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Pharmaceuticals
Special Issues
Bioactive Compounds through Structural Modification of Natural Products
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Bioactive Compounds through Structural Modification of Natural Products

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: closed (30 July 2024) | Viewed by 2237

Special Issue Editor

Prof. Dr. Patricia Fernandes

E-Mail Website
Guest Editor
Laboratory of Pain and Inflammation, Institute of Biomedical Sciences, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil
Interests: pharmacology of pain; inflammation; cancer; natural products
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Pharmacological activity and druggability are two essential factors for drug innovation. The pharmacological activity is indispensable, and the druggability is determined by the physico-chemical, biochemical, pharmacokinetic and safety properties of drugs. Natural products are a rich source of therapeutic drugs. They are unusually featured by structural diversity. The structural modification of natural products should result in a synthesis process ready for industrialization, protect the environment and resources, realize chemical modifications according to the molecular size and complexity of natural products, acquire novel structures through structure–activity relationship analysis, pharmacophore definition, and scaffold hopping. The strategy for structural modification is to increase potency and selectivity, improve physico-chemical, biochemical and pharmacokinetic properties, eliminate or reduce side effects, and attain intellectual properties. This Special Issue will focus on papers showing data with new molecules obtained after molecular modifications in natural products, on the synthesis and/or biological effects of new compounds designed using medicinal chemistry approaches looking to improve the activities of original molecules obtained from natural products against worldwide diseases, including, but not limited to, neglected diseases, chronic inflammatory diseases, cancer, tropical diseases (malaria, leishmaniosis, dengue, zika), neurological diseases, cancer, and COVID-19.

Dr. Patricia Dias Fernandes
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • cancer
  • COVID-19
  • inflammation
  • inflammatory bowel diseases
  • endometriosis
  • antinociceptive compounds
  • pulmonary inflammation

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Published Papers (2 papers)

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Research

15 pages, 2937 KiB  
Article
Anti-Inflammatory, Antinociceptive, and LC-MS Metabolic Profile from Pseudotrimezia juncifolia (Klatt) Lovo & A. Gil
by Alan Silva Minho, Pamela Gomes de Almeida, Natália Naomi Kato, Ana Laura Macedo Brand, Roberto Fontes Vieira, Rafael Garrett, Norberto Peporine Lopes, Claudia Moraes Rezende and Patricia Dias Fernandes
Pharmaceuticals 2024, 17(8), 1101; https://doi.org/10.3390/ph17081101 - 22 Aug 2024
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Abstract
Pseudotrimezia juncifolia (Klatt) Lovo & A. Gil (Iridaceae) is a popularly known species with primarily ornamental economic interest. It has traditional uses as purgative, in conditions related to the menstrual cycle, for blood purification, as wound healing, and as anti-inflammatory. The anti-inflammatory and [...] Read more.
Pseudotrimezia juncifolia (Klatt) Lovo & A. Gil (Iridaceae) is a popularly known species with primarily ornamental economic interest. It has traditional uses as purgative, in conditions related to the menstrual cycle, for blood purification, as wound healing, and as anti-inflammatory. The anti-inflammatory and antinociceptive activities of the decoction from its aerial stems, corms, and stamens are described here with dereplication studies on LC-MS/MS supported by the GNPS platform, where phenolic compounds were annotated and correlated with its biological activity. The decoction was evaluated in chemical (formalin and capsaicin) and thermal (hot plate) induced nociception or carrageenan-induced inflammation in mice. Decoction (at 10, 30, or 100 mg/kg doses) significantly reduced formalin- or capsaicin-induced nociception. All doses also demonstrated an antinociceptive effect in the hot plate model increasing the time the animal spent in responding to thermal signal. Naloxone partially reversed the antinociceptive effect. An anti-inflammatory effect was observed since a reduction in cell migration, protein extravasation interleukin-1, and tumor necrosis factor production induced by carrageenan in the subcutaneous air pouch was quantified. Metabolomic analyses showed a predominance of phenolic substances, mainly flavonoids and chlorogenic acids. The literature showed that these two groups have significant anti-inflammatory and analgesic activity, and chemical data corroborate the pharmacological results observed. Full article
(This article belongs to the Special Issue Bioactive Compounds through Structural Modification of Natural Products)
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18 pages, 2630 KiB  
Article
Agave-Laurate-Bioconjugated Fructans Decrease Hyperinsulinemia and Insulin Resistance, Whilst Increasing IL-10 in Rats with Metabolic Syndrome Induced by a High-Fat Diet
by Angélica Sofía González-Garibay, Georgina Sandoval, Omar Ricardo Torres-González, Blanca Estela Bastidas-Ramírez, Iván Moisés Sánchez-Hernández and Eduardo Padilla-Camberos
Pharmaceuticals 2024, 17(8), 1036; https://doi.org/10.3390/ph17081036 - 6 Aug 2024
Viewed by 1071
Abstract
Metabolic syndrome (MetS) comprises a cluster of metabolic risk factors, which include obesity, hypertriglyceridemia, high blood pressure, and insulin resistance. The purpose of this study was to evaluate the effects of laurate-bioconjugated fructans on pro- and anti-inflammatory cytokines in Wistar rats with MetS [...] Read more.
Metabolic syndrome (MetS) comprises a cluster of metabolic risk factors, which include obesity, hypertriglyceridemia, high blood pressure, and insulin resistance. The purpose of this study was to evaluate the effects of laurate-bioconjugated fructans on pro- and anti-inflammatory cytokines in Wistar rats with MetS induced by a high-fat diet. Laurate-bioconjugated fructans were synthesized with agave fructans, immobilized lipase B, and vinyl laureate as the acylant. Groups were fed a standard diet (NORMAL), a high-fat diet (HFD), or a high-fat diet plus laurate-bioconjugated fructans (FL PREV) for 9 weeks. A fourth group received a high-fat diet for 6 weeks, followed by simultaneous exposure to a high-fat diet and laurate-bioconjugated fructans for 3 additional weeks (FL REV). The dose of laurate-bioconjugated fructans was 130 mg/kg. Laurate-bioconjugated fructans reduced food and energy intake, body weight, body mass index, abdominal circumference, adipose tissue, adipocyte area, serum triglycerides, insulin, insulin resistance, and C-reactive protein but they increased IL-10 protein serum levels and mRNA expression. The impact of laurate-bioconjugated fructans on zoometric and metabolic parameters supports their potential as therapeutic agents to improve obesity, obesity comorbidities, insulin resistance, type 2 diabetes mellitus, and MetS. Full article
(This article belongs to the Special Issue Bioactive Compounds through Structural Modification of Natural Products)
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