کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1393854 1501108 2016 13 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Cationic lipid-conjugated hydrocortisone as selective antitumor agent
ترجمه فارسی عنوان
هیدروکورتیزون به عنوان عامل ضد توموری انتخابی کاتیونی
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی


• Cationic lipid-hydrocortisone conjugate, HYC16 exhibits high anticancer activity.
• HYC16 triggers up-regulation of p53.
• HYC16 down-regulates pro-angiogenic factor VEGFR2 and blood vessel formation.
• HYC16 effectively regress tumor growth in mice.

Hydrocortisone, the endogenously expressed steroidal, hormonal ligand for glucocorticoid receptor (GR), is body's natural anti-inflammatory and xenobiotic metabolizing agent. It has both palliative as well as adverse effects in different cancer patients. Herein, we show that conjugation product of C16-carbon chain-associated cationic lipid and hydrocortisone (namely, HYC16) induces selective toxicity in cancer (e.g. melanoma, breast cancer and lung adenocarcinoma) cells with least toxicity in normal cells, through induction of apoptosis and cell cycle arrest at G2/M phase. Further, significant tumor growth inhibition was observed in syngeneic melanoma tumor model with considerable induction of apoptosis in tumor-associated cells. In contrast to hydrocortisone, significantly higher anti-angiogenic behavior of HYC16 helped in effective tumor shrinkage. This is the first demonstration to convert natural hormone hydrocortisone into a selective bioactive entity possessing anti-tumor effect.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 108, 27 January 2016, Pages 309–321
نویسندگان
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