کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10837643 | 1066747 | 2005 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Nematocidal quassinoids and bicyclophosphorothionates: a possible common mode of action on the GABA receptor
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
علوم کشاورزی و بیولوژیک
علوم زراعت و اصلاح نباتات
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چکیده انگلیسی
The present study was undertaken to identify noncompetitive γ-aminobutyric acid receptor (GABAR) antagonists that are effective in nematodes, as well as to examine the hypothesis that the noncompetitive antagonism of the GABAR underlies the nematocidal activity of quassinoids against free-living nematodes of the Diplogastridae family. First, 14 known GABAR antagonists were screened for the effectiveness of their nematocidal activity in Diplogastridae. As a result, 3-isopropyl-1-phospha-2,6,7-trioxabicyclo[2.2.2]octane 1-sulfides (3-isopropyl-BPTs) were found to have high nematocidal activities, and 4-cyclohexyl-3-isopropyl-BPT (23) and 3-isopropyl-4-(2-propenyl)-BPT (27) were the two most potent analogues; these compounds are equipotent to samaderine B and more potent than the anthelmintic abamectin. 23-resistant nematodes, selected by challenge with 23, showed cross-resistance to samaderine B. 23 (10 μM) reduced [3H]23 binding to nematode membranes by 30.4%. Samaderine B (10 μM) resulted in a similar level of the inhibition, but had neither additive nor synergistic effects on the 23 inhibition of [3H]23 binding. These findings suggest that samaderine B shares a common binding site with the GABAR antagonist 23 in Diplogastridae. The results of comparative molecular field analysis, a method of three-dimensional quantitative structure-activity relationship analysis, supported this conclusion.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Pesticide Biochemistry and Physiology - Volume 81, Issue 3, March 2005, Pages 176-187
Journal: Pesticide Biochemistry and Physiology - Volume 81, Issue 3, March 2005, Pages 176-187
نویسندگان
Tadahiko Kuriyama, Xiu-Lian Ju, Sayaka Fusazaki, Hiroyuki Hishinuma, Tadaaki Satou, Kazuo Koike, Tamotsu Nikaido, Yoshihisa Ozoe,