| 生物活性 |
Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin, 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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| 体外研究 |
Pellitorine exhibits cytotoxicity against HL60 and MCF-7 cells, with IC50 values of 13.0 µg/mL and 1.8 µg/mL, respectively.
Pellitorine (0.01-1 mg/mL) inhibits capsaicin-induced Ca2+ uptake with an IC50 of 154 µg/mL (0.69 mM/L) in HaCaT cells.
Pellitorine (0.1 nM-100 µM) significantly prolongs the activated partial thromboplastin time (aPTT) and prothrombin time (PT), while inhibiting the activity of intracellular thrombin and activated factor X (FXa) in normal human plasma.
Pellitorine (0-20 µM) inhibits TNF-α-induced thrombin and FXa production in human umbilical vein endothelial cells, downregulates PAI-1 secretion, and reduces the PAI-1/t-PA ratio, thereby improving fibrinolytic balance.
Pellitorine (0-20 μM, 6-30 h) inhibits LPS induced barrier disruption, cell adhesion molecule (CAM) expression, and monocyte adhesion/transendothelial migration in human endothelial cells.
Pellitorine (0-20 μM, 7-22 h) inhibits the production of TNF-α and IL-6 in LPS-stimulated human umbilical vein endothelial cells or activates NF-κB and extracellular signal-regulated kinase (ERK) 1/2.
Pellitorine exhibits antibacterial activity against Bacillus subtilis, Bacillus sphaericus, Staphylococcus aureus, Klebsiella pneumoniae, and Pseudomonas aeruginosa, with MIC values of 28, 56, 56, 56, and 56 μM, respectively.
Cell Migration Assay
| Cell Line: |
Monocytes through HUVEC monolayers |
| Concentration: |
0, 3, 5, 10, 20 μM |
| Incubation Time: |
6 hours |
| Result: |
Inhibited the migration of monocytes across the endothelium. |
ELISA Assay
| 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
| Cell Line: |
Monocytes through HUVEC monolayers |
| Concentration: |
0, 3, 5, 10, 20 μM |
| Incubation Time: |
6 hours |
| Result: |
Significantly inhibited the upregulation of TLR4 induced by LPS.
Decreased VCAM-1, ICAM-1 and E-selectin mRNA. |
Immunofluorescence
| 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. |
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| 体内研究 |
Pellitorine (3.75 mM, containing 100 µM capsaicin, instilled into the eye, single dose) can inhibit pain defense responses in mice induced by irritating vanilloid substances.
Pellitorine (2.21-5 mg/L, suspended in distilled water containing Triton X-100, and Ae. aegypti mosquitoes were placed in paper cups containing the test solution) primarily targets the midgut epithelium and anal siphon of Ae. aegypti, causing larval osmotic collapse and subsequent death.
Pellitorine (0.1-0.6 mg/kg, intraperitoneal injection, once daily for 21 days) can prevent cognitive deficits induced by chronic restraint stress (CRS) in mice by inhibiting neuroinflammation and ferroptosis.
Pellitorine (4.5-9 μg/mouse, intravenous injection, single dose) significantly prolonged tail bleeding time in mice.
Pellitorine (9 μg/mouse, intravenous injection, single or double dose) can prevent or reduce mortality in mice with LPS-induced lethal septicemia models.
| Animal Model: |
Eye wipe test established in BALB/c mice |
| 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 |
| 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 |
| 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 |
| 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 |
| 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. |
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| 分子式 |
C14H25NO
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| 分子量 |
223.35
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| CAS号 |
18836-52-7
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| 中文名称 |
墙草碱
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
2-8°C, protect from light
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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| 溶解性数据 |
In Vitro:
DMSO : 50 mg/mL (223.86 mM; Need ultrasonic)
配制储备液
| 浓度 溶剂体积 质量 |
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 |
| 10 mM |
0.4477 mL |
2.2386 mL |
4.4773 mL |
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
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1.
请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline
Solubility: 2.5 mg/mL (11.19 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (11.19 mM) 的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
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2.
请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (11.19 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (11.19 mM) 的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
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3.
请依序添加每种溶剂： 10% DMSO → 90% corn oil
Solubility: ≥ 2.5 mg/mL (11.19 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.19 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
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Data Sheet
