Cytotoxicity and Pro-Apoptotic, Antioxidant and Anti-Inflammatory Activities of Geopropolis Produced by the Stingless Bee Melipona fasciculata Smith
by
Josianne Rocha Barboza 1,*
, Francisco Assis Nascimento Pereira 1, Renan Amphilophio Fernandes 2, Cleydlenne Costa Vasconcelos 3, Maria do Socorro de Sousa Cartágenes 3, Alberto Jorge Oliveira Lopes 1,3, Andreia Cristina de Melo 4, Isabella dos Santos Guimarães 4, 
Cláudia Quintino da Rocha 5,* and Maria Nilce de Sousa Ribeiro 1
Josianne Rocha Barboza 1,*, Francisco Assis Nascimento Pereira 1, Renan Amphilophio Fernandes 2, Cleydlenne Costa Vasconcelos 3, Maria do Socorro de Sousa Cartágenes 3, Alberto Jorge Oliveira Lopes 1,3, Andreia Cristina de Melo 4, Isabella dos Santos Guimarães 4, Cláudia Quintino da Rocha 5,* and Maria Nilce de Sousa Ribeiro 1
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.
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Keywords:
natural products; antitumor activity; new anticancer agents; apoptosis pathway; molecular docking; drug discovery
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MDPI and ACS Style
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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