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- Title
In Silico, In Vitro, and In Vivo Antitumor and Anti-Inflammatory Evaluation of a Standardized Alkaloid-Enriched Fraction Obtained from Boehmeria caudata Sw. Aerial Parts.
- Authors
Paiva, Paula P. de; Nunes, Julia H. B.; Nonato, Fabiana R.; Ruiz, Ana L. T. G.; Zafred, Rafael R. T.; Sousa, Ilza M. O.; Okubo, Márcia Y.; Kawano, Daniel F.; Monteiro, Paula A.; Foglio, Mary A.; Carvalho, João E.; Genovese, Salvatore; Fiorito, Serena
- Abstract
In the context of the cancer-inflammation relationship and the use of natural products as potential antitumor and anti-inflammatory agents, the alkaloid-enriched fraction of Boehmeriacaudata (BcAEF) aerial parts was evaluated. In vitro antiproliferative studies with human tumor cell lines showed high activity at low concentrations. Further investigation on NCI-H460 cells showed an irreversible effect on cell proliferation, with cell cycle arrest at G2/M phase and programmed cell death induction. Molecular docking studies of four alkaloids identified in BcAEF with colchicine's binding site on β-tubulin were performed, suggesting (−)-C (15R)-hydroxycryptopleurine as the main inductor of the observed mitotic death. In vivo studies showed that BcAEF was able to reduce Ehrlich tumor volume progression by 30 to 40%. Checking myeloperoxidase activity, BcAEF reduced neutrophils migration towards the tumor. The in vivo anti-inflammatory activity was evaluated by chemically induced edema models. In croton oil-induced ear edema and carrageenan (CG)-induced paw edema models, BcAEF reduced edema around 70 to 80% together with inhibition of activation and/or migration of neutrophils to the inflammatory area. All together the results presented herein show BcAEF as a potent antitumor agent combining antiproliferative and anti-inflammatory properties, which could be further explored in (pre)clinical studies.
- Subjects
TUBULINS; APOPTOSIS; MOLECULAR docking; CELL cycle; ANTINEOPLASTIC agents; BINDING sites
- Publication
Molecules, 2020, Vol 25, Issue 17, p4018
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules25174018