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基于姜黄素和白藜芦醇的新型杂化物:合成、细胞毒性及对结肠癌细胞的抗增殖活性。

New Hybrids Based on Curcumin and Resveratrol: Synthesis, Cytotoxicity and Antiproliferative Activity against Colorectal Cancer Cells.

机构信息

Química de Plantas Colombianas, Faculty of Exact and Natural Sciences, Institute of Chemistry, University of Antioquia (UdeA), Calle 70 No. 52-21, Medellín AA 1226, Colombia.

出版信息

Molecules. 2021 May 1;26(9):2661. doi: 10.3390/molecules26092661.

DOI:10.3390/molecules26092661
PMID:34062841
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8124228/
Abstract

We synthesized twelve hybrids based on curcumin and resveratrol, and their structures were elucidated by spectroscopic analysis. The chemopreventive potential of these compounds was evaluated against SW480 human colon adenocarcinoma cells, its metastatic derivative SW620, along with the non-malignant CHO-K1 cell line. Among the tested compounds, hybrids and (for SW480) and , and (for SW620) displayed the best cytotoxic activity with IC values ranging from 11.52 ± 2.78 to 29.33 ± 4.73 µM for both cell lines, with selectivity indices (SI) higher than 1, after 48 h of treatment. Selectivity indices were even higher than those reported for the reference drug, 5-fluorouracil (SI = 0.96), the starting compound resveratrol (SI = 0.45) and the equimolar mixture of curcumin plus resveratrol (SI = 0.77). The previous hybrids showed good antiproliferative activity.

摘要

我们合成了基于姜黄素和白藜芦醇的 12 种杂化物,并通过光谱分析阐明了它们的结构。这些化合物的化学预防潜力通过对 SW480 人结肠腺癌细胞及其转移性衍生物 SW620 以及非恶性 CHO-K1 细胞系进行评估。在测试的化合物中,杂化物和(针对 SW480)和,以及(针对 SW620)显示出最好的细胞毒性活性,IC 值范围为 11.52 ± 2.78 至 29.33 ± 4.73 μM,对于两种细胞系,在 48 小时的治疗后,选择性指数(SI)高于 1。选择性指数甚至高于参考药物 5-氟尿嘧啶(SI = 0.96)、起始化合物白藜芦醇(SI = 0.45)和姜黄素与白藜芦醇等摩尔混合物(SI = 0.77)。之前的杂化物表现出良好的抗增殖活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb6e/8124228/ccca89205566/molecules-26-02661-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb6e/8124228/8160fa402ec0/molecules-26-02661-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb6e/8124228/7aa68387f784/molecules-26-02661-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb6e/8124228/6a6a48ea38d4/molecules-26-02661-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb6e/8124228/ccca89205566/molecules-26-02661-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb6e/8124228/8160fa402ec0/molecules-26-02661-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb6e/8124228/7aa68387f784/molecules-26-02661-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb6e/8124228/6a6a48ea38d4/molecules-26-02661-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb6e/8124228/ccca89205566/molecules-26-02661-g003.jpg

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