Synthesis of a Water‐Soluble Pyrazole Curcumin Derivative: In Vitro and In Vivo AGE Inhibitory Activity and Its Mechanism

The new chemical entity, water‐soluble pyrazole curcumin derivative (PyCurOAc) was designed, synthesized and characterized for the purpose of inhibition of AGE formation. The compound showed an excellent in vitro AGEs inhibition activity than curcumin itself as well as the standard. Further, the AGE...

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Veröffentlicht in:ChemistrySelect (Weinheim) 2017-01, Vol.2 (3), p.1122-1128
Hauptverfasser: Sribalan, Rajendran, Shakambari, Ganeshan, Banuppriya, Govindharasu, Varalakshmi, Perumal, Subramanian, Elayia Raja, Sudhakar, Sivasubramanium, Padmini, Vediappen
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Sprache:eng
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Zusammenfassung:The new chemical entity, water‐soluble pyrazole curcumin derivative (PyCurOAc) was designed, synthesized and characterized for the purpose of inhibition of AGE formation. The compound showed an excellent in vitro AGEs inhibition activity than curcumin itself as well as the standard. Further, the AGE inhibition activity was substantiated in vivo using C.elegans as an animal model. The mechanistic investigation for the inhibition of AGEs with PyCurOAc was studied with glod‐4 expressions in C.elegans and glucose trapping method. This study suggests that the synthesized compound could be used to treat the formation of AGEs in hyperglycemic nematodes and higher animals. A new chemical entity, water‐soluble pyrazole curcumin disodium acetate (PyCurOAc) was designed and synthesized. The compound showed an excellent in vitro AGEs inhibition activity. The AGE inhibition activity was substantiated in vivo using C.elegans as an animal model. The mechanistic investigation for the inhibition of AGEs with PyCurOAc has studied with glod‐4 expressions in nematode and glucose trapping method.
ISSN:2365-6549
2365-6549
DOI:10.1002/slct.201601740