. Further, a 1000 mg/kgdose of P. ostreatus. did not induce sedation (hole-board test). This dose did not cause mortality or show signs of acute toxicity or stress. It is concluded that P. ostreatus. shows antinociception against neurogenic and continuous inflammatory pain possibly by opioid mechanisms, antioxidative and antihistamine activities.
Erinacine E as a kappa opioid receptor agonist and its new analogs from a basidiomycete, Hericium ramosum.
Saito T (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Saito%20T%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Aoki F (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Aoki%20F%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Hirai H (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Hirai%20H%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Inagaki T (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Inagaki%20T%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Matsunaga Y (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Matsunaga%20Y%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Sakakibara T (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Sakakibara%20T%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Sakemi S (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Sakemi%20S%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Suzuki Y (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Suzuki%20Y%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Watanabe S (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Watanabe%20S%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Suga O (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Suga%20O%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Sujaku T (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Sujaku%20T%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Smogowicz AA (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Smogowicz%20AA%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Truesdell SJ (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Truesdell%20SJ%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Wong JW (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Wong%20JW%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Nagahisa A (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Nagahisa%20A%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Kojima Y (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Kojima%20Y%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract), Kojima N (http://www.ncbi.nlm.nih.gov/pubmed?term=%22Kojima%20N%22%5BAuthor%5D&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsP anel.Pubmed_RVAbstract).
Natural Product & Lead Discovery Laboratory, Central Research Division, Pfizer Pharmaceuticals Inc., Taketoyo, Aichi, Japan.
A kappa opioid receptor binding inhibitor was isolated from the fermentation broth of a basidiomycete, Hericium ramosum CL24240 and identified as erinacine E (1). Three analogs of 1 were produced by fermentation in other media and by microbial biotransformation. Of these compounds, 1 was shown to be the most potent binding inhibitor. Preliminary SAR studies of these compounds indicated that all functional groups and side chains were required for the activity. Compound 1 was a highly-selective binding inhibitor for the kappa opioid receptor: 0.8 microM (IC50) for kappa, >200 microM for mu, and >200 microM for delta opioid receptor. Compound 1 suppressed electrically-stimulated twitch responses of rabbit vas deferens with an ED50 of 14 microM. The suppression was recovered by adding a selective kappa opioid receptor antagonist nor-binaltorphimine, indicating that 1 is a kappa opioid receptor agonist.
Antinociceptive Activity of Pleurotus ostreatus., an Edible Mushroom, in Rats
N.S. Vasudewahttp://informahealthcare.com/entityImage/?code=200B*, D.T.U. Abeytungahttp://informahealthcare.com/entityImage/?code=200B* and W.D. Ratnasooriyahttp://informahealthcare.com/entityImage/?code=200B*Department of Chemistry, University of Colombo, Colombo, Sri Lanka
Department of Zoology, University of Colombo, Colombo, Sri Lanka
Department of Chemistry, University of Colombo, Colombo 3, Sri Lanka thusitha@chem.cmb.ac.lk (http://informahealthcare.com/doi/abs/10.1080/thusitha@chem.cmb.ac.lk)
Abstract
The antinociceptive potential of Pleurotus ostreatus. (Jacquin: Fries) P. Kummer (Tricholomataceae) was investigated in rats (doses used: 125, 500, and 1000 mg/kg). Male rats and female rats in proestrous, estrous, and diestrous stages were orally administered 1000 mg/kg of freeze-dried P. ostreatus. and the reaction times on hot-plate and tail-flick tests were recorded. In the hot-plate test, the reaction time was significantly prolonged in male rats and diestrous female rats. Marked and significant prolongation in the reaction time at 1 h in males (28% mid and 32% high dose) and up to 2 h in diestrous females (57% mid and 79% high dose after 1 h) were observed on the hot-plate test. This effect was dose-dependent. In contrast, none of the rats showed increases in reaction time in the tail-flick test. In the formalin test, in rats administered a 1000 mg/kg dose of P. ostreatus., pain was significantly suppressed in both phases (females: licking time, 23%, 48%; licking frequency, 28%, 28%; males: licking time, 32%, 43%; licking frequency, no significant change). P. ostreatus. possessed antihistamine activity (histamine wheal test). Naloxone blocked the antinociceptive activity in the hot-plate test; however, metochlopramide did not abolish the activity. P. ostreatus. also showed mild antioxidant activity. Further, a 1000 mg/kgdose of P. ostreatus. did not induce sedation (hole-board test). This dose did not cause mortality or show signs of acute toxicity or stress. It is concluded that P. ostreatus. shows antinociception against neurogenic and continuous inflammatory pain possibly by opioid mechanisms, antioxidative and antihistamine activities.