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- 저자 : Prabhu Muthusamy (검색결과 1 건)
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Enhanced Efficacies of Ginsenoside Compound K conjugated with Polymers in cancer cells
Ramya Mathiyalagan,Sathiyamoorthy Subramaniyam,Prabhu Muthusamy,Deok Chun Yang 한의병리학회 2015 대한동의병리학회 학술대회논문집 Vol.2015 No.10
Cancer is a leading cause of death worldwide. Although numerous anticancer drugs are available, their lack of tumor-targeting and low water-solubility are major drawbacks to use in cancer treatment. Conjugation of anticancer drugs with water-soluble polymers has been exhibited increased water-solubility of hydrophobic drugs, reduced normal cell cytotoxicity, increased accumulation in tumor tissues by passive targeting, and enhanced permeation and retention (EPR) effect. This study, we used ginsenoside compound K (CK) which is triterpenoid found in oriental medical plant- Panax ginseng Meyer. CK is one of the major metabolite after oral administration of crude extracts, reaches systemic circulation and reported for various pharmacological activities. However, solubility and targeted delivery is the major drawback to use of CK in clinical trials. We attempted to developed polymer CK conjugates to enhance its solubility and targeted delivery. To this, hydrophobic CK was covalently conjugated to the hydrophilic glycol chitosan (GC) and polyethylene glycol (PEG) through an acid-labile ester linkage. The resulting GC-CK and PEG-CK conjugates were characterized by H NMR and FTIR. It formed self-assembled spherical shape nanoparticles in water. The conjugates were greatly increased solubility of CK. From in vitro release experiment, release of CK was enhanced under pH 5, whereas it was dramatically decreased under physiological conditions (pH 7.4) is similar to what would be expected in extracellular solid tumor tissues and intracellular endosomes and lysosomes. In vitro cytotoxicity assays revealed that conjugates exhibited higher cytotoxicity in HT29, HepG2, and HT22 cell lines and maintained good cell viability in RAW264.7 cells. These results suggest that these conjugates may be potentially useful as a tumor-specific delivery vehicle which may enhance the overall efficacy of CK.
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