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1.
J Nat Prod ; 81(5): 1209-1218, 2018 05 25.
Artigo em Inglês | MEDLINE | ID: mdl-29667820

RESUMO

The phytochemical study of Euphorbia resinifera afforded 18 structurally diverse diterpenoids, including 14 new ingol-type diterpenoids, euphorblins A-N (1-14), a new rhamnofolane diterpenoid, euphorblin O (15), and three known analogues (16-18). The structures of these compounds were deduced using 2D NMR spectroscopy and NOE experiments. The structure of compound 1 was confirmed by single-crystal X-ray crystallography. The abilities of the compounds to enhance lysosomal biosynthesis were evaluated through LysoTracker Red staining. Among the 10 active compounds, compounds 2, 4, and 18 showed remarkable immunofluorescence strength, and their LysoTracker staining intensities were 155.9%, 143.5%, and 140.7%, respectively, greater than that of the control. A series of lysosomal genes were also found to be upregulated by these compounds, which further confirms their ability to induce lysosome biosynthesis and suggests that these diterpenoids have potential as lead compounds for the development of drugs for the treatment of lysosome-related diseases.


Assuntos
Diterpenos/química , Diterpenos/farmacologia , Euphorbia/química , Lisossomos/efeitos dos fármacos , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Cristalografia por Raios X/métodos , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Células HeLa , Humanos , Espectroscopia de Ressonância Magnética/métodos , Ressonância Magnética Nuclear Biomolecular/métodos
2.
Nat Prod Res ; 31(21): 2531-2536, 2017 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-28475376

RESUMO

Two new kaurane-type diterpenoids, 3α-(angeloyloxy)-17-hydroxy-ent-kaur-15-en-19-oic acid (1) and 3α-(tigloyloxy)-17-hydroxy-ent-kaur-15-en-19-oic acid (2), along with 10 known compounds (3-12) were isolated from the whole plant of Wedelia chinensis (Osbeck.) Merr. Their structures were elucidated on the basis of extensive spectroscopic analyses (UV, IR, MS and NMR) and comparison with literature data. Compounds 3 and 4 showed moderate inhibitory activity against the Staphylococcus aureus subsp. aureus ATCC29213 with MIC50 19.35 and 18.31 µg/mL, respectively.


Assuntos
Antibacterianos/farmacologia , Diterpenos do Tipo Caurano/química , Diterpenos do Tipo Caurano/farmacologia , Wedelia/química , Antibacterianos/química , Diterpenos , Avaliação Pré-Clínica de Medicamentos/métodos , Escherichia coli/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Pseudomonas aeruginosa/efeitos dos fármacos , Salmonella enterica/efeitos dos fármacos , Espectrofotometria Ultravioleta , Staphylococcus aureus/efeitos dos fármacos
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