Publicado
Screening plants from the Brazilian Atlantic Forest identified Nectandra membranacea and Myrciaria strigipes as sources of acetylcholinesterase inhibitors
El análisis de plantas de la Mata Atlántica brasileña identificó a Nectandra membranacea y Myrciaria strigipes como fuentes de inhibidores de la acetilcolinesterasa
A triagem de plantas da Mata Atlântica brasileira identificou Nectandra membranacea e Myrciaria strigipes como fontes de inibidores da acetilcolinesterase
DOI:
https://doi.org/10.15446/rcciquifa.v55n3.123502Palabras clave:
Plant extracts, Nectandra membranacea, Myrciaria strigipes, acetylcholinesterase inhibitors, Alzheimer's disease (en)Extractos de plantas, Nectandra membranácea, Myrciaria strigipes, ; inhibidores de la acetilcolinesterasa, enfermedad de Alzheimer (es)
Extratos de plantas, Nectandra membranácea, Myrciaria strigipes, inibidores de acetilcolinesterase, doença de Alzheimer (pt)
Descargas
Introduction: The alkaloids galantamine and rivastigmine, derived from plant species, were recently approved for treating Alzheimer's disease (AD), highlighting the significance of natural products in discovering new acetylcholinesterase inhibitors. Aims: This study investigated the potential of Brazilian Atlantic plant extracts to inhibit acetylcholinesterase. Methods: The extracts were produced by maceration with dichloromethane (DCM) and methanol (MeOH) at a 1:1 (v/v) ratio. Acetylcholinesterase activity was determined using the Ellman quantitative colorimetric assay adapted for 96-well microplates. The most promising extracts were bio-guided fractionated using silica gel column chromatography. Results: This study screened 268 extracts (either aqueous or a mixture of dichloromethane and methanol) from 67 plant species for their ability to inhibit acetylcholinesterase. Consequently, an alkaloid-rich fraction of Nectandra membranacea inhibited 91% of acetylcholinesterase activity at 0.4 mg/mL. Following bio-guided fractionation, an ethyl acetate fraction of Myrciaria strigipes showed 83% inhibition of acetylcholinesterase activity. The phytochemical profile of the ethyl acetate fraction from M. strigipes revealed the presence of triterpenes, flavonoids, and phenolic compounds. Conclusion: Creating extract-based libraries remains an effective strategy for identifying new plant species and their bioactive compounds that inhibit acetylcholinesterase.
Introducción: Los alcaloides galantamina y rivastigmina, derivados de especies vegetales, fueron aprobados recientemente para el tratamiento de la enfermedad de Alzheimer (EA), destacando la importancia de los productos naturales en el descubrimiento de nuevos inhibidores de la acetilcolinesterasa. Objetivos: Este estudio investigó el potencial de extractos de plantas del Atlántico brasileño para inhibir la acetilcolinesterasa. Métodos: Los extractos se obtuvieron por maceración con diclorometano (DCM) y metanol (MeOH) en una proporción 1:1 (v/v). La actividad de la acetilcolinesterasa se determinó mediante el ensayo colorimétrico cuantitativo de Ellman adaptado para microplacas de 96 pocillos. Los extractos más prometedores se fraccionaron guiados por bioensayos mediante cromatografía en columna de gel de sílice. Resultados: Este estudio analizó 268 extractos (ya sean acuosos o mezclas de diclorometano y metanol) de 67 especies vegetales para evaluar su capacidad de inhibir la acetilcolinesterasa. En consecuencia, una fracción rica en alcaloides de Nectandra membranacea inhibió un 91 % de la actividad de la acetilcolinesterasa a 0,4 mg/mL. Tras la fraccionación guiada por bioensayos, una fracción de acetato de etilo de Myrciaria strigipes mostró un 83 % de inhibición de la actividad de la acetilcolinesterasa. El perfil fitoquímico de la fracción de acetato de etilo de M. strigipes reveló la presencia de triterpenos, flavonoides y compuestos fenólicos. Conclusión: La creación de bibliotecas basadas en extractos sigue siendo una estrategia eficaz para identificar nuevas especies vegetales y sus compuestos bioactivos que inhiben la acetilcolinesterasa.
Introdução: Os alcaloides galantamina e rivastigmina, derivados de espécies vegetais, foram recentemente aprovados para o tratamento da doença de Alzheimer (DA), destacando a importância dos produtos naturais na descoberta de novos inibidores da acetilcolinesterase. Objetivos: Este estúdio investigou o potencial de extratos de plantas do Atlântico brasileiro para inibir a acetilcolinesterase. Resultados: Este estudo analisou 268 extratos (seja aquosos, seja uma mistura de diclorometano e metanol) de 67 espécies vegetais para avaliar sua capacidade de inibir a enzima acetilcolinesterase por meio do método colorimétrico de Ellman. Como resultado, uma fração rica em alcaloides de Nectandra membranacea inibiu 91% da atividade da acetilcolinesterase a 0,4 mg/mL. Após uma fracionação guiada por bioensaios, uma fração de acetato de etila de Myrciaria strigipes apresentou taxas de inibição de 83% da atividade da acetilcolinesterase. O perfil fitoquímico da fração de acetato de etila de M. strigipes revelou a presença de triterpenos, flavonoides e compostos fenólicos. Conclusão: a criação de bibliotecas baseadas em extratos continua sendo uma estratégia eficaz para identificar novas espécies vegetais e seus compostos bioativos que inibem a acetilcolinesterase.
Referencias
1. Alzheimer’s Association. Alzheimer’s Disease Facts and Figures (Special Report). Alzheimers Dement. 20(5), 3708–3821 (2024). URL: https://www.alz.org/getmedia/76e51bb6-c003-4d84-8019-e0779d8c4e8d/alzheimers-facts-and-figures.pdf
2. M. Girgin, S. Isik & N. Kantarci-Carsibasi. Proposing novel natural compounds against Alzhei-mer's disease targeting acetylcholinesterase. PLoS One, 18(4), e0284994 (2023). https://doi.org/10.1371/ journal.pone.0284994
3. K. Gajendra, G.K. Pratap, D.V. Poornima, M. Shantaram & G. Ranjita. Natural acetylcholines-terase inhibitors: A multi-targeted therapeutic potential in Alzheimer's disease. European Jour-nal of Medicinal Chemistry Reports, 11, 100154 (2024). https://doi.org/10.1016/j.ejmcr.2024.100154
4. T.G. McCloud. High throughput extraction of plant, marine and fungal specimens for preserva-tion of biologically active molecules. Molecules, 15(7), 4526–4563 (2010). https://doi.org/10.3390/molecules15074526
5. G.G. Conrado, R. da Rosa, R.D. Reis & L.R. Pessa. Building natural product–based libraries for drug discovery: Challenges and opportunities from a Brazilian pharmaceutical industry per-spective. Revista Brasileira de Farmacognosia, 34, 706–721 (2024). https://doi.org/10.1007/s43450-024-00540-9
6. A.A. Almeida, G.D.A. Lima, M.V.R.C. Simão, G.A. Moreia, R.P. Siqueira, A.C. Zanatta, W. Vile-gas, M. Machado-Neves, G.C. Bressan & J.P.V. Leite. Screening of plants from the Brazilian At-lantic Forest led to the identification of Athenaea velutina (Solanaceae) as a novel source of an-timetastatic agentes. International Journal of Experimental Pathology, 101(3–4), 106–121 (2020). https://doi.org/ 10.1111/iep.12351
7. L.A. Rodrigues, A.D.C Almeida, D.C. Gontijo, I.V. Salustiano, A.A. Almeida, G.C. Brandão, A. Ribon & J.P.V. Leite. Antibacterial screening of plants from the Brazilian Atlantic Forest led to the identification of active compounds in Miconia latecrenata (DC.) Naudin. Natural Products Research, 35(24), 5904–5908 (2020). https://doi.org/10.1080/14786419.2020.1802271
8. A.A. Almeida, B.B. Cota, L.A. Rodrigues, L.L. Dutra, M. Kohlhoff, G.C. Bressan, G.C. Brandão & J.P.V. Leite. Withalutin, a new cytotoxic withanolide from Athenaea velutina (Sendtn.) D’Arcy. Natural Products Research, 36(24), 6304–6311 (2022). https://doi.org/10.1080/14786419.2022.2039135
9. L.A. Rodrigues, A.A. Almeida, A.P. Agrizii, N. Pacheco, B.C.R. Carvalho, A.C. Zanatta, M. Kohlhoff, C.M.M.E. Torres, G.C. Bressan & J.P.V. Leite. Cytotoxic screening of plants from the Brazilian Atlantic Forest has led to the identification of Casearia arborea and Sorocea hilarii as sources of antitumor compounds. Natural Products Research, 38(11), 1950–1955 (2023). https://doi.org/10.1080/ 14786419.2023.2225689
10. A.A. Almeida, A.P. Agrizzi, J.P. Mendes, L.A. Rodrigues, J.P.V. Braga, A.R. Páez, R. Augusti, J.O.F. Melo, M.R. Silva, A.d.O. Barros-Ribon & J.P.V. Leite. Screening of plant extracts from the Brazilian Atlantic Forest reveals a fraction rich in sesquiterpenes from Eugenia astringens as a potential antibacterial. Revista Brasileira de Farmacognosia, 35(4), 785–797 (2025). https://doi.org/10.1007/s43450-025-00656-6
11. C. Brühlmann, A. Marston, K. Hostettmann, P.-A. Carrupt & B. Testa. Screening of non‐alkaloidal natural compounds as acetylcholinesterase inhibitors. Chemistry & Biodiversity, 1(6), 819–829 (2004). https://doi.org/10.1002/cbdv.200490064
12. M.T.S. Trevisan & F.V.V. Macedo. Seleção de plantas com atividade anticolinasterase para tra-tamento da doença de Alzheimer [Screening for acetylcholinesterase inhibitors from plants to treat Alzheimer's disease]. Química Nova, 26(3), 301–304 (2003). https://doi.org/10.1590/s0100-40422003000300002
13. A.B. Penido, S.M. De Morais, A.B. Ribeiro, D.R. Alves, A.L.M. Rodrigues, L.H. dos Santos & J.S.A. de Menezes. Medicinal plants from northeastern Brazil against Alzheimer’s disease. Evidence-Based Complementary and Alternative Medicine, 2017, 753673 (2017). https://doi.org/10.1155/2017/1753673
14. A. Bustos-Rangel, J. Muñoz-Cabrera, L. Cuca, G. Arboleda, M. Ávila-Murillo & A.G. Sandoval-Hernández. Neuroprotective and antioxidant activities of Colombian plants against paraquat and C2-ceramide exposure in SH-SY5Y cells. Frontiers in Natural Products, 2, 1169182 (2023). https://doi.org/10.3389/fntpr.2023.1169182
15. M. Chinchilla-Carmona, I. Valerio-Campos, R. Sánchez-Porras, V. Bagnarello-Madrigal, L. Mar-tínez-Esquivel, A. González-Paniagua, J. Alpizar-Cordero, M. Cordero-Villalobos & D. Rodrí-guez-Chaves. Actividad contra Leishmania sp. (Kinetoplastida: Trypanosomatidae) de plantas en una reserva biológica de Costa Rica [Anti-leishmanial activity in plants from a biological re-serve of Costa Rica]. Revista de Biología Tropical, 62(3), 1229–1240 (2014). URL: https://www.scielo.sa.cr/ pdf/rbt/v62n3/a31v62n3.pdf
16. M. Chinchilla-Carmona, I. Valerio-Campos, R. Sánchez-Porras, V. Mora-Chaves, V. Bagnarello-Madrigal, L. Martínez-Esquivel, A. González-Paniagua & J.C. Vanegas. Evaluación in vivo de la actividad antimalárica de 25 plantas provenientes de una Reserva de Conservación Biológica de Costa Rica [In vivo evaluation of the antimalarial activity of 25 plants from a biological con-servation reserve of Costa Rica]. Revista Chilena de Historia Natural, 84(1), 115–123 (2011). URL: https://www.scielo.cl/pdf/rchnat/v84n1/art09.pdf
17. V. Bagnarello-Madrigal, D. Rodríguez-Chaves, J. Alpizar-Cordero, A. Calvo-Vargas, M. Corde-ro-Villalobos, M. Chinchilla-Carmona, I. Valerio-Campos & R. Sánchez-Porras. Antimalarial activity of an alkaloid mixture isolated from the tender leaves of the Nectandra membranacea (Laureaceae). Journal of Life Sciences, 12, 134–140 (2018). https://doi.org/10.17265/1934-7391/2018.03.003
18. J. S. Werka, A.K. Boehme & W.N. Setzer. Biological Activities of essential oils from Monteverde, Costa Rica. Natural Product Communications, 2(12), 1215–1219 (2007). https://doi.org/10.1177/ 1934578x0700201204
19. X. Wu, B. Vogler, W.A. Haber & W.N. Setzer. A phytochemical investigation of Nectandra mem-branacea from Monteverde, Costa Rica. Natural Product Communications, 1(6), 465–468 (2006). https://doi.org/10.1177/1934578x0600100607
20. S.R.F. Moreno, A. Arnobio, J.J. De Carvalho, A.L. Nascimento, M.O. Timoteo, B. Olej, E.K. Rocha, M. Pereira, M. Bernardo-Filho & L.Q.d.A. Caldas. The ingestion of a Nectandra membranacea ex-tract changes the bioavailability of technetium-99m radiobiocomplex in rat organs. Biological Research, 40(2), 131–135 (2007). URL: https://www.scielo.cl/pdf/bres/v40n2/art04.pdf
21. S.R.F. Moreno, J.J. de Carvalho, B. Rebello, E.K. Rocha, M.d.O. Timóteo, B. Olej, M. Bernardo-Filho & L.Q.d.A. Caldas. Experimental models using radionuclides for assessment of the effects of natural drugs. Brazilian Archives of Biology and Technology, 51, 169–174 (2008). https://doi.org/10.1590/ s1516-89132008000700027
22. A. Arnobio, S.R.F. Moreno & L.Q.A. Caldas. Evaluation of the genotoxicity potential of a Nectandra membranacea extract employing in vitro micronucleous test with metabolic activation. Toxicology Letters, 205, S173 (2011). https://doi.org/10.1016/j.toxlet.2011.05.601
23. R.D. Faitanin, J.V.D. Gomes, L.F.T. Menezes, B.G. Brasileiro & C.M. Jamal. Phytochemical screening, cytotoxic and thrombolytic activity evaluation of Myrciaria strigipes O. Berg., Ipo-moea alba L. and Solanum cordifolium Dunal leaves. Pharmacologyonline (Salerno), 3, 131–135 (2015). URL: https://pharmacologyonline.silae.it/files/archives/2015/vol3/PhOL_2015_3_A019_19_23_Faitanin_SIPIC_131_135.pdf
24. R.D. Faitanin, J.V.D. Gomes, P.M. Rodrigues, L.F.T. de Menezes, Á.C. Neto, R.C.R. Gonçalves, R.R. Kitagawa, D. Silveira & C.M. Jamal. Chemical study and evaluation of antioxidant activity and α glucosidase inhibition of Myrciaria strigipes O. Berg. (Myrtaceae). Journal of Applied Pharmaceutical Science, 8(3), 120–125 (2018). https://doi.org/10.7324/japs.2018.8317
25. M.M.L. Azevedo, M.M. Cascaes, G.M.S.P. Guilhon, E.H.A. Andrade, M.d.G.B. Zoghbi, J.K.R. da Silva, L.S. Santos & S.H.M. da Silva. Lupane triterpenoids, antioxidant potential and antimicro-bial activity of Myrciaria floribunda (H. West ex Willd.) O. Berg. Natural Product Research, 33(4), 506–515 (2019). https://doi.org/10.1080/14786419.2017.1402311
26. S. Dall'Acqua. Plant-derived acetylcholinesterase inhibitory alkaloids for the treatment of Alz-heimer's disease. Botanics: Targets and Therapy, 11(3), 19–28 (2013). https://doi.org/10.2147/btat.s17297
27. K.G. Yiannopoulou & S.G. Papageorgiou. Current and future treatments in Alzheimer disease: an update. Journal of Central Nervous System Disease, 12, 1179573520907397 (2020). https://doi.org/ 10.1177/1179573520907397
Dimensions
PlumX
Visitas a la página del resumen del artículo
Descargas
Cómo citar
Licencia
Derechos de autor 2026 Revista Colombiana de Ciencias Químico-Farmacéuticas
Esta obra está bajo una licencia internacional Creative Commons Atribución 4.0.
El Departamento de Farmacia de la Facultad de Ciencias de la Universidad Nacional de Colombia autoriza la fotocopia de artículos y textos para fines de uso académico o interno de las instituciones citando la fuente. Las ideas emitidas por los autores son responsabilidad expresa de estos y no de la revista.
Todo el contenido de esta revista, excepto dónde está identificado, está bajo una Licencia Creative Commons de Atribución 4.0 aprobada en Colombia. Consulte la normativa en: http://co.creativecommons.org/?page_id=13
