Soulattrolide
Soulattrolide is a non-nucleoside HIV-1 reverse transcriptase (RT) inhibitor with IC50 values of 0.34 µM for HIV-1 RT, 69.5 µM for E. coli RNase H, and >495 µM for human DNA polymerase β, and can be found in Calophyllum teysmannii latex. Soulattrolide can be used for the research of HIV-1 infection, pain, inflammation, and Mycobacterium tuberculosis infection.
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- CAS. Nr.: 65025-62-9
- Formel: C25H24O5
- Molecular Weight:404.46
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
HIV-1 0.34 μM (IC50) |
DNA Polymerase >495 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Vero | LD50 |
10 μg/mL
Compound: 13
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Cytotoxicity against African green monkey Vero cells by CellTiter 96 non-radioactive cell proliferation assay
Cytotoxicity against African green monkey Vero cells by CellTiter 96 non-radioactive cell proliferation assay
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[PMID: 28494250] |
In Vitro
Soulattrolide (Compound 1) (1.0×10-9-5.0×10-4 M; 1 h) potently inhibits the RNA-dependent DNA polymerase activity of purified dimeric HIV-1 (p66/p51) reverse transcriptase with an IC50 of 0.34 µM[1].
Soulattrolide (1.0×10-9-5.0×10-4 M; 1 h) inhibits the DNA-dependent DNA polymerase activity of purified dimeric HIV-1 (p66/p51) reverse transcriptase with an IC50 of 0.73 µM[1].
Soulattrolide (1.0×10-9-5.0×10-4 M; 30 min) inhibits purified Escherichia coli ribonuclease H activity with an IC50 of 69.5 µM[1].
Soulattrolide (495 µM; 1 h) shows no significant inhibitory activity against HIV-2 RT, TIBO-resistant (Tyr181) HIV-1 RT, avian myeloblastosis virus RT, human DNA polymerase α, human DNA polymerase β, or Escherichia coli RNA polymerase at concentrations up to 495 µM[1].
Soulattrolide (0.34 μM) potently inhibits HIV-1 reverse transcriptase with an IC50 of 0.34 μM in a cell-free biochemical assay[2].
Soulattrolide (3.13 μg/mL) inhibits Mycobacterium tuberculosis growth with an MIC of 3.13 μg/mL in a cell-free/biochemical assay[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Soulattrolide (0.1-50 mg/kg; p.o.; single dose) exhibits antinociceptive activity in both neurogenic (ED50 = 7 mg/kg p.o.) and inflammatory (ED50 = 22 mg/kg p.o.) phases of the formalin (30 μL)-induced mice paw licking model[2].
Soulattrolide (0.1-50 mg/kg; p.o.; single dose) induces 40% antinociception in the mice hot plate thermal nociception model when evaluated 120 minutes post-treatment[2].
Soulattrolide (0.1-10 μmol/ear; topical; single dose) exerts dose-dependent anti-inflammatory activity in the TPA (0.25 μg/μL)-induced mice ear edema model with an IC50 of 1.81 μmol/ear, and inhibits MPO activity by 87% at 1 μmol/ear[2].
Soulattrolide (1-50 mg/kg; p.o.; single dose) exerts sedative effects in the pentobarbital-induced mice sleeping time model, decreasing sleep onset by up to 39% and increasing sleep duration by up to 49%[2].
Soulattrolide (1-50 mg/kg; p.o.; single dose) impairs motor coordination in the mice rotarod model at 10 and 50 mg/kg with a transient effect that resolves by 60 minutes post-treatment initiation[2].
Soulattrolide (1-50 mg/kg; p.o.; single dose) lacks antidepressant activity in the mice tail suspension test[2].
Soulattrolide (1-50 mg/kg; p.o.; single dose) exhibits anxiolytic-like effects in the mice light-dark test significantly increasing time spent in the light compartment[2].
Soulattrolide (1-50 mg/kg; p.o.; single dose) exhibits anxiolytic-like effects in the open field test, increasing the distance of mice crossed in central squares in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c, CD-1 (male, 25-30 g)[2]
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Dosage:0.1 mg/kg; 1 mg/kg; 10 mg/kg; 50 mg/kg
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Administration:p.o.; single dose
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Result:Showed dose-dependent antinociceptive effects with an ED50 = 33 mg/kg.\nShowed antinociceptive activity in both phases of the formalin test, with an ED50 = 7 mg/kg for Phase 1 and an ED50 = 22 mg/kg for Phase 2.\nInduced 40% antinociception compared to the vehicle group 120 minutes post-treatment at the highest dose of 50 mg/kg.
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Animal Model:Balb/c, CD-1 (male, 25-30 g)[2]
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Dosage:0.1 μmol/ear; 1 μmol/ear; 10 μmol/ear
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Administration:topical; single dose
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Result:Showed dose-dependent anti-inflammatory activity with an IC50 = 1.81 μmol/ear in the TPA edema test.
Inhibited MPO activity by 87% at 1 μmol/ear.
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Animal Model:Balb/c, CD-1 (male, 25-30 g)[2]
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Dosage:1 mg/kg; 10 mg/kg; 50 mg/kg
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Administration:p.o.; single dose
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Result:Significantly decreased sleep onset by 21% (1 mg/kg), 19% (10 mg/kg), and 39% (50 mg/kg) compared to the vehicle group.
Significantly increased sleep duration by 42% (1 mg/kg), 46% (10 mg/kg), and 49% (50 mg/kg) compared to the vehicle group.\nSignificantly decreased time spent on the rotarod by 12% (10 mg/kg) and 22% (50 mg/kg) at 30 minutes post-treatment initiation.
Allowed mice to recover motor coordination by 60 minutes post-treatment initiation.\nDid not affect immobility time compared to the vehicle group.\nSignificantly increased time spent in the light compartment compared to the vehicle group, with effects similar to clonazepam (1.5 mg/kg), though not dose-dependent.\nSignificantly increased distance crossed in central squares in a dose-dependent manner, with effects similar to clonazepam (1.5 mg/kg).
Chemical Information
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CAS. Nr. 65025-62-9
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Molecular Weight 404.46
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Formel C25H24O5
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SMILES
O[C@@H]1C2=C(O[C@H]([C@@H]1C)C)C(C=CC(C)(O3)C)=C3C(C(C4=CC=CC=C4)=C5)=C2OC5=O
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Structure Classification
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Initial Source
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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]. Pengsuparp T, et al. Specific inhibition of human immunodeficiency virus type 1 reverse transcriptase mediated by soulattrolide, a coumarin isolated from the latex of calophyllum teysmannii. J Nat Prod. 1996;59(9):839-842. [Content Brief]
[2]. Alonso-Castro AJ, et al. Antinociceptive, anti-inflammatory, and central nervous system (CNS) effects of the natural coumarin soulattrolide. Drug Dev Res. 2018;79(7):332-338. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Soulattrolide Related Classifications
HY-182552 Related Classifications
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Keywords
- Soulattrolide
- 65025-62-9
- HIV
- Reverse Transcriptase
- DNA/RNA Synthesis
- Human immunodeficiency virus
- Calophyllum teysmannii
- HIV-2 RT
- E. coli RNase H
- AMV RT
- Mycobacterium tuberculosis
- Tyr181 mutant HIV-1 RT
- HIV-1 reverse transcriptase
- human DNA polymerase β
- RNA polymerase
- avian myeloblastosis virus RT
- Inhibitor
- inhibitor
- inhibit