Phellopterin
(Synonyms: 珊瑚菜素) 目录号 : GC38992
Phellopterin 是从 P. trifoliata 中分离得到的天然产物。Phellopterin 通过调节 Akt 和 PKC 通路降低 TNF-alpha 诱导的 VCAM-1 表达，从而抑制单核细胞与内皮细胞的粘附。
Cas No.:2543-94-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Phellopterin is a natural product isolated from P. trifoliata. Phellopterin reduce TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium[1].
[1]. Nizamutdinova IT, et al. Hesperidin, hesperidin methyl chalone and phellopterin from Poncirus trifoliata (Rutaceae) differentially regulate the expression of adhesion molecules in tumor necrosis factor-alpha-stimulated human umbilical vein endothelial cells. Int Immunopharmacol. 2008 May;8(5):670-8.
| Cas No. | 2543-94-4 | SDF | |
| 别名 | 珊瑚菜素 | ||
| Canonical SMILES | O=C1C=CC2=C(OC)C3=C(OC=C3)C(OC/C=C(C)/C)=C2O1 | ||
| 分子式 | C17H16O5 | 分子量 | 300.31 |
| 溶解度 | DMSO : 100 mg/mL (332.99 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3299 mL | 16.6495 mL | 33.2989 mL |
| 5 mM | 0.666 mL | 3.3299 mL | 6.6598 mL |
| 10 mM | 0.333 mL | 1.6649 mL | 3.3299 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Phellopterin alleviates atopic dermatitis-like inflammation and suppresses IL-4-induced STAT3 activation in keratinocytes
Int Immunopharmacol 2022 Nov;112:109270.PMID:36179418DOI:10.1016/j.intimp.2022.109270.
Anti-inflammation medication is one of the most important treatment for people with atopic dermatitis (AD) which presents persistent type 2 inflammation in skin lesions. Interaction between activated keratinocytes and immune cells in AD skin lesions amplifies inflammatory signaling by augmenting production of cytokines, such as keratinocyte-derived thymic stromal lymphopoietin (TSLP) and interleukin-33 (IL-33). Phellopterin is a bioactive compound isolated from ethanol extract of Angelica dahurica root which has been traditionally used for AD therapy in China. In the present study, we showed that Phellopterin possessed anti-type 2 inflammation activity and alleviated AD-like phenotypes including reduction in serum immunoglobulin E (IgE) levels and infiltration of eosinophils and mast cells in the AD-like skin lesions. Further molecular analysis found that Phellopterin suppressed phosphorylation of signal transducer and activator of transcription 3 (STAT3) at Tyr705, and the expression of TSLP and IL-33 in epidermal keratinocytes of AD-like lesions. In vitro studies in cultured human keratinocytes demonstrated that STAT3 was required for interleukin-4 (IL-4)-induced overexpression of TSLP and IL-33. Phellopterin inhibited IL-4-induced activation of STAT3, which leaded to suppress the STAT3-mediated transcription of TSLP and IL-33. Our study suggested that Phellopterin is an active compound with bioactivities of anti- type 2 inflammation and STAT3 inactivation, thus allowing to be a promising candidate for AD topical therapy.
Phellopterin cream exerts an anti-inflammatory effect that facilitates diabetes-associated cutaneous wound healing via SIRT1
Phytomedicine 2022 Dec;107:154447.PMID:36150345DOI:10.1016/j.phymed.2022.154447.
Background: Diabetic ulcers, which are characterized by chronic nonhealing wounds with a long-lasting inflammatory state, are a typical symptom in individuals with diabetes, and there is still no effective treatment for these lesions. Angelica dahurica plays a critical role in inflammatory diseases. Among numerous monomeric compounds, Phellopterin has been shown to have anti-inflammatory properties. Purpose: To research the bioactive constituents in Angelica dahurica and their mechanism of action in treating diabetic ulcers. Study design: Chemical research of Angelica dahurica led to the identification of a new coumarin, dahuricoumarin A (1), along with seven known compounds (2 - 8). All compounds were tested for anti-inflammatory activity, and Phellopterin, compound (3), significantly decreased the expression of intercellular cell adhesion molecule-1 (ICAM-1), a representative indicator of inflammation. Phellopterin can also increase SIRT1 protein, a key target for inflammation. In our research, we confirmed the anti-inflammatory effects of Phellopterin on diabetic ulcers and explored the underlying mechanism of action. Methods: The expression of IFN-γ, SIRT1, and ICAM-1 in human diabetic ulcer tissues was studied using immunohistochemistry. Streptozotocin was used to induce a diabetic model in C57BL/6J mice, and ulcers were surgically introduced. After Phellopterin treatment, the skin lesions of diabetic mice were observed over a period of time. The protein and mRNA expression levels of SIRT1 and ICAM-1 were measured using H&E, qRT-PCR and immunohistochemical staining. A HaCaT cell inflammatory model was induced by IFN-γ. Using a lentiviral packaging technique, MTT assay, and Western blotting, the effect of Phellopterin on the proliferation of HaCaT cells and the expression of ICAM-1 was evaluated under normal and SIRT1 knockdown conditions. Results: High levels of ICAM-1 and IFN-γ were identified, but low levels of SIRT1 were found in human diabetic ulcer tissues, and Phellopterin showed therapeutic benefits in the healing process by attenuating chronic inflammation and promoting re-epithelialization, along with SIRT1 upregulation and ICAM-1 downregulation. However, inhibiting SIRT1 reversed its proliferative and anti-inflammatory effects. Conclusion: In vitro and in vivo, Phellopterin exerts anti-inflammatory and proliferative effects that promote diabetic wound healing, and the potential mechanism depends on SIRT1.
Phellopterin isolated from Angelica dahurica reduces blood glucose level in diabetic mice
Heliyon 2018 Mar 19;4(3):e00577.PMID:29862342DOI:10.1016/j.heliyon.2018.e00577.
Insulin resistance is the critical condition for the development of metabolic syndromes including type II diabetes and heart disease. To investigate the active components of Angelica dahurica root which is known to increase insulin sensitivity, its methanol extract was subfractionated. The ethyl acetate (EtOAc) fraction of the Angelica dahurica root extract significantly promoted adipocyte differentiation in 3T3-L1 preadipocyte cells. Among the three compounds isolated from the EtOAc extract (bergapten (1), imperatorin (2) and Phellopterin (3)), Phellopterin (3) induced the highest adipocyte differentiation at 25 and 50 μg/mL. In addition, treatment with imperatorin (2) and Phellopterin (3) increased the mRNA expression of peroxisome proliferator-activated receptors γ (PPARγ). In diabetic animal model induced by high-fat diets (HFD) and streptozotocin (STZ), administration of Phellopterin ((3), 1 mg/kg and 2 mg/kg) significantly reduced the levels of blood glucose, triglycerides and total cholesterol. Taken together, these results indicate that Phellopterin (3) enhances adipocytes differentiation in 3T3-L1 preadipocytes, Phellopterin (3) significantly prevents HFD/STZ-induced type Ⅱ diabetes. The present study also provides Phellopterin (3) may be a valuable therapeutic alternative for enhancing insulin sensitivity through promotion of adipocyte differentiation and by increasing mRNA expression levels of PPARγ, which is a major mediator of insulin sensitivity.
Stimulation of phosphorylation of ERK and CREB by Phellopterin and auraptene isolated from Citrusjunos
Nat Prod Commun 2014 Oct;9(10):1491-4.PMID:25522543doi
Bioactive compounds from citrus fruits contribute many benefits to human health. Extracellular signal-regulated kinase (ERK) signaling plays an important role in the regulation of multiple cellular processes. Activation of the ERK-cAMP response element binding protein (CREB) signaling is required for long- term memory formation. In this study, auraptene, Phellopterin, thymol, coniferyl alcohol 9-methyl ether and methyl ferulate were isolated from Citrus junos. Among the five compounds isolated, auraptene and Phellopterin increased the phosphorylation of ERK and CREB. This study provides, to our knowledge, the first evidence that Phellopterin potently stimulates the phosphorylation of ERK and CREB. Phellopterin could be a novel neuroprotective agent.
Characterisation of the furanocoumarin Phellopterin as a rat brain benzodiazepine receptor partial agonist in vitro
Neurosci Lett 1996 Nov 29;219(3):151-4.PMID:8971802DOI:10.1016/s0304-3940(96)13183-9.
Phellopterin, a naturally occurring furanocoumarin found in the roots of Angelica dahurica, inhibits [3H]diazepam and ethyl 8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4] benzodiazepine-3-carboxylate ([3H]Ro 15-1788) binding to the benzodiazepine site of the rat brain gamma-aminobutyric acidA (GABAA) receptor in vitro with IC50 values of 400 and 680 nM, respectively. Two other naturally occurring furanocoumarins, byakangelicol and imperatorin were significantly less potent, with IC50 values for inhibition of [3H]diazepam binding of 8.0 and 12.3 microM, respectively. Scatchard plot analysis showed that the inhibitory activity of Phellopterin was due to competitive inhibition of the benzodiazepine ligand binding. The results of GABA- and t-butylbicyclophosphorothionate (TBPS)-shift assays suggest that Phellopterin is a partial agonist of the central benzodiazepine receptors in vitro.