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1.
Chem Biodivers ; 18(10): e2100401, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34415099

RESUMO

A new menthane-type monoterpene, alpigalanol (1), together with four known terpenes (2-5) were isolated from the ethyl acetate soluble fraction of the 70 % ethanol extract of the Alpinia galanga rhizomes. The structure of 1 was determined by spectroscopic analyses, including 1D- and 2D-NMR. The extract of the A. galanga rhizomes and all isolated compounds (1-5) possessed Vpr inhibitory activities against the TREx-HeLa-Vpr cells at a concentration of 1.25 µM without showing any cytotoxicity.


Assuntos
Alpinia/química , Produtos do Gene vpr/antagonistas & inibidores , Monoterpenos/farmacologia , Rizoma/química , Teoria da Densidade Funcional , Relação Dose-Resposta a Droga , Células HeLa , Humanos , Conformação Molecular , Monoterpenos/química , Monoterpenos/isolamento & purificação , Células Tumorais Cultivadas
2.
Bioorg Med Chem Lett ; 30(2): 126841, 2020 01 15.
Artigo em Inglês | MEDLINE | ID: mdl-31836445

RESUMO

Inflammation is an extensively recognized link to many pathological diseases. It is a host response for protection from infections and tissue damage. Infections trigger acute inflammation; however, persistent infection will contribute to chronic inflammation and higher disease susceptibility. Deregulated inflammatory responses can cause excessive or long-lasting tissue damage, manifested as cancer, immune disorders, diabetes, etc. NF-κB is a central mediator of pro-inflammatory gene induction and functions in both innate and adaptive immune cells; therefore, the anti-inflammatory regulation of NF-κB is needed. Natural products reportedly play an important role in controlling the inflammatory response pathways. However, the anti-inflammatory activities of isopimara-8-(14),15-diene diterpenoids have not yet been fully elucidated. To elucidate the anti-inflammatory activities of the isopimara-8(14),15-diene diterpenoids, we investigated 21 isopimara-8(14),15-diene diterpenoids previously isolated from Kaempferia pulchra rhizomes. Eleven compounds exhibited NO inhibitory activity against lipopolysaccharide (LPS)-induced RAW264.7 cells, with IC50 values ranging from 30 to 100 µM. Furthermore, the most potent kaempulchraols P and Q, with IC50 values of 39.88 and 36.05 µM, respectively, inhibited the NF-κB-mediated transactivation of a luciferase reporter gene, IL-6 production, and COX-2 expression, with an effective dose of 25 µM. These findings provide new insights into the anti-inflammatory activities of the isopimara-8(14),15-diene diterpenoids.


Assuntos
Anti-Inflamatórios/uso terapêutico , Diterpenos/uso terapêutico , Inflamação/tratamento farmacológico , Rizoma/química , Anti-Inflamatórios/farmacologia , Diterpenos/farmacologia , Humanos
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