Purification, Characterization and Evaluation of the Antitumoral Activity of a Phospholipase A2 from the Snake Bothrops moojeni

Frihling, Breno Emanuel Farias; Boleti, Ana Paula de Araújo; Oliveira, Caio Fernando Ramalho de; Sanches, Simone Camargo; Oliveira, Pedro Henrique Cardoso; Verbisck, Newton V.; Macedo, Maria Lígia Rodrigues; Rita, Paula Helena Santa; Carvalho, Cristiano Marcelo Espínola; Migliolo, Ludovico

doi:10.3390/ph15060724

Cited by 8 publications

(4 citation statements)

References 46 publications

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“…Another example is aurein peptides 1.2 and 3.1 from Litoria sp., which showed activity against the NCI cancer cell line, with LC 50 values of 4 and 10 μM, respectively [ 67 ]. Furthermore, data on RD cells and peptides are scarce in the literature nonetheless, recent studies have shown that phospholipase (BmPLA2) from Bothrops moojeni demonstrated an IC 50 of ~0.14 μM [ 68 ].…”

Section: Discussionmentioning

confidence: 99%

Evaluation of the Synthetic Multifunctional Peptide Hp-MAP3 Derivative of Temporin-PTa

Silva

Guindo

Oliveira

et al. 2023

Toxins

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In recent years, antimicrobial peptides isolated from amphibian toxins have gained attention as new multifunctional drugs interacting with different molecular targets. We aimed to rationally design a new peptide from temporin-PTa. Hp-MAP3 (NH2-LLKKVLALLKKVL-COOH), net charge (+4), hydrophobicity (0.69), the content of hydrophobic residues (69%), and hydrophobic moment (0.73). For the construction of the analog peptide, the physicochemical characteristics were reorganized into hydrophilic and hydrophobic residues with the addition of lysines and leucines. The minimum inhibitory concentration was 2.7 to 43 μM against the growth of Gram-negative and positive bacteria, and the potential for biofilm eradication was 173.2 μM. Within 20 min, the peptide Hp-MAP3 (10.8 μM) prompted 100% of the damage to E. coli cells. At 43.3 μM, eliminated 100% of S. aureus within 5 min. The effects against yeast species of the Candida genus ranged from 5.4 to 86.6 μM. Hp-MAP3 presents cytotoxic activity against tumor HeLa at a concentration of 21.6 μM with an IC50 of 10.4 µM. Furthermore, the peptide showed hemolytic activity against murine erythrocytes. Structural studies carried out by circular dichroism showed that Hp-MAP3, while in the presence of 50% trifluoroethanol or SDS, an α-helix secondary structure. Finally, Amphipathic Hp-MAP3 building an important model for the design of new multifunctional molecules.

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Section: Discussionmentioning

confidence: 99%

Evaluation of the Synthetic Multifunctional Peptide Hp-MAP3 Derivative of Temporin-PTa

Silva

Guindo

Oliveira

et al. 2023

Toxins

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“…Several studies have demonstrated the conformational changes in hydrophobic or hydrophilic environments for antimicrobial peptides through circular dichroism [ 64 , 65 , 66 ]. The CD analyses show that, in a hydrophobic environment, the conformational preference for Ca-MAP1 was α-helix, indicating that its structure favors the mechanism of action of the membrane permeabilization, as demonstrated in the Sytox Green assay.…”

Section: Discussionmentioning

confidence: 99%

“…Other compounds from animal venom have equal biotechnological importance; the Brazilian snake Bothrops moojeni produces an important phospholipase, A2, which can be collected due to its anticancer effects, at a concentration of 9.2 µM, in many cancers cell lines, including lung mucoepidermoid carcinoma NCI-H292 [ 65 ]. Another example is the wasp and bee venom of the species Vespa velutina , which possess antibacterial activity in Gram-negative and -positive bacteria, and anti-inflammatory activity in LPS-induced BV-2 inflammation at concentrations of 0.5 to 20 µg.mL −1 [ 66 ].…”

Section: Discussionmentioning

confidence: 99%

Evaluation of a Novel Synthetic Peptide Derived from Cytolytic Mycotoxin Candidalysin

Oliveira

Boleti

Silva

et al. 2022

Toxins

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The importance of neuroinflammation in neurology is becoming increasingly apparent. In addition to neuroinflammatory diseases such as multiple sclerosis, the role of neuroinflammation has been identified in many non-inflammatory neurological disorders such as stroke, epilepsy, and cancer. The immune response within the brain involves the presence of CNS resident cells; mainly glial cells, such as microglia, the CNS resident macrophages. We evaluated the peptide Ca-MAP1 bioinspired on the C. albicans immature cytolytic toxin candidalysin to develop a less hemolytic peptide with anti-neuroinflammatory, antibacterial, and cytotoxic activity against tumor cells. In silico and in vitro studies were performed at various concentrations. Ca-MAP1 exhibits low hemolytic activity at lower concentrations and was not cytotoxic to MRC-5 and BV-2 cells. Ca-MAP1 showed activity against Acinetobacter baumannii, Escherichia coli ATCC, E. coli KPC, Klebsiella pneumoniae ATCC, Pseudomonas aeruginosa, and Staphylococcus aureus ATCC. Furthermore, Ca-MAP1 exhibits anti-neuroinflammatory activity in the BV-2 microglia model, with 93.78% inhibition of nitrate production at 18.1 µM. Ca-MAP1 presents cytotoxic activity against tumor cell line NCI-H292 at 36.3 μM, with an IC50 of 38.4 µM. Ca-MAP1 demonstrates results that qualify it to be evaluated in the next steps to promote the control of infections and provide an alternative antitumor therapy.

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“…BmPLA 2 isolated from Bothrops moojeni venom showed anticancer activity against human epithelial colorectal adenocarcinoma (Caco‐2) and human rhabdomyosarcoma (RD) cell lines compared to controls (human fibroblast MRC‐5 and microglia BV‐2 cells) (Frihling et al, 2022). Using the IC 50 of BmPLA 2 against Caco‐2 and the controls, the selectivity index of 1.85 (when compared to MRC‐5) and 6.33 (when compared to BV2) was calculated, suggesting its promise as a potential anti‐tumour agent.…”

Section: Anticancer Effects Of Individual Snake Venom Toxinsmentioning

confidence: 99%

Snake venom toxins: Potential anticancer therapeutics

Offor,

Piater

2023

J of Applied Toxicology

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Snake venom contains a cocktail of compounds dominated by proteins and peptides, which make up the toxin. The toxin components of snake venom attack several targets in the human body including the neuromuscular system, kidney and blood coagulation system and cause pathologies. As such, the venom toxins can be managed and used for the treatment of these diseases. In this regard, Captopril used in the treatment of cardiovascular diseases was the first animal venom toxin‐based drug approved by the US Food and Drug Administration and the European Medicines Agency. Cancers cause morbidity and mortality worldwide. Due to side effects associated with the current cancer treatments including chemotherapy, radiotherapy, immunotherapy, hormonal therapy and surgery, there is a need to improve the efficacy of current treatments and/or develop novel drugs from natural sources including animal toxin‐based drugs. There is a long history of earlier and ongoing studies implicating snake venom toxins as potential anticancer therapies. Here, we review the role of crude snake venoms and toxins including phospholipase A2, L‐amino acid oxidase, C‐type lectin and disintegrin as potential anticancer agents tested in cancer cell lines and animal tumour models in comparison to normal cell lines. Some of the anti‐tumour activities of snake venom toxins include induction of cytotoxicity, apoptosis, cell cycle arrest and inhibition of metastasis, angiogenesis and tumour growth. We thus propose the advancement of multidisciplinary approaches to more pre‐clinical and clinical studies for enhanced bioavailability and targeted delivery of snake venom toxin‐based anticancer drugs.

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Purification, Characterization and Evaluation of the Antitumoral Activity of a Phospholipase A2 from the Snake Bothrops moojeni

Cited by 8 publications

References 46 publications

Evaluation of the Synthetic Multifunctional Peptide Hp-MAP3 Derivative of Temporin-PTa

Evaluation of the Synthetic Multifunctional Peptide Hp-MAP3 Derivative of Temporin-PTa

Evaluation of a Novel Synthetic Peptide Derived from Cytolytic Mycotoxin Candidalysin

Snake venom toxins: Potential anticancer therapeutics

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