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Neuroactive venom compounds obtained from Phlogiellus bundokalbo as potential leads for neurodegenerative diseases: insights on their acetylcholinesterase and beta-secretase inhibitory activities in vitro
Lopez, Simon Miguel M; Aguilar, Jeremey S; Fernandez, Jerene Bashia B; Lao, Angelic Gayle J; Estrella, Mitzi Rain R; Devanadera, Mark Kevin P; Ramones, Cydee Marie V; Villaraza, Aaron Joseph L; Guevarra Junior, Leonardo A; Santiago-Bautista, Myla R; Santiago, Librado A.
Afiliação
  • Lopez, Simon Miguel M; University of Santo Tomas. Faculty of Pharmacy. Department of Biochemistry. Manila. PH
  • Aguilar, Jeremey S; University of Santo Tomas. Faculty of Pharmacy. Department of Biochemistry. Manila. PH
  • Fernandez, Jerene Bashia B; University of Santo Tomas. Faculty of Pharmacy. Department of Biochemistry. Manila. PH
  • Lao, Angelic Gayle J; s.af
  • Estrella, Mitzi Rain R; University of Santo Tomas. Faculty of Pharmacy. Department of Biochemistry. Manila. PH
  • Devanadera, Mark Kevin P; University of Santo Tomas. Faculty of Pharmacy. Department of Biochemistry. Manila. PH
  • Ramones, Cydee Marie V; University of the Philippines Diliman. College of Science. Institute of Chemistry. Quezon City. PH
  • Villaraza, Aaron Joseph L; University of the Philippines Diliman. College of Science. Institute of Chemistry. Quezon City. PH
  • Guevarra Junior, Leonardo A; University of Santo Tomas. Faculty of Pharmacy. Department of Biochemistry. Manila. PH
  • Santiago-Bautista, Myla R; University of Santo Tomas. Faculty of Pharmacy. Department of Biochemistry. Manila. PH
  • Santiago, Librado A; University of Santo Tomas. Faculty of Pharmacy. Department of Biochemistry. Manila. PH
J. venom. anim. toxins incl. trop. dis ; 27: e20210009, 2021. tab, graf, ilus, mapas
Article em En | LILACS, VETINDEX | ID: biblio-1279406
Biblioteca responsável: BR68.1
ABSTRACT
Spider venom is a rich cocktail of neuroactive compounds designed to prey capture and defense against predators that act on neuronal membrane proteins, in particular, acetylcholinesterases (AChE) that regulate synaptic transmission through acetylcholine (ACh) hydrolysis - an excitatory neurotransmitter - and beta-secretases (BACE) that primarily cleave amyloid precursor proteins (APP), which are, in turn, relevant in the structural integrity of neurons. The present study provides preliminary evidence on the therapeutic potential of Phlogiellus bundokalbo venom against neurodegenerative diseases. Methods Spider venom was extracted by electrostimulation and fractionated by reverse-phase high-performance liquid chromatography (RP-HPLC) and characterized by matrix-assisted laser desorption ionization-time flight mass spectrometry (MALDI-TOF-MS). Neuroactivity of the whole venom was observed by a neurobehavioral response from Terebrio molitor larvae in vivo and fractions were screened for their inhibitory activities against AChE and BACE in vitro. Results The whole venom from P. bundokalbo demonstrated neuroactivity by inducing excitatory movements from T. molitor for 15 min. Sixteen fractions collected produced diverse mass fragments from MALDI-TOF-MS ranging from 900-4500 Da. Eleven of sixteen fractions demonstrated AChE inhibitory activities with 14.34% (± 2.60e-4) to 62.05% (± 6.40e-5) compared with donepezil which has 86.34% (± 3.90e-5) inhibition (p > 0.05), while none of the fractions were observed to exhibit BACE inhibition. Furthermore, three potent fractions against AChE, F1, F3, and F16 displayed competitive and uncompetitive inhibitions compared to donepezil as the positive control. Conclusion The venom of P. bundokalbo contains compounds that demonstrate neuroactivity and anti-AChE activities in vitro, which could comprise possible therapeutic leads for the development of cholinergic compounds against neurological diseases.(AU)
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Texto completo: 1 Base de dados: LILACS / VETINDEX Idioma: En Revista: J. venom. anim. toxins incl. trop. dis Ano de publicação: 2021 Tipo de documento: Article

Texto completo: 1 Base de dados: LILACS / VETINDEX Idioma: En Revista: J. venom. anim. toxins incl. trop. dis Ano de publicação: 2021 Tipo de documento: Article