Curare alkaloids from matis dart poison: Comparison with d-tubocurarine in interactions with nicotinic, 5-HT 3 serotonin and GABA A receptors
Spirova E. N., Ivanov I. A., Kasheverov I. E., Kudryavtsev D. S., Shelukhina I. V., Garifulina A. I., Son L. V., Lummis S. C. R., Malca-Garcia G. R., Bussmann R. W., Hennig L., Giannis A., Tsetlin V. I.
PLoS ONE
Vol.14, Issue1, Num.e0210182
Опубликовано: 2019
Тип ресурса: Статья
DOI:10.1371/journal.pone.0210182
Аннотация:
Several novel bisbenzylisoquinoline alkaloids (BBIQAs) have recently been isolated from a Matis tribe arrow poison and shown by two-electrode voltage-clamp to inhibit mouse muscle nicotinic acetylcholine receptors (nAChR). Here, using radioligand assay with Aplysia californica AChBP and radioiodinated α-bungarotoxin ([ 125 I]-αBgt), we show that BBIQA1, BBIQA2, and d-tubocurarine (d-TC) have similar affinities to nAChR orthosteric site. However, a competition with [ 125 I]-αBgt for binding to the Torpedo californica muscle-type nAChR revealed that BBIQAs1, 2, and 3 are less potent (IC 50 s = 26.3, 8.75, and 17.0 μM) than d-TC (IC 50 = 0.39 μM), while with α7 nAChR in GH 4 C 1 cells, BBIQA1 was less potent that d-TC (IC 50 s = 162 μM and 7.77 μM, respectively), but BBIQA2 was similar (IC 50 = 5.52 μM). In inhibiting the Ca 2+ responses induced by acetylcholine in Neuro2a cells expressing the mouse adult α1β1εδ nAChR or human α7 nAChR, BBIQAs1 and 2 had similar potencies to d-TC (IC 50 s
Ключевые слова:
4 aminobutyric acid A receptor; acetylcholine; alpha bungarotoxin; bisbenzylisoquinoline alkaloid; calcium ion; curare; cysteine; iodine 125; nicotinic receptor; serotonin 3 receptor; tubocurarine chloride; 4 aminobutyric acid A receptor; benzylisoquinoline derivative; curare; intoxication; nicotinic receptor; serotonin 3 receptor; tubocurarine chloride; adult; animal cell; Aplysia californica; Article; binding affinity; controlled study; drug potency; drug receptor binding; drug structure; female; human; IC50; mouse; Neuro-2a cell line; nonhuman; oocyte; protein expression; Torpedo californica; Xenopus laevis; animal; chemistry; metabolism; molecular docking; patch clamp technique; radioassay; structure activity relation; tumor cell line; Animals; Benzylisoquinolines; Cell Line, Tumor; Curare; Inhibitory Concentration 50; Mice; Molecular Docking Simulation; Oocytes; Patch-Clamp Techniques; Poisons; Radioligand Assay; Receptors, GABA-A; Receptors, Nicotinic; Receptors, Serotonin, 5-HT3
Язык текста: Английский
ISSN: 1932-6203
Spirova E. N.
Ivanov I. A.
Kasheverov I. E. Igor` Evgenyevich 1966-
Kudryavtsev D. S.
Shelukhina I. V.
Garifulina A. I.
Son L. V.
Lummis S. C. R.
Malca-Garcia G. R.
Bussmann R. W.
Hennig L.
Giannis A.
Tsetlin V. I.
Спирова Е. Н.
Иванов И. А.
Кашеверов И. Е. Игорь Евгеньевич 1966-
Кудрявцев Д. С.
Шелухина И. В.
Гарифулина А. И.
Сон Л. В.
Луммис С. C. Р.
Малcа-Гарcиа Г. Р.
Буссманн Р. W.
Хенниг Л.
Гианнис А.
Цетлин В. И.
Curare alkaloids from matis dart poison: Comparison with d-tubocurarine in interactions with nicotinic, 5-HT 3 serotonin and GABA A receptors
Текст визуальный непосредственный
PLoS ONE
Vol.14, Issue1 Num.e0210182
2019
Статья
4 aminobutyric acid A receptor acetylcholine alpha bungarotoxin bisbenzylisoquinoline alkaloid calcium ion curare cysteine iodine 125 nicotinic receptor serotonin 3 receptor tubocurarine chloride 4 aminobutyric acid A receptor benzylisoquinoline derivative curare intoxication nicotinic receptor serotonin 3 receptor tubocurarine chloride adult animal cell Aplysia californica Article binding affinity controlled study drug potency drug receptor binding drug structure female human IC50 mouse Neuro-2a cell line nonhuman oocyte protein expression Torpedo californica Xenopus laevis animal chemistry metabolism molecular docking patch clamp technique radioassay structure activity relation tumor cell line Animals Benzylisoquinolines Cell Line, Tumor Curare Inhibitory Concentration 50 Mice Molecular Docking Simulation Oocytes Patch-Clamp Techniques Poisons Radioligand Assay Receptors, GABA-A Receptors, Nicotinic Receptors, Serotonin, 5-HT3
Several novel bisbenzylisoquinoline alkaloids (BBIQAs) have recently been isolated from a Matis tribe arrow poison and shown by two-electrode voltage-clamp to inhibit mouse muscle nicotinic acetylcholine receptors (nAChR). Here, using radioligand assay with Aplysia californica AChBP and radioiodinated α-bungarotoxin ([ 125 I]-αBgt), we show that BBIQA1, BBIQA2, and d-tubocurarine (d-TC) have similar affinities to nAChR orthosteric site. However, a competition with [ 125 I]-αBgt for binding to the Torpedo californica muscle-type nAChR revealed that BBIQAs1, 2, and 3 are less potent (IC 50 s = 26.3, 8.75, and 17.0 μM) than d-TC (IC 50 = 0.39 μM), while with α7 nAChR in GH 4 C 1 cells, BBIQA1 was less potent that d-TC (IC 50 s = 162 μM and 7.77 μM, respectively), but BBIQA2 was similar (IC 50 = 5.52 μM). In inhibiting the Ca 2+ responses induced by acetylcholine in Neuro2a cells expressing the mouse adult α1β1εδ nAChR or human α7 nAChR, BBIQAs1 and 2 had similar potencies to d-TC (IC 50 s