کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9573550 | 1388906 | 2005 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Interactions of amphotericin B derivative of low toxicity with biological membrane components-the Langmuir monolayer approach
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی تئوریک و عملی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Interactions of amphotericin B derivative of low toxicity with biological membrane components-the Langmuir monolayer approach Interactions of amphotericin B derivative of low toxicity with biological membrane components-the Langmuir monolayer approach](/preview/png/9573550.png)
چکیده انگلیسی
Amphotericin B (AmB)-a polyene macrolide antibiotic-exhibits strong antifungal activity, however, is known to be very toxic to mammalian cells. In order to decrease AmB toxicity, a number of its derivatives have been synthesized. Basing on in vitro and in vivo research, it was evidenced that one of AmB derivatives, namely N-methyl-N-d-fructopyranosylamphotericin B methyl ester (in short MF-AME) retained most of the antifungal activity of the parent antibiotic, however, exhibited dramatically lower animal toxicity. Therefore, MF-AME seems to be a very promising modification product of AmB. However, further development of this derivative as potential new antifungal drug requires the elucidation of its molecular mechanism of reduced toxicity, which was the aim of the present investigations. Our studies were based on examining the binding energies by determining the strength of interaction between MF-AME and membrane sterols (ergosterol-fungi sterol, and cholesterol-mammalian sterol) and DPPC (model membrane phospholipid) using the Langmuir monolayer technique, which serves as a model of cellular membrane. Our results revealed that at low concentration the affinity of MF-AME to ergosterol is considerably stronger as compared to cholesterol, which correlates with the improved selective toxicity of this drug. It is of importance that the presence of phospholipids is essential since-due to very strong interactions between MF-AME and DPPC-the antibiotic used in higher concentration is “immobilized” by DPPC molecules, which reduces the concentration of free antibiotic, thus enabling it to selectively interact with both sterols.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biophysical Chemistry - Volume 116, Issue 1, 1 June 2005, Pages 77-88
Journal: Biophysical Chemistry - Volume 116, Issue 1, 1 June 2005, Pages 77-88
نویسندگان
K. HÄ
c-Wydro, P. Dynarowicz-ÅÄ
tka, J. Grzybowska, E. Borowski,