Improved bioactivities of curcumin pyrazole and its HP β CD inclusion complex compared to curcumin
JOURNAL OF CHEMICAL SCIENCES(2023)
摘要
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. Graphical abstract 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.
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关键词
Curcumin,HP β CD,inclusion complex,bioactivities
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