Amphibian skin extracts as source of bioactive multi-target agents against different pathways of Alzheimer’s disease

Spinelli, Roque; Aimaretti, Florencia María; López, Javier Alejandro; Siano, Álvaro Sebastián

doi:10.1080/14786419.2019.1591396

Cited by 13 publications

(15 citation statements)

References 19 publications

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“…Essentially similar results were found with the skin extracts from the butter frog Leptodactylus latrans, Cei's white-lipped frog Leptodactylus chaquensis, the mustached frog Leptodactylus mystacinus, Hensel's swamp frog Pseudopaludicola falcipes, and the Helvetia dwarf frog Physalaemus santafecinus in the Leptodactylidae family; and that from the twocolored oval frog Elachistocleis bicolor belonging to the Microhylidae [92]. All the skin extracts also exhibited in vitro monoamine oxidase B inhibitory activity and displayed in vitro antioxidant activity [92], suggesting that they may target additional pathways that may be of relevance to the pathophysiology of Alzheimer's disease [85,89].…”

Section: Anti-alzheimer's Compoundssupporting

confidence: 74%

“…For instance, the skin extracts from several South American hylidan species, namely Cordoba´s tree-frog Hypsiboas cordobae (Figure 2), the lesser swimming frog Pseudis minuta, the Montevideo tree frog Boana pulchella, the swimming frog Pseudis platensis, and the dwarf treefrog Dendropsophus nanus displayed encouraging acetylcholinesterase-and butyrylcholinesterase-inhibiting activities in vitro [92,93]. Essentially similar results were found with the skin extracts from the butter frog Leptodactylus latrans, Cei's white-lipped frog Leptodactylus chaquensis, the mustached frog Leptodactylus mystacinus, Hensel's swamp frog Pseudopaludicola falcipes, and the Helvetia dwarf frog Physalaemus santafecinus in the Leptodactylidae family; and that from the twocolored oval frog Elachistocleis bicolor belonging to the Microhylidae [92]. All the skin extracts also exhibited in vitro monoamine oxidase B inhibitory activity and displayed in vitro antioxidant activity [92], suggesting that they may target additional pathways that may be of relevance to the pathophysiology of Alzheimer's disease [85,89].…”

Section: Anti-alzheimer's Compoundsmentioning

confidence: 99%

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Exploring the global animal biodiversity in the search for new drugs -Amphibians

Mans¹,

Pawirodihardjo²,

Djotaroeno³

et al. 2021

J Transl Sci

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Many breakthrough drugs have been developed from plants with medicinal properties on the basis of ethnopharmacological information. In the search for structurally novel and mechanistically unique lead compounds, drug discovery and development progams are now also paying attention to the myriad of bioactive molecules provided by the animal biodiversity. A well-known example emerging from these efforts is the breakthrough angiotensin-converting enzyme inhibitor captopril used for the treatment of hypertension and congestive heart failure. Captopril has been developed as an analogue of bradykinin in the venom of the Brazilian pit viper Bothrops jararaca (Viperidae) following the observation that the latter agent lowered blood pressure by vasodilation. In the mean time, dozens of clinically useful and potentially therapaeutically applicable compounds from animal origin have been identified. The skin gland secretions of amphibians have been refined during millions of years of evolution to highly efficient defensive chemicals. These compounds have remarkable pharmacological activities and may also represent a treasure chest of potentially novel drugs against pathophysiological conditions. This paper addresses the importance of bioactive compounds in the skin secretions of frogs, toads, salamanders, newts, and caecilians, and elaborates on the therapeutic potential of some of them as anti-alzheimer, cardiotonic, antidiabetic, anti-HIV, analgesic, antimicrobial, and antiparasitic compounds.Mans DRA (2020) Exploring the global animal biodiversity in the search for new drugs -Amphibians

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Section: Anti-alzheimer's Compoundssupporting

confidence: 74%

Section: Anti-alzheimer's Compoundsmentioning

confidence: 99%

Exploring the global animal biodiversity in the search for new drugs -Amphibians

Mans¹,

Pawirodihardjo²,

Djotaroeno³

et al. 2021

J Transl Sci

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show abstract

“…[8] Besides their well-known antimicrobial activity, [9][10][11] there is increasing evidence that both complete extracts and isolated peptides from amphibians could modulate different targets involved in neurodegenerative diseases such as Alzheimer's disease (AD). [12][13][14][15] AD is a complex disease with an intricate etiology, in which low levels of the neurotransmitter acetylcholine (ACh) seem to play a significant role in its pathogenesis. [16] Cholinesterases (ChEs) are a family of enzymes including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), which role is to catalyze the hydrolysis of Ach.…”

Section: Introductionmentioning

confidence: 99%

Toxicity Evaluation of Anti‐cholinesterasic Amphibian Extracts by MTT and an Optimized Artemia salina Test

Spinelli,

Rietmann,

Sanchis

et al. 2024

Chemistry & Biodiversity

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The amphibian skin is an important source of bioactive compounds. Recently, our workgroup reported the bioactivity of new extracts from the Hylidae, Microhylidae and Leptodactylidae families against several pathways involved in Alzheimer’s disease. However, since cytotoxicity can be a limiting factor for their applicability, we evaluated the toxicity of nine amphibian skin extracts with reported anticholinesterase activity, using the traditional MTT assay and an optimized Artemia salina test. The proposed improvement, guided by experimental design, aims to reduce the amount of biological sample needed. Overall, we proved that the active extracts were non‐toxic at effective concentration against cholinesterases (AChE/BChE), positioning the amphibian skin as a promising and preliminary safe source of bioactive compounds in the anti‐Alzheimer's treatment. Interestingly, we demonstrated that both toxicity assays can discriminate between toxic and non‐toxic samples. We propose the A. salina bioassay as a reliable and cost‐effective alternative for early toxicity screening.

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“…More than 15 years of intensive research has led to the identi cation of an important number of dual inhibitors, where some present positive outcomes in clinical trials(Knez et al 2017). In 2019 we reported the rst study of amphibian extracts with the capability of inhibiting the activity of MAO-B and cholinesterases enzymes(Spinelli et al 2019;Spinelli et al 2021). In this sense, the amphibian peptide BcI-1003 showed the potential to inhibit MAO-B with an IC 50 value of 570.19 ± 8 µM.…”

mentioning

confidence: 99%

Biological Characterization of Natural Peptide BcI-1003 from Boana cordobae (anura): Role in Alzheimer’s Disease and Microbial Infections

Spinelli

Humpola

Sanchís

et al. 2022

Int J Pept Res Ther

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Nature continues to be one of the most important sources of molecules for the development of novel therapeutic agents. The skin of anuran's (frogs and toads) is a rich source of peptides with a great importance in the search of bioactive agents applying to human health. Alzheimer's disease (AD) is a complex disease associated with numerous pathological pathways, making their simultaneous modulation necessary. On the other hand, the increasing bacterial resistance against conventional antibiotics has made it essential to search for new antimicrobial drugs with different modes of action. Here in we report the natural peptide BcI-1003, isolated from Boana cordobae amphibian skin, as an agent capable to act on three key therapeutic targets of AD, inhibiting the activity of BChE (IC 50 = 669 µM) and MAO-B (IC 50 = 570 µM) enzymes, and showing a powerful and rapid antioxidant activity (EC 50 = 7.24 µM). Besides, BcI-1003 showed antimicrobial activity against clinically drug-resistant gram-positive and gram-negative bacterial strains, with MIC values ranging from 8 to 127 µM against Staphylococcus aureus MR-1; S. aureus MR-2 and Escherichia coli MDR-1.

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Amphibian skin extracts as source of bioactive multi-target agents against different pathways of Alzheimer’s disease

Cited by 13 publications

References 19 publications

Exploring the global animal biodiversity in the search for new drugs -Amphibians

Exploring the global animal biodiversity in the search for new drugs -Amphibians

Toxicity Evaluation of Anti‐cholinesterasic Amphibian Extracts by MTT and an Optimized Artemia salina Test

Biological Characterization of Natural Peptide BcI-1003 from Boana cordobae (anura): Role in Alzheimer’s Disease and Microbial Infections

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