Dataset Information

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).

ABSTRACT:

Background

In search of new antimicrobial and cytotoxic agents, a series of new naphthol diazenyl scaffold based Schiff bases (NS1-NS23) 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 NS-2 was found maximum active against E. coli, S. enterica and B. subtilis. The derivatives NS-12, NS-15, NS-21, and NS-23 showed maximum antifungal activity against A. fumigatus. The maximum cytotoxicity was observed from the derivatives NS-2, NS-8, NS-21, and NS-23 towards HT-29 cell line with IC₅₀ between 4 and 19 μg/ml. More than 90% and 62% of the cells were found in the apoptotic phase on treatment with NS-2 and NS-21 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.

SUBMITTER: Kaur H

PROVIDER: S-EPMC6661811 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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Publications

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).

Kaur Harmeet H Singh Jasbir J Narasimhan Balasubramanian B

BMC chemistry 20190402 1

<h4>Background</h4>In search of new antimicrobial and cytotoxic agents, a series of new naphthol diazenyl scaffold based Schiff bases (<b>NS1</b>-<b>NS23</b>) was efficiently synthesized by condensation of 2-hydroxy naphthaldehyde azo dyes with various substituted aromatic/heteroaromatic/aliphatic amines.<h4>Methodology</h4>The synthesized derivatives were characterized by various physicochemical and spectral techniques and assessed for in vitro antimicrobial and cytotoxic potential against huma ...[more]

PMID: 31384797

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Project description:Resistance of tumor cells to chemotherapy, such as 5‑fluorouracil (5‑FU), is an obstacle for successful treatment of cancer. As a follow‑up of a previous study we have investigated the effect of conditioned media (CM) from macrophages of M1 or M2 phenotypes on 5‑FU cytotoxicity on the colon cancer cell lines HT‑29 and CACO‑2. HT‑29 cells, but not CACO‑2 cells, having been treated with a combination of M1 CM and 5‑FU recovered their cell growth to a much larger extent compared to cells having been treated with 5‑FU alone when further cultured for 7 days in fresh media. M1 CM treatment of HT‑29, but not CACO‑2 cells, induced cell cycle arrest in the G0/G1 and G2/M phases. 5‑FU treatment induced accumulation of cells in S‑phase in both HT‑29 and CACO‑2 cells. This accumulation of cells in S‑phase was attenuated by combined M1 CM and 5‑FU treatment in HT‑29 cells, but not in CACO‑2 cells. The mRNA expression of cell cycle regulatory proteins and 5‑FU metabolic enzymes were analyzed in an attempt to find possible mechanisms for the M1 CM induced attenuation of 5‑FU cytotoxicity in HT‑29. Thymidylate synthetase (TS) and thymidine phosphorylase (TP) were found to be substantially downregulated and upregulated, respectively, in HT‑29 cells treated with M1 CM, making them unlikely as mediators of reduced 5‑FU cytotoxicity. Among cell cycle regulating proteins, p21 was induced in HT‑29 cells, but not in CACO‑2 cells, in response to M1 CM treatment. However, small interfering RNA (siRNA) knockdown of p21 had no effect on the M1 CM induced cell cycle arrest seen in HT‑29 and neither did it change the growth recovery after combined treatment of HT‑29 cells with M1 CM and 5‑FU. In conclusion, treatment of HT‑29 cells with M1 CM reduces the cytotoxic effect of 5‑FU and this is mediated by a M1 CM induced cell cycle arrest in the G0/G1 and G2/M phases. So far, we lack an explanation why this action is absent in the CACO‑2 cells. The current findings may be important for optimization of chemotherapy in colon cancer.

Dataset Information

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).

Background

Methodology

Results and conclusion

Publications

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).

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