Transport and metabolism of delta sleep-inducing peptide in cultured human intestinal epithelial cell monolayers.

Augustijns PF, Borchardt RT

Drug metabolism and disposition: the biological fate of chemicals1 Dec 1995Cited by 5 (Europe PMC)

PMID8689946DOI10.1016/s0090-9556(25)06870-9PepBankPUB-08689946

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Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study8

2 results from studies that gave the peptide. No result from this study comes from people.

01LabIn vitro (cells)Pharmacokinetics
When applied to the apical side of Caco-2 monolayers, DSIP was rapidly metabolized, with 8.2% remaining after 2 hours, mainly as Trp.
In plain wordsIn human gut-lining cells in a dish, DSIP was broken down quickly on the apical side, leaving 8.2% after 2 hours.
Peptide
Delta sleep-inducing peptide (DSIP)
Outcome
DecreaseDSIP remaining after 2 h on apical side
Study
humann: not reported in source
Caco-2 human intestinal epithelial cell monolayer
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · 2 hr incubationAs given in this study (human).
Measurements
DSIP remaining
8.2%
apical side, 2 hr
Source sentences
Summary
When applied to the apical (AP) side of Caco-2 cell monolayers, DSIP was rapidly metabolized (8.2 +/- 1.1% remaining after a 2-hr incubation), affording Trp as the major metabolite and Trp-Ala as a minor metabolite.
1 context sentence(design, population, supporting numbers)
Summary · context
A cultured human intestinal epithelial (Caco-2) cell monolayer was used to study the transport and metabolism of delta sleep-inducing peptide [DSIP (Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu)].
Report a problemFND-0868994601
02LabIn vitro (cells)Pharmacokinetics
When added to the basolateral side of Caco-2 monolayers, DSIP gave the same metabolites but was more stable, with 70.6% remaining after 2 hours.
In plain wordsIn human gut-lining cells in a dish, DSIP broke down more slowly on the basolateral side, leaving 70.6% after 2 hours.
Peptide
Delta sleep-inducing peptide (DSIP)
Outcome
DecreaseDSIP remaining after 2 h on basolateral side
Study
humann: not reported in source
Caco-2 human intestinal epithelial cell monolayer
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · 2 hr incubationAs given in this study (human).
Measurements
DSIP remaining
70.6%
basolateral side, 2 hr
Source sentences
Summary
When DSIP was added to the basolateral (BL) side of the monolayer, the same metabolites were detected, but the peptide was more stable (70.6 +/- 3.0% remaining after a 2-hr incubation).
1 context sentence(design, population, supporting numbers)
Summary · context
A cultured human intestinal epithelial (Caco-2) cell monolayer was used to study the transport and metabolism of delta sleep-inducing peptide [DSIP (Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu)].
Report a problemFND-0868994602

Studies that did not test the peptide alone6

In this study, Delta sleep-inducing peptide (DSIP) was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Delta sleep-inducing peptide (DSIP).

03LabNot a test of Delta sleep-inducing peptide (DSIP) aloneIn vitro (cells)Pharmacokinetics
No DSIP was detected on the basolateral side of Caco-2 monolayers, even when the major apical metabolic pathways were inhibited.
In plain wordsIn human gut-lining cells in a dish, no DSIP crossed to the other side, even with the main breakdown routes blocked.
Peptide
Delta sleep-inducing peptide (DSIP)
Outcome
No significant changeDetection of DSIP on basolateral side after apical application
Study
humann: not reported in source
Caco-2 human intestinal epithelial cell monolayer
Outcome group
Pharmacokinetics · Pharmacology
Source sentences
Summary
However, even when the major metabolic pathways were inhibited on the AP side of the cell monolayer, no DSIP was detected on the BL side of a Caco-2 cell monolayer.
1 context sentence(design, population, supporting numbers)
Summary · context
A cultured human intestinal epithelial (Caco-2) cell monolayer was used to study the transport and metabolism of delta sleep-inducing peptide [DSIP (Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu)].
In this study, Delta sleep-inducing peptide (DSIP) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Delta sleep-inducing peptide (DSIP).
Report a problemFND-0868994603
04LabNot a test of Delta sleep-inducing peptide (DSIP) aloneIn vitro (cells)Pharmacokinetics
Bestatin on the apical side increased DSIP stability only slightly but changed the distribution of metabolites, with Trp-Ala becoming the major metabolite.
In plain wordsIn human gut-lining cells in a dish, adding bestatin protected DSIP only slightly but changed which breakdown products formed.
Peptide
Delta sleep-inducing peptide (DSIP)
Outcome
IncreaseEffect of bestatin on DSIP stability and metabolites on apical side
Study
humann: not reported in source
Caco-2 human intestinal epithelial cell monolayer
Outcome group
Pharmacokinetics · Pharmacology
Source sentences
Summary
Inclusion of bestatin, an inhibitor of aminopeptidases, at concentrations up to 0.29 mM with DSIP on the AP side of the Caco-2 cell monolayer increased the stability of the peptide only slightly but dramatically altered the distribution of the metabolites (Trp-Ala became the major metabolite, and Tr…
1 context sentence(design, population, supporting numbers)
Summary · context
A cultured human intestinal epithelial (Caco-2) cell monolayer was used to study the transport and metabolism of delta sleep-inducing peptide [DSIP (Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu)].
In this study, Delta sleep-inducing peptide (DSIP) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Delta sleep-inducing peptide (DSIP).
Report a problemFND-0868994604
05LabNot a test of Delta sleep-inducing peptide (DSIP) aloneIn vitro (cells)Pharmacokinetics
Amastatin, puromycin, diprotin A, Gly-Pro, EDTA, 1,10-phenanthroline or leupeptin alone did not significantly stabilize DSIP in Caco-2 monolayers.
In plain wordsIn human gut-lining cells in a dish, other single enzyme blockers did not significantly protect DSIP from breakdown.
Peptide
Delta sleep-inducing peptide (DSIP)
Outcome
No significant changeEffect of other single protease inhibitors on DSIP stability
Study
humann: not reported in source
Caco-2 human intestinal epithelial cell monolayer
Outcome group
Pharmacokinetics · Pharmacology
Source sentences
Summary
Inclusion of other aminopeptidase inhibitors (e.g. amastatin, puromycin) alone, dipeptidylpeptidase IV inhibitors (e.g. diprotin A, Gly-Pro) alone, inhibitors of proteases that require heavy metals for proper activity (e.g. EDTA, 1,10-phenanthroline) alone, or cysteine protease inhibitors (e.g. leup…
1 context sentence(design, population, supporting numbers)
Summary · context
A cultured human intestinal epithelial (Caco-2) cell monolayer was used to study the transport and metabolism of delta sleep-inducing peptide [DSIP (Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu)].
In this study, Delta sleep-inducing peptide (DSIP) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Delta sleep-inducing peptide (DSIP).
Report a problemFND-0868994605
06LabNot a test of Delta sleep-inducing peptide (DSIP) aloneIn vitro (cells)Pharmacokinetics
Bestatin with diprotin A substantially increased DSIP stability, with 83.2% remaining after 2 hours.
In plain wordsIn human gut-lining cells in a dish, two enzyme blockers together protected DSIP well, leaving 83.2% after 2 hours.
Peptide
Delta sleep-inducing peptide (DSIP)
Outcome
IncreaseDSIP remaining with bestatin plus diprotin A
Study
humann: not reported in source
Caco-2 human intestinal epithelial cell monolayer
Outcome group
Pharmacokinetics · Pharmacology
Measurements
DSIP remaining
83.2%
bestatin 0.29 mM + diprotin A 1 mM, apical, 2 hr
Source sentences
Summary
However, inclusion of a combination of 0.29 mM bestatin and 1 mM diprotin A with DSIP on the AP side of the monolayers resulted in a substantial increase in the stability of the peptide (83.2 +/- 3.7% remaining after a 2-hr incubation).
1 context sentence(design, population, supporting numbers)
Summary · context
A cultured human intestinal epithelial (Caco-2) cell monolayer was used to study the transport and metabolism of delta sleep-inducing peptide [DSIP (Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu)].
In this study, Delta sleep-inducing peptide (DSIP) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Delta sleep-inducing peptide (DSIP).
Report a problemFND-0868994606
07LabNot a test of Delta sleep-inducing peptide (DSIP) aloneIn vitro (cells)Pharmacokinetics
Bestatin, diprotin A and captopril together further increased DSIP stability, with 95.1% remaining after 2 hours.
In plain wordsIn human gut-lining cells in a dish, three enzyme blockers together protected DSIP almost fully, leaving 95.1% after 2 hours.
Peptide
Delta sleep-inducing peptide (DSIP)
Outcome
IncreaseDSIP remaining with bestatin, diprotin A and captopril
Study
humann: not reported in source
Caco-2 human intestinal epithelial cell monolayer
Outcome group
Pharmacokinetics · Pharmacology
Measurements
DSIP remaining
95.1%
bestatin 0.29 mM + diprotin A 1 mM + captopril 1 mM, apical, 2 hr
Source sentences
Summary
Therefore, the stability of DSIP could be further increased (95.1 +/- 1.6% remaining after a 2-hr incubation) by incubating the peptide with 0.29 mM bestatin, 1 mM diprotin A, and 1 mM captopril.
1 context sentence(design, population, supporting numbers)
Summary · context
A cultured human intestinal epithelial (Caco-2) cell monolayer was used to study the transport and metabolism of delta sleep-inducing peptide [DSIP (Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu)].
In this study, Delta sleep-inducing peptide (DSIP) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Delta sleep-inducing peptide (DSIP).
Report a problemFND-0868994607
08LabNot a test of Delta sleep-inducing peptide (DSIP) aloneIn vitro (cells)Pharmacokinetics
In Caco-2 monolayers with bestatin and diprotin A on the apical side, a new DSIP metabolite (Trp-Ala-Gly-Gly-Asp-Ala-Ser) formed, and captopril inhibited its formation.
In plain wordsIn human gut-lining cells in a dish, a new DSIP breakdown product formed when two enzyme blockers were present, and a third blocker stopped it.
Peptide
Delta sleep-inducing peptide (DSIP)
Outcome
DecreaseFormation of a new DSIP metabolite with bestatin plus diprotin A
Study
humann: not reported in source
Caco-2 human intestinal epithelial cell monolayer
Outcome group
Pharmacokinetics · Pharmacology
Source sentences
Summary
However, under these conditions, a new metabolite (Trp-Ala-Gly-Gly-Asp-Ala-Ser) was observed with a formation that could be inhibited by inclusion of 1 mM captopril, an inhibitor of peptidyl dipeptidase A.
In this study, Delta sleep-inducing peptide (DSIP) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Delta sleep-inducing peptide (DSIP).
Report a problemFND-0868994608

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
10 Oct 2026, 08:55 UTC
Study results updated
Version 1
9 Oct 2026, 03:04 UTC
First added · source update from Europe PMC

Subjects

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