2. Membrane Transporter/Ion Channel Neuronal Signaling Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis MAPK/ERK Pathway Stem Cell/Wnt Others Anti-infection
  3. TRP Channel Amyloid-β Toll-like Receptor (TLR) Keap1-Nrf2 Heme Oxygenase (HO) Dihydroorotate Dehydrogenase Ferroptosis PAI-1 NF-κB ERK Proton Pump Glutathione Peroxidase Thrombin Insecticide Bacterial
  4. Pellitorine

Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria.

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Pellitorine

Pellitorine Chemical Structure

CAS No. : 18836-52-7

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Based on 1 publication(s) in Google Scholar

Other Forms of Pellitorine:

Pellitorine Related Antibodies

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ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria[1][2][3][4][5][6][7].

IC50 & Target[4][6]

ERK1

 

ERK2

 

TLR4

 

NF-κB

 

HO-1

 

Cellular Effect
Cell Line Type Value Description References
BV-2 IC50
45 μM
Compound: 23
Antineuroinflammatory activity against mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 20 hrs by Griess assay
Antineuroinflammatory activity against mouse BV2 cells assessed as inhibition of LPS-induced NO production incubated for 20 hrs by Griess assay
[PMID: 33822610]
Hepatocyte IC50
9.3 μM
Compound: 30
Hepatoprotective activity in ddY mouse hepatocytes assessed as inhibition of D-galactosamine-induced cytotoxicity after 44 hrs by MTT assay
Hepatoprotective activity in ddY mouse hepatocytes assessed as inhibition of D-galactosamine-induced cytotoxicity after 44 hrs by MTT assay
[PMID: 19775895]
THP-1 IC50
13.5 μg/mL
Compound: 7
Inhibition of sICAM1/LFA1 interaction-mediated human THP1 cell adhesion after 1 hr by ELISA
Inhibition of sICAM1/LFA1 interaction-mediated human THP1 cell adhesion after 1 hr by ELISA
[PMID: 18672369]
In Vitro

Pellitorine exhibits cytotoxic against HL60 and MCF-7 with IC50 values of 13.0 µg/mL and 1.8 µg/mL[1].
Pellitorine (0.01-1 mg/mL) blocks Capsaicin-evoked Ca2+ uptake with an IC50 of 154 µg/mL (0.69 mM/L) in HaCaT cells[2].
Pellitorine (0.1 nM-100 µM) significantly prolongs partial thromboplastin time (aPTT) and prothrombin time (PT) and inhibits the activities of cell-based thrombin and activated factor X (FXa) in normal human plasma[5].
Pellitorine (0-20 µM) Inhibits the production of thrombin and FXa induced by TNF-α and down-regulates the secretion of PAI-1, reduces the PAI-1/t-PA ratio to improve the fibrinolytic balance in HUVECs[5].
Pellitorine (0-20 μM, 6-30 h) inhibits LPS (HY-D1056)-induced barrier disruption, expression of cell adhesion molecules (CAMs) and adhesion/transendothelial migration of monocytes to human endothelial cells[6].
Pellitorine (0-20 μM, 7-22 h) suppresses the production of TNF-α or IL-6 and activation of NF-κB or extracellular regulated kinases (ERK) 1/2 by LPS in HUVECs[6].
Pellitorine is active against Bacillus subtilis, Bacillus sphaericus, Staphylococcus aureus, Klebsiella aerogenes and Chromobacterium violaceum with MIC values of 28, 56, 56, 56 and 56 μM[7].

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

Pellitorine Related Antibodies

Cell Migration Assay [6]

Cell Line: Monocytes through HUVEC monolayers
Concentration: 0, 3, 5, 10, 20 μM
Incubation Time: 6 h
Result: Inhibited the migration of monocytes across the endothelium.

ELISA Assay[6]

Cell Line: HUVECs
Concentration: 0, 3, 5, 10, 20 μM
Incubation Time: Incubated for 6 h followed by LPS for 3 h (TLR4 and p-p38), 16 h (VCAM-1, ICAM-1, TNF-α and IL-6) or 24 h (E-Selectin)
Result: Inhibited expression of TLR4 and p-p38 level.
Decreased VCAM-1, ICAM-1 and E-selectin.
Decreased TNF-α and IL-6.
Inhibited phosphorylation of ERK1/2 and NF-κB expression.

RT-PCR[6]

Cell Line: Monocytes through HUVEC monolayers
Concentration: 0, 3, 5, 10, 20 μM
Incubation Time: 6 h
Result: Significantly inhibited the upregulation of TLR4 induced by LPS.
Decreased VCAM-1, ICAM-1 and E-selectin mRNA.

Immunofluorescence[6]

Cell Line: HUVECs
Concentration: 0, 3, 5, 10, 20 μM
Incubation Time: Incubated for 6 h followed by LPS for 1 h
Result: Reduced the nuclear translocation of NF-κB p65.
In Vivo

Pellitorine (3.75 mM with 100 µM Capsaicin, eye drops, single dose) inhibits the pain-evoked defensive movements of mice in response to pungent vanilloids[2].
Pellitorine (2.21-5 mg/L, suspended in distilled water with Triton X-100, put Ae. Aegypti into paper cups containing the test solution) led to the collapse of the larva's osmotic pressure and its subsequent death by attacking mainly on midgut epithelium and anal gills of Aedes aegypt[3].
Pellitorine (0.1-0.6 mg/kg, i.p., once daily for 21 days) protects chronic restraint stress (CRS)-induced cognitive deficits via inhibiting neural inflammation and ferroptosis in mice[4].
Pellitorine (4.5-9 μg/mouse, i.v., single dose) significantly prolongs mice tail bleeding times[5].
Pellitorine (9 μg/mouse, i.v., single or doule doses) prevents mice or results in reduction of mice mortality in the LPS-induced lethal endotoxemia model[6].

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

Animal Model: Eye wipe test established in BALB/c mice[2]
Dosage: 3.75 mM applied together with 100 µM Capsaicin
Administration: Eye drops, single dose
Result: Significantly decreased the frequency of vanilloid-evoked defending movements.
Did not change significantly following either a 1 h or 15 min pretreatment with 3.75mM or 4.5 mM alone.
Animal Model: Insecticide test established in insecticide-susceptible Ae. Aegypti[3]
Dosage: 2.21 and 5 mg/L, suspended in distilled water with Triton X-100 (20 ml/L)
Administration: Put Ae. Aegypti into paper cups containing the test solution
Result: Caused the epithelial cells of the gastric caeca to swell, disintegrate, and the cell nuclei to fragment.
Dissolved the electron-dense substances in the epithelial cells and leaves the residual peritubular membrane.
Damaged the anal-gill structure, resulting in neuronal damage.
Inhibited AaAQP4 expression levels and disturbed the Na+, Cl-, and K+ co-transport system mainly.
Caused the histopathological alterations and inhibition of gene expression of V-type H+-ATPase and aquaporin protein in the anal gills.
Animal Model: CRS model established in seven-week-old male C57BL/6 J mice[4]
Dosage: 0.1 and 0.6 mg/kg
Administration: Intraperitoneally injection (i.p.), once daily for 21 days
Result: Significantly reduced the resting time of CRS mice in tails suspension test (TST).
Improved spatial memory of mice in novel object recognition test (NOR) and morris water maze (MWM).
Suppressed ferroptosis-associated signaling pathways and neuroinflammation.
Upregulated the expressions of GPX4, DHODH and FSP1.
Prevented neuronal loss, preserved the expression of neuroprotective molecules such as BDNF, Nrf2, HO-1, phosphorylated-CREB, and phosphorylated-ERK1/2.
Reduced the protein levels of inflammation-related markers including NLRP3, HMGB1, and NF-κB.
Reduced the number of activated microglia, as indicated by decreased Iba-1+, TREM2+, CD86+, and CX3CR1+ cell populations in the hippocampus.
Did not exhibit neurotoxicity in healthy mice.
Animal Model: Bleeding time test established in ICR mice[5]
Dosage: 4.5 and 9 μg/mouse
Administration: Intravenous administration (i.v.), single dose
Result: Prolonged tail bleeding times from 41.6 s to 57.6 s and 71.8 s, respectively.
Animal Model: LPS-induced lethal endotoxemia model established in male C57BL/6 mice[6]
Dosage: 9 μg/mouse
Administration: Intravenous administration (i.v.), two times at 12 h and 50 h after LPS injection or single dose at 12 h before LPS injection
Result: Prevented LPS-induced lethal endotoxemia.
Resulted in an increase in the survival rate from 0 to 30% by Kaplan-Meier survival analysis.
Suppressed LPS-induced hyperpermeability and leukocyte migration.
Molecular Weight

223.35

Formula

C14H25NO
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)CNC(/C=C/C=C/CCCCC)=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (223.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.4773 mL 22.3864 mL 44.7728 mL
5 mM 0.8955 mL 4.4773 mL 8.9546 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (11.19 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (11.19 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.4773 mL 22.3864 mL 44.7728 mL 111.9319 mL
5 mM 0.8955 mL 4.4773 mL 8.9546 mL 22.3864 mL
10 mM 0.4477 mL 2.2386 mL 4.4773 mL 11.1932 mL
15 mM 0.2985 mL 1.4924 mL 2.9849 mL 7.4621 mL
20 mM 0.2239 mL 1.1193 mL 2.2386 mL 5.5966 mL
25 mM 0.1791 mL 0.8955 mL 1.7909 mL 4.4773 mL
30 mM 0.1492 mL 0.7462 mL 1.4924 mL 3.7311 mL
40 mM 0.1119 mL 0.5597 mL 1.1193 mL 2.7983 mL
50 mM 0.0895 mL 0.4477 mL 0.8955 mL 2.2386 mL
60 mM 0.0746 mL 0.3731 mL 0.7462 mL 1.8655 mL
80 mM 0.0560 mL 0.2798 mL 0.5597 mL 1.3991 mL
100 mM 0.0448 mL 0.2239 mL 0.4477 mL 1.1193 mL
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Pellitorine Related Classifications

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  • Do most proteins show cross-species activity?

    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:

Pellitorine18836-52-7TRP ChannelAmyloid-βToll-like Receptor (TLR)Keap1-Nrf2Heme Oxygenase (HO)Dihydroorotate DehydrogenaseFerroptosisPAI-1NF-κBERKProton PumpGlutathione PeroxidaseThrombinInsecticideBacterialTransient receptor potential channelsβ-amyloid peptideAβAbetaHeme OxygenaseDHODHPlasminogen activator inhibitor-1Nuclear factor-κBNuclear factor-kappaBExtracellular signal regulated kinasesPiper nigrumAlkaloidscytotoxicityMicrobial transformationAspergillus nigerInhibitorinhibitorinhibit

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