Neticonazole, an imidazole derivative, is a potent and long-acting antifungal agent. Neticonazole has anti-infective and anticancer effects[1][2][3].In C4-2B cells, Neticonazole reduced the levels of Alix and Rab27a and significantly reduced the levels of nSMase2 at a concentration of 10 µM for 48 h. Neticonazole significantly inhibited the levels of p-ERK[2].Neticonazole inhibits exosome release from C4-2B cells in a dose-dependent manner over a concentration range of less than 10 µM[2].Neticonazole is also an orally active inhibitor of exosome biogenesis and secretion[3].
Neticonazole 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HPXR-Luc HepG2 cells
5.48 µM
24 hours
To evaluate the effect of Neticonazole on PXR activation, results showed it activated PXR.
Toxicol Sci. 2019 Jan 1;167(1):282-292.
C4-2B-CD63-GFP cells
1 µM
48 hours
To validate the inhibitory effect of neticonazole on exosome biogenesis and secretion in prostate cancer cells. Results showed that neticonazole significantly decreased exosome concentration.
Sci Rep. 2018 May 25;8(1):8161.
Trichophyton mentagrophytes
0.25 mg/ml
7 days
Evaluate the in vitro antifungal activity of KP-103 against Trichophyton mentagrophytes, showing that KP-103 was as active as clotrimazole and neticonazole but less active than lanoconazole and butenafine.
Evaluate the in vitro antifungal activity of KP-103 against Trichophyton rubrum, showing that KP-103 was as active as clotrimazole and neticonazole but less active than lanoconazole and butenafine.
Evaluate the therapeutic efficacy of KP-103 in guinea pigs with experimental plantar tinea pedis, showing that 1% KP-103 solution was superior to neticonazole and comparable to lanoconazole and butenafine.
Administered orally by gavage at doses of 1-100 ng/kg, daily for 15 days, Neticonazole significantly improved the survival of colorectal cancer xenograft tumour-bearing mice with dysbiosis of the intestinal flora, which may be achieved by increasing apoptosis of colorectal cancer xenograft tumour cells[3].
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