کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2064022 1544117 2016 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
The voltage-gated sodium ion channel inhibitory activities of a new tetrodotoxin analogue, 4,4a-anhydrotetrodotoxin, and three other analogues evaluated by colorimetric cell-based assay
ترجمه فارسی عنوان
فعالیت های مهاری یون سدیم با ولتاژ دارای محدودیت کانال آنالوگ جدید تترودوتوکسین، 4،4a-anhydrotetrodotoxin و سه آنالوگ دیگر ارزیابی شده با روش سنجشی رنگ سنجی مبتنی بر سلول
کلمات کلیدی
تترودوتوکسین؛ کانال یون سدیم با ولتاژ دارای محدودیت ؛ عصب 2A؛ 11-Oxotetrodotoxin؛ 4،4a-anhydrotetrodotoxin؛ مالیمید
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی بیوشیمی، ژنتیک و زیست شناسی مولکولی (عمومی)
چکیده انگلیسی


• Nav inhibitory activities of four TTX analogues were evaluated by cytotoxicity protection assay.
• EC50 of 4,4a-anhydroTTX was 750 fold larger than that of TTX, supporting the implication of 4-OH.
• The high activity of 11-oxoTTX as same as TTX was confirmed by this assay.
• The activity of 11-norTTX-6,6-diol by this assay was much less than that previously reported.
• Modification of C-6 in 11-norTTX-6,6-diol by introducing a maleimide moiety reduced activity.

The voltage-gated sodium ion channel inhibitory activities of four tetrodotoxin analogues were evaluated for their ability to reduce the cytotoxicity of ouabain and veratridine in mouse neuroblastoma Neuro-2a cells. EC50 of the novel analogue, 4,4a-anhydrotetrodotoxin purified from pufferfish, was 750 fold larger than that of tetrodotoxin, supporting the implication of 4-OH in activity. The high activity of 11-oxotetrodotoxin was confirmed. Modification of C-6 of 11-nortetrodotoxin-6,6-diol to form an oxime derivative decreased the activity to 1/22.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Toxicon - Volume 119, 1 September 2016, Pages 72–76
نویسندگان
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