Cyclosporin A: Difference between revisions
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{{MitoPedia | {{MitoPedia | ||
|abbr=CsA | |abbr=CsA | ||
|description='''Cyclosporin A''' (CsA) is a cyclic undecapeptide from an extract of soil fungi that binds the cyclophilin D and thus preventing the formation of the mitochondrial permeability transition pore. The interaction of CsA with the cyclophilin D is phosphate mediated but the full mechanism of interaction is not well understood. For example, the deficiency of cyclophilin D in KO models does not prevent mitochondria from permeability transition and from CsA inhibition. Moreover, it is also a is a calcineurin inhibitor and potent immunosuppressive agent used largely as a means of prophylaxis against cellular rejection after solid organ transplantation. | |description='''Cyclosporin A''' (CsA) is a cyclic undecapeptide from an extract of soil fungi that binds the cyclophilin D and thus preventing the formation of the mitochondrial [[PTP|permeability transition pore]]. The interaction of CsA with the cyclophilin D is phosphate mediated but the full mechanism of interaction is not well understood. For example, the deficiency of cyclophilin D in KO models does not prevent mitochondria from permeability transition and from CsA inhibition. Moreover, it is also a is a calcineurin inhibitor and potent immunosuppressive agent used largely as a means of prophylaxis against cellular rejection after solid organ transplantation. | ||
|info= | |info= | ||
}} | }} | ||
__TOC__ | |||
== Application in [[HRR]] == | == Application in [[HRR]] == | ||
{{Chemical_description | |||
|abbr=CsA | |||
|trivial name=Cyclosporin A | |||
|complete name=Antibiotic S 7481F1 | |||
|chem formula=C<sub>62</sub>H<sub>111</sub>N<sub>11</sub>O<sub>12</sub> | |||
|molar mass=1202.61 | |||
|vendor=Sigma-Aldrich | |||
|product number=30024 | |||
|store at=2-8 Β°C | |||
|sensitivity= | |||
|cas=59865-13-3 | |||
|h statements=H302, H350, H360FD | |||
|h info=harmful if swallowed, may cause cancer, may damage fertility, may damage the unborn child. | |||
}}<!--:::'''CsA:Cyclosporin A''' (C<sub>62</sub>H<sub>111</sub>N<sub>11</sub>O<sub>12</sub>); Sigma 30024, 25 mg, store commercial stock at 2-8Β°C; M = 1202.61 gΒ·mol<sup>-1</sup> (β₯ 95%).--> | |||
:::: '''Preparation of 400 Β΅M stock solution''' (dissolved in ethanol abs.) | |||
::::# Weigh 1 mg of CsA and dissolve in 2.11 ml of ethanol abs.. | |||
Β | ::::# Divide in aliquots. Β | ||
::::# Weigh | |||
::::# Divide aliquots. Β | |||
::::# Store frozen at -20 Β°C. | ::::# Store frozen at -20 Β°C. | ||
::: '''O2k manual titrations'''Β [[MiPNet09.12 O2k-Titrations]] | :::Β» '''O2k manual titrations'''Β [[MiPNet09.12 O2k-Titrations]] | ||
::::* Titration volume: 5 | ::::* Titration volume: 5 Β΅L using a 10 Β΅L syringe (2 mL O2k-chamber). | ||
::::* Final concentration: 1 Β΅M. | ::::* Final concentration: 1 Β΅M. | ||
Even if 1 Β΅M is recommended as the working concentration in most of the publications it is highly relevant to test the optimal concentration for your research model. | |||
== Inhibition of | == Inhibition of mtPTP by CsA == | ||
:::* Gainutdinov T, Molkentin JD, Siemen D, Ziemer M, Debska-Vielhaber G, Vielhaber S, Gizatullina Z, Orynbayeva Z, Gellerich FN (2015) Knockout of cyclophilin D in Ppif<sup>-</sup>/<sup>-</sup> mice increases stability of brain mitochondria against Ca<sup>2+</sup> stress. Arch Biochm Biophys 579:40β46. | :::* Gainutdinov T, Molkentin JD, Siemen D, Ziemer M, Debska-Vielhaber G, Vielhaber S, Gizatullina Z, Orynbayeva Z, Gellerich FN (2015) Knockout of cyclophilin D in Ppif<sup>-</sup>/<sup>-</sup> mice increases stability of brain mitochondria against Ca<sup>2+</sup> stress. Arch Biochm Biophys 579:40β46. | ||
:::* Briston T, Roberts M, Lewis S, Powney B, Staddon JM, Szabadkai G, Duchen MR (2017) Mitochondrial permeability transition pore: sensitivity to opening and mechanistic dependence on substrate availability.Β Scientific reportsΒ 7: 10492. | |||
{{MitoPedia concepts}} | {{MitoPedia concepts}} |
Latest revision as of 11:04, 14 June 2022
Description
Cyclosporin A (CsA) is a cyclic undecapeptide from an extract of soil fungi that binds the cyclophilin D and thus preventing the formation of the mitochondrial permeability transition pore. The interaction of CsA with the cyclophilin D is phosphate mediated but the full mechanism of interaction is not well understood. For example, the deficiency of cyclophilin D in KO models does not prevent mitochondria from permeability transition and from CsA inhibition. Moreover, it is also a is a calcineurin inhibitor and potent immunosuppressive agent used largely as a means of prophylaxis against cellular rejection after solid organ transplantation.
Abbreviation: CsA
Application in HRR
- CsA: Cyclosporin A (Antibiotic S 7481F1; C62H111N11O12), Sigma-Aldrich: 30024, store at 2-8 Β°C, CAS: 59865-13-3, M = 1202.61 gΒ·mol-1
- Hazard statements: H302, H350, H360FD; harmful if swallowed, may cause cancer, may damage fertility, may damage the unborn child.
- CsA: Cyclosporin A (Antibiotic S 7481F1; C62H111N11O12), Sigma-Aldrich: 30024, store at 2-8 Β°C, CAS: 59865-13-3, M = 1202.61 gΒ·mol-1
- Preparation of 400 Β΅M stock solution (dissolved in ethanol abs.)
- Weigh 1 mg of CsA and dissolve in 2.11 ml of ethanol abs..
- Divide in aliquots.
- Store frozen at -20 Β°C.
- Β» O2k manual titrations MiPNet09.12 O2k-Titrations
- Titration volume: 5 Β΅L using a 10 Β΅L syringe (2 mL O2k-chamber).
- Final concentration: 1 Β΅M.
Even if 1 Β΅M is recommended as the working concentration in most of the publications it is highly relevant to test the optimal concentration for your research model.
Inhibition of mtPTP by CsA
- Gainutdinov T, Molkentin JD, Siemen D, Ziemer M, Debska-Vielhaber G, Vielhaber S, Gizatullina Z, Orynbayeva Z, Gellerich FN (2015) Knockout of cyclophilin D in Ppif-/- mice increases stability of brain mitochondria against Ca2+ stress. Arch Biochm Biophys 579:40β46.
- Briston T, Roberts M, Lewis S, Powney B, Staddon JM, Szabadkai G, Duchen MR (2017) Mitochondrial permeability transition pore: sensitivity to opening and mechanistic dependence on substrate availability. Scientific reports 7: 10492.
MitoPedia topics: Inhibitor