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7.4
4.1
Journals
Microorganisms
Special Issues
Development of New Drugs to Treat Infectious Diseases
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Development of New Drugs to Treat Infectious Diseases

A special issue of Microorganisms (ISSN 2076-2607). This special issue belongs to the section "Antimicrobial Agents and Resistance".

Deadline for manuscript submissions: 15 March 2025 | Viewed by 509

Special Issue Editor

Dr. Valnês da Silva Rodrigues-Junior

E-Mail Website
Guest Editor
Department of Pharmaceutical Sciences, Universidade Federal da Paraíba, João Pessoa, Brazil
Interests: infectious diseases; drug development; mycobacteriology

Special Issue Information

Dear Colleagues,

Infectious diseases constitute a serious global health concern. The increasing prevalence and spread of antimicrobial resistance, high mortality rates in hospital-acquired infections, and lack of adequate treatments for several “neglected tropical diseases”, particularly in developing countries, are points that deserve special attention from the international scientific community and the World Health Organization. Furthermore, the COVID-19 pandemic has highlighted the importance of advancing studies for developing novel prophylactic and therapeutic strategies for viral infections. In this context, it is essential to develop new effective and safe pharmacological therapies to treat infections caused by viruses, bacteria, fungi, and protozoa. This Special Issue, entitled "Development of New Drugs to Treat Infectious Diseases", aims to present recent research on different aspects of the field, providing a broad scientific platform for scientists performing fundamental, applied and translational research related to the development of new drugs to treat infectious diseases. Some focal points include, but are not limited to, the following:

  1. Target-based drug discovery and development of novel antimicrobial agents.
  2. Host-directed strategies.
  3. Drug repurposing for infectious diseases.
  4. Natural products as sources of anti-infective compounds.
  5. Target characterization and validation.
  6. Preclinical efficacy studies.
  7. Toxicity investigations.
  8. Pharmacokinetics and pharmacodynamics.
  9. Computational approaches for anti-infective drug design.
  10. Combination therapy strategies. 

Reviews, original research, and communications will be welcome.

Dr. Valnês da Silva Rodrigues-Junior
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. Microorganisms 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 2700 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

  • antimicrobial agents
  • natural products
  • tropical diseases
  • therapeutic strategies
  • viral infections

Benefits of Publishing in a Special Issue

  • Ease of navigation: Grouping papers by topic helps scholars navigate broad scope journals more efficiently.
  • Greater discoverability: Special Issues support the reach and impact of scientific research. Articles in Special Issues are more discoverable and cited more frequently.
  • Expansion of research network: Special Issues facilitate connections among authors, fostering scientific collaborations.
  • External promotion: Articles in Special Issues are often promoted through the journal's social media, increasing their visibility.
  • e-Book format: Special Issues with more than 10 articles can be published as dedicated e-books, ensuring wide and rapid dissemination.

Further information on MDPI's Special Issue policies can be found here.

Published Papers (1 paper)

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Research

29 pages, 6948 KiB  
Article
Host-Mediated Antimicrobial Effects and NLRP3 Inflammasome Modulation by Caulerpin and Its Derivatives in Macrophage Models of Mycobacterial Infections
by Maria Gabriella S. Sidrônio, Maria Eugênia G. Freitas, Daniel W. A. Magalhães, Deyse C. M. Carvalho, Vinícius A. B. Gonçalves, Ana Caroline M. de Queiroz Oliveira, Gisela C. Paulino, Gabriela C. Borges, Rafaelle L. Ribeiro, Natália Ferreira de Sousa, Marcus T. Scotti, Demétrius A. M. de Araújo, Francisco Jaime B. Mendonça-Junior, Kristerson R. de Luna Freire, Sandra Rodrigues-Mascarenhas, Bárbara Viviana de O. Santos and Valnês S. Rodrigues-Junior
Microorganisms 2025, 13(3), 561; https://doi.org/10.3390/microorganisms13030561 - 1 Mar 2025
Viewed by 292
Abstract
Caulerpin, a bis-indole alkaloid isolated from Caulerpa racemosa, has several documented pharmacological activities, including antineoplastic and antiviral properties. This study aimed to evaluate the anti-inflammatory and anti-tubercular potentials of caulerpin and its analogues in RAW 264.7 macrophages infected with Mycobacterium spp. Additionally, [...] Read more.
Caulerpin, a bis-indole alkaloid isolated from Caulerpa racemosa, has several documented pharmacological activities, including antineoplastic and antiviral properties. This study aimed to evaluate the anti-inflammatory and anti-tubercular potentials of caulerpin and its analogues in RAW 264.7 macrophages infected with Mycobacterium spp. Additionally, we evaluated cytokine production and NLRP3 expression in this infection model. Toxicity tests were performed using Vero E6 and HepG2 cell lines and Artemia salina. Pre-incubation of RAW 264.7 cells with caulerpin and its analogues decreased internalized M. smegmatis and M. tuberculosis H37Ra. Furthermore, treatment of M. smegmatis-infected macrophages with caulerpin and its analogues reduced bacterial loads. Caulerpin reduced the CFU count of internalized bacilli in the M. tuberculosis H37Ra infection model. In addition, caulerpin and its diethyl derivative were notably found to modulate IL-1β and TNF-α production in the M. smegmatis infection model after quantifying pro-inflammatory cytokines and NLRP3. Caulerpin and its derivates did not affect the viability of Vero E6 and HepG2 cell lines or nauplii survival in toxicity studies. These findings demonstrate that caulerpin and its analogues exhibit anti-inflammatory activity against Mycobacterium spp. infection in RAW 264.7 macrophages and show promising potential for further efficacy and safety evaluation. Full article
(This article belongs to the Special Issue Development of New Drugs to Treat Infectious Diseases)
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Figure 1

Figure 1
<p>Chemical structure of CP.</p> Full article ">Figure 2
<p>Both 2 and 3 are derivatives of CP (<b>1</b>). Reagents and conditions: (a) <b>2</b>: KOH, Me<sub>2</sub>SO<sub>4</sub>; MeOH, acetone/room temperature, magnetic stirring. (b) <b>3</b>: KOH, acetonitrile: water, 60 °C, magnetic stirring [<a href="#B15-microorganisms-13-00561" class="html-bibr">15</a>].</p> Full article ">Figure 3
<p>Objects 4–7 are derivatives of CP (<b>1</b>). Reagents and conditions: (a) SOCl<sub>2</sub>, ethyl alcohol (<b>4</b>), propyl alcohol (<b>5</b>), isobutyl alcohol (<b>6</b>), amyl alcohol (<b>7</b>), 60 °C, magnetic stirring.</p> Full article ">Figure 4
<p>Effects of CP and analogues on RAW 264.7 cells’ viability after 24 h incubation. CP (<b>A</b>), DE (<b>B</b>), CA (<b>C</b>), DP (<b>D</b>), Diisobutyl (<b>E</b>), <span class="html-italic">N</span>-methyl (<b>F</b>), and Diamyl (<b>G</b>). Control: 0.5% DMSO-treated wells, considered as 100% of cell viability.</p> Full article ">Figure 5
<p>Effects of CP and analogues on RAW 264.7 cells’ viability after 48 h incubation. CP (<b>A</b>), DE (<b>B</b>), CA (<b>C</b>), and DP (<b>D</b>). Control: 0.5% DMSO-treated wells, considered as 100% of cell viability.</p> Full article ">Figure 6
<p>Evaluation of the effects of CP and its analogues on the viability of <span class="html-italic">M. smegmatis</span> bacillus after 24 h incubation. CP (<b>A</b>), DE (<b>B</b>), CA (<b>C</b>), and DP (<b>D</b>). Control: 2.5% DMSO-treated group. *** <span class="html-italic">p</span> &lt; 0.001 and ** <span class="html-italic">p</span> &lt; 0.01 compared to the control. Data were evaluated by ANOVA, followed by Dunnett’s post hoc test, using GraphPad Prism 5.0.</p> Full article ">Figure 7
<p>Effects of CP and its analogues in macrophages infected with <span class="html-italic">M. smegmatis</span>. CP (<b>A</b>), DE (<b>B</b>), CA (<b>C</b>), and DP (<b>D</b>). Control: 0.5% DMSO-treated group. *** <span class="html-italic">p</span> &lt; 0.001 ** <span class="html-italic">p</span> &lt; 0.01 and * <span class="html-italic">p</span> &lt; 0.05 compared to the control group. Data were evaluated by ANOVA, followed by Dunnett’s post hoc test, using GraphPad Prism 5.0.</p> Full article ">Figure 8
<p>Effects of pre-incubation of CP and its analogues with RAW 264.7 infected with <span class="html-italic">M. smegmatis.</span> (<b>A</b>): immediately after 2 h of infection, (<b>B</b>): 12 h after infection. Control: 0.5% DMSO-treated group. *** <span class="html-italic">p</span> &lt; 0.001 and ** <span class="html-italic">p</span> &lt; 0.01 compared to the control group. Data were evaluated by ANOVA, followed by Dunnett’s post hoc test, using GraphPad Prism 5.0.</p> Full article ">Figure 9
<p>Effects of CP and DE on cytokine levels and inflammasome (NLRP3) expression during infection of RAW 264.7 cells with <span class="html-italic">M. smegmatis</span> after 24 h incubation. Control: RAW 264.7 cells only; Infected Control: RAW 264.7 cells infected with <span class="html-italic">M. smegmatis</span> (MOI 1:1). CP: infected cells treated with CP (15 μM); DE: infected cells treated with DE (15 μM). *** <span class="html-italic">p</span> &lt; 0.001, ** <span class="html-italic">p</span> &lt; 0.01 and * <span class="html-italic">p</span> &lt; 0.05 compared to Infected Control; # <span class="html-italic">p</span> &lt; 0.1 compared to Control. Data were analyzed by ANOVA, followed by Tukey’s post hoc test, using GraphPad Prism 5.0. (<b>A</b>) TNF-α production in pg/mL; (<b>B</b>) IL-10 production in pg/mL; (<b>C</b>) IL-1β production in pg/mL; (<b>D</b>) MFI percentage in NLRP3+ cells.</p> Full article ">Figure 10
<p>Evaluation of the effects of CP and its analogues on the viability of <span class="html-italic">M. tuberculosis</span> after 48 h incubation. Control: 2.5% DMSO-treated group. RIF: 0.03 μM. * <span class="html-italic">p</span> &lt; 0.05 compared to the control group. Data were evaluated by ANOVA, followed by Dunnett’s post hoc test, using GraphPad Prism 5.0.</p> Full article ">Figure 11
<p>Effects of CP and its analogues in macrophages infected with <span class="html-italic">M. tuberculosis</span>. Incubation with CP for 24 h (<b>A</b>). Incubation with DE and CA for 24 h (<b>B</b>) and 48 h (<b>C</b>). Control: 0.5% DMSO-treated group. * <span class="html-italic">p</span> &lt; 0.05 compared to the control group. Data were evaluated by ANOVA, followed by Dunnett’s post hoc test, using GraphPad Prism 5.0.</p> Full article ">Figure 12
<p>Effects of pre-incubation of CP and its analogues with RAW 264.7 infected with <span class="html-italic">M. tuberculosis.</span> (<b>A</b>): immediately after 3 h of infection, (<b>B</b>): 12 h after infection. Control: 0.5% DMSO-treated group. *** <span class="html-italic">p</span> &lt; 0.001 and * <span class="html-italic">p</span> &lt; 0.05 compared to the control group. Data were evaluated by ANOVA, followed by Dunnett’s post hoc test, using GraphPad Prism 5.0.</p> Full article ">Figure 13
<p>Molecular interaction maps of the CP (<b>A</b>) and DE (<b>B</b>) compounds and Ibuprofen (<b>C</b>). Interactions: Conventional hydrogen interaction (dark green dashed line), carbon–hydrogen interaction (light green dashed line), alkyl interaction (light pink dashed line). Residues: Gln (Glutamine), Ile (Isoleucine), Ser (serine), Pro (Proline), Glu (Glutamic Acid), and Lys (Lysine).</p> Full article ">Figure 14
<p>Molecular interaction maps of the CP (<b>A</b>) and DE (<b>B</b>) compounds and the PDB SC-558 ligand (<b>C</b>). Interactions: Conventional hydrogen interaction (dark green dashed line), carbon–hydrogen interaction (light green dashed line), alkyl and pi–alkyl interaction (light pink dashed line), Pi–Pi T-shaped and Pi–Stacked Amide interaction (dark pink dashed line), Pi–sigma interaction (purple), Pi–sulfur interaction (orange dashed line), unfavorable interaction (red dashed line). Residues: Val (Valine), Tyr (Tyrosine), Ser (serine), Val (Valine), Gly (Glycine), Trp (Tryptophan), Met (Methionine), Leu (Leucine), Ala (Alanine), Arg (Arginine), His (Histidine), Phe (Phenylalanine) and Gln (Glutamine).</p> Full article ">Figure 15
<p>Effects of CP (<b>A</b>), DE (<b>B</b>), and CA (<b>C</b>) on Vero E6 viability after 24 h incubation. Control: 1.5% DMSO-treated group, considered as 100% of cell viability. *** <span class="html-italic">p</span> &lt; 0.001 compared to the control group. Data were evaluated by ANOVA, followed by Dunnett’s post hoc test, using GraphPad Prism 5.0.</p> Full article ">Figure 16
<p>Effects of CP (<b>A</b>), DE (<b>B</b>), and CA (<b>C</b>) on HepG2 viability after 24 h incubation. Control: 1.5% DMSO-treated group, considered as 100% of cell viability. ** <span class="html-italic">p</span> &lt; 0.01 compared to the control group. Data were evaluated by ANOVA, followed by Dunnett’s post hoc test, using GraphPad Prism 5.0.</p> Full article ">Figure 17
<p>Effects of CP (<b>A</b>), DE (<b>B</b>), and CA (<b>C</b>) on <span class="html-italic">A. salina</span> survival after 24 h incubation. Control: 2.5% DMSO-treated group considered as 100% of <span class="html-italic">A. salina</span> survival. *** <span class="html-italic">p</span> &lt; 0.001 ** <span class="html-italic">p</span> &lt; 0.01 compared to the control group. Data were evaluated by ANOVA, followed by Dunnett’s post hoc test, using GraphPad Prism 5.0.</p> Full article ">Figure 18
<p>Summarization of the effects of CP, DE, and CA in RAW 264.7 macrophages infected with <span class="html-italic">Mycobacterium</span> spp.</p> Full article ">
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