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1.
Fitoterapia ; 171: 105654, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37595644

RESUMO

Nine previously undescribed clerodane-type diterpenoids (1-9), named caseabalanspenes A-I, along with six know compounds (10-15), were isolated from the twigs and leaves of Casearia velutina. Spectroscopic data (1D and 2D NMR) analysis permitted the definition of their structures and then determination of the molecular formula of the compound by high resolution mass spectrometry (HR-ESI-MS). It is worth noting that compound 7 contains N- heterocycle. Compounds 1-8 were tested the anti-inflammasome activity, and compound 3 exhibited potent activity and decreased LDH level in a dose-dependent manner, with IC50 values of 2.90 µM.


Assuntos
Antineoplásicos Fitogênicos , Casearia , Diterpenos Clerodânicos , Casearia/química , Estrutura Molecular , Ensaios de Seleção de Medicamentos Antitumorais , Folhas de Planta/química
2.
J Nat Prod ; 86(5): 1211-1221, 2023 05 26.
Artigo em Inglês | MEDLINE | ID: mdl-37079749

RESUMO

Three new rearranged diterpenoids, strophioblachins A-C (1-3), eight new diterpenoids, strophioblachins D-K (4-11), and seven previously described diterpenoids (12-18) were purified from the aerial parts of Strophioblachia fimbricalyx. Compounds 1 and 2 contain a rare 6/6/5/6 ring system, while 3 has an uncommon tricyclo[4.4.0.08,9]tridecane-bridged unit, and their diterpenoid skeletons are being reported for the first time. Utilizing spectroscopic and HRESIMS data analysis, the structures of the new compounds (1-11) were established, and ECD and 13C NMR calculations were used to confirm the relative and absolute configurations of 11 and 9. The absolute configurations of compounds 1, 3, and 10 were established using single-crystal X-ray diffraction. The results of testing for anticardiac hypertrophic activity demonstrated that compounds 10 and 15 dose-dependently lowered the mRNA expression of Nppa and Nppb. Protein levels were confirmed by Western blotting, which also demonstrated that compounds 10 and 15 lowered the expression of the hypertrophic marker ANP. The cytotoxic activity against neonatal rat cardiomyocytes was assayed in vitro by the CCK-8 and ELISA methods, and the results showed that compounds 10 and 15 were only very weakly active in the range.


Assuntos
Diterpenos , Euphorbiaceae , Ratos , Animais , Diterpenos/farmacologia , Diterpenos/química , Euphorbiaceae/química , Espectroscopia de Ressonância Magnética , Cristalografia por Raios X , Estrutura Molecular
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