Fatty Acid Synthase Inhibitors from Plants:  Isolation, Structure Elucidation, and SAR Studies

Li, Xing-Cong; Joshi, Alpana S.; ElSohly, Hala N.; Khan, Shabana I.; Jacob, Melissa R.; Zhang, Zhizheng; Khan, Ikhlas A.; Ferreira, Daneel; Walker, Larry; Broedel, Sheldon E.; Raulli, Robert; Cihlar, R. L.

doi:10.1021/np020289t

Cited by 92 publications

(78 citation statements)

References 40 publications

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“…Sobre as espécies P. guianensis e D. excelsa ainda não se tem dados, mas B. parviflora apresenta compostos como isoflavonas, flavonas, biflavonóides, derivados hidrolisados de taninos e triterpenóides (Li et al, 2002). Neste caso, os resultados observados demonstram que a atividade termicida ou de repelência dos extrativos poderiam ser atribuídas à atuação de alguns desses compostos, especialmente dos terpenos.…”

Section: Estudos De Propriedades Antitermíticas De Extratos Brutos Deunclassified

“…Diante disso, a eficiência de vários compostos vegetais há muito tem sido avaliada, visando encontrar substâncias que possam ser empregadas na formulação de produtos preservantes de madeira, que apresentem não somente a eficiência como também menor dano ao meio ambiente (Logan et al, 1990;Lajide et al, 1995;Nascimento et al, 1999Nascimento et al, , 2000Blaske & Hertel, 2001;Li et al, 2002).…”

Section: Introductionunclassified

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Estudos de propriedades antitermíticas de extratos brutos de madeira e casca de espécies florestais da Amazônia Central, Brasil

Barbosa

Nascimento²,

Morais

2007

Acta Amaz.

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RESUMONo ramo da preservação de madeira, a eficiência de compostos naturais há muito tem sido avaliada, visando encontrar substâncias que não só aumentem a vida útil de madeiras de baixa durabilidade, mas também causem menor dano ao meio ambiente. Nesse contexto, o potencial de extrativos do lenho e da casca das espécies madeireiras Pouteria guianensis, Buchenavia parviflora e Dinizia excelsa em repelir o ataque de cupins Nasutitermes sp. foi avaliado, utilizando-se como substrato a espécie Simarouba amara, de baixa durabilidade. Os extrativos foram obtidos em etanol 95%, diluídos em solução hidroalcoólica (1 e 0,1%), e impregnados em blocos de S. amara, segundo ASTM D1413-76. Os blocos foram montados em quadrado latino em uma plataforma e submetidos ao ataque dos cupins. O efeito das soluções foi classificado pela perda de peso dos blocos de S. amara. Os resultados mostraram que a maioria dos tratamentos conferiu ótima resistência à madeira de S. amara. O melhor tratamento foi aquele efetuado com extrativos da casca de P. guianensis, onde a perda foi somente de 10% do peso inicial dos blocos, enquanto que o menos efetivo foi aquele com extrativos da casca de D. excelsa, com perda de 70% de peso do bloco. Assim, pode-se concluir que os extrativos do lenho e da casca de P. guianensis e B. parviflora e do lenho de D. excelsa apresentam, a princípio, compostos com propriedades de repelência a Nasutitermes sp., e os extrativos da casca de D. excelsa não apresentam estes componentes. PALAVRAS-CHAVE

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Section: Estudos De Propriedades Antitermíticas De Extratos Brutos Deunclassified

Section: Introductionunclassified

Estudos de propriedades antitermíticas de extratos brutos de madeira e casca de espécies florestais da Amazônia Central, Brasil

Barbosa

Nascimento²,

Morais

2007

Acta Amaz.

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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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“…Li et al reported that isoflavones, favones, biflavonoids, hydrolysable tannin-related derivatives, and triterpenoids from plants showed FAS inhibitory activity in vitro. 27) We have reported that feeding of tea catechins, rich in (À)-epigallocatechin gallate and (À)-epicatechin gallate, resulted in visceral fat deposition through a reduction of hepatic FAS activity in Sprague-Dawley rats. 28) In addition, Murase et al reported that green tea extract, which contains high levels of polyphenolic compounds, increased fatty acid beta-oxidation in the liver and muscles of mice.…”

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confidence: 97%

Effect ofVaccinium ashei readeLeaves on Lipid Metabolism in Otsuka Long-Evans Tokushima Fatty Rats

Nagao

Higa

Shirouchi

et al. 2008

Bioscience, Biotechnology, and Biochemistry

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The effects of blueberry leaf (BBL) on lipid metabolism were studied in obese rats. Feeding of BBL lowered levels of serum lipids and C-reactive protein and alleviated hepatic triglyceride accumulation in the rats. The hypolipidemic effect might be attributable to a reduction of lipogenesis and enhancement of lipolysis in the liver. These results suggest the use of blueberry leaf as a dietary hypolipidemic component.Key words: Vaccinium ashei reade; blueberry leaf; lipid metabolism; Otsuka Long-Evans Tokushima Fatty ratLifestyle-related diseases, such as hyperlipidemia, arteriosclerosis, diabetes mellitus, and hypertension, are widespread and increasingly prevalent diseases in industrialized countries, and they contribute to increases in cardiovascular morbidity and mortality. 1,2) Accompanied by rapid increases in the numbers of elderly people, this is important not only medically but also socioeconomically. Although the pathogenesis of lifestyle-related diseases is complicated and the precise mechanisms have not yet been elucidated, obesity has emerged as a major cardiovascular risk factor according to epidemiologic studies. [3][4][5] Obesity is defined as an increased mass of adipose tissue, and its prevalence and severity are markedly increasing in westernized countries. Otsuka Long-Evans Tokushima Fatty (OLETF) rats develop a syndrome with multiple metabolic and hormonal disorders that shares many features with human obesity. 6-9) OLETF rats have hyperphagia because they lack receptors for cholecystokinin, and become obese, developing hyperlipidemia, fatty liver, and type-2 diabetes. In this study, we examined effects of blueberry leaf (BBL) on lipid metabolism in obese OLETF rats.Vaccinium ashei reade (blueberry) belongs to the Ericaceae plant group, and infusions of its leaf are used as a folk medicine treatment for lifestyle-related diseases in Europe. 10,11) Martineau et al. demonstrated anti-diabetic properties of the Canadian lowbush blueberry in vitro. 11) Recently, we reported that blueberry leaf revealed strong inhibitory effects on angiotensinconverting enzyme activity in vitro, and that feeding of blueberry leaf suppressed the development of essential hypertension in spontaneously hypertensive rats in vivo. 12) The effects of blueberry leaf on lipid metabolism, however, have not been fully evaluated.To determine the physiological function of BBL, we evaluated the effect of BBL feeding on hepatic enzyme activities in relation to lipid metabolism in obese OLETF rats.Four-week-old male OLETF rats were provided by the Tokusima Research Institute (Otsuka Pharmaceutical, Tokushima, Japan). The rats were housed individually in metal cages in a temperature-controlled room (24 C) under a 12-h light/dark cycle. After a 1-week adaptation period on a powder chow diet (CE-2, Clea Japan, Tokyo), they were assigned to three groups (six rats each), each fed one of three diets: (i) a semisynthetic diet containing (in weight %) casein, 20; corn oil, 7; cornstarch, 15; vitamin mixture (AIN-76Ô), 1; mineral mixture ...

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Fatty Acid Synthase Inhibitors from Plants: Isolation, Structure Elucidation, and SAR Studies

Cited by 92 publications

References 40 publications

Estudos de propriedades antitermíticas de extratos brutos de madeira e casca de espécies florestais da Amazônia Central, Brasil

Estudos de propriedades antitermíticas de extratos brutos de madeira e casca de espécies florestais da Amazônia Central, Brasil

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

Effect ofVaccinium ashei readeLeaves on Lipid Metabolism in Otsuka Long-Evans Tokushima Fatty Rats

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