Macropinocytosis-Inducible Extracellular Vesicles Modified with Antimicrobial Protein CAP18-Derived Cell-Penetrating Peptides for Efficient Intracellular Delivery.

Noguchi, Kosuke et al.·Molecular pharmaceutics·2021·Preliminary Evidencebasic-research
RPEP-05650Basic ResearchPreliminary Evidence2021RETHINKTHC RESEARCH DATABASErethinkthc.com/research

Quick Facts

Study Type
basic-research
Evidence
Preliminary Evidence
Sample
N=in vitro
Participants
Cell lines (CHO, HeLa, MCF-7; in vitro)

What This Study Found

The dimerized (doubled) form of the CAP18-derived peptide, called (sC18)2, was easily attached to extracellular vesicle (EV) membranes when linked to a fat-loving molecule. Once attached, the peptide triggered macropinocytosis, a process where cells engulf large amounts of surrounding fluid and particles.

This dramatically increased how many EVs got inside target cells. The process depended on glycosaminoglycans (sugar chains on cell surfaces). The team showed this could deliver a functional toxin protein (saporin) that was loaded into the EVs by electroporation.

The saporin-loaded, peptide-modified EVs killed target cells, proving the cargo reached the inside of the cell and was biologically active.

Key Numbers

(sC18)2 peptide modification; glycosaminoglycan-dependent macropinocytosis; saporin toxin delivery confirmed

How They Did This

Researchers modified the (sC18)2 peptide with a hydrophobic (fat-loving) anchor so it would stick to EV membranes. They tested cellular uptake in multiple cell lines (CHO, HeLa, MCF-7). They loaded saporin toxin into EVs by electroporation and measured cell killing to confirm intracellular delivery. They also tested which uptake pathway was responsible using pathway-blocking experiments.

Why This Research Matters

Extracellular vesicles are promising drug delivery vehicles because cells naturally take them up. But uptake is often too low for therapeutic use. This peptide modification solves that problem by forcing cells to gulp in more EVs, opening the door to EV-based delivery of proteins, toxins, or other drugs.

What This Study Doesn't Tell Us

All experiments were done in cell lines in the lab, not in animals or humans. The study did not test whether the peptide-modified EVs cause immune reactions in a living body. Long-term stability of the peptide coating was not assessed. Only one toxin payload was tested.

Trust & Context

Original Title:
Macropinocytosis-Inducible Extracellular Vesicles Modified with Antimicrobial Protein CAP18-Derived Cell-Penetrating Peptides for Efficient Intracellular Delivery.
Published In:
Molecular pharmaceutics, 18(9), 3290-3301 (2021)
Database ID:
RPEP-05650

Evidence Hierarchy

Meta-Analysis / Systematic Review
Randomized Controlled Trial
Cohort / Case-Control
Cross-Sectional / ObservationalSnapshot without intervening
This study
Case Report / Animal Study
What do these levels mean? →

Read More on RethinkPeptides

Cite This Study

RPEP-05650·https://rethinkpeptides.com/research/RPEP-05650

APA

Noguchi, Kosuke; Obuki, Momoko; Sumi, Haruka; Klußmann, Merlin; Morimoto, Kenta; Nakai, Shinya; Hashimoto, Takuya; Fujiwara, Daisuke; Fujii, Ikuo; Yuba, Eiji; Takatani-Nakase, Tomoka; Neundorf, Ines; Nakase, Ikuhiko. (2021). Macropinocytosis-Inducible Extracellular Vesicles Modified with Antimicrobial Protein CAP18-Derived Cell-Penetrating Peptides for Efficient Intracellular Delivery.. Molecular pharmaceutics, 18(9), 3290-3301. https://doi.org/10.1021/acs.molpharmaceut.1c00244

MLA

Noguchi, Kosuke, et al. "Macropinocytosis-Inducible Extracellular Vesicles Modified with Antimicrobial Protein CAP18-Derived Cell-Penetrating Peptides for Efficient Intracellular Delivery.." Molecular pharmaceutics, 2021. https://doi.org/10.1021/acs.molpharmaceut.1c00244

RethinkPeptides

RethinkPeptides Research Database. "Macropinocytosis-Inducible Extracellular Vesicles Modified w..." RPEP-05650. Retrieved from https://rethinkpeptides.com/research/noguchi-2021-macropinocytosisinducible-extracellular-vesicles-modified

Access the Original Study

Study data sourced from PubMed, a service of the U.S. National Library of Medicine, National Institutes of Health.

This study breakdown was produced by the RethinkPeptides research team. We analyze and report published research findings without making health recommendations. All interpretations are based solely on the published abstract and study data.