2004
DOI: 10.1055/s-2004-832655
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Trypanocidal Activity of a New Diterpene fromCasearia sylvestrisvar.lingua

Abstract: Bioassay-guided fractionation of the hexanic root bark extract of Casearia sylvestris var. lingua led to the isolation of a new clerodane diterpene, whose structure was elucidated as rel-(2 S,5 R,6 R,8 S,9 S,10 R,18 S,19 R)-19-acetoxy-18,19-epoxy-6-hydroxy-18-butanoyloxy-2-(2-methylbutanoyloxy)cleroda-3,13(16), 14-triene by spectroscopic means, including 1D and 2D NMR analyses. This compound showed pronounced activity on Trypanosoma cruzi, the casual agent of Chagas' disease, with minimal inhibitory concentrat… Show more

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Cited by 60 publications
(60 citation statements)
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“…Twenty eight clerodane diterpenes typical of Casearia were isolated from C. sylvestris: casearins A-X (Carvalho et al 1998, Itokawa et al 1990, Morita et al 1991, Wang et al 2009, Santos et al 2010 and caseargrewiin F (Santos et al 2010), isolated from leaves; casearvestrins A-C, isolated from leaves and branches (Oberlies et al 2002);and rel-19S-acetoxy-18R-butanoyloxy-18,19-epoxy-6S-hidroxy-2R-(2-methylbutanoyloxy) -5S, 8R, 9R, 10S-cleroda-3,13(16),14-triene, isolated from roots (Espíndola et al 2004) (Fig. 1).…”
Section: Antitumor Activitymentioning
confidence: 99%
See 1 more Smart Citation
“…Twenty eight clerodane diterpenes typical of Casearia were isolated from C. sylvestris: casearins A-X (Carvalho et al 1998, Itokawa et al 1990, Morita et al 1991, Wang et al 2009, Santos et al 2010 and caseargrewiin F (Santos et al 2010), isolated from leaves; casearvestrins A-C, isolated from leaves and branches (Oberlies et al 2002);and rel-19S-acetoxy-18R-butanoyloxy-18,19-epoxy-6S-hidroxy-2R-(2-methylbutanoyloxy) -5S, 8R, 9R, 10S-cleroda-3,13(16),14-triene, isolated from roots (Espíndola et al 2004) (Fig. 1).…”
Section: Antitumor Activitymentioning
confidence: 99%
“…Besides this antitumor potentiality, different parts of the plant also exhibit activity against Leishmania donovani promastigotes (Mesquita et al 2005), Trypanosoma cruzi amastigotes (Espíndola et al 2004, Mesquita et al 2005, Plasmodium falciparum strains resistant to chloroquine (Mesquita et al 2007) and Aedes aegypti larvae (Rodrigues et al 2006). Leaf methanolic extract shows anti-hyperlipidemic properties, decreasing serum triglycerides and lipases (Schoenfelder et al 2008) and the water extract displays neuromodulatory effects on central nervous system by the interference on enzymatic action of the purinergic and cholinergic systems since it inhibits Na + -/K + /ATPase and 5 -nucleotidase activities (Silva et al 2006).…”
Section: Antitumor Activitymentioning
confidence: 99%
“…Para ação antilarvativa foi realizado o extrato hexânico e etanólico, sendo testados in vitro, em doses de 500 ìg/mL, apresentando atividade larvativa contra Aedes aegypti (Rodrigues et al, 2006). Para ação antiprotozoária foi analisado o extrato hexânico da casca da raiz, sendo testado in vitro, em doses de 0,1 a 4,9 ìg/mL, apresentando atividade contra Trypanosoma cruzi (doença de Chagas) (Mesquita et al,2005;Espindola et al, 2004).…”
Section: Rodrigues Etunclassified
“…At least 16 Casearia species have shown biological activity such as cytotoxic [C. arborea; C. grayi; C. grewiifolia; C. lucida; C. multinervosa; C. nigrescens; C. obliqua (2)(3)(4)(5)(6)(7)(8)]; antifungal [C. decandra (9)]; antidiabetic [C. esculenta (10)]; immunomodulatory [C. guianensis (11)]; antifertility [C. ilicifolia (12)]; antiophidian [C. mariquitensis (13)]; antitumor [C. membranacea (14)]; genotoxic [C. tomentosa (15)]; and antioxidant actions [C. velutina (16)]. The most studied among them is Casearia sylvestris Sw. that has shown several biological activities, including antitumor, antiulcer, analgesic, anti-inflammatory, cytotoxic, antifungal, anticancer, anti-snake and bee venom PLA 2 , genotoxic, trypanocidal, enzyme inhibitory, antihyperlipidemic and antibothropic properties (17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27). The latter have been used as antivenom in folk medicine by isolated Brazilian communities (22).…”
Section: Introductionmentioning
confidence: 99%