Natural Products as Enzyme Inhibitors

Pereira, David M.; Andrade, Casimiro de; Valentão, Patrı́cia; Andrade, Paula B.

doi:10.1002/9783527805921.ch1

Cited by 6 publications

(4 citation statements)

References 85 publications

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“…In this respect, several inhibitors (tacrine and donepezil for Alzheimer's disease; acarbose and voglibose for type 2 diabetes) have been synthetically developed in an attempt to control the afore‐mentioned ailments. However, most of the current inhibitors are associated with several unpleasant side effects such as gastrointestinal disorders and toxicity [24,25] . Therefore, investigations into novel and safe enzyme inhibitors from natural resources which have clinical relevance have attracted much attention of the scientific community.…”

Section: Introductionmentioning

confidence: 99%

Anti‐Inflammatory, Antioxidant and Enzyme Inhibition Activities in Correlation with Mycochemical Profile of Selected Indigenous Ganoderma spp. from Balkan Region (Serbia)

Rašeta

Popović

Beara

et al. 2020

Chemistry & Biodiversity

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The aim of this research work was to study the bioactivity potentials (antioxidant, anti‐inflammatory, and enzyme inhibitory) of ethanol (EtOH), water (H2O) and chloroform (CHCl3) extracts of G. applanatum, G. lucidum, G. pfeifferi and G. resinaceum as well as their mycochemical profile: the total content of phenolics (TP) and sugars (TS) and LC/MS/MS detection of phenolics. LC/MS/MS profile showed that p‐hydroxybenzoic and protocatechuic acids were mostly found. The highest ABTS and DPPH activities were detected in polar G. applanatum extracts (159.84±0.59 mg TE/g d.w., IC50=0.85±0.30 μg/mL, respectively), while G. resinaceum CHCl3 extract was the most potent in NO assay (IC50=41.21±0.18−81.89±0.81 μg/mL). The highest TP and TS were generally determined in G. applanatum EtOH extracts. Enzyme inhibitory effects were determined in H2O extracts. Generally, CHCl3 extracts showed the most powerful anti‐inflammatory potential. These results suggest that analyzed species are a promising source of bioactive compounds and may be considered as candidates for new food supplements or drug formulations.

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Section: Introductionmentioning

confidence: 99%

Anti‐Inflammatory, Antioxidant and Enzyme Inhibition Activities in Correlation with Mycochemical Profile of Selected Indigenous Ganoderma spp. from Balkan Region (Serbia)

Rašeta

Popović

Beara

et al. 2020

Chemistry & Biodiversity

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“…They are active in chemical defenses against predators (Winters et al., 2022). The bioactive metabolites from nudibranchs display feeding‐deterrent, cytotoxic, and ichthyotoxic properties, have antibacterial and antifungal activities, and also act as pheromones (Benkendorff, 2010; Pereira et al., 2017). Some of compounds such as bis‐tetrahydroisoquinoline‐quinone alkaloids are considered as indicators of the predator–prey relationships (He et al., 2014; Wu et al., 2021).…”

Section: Introductionmentioning

confidence: 99%

Food preferences of two nudibranch species from the South China Sea revealed by fatty acid trophic markers

Komisarenko,

Zhukova

2024

Marine Ecology

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Nudibranchs are mostly predators preying on a variety of invertebrates. The dietary preferences of tropical nudibranchs were studied by the method of fatty acid trophic markers (FATM) in order to for better understanding of their trophic ecology. For this, the fatty acid profiles of two nudibranch species from the South China Sea, Doriprismatica atromarginata (Cuvier, 1804) and Jorunna funebris (Kelaart, 1859), were analyzed and trophic markers were identified. The high level of very long chain fatty acids (from C24 to C28), which are characteristic of sponges, in nudibranchs was evidence of their predation on sponges. However, the distribution of these components differed significantly between the species. The acids 24:2Δ5,9, 25:2Δ5,9, 26:2Δ9,19, and especially 26:2Δ5,9 dominated in D. atromarginata, but were not found in J. funebris that was rich in 28:2Δ5,9 and 28:3Δ5,9,19. The significant differences in the profile of these demospongic acids indicate that these nudibranchs consumed different species of sponges. The similarity between the FATMs of J. funebris and its potential prey, the sponge Xestospongia, confirmed their predator–prey relationship. Doriprismatica atromarginata from different sites along the Vietnam coast had different FATM profiles, which showed this nudibranch as having no any strict food specialization and feeding on various Demospongiae species. The abundance of bacterial FATMs in the nudibranchs suggests the importance of bacteria in their diet. Thus, the FATM method has proven to be useful for identifying the feeding specialization and assessing the effect of food availability on the diet of these tropical nudibranch species.

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“…For this reason, the chemical/metabolic pathways and corresponding products of these organisms have also been subjected to evolutionary pressures. Natural molecules are, for this reason, privileged for their chemical and structural diversity, and for their potential to bind and interact with multiple biological structures and targets, which vastly increases the probability of these molecules exhibiting pharmacological activity [4].…”

Section: Introductionmentioning

confidence: 99%

Structural modification of naturally-occurring phenolics as a strategy for developing cytotoxic molecules towards cancer cells

Olim

Pereira

Fernandes

et al. 2023

Preprint

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Natural products belonging to different chemical classes have been established as a promising source of novel anticancer drugs. Several low molecular weight compounds from the classes of monoterpenes, phenylpropanoids and flavonoids were shown to possess anticancer activities in previous studies. In this work, over 20 semisynthetic derivatives of molecules belonging to these classes, namely thymol, eugenol and 6-hydroxyflavanone were synthesized and tested for their cytotoxicity against two human cancer cell lines, namely gastric adenocarcinoma (AGS cells) and human lung carcinoma (A549 cells). An initial screening based on viability assessment was performed in order to identify the most cytotoxic compounds at 100 μM. The results evidenced that two 6-hydroxyflavanone derivatives were the most cytotoxic among the compounds tested, being selected for further studies. Noteworthy, in a general way some of the derivatives synthesized displayed enhanced toxicity when compared with their natural counterparts. Moreover, LDH assay showed that the loss of cell viability was not accompanied by a loss of membrane integrity, thus ruling out a necrotic process. Morphological studies with AGS cells demonstrated chromatin condensation compatible with apoptosis, confirmed by the activation of caspase 3/7. Furthermore, a viability assay on non-cancer human embryonic lung fibroblast cell line (MRC-5) confirmed these two derivatives possess selective anticancer activity.

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Natural Products as Enzyme Inhibitors

Cited by 6 publications

References 85 publications

Anti‐Inflammatory, Antioxidant and Enzyme Inhibition Activities in Correlation with Mycochemical Profile of Selected Indigenous Ganoderma spp. from Balkan Region (Serbia)

Anti‐Inflammatory, Antioxidant and Enzyme Inhibition Activities in Correlation with Mycochemical Profile of Selected Indigenous Ganoderma spp. from Balkan Region (Serbia)

Food preferences of two nudibranch species from the South China Sea revealed by fatty acid trophic markers

Structural modification of naturally-occurring phenolics as a strategy for developing cytotoxic molecules towards cancer cells

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