Anti-atherosclerotic action of GW9508 – Free fatty acid receptors activator – In apoE-knockout mice

<p>Agonism of Gpr40 Protects the Capacities of Epidermal Stem Cells (ESCs) Against Ultraviolet-B (UV-B)</p>

“…GW9508 is a Gpr40 agonist that has been recently used in studies on atherosclerosis and insulin secretion. 18,19 In the present study, we demonstrate the ability of Gpr40 agonism by GW9508 to rescue the protective functions of ESCs exposed to UV-B radiation. These findings demonstrate a novel use of GW9508 as a treatment for UV-Binduced skin damage.…”

The Anti-Atherosclerotic Action of FFAR4 Agonist TUG-891 in ApoE–Knockout Mice Is Associated with Increased Macrophage Polarization towards M2 Phenotype

“…Only recently, we have directly shown that activation of FFARs led to the inhibition of atherosclerosis in apoE−/− mice [ 13 ]. In this study, anti-atherosclerotic action of GW9508, a synthetic agonist of FFAR1 and FFAR4, was associated with a decrease of M1 macrophage content within the plaque [ 14 ]. It was the first study with the administration of a synthetic agonist of the FFARs in a mouse model of atherosclerosis, however its results are limited due to the non-selective action of GW9508 and its marked toxicity during prolonged administration [ 14 ].…”

“…In this study, anti-atherosclerotic action of GW9508, a synthetic agonist of FFAR1 and FFAR4, was associated with a decrease of M1 macrophage content within the plaque [ 14 ]. It was the first study with the administration of a synthetic agonist of the FFARs in a mouse model of atherosclerosis, however its results are limited due to the non-selective action of GW9508 and its marked toxicity during prolonged administration [ 14 ]. The potency of GW9508 towards FFAR4 is 100 times lower compared to FFAR1 [ 13 ], while TUG-891 shows approximately 100 times greater potency and 10 times higher selectivity towards murine FFAR4 over FFAR1.…”

Diminazene Aceturate Stabilizes Atherosclerotic Plaque and Attenuates Hepatic Steatosis in apoE-Knockout Mice by Influencing Macrophages Polarization and Taurine Biosynthesis

“…To detect the content of macrophages and smooth muscles cells in atherosclerotic plaques, the sections were stained with primary antibodies against CD68 (Serotec, Kidlington, UK) (dilution 1:800) and smooth muscle α-actin (SMA) (Sigma-Aldrich, St. Louis, MO, USA) (dilution 1:800), respectively. Macrophage polarization was assessed as described before [ 49 ]. Antibodies were used against F4/80 (Abcam, Cambridge, UK) (dilution 1:100), nitric oxide synthase 2 (iNOS) (Abcam, Cambridge, UK) (dilution 1:200), arginase 1 (Abcam, Cambridge, UK) (dilution 1:100), and 4’6-diamidino-2-phenylindole (DAPI), for total macrophages, M1-like, M2-like, and cell nuclei, respectively.…”