Improved bioactivities of curcumin pyrazole and its HPβCD inclusion complex compared to curcumin.

Autor: Khatun, Bably, Rohilla, Shubham, Rather, Muzamil Ahmad, Sinha, Archana, Dasgupta, Suman, Mandal, Manabendra, Maji, T K
Zdroj: Journal of Chemical Sciences; Mar2023, Vol. 135 Issue 1, p1-14, 14p
Abstrakt: Curcumin is less bioavailable and therefore gets rapidly eliminated from the body. Structural modification of curcumin and its complexation with excipients like 2-Hydroxypropyl- β -cyclodextrin (HP β CD) can circumvent such limitations in respective manners. This study expects to enhance curcumin’s bioactivity by amalgamating both the techniques. Curcumin had been structurally modified and then complexed with HP β CD, characterized, and evaluated for different bioactivities. This manuscript demonstrates that the death of cancer cells followed the apoptotic pathway as estimated from the apoptosis assay. Further, the prepared samples acted as a potent antibacterial and antifungal agents against several bacteria and a fungus, respectively. The samples have more polyphenolic and flavonoid contents compared to curcumin and thereby exhibited better antioxidant activities as estimated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) & 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS) assays. The samples also exhibited better metal chelation activities. All the samples, especially CPCD, prevented the impairment of insulin-stimulated 2-NBDG uptake by L6 myotubes. The samples reduced the LPS-induced κ B luciferase reporter activity. Despite having so many properties, the samples were found to be non-toxic to human PBMCs and RBCs. Curcumin pyrazole-HPβCD inclusion complex is found to be more water soluble compared to either curcumin or curcumin pyrazole and hence has better anticancer, antioxidant, antibacterial, antifungal, antidiabetic & anti-inflammatory activities without being toxic to human PBMCs and RBCs as examined by different in vitro assays. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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