The Monascus species has been used in foods for thousands of years in China. In this study;
10 azaphilone pigments;
including four yellow and six orange pigments;
were isolated from the fermented rice and dioscorea of Monascus purpureus NTU 568. By employing lipopolysaccharide (LPS)-stimulated murine macrophage RAW 264.7 cells;
we determined the inhibitory activities of these pigments on nitric oxide (NO) production. As a result;
four orange pigments;
monaphilols A-D;
showed the highest activities (IC50 = 1.0-3.8 μM);
compared with the other two orange pigments;
monascorubrin (IC 50 > 40 μM) and rubropunctatin (IC50 = 21.2 μM);
and the four yellow pigments ankaflavin (IC50 = 21.8 μM);
monascin;
(IC50;
29.1;
μM);
monaphilone A (IC50 = 19.3 μM);
and monaphilone B (IC50 = 22.6 μM). Using Western blot and ELISA kits;
we found that treatments with 30 μM of the yellow pigments and 5 μM of the orange pigments could down-regulate the protein expression of inducible nitric oxide synthase (iNOS) and suppress the production of tumor necrosis factor-α (TNF-α);
interleukin-1β;
(IL-1β);
and interleukin-6 (IL-6). We also used two animal experiments to evaluate the anti-inflammatory effects of these pigments. In a 12-O-tetradecanoylphorbol-13- acetate (TPA)-induced ear edema model;
eight of these pigments (0.5 mg/ear) could prevent ear edema against TPA administrations on the ears of BALB/c mice. In an LPS-injection mice model;
several of these pigments (10 mg/kg) could inhibit the NO;
TNF-α;
IL-1β;
and IL-6 levels in the plasma of BALB/c mice. As concluded from the in vitro and in vivo studies;
six azaphilonoid pigments;
namely;
ankaflavin;
monaphilone A;
and monaphilols A-D;
showed high potential to be developed into chemopreventive foods or drugs against inflammation-associated diseases. © 2013 American Chemical Society;