Author(s):
Oda, Fernando Bombarda [UNESP] ; Crevelin, Eduardo José ; Crotti, Antônio Eduardo Miller ; Orlando, Allan Botinhon [UNESP] ; de Medeiros, Alexandra Ivo [UNESP] ; Nogueira, Flávia Aparecida Resende ; dos Santos, André Gonzaga [UNESP]
Date: 2019
Persistent ID: http://hdl.handle.net/11449/189247
Origin: Oasisbr
Subject(s): Casearia sylvestris; Clerodane diterpene; Cytotoxicity; Nitric oxide inhibition; S9 rat liver fraction; Simulated gastric fluid; Casearia sylvestris; Casearia sylvestris; Clerodane diterpene; Clerodane diterpene; Cytotoxicity; Cytotoxicity; Nitric oxide inhibition; Nitric oxide inhibition; S9 rat liver fraction; S9 rat liver fraction; Simulated gastric fluid; Simulated gastric fluid
Description
Made available in DSpace on 2019-10-06T16:34:41Z (GMT). No. of bitstreams: 0 Previous issue date: 2019-09-01
Clerodane diterpenes from Casearia sylvestris are antiulcerogenic and anti-inflammatory. The finding that they may undergo acid degradation or hepatic metabolization led to an investigation of their degradation products. Purified clerodane diterpenes (casearins J and O) were subjected to in vitro assays to simulate their oral administration. Resulting derivatives were identified using chromatographic and spectrometric techniques. Nitric oxide synthesis by LPS-stimulated macrophages was assayed to verify whether structural modifications alter the anti-inflammatory activity of diterpenes. Nine compounds (1–9) were identified after acid degradation remaining 5.05% of casearin J. Besides the remaining casearin O (13.1%), eight compounds (10–17) were identified. The dialdehydes from each casearin were the major constituents. S9 rat liver treatment of casearins J and O generated two compounds identical to some of those produced by acid degradation, which remained 36.8% and 36.5% intact, respectively. Both casearins and its derivatives were not cytotoxicity at concentrations lower than 0.312 μg/mL (0.555 μM for casearin J and 0.516 μM for casearin O) and did not inhibit the nitric oxide production in this concentration. Thus, the structural modifications conducted did not alter the activity of casearins and the anti-inflammatory pathway of diterpenes probably is not involved on nitric oxide modulation.
São Paulo State University (Unesp) School of Pharmaceutical Sciences Department of Natural Principles and Toxicology
University of São Paulo (USP) Faculty of Philosophy Sciences and Letters Department of Chemistry
São Paulo State University (Unesp) School of Pharmaceutical Sciences Department of Biological Sciences
University of Araraquara Department of Health and Biological Sciences
São Paulo State University (Unesp) School of Pharmaceutical Sciences Department of Natural Principles and Toxicology
São Paulo State University (Unesp) School of Pharmaceutical Sciences Department of Biological Sciences
