Tags

Type your tag names separated by a space and hit enter

Actions of octocoral and tobacco cembranoids on nicotinic receptors.
Toxicon 2009; 54(8):1174-82T

Abstract

Nicotinic acetylcholine receptors (AChRs) are pentameric proteins that form agonist-gated cation channels through the plasma membrane. AChR agonists and antagonists are potential candidates for the treatment of neurodegenerative diseases. Cembranoids are naturally occurring diterpenoids that contain a 14-carbon ring. These diterpenoids interact with AChRs in complex ways: as irreversible inhibitors at the agonist sites, as noncompetitive inhibitors, or as positive modulators, but no cembranoid was ever shown to have agonistic activity on AChRs. The cembranoid eupalmerin acetate displays positive modulation of agonist-induced currents in the muscle-type AChR and in the related gamma-aminobutyric acid (GABA) type A receptor. Moreover, cembranoids display important biological effects, many of them mediated by nicotinic receptors. Cembranoids from tobacco are neuroprotective through a nicotinic anti-apoptotic mechanism preventing excitotoxic neuronal death which in part could result from anti-inflammatory properties of cembranoids. Moreover, tobacco cembranoids also have anti-inflammatory properties which could enhance their neuroprotective properties. Cembranoids from tobacco affect nicotine-related behavior: they increase the transient initial ataxia caused by first nicotine injection into naive rats and inhibit the expression of locomotor sensitization to repeated injections of nicotine. In addition, cembranoids are known to act as anti-tumor compounds. In conclusion, cembranoids provide a promising source of lead drugs for many clinical areas, including neuroprotection, smoking-cessation, and anti-cancer therapies.

Authors+Show Affiliations

Department of Biochemistry, Universidad Central del Caribe, Bayamon, PR, USA.

Pub Type(s)

Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Review

Language

eng

PubMed ID

19281835

Citation

Ferchmin, P A., et al. "Actions of Octocoral and Tobacco Cembranoids On Nicotinic Receptors." Toxicon : Official Journal of the International Society On Toxinology, vol. 54, no. 8, 2009, pp. 1174-82.
Ferchmin PA, Pagán OR, Ulrich H, et al. Actions of octocoral and tobacco cembranoids on nicotinic receptors. Toxicon. 2009;54(8):1174-82.
Ferchmin, P. A., Pagán, O. R., Ulrich, H., Szeto, A. C., Hann, R. M., & Eterović, V. A. (2009). Actions of octocoral and tobacco cembranoids on nicotinic receptors. Toxicon : Official Journal of the International Society On Toxinology, 54(8), pp. 1174-82. doi:10.1016/j.toxicon.2009.02.033.
Ferchmin PA, et al. Actions of Octocoral and Tobacco Cembranoids On Nicotinic Receptors. Toxicon. 2009 Dec 15;54(8):1174-82. PubMed PMID: 19281835.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Actions of octocoral and tobacco cembranoids on nicotinic receptors. AU - Ferchmin,P A, AU - Pagán,Oné R, AU - Ulrich,Henning, AU - Szeto,Ada C, AU - Hann,Richard M, AU - Eterović,Vesna A, Y1 - 2009/03/10/ PY - 2009/3/14/entrez PY - 2009/3/14/pubmed PY - 2010/3/6/medline SP - 1174 EP - 82 JF - Toxicon : official journal of the International Society on Toxinology JO - Toxicon VL - 54 IS - 8 N2 - Nicotinic acetylcholine receptors (AChRs) are pentameric proteins that form agonist-gated cation channels through the plasma membrane. AChR agonists and antagonists are potential candidates for the treatment of neurodegenerative diseases. Cembranoids are naturally occurring diterpenoids that contain a 14-carbon ring. These diterpenoids interact with AChRs in complex ways: as irreversible inhibitors at the agonist sites, as noncompetitive inhibitors, or as positive modulators, but no cembranoid was ever shown to have agonistic activity on AChRs. The cembranoid eupalmerin acetate displays positive modulation of agonist-induced currents in the muscle-type AChR and in the related gamma-aminobutyric acid (GABA) type A receptor. Moreover, cembranoids display important biological effects, many of them mediated by nicotinic receptors. Cembranoids from tobacco are neuroprotective through a nicotinic anti-apoptotic mechanism preventing excitotoxic neuronal death which in part could result from anti-inflammatory properties of cembranoids. Moreover, tobacco cembranoids also have anti-inflammatory properties which could enhance their neuroprotective properties. Cembranoids from tobacco affect nicotine-related behavior: they increase the transient initial ataxia caused by first nicotine injection into naive rats and inhibit the expression of locomotor sensitization to repeated injections of nicotine. In addition, cembranoids are known to act as anti-tumor compounds. In conclusion, cembranoids provide a promising source of lead drugs for many clinical areas, including neuroprotection, smoking-cessation, and anti-cancer therapies. SN - 1879-3150 UR - https://www.unboundmedicine.com/medline/citation/19281835/Actions_of_octocoral_and_tobacco_cembranoids_on_nicotinic_receptors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0041-0101(09)00135-4 DB - PRIME DP - Unbound Medicine ER -