ABSTRACT
A series of novel 1,3,4-oxadiazole-artemisinin hybrids have been designed and synthesized. An MTT assay revealed that most of tested hybrids showed more enhanced anti-proliferative activities than artemisinin, among which A8 had the superior potency with IC50 values ranging from 4.07 µM to 9.71 µM against five tested cancer cell lines. Cell colony formation assays showed that A8 could inhibit significantly more cell proliferation than artemisinin and 5-fluorouracil. Further mechanism studies reveal that A8 induces apoptosis and ferroptosis in MCF-7 cells in a dose-dependent manner, and CYPs inhibition assays reveal that A8 has a moderate inhibitory effect on CYP1A2 and CYP3A4 in the human body at 10 µM. The present work indicates that hybrid A8 may merit further investigation as a potential therapeutic agent.
Subject(s)
Antineoplastic Agents , Artemisinins , Ferroptosis , Humans , MCF-7 Cells , Molecular Structure , Antineoplastic Agents/pharmacology , Drug Screening Assays, Antitumor , Apoptosis , Artemisinins/pharmacology , Cell Proliferation , Structure-Activity Relationship , Cell Line, TumorABSTRACT
Echinococcus infection in elderly population (60-87 years old) was investigated by serological assay, medical imaging and epidemiology history in August, 2008. A total of 234 subjects from different nationalities were examined. Seven cases were serologically positive for echinococcosis and confirmed by medical imaging. Out of 30 suspected sera-positive cases, 3 were positive by medical imaging. There were 10 confirmed echinococcosis cases with a positive rate of 4.3%. There was significant difference on the prevalence among different towns (P < 0.05), but no significant statistical difference on the prevalence among nationalities, careers and sex. The prevalence in females (4.8%) was higher than that of males (3.6%).