Metabolomic approach in anticancer biomarker discovery of folious lichens DOI Creative Commons
Chintya Permata Zahky Sukrisno Putri, Dinar Mutia Rani, Ludmilla Fitri Untari

et al.

Advanced Pharmaceutical Bulletin, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 14, 2024

Purpose: Lichens are well-known as a source of pharmacologically active compounds. This includes anticancer compounds which have biomass constraints including using traditional techniques lichen bioprospecting. current study reports the use cutting-edge metabolomics and computational approach to discover biomarkers from Indonesian lichens. Methods: Seven crude extracts were evaluated against cervical cell lines HeLa MTT assay secondary metabolites profiled recorded via GCMS protocol. A multivariate analysis OPLSDA was employed determine biomarker structure-based cancer related protein targets (BCL-2 (4MAN), AKT-1 (4GV1), MCL-1 (5FDO), BRAF (5VAM)) used most potent biomarker. Results: The assessment indicated seven lichens possessed strong, medium weak cytotoxicity. Multivariate showed an OPLS-DA score plot with distinct separation among cytotoxic groups. biplot GC-MS proposed 13 Parmelia caroliniana 12 Physcia cf. millegrana candidates. Docking experiments revealed 6-amino-3,4,7-triphenylpyrido[2',3':4,5]thieno[2,3-c]pyridazine 4 P. possess highest binding affinity BCL-2 (5VAM) proteins energy values -10.0, -11.6, -10.4, -12.6, respectively. Conclusion: successfully compound in can be further explored through vitro vivo studies. Further, metabolomic protocol established adapted tool for discoveries other medicinal plants.

Language: Английский

Development and synthesis of diffractaic acid analogs as potent inhibitors of colorectal cancer stem cell traits DOI Creative Commons
Mücahit Varlı, Suresh R. Bhosle, Eunhye Jo

et al.

Scientific Reports, Journal Year: 2025, Volume and Issue: 15(1)

Published: Feb. 25, 2025

In recent years, evidence for the anti-cancer activity of lichen secondary metabolites has been rapidly increasing. this study, we synthesised analogues diffractaic acid, a metabolite, and evaluated their ability to suppress colorectal cancer stem potential. Among 10 compounds after H/CH₃/benzylation acid structure or modifications in an aromatic hydrophobic domain, TU3 more inhibition effect on potential compared other compounds. The compound targets ALDH1 suppresses key signalling pathways such as WNT, STAT3, NF-κB, Hedgehog, AP-1. Inhibition these by contribute attenuate survival mechanisms cell thus inhibit progression.

Language: Английский

Citations

0
Metabolomic approach in anticancer biomarker discovery of folious lichens DOI Creative Commons
Chintya Permata Zahky Sukrisno Putri, Dinar Mutia Rani, Ludmilla Fitri Untari

et al.

Advanced Pharmaceutical Bulletin, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 14, 2024

Purpose: Lichens are well-known as a source of pharmacologically active compounds. This includes anticancer compounds which have biomass constraints including using traditional techniques lichen bioprospecting. current study reports the use cutting-edge metabolomics and computational approach to discover biomarkers from Indonesian lichens. Methods: Seven crude extracts were evaluated against cervical cell lines HeLa MTT assay secondary metabolites profiled recorded via GCMS protocol. A multivariate analysis OPLSDA was employed determine biomarker structure-based cancer related protein targets (BCL-2 (4MAN), AKT-1 (4GV1), MCL-1 (5FDO), BRAF (5VAM)) used most potent biomarker. Results: The assessment indicated seven lichens possessed strong, medium weak cytotoxicity. Multivariate showed an OPLS-DA score plot with distinct separation among cytotoxic groups. biplot GC-MS proposed 13 Parmelia caroliniana 12 Physcia cf. millegrana candidates. Docking experiments revealed 6-amino-3,4,7-triphenylpyrido[2',3':4,5]thieno[2,3-c]pyridazine 4 P. possess highest binding affinity BCL-2 (5VAM) proteins energy values -10.0, -11.6, -10.4, -12.6, respectively. Conclusion: successfully compound in can be further explored through vitro vivo studies. Further, metabolomic protocol established adapted tool for discoveries other medicinal plants.

Language: Английский

Citations

0