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Cytotoxicity and Pro-Apoptotic, Antioxidant and Anti-Inflammatory Activities of Geopropolis Produced by the Stingless Bee Melipona fasciculata Smith

1
Laboratório de Farmacognosia, Departamento de Farmácia, Campus Bacanga, Universidade Federal do Maranhão, Av. dos Portugueses, 1966, São Luís 65080-805, Maranhão, Brazil
2
Programa de Pós-Graduação em Farmacologia e Química Medicinal, Instituto de Ciências Biológicas, Universidade Federal do Rio de Janeiro, Rio de Janeiro 21041-250, Rio de Janeiro, Brazil
3
Laboratório de Estudo Experimental da Dor, Campus Bacanga, Universidade Federal do Maranhão, Av. dos Portugueses, 1966, São Luís 65080-805, Maranhão, Brazil
4
Divisão de Pesquisa Clínica e Desenvolvimento Tecnológico, Instituto Nacional de Câncer, Rua André Cavalcanti, 37, Rio de Janeiro 20231-050, Rio de Janeiro, Brazil
5
Laboratório de Química de Produtos Naturais, Departamento de Química, Campus Bacanga, Universidade Federal do Maranhão, Av. dos Portugueses, 1966, São Luís 65080-805, Maranhão, Brazil
*
Authors to whom correspondence should be addressed.
Biology 2020, 9(9), 292; https://doi.org/10.3390/biology9090292
Received: 3 August 2020 / Revised: 8 September 2020 / Accepted: 9 September 2020 / Published: 15 September 2020
(This article belongs to the Special Issue Bioactivity of Medicinal Plants and Extracts)
Geopropolis is produced by some stingless bee species, such as Melipona fasciculata Smith, a native species from Brazil. This study aims to investigate the antioxidant and anti-inflammatory activities and cytotoxicity effects of geopropolis hydroethanolic extracts against lung (H460 and A549) and ovarian (A2780 and ES2) cancer cell lines and non-tumor (HUVEC) cell lines using chemical identification by LC/MS/MS analysis and in silico assays to determine which compounds are associated with bioactivity. The antioxidant activity of extracts and inhibitory activity against COX enzymes were assessed by in vitro assays; cytotoxicity effect was evaluated by the MTT assay; cell cycle was assessed by flow cytometry and apoptosis by Western blotting. The geopropolis extracts showed great radical scavenging potential, preferential inhibition of COX-2, decreased cancer cell viability, non-cytotoxic effects against the non-tumoral cell line, besides modulating the cell cycle and inducing cancer cell apoptosis through the activation of caspase-3 and PARP protein cleavage. The in silico study suggests that corilagin, typhaneoside, taraxerone and marsformosanone, identified by LC/MS/MS, can be associated with anti-inflammatory activity and cytotoxic effects. Thus, the current study suggests the potential of geopropolis concerning the research field of new pharmacological alternatives regarding cancer therapy. View Full-Text
Keywords: natural products; antitumor activity; new anticancer agents; apoptosis pathway; molecular docking; drug discovery natural products; antitumor activity; new anticancer agents; apoptosis pathway; molecular docking; drug discovery
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Barboza, J.R.; Pereira, F.A.N.; Fernandes, R.A.; Vasconcelos, C.C.; Cartágenes, M.S.S.; Oliveira Lopes, A.J.; Melo, A.C.; Guimarães, I.S.; Rocha, C.Q.; Ribeiro, M.N.S. Cytotoxicity and Pro-Apoptotic, Antioxidant and Anti-Inflammatory Activities of Geopropolis Produced by the Stingless Bee Melipona fasciculata Smith. Biology 2020, 9, 292.

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