Novel Tetraene Macrodiolides Are Effective Inducers of Mitochondrial Apoptosis in Jurkat Cells DOI Open Access
Ilgiz I. Islamov, Lilya U. Dzhemileva, Ilgam Gaisin

и другие.

International Journal of Molecular Sciences, Год журнала: 2025, Номер 26(11), С. 5139 - 5139

Опубликована: Май 27, 2025

We synthesized 16 representatives of a new class tetraene macrodiolides with two pharmacophore cis,cis-1,5-diene fragments the molecule in their structure rather high yields (from 67 to 84%), which, turn, were by catalytic intermolecular cyclocondensation reaction α,ω-alka-nZ,(n+4)Z-diendiols α,ω-alka-nZ,(n+4)Z-diendioic acids using Hf(OTf)4. The synthesis starting substrates 1Z,5Z-diene moieties degree stereoselectivity was carried out authors’ original homo-cyclomagnesiation O-containing allenes. cytotoxic potential examined compounds assessed following cell lines: Jurkat, K562, U937, HL60, HEK293, and Wi-38 (fibroblasts). Biological tests showed direct effect on mitochondrial biogenesis dissociation oxidation phosphorylation release cytochrome P450 into cytosol, as well induction apoptosis. selectivity index demonstrates significant variability, ranging from approximately 2.5 5.3 for Jurkat cells 3.0 5.8 other lines.

Язык: Английский

Dietary Triterpenoids in Functional Food and Drug Ingredients: a review of structure-activity relationships, biosynthesis, applications, and AI-driven strategies DOI
Chao Fang, Haixia Yang, Daidi Fan

и другие.

Trends in Food Science & Technology, Год журнала: 2025, Номер unknown, С. 104961 - 104961

Опубликована: Март 1, 2025

Язык: Английский

Процитировано

1
Exploration of quinoxaline triazoles as antimycobacterial agents: design, synthesis and biological evaluation DOI

Boddupalli Venkata Siva Kumar,

Tanweer Kumar, Adinarayana Nandikolla

и другие.

Bioorganic & Medicinal Chemistry Letters, Год журнала: 2025, Номер unknown, С. 130177 - 130177

Опубликована: Март 1, 2025

Язык: Английский

Процитировано

0
Helicity‐Dependent Enzymatic Peptide Cyclization DOI Creative Commons

Canan Durukan,

Jannik Faierson,

Isabel van der Wal

и другие.

Journal of Peptide Science, Год журнала: 2025, Номер 31(6)

Опубликована: Апрель 27, 2025

ABSTRACT The secondary structure plays a crucial role in the biological activity of peptides. Various strategies have been developed to stabilize particular peptide conformations, including sequence modifications and macrocyclization approaches. Often, interplay between conformational constraint flexibility is central bioactivity. Here, we investigate how α‐helicity influences enzymatic head‐to‐tail cyclization using an engineered Sortase. We show that peptides with low helicity readily undergo intramolecular cyclization, while more rigid, helical exhibit complex behaviors cyclic dimer formation. These findings reveal increased rigidity can redirect reactions from intermolecular processes, demonstrates changes molecular guide chemical reactivity. insights advance design peptide‐derived materials, hydrogels, stimuli‐responsive probes.

Язык: Английский

Процитировано

0
Novel Tetraene Macrodiolides Are Effective Inducers of Mitochondrial Apoptosis in Jurkat Cells DOI Open Access
Ilgiz I. Islamov, Lilya U. Dzhemileva, Ilgam Gaisin

и другие.

International Journal of Molecular Sciences, Год журнала: 2025, Номер 26(11), С. 5139 - 5139

Опубликована: Май 27, 2025

We synthesized 16 representatives of a new class tetraene macrodiolides with two pharmacophore cis,cis-1,5-diene fragments the molecule in their structure rather high yields (from 67 to 84%), which, turn, were by catalytic intermolecular cyclocondensation reaction α,ω-alka-nZ,(n+4)Z-diendiols α,ω-alka-nZ,(n+4)Z-diendioic acids using Hf(OTf)4. The synthesis starting substrates 1Z,5Z-diene moieties degree stereoselectivity was carried out authors’ original homo-cyclomagnesiation O-containing allenes. cytotoxic potential examined compounds assessed following cell lines: Jurkat, K562, U937, HL60, HEK293, and Wi-38 (fibroblasts). Biological tests showed direct effect on mitochondrial biogenesis dissociation oxidation phosphorylation release cytochrome P450 into cytosol, as well induction apoptosis. selectivity index demonstrates significant variability, ranging from approximately 2.5 5.3 for Jurkat cells 3.0 5.8 other lines.

Язык: Английский

Процитировано

0