Casearin X,Its Degradation Product and Other Clerodane Diterpenes from Leaves of Casearia sylvestris: Evaluation of Cytotoxicity against Normal and Tumor Human Cells |
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| Authors: | André Gonzaga dos Santos Paulo Michel Pinheiro Ferreira Gerardo Magela Vieira Júnior Carla Cristina Perez Aristeu Gomes Tininis Geraldo Humberto Silva Vanderlan da Silva Bolzani Letícia Veras Costa‐Lotufo Cláudia do Ó Pessoa Alberto José Cavalheiro |
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| Affiliation: | 1. Núcleo de Bioensaios, Biossíntese e Ecofisiologia de Produtos Naturais, Instituto de Química, S?o Paulo State University, CP 355, 14800‐900, Araraquara‐SP, Brazil, (phone: +55‐16‐33016667;2. fax: +55‐16‐33016692);3. Centro de Ciências da Saúde, Campus Senador Helvídio Nunes de Barros (CSHNB), Universidade Federal do Piauí, 64600‐000, Picos‐PI, Brazil;4. Departamento de Fisiologia e Farmacologia, Faculdade de Medicina, Universidade Federal do Ceará, CP 3157, 60430‐270, Fortaleza‐CE, Brazil |
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| Abstract: | An EtOH extract of the leaves of Casearia sylvestris afforded new clerodane diterpene, casearin X, together with the known compounds casearins B, D, L, and O, and caseargrewiin F. Casearin X degraded to the corresponding dialdehyde when stored in CDCl3. The diterpenes isolated were cytotoxic to human cancer cell lines, with caseargrewiin F being the most active and the new clerodane, casearin X, the second active compound with IC50 values comparable to the positive control doxorubicin. All isolated diterpenes showed lower activities against normal human cells than against cancer cell lines, which might indicate a possible selective action on cancer cells. Casearin X dialdehyde was not cytotoxic to cancer cells indicating that the occurrence of these CO groups at C(18) and C(19) is incompatible with the cytotoxic activity. |
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| Keywords: | Casearia sylvestris Clerodane diterpene Casearin X Cytotoxic activity Antitumor activity |
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