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1.
Altern Ther Health Med ; 30(2): 118-123, 2024 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-37820681

RESUMO

Objective: This study aimed to assess the clinical efficacy of combining multi-slice spiral CT with gastrointestinal angiography for diagnosing gastric cancer. Methods: We conducted a retrospective analysis of clinical data from 151 patients with suspected gastric cancer admitted to our hospital between January 2014 and January 2022. Among them, 70 patients underwent multi-slice spiral CT alone (control group), while the remaining 81 patients underwent multi-slice spiral CT in combination with gastrointestinal barium contrast (combination group). Finally, pathological examination confirmed gastric cancer in 81 patients. We analyzed the diagnostic efficacy of multi-slice spiral CT combined with gastrointestinal angiography for staging gastric cancer and detecting lymph node metastasis. Results: The sensitivity and accuracy of diagnosing gastric cancer using multi-slice spiral CT combined with gastrointestinal angiography were significantly superior to CT alone (P < .05). This combined approach exhibited substantial advancements in detecting stage I and II tumors compared to a single CT, although the difference in stage III detection rate was marginal (P < .05). Furthermore, among the 81 gastric cancer cases, 67 were confirmed to have lymph node metastasis through surgical and pathological examination. The lymph node detection rate with multi-slice spiral CT combined with gastrointestinal angiography was significantly higher than that achieved with single CT (P < .05). Conclusions: Combining multi-slice spiral CT with gastrointestinal angiography proved to be an effective diagnostic strategy for gastric cancer.


Assuntos
Neoplasias Gástricas , Humanos , Metástase Linfática/diagnóstico por imagem , Neoplasias Gástricas/diagnóstico por imagem , Neoplasias Gástricas/patologia , Estudos Retrospectivos , Tomografia Computadorizada Espiral , Angiografia
2.
J Med Chem ; 63(24): 15541-15563, 2020 12 24.
Artigo em Inglês | MEDLINE | ID: mdl-33264017

RESUMO

Poly (ADP-ribose) polymerase (PARP) plays a significant role in DNA repair responses; therefore, this enzyme is targeted by PARP inhibitors in cancer therapy. Here we have developed a number of fused tetra- or pentacyclic dihydrodiazepinoindolone derivatives with excellent PARP enzymatic and cellular PARylation inhibition activities. These efforts led to the identification of pamiparib (BGB-290, 139), which displays excellent PARP-1 and PARP-2 inhibition with IC50 of 1.3 and 0.9 nM, respectively. In a cellular PARylation assay, this compound inhibits PARP activity with IC50 = 0.2 nM. Cocrystal of pamiparib shows similar binding sites with PARP with other PARP inhibitors, but pamiparib is not a P-gp substrate and shows excellent drug metabolism and pharmacokinetics (DMPK) properties with significant brain penetration (17-19%, mice). The compound is currently being investigated in phase III clinical trials as a maintenance therapy in platinum-sensitive ovarian cancer and gastric cancer.


Assuntos
Fluorenos/química , Inibidores de Poli(ADP-Ribose) Polimerases/química , Poli(ADP-Ribose) Polimerases/química , Animais , Sítios de Ligação , Carbazóis/química , Carbazóis/metabolismo , Carbazóis/farmacologia , Carbazóis/uso terapêutico , Proliferação de Células/efeitos dos fármacos , Cães , Feminino , Fluorenos/metabolismo , Fluorenos/farmacologia , Fluorenos/uso terapêutico , Meia-Vida , Humanos , Indóis/química , Indóis/metabolismo , Indóis/farmacologia , Indóis/uso terapêutico , Isoenzimas/antagonistas & inibidores , Isoenzimas/metabolismo , Camundongos , Microssomos/metabolismo , Simulação de Acoplamento Molecular , Neoplasias/tratamento farmacológico , Inibidores de Poli(ADP-Ribose) Polimerases/metabolismo , Poli(ADP-Ribose) Polimerases/metabolismo , Ratos , Relação Estrutura-Atividade , Ensaios Antitumorais Modelo de Xenoenxerto
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