ArticleScientific reports2018
Pharmacokinetic parameters explain the therapeutic activity of antimicrobial agents in a silkworm infection model.
Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 32 citations in OpenAlex.
- Review
- Silkworm model of bacterial infection facilitates the identification of lysocin E, a potent, ultra-rapid bactericidal antibiotic.The Journal of antibiotics · 2024Review
- Self-emulsifying micelles as a drug nanocarrier system for itraconazole oral bioavailability enhancement;Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2023Article
- Article
- AInsects · 2022Article
- Silkworm model forVirulence · 2021Article
- Article
- Pharmacokinetic evaluation of Chalcone derivatives with antimalarial activity in New Zealand White Rabbits.BMC research notes · 2021Article
- Direct Visualization of Fungal Burden in Filamentous Fungus-Infected Silkworms.Journal of fungi (Basel, Switzerland) · 2021Article
- A novel silkworm infection model with fluorescence imaging using transgenic Trichosporon asahii expressing eGFP.Scientific reports · 2020Article
- A Silkworm Infection Model for In Vivo Study of Glycopeptide Antibiotics.Antibiotics (Basel, Switzerland) · 2020Article
Corrections and comments
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Authors and funding
6 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Poor pharmacokinetic parameters are a major reason for the lack of therapeutic activity of some drug candidates. Determining the pharmacokinetic parameters of drug candidates at an early stage of development requires an inexpensive animal model with few associated ethical issues. In this study, we used the silkworm infection model to perform structure-activity relationship studies of an antimicrobial agent, GPI0039, a novel nitrofuran dichloro-benzyl ester, and successfully identified compound 5, a nitrothiophene dichloro-benzyl ester, as a potent antimicrobial agent with superior therapeutic activity in the silkworm infection model. Further, we compared the pharmacokinetic parameters of compound 5 with a nitrothiophene benzyl ester lacking chlorine, compound 7, that exerted similar antimicrobial activity but had less therapeutic activity in silkworms, and examined the metabolism of these antimicrobial agents in human liver fractions in vitro. Compound 5 had appropriate pharmacokinetic parameters, such as an adequate half-life, slow clearance, large area under the curve, low volume of distribution, and long mean residence time, compared with compound 7, and was slowly metabolized by human liver fractions. These findings suggest that the therapeutic effectiveness of an antimicrobial agent in the silkworms reflects appropriate pharmacokinetic properties.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.