AI Article Synopsis
- Three new compounds called Callicarpnoids A-C were discovered from the stems of Callicarpa arborea, and their structures were determined using advanced techniques like spectroscopic analysis and X-ray diffraction.
- Compounds 2 and 3 showed strong anti-cancer activity against breast and colorectal cancer cells, with effective concentrations ranging from 5.2 to 7.2 μM that were comparable to existing treatments.
- Analysis of protein levels indicated that these compounds promote cancer cell death (apoptosis) by increasing certain proteins (like Bax) and decreasing others (like caspases), suggesting they work through multiple pathways to induce apoptosis.
Article Abstract
Callicarpnoids A-C (1-3), three new ent-clerodane diterpenoid dimers formed via a [4 + 2] hetero Diels-Alder cycloaddition, appeared as a third example of this type of dimers, were isolated from the stems of Callicarpa arborea Roxb.. Their structures were elucidated by comprehensive spectroscopic analysis, and the absolute configurations were confirmed by single-crystal X-ray diffraction and electronic circular dichroism (ECD) calculations, as well as DP4 + analysis. Cytotoxicity test in two cell lines indicated that compounds 2 and 3 had significant cytotoxic effect against breast cancer cell (MCF-7) and colorectal cancer cell (HCT-116) with IC ranging from 5.2 to 7.2 μM, comparable to those of the positive control. Furthermore, the western blot analysis revealed that the protein expression levels of Bax were increased following compounds 2 and 3 treatment, whereas the expression levels of caspase 8, caspase 3, caspase 9 and Bcl were decreased in a dose-dependent manner, indicating that compounds 2 and 3 may induce apoptosis via both intrinsic and extrinsic pathways in MCF-7 and HCT-116 cells.
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| http://dx.doi.org/10.1016/j.bioorg.2022.106111 | DOI Listing |
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Callicarpnoids A-C, structurally intriguing ent-Clerodane diterpenoid dimers with cytotoxicity against MCF-7 and HCT-116 cell lines from Callicarpa arborea Roxb.
Bioorg Chem
December 2022
Key Laboratory of Medicinal Chemistry for Natural Resource of Ministry of Education, Yunnan Characteristic Plant Extraction Laboratory, Yunnan Research & Development Center for Natural Products, School of Chemical Science and Technology, and School of Medicine, Yunnan University, Kunming 650091, PR China; State Key Laboratory for Conservation and Utilization of Bio-Resources in Yunnan, Yunnan University, Kunming 650091, PR China. Electronic address:
Article Synopsis
- Three new compounds called Callicarpnoids A-C were discovered from the stems of Callicarpa arborea, and their structures were determined using advanced techniques like spectroscopic analysis and X-ray diffraction.
- Compounds 2 and 3 showed strong anti-cancer activity against breast and colorectal cancer cells, with effective concentrations ranging from 5.2 to 7.2 μM that were comparable to existing treatments.
- Analysis of protein levels indicated that these compounds promote cancer cell death (apoptosis) by increasing certain proteins (like Bax) and decreasing others (like caspases), suggesting they work through multiple pathways to induce apoptosis.
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