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Kaempferide exhibits an anticancer effect against hepatocellular carcinoma in vitro and in vivo. | LitMetric

Kaempferide exhibits an anticancer effect against hepatocellular carcinoma in vitro and in vivo.

Naunyn Schmiedebergs Arch Pharmacol

Department of Pharmacognosy, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, AIMS Health Science Campus, Ponekkara P.O., Kochi, Kerala, 682041, India.

Published: October 2023

AI Article Synopsis

  • Kaempferide, a mono methoxy flavone, shows strong anticancer properties against hepatocellular carcinoma (HCC) in both lab and animal studies.
  • The research employed MTT assays to assess cytotoxicity in various HCC cell lines and utilized in vivo models to evaluate tumor response to kaempferide treatment.
  • Results indicated that kaempferide reduced tumor size and volume, induced apoptosis through caspase activation, and lowered levels of the tumor marker TGF-β 1, suggesting its potential as a therapeutic option for HCC.

Article Abstract

Context: Phytochemicals have been promising candidates for cancer therapy, affecting various cancer initiation and progression stages. Kaempferide is a mono methoxy flavone that shows potent anticancer effects on multiple cancers both in vitro and in vivo.

Materials And Methods: We evaluated the anticancer activity of kaempferide against HCC using an MTT ((3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) assay. HepG2, Huh7, and N1S1 were used for preliminary in vitro studies. This is followed by an apoptosis analysis assessed by caspase-3 and 9. The in vivo effects of the compound were studied in the N1S1 orthotopically injected SD (Sprague Dawley) rat model, where the animal was given kaempferide (25 mg/kg thrice a week) and vehicle (Cremophor:ethanol) iv. The expression of caspase-9 and a critical tumor marker, transforming growth factor beta 1 (TGF-β 1), were assessed in both control and treatment tumor samples.

Results: Kaempferide-induced dose-dependent cytotoxicity in three HCC cell lines (HepG2: IC50 = 27.94 ± 2.199 µM; Huh7: IC50 = 25.65 ± 0.956 µM; and N1S1: IC50 = 15.18 ± 3.68 µM). Furthermore, caspase-dependent apoptosis was confirmed in vitro. Kaempferide showed a significant reduction in tumor size and tumor volume in vivo. Histopathological evaluation by hematoxylin and eosin (H&E) staining confirmed that altered cells were significantly demolished in the kaempferide-treated animals, which correlates with tumor reduction compared to the vehicle-treated group. Caspase-9 levels were also found to be increased in the treatment group. TGF-β 1, a crucial marker in invasion and metastasis of liver cancer, was also downregulated in the treatment group (control = 207.8 ± 22.9 pg/mL and kaempferide-treated = 157.3 ± 13.8 pg/mL).

Conclusion: We report for the first time the potential of kaempferide as a promising alternative against HCC, which further warrants its clinical validation.

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Source
http://dx.doi.org/10.1007/s00210-023-02468-8DOI Listing

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