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Article: Evolution of the Quinoline Scaffold for the Treatment of Leishmaniasis: A Structural Perspective.

Silva, Carlos F M / Pinto, Diana C G A / Fernandes, Pedro A / Silva, Artur M S

2024 Volume 17, Issue 3

Abstract: Since the beginning of the XXI century, Leishmaniasis has been integrated into the World Health Organization's list of the 20 neglected tropical diseases, being considered a public health issue in more than 88 countries, especially in the tropics, ... ...

Abstract	Since the beginning of the XXI century, Leishmaniasis has been integrated into the World Health Organization's list of the 20 neglected tropical diseases, being considered a public health issue in more than 88 countries, especially in the tropics, subtropics, and the Mediterranean area. Statistically, this disease presents a world prevalence of 12 million cases worldwide, with this number being expected to increase shortly due to the 350 million people considered at risk and the 2-2.5 million new cases appearing every year. The lack of an appropriate and effective treatment against this disease has intensified the interest of many research groups to pursue the discovery and development of novel treatments in close collaboration with the WHO, which hopes to eradicate it shortly. This paper intends to highlight the quinoline scaffold's potential for developing novel antileishmanial agents and provide a set of structural guidelines to help the research groups in the medicinal chemistry field perform more direct drug discovery and development programs. Thus, this review paper presents a thorough compilation of the most recent advances in the development of new quinoline-based antileishmanial agents, with a particular focus on structure-activity relationship studies that should be considerably useful for the future of the field.
Language	English
Publishing date	2024-02-22
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2193542-7
ISSN	1424-8247
ISSN	1424-8247
DOI	10.3390/ph17030285
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Marine-Derived Xanthone from 2010 to 2021: Isolation, Bioactivities and Total Synthesis.

Veríssimo, Ana C S / Pinto, Diana C G A / Silva, Artur M S

Marine drugs

2022 Volume 20, Issue 6

Abstract: Marine life has proved to be an invaluable source of new compounds with significant bioactivities, such as xanthones. This review summarizes the advances made in the study of marine-derived xanthones from 2010 to 2021, from isolation towards synthesis, ... ...

Abstract	Marine life has proved to be an invaluable source of new compounds with significant bioactivities, such as xanthones. This review summarizes the advances made in the study of marine-derived xanthones from 2010 to 2021, from isolation towards synthesis, highlighting their biological activities. Most of these compounds were isolated from marine-derived fungi, found in marine sediments, and associated with other aquatic organisms (sponge and jellyfish). Once isolated, xanthones have been assessed for different bioactivities, such as antibacterial, antifungal, and cytotoxic properties. In the latter case, promising results have been demonstrated. Considering the significant bioactivities showed by xanthones, efforts have been made to synthesize these compounds, like yicathins B and C and the secalonic acid D, through total synthesis.
MeSH term(s)	Anti-Bacterial Agents/pharmacology ; Aquatic Organisms ; Fungi ; Xanthones/pharmacology
Chemical Substances	Anti-Bacterial Agents ; Xanthones
Language	English
Publishing date	2022-05-25
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2175190-0
ISSN	1660-3397 ; 1660-3397
ISSN (online)	1660-3397
ISSN	1660-3397
DOI	10.3390/md20060347
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Article ; Online: Macroalgae Specialized Metabolites: Evidence for Their Anti-Inflammatory Health Benefits.

Rocha, Djenisa H A / Pinto, Diana C G A / Silva, Artur M S

Marine drugs

2022 Volume 20, Issue 12

Abstract: Inflammation is an organism's response to chemical or physical injury. It is split into acute and chronic inflammation and is the last, most significant cause of death worldwide. Nowadays, according to the World Health Organization (WHO), the greatest ... ...

Abstract	Inflammation is an organism's response to chemical or physical injury. It is split into acute and chronic inflammation and is the last, most significant cause of death worldwide. Nowadays, according to the World Health Organization (WHO), the greatest threat to human health is chronic disease. Worldwide, three out of five people die from chronic inflammatory diseases such as stroke, chronic respiratory diseases, heart disorders, and cancer. Nowadays, anti-inflammatory drugs (steroidal and non-steroidal, enzyme inhibitors that are essential in the inflammatory process, and receptor antagonists, among others) have been considered as promising treatments to be explored. However, there remains a significant proportion of patients who show poor or incomplete responses to these treatments or experience associated severe side effects. Seaweeds represent a valuable resource of bioactive compounds associated with anti-inflammatory effects and offer great potential for the development of new anti-inflammatory drugs. This review presents an overview of specialized metabolites isolated from seaweeds with in situ and in vivo anti-inflammatory properties. Phlorotannins, carotenoids, sterols, alkaloids, and polyunsaturated fatty acids present significant anti-inflammatory effects given that some of them are involved directly or indirectly in several inflammatory pathways. The majority of the isolated compounds inhibit the pro-inflammatory mediators/cytokines. Studies have suggested an excellent selectivity of chromene nucleus towards inducible pro-inflammatory COX-2 than its constitutive isoform COX-1. Additional research is needed to understand the mechanisms of action of seaweed's compounds in inflammation, given the production of sustainable and healthier anti-inflammatory agents.
Language	English
Publishing date	2022-12-19
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2175190-0
ISSN	1660-3397 ; 1660-3397
ISSN (online)	1660-3397
ISSN	1660-3397
DOI	10.3390/md20120789
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Article ; Online: Recent

Batista, Vasco F / Pinto, Diana C G A / Silva, Artur M S

Expert opinion on drug discovery

2022 Volume 17, Issue 6, Page(s) 603–618

Abstract: Introduction: Spirocyclic scaffolds are an exceptional tool in drug design, allowing fine-tuning of a molecule's conformational and physicochemical properties. As it expands and diversifies, so does the number of therapeutics that contain this core. ... ...

Abstract	Introduction: Spirocyclic scaffolds are an exceptional tool in drug design, allowing fine-tuning of a molecule's conformational and physicochemical properties. As it expands and diversifies, so does the number of therapeutics that contain this core. Several spirocyclic drugs are already marketed, and considerably more have shown promising results. Areas covered: This review addresses recent Expert opinion: Spirocyclic compounds present an exciting opportunity as an unexplored chemical space in medicinal chemistry. However, their development is hindered by their complexity and synthesis challenges. Furthermore, a clear preference is still seen for readily available spirocyclic compounds involving amine or amide bonds. Nevertheless, these are temporary as high-throughput synthesis, and computational techniques allow fast optimization studies. In our opinion, the field of spirocyclic chemistry will continue to thrive and contribute to drug development, improving activity and selectivity on emergent ailments, such as cancer, metabolic, infectious, and neurological diseases.
MeSH term(s)	Chemistry, Pharmaceutical ; Drug Design ; Drug Discovery/methods ; Humans ; Molecular Conformation ; Spiro Compounds/chemistry ; Spiro Compounds/pharmacology
Chemical Substances	Spiro Compounds
Language	English
Publishing date	2022-03-25
Publishing country	England
Document type	Journal Article ; Review ; Research Support, Non-U.S. Gov't
ZDB-ID	2259618-5
ISSN	1746-045X ; 1746-0441
ISSN (online)	1746-045X
ISSN	1746-0441
DOI	10.1080/17460441.2022.2055544
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Article: Metabolomic Profile of

Magni, Natasha N / Veríssimo, Ana C S / Silva, Helena / Pinto, Diana C G A

Metabolites

2023 Volume 13, Issue 2

Abstract: Salicornia ... ...

Abstract	Salicornia perennis
Language	English
Publishing date	2023-02-15
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2662251-8
ISSN	2218-1989
ISSN	2218-1989
DOI	10.3390/metabo13020280
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Article: Metabolomics as a Tool to Understand Nano-Plant Interactions: The Case Study of Metal-Based Nanoparticles.

Silva, Sónia / Dias, Maria Celeste / Pinto, Diana C G A / Silva, Artur M S

Plants (Basel, Switzerland)

2023 Volume 12, Issue 3

Abstract: Metabolomics is a powerful tool in diverse research areas, enabling an understanding of the response of organisms, such as plants, to external factors, their resistance and tolerance mechanisms against stressors, the biochemical changes and signals ... ...

Abstract	Metabolomics is a powerful tool in diverse research areas, enabling an understanding of the response of organisms, such as plants, to external factors, their resistance and tolerance mechanisms against stressors, the biochemical changes and signals during plant development, and the role of specialized metabolites. Despite its advantages, metabolomics is still underused in areas such as nano-plant interactions. Nanoparticles (NPs) are all around us and have a great potential to improve and revolutionize the agri-food sector and modernize agriculture. They can drive precision and sustainability in agriculture as they can act as fertilizers, improve plant performance, protect or defend, mitigate environmental stresses, and/or remediate soil contaminants. Given their high applicability, an in-depth understanding of NPs' impact on plants and their mechanistic action is crucial. Being aware that, in nano-plant interaction work, metabolomics is much less addressed than physiology, and that it is lacking a comprehensive review focusing on metabolomics, this review gathers the information available concerning the metabolomic tools used in studies focused on NP-plant interactions, highlighting the impact of metal-based NPs on plant metabolome, metabolite reconfiguration, and the reprogramming of metabolic pathways.
Language	English
Publishing date	2023-01-21
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	2704341-1
ISSN	2223-7747
ISSN	2223-7747
DOI	10.3390/plants12030491
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article ; Online: Macroalgae Specialized Metabolites: Evidence for Their Anti-Inflammatory Health Benefits

Rocha, Djenisa H. A. / Pinto, Diana C. G. A. / Silva, Artur M. S.

Mar Drugs. 2022 Dec. 19, v. 20, no. 12

2022

Abstract: Inflammation is an organism’s response to chemical or physical injury. It is split into acute and chronic inflammation and is the last, most significant cause of death worldwide. Nowadays, according to the World Health Organization (WHO), the greatest ... ...

Abstract	Inflammation is an organism’s response to chemical or physical injury. It is split into acute and chronic inflammation and is the last, most significant cause of death worldwide. Nowadays, according to the World Health Organization (WHO), the greatest threat to human health is chronic disease. Worldwide, three out of five people die from chronic inflammatory diseases such as stroke, chronic respiratory diseases, heart disorders, and cancer. Nowadays, anti-inflammatory drugs (steroidal and non-steroidal, enzyme inhibitors that are essential in the inflammatory process, and receptor antagonists, among others) have been considered as promising treatments to be explored. However, there remains a significant proportion of patients who show poor or incomplete responses to these treatments or experience associated severe side effects. Seaweeds represent a valuable resource of bioactive compounds associated with anti-inflammatory effects and offer great potential for the development of new anti-inflammatory drugs. This review presents an overview of specialized metabolites isolated from seaweeds with in situ and in vivo anti-inflammatory properties. Phlorotannins, carotenoids, sterols, alkaloids, and polyunsaturated fatty acids present significant anti-inflammatory effects given that some of them are involved directly or indirectly in several inflammatory pathways. The majority of the isolated compounds inhibit the pro-inflammatory mediators/cytokines. Studies have suggested an excellent selectivity of chromene nucleus towards inducible pro-inflammatory COX-2 than its constitutive isoform COX-1. Additional research is needed to understand the mechanisms of action of seaweed’s compounds in inflammation, given the production of sustainable and healthier anti-inflammatory agents.
Keywords	World Health Organization ; carotenoids ; chronic diseases ; cytokines ; death ; enzymes ; heart ; human health ; inflammation ; macroalgae ; metabolites ; people ; phlorotannins ; sterols ; stroke
Language	English
Dates of publication	2022-1219
Publishing place	Multidisciplinary Digital Publishing Institute
Document type	Article ; Online
ZDB-ID	2175190-0
ISSN	1660-3397
ISSN	1660-3397
DOI	10.3390/md20120789
Database	NAL-Catalogue (AGRICOLA)

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Article: Marine-Derived Xanthone from 2010 to 2021: Isolation, Bioactivities and Total Synthesis

Veríssimo, Ana C. S. / Pinto, Diana C. G. A. / Silva, Artur M. S.

Marine drugs. 2022 May 25, v. 20, no. 6

2022

Abstract	Marine life has proved to be an invaluable source of new compounds with significant bioactivities, such as xanthones. This review summarizes the advances made in the study of marine-derived xanthones from 2010 to 2021, from isolation towards synthesis, highlighting their biological activities. Most of these compounds were isolated from marine-derived fungi, found in marine sediments, and associated with other aquatic organisms (sponge and jellyfish). Once isolated, xanthones have been assessed for different bioactivities, such as antibacterial, antifungal, and cytotoxic properties. In the latter case, promising results have been demonstrated. Considering the significant bioactivities showed by xanthones, efforts have been made to synthesize these compounds, like yicathins B and C and the secalonic acid D, through total synthesis.
Keywords	Scyphozoa ; cytotoxicity ; xanthone
Language	English
Dates of publication	2022-0525
Publishing place	Multidisciplinary Digital Publishing Institute
Document type	Article
ZDB-ID	2175190-0
ISSN	1660-3397
ISSN	1660-3397
DOI	10.3390/md20060347
Database	NAL-Catalogue (AGRICOLA)

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Article: Gall midge Baldratia salicorniae Kieffer, 1897 (Diptera: Cecidomyiidae) infestation on Salicornia europaea L. induces the production of specialized metabolites with biotechnological potential

Ameixa, Olga M.C.C. / Rebelo, João / Silva, Helena / Pinto, Diana C.G.A.

Phytochemistry. 2022 Apr. 09,

2022

Abstract: Saltmarsh plants have several defense mechanisms against threatening abiotic conditions, such as salinity, inundation, or exposure to intense radiation, less is known regarding response to insect pests attack. Salicornia europaea L. plant stands are ... ...

Abstract	Saltmarsh plants have several defense mechanisms against threatening abiotic conditions, such as salinity, inundation, or exposure to intense radiation, less is known regarding response to insect pests attack. Salicornia europaea L. plant stands are produced as cash crops in Portuguese coastal areas. In 2017, these crops suffered significant attacks from a gall midge fly (Baldratia salicorniae Kieffer, 1897), reducing its economic value. To understand how this attack influenced S. europaea chemical composition, infested and non-infested branches were collected, and their extracts were analysed by GS-MS and UHPLC-MS. Results revealed that different degrees of infestations displayed different chemical composition. Several compounds were for the first time identified in S. europaea, such as, arachidic acid, alpha-tocopherol, henicos-1-ene, and squalene. Most evident results were the reduced amount of alkanes in the infested conditions, which seems to be a direct consequence of insect infestation. Several compounds identified in the infested branches are known to have negative effects on insect larvae by reducing larval growth (linoleic acid) or increasing insect mortality (oleic acid). Halophyte plants production is increasing and it is accompanied by the urge to develop early control strategies against potential pests. These strategies may include ecological friendly solutions such as endogenous production of specialized metabolites to retrieve plant self-defences. Further, our results showed that B. salicorniae herbivory also induced the production of higher number of specialized metabolites with important known biological activities. In years in which high infestations reduce organoleptic qualities for fresh consumption plants can be used in biorefinery industries for metabolite extraction.
Keywords	Cecidomyiidae ; Salicornia europaea ; alpha-tocopherol ; biorefining ; chemical composition ; economic valuation ; halophytes ; herbivores ; insect infestations ; larval development ; linoleic acid ; metabolites ; midges ; mortality ; oleic acid ; plant biochemistry ; salinity ; salt marshes ; squalene
Language	English
Dates of publication	2022-0409
Publishing place	Elsevier Ltd
Document type	Article
Note	Pre-press version
ZDB-ID	208884-8
ISSN	1873-3700 ; 0031-9422
ISSN (online)	1873-3700
ISSN	0031-9422
DOI	10.1016/j.phytochem.2022.113207
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: Microwave Irradiation: Alternative Heating Process for the Synthesis of Biologically Applicable Chromones, Quinolones, and Their Precursors.

Albuquerque, Hélio M T / Pinto, Diana C G A / Silva, Artur M S

Molecules (Basel, Switzerland)

2021 Volume 26, Issue 20

Abstract: Microwave irradiation has become a popular heating technique in organic synthesis, mainly due to its short reaction times, solventless reactions, and, sometimes, higher yields. Additionally, microwave irradiation lowers energy consumption and, ... ...

Abstract	Microwave irradiation has become a popular heating technique in organic synthesis, mainly due to its short reaction times, solventless reactions, and, sometimes, higher yields. Additionally, microwave irradiation lowers energy consumption and, consequently, is ideal for optimization processes. Moreover, there is evidence that microwave irradiation can improve the regioselectivity and stereoselectivity aspects of vital importance in synthesizing bioactive compounds. These crucial features of microwave irradiation contribute to its inclusion in green chemistry procedures. Since 2003, the use of microwave-assisted organic synthesis has become common in our laboratory, making our group one of the first Portuguese research groups to implement this heating source in organic synthesis. Our achievements in the transformation of heterocyclic compounds, such as (
MeSH term(s)	Chemistry, Pharmaceutical/methods ; Chromones/chemical synthesis ; Chromones/radiation effects ; Combinatorial Chemistry Techniques/methods ; Enzyme Inhibitors/chemical synthesis ; Heating/methods ; Humans ; Microwaves ; Molecular Structure ; Pyrazoles/chemical synthesis ; Pyrazoles/radiation effects ; Quinolones/chemical synthesis ; Quinolones/radiation effects
Chemical Substances	Chromones ; Enzyme Inhibitors ; Pyrazoles ; Quinolones ; pyrazole (3QD5KJZ7ZJ)
Language	English
Publishing date	2021-10-18
Publishing country	Switzerland
Document type	Journal Article ; Review
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules26206293
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