Aristoforin
Aristoforin, a hypericin derivative, inhibits the activities of SIRT1 and SIRT2. Aristoforin induces G1 phase cell cycle arrest, scavenges hydroxyl free radicals, and exhibits protective activity against Fe2+-induced DNA breakage. Aristoforin can be used in studies related to breast cancer and colon adenocarcinoma.
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- CAS. Nr.: 849215-53-8
- Formel: C37H54O6
- Molecular Weight:594.82
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Speicherung:
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
In Vitro
Aristoforin (24 h) potently inhibits primary human umbilical vein endothelial cell proliferation with a mean IC50 of 3.14 μM[1].
Aristoforin (24 h) potently inhibits primary human dermal lymphatic endothelial cell proliferation with a mean IC50 of 2.54 μM, and completely blocks proliferation at 5 μM[1].
Aristoforin (24 h) potently inhibits primary human lung lymphatic endothelial cell proliferation with a mean IC50 of 2.63 μM[1].
Aristoforin (10-50 μM; 24 h) induces dose-dependent apoptosis in primary human dermal lymphatic endothelial cells, with significant effects observed at concentrations of 10 μM and above, and exhibits greater proapoptotic potency than hyperforin[1].
Aristoforin (5-30 μM; 48 h) induces G1 phase cell cycle arrest in primary human dermal lymphatic endothelial cells at 5 μM, and induces apoptosis (evidenced by increased sub-G1 cells) at 30 μM[1].
Aristoforin (30 μM; 48 h) activates the intrinsic apoptosis pathway in primary human dermal lymphatic endothelial cells at 30 μM, as shown by activation of caspase-3 and caspase-9 without caspase-8 activation[1].
Aristoforin (20 μM; 20 min at 37°C) induces a rapid loss of mitochondrial membrane potential in primary human dermal lymphatic endothelial cells[1].
Aristoforin (1-5 μM; 16 h) alters MRP1, MRP2, BCRP, and P-gp protein levels in human colon adenocarcinoma HT-29 cells in a time- and light-dependent manner, including decreased MRP2 at T0- and T6+, increased MRP1 at T0-, and increased P-gp at T6+ and T6-[2].
Aristoforin (1-5 μM; 16 h) alters CYP3A4 protein levels in human colon adenocarcinoma HT-29 cells in vitro in a concentration-, time-, and light-dependent manner, including increased levels at T0-, T6-, and T6+ (1 μM), and decreased levels at T0+ (5 μM)[2].
Aristoforin (1-5 μM; 16 h) induces BCRP mRNA expression at T0- in human colon adenocarcinoma HT-29 cells[2].
Aristoforin (1-5 μM; 16 h) modulates CYP3A4 mRNA expression in human colon adenocarcinoma HT-29 cells in vitro in a concentration-, time-, and light-dependent manner, including induction at T0+ (1 μM) and T6+ (5 μM), and reduction at T6-[2].
Aristoforin (5-10 μM; 30 min) significantly decreases BCRP activity in human colon adenocarcinoma HT-29 cells, with no significant effect on MRP1 or MRP2 activity[2].
Aristoforin (10 μM; 16 h) significantly decreases CYP3A4 activity in both human colon adenocarcinoma HT-29 cells and Oxaliplatin (HY-17371)-resistant HT-29-OxR cells, independent of light activation[2].
Aristoforin (0.01-10 mM; 25 min) exhibits concentration-dependent DPPH radical scavenging activity, with 5.76%, 12.03%, 17.89%, and 28.02% scavenging at 0.01, 0.1, 1, and 10 mM respectively[3].
Aristoforin (0.01-10 mM; 20 min at 50°C) exhibits very low reducing power, with absorbance values of 0.002, 0.002, 0.068, and 0.085 at 0.01, 0.1, 1, and 10 mM respectively[3].
Aristoforin (0.01-10 mM; 10 min) does not chelate ferrous ions at concentrations ranging from 0.01 to 10 mM[3].
Aristoforin (0.01-1 mM; 90 min at 25°C) exhibits concentration-dependent hydroxyl radical scavenging activity, with 18.18 ± 6.54%, 33.0 ± 2.75%, and 55.84 ± 8.21% scavenging at 0.01, 0.1, and 1 mM respectively[3].
Aristoforin (1-5 μM) at 5 μM, when used as a 16 h pre-incubation followed by 50 nM Hypericin (HY-N0453)-mediated PDT, significantly enhances apoptosis in HT-29 colon adenocarcinoma cells[4].
Aristoforin (1-5 μM) at 5 μM, when used as a 16 h pre-incubation followed by 50 nM Hypericin-mediated PDT, normalizes the cell cycle distribution of HT-29 colon adenocarcinoma cells at 24 h post-PDT, counteracting the S-phase accumulation induced by PDT alone[4].
Aristoforin (1-5 μM) at 5 μM, when used as a 16 h pre-incubation followed by 50 nM hypericin-mediated PDT, significantly suppresses MMP2 and MMP9 expression in HT-29 colon adenocarcinoma cells at 6 h post-PDT[4].
Aristoforin (1-5 μM) at 5 μM, when used as a 16 h pre-incubation followed by 50 nM hypericin-mediated PDT, drastically reduces cellular adhesivity of HT-29 colon adenocarcinoma cells[4].
Aristoforin (1-5 μM) at 5 μM, when used as a 16 h pre-incubation followed by 50 nM hypericin-mediated PDT, potently suppresses clonogenic survival of HT-29 colon adenocarcinoma cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human colon adenocarcinoma HT-29 cells
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Concentration:1 μM; 5 μM
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Incubation Time:16 h
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Result:Decreased MRP2 and BCRP protein levels, and increased MRP1 protein levels at T0- (dark, immediate post-treatment).
Increased MRP2 protein levels, decreased BCRP protein levels, and decreased MRP1 protein levels at T0+ (post-PDT, immediate post-treatment).
Increased MRP2, BCRP, and P-gp protein levels at T6- (dark, 6 h post-treatment).
Decreased MRP2 and BCRP protein levels, and increased P-gp protein levels at T6+ (post-PDT, 6 h post-treatment).\nIncreased CYP3A4 protein levels 2.15-fold (1 μM) and 2.55-fold (5 μM) relative to control at T0- (dark, immediate post-treatment).
Decreased CYP3A4 protein levels 0.74-fold relative to control at T0+ (post-PDT, immediate post-treatment) at 5 μM.
Increased CYP3A4 protein levels 1.11-fold (1 μM) and 1.21-fold (5 μM) relative to control at T6- (dark, 6 h post-treatment).
Increased CYP3A4 protein levels 1.98-fold relative to control at T6+ (post-PDT, 6 h post-treatment) at 1 μM.
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Cell Line:HT-29 colon adenocarcinoma cells
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Concentration:1 μM; 5 μM
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Incubation Time:16 h
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Result:Partially reversed the S-phase accumulation caused by PDT alone, restoring cell cycle distribution to levels similar to untreated control cells when combined with 50 nM hypericin-mediated PDT.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (female)[1]
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Dosage:2 mM (delivered as 100 μL per injection)
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Administration:s.c.; daily; 14 days
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Result:Reduced peritumoral podoplanin-positive lymphatic vessel density significantly compared to DMSO control.
Left tumor volumes equivalent to control groups at the time of sacrifice.
Chemical Information
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CAS. Nr. 849215-53-8
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Molecular Weight 594.82
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Formel C37H54O6
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SMILES
CC(C)C([C@@]12[C@@](C)([C@H](C[C@@](C1=O)(C(OCC(O)=O)=C(C2=O)C/C=C(C)\C)C/C=C(C)\C)C/C=C(C)\C)CC/C=C(C)/C)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Rothley M, et al. Hyperforin and aristoforin inhibit lymphatic endothelial cell proliferation in vitro and suppress tumor-induced lymphangiogenesis in vivo. Int J Cancer. 2009;125(1):34-42. [Content Brief]
[2]. Šemeláková M, et al. Drug membrane transporters and CYP3A4 are affected by hypericin, hyperforin or aristoforin in colon adenocarcinoma cells. Biomed Pharmacother. 2016;81:38-47. [Content Brief]
[3]. Ševčovičová A, et al. DNA-protective activities of hyperforin and aristoforin. Toxicol In Vitro. 2015;29(3):631-637. [Content Brief]
[4]. Šemeláková M, et al. The pro-apoptotic and anti-invasive effects of hypericin-mediated photodynamic therapy are enhanced by hyperforin or aristoforin in HT-29 colon adenocarcinoma cells. J Photochem Photobiol B. 2012;117:115-125. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Aristoforin Related Classifications
HY-133849 Related Classifications
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