Efavirenz Repurposing Challenges: A Novel Nanomicelle-Based Antiviral Therapy Against Mosquito-Borne Flaviviruses DOI Creative Commons
Sara Maldonado,

Pedro Fuentes,

Ezequiel Bernabeu

и другие.

Pharmaceutics, Год журнала: 2025, Номер 17(2), С. 241 - 241

Опубликована: Фев. 12, 2025

Background/Objective: World Health Organization latest statistics state that 17% of infectious diseases are transmitted by vectors, causing more than 700,000 deaths each year. Particularly, dengue (DENV), Zika (ZIKV) and yellow fever (YFV) viral infections have generated international awareness due to their epidemic proportion risks spread. In this framework, the repositioning strategy Efavirenz (EFV) represents a key clinical feature improve different antiviral therapies. Therefore, development Soluplus®-based nanomicelles (NMs) loaded with EFV (10 mg/mL) for optimized oral pharmacotherapy against ZIKV, DENV YFV was investigated. Methods: EFV-NMs were obtained an acetone diffusion technique. Micellar size in vitro micellar interaction mucin assessed dynamic light scattering. cytocompatibility investigated A549 Vero cells activity evaluated. vivo bioavailability histological studies Wistar rats. Results: encapsulation within Soluplus® NMs increased drug's apparent aqueous solubility up 4803-fold unimodal distribution ~90 nm at 25 37 °C. also pH range 1.2-7.5 its storage physicochemical stability 4 °C confirmed over 2 years. assays dispersions resulted safe nanoformulations. Interestingly, EFV-loaded exhibited significantly higher compared solution all tested flaviviruses. addition, selectivity index (SI) values reveal considerably biological efficacy cell lines infection (SI > 10). Further, drug pharmacokinetics parameters enhanced after administration NMs, being biocompatible not damage gastrointestinal segments. Conclusions: Overall, our nanoformulation highlighted potential as novel delivery platform therapy.

Язык: Английский

Bioprospecting of Natural Compounds for Industrial and Medical Applications DOI
Sameer Dixit, Akanchha Shukla, Vinayak Singh

и другие.

Опубликована: Июнь 25, 2021

Bioprospecting is the investigation of biodiversity to search new resources commercial value. The bioprospecting program includes scientific and economic activities that explore genes, organisms, species in diverse habitats ecosystem while safeguarding conservation, traditional knowledge, growth local communities. natural products obtained from have contributed immensely medicinal agricultural fields recently bioremediation, biomimetic engineering, aquaculture, nanotechnology fields. These include pharmaceuticals, industrial chemicals, metabolic pathways, behaviors, materials. They are used as such product development or may be physical blueprints designs leads. Since involves worldwide activities, ethical legal issues also addressed prevent biopiracy other malpractices. In this chapter, we will discuss about bioprospecting, rational processes, their drawbacks, approaches advance utility agricultural, medical,

Язык: Английский

Процитировано

30

Comparison of In Vitro Approaches to Assess the Antibacterial Effects of Nanomaterials DOI Creative Commons
Abdulkader Masri, David M. Brown,

David G. E. Smith

и другие.

Journal of Functional Biomaterials, Год журнала: 2022, Номер 13(4), С. 255 - 255

Опубликована: Ноя. 19, 2022

The antibacterial properties of nanomaterials (NMs) can be exploited in a range consumer products (e.g., wound dressings, food packaging, textiles, medicines). There is also interest the exploitation NMs as treatments for infectious diseases to help combat antibiotic resistance. Whilst activity has been assessed vitro and vivo numerous studies, methodology used very varied. Indeed, while approaches are available assess effect vitro, they have not yet systematically their suitability sensitivity testing NMs. It therefore timely consider what assays should prioritised screen majority existing studies focused on investigating effects exhibited by silver (Ag) employed limited assays. We compared copper oxide (CuO) Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis at various concentrations (12.5–200 µg/mL) using battery tests (well disc diffusion, plate counts—time-kill method, optical density measurement—OD, Alamar Blue live/dead viability assays, quantitative polymerase chain reaction). CuO were most toxic B. E. P. aeruginosa was least sensitive strain. All detected NMs; however, varied sensitivity, time, cost, technical difficulty requirement specialized equipment. In future, we suggest that combination provide robust assessment particular, recommend time-kill OD due greater sensitivity. standard operating protocols developed so harmonised approach.

Язык: Английский

Процитировано

22

Discovery of furopyridine-based compounds as novel inhibitors of Janus kinase 2: In silico and in vitro studies DOI
Utid Suriya, Panupong Mahalapbutr, Athina Geronikaki

и другие.

International Journal of Biological Macromolecules, Год журнала: 2024, Номер 260, С. 129308 - 129308

Опубликована: Янв. 11, 2024

Язык: Английский

Процитировано

5

Potential of supercritical fluid myrtle extracts as an active ingredient and co-preservative for cosmetic and topical pharmaceutical applications DOI Creative Commons
Paula Pereira, Elisabete Muchagato Maurício, Maria Paula Duarte

и другие.

Sustainable Chemistry and Pharmacy, Год журнала: 2022, Номер 28, С. 100739 - 100739

Опубликована: Июнь 11, 2022

This study investigated the applications of a myrtle extract obtained by supercritical fluid extraction (SFE), technique considered environmentally friendly, as possible antimicrobial ingredient in cosmetic and pharmaceutical formulations. The was at 230 bar 45 °C, for 2 h, with flow CO2 0.3 kg h−1. A cosolvent (ethanol) also used, 0.09 extracts thus were tested against seven Gram-positive bacteria one yeast using well diffusion broth dilution techniques. results showed that exhibits good antibacterial activity all strains studied is superior to most those conventional methods. Antifungal present but lesser extent. Cell viability studies carried out exposing HaCat cells range concentrations, from 0.1 μg/mL up 60 24 MTT assay. Salmonella mutagenicity assay applied evaluate antimutagenicity extract. suggest green solvent, CO2, safe could reduce genotoxic damage induced reactive oxygen species (ROSs).

Язык: Английский

Процитировано

19

Construction and characterization of two SARS‐CoV‐2 minigenome replicon systems DOI
Hu Zhang,

D Fischer,

Masahiro Shuda

и другие.

Journal of Medical Virology, Год журнала: 2022, Номер 94(6), С. 2438 - 2452

Опубликована: Фев. 9, 2022

The ongoing COVID-19 pandemic severely impacts global public health and economies. To facilitate research on severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) virology antiviral discovery, a noninfectious viral replicon system operating under biosafety level containment is warranted. We report herein the construction characterization of two SARS-CoV-2 minigenome systems. First, we constructed IVT-CoV2-Rep complementary DNA template to generate messenger RNA (mRNA) with nanoluciferase (NLuc) reporter via in vitro transcription (IVT). mRNA transfection assay demonstrated rapid transient replication variety cell lines, which could be completely abolished by known inhibitors. Our data also suggest that phenotype not due host innate responses. In addition, have developed DNA-launched BAC-CoV2-Rep, supports in-cell as initial template. BAC-CoV2-Rep exhibited much stronger longer signal compared version. found portion NLuc was derived from spliced resistant treatment, especially during early phase after transfection. summary, established systems are suitable for basic research, hold promise stable line development further optimization.

Язык: Английский

Процитировано

17

Multifunctional nanoreactors with nutrient consumption and ROS generation capabilities for antibacterial and skin repair DOI

Han Yang,

Xiang Gu,

Yan Li

и другие.

Journal of Materials Chemistry B, Год журнала: 2022, Номер 10(42), С. 8664 - 8671

Опубликована: Янв. 1, 2022

Bacterial wound infection has brought a serious threat to human health and caused huge economic losses. Attempts develop biomaterials with excellent antibacterial effects are meaningful promote healing. Herein, we report multifunctional nanoreactor nutrient consumption reactive oxygen species (ROS) generation capabilities for skin repair. The was constructed by the encapsulation of glucose oxidase (GOx) into Cu2+-doped zeolite-based imidazole framework (ZIF-8) through one-pot synthesis method. not only consumes nutrients bacteria GOx-driven oxidation reaction, but also generates highly toxic hydroxyl radicals (˙OH) kill via Cu+-mediated Fenton-like reaction. Moreover, Zn2+ released from is capable exhibiting synergistic activity. In addition mediating reactions, Cu2+ promotes angiogenesis accelerate Thus, ability cut off supply starve bacteria, produce ROS healing, enabling it be promising treatment infection.

Язык: Английский

Процитировано

17

Antibiofilm and Immune-Modulatory Activity of Cannabidiol and Cannabigerol in Oral Environments—In Vitro Study DOI Creative Commons
Hernan Garzón, Manuela Loaiza-Oliva, María Cecilia Martínez Pabón

и другие.

Antibiotics, Год журнала: 2024, Номер 13(4), С. 342 - 342

Опубликована: Апрель 9, 2024

To evaluate the in vitro antimicrobial and antibiofilm properties immune modulatory activity of cannabidiol (CBD) cannabigerol (CBG) on oral bacteria periodontal ligament fibroblasts (PLF).

Язык: Английский

Процитировано

4

Total Synthesis of Mycinolide IV and Path‐Scouting for Aldgamycin N DOI Creative Commons
Bart Herlé,

Georg Späth,

Lucas Schreyer

и другие.

Angewandte Chemie International Edition, Год журнала: 2021, Номер 60(14), С. 7893 - 7899

Опубликована: Янв. 15, 2021

Abstract Proof‐of‐concept is provided that a large estate of 16‐membered macrolide antibiotics can be reached by “unified” approach. The key building block was formed on scale an asymmetric vinylogous Mukaiyama aldol reaction; its alkene terminus then converted either into the corresponding methyl ketone Wacker oxidation or chain‐extended aldehyde catalyst‐controlled branch‐selective hydroformylation. These transformations ultimately opened access to two structurally distinct series targets. Notable late‐stage maneuvers comprise rare example ruthenium‐catalyzed redox isomerization 1,3‐enyne‐5‐ol 1,3‐diene‐5‐one derivative, as well elaboration tertiary propargylic alcohol acyloin trans ‐hydrostannation/Chan‐Lam‐type coupling. Moreover, this case study illustrates underutilized possibility forging complex macrolactone rings transesterification under essentially neutral conditions.

Язык: Английский

Процитировано

23

In vitro Inhibition of HIV-1 by Cyclotide-Enriched Extracts of Viola tricolor DOI Creative Commons
Carina Conzelmann, Edin Muratspahić, Nataša Tomašević

и другие.

Frontiers in Pharmacology, Год журнала: 2022, Номер 13

Опубликована: Май 27, 2022

Since viral infectious diseases continue to be a global health threat, new antiviral drugs are urgently needed. A unique class of therapeutic compounds antimicrobial peptides (AMPs). They can found in humans, bacteria and plants. Plants express wide variety such defense as part their innate immune system protect from invading pathogens. Cyclotides non-classical AMPs that share similar structure. Their topology consists circular peptide backbone disulfide bonds. In previous studies they have been attributed range biological activities. To identify novel cyclotides with activity, we established library plant extracts largely consisting cyclotide-rich species screened them inhibitors HIV-1 infection. Subsequent extraction fractionation revealed four cyclotide-containing subfractions Viola tricolor activity. These inhibited infection IC50 values between 0.6 11.2 μg/ml, selectivity indices up 8.1. The identification characterization the determination mechanisms may allow develop agents combat infections. Therefore, represent natural source bioactive molecules prospects for development therapeutics.

Язык: Английский

Процитировано

15

Overview on Strategies and Assays for Antibiotic Discovery DOI Creative Commons

Anika Rütten,

Teresa Kirchner,

Ewa Maria Musiol-Kroll

и другие.

Pharmaceuticals, Год журнала: 2022, Номер 15(10), С. 1302 - 1302

Опубликована: Окт. 21, 2022

The increase in antibiotic resistance poses a major threat to global health. Actinomycetes, the Gram-positive bacteria of order Actinomycetales, are fertile producers bioactive secondary metabolites, including antibiotics. Nearly two-thirds antibiotics that used for treatment bacterial infections were originally isolated from actinomycetes strains belonging genus Streptomyces. This emphasizes importance discovery. However, identification new antimicrobial compound and exploration its mode action very challenging tasks. Therefore, different approaches enable “detection” an characterization mechanisms leading biological activity indispensable. Beyond bioinformatics tools facilitating biosynthetic gene clusters (BGCs), whole cell-screenings—in which cells exposed actinomycete-derived compounds—are common strategy applied at early stage drug development. More recently, target-based have been established. In this case, candidates tested interactions with usually validated targets. review focuses on bioactivity-based screening methods provides readers overview most relevant assays investigation action. Moreover, article includes examples successful application these suggestions improvement.

Язык: Английский

Процитировано

15