RESUMO
Three phenylpropanoid glucosides (1: â-â3: ) and one iridoid glucoside (11: ), together with eleven known glucosides, were isolated from the ethanol extract of the whole plant of Hemiphragma heterophyllum. Their structures were elucidated by means of 1D and 2D NMR spectroscopy, HRMS, and chemical methods. All compounds except 11: and 13: â-â15: showed varying degrees of α-glucosidase inhibitory activity. Compounds 5, 9: , and 12: were marginally active in the bioassay, while compounds 1: â-â4: , 6: â-â8: , and 10: exhibited appreciable inhibitory activity with an IC50 value of 33.6 ~ 83.1 µM, which was much lower than that of the positive control acarbose (IC50 = 310.8 µM).
Assuntos
Glucosídeos Iridoides , alfa-Glucosidases , Glucosídeos , Inibidores de Glicosídeo Hidrolases , Iridoides , Estrutura Molecular , Extratos VegetaisRESUMO
A pilot study on the ethanol extracts of Agrimonia pilosa found to have anti-α-glucosidase and anti-inflammatory activities. Subsequent chemical study afforded a new phenylethyl isocoumarin glycoside (1) and eight known compounds (2-9). The structure of 1 was elucidated by comprehensive spectroscopic analysis and chemical transformations. All compounds showed modest α-glucosidase inhibitory activity (IC50 values ranging from 36.8 to 210.7 µM), which was lower than that of the positive control acarbose (IC50=301.9 µM). Those compounds except inactive compounds 3 and 6 showed weak anti-inflammatory activity.[Formula: see text].
Assuntos
Agrimonia , Inibidores de Glicosídeo Hidrolases/farmacologia , Glicosídeos , Projetos Piloto , Extratos Vegetais/farmacologia , alfa-GlucosidasesRESUMO
Phytochemical study on the 95% ethyl alcohol extract of stems of Chenopodium ambrosioides resulted in the isolation of two new polyol monoterpenes, 4-hydroxy-4(α or ß)-isopropyl-2-methyl-2-cyclohexen-1-one (1) and 1-methyl-4ß- isopropyl-1-cyclohexene-4α,5α,6α-triol (2), together with five known compounds, (1S,2S,3R,4S)-1-methyl-4-(propan-2-yl)cyclohexane-1,2,3,4-tetrol (3), (1R,2S,3S,4S)- 1,2,3,4-tetrahydroxy-p-menthane (4), (1R,2S)-3-p-menthen-1,2-diol (5), (1R,4S)-p- menth-2-en-1-ol (6) and 1,4-dihydroxy-p-menth-2-ene (7). The structures of the new compounds were established on the basis of detailed spectroscopic evidence including extensive 1D and 2D NMR techniques. Compounds 1-7 were evaluated for their anti-inflammatory activity, and compound 1 showed moderate ability to inhibit NO production of LPS-stimulated RAW 264.7 macrophages with an IC50 value of 16.83 µM.
Assuntos
Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Chenopodium ambrosioides/química , Monoterpenos/isolamento & purificação , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Linhagem Celular , Avaliação Pré-Clínica de Medicamentos/métodos , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Espectroscopia de Ressonância Magnética , Camundongos , Estrutura Molecular , Monoterpenos/química , Monoterpenos/farmacologia , Caules de Planta/química , Polímeros/químicaRESUMO
AIM: To obtain fetal mesenchymal stem cells isolated from human placental tissue (hfPMSCs) and study the effects of IFN-γ on immunomodulatory property of hfPMSCs in vitro. METHODS: hfPMSCs were isolated from the fetal side of human placentas by enzyme digestion. Expressions of cell surface antigens CD73, CD90, CD105, CD14, CD34, CD45 and HLA-DR were tested by flow cytometry. The fetal origin of the placental cells was verified by DNA identity test using four known short tandem repeat (STR) polymorphic markers D2S1399, D10S2325, D18S535 and GATA198B05. After hfPMSCs were treated with 10 ng/mL IFN-γ, the expressions of IL-6, IL-8, IL-10 and HGF at both mRNA and protein levels were measured using quantitative real-time PCR (q-PCR) and ELISA. The expressions in controls without IFN-γ treatment were examined in the same way. RESULTS: The isolated cells expressed MSCs surface markers CD73, CD90 and CD105, but did not express CD14, CD34, CD45 and HLA-DR. For all the STR markers tested, the MSCs from the fetal side of the placenta carried the alleles of both maternal and paternal origin, indicative of the fetal genome. q-PCR indicated that the expression of IL6 mRNA in IFN-γ treated group was significantly higher than those in the control group (P<0.05), whereas the levels of IL-10 and HGF mRNA were down-regulated by IFN-γ treatment (P<0.05). ELISA revealed that IFN-γ treated group expressed strikingly the higher level of IL-6 protein compared with the control group (P<0.05), and the lower levels of IL-8, IL-10 and HGF (P<0.05). CONCLUSION: The method used in the study can obtain hfPMSCs from human placenta tissues, and IFN-γ has a negative effect on immune suppression function of the hfPMSCs.