Flumequine (R-802) acts as a topoisomerase II inhibitor, with an IC50 of 3.92 μg/mL, and inhibits Gyrase less effectively, with an IC50 of 1764 μg/mL. Flumequine (0-625 μg/mL) leads to increased migration of nuclear DNA from CHL cells[1]. Flumequine (R-802) effectively inhibits Spanish field isolates of B. hyodysenteriae with MIC50 and MIC90 of 50 and 100 μg/mL, and MBC50 and MBC90 of 50, 200 μg/mL, respectively[2]. Flumequine (R-802) inhibits A. salmonicida isolates with MIC values ranging from 0.06 to 32 μg/mL[3].
体内研究
Flumequine (R-802) (0-500 mg/kg, p.o.) induces dose-dependent DNA damage in the stomach, colon, and urinary bladder of mice, observable 1 and 3 hours, but not 24 hours post administration[1].
体外研究
Flumequine (R-802) acts as a topoisomerase II inhibitor, with an IC50 of 3.92 μg/mL, and inhibits Gyrase less effectively, with an IC50 of 1764 μg/mL. Flumequine (0-625 μg/mL) leads to increased migration of nuclear DNA from CHL cells[1].
Flumequine (R-802) effectively inhibits Spanish field isolates of B. hyodysenteriae with MIC50 and MIC90 of 50 and 100 μg/mL, and MBC50 and MBC90 of 50, 200 μg/mL, respectively[2].
Flumequine (R-802) inhibits A. salmonicida isolates with MIC values ranging from 0.06 to 32 μg/mL[3].
Flumequine/氟甲喹 细胞实验
Cell Line
Concentration
Treated Time
Description
References
B16F10 cells
0–50 μM
72 hours
To investigate the effect of flumequine on melanogenesis. Results showed that flumequine significantly increased extracellular and intracellular melanin content in B16F10 cells and promoted the expression of MITF and tyrosinase.
Biomolecules. 2019 Oct 11;9(10):596
human lymphocytes
25 μg/ml
5 days
To evaluate the effect of Flumequine on [3H]thymidine incorporation in PHA-stimulated human lymphocytes. Results showed that Flumequine significantly increased [3H]thymidine incorporation at 25 μg/ml.
Compare the ability of Flumequine and other quinolones to inhibit the supercoiling activity of DNA gyrase, results showed Flumequine completely inhibited supercoiling activity at 625 μg/ml
To evaluate the effect of flumequine on melanogenesis in vivo. Results showed that flumequine significantly increased melanin pigmentation in zebrafish larvae without any toxicity.
Biomolecules. 2019 Oct 11;9(10):596
Male Wistar rats
Pubertal male rats
Oral
53, 200, 750 mg/kg
Daily for six weeks
To evaluate the toxicological effects of FLU on the endocrine and immune systems. Results showed that weight gain was poorer in the FLU 750 group, with notably higher relative weights of the brain, adrenal and thyroid glands, and testes. Haematological and lipid profile parameters, cardiac markers, and inorganic phosphate significantly increased in the FLU 750 group. Blood glucose, oestradiol and serum concentrations of immunoglobulins G (IgG) and E (IgE) significantly decreased after treatment. The levels of interleukins 10 (IL-10) and 6 (IL-6) fell significantly in the FLU 200 and FLU 750 groups. Cytochrome P450, family 1, subfamily A, polypeptide 1 (CYP1A1) and cyclooxygenase-2 (Cox-2) expression amplified after treatment. Serum levels of free triiodothyronine (fT3) and free thyroxine (fT4) reduced in the FLU 200 and FLU 750 groups without changes in total T3 or T4 level. All doses of FLU significantly depressed concentrations of thyroid-stimulating hormone (TSH) and testosterone. Histopathology of thyroid glands from rats treated with FLU 750 showed degeneration and depletion of thyroid follicular epithelial cells.
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