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1.
Sichuan Da Xue Xue Bao Yi Xue Ban ; 53(4): 676-681, 2022 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-35871740

RESUMO

Objective: To explore the application value of the "three-low" technique (low radiation dose, low contrast agent dosage and low contrast agent flow rate) combined with artificial intelligence iterative reconstruction (AIIR) in aortic CT angiography (CTA). Methods: A total of 33 patients who underwent aortic CTA were prospectively enrolled. Based on the time of their follow-up examinations, the imaging data were divided into Group A and Group B, with Group A being the control group (100 kV, 0.8 mL/kg, 5 mL/s) and Group B being the "three-low" technique group (70 kV, 0.5 mL/kg, 3 mL/s). In group A, the images were reconstructed by Karl iterative algorithm. Group B was divided into B1 and B2 subgroups, with their images being reconstructed by Karl iterative algorithm and AIIR, respectively. The CT and SD values of the ascending aorta, descending aorta, abdominal aorta, left common iliac artery and right common iliac artery were measured, and the signal-to-noise ratio (SNR) and contrast-to-noise ratio (CNR) were calculated. The subjective scoring of image quality was performed. The radiation dose parameters were documented. Results: Differences in the CT value, SD value, SNR and CNR of the three groups were statistically significant ( P<0.001). The CT value, SNR and CNR of group B2 were significantly higher than those of group B1, while the SD value of group B2 was significantly lower than that of group B1 ( P<0.017). There was no significant difference between the CT values of group A and those of group B2 ( P>0.017). The SD values, SNR and CNR in group B2 were better than those in group A ( P>0.017). There was significant difference in the subjective evaluation of image quality among the three groups ( P<0.05), but there was no significant difference between group A and group B2 ( P>0.017). The radiation dose and contrast medium dosage in group B decreased 84.14% and 37.08%, respectively, compared with those of group A. Conclusion: With the "three-low" technique combined with AIIR algorithm, the image quality of aortic CTA obtained is comparable to that of conventional dose scanning, while the radiation dose, contrast agent dosage and contrast agent flow rate of patients are significantly reduced.


Assuntos
Inteligência Artificial , Angiografia por Tomografia Computadorizada , Algoritmos , Aorta/diagnóstico por imagem , Angiografia por Tomografia Computadorizada/métodos , Meios de Contraste , Humanos , Doses de Radiação , Interpretação de Imagem Radiográfica Assistida por Computador , Tomografia Computadorizada por Raios X
2.
Anticancer Agents Med Chem ; 20(10): 1241-1249, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32116205

RESUMO

BACKGROUND: Rabdosia japonica has been historically used in China as a popular folk medicine for the treatment of cancer, hepatitis, and gastricism. Glaucocalyxin A (GLA), an ent-kaurene diterpene isolated from Rabdosia japonica, is one of the main active ingredients showing potent inhibitory effects against several types of tumor cells. To the best of our knowledge, studies regarding the structural modification and Structure- Activity Relations (SAR) of this compound have not yet been reported. OBJECTIVE: The aim of this study was to discover more potent derivatives of GLA and investigate their SAR and cytotoxicity mechanisms. METHODS: Novel 7-O- and 14-O-derivatives of GLA were synthesized by condensation of acids or acyl chloride. The anti-tumor activities of these derivatives against various human cancer cell lines were evaluated in vitro by MTT assays. Apoptosis assays of compound 17 (7,14-diacylation product) were performed on A549 and HL-60 cells by flow cytometry and TUNNEL. The acute toxicity of this compound was tested on mice, at the dose of 300mg per kg body weight. RESULTS: Seventeen novel 7-O- and 14-O-derivatives of GLA (1-17) were synthesized. These compounds showed potent cytotoxicity against the tested cancer cell lines, and almost all of them were found to be more cytotoxic than GLA and oridonin. Of the synthesized derivatives, compound 17 presented the greatest cytotoxicity, with IC50 values of 0.26µM and 1.10µM in HL-60 and CCRF-CEM cells, respectively. Furthermore, this compound induced weak apoptosis of A549 cells but showed great potential in stimulating the apoptosis of HL- 60 cells. Acute toxicity assays indicated that compound 17 is relatively safer. CONCLUSION: The results reported herein indicate that the synthesized GLA derivatives exhibited greater cytotoxicity against leukemia cells than against other types of tumors. In particular, 7,14-diacylation product of GLA was found to be an effective anti-tumor agent. However, the cytotoxicity mechanism of this product in A549 cells is expected to be different than that in other tumor cell lines. Further research is needed to confirm this hypothesis.


Assuntos
Antineoplásicos/farmacologia , Diterpenos do Tipo Caurano/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Diterpenos do Tipo Caurano/síntese química , Diterpenos do Tipo Caurano/química , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Relação Estrutura-Atividade
3.
Fitoterapia ; 118: 94-100, 2017 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-28300699

RESUMO

Two new ent-kauranoid-type diterpenoids (1 and 2) and one new rare dimer of ent-kauranoids (3) with a cyclobutane ring by a [2+2] cycloaddition, together with nine known diterpenoids (4-12) were obtained from the aerial parts of Rabdosia japonica. Their chemical structures were established by 1D and 2D NMR techniques and mass spectrometry and by comparison with spectroscopic data reported. All ent-kauranoids were test for their cytotoxic effects against A549, HCT116, CCRF-CEM and HL-60 tumor cell lines. Compounds 1, 2, 4, 5, 7, 10 and 12 showed potent and selective cytotoxicity. In addition, some selected ent-kauranoids were test for their anti-HBV activities, and the results showed compound 8 had inhibitory effect on HBsAg with a 59% inhibition ratio at the concentration of 20µg/mL.


Assuntos
Antivirais/química , Diterpenos do Tipo Caurano/química , Isodon/química , Antivirais/isolamento & purificação , Linhagem Celular Tumoral , Diterpenos do Tipo Caurano/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais , Células HL-60 , Vírus da Hepatite B/efeitos dos fármacos , Humanos , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Estrutura Molecular , Componentes Aéreos da Planta/química , Extratos Vegetais/química
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