RESUMO
Ferulasinkins A-D (1-4), four new norlignans, were isolated from the resins of Ferula sinkiangensis, a medicinal plant of the Apiaceae family. All of them were obtained as racemic mixtures, chiral HPLC was used to produce their (+)- and (-)-antipodes. The structures of these new compounds, including their absolute configurations, were elucidated by spectroscopic and computational methods. This isolation provides new insight into the chemical profiling of F. sinkiangensis resins beyond the well-investigated structure types such as sesquiterpene coumarins and disulfides. Compounds 2a and 3a were found to significantly inhibit the invasion and migration of triple-negative breast cancer (TNBC) cell lines via CCK-8 assay. On the other hand, the wound-healing assay also demonstrated that compounds 4a and 4b could promote the proliferation of human umbilical vein endothelial cells (HUVECs). Notably, the promoting effects of 4a and 4b were observed as more significant versus a positive control using basic fibroblast growth factor (bFGF).
Assuntos
Ferula , Sesquiterpenos , Cumarínicos/química , Cumarínicos/farmacologia , Células Endoteliais , Ferula/química , Humanos , Estrutura Molecular , Resinas Vegetais , Sesquiterpenos/química , Sesquiterpenos/farmacologiaRESUMO
Two new compounds of acutacosides 1 and 2, pentasaccharide resin glycosides were isolated from the aerial parts of Argyreia acuta. The core of the two compounds was operculinic acid A, and they were esterfied at the same position, just one substituent group was linked at C-2 of Rha. The absolute configuration of the aglycone in the two compounds was established by Mosher's method, which was (11S)-hydroxyhexadecanoic acid (jalapinolic acid). Their structures were established by a combination of spectroscopic and chemical methods.
Assuntos
Convolvulaceae/química , Oligossacarídeos/química , Resinas Vegetais/química , Glicosídeos/química , Espectroscopia de Ressonância Magnética , Oligossacarídeos/isolamento & purificação , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Plantas Medicinais/químicaRESUMO
CONTEXT: Since AMP-activated protein kinase (AMPK) activation in skeletal muscle of obese rodents stimulates fatty acid oxidation, it is reasonable to hypothesize that pharmacological activation of AMPK might be of therapeutic benefit in obesity. OBJECTIVE: To investigate the effects of the traditional Korean anti-obesity drug GGEx18, a mixture of three herbs, Laminaria japonica Aresch (Laminariaceae), Rheum palmatum L. (Polygonaceae), and Ephedra sinica Stapf (Ephedraceae), on obesity and the involvement of AMPK in this process. MATERIALS AND METHODS: After high fat diet-induced obese mice were treated with GGEx18, we studied the effects of GGEx18 on body weight, fat mass, skeletal muscle lipid accumulation, and the expressions of AMPK, peroxisome proliferator-activated receptor ά (PPARα), and PPARα target genes. The effects of GGEx18 and/or the AMPK inhibitor compound C on lipid accumulation and expression of the above genes were measured in C2C12 skeletal muscle cells. RESULTS: Administration of GGEx18 to obese mice for 9 weeks significantly (p < 0.05) decreased body and adipose tissue weights compared with obese control mice (p < 0.05). Lipid accumulation in skeletal muscle was inhibited by GGEx18. GGEx18 significantly (p < 0.05) increased skeletal muscle mRNA levels of AMPKα1 and AMPKα2 as well as PPARα and its target genes. Consistent with the in vivo data, GGEx18 inhibited lipid accumulation, and similar activation of genes was observed in GGEx18-treated C2C12 cells. However, compound C inhibited these effects in C2C12 cells. DISCUSSION AND CONCLUSION: These results suggest that GGEx18 improves obesity through skeletal muscle AMPK and AMPK-stimulated expression of PPARα and its target enzymes for fatty acid oxidation.
Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Fármacos Antiobesidade/farmacologia , Ephedra sinica , Laminaria , Músculo Esquelético/efeitos dos fármacos , Obesidade/tratamento farmacológico , PPAR alfa/metabolismo , Preparações de Plantas/farmacologia , Rheum , Proteínas Quinases Ativadas por AMP/antagonistas & inibidores , Proteínas Quinases Ativadas por AMP/genética , Adiposidade/efeitos dos fármacos , Animais , Fármacos Antiobesidade/química , Linhagem Celular , Dieta Hiperlipídica , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Regulação da Expressão Gênica/efeitos dos fármacos , Metabolismo dos Lipídeos/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Músculo Esquelético/enzimologia , Obesidade/enzimologia , Obesidade/etiologia , Obesidade/genética , Obesidade/fisiopatologia , PPAR alfa/genética , Extratos Vegetais , Preparações de Plantas/química , Plantas Medicinais , Inibidores de Proteínas Quinases/farmacologia , Pirazóis/farmacologia , Pirimidinas/farmacologia , RNA Mensageiro/metabolismo , Transdução de Sinais/efeitos dos fármacos , Fatores de Tempo , Redução de Peso/efeitos dos fármacosRESUMO
Two new triterpenoids, 3-oxotirucalla-7,9(11),24-trien-21-oic acid (1) and 18Hα,3ß,20ß-ursanediol (2), along with 15 known triterpenes, α-amyrin, α-boswellic acid, ß-boswellic acid, acetyl α-boswellic acid, acetyl ß-boswellic acid, 9,11-dehydro-ß-boswellic acid, 9,11-dehydro-α-boswellic acid, acetyl 11α-methoxy-ß-boswellic acid, 11-keto-ß-boswellic acid, acetyl 11-keto-ß-boswellic acid, acetyl α-elemolic acid, 3ß-hydroxytirucalla-8,24-dien-21-oic acid, elemonic acid, 3α-hydroxytirucalla-7,24-dien-21-oic acid, and 3α-hydroxytirucall-24-en-21-oic acid, were isolated from the resin of Boswellia carterii Birdw.
Assuntos
Boswellia/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Triterpenos/isolamento & purificação , Medicamentos de Ervas Chinesas/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Resinas Vegetais/química , Estereoisomerismo , Triterpenos/químicaRESUMO
OBJECTIVE: To establish a method used for optimization of harvesting time and determine the best time for harvesting Rumex gmelini. METHOD: An HPLC method was applied to determinate the contents of seven active constituents(resveratrol, polydatin, chrysophanol 1-glucoside, nepodin, emodin, chrysophanol and physcion)of R. gmelini at different development stage. The result was analyzed by principal component analysis. RESULT: The accumulation of active constituents showed a regular pattern. CONCLUSION: The best harvesting time of R. gmelini is early July.