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杂环卡宾铁配合物作为抗癌剂：体外和体内生物学研究。

-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies.

机构信息

ITQB NOVA, Instituto de Tecnologia Química e Biológica António Xavier, Av. da República, 2780-157 Oeiras, Portugal.

UCIBIO, Departamento Ciências da Vida, NOVA School of Science and Technology, NOVA University, Campus de Caparica, 2829-516 Caparica, Portugal.

出版信息

Molecules. 2021 Sep 12;26(18):5535. doi: 10.3390/molecules26185535.

DOI:10.3390/molecules26185535
PMID:34577006
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8470334/
Abstract

Cisplatin and its derivatives are commonly used in chemotherapeutic treatments of cancer, even though they suffer from many toxic side effects. The problems that emerge from the use of these metal compounds led to the search for new complexes capable to overcome the toxic side effects. Here, we report the evaluation of the antiproliferative activity of Fe(II) cyclopentadienyl complexes bearing -heterocyclic carbene ligands in tumour cells and their in vivo toxicological profile. The in vitro antiproliferative assays demonstrated that complex displays the highest cytotoxic activity both in human colorectal carcinoma cells (HCT116) and ovarian carcinoma cells (A2780) with IC values in the low micromolar range. The antiproliferative effect of was even higher than cisplatin. Interestingly, showed low in vivo toxicity, and in vivo analyses of and compounds using colorectal HCT116 zebrafish xenograft showed that both reduce the proliferation of human HCT116 colorectal cancer cells in vivo.

摘要

顺铂及其衍生物常用于癌症的化疗治疗，尽管它们存在许多毒性副作用。这些金属化合物的使用所带来的问题促使人们寻找新的配合物来克服这些毒性副作用。在这里，我们报告了评估具有 -杂环卡宾配体的 Fe(II)茂金属配合物在肿瘤细胞中的抗增殖活性及其体内毒理学特征。体外增殖活性测定表明，配合物 对人结直肠癌细胞 (HCT116) 和卵巢癌细胞 (A2780) 具有最高的细胞毒性活性，IC 值在低微摩尔范围内。 的抗增殖作用甚至高于顺铂。有趣的是， 表现出低的体内毒性，并且使用结直肠 HCT116 斑马鱼异种移植对 和 化合物的体内分析表明，两者都能在体内减少人 HCT116 结直肠癌细胞的增殖。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/8a4a0f0074ed/molecules-26-05535-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/14ed03750f3b/molecules-26-05535-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/085fd4e61aae/molecules-26-05535-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/1ad0927d4d90/molecules-26-05535-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/50a48f964fd9/molecules-26-05535-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/069997660bd0/molecules-26-05535-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/2901bae77b58/molecules-26-05535-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/edc636293932/molecules-26-05535-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/8a4a0f0074ed/molecules-26-05535-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/14ed03750f3b/molecules-26-05535-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/085fd4e61aae/molecules-26-05535-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/1ad0927d4d90/molecules-26-05535-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/50a48f964fd9/molecules-26-05535-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/069997660bd0/molecules-26-05535-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/2901bae77b58/molecules-26-05535-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/edc636293932/molecules-26-05535-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8ed9/8470334/8a4a0f0074ed/molecules-26-05535-g008.jpg

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