Details

Autor(en) / Beteiligte

• Liu, Yong-Ping
• Lei, Jian
• Tang, Li-Wen
• Peng, Yao
• Au, Chak-Tong
• Chen, Yi
• Yin, Shuang-Feng

Titel

Studies on the cytotoxicity and anticancer performance of heterocyclic hypervalent organobismuth(III) compounds

Ist Teil von

• European journal of medicinal chemistry, 2017-10, Vol.139, p.826-835

Ort / Verlag

France: Elsevier Masson SAS

Erscheinungsjahr

2017

Quelle

Access via ScienceDirect (Elsevier)

Beschreibungen/Notizen

• Novel organobismuth(III) complex of 5H-dibenzo[c,f][1,5]oxabismocin-12(7H)-yl nitrate (C2) was synthesized and characterized by spectral and elemental analysis. It was compared with other five C,E,C-chelating (E = N, O, S) organobismuth(III) complexes against human adenocarcinoma alveolar basal epithelial cells (A549), human liver cancer cell line (SMCC7721), human gastric cancer cell line (SGC-7901), human colon adenocarcinoma cell line (SW480) and healthy human bronchial cell line (16HBE14o-) in vitro. It was found that C2 exhibited the best anticancer activity. Further mechanistic investigation indicated that toxicological activity of C2 was ascribable to apoptosis rather than anti-proliferative activity. Apoptosis was induced through up-regulating the level of Bcl-2/Bax as well as the activation of caspase-3. The results demonstrate that heterocyclic organobismuth(III) complexes of this type have great potential in the treatment of cancer. [Display omitted] •Novel 5H-dibenzo[c,f][1,5] oxabismocin-12(7H)-yl nitrate was synthesized.•It showed the highest potent cytotoxicity against various cancerous cell lines.•Its cytotoxicity resulted from apoptosis rather than anti-proliferative activity.•It induced apoptosis through the mitochondrial cell death pathway.