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新型萘酚重氮基支架类席夫碱作为抗人结肠癌细胞系（HT-29）潜在抗菌和细胞毒性剂的合成与评价

Synthesis and evaluation of novel naphthol diazenyl scaffold based Schiff bases as potential antimicrobial and cytotoxic agents against human colorectal carcinoma cell line (HT-29).

作者信息

Kaur Harmeet, Singh Jasbir, Narasimhan Balasubramanian

机构信息

1Faculty of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, 124001 India.

2College of Pharmacy, Postgraduate Institute of Medical Sciences, Rohtak, 124001 India.

出版信息

BMC Chem. 2019 Apr 2;13(1):49. doi: 10.1186/s13065-019-0558-y. eCollection 2019 Dec.

DOI:10.1186/s13065-019-0558-y
PMID:31384797
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6661811/
Abstract

BACKGROUND

In search of new antimicrobial and cytotoxic agents, a series of new naphthol diazenyl scaffold based Schiff bases (-) was efficiently synthesized by condensation of 2-hydroxy naphthaldehyde azo dyes with various substituted aromatic/heteroaromatic/aliphatic amines.

METHODOLOGY

The synthesized derivatives were characterized by various physicochemical and spectral techniques and assessed for in vitro antimicrobial and cytotoxic potential against human colorectal carcinoma cell line (HT-29). The active derivatives were further evaluated for their apoptotic potential by Annexin-V/propidium iodide double staining assay using flow cytometer and analyzed for cell-cycle arrest studies.

RESULTS AND CONCLUSION

The derivative was found maximum active against . , and . The derivatives , , , and showed maximum antifungal activity against . The maximum cytotoxicity was observed from the derivatives , , , and towards HT-29 cell line with IC between 4 and 19 μg/ml. More than 90% and 62% of the cells were found in the apoptotic phase on treatment with and respectively in comparison to the 68% for doxorubicin. Further, these derivatives arrested the cell growth in S and G2/M phase of the cell cycle.

摘要

背景

为寻找新型抗菌和细胞毒性药物，通过2-羟基萘甲醛偶氮染料与各种取代的芳香族/杂环芳香族/脂肪族胺缩合，高效合成了一系列基于萘酚二氮烯基骨架的新型席夫碱（-）。

方法

通过各种物理化学和光谱技术对合成的衍生物进行表征，并评估其对人结肠癌细胞系（HT-29）的体外抗菌和细胞毒性潜力。使用流式细胞仪通过膜联蛋白-V/碘化丙啶双染色法进一步评估活性衍生物的凋亡潜力，并分析细胞周期阻滞研究。

结果与结论

发现衍生物 对.、. 和. 具有最大活性。衍生物 、 、 和 对. 表现出最大的抗真菌活性。衍生物 、 、 和 对HT-29细胞系的细胞毒性最大，IC在4至19μg/ml之间。与阿霉素的68%相比，用 和 处理时分别有超过90%和62%的细胞处于凋亡期。此外，这些衍生物使细胞生长停滞在细胞周期的S期和G2/M期。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/c3d40a8aeef1/13065_2019_558_Fig10_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/ed3caad4636f/13065_2019_558_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/671445503a58/13065_2019_558_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/51aaf5a4e012/13065_2019_558_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/9d27637619c6/13065_2019_558_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/5a6c65fbad39/13065_2019_558_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/4ca88ac01c06/13065_2019_558_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/4ddd44947ba1/13065_2019_558_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/82ba37929d4d/13065_2019_558_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/0d7f669ebfdf/13065_2019_558_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/c3d40a8aeef1/13065_2019_558_Fig10_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/ed3caad4636f/13065_2019_558_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/671445503a58/13065_2019_558_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/51aaf5a4e012/13065_2019_558_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/9d27637619c6/13065_2019_558_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/5a6c65fbad39/13065_2019_558_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/4ca88ac01c06/13065_2019_558_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/4ddd44947ba1/13065_2019_558_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/82ba37929d4d/13065_2019_558_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/0d7f669ebfdf/13065_2019_558_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14bd/6661811/c3d40a8aeef1/13065_2019_558_Fig10_HTML.jpg

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