ABSTRACT
Three new phenylacetamide glycosides (1-3) together with one known phenylacetamide glycoside (4) and two known flavonoid glycosides (5-6) were isolated from whole plants of Dracocephalum tanguticum. The structure of all compounds were elucidated based on spectroscopic data analysis and comparison with data reported in related literature. Compounds (1-3) were evaluated for their anti-hyperglycemic and anti-fungal (Candida albicans) activities, the results revealed that all of them showed moderate activity with 3T3-L1 adipocytes glucose consumption rate of 20.80 ± 1.47%, 21.48 ± 2.44%, and 21.57 ± 1.35%, respectively at the final concentration of 25 µM. However, none of them showed obvious Candida albicans inhibitory activity.
Subject(s)
Antifungal Agents/isolation & purification , Glycosides/pharmacology , Hypoglycemic Agents/isolation & purification , Lamiaceae/chemistry , Animals , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Candida albicans/drug effects , Cell Line , Flavonoids/chemistry , Flavonoids/isolation & purification , Flavonoids/pharmacology , Glucose/pharmacokinetics , Glycosides/chemistry , Glycosides/isolation & purification , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/pharmacology , Mice , Molecular Structure , Spectrum AnalysisABSTRACT
Two new xanthone glycosides (1-2), together with seven known analogues (3-9), were isolated from whole herb of Swertia punicea. The structures of these metabolites were established on the basis of detailed spectroscopic analysis and comparison with data reported in the literature. In an in vitro test, all isolates were evaluated for their anti-inflammatory activity. The results revealed that all of them showed significant anti-inflammatory activity with IC50 values ranging from 1.237 to 3.319 mM. Compounds 3, 4, and 5 (IC50 values in the range 1.237-1.987 mM) displayed more potent anti-inflammatory activity than the positive control, indomethacin (IC50 value of 2.004 mM).
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Swertia/chemistry , Xanthones/chemistry , Animals , Drug Evaluation, Preclinical , Drugs, Chinese Herbal/chemistry , Glycosides/chemistry , Magnetic Resonance Spectroscopy , Mice , Molecular Structure , RAW 264.7 CellsABSTRACT
Cytosine5-hyxymethylation (5hmC)which is a new epigenetic modification form plays important roles in the development and progression of tumors. In the present study, we observed that levels of 5hmC in the promoter region of Von Hippel-Lindau (VHL) were lower in 97 samples of renal clear cell carcinoma tissue than in matched adjacent benign tissues. Moreover, when the cancer tissue samples were divided based on pathological staging, VHL expression and the level of 5hmC in the VHL promoter were both lower in pathological grade III tumors than in grades I or II. Correspondingly, expression of TET1, which catalyzes the formation of 5hmC, was also lower in grade III renal clear cell carcinomas than in grade I or II disease. These findings suggest the 5hmC level on VHL is a key determinant of the gene's expression and may participate in the occurrence and development of renal clear cell carcinoma. Thus the 5hmC level may be a useful indicator for early diagnosis and appropriate treatment of renal clear cell carcinoma.
