Anticancer and antimicrobial activities of new thiazolyl-urea derivatives: gene expression, DNA damage, DNA fragmentation and SAR studies

Sroor, Farid M.; Othman, Abdelmageed M.; Aboelenin, Mohamad M.; Mahrous, Karima F.

doi:10.1007/s00044-022-02849-3

Cited by 25 publications

(11 citation statements)

References 54 publications

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“…The absorbance of intact DNA and fragment DNA at 600 nm was determined using a spectrophotometer (UV-9000, Shanghai, China). The assay method of the AGE was the same as that described elsewhere [ 42 ].…”

Section: Methodsmentioning

confidence: 99%

Exploring the Mystery of the Tetrahydrobiopterin Synthetic Defect Lethal Mutant leml from Birth to Death in the Silkworm Bombyx mori

Liang

Shu

Jiang

et al. 2022

IJMS

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Tetrahydrobiopterin (BH4) is a vital coenzyme for several enzymes involved in diverse enzymatic reactions in animals, and BH4 deficiency can lead to metabolic and neurological disorders due to dysfunction in its metabolism. In the silkworm natural homozygous mutant leml, the key enzyme sepiapterin reductase (BmSPR) in the de novo synthesis pathway of BH4 is inactivated, resulting in severe deficiency of BH4 synthesis. However, it is not known why the leml larvae can survive to the second-instar stage and which pathways lead to their death when BH4 is deficient. Here, we quantified BH4 and found that the fertilized eggs contained large amounts of BH4 transferred from the mother to the offspring, maintaining its normal development in the embryo and the first instar. Subsequently, we investigated the multiple pathways in which BH4 is involved as a cofactor. The results showed that BH4 deficiency in silkworms blocked the melanin synthesis pathway, caused an insufficient degree of epidermal sclerosis, disordered tyrosine metabolism, and damaged mitochondria. On the other hand, BH4 deficiency led to the uncoupling of nitric oxide synthase (BmNOS), a reduced NO production, and a significantly reduced fat in fat body catalyzation by phospholipase A2, resulting in an impaired immune system. Meanwhile, the uncoupling of BmNOS increased the O2− content, damaged the DNA, and caused the apoptosis of the body cells. Taken together, BH4 is critical for the life and death of leml mutants. This study lays a foundation for the further exploration of lepidopteran insects and provides an important basis for the treatment of human BH4 deficiency-related diseases.

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Section: Methodsmentioning

confidence: 99%

Exploring the Mystery of the Tetrahydrobiopterin Synthetic Defect Lethal Mutant leml from Birth to Death in the Silkworm Bombyx mori

Liang

Shu

Jiang

et al. 2022

IJMS

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“…As a positive control, gentamicin (10 mcg) was employed. The sizes of clear zones were measured in millimeters after adequate incubation (overnight at 37 C) [54][55][56].…”

Section: Synthesis Of Methylmentioning

confidence: 99%

Design, synthesis and in‐vitro evaluation of new furan‐substituted thiadiazolyl hydrazone derivatives as promising antimicrobial agents

Helmy

Sroor

Othman

et al. 2022

Journal of Heterocyclic Chem

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Seventeen new furan‐substituted thiadiazolyl hydrazone derivatives bearing 4‐nitrophenyl moiety were designed, synthesized and tested for their in vitro antimicrobial activity. Reaction of N‐(4‐nitrophenyl)‐C‐(furan‐2‐yl)methanohydrazonoyl chloride 1 with 2‐((methylthio)carbonthioyl)hydrazine derivatives 3, 7, 8 and 11–13 in absolute ethanol in the presence of triethylamine at room temperature afforded the corresponding 1,3,4‐thiadiazole derivatives 6, 9, 10 and 14–16. Refluxing of 1‐(3‐(furan‐2‐yl)‐5‐methyl‐1‐(4‐nitrophenyl)‐1H‐pyrazol‐4‐yl)ethan‐1‐one 17 with methyl hydrazinecarbodithioate 18 in absolute ethanol in the presence of few drops of hydrochloric acid yielded methyl‐2‐(1‐(3‐(furan‐2‐yl)‐5‐methyl‐1‐(4‐nitrophenyl)‐1H‐pyrazol‐4‐yl)ethylidene)hydrazine‐1‐carbodithioate 19. The compound 19 was reacted with hydrazonoyl halides 20a‐e in absolute ethanol in the presence of triethylamine afforded the corresponding 1,3,4‐thiadiazoles 24a‐e. The specified compounds were tested for antimicrobial activity against selected model microorganisms. Antimicrobial studies revealed that compounds 6c, 6d and 15 against E. coli, compounds 6b, 6c, 10, 14, 15, 24b and 24c against B. mycoides, and compounds 14, 16, 19 and 24d against C. albicans outperformed other developed compounds in terms of antimicrobial activity.

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“…These primers were cited by Chu et al (2007) and used for identification of genetic polymorphisms in INHβA gene by using PCR-SSCP technique and nucleotide sequence analysis. The annealing temperature of each pair was optimized using a conventional PCR to exclude the presence of unspecific products or primer dimer, and the PCR products were analyzed by 2% agarose gel electrophoresis as described previously (Madkour et al, 2020;Mahrous et al, 2020a;Mahrous et al, 2020b;Mahrous et al, 2020d;Sroor et al, 2020;Madkour et al, 2021a;Madkour et al, 2021b;Mahrous et al, 2021;Sroor et al, 2022). The Polymerase chain reaction had been carried out in 25µl volume involving 2.5 µl of 10 x PCR buffer (50 mmol/L KCL, 10 mmol/L Tris-HCl (pH 8.0), 0.1% Triton X-100) 1.5 mmol/L MgCl2, 200µmol/L each dNTP, 1µmol/L each primer, 50 ng genomic DNA, and 1 U Taq DNA polymerase.…”

Section: Primers and Pcr Amplificationmentioning

confidence: 99%

Untitled

2022

JJBS

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Study areas include cell biology, genomics, microbiology, immunology, molecular biology, biochemistry, embryology, immunogenetics, cell and tissue culture, molecular ecology, genetic engineering and biological engineering, bioremediation and biodegradation, bioinformatics, biotechnology regulations, gene therapy, organismal biology, microbial and environmental biotechnology, marine sciences. The JJBS welcomes the submission of manuscript that meets the general criteria of significance and academic excellence. All articles published in JJBS are peerreviewed. Papers will be published approximately one to two months after acceptance.

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Anticancer and antimicrobial activities of new thiazolyl-urea derivatives: gene expression, DNA damage, DNA fragmentation and SAR studies

Cited by 25 publications

References 54 publications

Exploring the Mystery of the Tetrahydrobiopterin Synthetic Defect Lethal Mutant leml from Birth to Death in the Silkworm Bombyx mori

Exploring the Mystery of the Tetrahydrobiopterin Synthetic Defect Lethal Mutant leml from Birth to Death in the Silkworm Bombyx mori

Design, synthesis and in‐vitro evaluation of new furan‐substituted thiadiazolyl hydrazone derivatives as promising antimicrobial agents

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