A flavonoid with diverse biological activities
Cirsiliol is a flavonoid that has been found in S. indicum and has diverse biological activities.1 It inhibits 5-lipoxygenase (5-LO) and 12-LO (IC50s = 0.1 and 1 ?M, respectively).1 Cirsiliol inhibits the release of slow-reacting substance of anaphylaxis (SRS-A) in passively sensitized isolated guinea pig lung (IC50 = 0.4 ?M). It induces relaxation of precontracted isolated rat uterus, urinary bladder, proximal aorta, and trachea in a concentration-dependent manner.2 Cirsiliol inhibits colony formation and migration of B16/F10 murine melanoma cells.3 In vivo, cirsiliol (200 ?g/kg) enhances radiation-induced inhibition of tumor growth in an H1299 non-small cell lung cancer (NSCLC) mouse xenograft model.4
1.Yoshimoto, T., Furukawa, M., Yamamoto, S., et al.Flavonoids: Potent inhibitors of arachidonate 5-lipoxygenaseBiochem. Biophys. Res. Commun.116(2)612-618(1983) 2.Mustafa, E.H., Zarga, M.A., Sabri, S., et al.Effects of cirsiliol, a flavone isolated from Achillea fragrantissima, on rat isolated smooth muscleInt. J. Pharm.33(3)204-209(1995) 3.Prasad, P., Vasas, A., Hohmann, J., et al.Cirsiliol suppressed epithelial to mesenchymal transition in B16F10 malignant melanoma cells through alteration of the PI3K/Akt/NF-κB signaling pathwayInt. J. Mol. Sci.20(3)608(2019) 4.Kang, J., Kim, E., Kim, W., et al.Rhamnetin and cirsiliol induce radiosensitization and inhibition of epithelial-mesenchymal transition (EMT) by miR-34a-mediated suppression of Notch-1 expression in non-small cell lung cancer cell linesJ. Biol. Chem.288(38)27343-27357(2013)
Cell experiment: | NSCLC, NCI-H1299, NCI-H460, WI-26 VA4 and MRC-5 cell lines are exposed to a single dose of γ-rays. Cells are then treated with rhamnetin and cirsiliol (5, 10, 15, 20, 25 μM) dissolved in DMSO for 4 h[2]. |
Animal experiment: | Mice[1]BALB/c athymic nude mice are injected with 2×106 NCI-H1299 cells. When the tumor has acquired a minimal volume of 200 mm3, DMSO or Cirsiliol (200 μg/kg body weight) is administered intraperitoneally every day for 25 days. The animals are also irradiated with 10 Gy once a week for 3 weeks. On day 25, the tumors are excised and subjected to further analyses[1]. |
参考文献: [1]. Mustafa EH, et al. Effects of cirsiliol, a flavone isolated from Achillea fragrantissima, on rat isolated ileum. Gen Pharmacol. 1992 May;23(3):555-60. | |
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