2. Neuronal Signaling Anti-infection MAPK/ERK Pathway
  3. Cholinesterase (ChE) Bacterial Fungal Parasite p38 MAPK
  4. Cubebin

Cubebin ((-)-Cubebin), a dibenzyl butyrolactone lignan, is an orally active AChE inhibitor. Cubebin binds to active sites of NF-κB, TNF-α, and TGF-β1 via hydrogen and hydrophobic interactions, obstructing critical residues to inhibit pro-inflammatory or renal fibrosis-related activity. Cubebin enhances p38 MAPK phosphorylation to increase tyrosinase gene expression, stimulating melanogenesis via elevated tyrosinase activity, expression, and mRNA levels. Cubebin reduces oxidative stress via enhanced endogenous antioxidant enzyme activity and inhibited lipid peroxidation, regulates lipid metabolism, improves glycemic control, and exerts renoprotective effects via reduced renal dysfunction markers and improved renal architecture. Cubebin shows antimicrobial activity. Cubebin exerts larvicidal activity against Angiostrongylus cantonensis larvae, with no cytotoxicity toward monkey or human cell lines or Caenorhabditis elegans. Cubebin can be used for the research of diabetic nephropathy, melanoma, colon adenocarcinoma, neuroangiostrongyliasis, Alzheimer’s disease (AD) and depression.

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Cubebin

Cubebin 構造式

CAS 番号 : 18423-69-3

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Cubebin 関連抗体

Top Publications Citing Use of Products

Cholinesterase (ChE) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
AChE BChE

Parasite アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

p38 MAPK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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製品説明

Cubebin ((-)-Cubebin), a dibenzyl butyrolactone lignan, is an orally active AChE inhibitor. Cubebin binds to active sites of NF-κB, TNF-α, and TGF-β1 via hydrogen and hydrophobic interactions, obstructing critical residues to inhibit pro-inflammatory or renal fibrosis-related activity. Cubebin enhances p38 MAPK phosphorylation to increase tyrosinase gene expression, stimulating melanogenesis via elevated tyrosinase activity, expression, and mRNA levels. Cubebin reduces oxidative stress via enhanced endogenous antioxidant enzyme activity and inhibited lipid peroxidation, regulates lipid metabolism, improves glycemic control, and exerts renoprotective effects via reduced renal dysfunction markers and improved renal architecture. Cubebin shows antimicrobial activity. Cubebin exerts larvicidal activity against Angiostrongylus cantonensis larvae, with no cytotoxicity toward monkey or human cell lines or Caenorhabditis elegans. Cubebin can be used for the research of diabetic nephropathy, melanoma, colon adenocarcinoma, neuroangiostrongyliasis, Alzheimer’s disease (AD) and depression[1][2][3][4][5][6][7].

IC50 & Target[7]

AChE

 

Cellular Effect
Cell Line Type Value Description References
MDCK IC50
>200 μM
Compound: 1
Inhibition of human NET expressed in MDCK cells using [3H]-norepinephrine as substrate after 10 mins by scintillation counting
Inhibition of human NET expressed in MDCK cells using [3H]-norepinephrine as substrate after 10 mins by scintillation counting
[PMID: 24112084]
MDCK IC50
>200 μM
Compound: 1
Inhibition of human SERT expressed in MDCK cells using [3H]-serotonin as substrate after 10 mins by scintillation counting
Inhibition of human SERT expressed in MDCK cells using [3H]-serotonin as substrate after 10 mins by scintillation counting
[PMID: 24112084]
MDCK IC50
12 μM
Compound: 1
Inhibition of human DAT expressed in MDCK cells using [3H]-dopamine as substrate after 10 mins by scintillation counting
Inhibition of human DAT expressed in MDCK cells using [3H]-dopamine as substrate after 10 mins by scintillation counting
[PMID: 24112084]
体外実験

Cubebin (2-20 μM; 72 h) stimulates melanogenesis in a concentration-dependent manner in murine B16 melanoma cells, with no significant impact on cell proliferation at 2, 5, and 10 μM[3].
Cubebin (10 μM; 24-96 h) enhances tyrosinase activity, and increases intracellular melanin amount significantly starting at 48 h and reaching maximum levels at 72 and 96 h in murine B16 melanoma cells[3].
Cubebin (10 μM; 24-72 h) enhances tyrosinase protein expression, reaching a 6.2-fold increase relative to pre-treated cells at 48 h in murine B16 melanoma cells[3].
Cubebin (10 μM; 12-48 h) increases tyrosinase mRNA expression, reaching a 1.8-fold increase relative to pre-treated cells at 12 h in murine B16 melanoma cells[3].
Cubebin (10 μM; 2-12 h) significantly enhances p38 MAPK phosphorylation at 4-8 h, with no impact on ERK1/2 or p70 S6K1 phosphorylation in murine B16 melanoma cells[3].
Cubebin (2.8-280 μM; 24-72 h) is non-cytotoxic to HT29 cells at 2.8 and 28 μM for 24, 48, or 72 h, but induces significant cytotoxicity (≈50% viability reduction at 24 h) at 280 μM for 24, 48, or 72 h[4].
Cubebin (50-200 μM; 24 h) shows no cytotoxicity toward Vero monkey kidney epithelial cells or HaCaT human keratinocytes at concentrations up to 200 μM, resulting in high selectivity indices against Angiostrongylus cantonensis larvae[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cubebin 関連抗体

Cell Proliferation Assay[3]

Cell Line: murine B16 melanoma cells
Concentration: 2, 5, 10, 20 μM
Incubation Time: 72 h
Result: Stimulated melanogenesis in a concentration-dependent manner.
Significantly increased melanin amount at 2 μM relative to control cells.
Showed greater significant increases in melanin amount at 5, 10, and 20 μM relative to control cells.
Showed no significant effects on cell proliferation at 2, 5, and 10 μM.
Slightly decreased cell proliferation at 20 μM.

Western Blot Analysis[3]

Cell Line: murine B16 melanoma cells
Concentration: 10 μM
Incubation Time: 24, 48, 72 h
Result: Enhanced tyrosinase expression to 4.9-fold of pre-treated cells at 24 h.
Enhanced tyrosinase expression to 6.2-fold of pre-treated cells at 48 h.
Enhanced tyrosinase expression to 1.7-fold of pre-treated cells at 72 h.

RT-PCR[3]

Cell Line: murine B16 melanoma cells
Concentration: 10 μM
Incubation Time: 12, 24, 48 h
Result: Increased tyrosinase mRNA expression 1.8-fold relative to pre-treated cells at 12 h.
Showed 1.7-fold increases in tyrosinase mRNA expression at 24 and 48 h relative to pre-treated cells.

Western Blot Analysis[3]

Cell Line: murine B16 melanoma cells
Concentration: 10 μM
Incubation Time: 2, 4, 6, 8, 10, 12 h
Result: Significantly enhanced phosphorylation of p38 MAPK at 4-8 h after treatment.
Showed no effects on the phosphorylation levels of ERK1/2 or p70 S6K1.

RT-PCR[3]

Cell Line: murine B16 melanoma cells
Concentration: 10 μM
Incubation Time: 12 h
Result: Increased tyrosinase mRNA expression 1.9-fold relative to pre-treated cells.
Showed complete block of this cubebin-induced increase in tyrosinase mRNA expression when co-treated with SB203580.
体内実験

Cubebin (10-20 mg/kg; p.o.; daily; 8 weeks) significantly improves glycemic control, lipid metabolism, renal function, oxidative stress, inflammatory marker levels, and renal histopathology in Streptozotocin (HY-13753)-induced diabetic nephropathy rats[1].
Cubebin (10 mg/kg; p.o.; single dose) inhibits carrageenin-induced rat paw edema by 53%, with statistically significant anti-inflammatory activity[2].
Cubebin (10 mg/kg; p.o.; single dose) inhibits PGE2-induced rat paw edema by 20%, with statistically significant anti-inflammatory activity[2].
Cubebin (10 mg/kg; p.o.; single dose) inhibits serotonin-induced rat paw edema by 23%, with statistically significant anti-inflammatory activity[2].
Cubebin (10 mg/kg; p.o.; single dose) does not produce a statistically significant reduction in carrageenin-induced peritoneal cell migration in rats, with only 12% inhibition observed[2].
Cubebin (10 mg/kg; p.o.; single dose) inhibits acetic acid-induced writhing in mice by 50%, with statistically significant peripheral antinociceptive activity[2].
Cubebin (10 mg/kg; p.o.; single dose) inhibits PGI2-induced writhing in mice by 71%, with statistically significant peripheral antinociceptive activity[2].
Cubebin (10-40 mg/kg; i.g.; daily; 35 days) significantly alleviates CUMS-induced depression-like behavior in male C57BL/6 mice by restoring brain neurotransmitter levels, reducing neuronal tissue damage, and normalizing gut microbiota composition and function[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar (male, 8-10-week-old, 180 g, Streptozotocin-induced diabetic nephropathy)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: p.o.; daily; 8 weeks
Result: Significantly reduced fasting blood glucose levels and restored serum insulin levels.
Significantly reduced HbA1c levels.
Significantly reduced total cholesterol and triglyceride levels, and increased high-density lipoprotein levels.
Significantly reduced serum creatinine, blood urea nitrogen, and 24-hour urine volume.
Significantly increased kidney superoxide dismutase, catalase, and glutathione reductase activity, and reduced kidney malondialdehyde levels.
Significantly reduced kidney tumor necrosis factor-α, interleukin-1β, interleukin-6, nuclear factor-kappa B, and transforming growth factor-β1 levels.
Significantly improved renal histopathology, restoring normal glomerular and tubular structures and reducing lesions including glomerular basement membrane thickening, cellular necrosis, interstitial inflammation, and hemorrhage.
Animal Model: C57BL/6 (male, 6-8 weeks old, 18-22 g, CUMS-induced depression-like behavior)[6]
Dosage: 10 mg/kg; 20 mg/kg; 40 mg/kg
Administration: i.g.; daily; 35 days
Result: Significantly increased total distance traveled in the open field test and sucrose preference percentage, and significantly decreased immobility time in the tail suspension test and forced swimming test compared to the model group.
Reduced pathological damage to hippocampal and cortical neuronal cells, with restored arrangement, number, and morphology of neurons compared to the model group; significantly increased cortical neuron count in the 40 mg/kg group compared to the model group.
Significantly increased norepinephrine (NE) and dopamine (DA) levels in cortical tissue in the 20 mg/kg and 40 mg/kg groups compared to the model group; significantly increased NE levels in hypothalamic tissue in all dose groups, and significantly increased DA levels in hypothalamic tissue in the 20 mg/kg group compared to the model group; significantly increased serotonin (5-HT) levels in cortical tissue in all dose groups compared to the model group.
Reversed CUMS-induced gut microbiota alterations, including reduced relative abundance of Clostridium, Dorea, Ruminococcus, Eubacterium, Escherichia, Phascolarctobacterium, Lactobacillus, Roseburia, Coprococcus, Sutterella, Akkermansia, Parabacteroides, and Allobaculum, and increased relative abundance of Prevotella, Dehalobacterium, Flavobacterium, and Blautia compared to the model group.
Reversed CUMS-induced dysregulation of gut microbiota metabolic pathways, with restored expression levels of KEGG and COG pathway sequences toward control group levels.
分子量

356.37

分子式

C20H20O6
CAS 番号
SMILES

O[C@@H]1[C@@H]([C@H](CO1)CC2=CC=C3C(OCO3)=C2)CC4=CC=C5C(OCO5)=C4
Structure Classification
Initial Source
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
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参考文献
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Cubebin Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cubebin18423-69-3(-)-CubebinCholinesterase (ChE)BacterialFungalParasitep38 MAPKcolon adenocarcinoma cellsstreptozotocin-induced diabetic nephropathy ratsmurine B16 melanoma cellsTNF-αTGF-β1HT29 cellsAngiostrongylus cantonensisNF-κBtyrosinaseInhibitorinhibitorinhibit

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