Synthesis and cellular characterization of various nano-assemblies of cell penetrating peptide-epirubicin-polyglutamate conjugates for the enhancement of antitumor activity
Synthesis and cellular characterization of various nano-assemblies of cell penetrating peptide-epirubicin-polyglutamate conjugates for the enhancement of antitumor activity
نویسندگان: هادی ولیزاده , پروین ذاکری میلانی , جاوید شهبازی , صمد موسی فرخانی , علی نخودچی
کلمات کلیدی: Cell penetrating peptides; epirubicin; solid phase peptide synthesis; glutamate; nanoparticles; drug delivery
نشریه: 39930 , 8 , 46 , 2018
| نویسنده ثبت کننده مقاله |
هادی ولیزاده |
| مرحله جاری مقاله |
تایید نهایی |
| دانشکده/مرکز مربوطه |
مرکز تحقیقات کاربردی دارویی |
| کد مقاله |
65888 |
| عنوان فارسی مقاله |
Synthesis and cellular characterization of various nano-assemblies of cell penetrating peptide-epirubicin-polyglutamate conjugates for the enhancement of antitumor activity |
| عنوان لاتین مقاله |
Synthesis and cellular characterization of various nano-assemblies of cell penetrating peptide-epirubicin-polyglutamate conjugates for the enhancement of antitumor activity |
| ناشر |
8 |
| آیا مقاله از طرح تحقیقاتی و یا منتورشیپ استخراج شده است؟ |
بلی |
| عنوان نشریه (خارج از لیست فوق) |
|
| نوع مقاله |
Original Article |
| نحوه ایندکس شدن مقاله |
ایندکس شده سطح یک – ISI - Web of Science |
| آدرس لینک مقاله/ همایش در شبکه اینترنت |
|
| A new class of cell penetrating peptides (CPPs) named peptide amphiphile was designed to improve
the intracellular uptake and the antitumor activity of epirubicin (EPR). Various amphiphilic CPPs were
synthesized by solid phase peptide synthesis method and were chemically conjugated to EPR. Their corresponding nanoparticles (CPPs-E4 and CPPs-E8) were prepared via non-covalent binding of the peptides and polyanions. Cytotoxicity and anti-proliferative activity were evaluated by MTT assay. Cellular
uptake was examined by flow cytometry and fluorescence microscopy. The CPPs exhibited slight cytotoxicity. Binding of polyglutamate to CPPs (CPPs-E4 and CPPs-E8 nanoparticles) decreased their cytotoxicity. CPPs-E8 nanoparticles showed lower cytotoxicity than CPPs-E4 nanoparticles. Cellular uptake of
K3W4K3-E8, K2W4K2-E8 and W3K4W3-E8 reached 100% with no difference between each of the mentioned CPPs and its nanoparticles at 50 mM. The anti-proliferative activity of EPR was enhanced following conjugation to peptides and nanoparticles at 25 mM. CPPs-EPR-E4 and CPPs-E8-EPR nanoparticles
displayed higher anti-proliferative activity than CPPs-EPR at 25 mM. CPPs-E8-EPR nanoparticles showed
higher anti-proliferative activity than CPPs-E4-EPR. K3W4K3-E8-EPR nanoparticles exhibited the highest
anti-proliferative activity at 25 mM. The synthesized peptide nanoparticles are proposed as suitable carriers for improving the intracellular delivery of EPR into tumor cells with low cytotoxicity and high
antitumor activity. |
| نام فایل |
تاریخ درج فایل |
اندازه فایل |
دانلود |
| Synthesis and cellular characterization of various nano-assemblies of cell penetrating peptideepirubicin-polyglutamate conjugates for the enhancement of antitumor activity.pdf | 1397/11/24 | 1832581 | دانلود |