RESUMO
Maleopimaric acid N-aryl imides (2) and methyl maleopimaric acid N-aryl imides (3) were designed and synthesized. Their atropisomers (A and B) were separated into their enantiomeric pure forms and the anti-proliferative activity was tested against NCI, A549, Hep G-2, MGC-803 and Hct-116 cell lines, respectively. A significant difference in the level of cytotoxicity was observed between R and S conformers. Atropisomers A with an R configuration exhibited significant toxicity (the IC50 values ranging from 7.51 to 32.1 µM). Further experiments proved that antitumor activity of 2A was achieved through the induction of cell apoptosis by G1 cell-cycle arrest.
Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Imidas/química , Imidas/farmacologia , Triterpenos/química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Cristalografia por Raios X , Ensaios de Seleção de Medicamentos Antitumorais , Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos , Células HCT116 , Células Hep G2 , Humanos , Imidas/síntese química , Espectroscopia de Ressonância Magnética , Conformação Molecular , EstereoisomerismoRESUMO
OBJECTIVE: To study the diagnostic value of high frequency ultrasound in diagnosing rotator cuff tears. METHODS: Total 37 patients (37 shoulders) with rotator cuff tears were detected by ultrasound, MRI examination and arthroscopy retrospectively. Among the patients,21 patients were male and 16 patients were female. The average age was 64 years old (ranged, 51 to 75 years old). High frequency ultrasonography and MRI were applied to exam the shoulder under the standardizeds to point types and compare with arthroscopy results. RESULTS: Thirty-two shoulders were diagnosed as rotator cuff injury by ultrasound, and 5 shoulders were detected as normal rotator cuff by ultrasound. Twenty-nine shoulders were diagnosed as rotator cuff injury by MRI, and 8 shoulders were detected as normal rotator cuff by MRI. Thirty-three shoulders were diagnosed as rotator cuff injury during the operation, and 4 shoulders were regarded as rotator cuff during the operation. The sensitivity of ultrasound diagnosis was 93.4% (31/33), and specific degree was 75.0%(3/4). The sensitivity of MRI diagnosis was 87.5% (28/32), and specific degree was 80.0% (4/5). CONCLUSION: High frequency ultrasound in the diagnosis of rotator cuff tears injuries has a high sensitivity and specificity. High frequency ultrasound can be used as a routine method to diagnose rotator cuff tears injuries.