Biological and physical approaches on the role of piplartine (piperlongumine) in cancer

Author(s):Show less -

Henrique, Tiago ^[1] ; Zanon, Caroline de F. ^[2] ; Girol, Ana P. ^{[2, 3]} ; Buzzo Stefanini, Ana Carolina ^{[1, 4]} ; Contessoto, Nayara S. de A. ^[5] ; da Silveira, Nelson J. F. ^[6] ; Bezerra, Daniel P. ^[7] ; Silveira, Edilberto R. ^[8] ; Barbosa-Filho, Jose M. ^[9] ; Cornelio, Marinonio L. ^[5] ; Oliani, Sonia M. ^[2] ; Tajara, Eloiza H. ^{[1, 4]}

Affiliation

^[1] Sch Med Sao Jose do Rio Preto FAMERP, Dept Mol Biol, Av Brigadeiro Faria Lima 5416, BR-15090000 Sao Jose Do Rio Preto, SP - Brazil

^[2] Sao Paulo State Univ, Dept Biol, UNESP, Inst Biosci Humanities & Exact Sci IBILCE, Campus Sao Jose do Rio Preto, BR-15054000 Sao Jose Do Rio Preto, SP - Brazil

^[3] Integrated Coll Padre Albino Fdn FIPA, BR-15806310 Catanduva, SP - Brazil

^[4] Univ Sao Paulo, Inst Biosci, Dept Genet & Evolut Biol, BR-05508090 Sao Paulo, SP - Brazil

^[5] Sao Paulo State Univ, UNESP, Dept Phys, Inst Biosci Humanities & Exact Sci IBILCE, Campus Sao Jose do Rio Preto, BR-15054000 Sao Jose Do Rio Preto, SP - Brazil

^[6] Univ Fed Alfenas, Inst Chem, Lab Mol Modeling & Comp Simulat MolMod CS, BR-37130001 Alfenas, MG - Brazil

^[7] Oswaldo Cruz Fdn IGM FIOCRUZ BA, Goncalo Moniz Inst, BR-40296710 Salvador, BA - Brazil

^[8] Univ Fed Ceara, Dept Chem, BR-60020181 Fortaleza, Ceara - Brazil

^[9] Univ Fed Paraiba, Lab Pharmaceut Technol, BR-58051900 Joao Pessoa, Paraiba - Brazil

• Document type: Journal article
• Source: SCIENTIFIC REPORTS; v. 10, n. 1 DEC 17 2020.
• Web of Science Citations: 0

Abstract

Chronic inflammation provides a favorable microenvironment for tumorigenesis, which opens opportunities for targeting cancer development and progression. Piplartine (PL) is a biologically active alkaloid from long peppers that exhibits anti-inflammatory and antitumor activity. In the present study, we investigated the physical and chemical interactions of PL with anti-inflammatory compounds and their effects on cell proliferation and migration and on the gene expression of inflammatory mediators. Molecular docking data and physicochemical analysis suggested that PL shows potential interactions with a peptide of annexin A1 (ANXA1), an endogenous anti-inflammatory mediator with therapeutic potential in cancer. Treatment of neoplastic cells with PL alone or with annexin A1 mimic peptide reduced cell proliferation and viability and modulated the expression of MCP-1 chemokine, IL-8 cytokine and genes involved in inflammatory processes. The results also suggested an inhibitory effect of PL on tubulin expression. In addition, PL apparently had no influence on cell migration and invasion at the concentration tested. Considering the role of inflammation in the context of promoting tumor initiation, the present study shows the potential of piplartine as a therapeutic immunomodulator for cancer prevention and progression. (AU)

• FAPESP's process: 16/02012-4 - Evaluation of the immunomodulatory activity of annexin A1 protein in the regulation of inflammatory disorders of the gastrointestinal system: studies in vivo and in vitro experimental models
• Grantee: Sonia Maria Oliani
• Support Opportunities: Regular Research Grants