1. Withaphysalin Derivatives from Iochroma arborescens Induce Antiproliferative and Antimigratory Activities in vitro.
- Author
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de Sá, Rodrigo Elísio, de Araújo, Gisele Santos, Machado, Fabrício dos Santos, Souza, Jessica Maria Teles, Barros, Ayslan Batista, Pinto, Francisco das Chagas Lima, Agostinho, Joana Deyse Lima, Ayala, Alejandro Pedro, Marinho Filho, José Delano Barreto, Pessoa, Otília Deusdênia Loiola, and Araújo, Ana Jérsia
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CELL migration inhibition , *IN vitro studies , *CRYSTALLIZATION , *CYTOLOGY , *RESEARCH funding , *COLONY-forming units assay , *BREAST tumors , *ANTINEOPLASTIC agents , *CELL adhesion molecules , *CARBON , *BIOLOGICAL products , *IMMUNODIAGNOSIS , *DNA , *QUANTITATIVE research , *PLANT extracts , *CELL lines , *MEDICINAL plants , *MOLECULAR structure , *CELL death , *SODIUM , *SPECTRUM analysis , *DRUG efficacy , *ORGANIC compounds , *CELL survival , *LEAVES , *MICROSCOPY , *CELL surface antigens , *PHARMACODYNAMICS - Abstract
Withanolides are steroidal lactones commonly found in plants of the Solanaceae family that have significant medicinal value. In this study, three withanolides extracted from Iochroma arborescens leaves were isolated and characterized. These included withaphysalin F (3) and two newly identified epimeric compounds: 18 R - and 18 S - O -methyl-withaphysalin F (1 and 2). Their structures were elucidated by NMR, IR, MS, CD, and X-ray diffraction analysis, and their potential against cell proliferation and migration was investigated. The cytotoxic assay revealed activity against different tumor and non-tumor cell lines. (18 S)- O -methyl-withaphysalin F (2) presented cell death effects after at least 6 hours of exposure. MDA-MB-231 cells were exposed to 0.06 and 0.6 µM of (18 S)- O -methyl-withaphysalin F (2), and reductions in cell adhesion, migration, and clonogenicity were observed. Morphological analysis revealed negative regulation in filopodia, salience, and roughness, as well as alterations in cellular microarchitecture. These results provide clues as to the effects of (18 S)- O -methyl-withaphysalin F (2), allowing new molecular modifications to improve potency and selectivity and increase our antineoplastic arsenal. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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