Design, synthesis and anticancer activity studies of oleanolic acidderivatives targeting mTOR / 药学学报

Ten novel oleanolic acid (OA) derivatives containing urea or thiourea group were designed and synthesized, the chemical structures were confirmed by 1H NMR, 13C NMR and HR-MS. All of these compounds were evaluated for the inhibitory activity against growth of HepG2 and SGC7901 cells. The results showed that compounds I3 and II3 exhibited significant antitumor activities with IC50 of 9.4 and 5.5 μmol·L-1, respectively. Molecular docking studies showed that all these compounds exhibit inhibitory ability against mTOR kinase. Compounds I3 and II3 were further evaluated for the inhibitory activity against mTOR kinase. The results showed that I3 and II3 exhibited strong inhibitory effect on mTOR kinase with IC50 values of 0.83 and 0.26 μmol·L-1.

Design, synthesis and anti-tumor activity studies of oleanolic acid derivatives using VEGFR as target / 药学学报

In this study, twenty containing ethylenediamine groups derivatives of oleanolic acid (OA) were synthesized, their structures were determined by 1H NMR, 13C NMR and HR-MS. The anti-tumor activities in HepG2 and SGC7901 cells were evaluated by MTT assay. The results showed that all compounds exhibited anti-tumor activity, compounds I6, I8 and I9 exhibited significant anti-tumor activities with IC50 values of 16.7, 9.8 and 6.3 μmol·L-1, respectively. Molecular docking studies showed that compounds I6-I9 produce higher combining ability with VEGFR. Compound I6-I9 were further evaluated for the inhibitory activity against VEGFR-2, the result showed I9 had a strong inhibitory effect on VEGFR with IC50 values of 0.56 μmol·L-1.

Advances in study of Survivin inhibitors / 药学学报

Survivin, a member of the inhibitor of apoptosis proteins family, is considered to be an important target of anticancer treatment for its key role in the control of cell division and cell apoptosis. Currently, only a few Survivin inhibitors have been developed, and most of them reduce Survivin level by interacting with other biomolecules instead of directly interacting with Survivin protein. This review summarizes the structure of Survivin protein, the mechanism of action and research progress of Survivin inhibitors, which may has a great significance in the study of selective Survivin inhibitors in the future.

Effect of HbA1c combined FPG on screening diabetes in health check-up

OBJECTIVE@#To appraise the effectiveness of HbA(1c) and fasting plasma glucose (FPG) on screening diabetes in health check-up.@*METHODS@#A total of 1,337 individuals (male 850, female 487), aged 27 to 91 years with HbA(1c) test were included. Participates with HbA(1c) ≥6.0% or FPG≥6.1 mmol/L underwent oral glucose tolerance test (OGTT). Diabetes mellitus was diagnosed according to the criteria of WHO in 1999, FPG≥7.0 mmol/L and/or OGTT 2 h-postload plasm glucose (2 h-PG)≥11.1 mmol/L. The sensitivity and specificity of HbA(1c) thresholds and FPG or combination test on screening of diabetes were analyzed.@*RESULTS@#A total of 842 subjects had HbA(1c) <6.0%, in which 32 had isolated FPG≥6.1 mmol/L, of 495 had HbA(1c)≥6.0%. Subjects with HbA(1c)≥6.0% had significant increased disorder indexes than those with HbA(1c)<6.0%. 527 subjects who had HbA(1c)≥6.0% or FPG≥6.1 mmol/L underwent OGTT. A total of 234 subjects were newly diagnosed diabetes, including 123 (123/234, 52.56%) with FPG≥7.0 mmol/L, and 111 subjects (111/234, 47.43%) with isolated 2 h-PG≥11.1 mmol/L. Among 234 new diabetes, 91.88% (215 subjects) had HbA(1c)≥6.3%, and 77.40% (181 subjects) had HbA(1c)≥6.5%. HbA(1c)≥6.3% combined FPG ≥7.0 mmol/L increased the positive rate of newly diagnosed diabetes from 91.88% to 96.58%.@*CONCLUSIONS@#HbA(1c) is a practical and convenient tool for screening undiagnosed diabetes in routine health check-up of a large population. Combined use of HbA(1c)≥6.3% and/or FPG≥7.0 mmol/L is efficient for early detection of diabetes.