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Pharmaceutics
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Bioactive Agents for the Treatment against Tuberculosis
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Bioactive Agents for the Treatment against Tuberculosis

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: closed (20 September 2024) | Viewed by 5285

Special Issue Editor

Dr. Fernando Rogério Pavan

E-Mail Website
Guest Editor
School of Pharmacy, São Paulo State University (UNESP), Araraquara-Jaú Road, Araraquara 148000-903, SP, Brazil
Interests: mycobacterium tuberculosis; new drugs; biological assays; antibiotics; antibiotics resistance
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis (MTB), which has, in the last three years during the COVID-19 pandemic, remained "slightly invisible". The new WHO report indicates the prevalence and a significant increase in active tuberculosis, as well as the incidence of cases of resistance to rifampicin and isoniazid. The World Health Organization indicates that urgent antimycobacterial agents must be studied, as the search for new molecules is still a great challenge.

This Special Issue aims to highlight the application of bioactive agents, synthesized (as biomacromolecules, peptides, conjugates, nanocomposites, etc.) agents, or promising isolates (such as toxins, proteins, lipids, enzymes, etc.) with high pharmacological and therapeutic activity against sensible and multi-drug-resistant MTB. Studies concerning administration methods as well as carriers are accepted Special Issue, as well as those related to their physicochemical characterization studies, pharmacological and enzymological parameters, drug release, biological activity and in vitro and/or in vivo studies. Reviews of current challenges and potential new drugs launched in recent years are also acceptable. It is hoped that the articles published in this Special Issue can solve the current challenges facing society related to the discovery and knowledge of drugs, as well as explore the advances in medicinal chemistry against MTB.

We look forward to receiving your contributions.

Prof. Dr. Fernando Rogério Pavan
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. Pharmaceutics 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

  • antimicrobial activity
  • anti-inflammatory activity
  • biological activity
  • biomacromolecules
  • biomaterials
  • pharmaceutical biotechnology
  • drug delivery
  • infectious diseases
  • nanotechnology
  • pharmacy
  • pharmacology
  • therapeutics
  • toxins
  • venom

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Published Papers (4 papers)

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Research

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16 pages, 2634 KiB  
Article
Derivatives of Pyrimidine Nucleosides Affect Artificial Membranes Enriched with Mycobacterial Lipids
by Olga S. Ostroumova, Svetlana S. Efimova, Polina D. Zlodeeva, Liudmila A. Alexandrova, Dmitry A. Makarov, Elena S. Matyugina, Vera A. Sokhraneva, Anastasia L. Khandazhinskaya and Sergey N. Kochetkov
Pharmaceutics 2024, 16(9), 1110; https://doi.org/10.3390/pharmaceutics16091110 - 23 Aug 2024
Viewed by 507
Abstract
The mechanisms of action of pyrimidine nucleoside derivatives on model lipid membranes of various compositions were studied. A systematic analysis of the tested agents’ effects on the membrane physicochemical properties was performed. Differential scanning microcalorimetry data indicated that the ability of nucleoside derivatives [...] Read more.
The mechanisms of action of pyrimidine nucleoside derivatives on model lipid membranes of various compositions were studied. A systematic analysis of the tested agents’ effects on the membrane physicochemical properties was performed. Differential scanning microcalorimetry data indicated that the ability of nucleoside derivatives to disorder membrane lipids depended on the types of nucleoside bases and membrane-forming lipids. The 5′-norcarbocyclic uracil derivatives were found to be ineffective, while N4-alkylcytidines demonstrated the most pronounced effects, significantly decreasing the dipalmitoylphosphocholine melting temperature and cooperativity of phase transition. The elongation of hydrophobic acyl radicals potentiated the disordering action of N4-alkylcytidines, while an increase in hydrophilicity due to replacing deoxyribose with ribose inhibited this effect. The ability of compounds to form transmembrane pores was also tested. It was found that 5-alkyluridines produced single, ion-permeable pores in phosphatidylglycerol membranes, and that methoxy-mycolic acid and trehalose monooleate potentiated the pore-forming activity of alkyloxymethyldeoxyuridines. The results obtained open up perspectives for the development of innovative highly selective anti-tuberculosis agents, which may be characterized by a low risk of developing drug resistance due to the direct action on the membranes of the pathogen. Full article
(This article belongs to the Special Issue Bioactive Agents for the Treatment against Tuberculosis)
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14 pages, 1662 KiB  
Article
Assessment of the Efficacy of the Antihistamine Drug Rupatadine Used Alone or in Combination against Mycobacteria
by Xirong Tian, Wanli Ma, Buhari Yusuf, Biyi Su, Jinxing Hu and Tianyu Zhang
Pharmaceutics 2024, 16(8), 1049; https://doi.org/10.3390/pharmaceutics16081049 - 7 Aug 2024
Viewed by 793
Abstract
The emergence of drug-resistant mycobacteria has rendered many clinical drugs and regimens ineffective, imposing significant economic and healthcare burden on individuals and society. Repurposing drugs intended for treating other diseases is a time-saving, cost-effective, and efficient approach for identifying excellent antimycobacterial candidates or [...] Read more.
The emergence of drug-resistant mycobacteria has rendered many clinical drugs and regimens ineffective, imposing significant economic and healthcare burden on individuals and society. Repurposing drugs intended for treating other diseases is a time-saving, cost-effective, and efficient approach for identifying excellent antimycobacterial candidates or lead compounds. This study is the first to demonstrate that rupatadine (RTD), a drug used to treat allergic rhinitis, possesses excellent activity against mycobacteria without detectable resistance, particularly Mycobacterium tuberculosis and Mycobacterium marinum, with a minimal inhibitory concentration as low as 3.13 µg/mL. Furthermore, RTD exhibited moderate activity against nonreplicating M. tuberculosis with minimal inhibitory concentrations lower than drugs targeting the cell wall, suggesting that RTD has great potential to be modified and used for the treatment of nonreplicating M. tuberculosis. Additionally, RTD exhibits partial synergistic effects when combined with clofazimine, pretomanid, and TB47 against M. tuberculosis, providing the theoretical foundation for the development of treatment regimens. Transcriptomic profiling leads us to speculate that eight essential genes may be the targets of RTD or may be closely associated with mycobacterial resistance to RTD. In summary, RTD may be a promising hit for further antimycobacterial drug or regimen optimization, especially in the case of nonreplicating mycobacteria. Full article
(This article belongs to the Special Issue Bioactive Agents for the Treatment against Tuberculosis)
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15 pages, 4253 KiB  
Article
TB/FLU-06E Influenza Vector-Based Vaccine in the Complex Therapy of Drug-Susceptible and Drug-Resistant Experimental Tuberculosis
by Anna-Polina S. Shurygina, Natalia V. Zabolotnykh, Tatiana I. Vinogradova, Maria L. Vitovskaya, Marine Z. Dogonadze, Kirill A. Vasilyev, Zhanna V. Buzitskaya, Petr K. Yablonskiy, Dmitriy A. Lioznov and Marina A. Stukova
Pharmaceutics 2024, 16(7), 857; https://doi.org/10.3390/pharmaceutics16070857 - 25 Jun 2024
Viewed by 974
Abstract
The steady rise of drug-resistant tuberculosis (TB), which renders standard therapy regimens ineffective, necessitates the development of innovative treatment approaches. Immunotherapeutic vaccines have the potential to effectively regulate the anti-TB immune response and enhance the efficacy of anti-TB treatment. In the present study, [...] Read more.
The steady rise of drug-resistant tuberculosis (TB), which renders standard therapy regimens ineffective, necessitates the development of innovative treatment approaches. Immunotherapeutic vaccines have the potential to effectively regulate the anti-TB immune response and enhance the efficacy of anti-TB treatment. In the present study, we aimed to evaluate the potency of the mucosal vector vaccine TB/FLU-06E as part of a complex treatment regimen for drug-susceptible (DS) or drug-resistant (DR) tuberculosis in C57BL/6 mice. Incorporating TB/FLU-06E into the treatment protocol significantly increased the effectiveness of therapy for both forms of tuberculosis. It was evidenced by higher survival rates and reduced pulmonary bacterial load (1.83 lg CFU for DS tuberculosis and 0.93 lg CFU for DR tuberculosis). Furthermore, the treatment reduced pathomorphological lesions in the lungs and stimulated the local and systemic T-helper 1 (Th1) and cytotoxic T-lymphocyte (CTL) anti-TB immune responses. Thus, therapeutic immunization with the TB/FLU-06E vaccine significantly enhances the efficacy of tuberculosis treatment, which is particularly important in DR tuberculosis. Full article
(This article belongs to the Special Issue Bioactive Agents for the Treatment against Tuberculosis)
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Review

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24 pages, 3366 KiB  
Review
Advances in Diagnostics and Drug Discovery against Resistant and Latent Tuberculosis Infection
by Christian Shleider Carnero Canales, Jessica Marquez Cazorla, André Henrique Furtado Torres, Eloise T. Monteiro Filardi, Leonardo Delello Di Filippo, Paulo Inácio Costa, Cesar Augusto Roque-Borda and Fernando Rogério Pavan
Pharmaceutics 2023, 15(10), 2409; https://doi.org/10.3390/pharmaceutics15102409 - 30 Sep 2023
Cited by 9 | Viewed by 2363
Abstract
Latent tuberculosis infection (LTBI) represents a subclinical, asymptomatic mycobacterial state affecting approximately 25% of the global population. The substantial prevalence of LTBI, combined with the risk of progressing to active tuberculosis, underscores its central role in the increasing incidence of tuberculosis (TB). Accurate [...] Read more.
Latent tuberculosis infection (LTBI) represents a subclinical, asymptomatic mycobacterial state affecting approximately 25% of the global population. The substantial prevalence of LTBI, combined with the risk of progressing to active tuberculosis, underscores its central role in the increasing incidence of tuberculosis (TB). Accurate identification and timely treatment are vital to contain and reduce the spread of the disease, forming a critical component of the global strategy known as “End TB.” This review aims to examine and highlight the most recent scientific evidence related to new diagnostic approaches and emerging therapeutic treatments for LTBI. While prevalent diagnostic methods include the tuberculin skin test (TST) and interferon gamma release assay (IGRA), WHO’s approval of two specific IGRAs for Mycobacterium tuberculosis (MTB) marked a significant advancement. However, the need for a specific test with global application viability has propelled research into diagnostic tests based on molecular diagnostics, pulmonary immunity, epigenetics, metabolomics, and a current focus on next-generation MTB antigen-based skin test (TBST). It is within these emerging methods that the potential for accurate distinction between LTBI and active TB has been demonstrated. Therapeutically, in addition to traditional first-line therapies, anti-LTBI drugs, anti-resistant TB drugs, and innovative candidates in preclinical and clinical stages are being explored. Although the advancements are promising, it is crucial to recognize that further research and clinical evidence are needed to solidify the effectiveness and safety of these new approaches, in addition to ensuring access to new drugs and diagnostic methods across all health centers. The fight against TB is evolving with the development of more precise diagnostic tools that differentiate the various stages of the infection and with more effective and targeted treatments. Once consolidated, current advancements have the potential to transform the prevention and treatment landscape of TB, reinforcing the global mission to eradicate this disease. Full article
(This article belongs to the Special Issue Bioactive Agents for the Treatment against Tuberculosis)
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