کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2486141 | 1556514 | 2011 | 13 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Effects of Different Carboxylic Ester Spacers on Chemical Stability, Release Characteristics, and Anticancer Activity of Mono-PEGylated Curcumin Conjugates
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Effects of Different Carboxylic Ester Spacers on Chemical Stability, Release Characteristics, and Anticancer Activity of Mono-PEGylated Curcumin Conjugates Effects of Different Carboxylic Ester Spacers on Chemical Stability, Release Characteristics, and Anticancer Activity of Mono-PEGylated Curcumin Conjugates](/preview/png/2486141.png)
چکیده انگلیسی
We investigated the effects of different carboxylic ester spacers of monoâPEGylated curcumin conjugates on chemical stability, release characteristics, and anticancer activity. Three novel conjugates were synthesized with succinic acid, glutaric acid, and methylcarboxylic acid as the respective spacers between curcumin and monomethoxy polyethylene glycol of molecular weight 2000 (mPEG2000): mPEG2000-succinyl-curcumin (PSC), mPEG2000-glutaryl-curcumin (PGC), and mPEG2000-methylcarboxyl-curcumin (PMC), respectively. Hydrolysis of all conjugates in buffer and human plasma followed pseudo firstâorder kinetics. In phosphate buffer, the overall degradation rate constant and halfâlife values indicated an order of stability of PGC > PSC > PMC > curcumin. In human plasma, more than 90% of curcumin was released from the esters after incubation for 0.25, 1.5, and 2 h, respectively. All conjugates exhibited cytotoxicity against four human cancer cell lines: Cacoâ2 (colon), KB (oral cavity), MCF7 (breast), and NCIâH187 (lung) with half maximal inhibitory concentration (IC50) values in the range of 1-6 µM, similar to that observed for curcumin itself. Our results suggest that monoâPEGylation of curcumin produces prodrugs that are stable in buffer at physiological pH, release curcumin readily in human plasma, and show anticancer activity.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 100, Issue 12, December 2011, Pages 5206-5218
Journal: Journal of Pharmaceutical Sciences - Volume 100, Issue 12, December 2011, Pages 5206-5218
نویسندگان
Wisut Wichitnithad, Ubonthip Nimmannit, Patrick S. Callery, Pornchai Rojsitthisak,