98%
921
2 minutes
20
Saint Peter and Saint Paul's Archipelago is a collection of 15 islets and rocks remotely located in the equatorial Atlantic Ocean. In this particular site, the present project intended to assess the biodiversity and biotechnological potential of bacteria from the actinomycete group. This study presents the first results of this assessment. From 21 sediment samples, 268 strains were isolated and codified as BRA followed by three numbers. Of those, 94 strains were grown in liquid media and submitted to chemical extractions with AcOEt (A), BuOH (B), and MeOH (M). A total of 224 extracts were screened for their cytotoxic activity and 41 were significantly active against HCT-116 cancer cells. The obtained IC values ranged from 0.04 to 31.55 μg/ml. The HR-LC/MS dereplication analysis of the active extracts showed the occurrence of several known anticancer compounds. Individual compounds, identified using HR-MS combined with analysis of the AntiMarin database, included saliniketals A and B, piericidins A and C and glucopiericidin A, staurosporine, N-methylstaurosporine, hydroxydimethyl-staurosporine and N-carbamoylstaurosporine, salinisporamycin A, and rifamycins S and B. BRA-199, identified as Streptomyces sp., was submitted to bioassay-guided fractionation, leading to isolation of the bioactive piericidins A and C, glucopiericidin, and three known diketopiperazines, cyclo(l-Phe-trans-4-OH-l-Pro), cyclo(l-Phe-l-Pro), and cyclo(l-Trp-l-Pro).
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1002/cbdv.201500514 | DOI Listing |
RSC Adv
September 2025
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University Zagazig 44511 Egypt
A novel isatin-thiazole-coumarin hybrid and three isatin-hydantoin hybrids were synthesized and assessed for their α-glucosidase and anticholinesterase inhibitory activities. Moreover, their anticancer properties have been observed against the breast cancer cell lines MCF-7 and MDA-MB-231. The coumarin-containing hybrid exhibited the most potent biological activity across all assays.
View Article and Find Full Text PDFRSC Adv
September 2025
Department of Medicinal Chemistry, Faculty of Pharmacy, Galala University P. O. 43713 New Galala Egypt
Isatin (1-indole-2,3-dione) is a privileged nitrogen-containing heterocyclic framework that has received considerable attention in anticancer drug discovery owing to its general biological behavior and structural diversity. This review focuses on isatin-heterocyclic hybrids as a valuable model in the development of new anti-cancer drugs that may reduce side effects and help overcome drug resistance, discussing their synthetic approaches and mechanism of action as apoptosis induction through kinase inhibition. With various chemical modifications, isatin had an excellent ability to build powerful isatin hybrids and conjugates targeting multiple oncogenic pathways.
View Article and Find Full Text PDFRSC Adv
September 2025
Process and Environmental Engineering Laboratory (LIPE), Faculty of Chemistry, University of Science and Technology of Oran Mohamed Boudiaf P. O. Box 1503, El Mnaouer 31000 Oran Algeria.
In this contribution, Molecular Electron Density Theory (MEDT) is employed to investigate the (3 + 2) cycloaddition reaction between ()--methyl--(2-furyl)-nitrone 1 and but-2-ynedioic acid 2. DFT calculations at the M06-2X-D3/6-311+G(d,p) level of theory under solvent-free conditions at room temperature show that this reaction proceeds CA3-Z diastereoselectivity, with the formation of the CA3-Z cycloadduct being both thermodynamically and kinetically more favoured than the CA4-Z one. Reactivity parameters obtained from CDFT calculations reveal that compound 1 predominantly behaves as a nucleophile with moderate electrophilic features, in contrast to compound 2, which demonstrates strong electrophilicity and limited nucleophilic ability.
View Article and Find Full Text PDFRSC Adv
September 2025
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University Assiut 71526 Egypt
Thunb is endogenous to Southeast Asia and traditionally used for the treatment of bacterial and viral infections. Previous studies reported various pharmacological activities, including cytotoxic activity. The aim of this work was to identify phytoconstituents of the ethanolic extract of aerial parts using extensive 1D- and 2D-NMR analysis and HR-MS.
View Article and Find Full Text PDFClin Pharmacol
September 2025
Department of Biology, College of Science Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia.
Cancer remains the second leading cause of death worldwide, highlighting the urgent need for novel therapeutic approaches. Fungi are a rich source of bioactive metabolites, some of which exhibit potent anticancer properties. This scoping review evaluates the current research on fungal metabolites with anticancer potential, focusing on species native to Saudi Arabia's unique ecosystem.
View Article and Find Full Text PDF