Castalagin
Castalagin is an orally active natural product with multiple biological activities including antibacterial activity against bacteria and anti-leishmanial activity against Leishmania aethiopica. Castalagin exhibits inhibitory activity against PARP1 and DNA topoisomerase II, with an IC50 of 0.86 μM for bovine PARP1. Castalagin reduces poly (ADP-ribosyl) ation modification in cells. Castalagin binds to the cell envelope of Ruminococcus bromii, increases the ratio of CD8+/FOXP3+CD4+ T cells in the tumor microenvironment, and acts as a prebiotic to enhance the activity of anti-PD-1 therapy. Castalagin induces morphological changes in Leishmania aethiopica promastigotes and inhibits their proliferation. Castalagin inhibits PBP2a-mediated peptidoglycan layer stabilization, disrupts bacterial peptidoglycan assembly, and inhibits and disintegrates bacterial biofilms. Castalagin can be used in research related to diseases such as cancer, leishmaniasis, and bacterial infections.
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- CAS No.: 24312-00-3
- Formule: C41H26O26
- Masse moléculaire:934.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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PARP1 0.86 μM (IC50) |
Topoisomerase II |
Leishmania |
Castalagin potently inhibits purified bovine thymus PARP1 in a mixed-type manner, with an IC50 of 0.86 μM and a Ki of 1.64 μM; it inhibits the activity of human recombinant DNA topoisomerase II in vitro at concentrations of 0.1 and 0.3 μM[1].
Castalagin (0.1-3.2 μM; 24 h) reduces poly (ADP-ribosyl) ation in human neuroblastoma SH-SY5Y cells[1].
Castalagin exhibits stronger DPPH free radical scavenging activity than the non-enriched cork water extract[4].
Castalagin (0.125-2.00 mg/mL; 24 h) shows cytocompatibility with L929 fibroblasts at its anti-MRSA MIC concentration of 0.125 mg/mL after 24 h of incubation, but exhibits cytotoxicity at higher concentrations[4].
Castalagin labeled with fluorescein (2 μmol/L; 1 h at 37°C) preferentially binds to the cell envelope of Ruminococcus bromii, and the intensity of its specific competitive binding is higher than that to Ruminococcus bicirculans, Bacteroides thetaiotaomicron, or Escherichia coli[2].
Castalagin inhibits and kills MRSE (MIC = 0.250 mg/mL), SA (MIC = 0.500 mg/mL), MRSA (MIC = 0.125 mg/mL) and PA (MIC = 1.000 mg/mL) in the microbroth dilution assay, and exhibits stronger efficacy against methicillin-resistant Gram-positive strains[4].
Castalagin (0.125-1.000 mg/mL; 24 h) significantly reduces the viable cell count, damages the cell wall, and decreases the cell density of MRSE, SA, MRSA, and PA at its corresponding MIC[4].
Castalagin (0.020-1.00 mg/mL; 24 h) disrupts preformed biofilms of MRSE, SA, MRSA and PA, and exerts effective activity against Gram-positive strains at concentrations below its MIC[4].
Castalagin (0.050-0.500 mg/mL; 24 h) inhibits biofilm and β-sheet structure formation of MRSE, SA and MRSA, and disturbs the synthesis of biofilm constituents in PA[4].
Castalagin-loaded alginate hydrogel inhibits the growth of MRSE, MRSA and SA, exerts no growth inhibitory effect on PA, and exhibits cytocompatibility when incubated with L929 fibroblasts[4].
Castalagin potently inhibits the proliferation and kills promastigotes of Leishmania aethiopica and Leishmania amazonensis, with corresponding MIC values of 55 μg/mL (0.059 μM) and 65 μg/mL (0.070 μM)[3].
Castalagin (55 μg/mL; 24 h) induces morphological damage, including swelling and loss of spindle shape, in promastigotes of Leishmania aethiopica, which subsequently leads to their death; it also causes ultrastructural damage in Leishmania aethiopica promastigotes, including cytoplasmic swelling, nuclear changes, and flagellar pocket swelling, thereby resulting in death[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human neuroblastoma SH-SY5Y cells
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Concentration:0.1, 0.3, 1.1, 3.2 μM
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Incubation Time:24 h
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Result:Attenuated cellular poly(ADP-ribosyl)ation.
Caused a noticeable reduction in PARylated proteins (including automodified PARP1) at 3.2 μM.
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Cell Line:L929 mouse fibroblast cell line
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Concentration:0.125, 0.25, 0.5, 1, 2 mg/mL
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Incubation Time:24 h
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Result:Was cytocompatible at 0.125 mg/mL (its MRSA MIC concentration), with no significant reduction in metabolic activity relative to untreated controls.
Caused statistically significant reductions in metabolic activity at concentrations ≥ 0.250 mg/mL.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, seven weeks old, subcutaneous implantation of 0.8 × 106 MCA-205 fibrosarcoma cells)[2]
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Dosage:0.21 mg/kg; 0.85 mg/kg; 1.28 mg/kg; 2.55 mg/kg
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Administration:p.o.; daily
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Result:Equaled CC in tumor shrinkage at 0.85 mg/kg and outperformed water controls.
Generated saturated antitumor activity at doses ≥ 0.85 mg/kg.
Showed no antitumor activity at 0.21 mg/kg.
Raised fecal Ruminococcaceae abundance at 0.85 mg/kg, with no improvement at higher doses.
Chemical Information
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CAS No. 24312-00-3
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Masse moléculaire 934.63
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Formule C41H26O26
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SMILES
O=C(O[C@]1([C@@H]([C@@]([H])(OC(C2=C3C(O)=C(C(O)=C2C4=C(C(O)=C(C(C5=C(C(O)=C(C=C56)O)O)=C47)O)O)O)=O)[C@H]3O)OC7=O)[H])C8=CC(O)=C(C(O)=C8C9=C(C=C(C(O)=C9O)O)C(OC[C@]1(OC6=O)[H])=O)O
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Kamada Y, et al. Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II. Fitoterapia. 2018 Sep;129:94-101. [Content Brief]
[2]. Messaoudene M, et al. A Natural Polyphenol Exerts Antitumor Activity and Circumvents Anti-PD-1 Resistance through Effects on the Gut Microbiota. Cancer discovery. 2022 Apr 01;12(4):1070-1087. [Content Brief]
[4]. Araújo AR, et al. Vescalagin and Castalagin Present Bactericidal Activity toward Methicillin-Resistant Bacteria. ACS biomaterials science & engineering. 2021 Mar 08;7(3):1022-1030. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Castalagin Related Classifications
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