Cellular uptake and anti-tumor activity of gemcitabine conjugated with new amphiphilic cell penetrating peptides
Cellular uptake and anti-tumor activity of gemcitabine conjugated with new amphiphilic cell penetrating peptides
نویسندگان: پروین ذاکری میلانی , جاوید شهبازی , هادی ولیزاده
کلمات کلیدی: cell penetrating peptide, gemcitabine, toxicity, drug delivery
نشریه: 11475 , 16 , 2017 , 2017
| نویسنده ثبت کننده مقاله |
هادی ولیزاده |
| مرحله جاری مقاله |
تایید نهایی |
| دانشکده/مرکز مربوطه |
مرکز تحقیقات کاربردی دارویی |
| کد مقاله |
60700 |
| عنوان فارسی مقاله |
Cellular uptake and anti-tumor activity of gemcitabine conjugated with new amphiphilic cell penetrating peptides |
| عنوان لاتین مقاله |
Cellular uptake and anti-tumor activity of gemcitabine conjugated with new amphiphilic cell penetrating peptides |
| ناشر |
7 |
| 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 |
http://www.excli.de/vol16/Valizadeh_09052017_proof.pdf |
| ABSTRACT
Gemcitabine (Gem) is used as a single agent or in combination with other anticancer agents to treat many types of solid tumors. However, it has many limitations such as a short plasma half-life, dose-limiting toxicities and drug resistance. Cell-penetrating peptides (CPPs) are short peptides which may deliver a large variety of cargo molecules into the cancerous cells. The current study was designed to evaluate the antiproliferative activity of gemcitabine chemically conjugated to CPPs. The peptides were synthesized using solid phase synthesis proce-dure. The uptake efficiency of CPPs into cells was examined by flow cytometry and fluorescent microscopy. The synthesized peptides were chemically conjugated to Gem and the in vitro cytotoxicity of conjugates was tested by MTT assay on A594 cell line. According to the obtained results, cellular uptake was increased with in-creasing the concentration of CPPs. On the other hand the coupling of Gem with peptides containing block se-quence of arginine (R5W3R4) and some alternating sequences (i.e. [RW]6 and [RW]3) exhibited improved anti-tumor activity of the drug. The findings in this study support the advantages of using cell-penetrating peptides for improving intracellular delivery of Gem into tumor as well as its activity. |
| نام فایل |
تاریخ درج فایل |
اندازه فایل |
دانلود |
| Cellular uptake and anti-tumor activity of gemcitabine conjugated with new amphiphilic cell penetrating peptides.pdf | 1396/02/27 | 1219961 | دانلود |