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Transcriptome sequencing of HepG2 cells upon treatment of Butyrolactone I (PQY09) or derivatives (PQY23_1) butenolide compounds for exploring the targets of PQYs to further study the pharmacological activities

ABSTRACT: Transcriptome sequencing of HepG2 cells upon treatment of Butyrolactone I (PQY09) or derivatives (PQY23_1) butenolide compounds for exploring the targets of PQYs to further study the pharmacological activities

PROVIDER: PRJNA825245 | ENA |

REPOSITORIES: ENA

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			Action	DRS
	SRR18700800_1.fastq.gz	Fastqsanger.gz
	SRR18700800_2.fastq.gz	Fastqsanger.gz
	SRR18700801_1.fastq.gz	Fastqsanger.gz
	SRR18700801_2.fastq.gz	Fastqsanger.gz
	SRR18700802_1.fastq.gz	Fastqsanger.gz

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Transcriptome sequencing of HepG2 cells upon treatment of Butyrolactone I (PQY09) or derivatives (PQY23_1) butenolide compounds for exploring the targets of PQYs to further study the pharmacological activities

Project description:Transcriptome sequencing (RNA-Seq) of HepG2 cells upon treatment of the 50μM Butyrolactone I (PQY09) or derivatives (PQY23_1) butenolide compounds isolated from marine-derived fungi or DMSO(0.1%) as blank contrast for exploring the targets of PQYs to further study the pharmacological activities Butenolide, a mycotoxin produced by several toxigenic Fusarium species, fre-quently invades many important grains, and evokes a broad spectrum of toxic effects. But several butenolide derivatives, especially the well-known compound butyrolactone I, have been reported to show diverse biological activities, including an-ti-inflammatory , antibacterial , antiviral, antitumor, and α-/β-glucosidase inhibitory activities. So in order to investigate the other effect of PQYs and toxicity target, we used the second-generation transcriptome sequencing(RNA-seq) to determine the expression changes of each gene in HepG2 cells.

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Project description:Twelve aminoarylazocompounds (A-C) and 46 aryltriazene 7 derivatives (D-G) have been synthesized and evaluated in cell-based assays for cytotoxicity and antiviral activity against a panel of 10 RNA and DNA viruses. Eight aminoazocompounds and 27 aryltriazene derivatives exhibited antiviral activity, sometimes of high level, against one or more viruses. A marked activity against BVDV and YFV was prevailing among the former compounds, while the latter type of compounds affected mainly CVB-2 and RSV. None of the active compounds inhibited the multiplication of HIV-1, VSV and VV. Arranged in order of decreasing potency and selectivity versus the host cell lines, the best compounds are the following; BVDV: 1>7>8>4; YFV: 7>5; CVB-2: 25>56>18; RSV: 14>20>55>38>18>19; HSV-1: 2. For these compounds the EC(50) ranged from 1.6 microM (1) to 12 microM (18), and the S. I. from 19.4 (1) to 4.2 (2). Thus the aminoarylazo and aryltriazene substructures appear as interesting molecular component for developing antiviral agents against ss RNA viruses, particularly against RSV and BVDV, which are important human and veterinary pathogens. Finally, molecular modeling investigations indicated that compounds of structure A-C, active against BVDV, could work targeting the viral RNA-dependent RNA-polymerase (RdRp), having been observed a good agreement between the trends of the estimated IC(50) and the experimental EC(50) values.

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