Size Controlled Heparin Fragment-Deoxycholic Acid Conjugate Showed Anticancer Property by Inhibiting VEGF(165)

Title
Size Controlled Heparin Fragment-Deoxycholic Acid Conjugate Showed Anticancer Property by Inhibiting VEGF(165)
Author(s)
정지헌박주호[박주호]Taslim A. Al-Hillal[Taslim A. Al-Hillal]김지영[김지영]변영로[변영로]
Keywords
MOLECULAR-WEIGHT HEPARIN; FIBROBLAST-GROWTH-FACTOR; VENOUS THROMBOEMBOLISM; ORAL DELIVERY; ANGIOGENESIS; CANCER; DERIVATIVES; ANTICOAGULANT; PREVENTION; BEMIPARIN
Issue Date
201505
Publisher
AMER CHEMICAL SOC
Citation
BIOCONJUGATE CHEMISTRY, v.26, no.5, pp.932 - 940
Abstract
Heparin is a highly sulfated, long, and linear polysaccharide, which can inhibit tumor growth by interacting with growth factors such as bFGF and VEGF. Several researchers have shown the anti-angiogenic effect of heparin and its conjugates in relation to growth factor inhibition. For drug development and inhibition of growth factors using heparin conjugates, the molecular size of heparin may be crucial considering the size of the heparin binding site of growth factors. In this study, we synthesized heparin fragments and deoxycholic acid conjugated heparin fragments (HFD) to search for the optimal Size-controlled conjugate that will inhibit the angiogenic effect of VEGF(165). We have also shown that the HFDs could have an enhanced therapeutic effect in vitro and in vivo consequent to the molecular size control. HFDs have significant anti-angiogenic:effects by blocking the angiogenic activity of VEGF(165) depending on its molecular size. Among them, HFD2 was a promising Candidate for oral angiogenesis inhibitor. These results suggest that size-controlled synthesis is necessary for heparin-based drug development.
URI
http://hdl.handle.net/YU.REPOSITORY/32244http://dx.doi.org/10.1021/acs.bioconjchem.5B00133
ISSN
1043-1802
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약학대학 > 약학부 > Articles
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