Methyl-β-cyclodextrin is a cyclic heptasaccharide utilized for delivering hydrophobic agents due to its property of dissolving nonpolar substances. It is also extensively used as a cholesterol-depleting agent[1]. Methyl-β-cyclodextrin possesses multiple biological activities. It significantly reduces clathrin-dependent endocytosis, thus serving as an endocytosis inhibitor[2]. Methyl-β-cyclodextrin inhibits cell migrasome formation[3]. Methyl-β-cyclodextrin is widely used to enhance cell permeability, thereby increasing the uptake of small molecules such as glucose and nanoparticles. In pharmaceutical formulations, Methyl-β-cyclodextrin is utilized to enhance the bioavailability of drugs[4].
Methyl-β-cyclodextrin/甲基-β-环糊精 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HEK293 cells
2 mM
MβCD significantly increased TMEM16A currents
J Adv Res. 2020 Sep 15;29:23-32
Escherichia coli MscS in PC10-doped liposomes
750 μM
within 90 s
Activation of MscS in PC10-doped liposomes, showing lower CD concentration required
Proc Natl Acad Sci U S A. 2021 Sep 7;118(36):e2104820118
WT fibroblasts
100 μM
24 hours
Increased autophagosome formation but did not block autophagy flux
Autophagy. 2017 Aug 3;13(8):1435-1451
NPC1 fibroblasts
100 μM
24 hours
Restored impaired autophagy flux in NPC1 cells and reduced cholesterol accumulation
Autophagy. 2017 Aug 3;13(8):1435-1451
16HBE cells
1, 5, 7.5 mg/mL
1 hour
To investigate the effect of M βCD on hMPV infection, results showed that M βCD significantly reduced hMPV titers in a dose-dependent manner.
J Med Virol. 2019 Jun;91(6):949-957
Gly22Ser mutant MscL
5 mM
within 90 s
Activation of Gly22Ser mutant MscL, showing lower CD concentration required
Proc Natl Acad Sci U S A. 2021 Sep 7;118(36):e2104820118
Escherichia coli MscL
25 mM
within 90 s
Activation of MscL channels, showing CD can activate structurally unrelated mechanosensitive channels
Proc Natl Acad Sci U S A. 2021 Sep 7;118(36):e2104820118
Gly113Ala mutant MscS in PE18:1-doped liposomes
5 mM
within 90 s
Activation of Gly113Ala mutant MscS in PE18:1-doped liposomes, showing lower CD concentration required
Proc Natl Acad Sci U S A. 2021 Sep 7;118(36):e2104820118
Escherichia coli MscS in PE18:1-doped liposomes
15 mM
within 90 s
Activation of MscS in PE18:1-doped liposomes, showing higher CD concentration required
Proc Natl Acad Sci U S A. 2021 Sep 7;118(36):e2104820118
Escherichia coli MscS
10 mM
within 45 s
Activation of MscS channels, mimicking membrane tension
Proc Natl Acad Sci U S A. 2021 Sep 7;118(36):e2104820118
H2228 cells
5 mM
2 hours
Cholesterol depletion enhanced LTβR-dependent activation of the NF-κB pathway, manifested by upregulation of NF-κB target gene expression.
Cell Commun Signal. 2019 Dec 26;17(1):171
HUVEC cells
5 mM
1 hour
Cholesterol depletion potentiated LTβR-dependent activation of the canonical NF-κB pathway, manifested by enhanced degradation of IκBα and increased phosphorylation of RelA.
Cell Commun Signal. 2019 Dec 26;17(1):171
A549 cells
5 mM
1 hour
Cholesterol depletion potentiated LTβR-dependent activation of the canonical NF-κB pathway, manifested by enhanced degradation of IκBα and increased phosphorylation of RelA.
Cell Commun Signal. 2019 Dec 26;17(1):171
Human aortic endothelial cells (HAECs)
10 mM
0–48 h
MβCD increased TMEM16A expression in HAECs
J Adv Res. 2020 Sep 15;29:23-32
A549 cells (FR-α negative)
5 mM
2 hours
Evaluate the effect of FA-M-β-CyD on ATP production. FA-M-β-CyD did not significantly affect ATP production in A549 cells.
Int J Nanomedicine. 2017 Apr 28;12:3433-3446
KB cells (FR-α positive)
5 mM
24 hours
Evaluate the in vitro cytotoxic activity of FA-M-β-CyD in spheroids of KB cells. FA-M-β-CyD showed potent cytotoxic effects on KB cell spheroids, while M-β-CyD had no such effect.
Int J Nanomedicine. 2017 Apr 28;12:3433-3446
human monocyte-derived macrophages (MDMs)
1 mM
30 minutes
Used to disrupt lipid rafts, reversing the exNef-induced trained immunity-specific increase in TNF-α production.
Cell Rep. 2022 Nov 22;41(8):111674
Caco-2 cells
5 mM
1 hour
Inhibition of lipid raft formation, significantly reduced pseudovirion infection
J Med Virol. 2023 Jan;95(1):e28266
A549 cells
5 mM
1 hour
Inhibition of lipid raft formation, significantly reduced pseudovirion infection
J Med Virol. 2023 Jan;95(1):e28266
Methyl-β-cyclodextrin/甲基-β-环糊精 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nu/nu mice
KB cell xenograft model
Intravenous injection
20 mg/kg
Single dose, monitored for 42 days
Evaluate the in vivo antitumor activity of FA-M-β-CyD in KB cell xenografted mice. FA-M-β-CyD significantly inhibited tumor growth without significant side effects.
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