New antitumor principles, casearins A-F, for Casearia sylvestris Sw. (Flacourtiaceae).

Itokawa, Hideji; Totsuka, Nobuo; Morita, Hiroshi; Takeya, Koichi; Iitaka, Yōichi; Schenkel, Eloir Paulo; Motidome, Mário

doi:10.1248/cpb.38.3384

Cited by 88 publications

(122 citation statements)

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“…In view of the fact that the water extract was more efficient in neutralizing hemorrhagic metalloproteinases Carvalho et al 1998, Itokawa et al 1990, Morita et al 1991, Oberlies et al 2002, Wang et al 2009, Ferreira et al 2010, Santos et al 2010 from bothropic venoms than neutralize serina-proteases, it is proposed that this extract may act as a metal natural chelating (Borges et al 2001). Other possibility would be linkage of the active compound, present in the extract, to the enzyme catalytic site which could avoid coupling of the substrate to the enzyme in a covalent or non-covalent interaction way.…”

Section: Anti-ophidian Activitymentioning

confidence: 99%

“…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%

“…The main structural difference among these six diterpenes is the presence of a casearin C decanoate substituent at C-7 (Fig. 1), which could explain its higher cytotoxicity on V-79 cells (Itokawa et al 1990) likely based on its remarkably larger hydrophobicity and facility to penetrate cytoplasm membrane cell.…”

Section: Antitumor Activitymentioning

confidence: 99%

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Folk uses and pharmacological properties of Casearia sylvestris: a medicinal review

Ferreira

Costa-Lotufo

Moraes

et al. 2011

An. Acad. Bras. Ciênc.

105

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Folk uses and scientific investigations have highlighted the importance of Casearia sylvestris extracts and their relevant bioactive potential. The aim of this work was to review the pharmacological properties of C. sylvestris, emphasizing its anti-ulcer, anti-inflammatory, anti-ophidian and antitumor potentialities. Ethanolic extracts and essential oil of their leaves have antiulcerogenic activity and reduce gastric volume without altering the stomach pH, which corroborates their consumption on gastrointestinal disorders. Leaf water extracts show phospholipase A 2 inhibitory activity that prevents damage effects on the muscular tissue after toxin inoculation. This antiphospholipasic action is probably related to the use as an anti-inflammatory, proposing a pharmacological blockage similar to that obtained with non-steroidal anti-inflammatory drugs on arachidonic acid and cyclooxygenase pathways. Bioguided-assay fractionations lead to the identification of secondary metabolites, especially the clerodane diterpenes casearins (A-X) and casearvestrins (A-C), compounds with a remarkable cytotoxic and antitumor action. Therefore, the C. sylvestris shrub holds a known worldwide pharmacological arsenal by its extensive folk utilization, exciting searches for new molecules and a better comprehension about biological properties.

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Section: Anti-ophidian Activitymentioning

confidence: 99%

Section: Antitumor Activitymentioning

confidence: 99%

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Folk uses and pharmacological properties of Casearia sylvestris: a medicinal review

Ferreira

Costa-Lotufo

Moraes

et al. 2011

An. Acad. Bras. Ciênc.

105

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“…The screening of medicinal plants presents an avenue for the discovery of new drugs (Ribnicky et al, 2008). Phytochemical screening of Casearia sylvestris revealed the presence of diterpenes, triterpenes, flavonoids, caproic and ellagic acids (Basile et al, 1990;Itokawa et al, 1990;de Carvalho et al, 1998;Borges et al, 2000).…”

Section: Introductionmentioning

confidence: 99%

Ethanolic extract of Casearia sylvestris Sw exhibitsin vitro antioxidant and antimicrobial activities andin vivo hypolipidemic effect in rats

Espinosa

Souza

Casali

2015

Rev. bras. plantas med.

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ABSTRACT:The Casearia sylvestris Sw (Flacourtiaceae) is a shrub that occurs in forests of Southern Brazil; its leaves are widely used in folk medicine as a depurative, analgesic, anti-inflammatory and antiulcerogenic agent. The objective of this study was to perform the phytochemical description and to evaluate the pharmacological activities (antimicrobial, antifungal, antioxidant and toxicity) of the ethanolic extract (EE) of C. sylvestris Sw. In addition, we also evaluated the effect of the EE of C. sylvestris Sw on the glucose levels and lipid profile in blood serum of rats submitted to a model of streptozotocin-induced diabetes. Material and Methods: In vitro assay: the detection of chemical groups was done through chemical reactions with the development of color or precipitate and by chromatographic profile; the antioxidant activity was measured by the method of reduction of DPPH free radical (2,2-diphenyl-1-picrylhydrazyl); the Minimum Inhibitory Concentration was evaluated by the broth microdilution method, and the Minimum Bactericide Concentration and the Minimum Fungicide Concentration were performed in Petri dishes; the cytotoxic activity was measured by the Artemia salina test. In vivo assay: diabetic and non-diabetic rats were treated with EE of C. sylvestris Sw (300 mg/ kg) for 45 days, and the glycaemia and lipid profile were analyzed. Results: The EE showed a Lethal Dose 50 of 724.76 µg.mL -1 and important antioxidant, fungicide and fungistatic activities. The EE showed better antimicrobial activity regarding the microorganisms Staphylococcus aureus, Escherichia coli and Salmonella setubal. Conclusion: The EE of C. sylvestris Sw produces a significant decrease in triglycerides, total cholesterol and VLDL levels without any significant alteration in the glycaemia. The EE of C. sylvestris Sw presents antioxidant and antimicrobial activities and it exhibits a potent hypolipidemic effect.Keywords: antioxidant activity, antimicrobial activity, diabetes, glycaemia, lipid profile. RESUMO: Extrato etanólico de Casearia sylvestris Sw apresenta atividade antioxidante e antimicrobiana in vitro e efeito hipolipemiante em ratos. Casearia sylvestris Sw(Flacourtiaceae) é uma planta comumente encontrada em florestas do sul do Brasil; suas folhas são amplamente utilizadas na medicina popular como depurativa, analgésica, anti-inflamatória e anti ulcerogênica. O objetivo deste estudo foi apresentar uma descrição fitoquímica e da atividade farmacológica (antimicrobiana, antifúngica, antioxidante e toxicidade) do extrato etanólico (EE) da C. Sylvestris Sw. Adicionalmente, procurou-se avaliar o efeito do EE da C. Sylvestris Sw sobre os níveis séricos de glicose e perfil lipídico de ratos submetidos a um modelo de diabetes induzida por estreptozotocina. A detecção de grupos químicos foi realizada por reações químicas de coloração ou precipitação, e também por cromatografia; a atividade antioxidante foi mensurada pelo método de redução do DPPH (2,2-difenil-1-picril-hidrazil); a concentração mínima inibitória foi realizad...

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“…Studies on C. sylvestris extract have confirmed its antiulcerogenic, 65 anti-inflammatory, 66 antimicrobial, antivenom, 67 and cytotoxic activities. 68,69 Moreover, no significant toxicological effects have been observed after oral administration of ethanolic extracts of C. sylvestris leaves to animals. 70 Additionally, no genotoxicity was detected when the extracts were assayed against hepatoma tissue and lung fibroblast V-79 cell cultures.…”

Section: Brazilian Biodiversity: An Unknown Potential Source For Drugmentioning

confidence: 99%

Tropical biodiversity: has it been a potential source of secondary metabolites useful for medicinal chemistry?

Valli¹,

Pivatto²,

Danuello³

et al. 2012

Quím. Nova

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Recebido em 22/5/12; aceito em 19/7/12; publicado na web em 26/10/12The use of natural products has definitely been the most successful strategy in the discovery of novel medicines. Secondary metabolites from terrestrial and marine organisms have found considerable use in the treatment of numerous diseases and have been considered lead molecules both in their natural form and as templates for medicinal chemistry. This paper seeks to show the great value of secondary metabolites and emphasize the rich chemical diversity of Brazilian biodiversity. This natural chemical library remains understudied, but can be a useful source of new secondary metabolites with potential application as templates for drug discovery.

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New antitumor principles, casearins A-F, for Casearia sylvestris Sw. (Flacourtiaceae).

Cited by 88 publications

References 0 publications

Folk uses and pharmacological properties of Casearia sylvestris: a medicinal review

Folk uses and pharmacological properties of Casearia sylvestris: a medicinal review

Ethanolic extract of Casearia sylvestris Sw exhibitsin vitro antioxidant and antimicrobial activities andin vivo hypolipidemic effect in rats

Tropical biodiversity: has it been a potential source of secondary metabolites useful for medicinal chemistry?

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