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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 24312-00-3
- 分子式: C41H26O26
- 分子量:934.63
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
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PARP1 0.86 μM (IC50) |
Topoisomerase II |
Leishmania |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 24312-00-3
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分子量 934.63
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
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Castalagin 関連分類
HY-N20707 関連分類
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