RESUMO
Two new nervogenic acid derivatives liparisnervosides Q (1) and R (5), as well as five known nervogenic acid derivatives (2-4, 6, 7) and four phenanthrenes (8-11) were isolated from the whole plant of Liparis nervosa (Thunb. ex A. Murray) Lindl.. Their structures were detremined using extensive spectroscopic techniques, including 1D, 2D NMR, and HR-ESI-MS, and acid hydrolysis. Furthermore, their antimicrobial and immunosuppressive activities were evaluated. Nervosine VII (3) exhibited antimicrobial activity against Staphylococcus aureus with an MIC of 62.5â µg/mL and inhibited the proliferation of human T cells with an IC50 value of 9.67±0.96â µM. These findings contribute to our understanding of the potential pharmacological properties of these compounds.
Assuntos
Proliferação de Células , Imunossupressores , Testes de Sensibilidade Microbiana , Fenantrenos , Staphylococcus aureus , Humanos , Imunossupressores/farmacologia , Imunossupressores/química , Imunossupressores/isolamento & purificação , Staphylococcus aureus/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Fenantrenos/farmacologia , Fenantrenos/química , Fenantrenos/isolamento & purificação , Antibacterianos/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Linfócitos T/efeitos dos fármacos , Relação Estrutura-Atividade , Estrutura Molecular , Relação Dose-Resposta a DrogaRESUMO
Investigation on the chemical components of Valeriana jatamansi Jones (Caprifoliaceae), a new lignan with pyran-ring, dipsalignan G (1), along with eight known compounds (2-9) were isolated. Their structures were elucidated by extensive analysis of 1D, 2D NMR and HR-ESI-MS spectroscopic data. Additionally, possible biosynthetic pathway of 1 was proposed. Finally, biological evaluation results showed that 8 had significant scavenging ability to ABTS and DPPH free radicals, with IC50 values of 1.35 ± 0.01 and 2.94 ± 0.01 µg/ml, respectively.
RESUMO
Lignans, with various biological activities, such as antitumor, antioxidant, antibacterial, and antiviral activities, are widely distributed in nature and mainly exist in the xylem of plants. In this paper, we summarized the structures and bioactivities of lignans reported in recent years (2019-2021) from five parts, including (1) a summary and classification of newly reported compounds; (2) the pharmacological activities of lignans; (3) molecular resources and activity distribution; (4) the structure-activity relationships; and (5) the clinical application of lignans. This review covers all undescribed compounds that were reported within the covered period of time and all bioactivity data about previously isolated lignans. The distribution of lignans in different plants and families is visualized, which improves the efficiency of searching for specific molecules. The diverse activities of different types of lignans provide an important reference for the rapid screening of these compounds. Discussion about the structure-activity relationships of lignans provides a direction for the structural modification of skeleton molecules. Combined with the clinical application of such molecules, this work will provide a valuable reference for pharmaceutical chemists.
Assuntos
Lignanas , Antioxidantes/química , Antivirais/química , Antivirais/farmacologia , Lignanas/química , Estrutura Molecular , Plantas/química , Relação Estrutura-AtividadeRESUMO
The serotonin (5-hydroxytryptamine) type 3 receptor is an important target in the control of digestive dysfunction such as anorexia and bulimia, and 5-HT3 receptor antagonists are effective against eating disorder and the early-phase chemotherapy and radiotherapy evoked vomiting. Our previous research of Valeriana jatamansi revealed the presence of iridoids, which showed potent antitumor activities. Here, we explored the effects of 10π aromatic iridoid desacylbaldrinal isolated from V. jatamansi on the 5-HT3 receptor current. We performed whole cell recordings of 5-HT3A receptor currents in the presence of the compound. The result indicated that desacylbaldrinal inhibited the 5-HT-mediated 5-HT3A receptor current.
Assuntos
Iridoides/farmacologia , Receptores 5-HT3 de Serotonina , Antagonistas do Receptor 5-HT3 de Serotonina/farmacologia , Serotonina , Valeriana/química , Humanos , Iridoides/isolamento & purificação , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Antagonistas do Receptor 5-HT3 de Serotonina/isolamento & purificaçãoRESUMO
A new abietane diterpenoid glycoside, ajugaside B (1), along with three known compounds (2-4), were isolated from the whole plants of Ajuga ovalifolia var. calantha. The structure of the new compound (1) was elucidated by means of spectroscopic analyses (HRESIMS, IR, NMR and ECD). All of the isolated compounds were evaluated for their antitumor activities against MGC803, MCF-7, A549, HT29 and HepG2 cell lines. Compounds 3-4 showed moderate cytotoxicity against all tested cell lines with IC50 values of 1.8-7.3 µM.
Assuntos
Abietanos/farmacologia , Ajuga/química , Antineoplásicos Fitogênicos/farmacologia , Abietanos/química , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Glicosídeos/química , Glicosídeos/farmacologia , Humanos , Estrutura Molecular , Extratos Vegetais/químicaRESUMO
The ethyl acetate extract from the seeds of Herpetospermum caudigerum was found to show protective effects on carbon tetrachloride (CCl(4)) and thioacetamide (TAA)-induced acute hepatic injuries in mice. From the ethyl acetate extract, two new coumarins, herpetolide A (1) and herpetolide B (2), along with four known compounds, herpetone (3), dehydrodiconiferyl alcohol (4), 2,4-dihydroxypyrimidine (5) and stigmasterol (6) were isolated. The structures of the new coumarins were elucidated on the basis of chemical and physicochemical evidences. Herpetone exhibited protective effects on CCl(4)-induced hepatocyte injury.