Inhibitory Effects of Flavonoids on Animal Fatty Acid Synthase

Li, Bing Hui; Tian, Wei

doi:10.1093/jb/mvh010

Cited by 66 publications

(53 citation statements)

References 15 publications

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“…25) The inhibitory effects of quercetin on fatty acid synthase activity have also been shown in an in vitro experiment. 26) In this present experiment, no effect of quercetin on decreasing triacylglycerol and cholesterol in the plasma was apparent in the rats fed with the highfat high-sucrose diet. These results suggest that quercetin had no significant hypolipidemic effect when added to the diet at a concentration of less than 0.5%.…”

Section: Discussioncontrasting

confidence: 50%

Antihypertensive Effect of Quercetin in Rats Fed with a High-Fat High-Sucrose Diet

Yamamoto

Oue

2006

Bioscience, Biotechnology, and Biochemistry

114

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Section: Discussioncontrasting

confidence: 50%

Antihypertensive Effect of Quercetin in Rats Fed with a High-Fat High-Sucrose Diet

Yamamoto

Oue

2006

Bioscience, Biotechnology, and Biochemistry

114

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“…32 Many flavonoids (genistein, morin) were reported to efficiently inhibit FAS with IC 50 values ranging from 2 to 112 mM. 33 As cirsimarin shares some characteristics with these flavonoids described to inhibit FAS, it is tempting to speculate that cirsimarin could decrease WAT lipogenesis through a direct inhibition of FAS. Surprisingly, the effect of some FAS inhibitors on BW were mediated through their action on central nervous system rather than their direct action on adipose tissue.…”

Section: Discussionmentioning

confidence: 99%

Cirsimarin, a potent antilipogenic flavonoid, decreases fat deposition in mice intra-abdominal adipose tissue

et al. 2010

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Objective: We previously reported that the flavonoid cirsimarin exerts in vitro a strong lipolytic activity on isolated adipocytes. This study was therefore designed to evaluate in vivo the effects of cirsimarin on white adipose tissue (WAT) accretion in mice. Methods: Male CD1 mice were injected daily with either vehicle (intraperitoneal (i.p.)) or cirsimarin (25 or 50 mg kg -1 per day, i.p.) for 18 days. Mice were killed and fat pads weighted. Epididymal fat pads were used for cellularity measurement. Effects of cirsimarin treatment on lipolysis and lipogenesis in WAT were assessed. Results: Mice treated with 25 or 50 mg kg -1 per day cirsimarin showed a decrease in retroperitoneal (À29 and À37% respectively, Po0.005) and epididymal (À25 and À28% respectively, Po0.005) fat pad weights compared with controls. This effect was restricted to intra-abdominal WAT as no difference was noticed for subcutaneous inguinal WAT. The decrease in intra-abdominal WAT accretion was due to a decrease in adipose cell diameter (À5 and À8% for 25 and 50 mg kg -1 per day cirsimarin, respectively) resulting in a 14 and 35% decrease in adipose cell volume while no change was noticed in total adipocyte number. Direct injection of cirsimarin (50 mg kg -1 ) to rats did not trigger lipolysis. In contrast, cirsimarin showed in vivo as well as in vitro a strong antilipogenic activity, which may be the critical aspect of its effects on fat accretion in mice. The inhibitory concentration 50% of cirsimarin on lipogenic activity in isolated adipocytes was found to be 1.28 ± 0.04 mM. Cirsimarin given orally reduced intra-abdominal fat accretion in mice. Conclusion: Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. Cirsimarin could therefore be a potential candidate for the treatment of obesity.

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“…A number of flavonoids have been shown to inhibit both fungal and human FAS-I (Li & Tian, 2004;Li et al, 2002;Wang et al, 2003). Flavonoids comprise a large group of polyphenolic secondary metabolites that are widespread throughout the plant kingdom (Koes et al, 1994).…”

Section: Introductionmentioning

confidence: 99%

Flavonoid inhibitors as novel antimycobacterial agents targeting Rv0636, a putative dehydratase enzyme involved in Mycobacterium tuberculosis fatty acid synthase II

et al. 2007

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Flavonoids comprise a large group of bioactive polyphenolic plant secondary metabolites. Several of these possess potent in vivo activity against Escherichia coli and Plasmodium falciparum, targeting enzymes involved in fatty acid biosynthesis, such as enoyl-ACP-reductase, b-ketoacyl-ACP reductase and b-hydroxyacyl-ACP dehydratase. Herein, we report that butein, isoliquirtigenin, 2,29,49-trihydroxychalcone and fisetin inhibit the growth of Mycobacterium bovis BCG. Furthermore, in vitro inhibition of the mycolic-acid-producing fatty acid synthase II (FAS-II) of Mycobacterium smegmatis suggests a mode of action related to those observed in E. coli and P. falciparum. Through a bioinformatic approach, we have established the product of Rv0636 as a candidate for the unknown mycobacterial dehydratase, and its overexpression in M. bovis BCG conferred resistance to growth inhibition by butein and isoliquirtigenin, and relieved inhibition of fatty acid and mycolic acid biosynthesis in vivo. Furthermore, after overexpression of Rv0636 in M. smegmatis, FAS-II was less sensitive to these inhibitors in vitro. Overall, the data suggest that these flavonoids are inhibitors of mycobacterial FAS-II and in particular Rv0636, which represents a strong candidate for the b-hydroxyacyl-ACP dehydratase enzyme of M. tuberculosis FAS-II.

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Inhibitory Effects of Flavonoids on Animal Fatty Acid Synthase

Cited by 66 publications

References 15 publications

Antihypertensive Effect of Quercetin in Rats Fed with a High-Fat High-Sucrose Diet

Antihypertensive Effect of Quercetin in Rats Fed with a High-Fat High-Sucrose Diet

Cirsimarin, a potent antilipogenic flavonoid, decreases fat deposition in mice intra-abdominal adipose tissue

Flavonoid inhibitors as novel antimycobacterial agents targeting Rv0636, a putative dehydratase enzyme involved in Mycobacterium tuberculosis fatty acid synthase II

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