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Leflunomide is an agonist of aryl hydrocarbon receptor (AHR) [1]. As an immunoregulatory agent, Leflunomide can be administrated orally. A771726 (teriflunomide) is an active drug formed non-enzymatically from leflunomide [2].
Leflunomide has been demonstrated to expand Tregs levels in peripheral blood and stem cells subsets as well as to increase the migration of these cells into the injured kidney. Leflunomide has been displayed to increase cells expressed IL-10 and reduce cells expressed IL-17- and IL-23 in ischemic-reperfused kidney [1].
Leflunomide has shown to significantly lower the lipid peroxidation in male Wistar albino rats of sepsis. Meanwhile, leflunomide successfully inhibited the protein carbonyl rise and NO rise in bowel [2]. Leflunomide has shown to reduce cell proliferation, inhibit tumor marker expression, as well as down-regulate neuroendocrine marker ASCL1 protein expression in a dose- and time-dependent manner in human MTC-TT cells [3].
References:[1] Baban B1, Liu JY, Mozaffari MS. Aryl hydrocarbon receptor agonist, leflunomide, protects the ischemic-reperfused kidney: role of Tregs and stem cells. Am J Physiol Regul Integr Comp Physiol. 2012 Dec;303(11):R1136-46.[2] Ozturk E1, Surucu M2, Karaman A3, Samdancı E4, Fadillioglu E5. Protective effect of leflunomide against oxidative intestinal injury in a rodent model of sepsis. J Surg Res. 2014 Apr;187(2):610-5. [3] Alhefdhi A1, Burke JF, Redlich A, Kunnimalaiyaan M, Chen H. Leflunomide suppresses growth in human medullary thyroid cancer cells. J Surg Res. 2013 Nov;185(1):212-6.
Cell lines
Human medullary thyroid cancer cell line TT (MTC-TT cells)
Reaction Conditions
75 ~ 150 μmol/L leflunomide for 2, 4, or 6 d incubation
Applications
Leflunomide treatment down-regulated neuroendocrine markers achaete-scute complex-like 1 (ASCL1) and chromogranin A. Moreover, leflunomide significantly inhibited the growth of MTC-TT cells in a dose- and time- dependent manner.
Animal models
Male C57BL/6 mice (10 ~ 12 wk of age)
Dosage form
40 mg/kg
Injected intraperitoneally16 h prior to the induction of renal ischemic reperfusion insult
Leflunomide treatment increased regulatory T cells and IL-10-positive cells but reduced IL-17- and IL-23-expressing cells in both the peripheral blood and kidney cells, indicative of down-regulation of inflammatory responses. Leflunomide treatment also increased mobilization of stems cells subsets in the peripheral blood and promoted their recruitment into the ischemic-reperfused kidney. Eventually, leflunomide treatment was able to preserve mitochondrial membrane potential as well as decrease apoptosis and necrosis of renal cells.
Note
The technical data provided above is for reference only.
References:
1. Alhefdhi A, Burke JF, Redlich A, et al. Leflunomide suppresses growth in human medullary thyroid cancer cells. Journal of Surgical Research, 2013, 185(1): 212-216.
2. Baban B, Liu JY, Mozaffari MS. Aryl hydrocarbon receptor agonist, leflunomide, protects the ischemic-reperfused kidney: role of Tregs and stem cells. American Journal of Physiology - Regulatory, Integrative and Comparative Physiology, 2012, 303(11): R1136-1146.
