Coniferyl ferulate
(Synonyms: 阿魏酸松柏酯) 目录号 : GC35727
A monolignal conjugate with diverse biological activities
Cas No.:63644-62-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Coniferyl ferulate is a monolignol conjugate that has been found in A. sinensis and has diverse biological activities, including antibacterial, antioxidant, enzyme inhibitory, and neuroprotective properties.1,2,3,4 It is active against the Gram-positive bacteria B. subtilis and S. aureus.2 Coniferyl ferulate scavenges 2,2-diphenyl-1-picrylhydrazyl radicals (EC50 = 3.6 ?g/ml) and inhibits glutathione S-transferase (GST; IC50 = 0.3 ?M for the human placental enzyme) in cell-free assays.3,4 Coniferyl ferulate (10 and 50 ?g/ml) reduces cytotoxicity induced by amyloid-β (1-40) (Aβ40) in PC12 cells.3
1.Grabber, J.H., Schatz, P.F., Kim, H., et al.Identifying new lignin bioengineering targets: 1. Monolignol-substitute impacts on lignin formation and cell wall fermentabilityBMC Plant Biol.10114(2010) 2.Chou, S.-H., Everngam, M.C., Sturtz, G., et al.Antibacterial activity of components from Lomatium californicumPhytother. Res.20(2)153-156(2006) 3.Ho, C.C., Kumaran, A., and Hwang, L.S.Bio-assay guided isolation and identification of anti-Alzheimer active compounds from the root of Angelica sinensisFood Chem.114(1)246-252(2009) 4.Chen, C., Wu, C., Lu, X., et al.Coniferyl ferulate, a strong inhibitor of glutathione S-transferase isolated from Radix Angelicae sinensis, reverses multidrug resistance and downregulates P-glycoproteinEvid. Based Complement. Alternat. Med.639083(2013)
| Cas No. | 63644-62-2 | SDF | |
| 别名 | 阿魏酸松柏酯 | ||
| Canonical SMILES | O=C(OC/C=C/C1=CC=C(O)C(OC)=C1)/C=C/C2=CC=C(O)C(OC)=C2 | ||
| 分子式 | C20H20O6 | 分子量 | 356.37 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 3 mg/ml | 储存条件 | 4°C, protect from light |
| 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 | 2.8061 mL | 14.0304 mL | 28.0607 mL |
| 5 mM | 0.5612 mL | 2.8061 mL | 5.6121 mL |
| 10 mM | 0.2806 mL | 1.403 mL | 2.8061 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。
Oral Coniferyl ferulate attenuated depression symptoms in mice via reshaping gut microbiota and microbial metabolism
Food Funct 2021 Dec 13;12(24):12550-12564.PMID:34812830DOI:10.1039/d1fo02655k.
The gut microbiome is known to be involved in depression development. Thus, phytochemicals changing gut microbiota may alleviate depression-like behaviors. Coniferyl ferulate (CF) is a long studied natural product and known to alleviate psychiatric disorders. However, its mechanism of action remains unclear. In this experimental study, oral administration of 50 mg kg-1 CF once daily attenuated weight loss and depression-like and anxiety-like behaviors induced by chronic unpredicted mild stress (CUMS) in mice. Four weeks of CF administration significantly ameliorated colonic inflammation, lowered the levels of IL-6, IL-1β, and TNF-α, and restructured the gut microbiome, and microbial metabolism. Intestinal microbiota can impact the development and function of the brain via the microbiota-gut-brain axis. Therefore, oral administration of CF is a promising nutritional strategy to treat CUMS-induced depression via the regulation of microbiota and microbial metabolism.
Coniferyl ferulate exerts antidepressant effect via inhibiting the activation of NMDAR-CaMKII-MAPKs and mitochondrial apoptotic pathways
J Ethnopharmacol 2020 Apr 6;251:112533.PMID:31911178DOI:10.1016/j.jep.2019.112533.
Ethnopharmacological relevance: Xiaoyaosan (XYS), composed of Radix Bupleuri, Radix Angelicae Sinensis, Radix Paeoniae Alba, Rhizoma Atractylodis Macrocephalae, Poria, Herba Menthae, Rhizoma Zingiberis Recens and Radix Glycyrrhizae, is a valuable traditional Chinese medicine (TCM) which is used for the treatment of depression in China. In our previous experiments, we found that Coniferyl ferulate (CF) was the main active constituent of Xiaoyaosan based on UPLC-PDA guided isolation technique. However, the antidepressant effect and mechanisms of CF is still unknown. Aim of the study: In the current study, we aim to explore the possible mechanisms involved in the neuroprotective effect of CF in glutamate-injured PC12 cells, and further to confirm the anti-depressant effect of CF on the model of behavioral despair in vivo. Material and methods: The model of glutamate-injured PC12 cells was employed to investigate the possible mechanisms involved in the neuroprotective effect of CF. The model of behavioral despair was carried out to examine the in vivo anti-depressant effect of CF. Results: The results showed that CF significantly attenuated the decrease of cell viability, the release of lactate dehydrogenase (LDH), and the increase of apoptosis rates induced by glutamate. CF could also suppress the influx of Ca2+ and the elevation of p-NR2B, p-CaMK II, p-JNK, and p-p38 level induced by glutamate. Besides, CF could also inhibit the generation of reactive oxygen species (ROS), the decrease of SOD activity, the elevation of malondialdehyde (MDA) level, and suppress the loss of mitochondrial membrane potential (MMPs) and the activation Bcl-2/Bax mediated apoptotic pathways induced by glutamate. Furthermore, CF obviously decreased the immobility time in tail suspension test (TST) and forced swimming test (FST). Conclusion: In conclusion, CF exert the indeed anti-depressant effect. The inhibition of NMDAR-CaMKII-MAPKs signaling pathway, oxidative stress, and mitochondrial apoptotic pathways were involved in the anti-depressant effect of CF.
Coniferyl ferulate incorporation into lignin enhances the alkaline delignification and enzymatic degradation of cell walls
Biomacromolecules 2008 Sep;9(9):2510-6.PMID:18712922DOI:10.1021/bm800528f.
Incorporating ester interunit linkages into lignin could facilitate fiber delignification and utilization. In model studies with maize cell walls, we examined how partial substitution of coniferyl alcohol (a normal monolignol) with Coniferyl ferulate (an ester conjugate from lignan biosynthesis) alters the formation and alkaline extractability of lignin and the enzymatic hydrolysis of structural polysaccharides. Coniferyl ferulate moderately reduced lignification and cell-wall ferulate copolymerization with monolignols. Incorporation of Coniferyl ferulate increased lignin extractability by up to 2-fold in aqueous NaOH, providing an avenue for producing fiber with less noncellulosic and lignin contamination or of delignifying at lower temperatures. Cell walls lignified with Coniferyl ferulate were more readily hydrolyzed with fibrolytic enzymes, both with and without alkaline pretreatment. Based on our results, bioengineering of plants to incorporate Coniferyl ferulate into lignin should enhance lignocellulosic biomass saccharification and particularly pulping for paper production.
Development of a sensitive LC-MS/MS method for quantification of Coniferyl ferulate and its metabolite coniferyl alcohol in rat plasma: Application to a pharmacokinetic study
J Pharm Biomed Anal 2017 Nov 30;146:201-205.PMID:28886520DOI:10.1016/j.jpba.2017.08.033.
A rapid and simple LC-MS/MS method was developed and validated for the simultaneous determination of Coniferyl ferulate (CF) and its metabolite coniferyl alcohol (CA) using bavachromene as an internal standard (IS). A TSQ Quantum Access mass spectrometer was operated under selected-reaction monitoring mode using negative electrospray ionization. Extraction with ether was used in sample preparation. The plasma samples were prepared and then chromatographed on a Phenomenex Luna C18 column (2.1mm×50mm, 1.7μm; Torrance, USA) at 35°C, using acetonitrile: water (65:35, v/v) in an isocratic mode at a flow rate of 0.3mL/min. Method validation was performed as per the FDA guidelines and calibration curves showed good linearity over the concentration range of 2.5-1000ng/mL for both CF and CA. The intra- and inter-day precision and accuracy were within the acceptable limits. The developed assay was successfully applied to a pharmacokinetic study of CA in rats.
Coniferyl ferulate, a Strong Inhibitor of Glutathione S-Transferase Isolated from Radix Angelicae sinensis, Reverses Multidrug Resistance and Downregulates P-Glycoprotein
Evid Based Complement Alternat Med 2013;2013:639083.PMID:24058374DOI:10.1155/2013/639083.
Glutathione S-transferase (GST) is the key enzyme in multidrug resistance (MDR) of tumour. Inhibition of the expression or activity of GST has emerged as a promising therapeutic strategy for the reversal of MDR. Coniferyl ferulate (CF), isolated from the root of Angelica sinensis (Oliv.) Diels (Radix Angelicae sinensis, RAS), showed strong inhibition of human placental GST. Its 50% inhibition concentration (IC50) was 0.3 μ M, which was greater than a known GSTP1-1 inhibitor, ethacrynic acid (EA), using the established high-throughput screening model. Kinetic analysis and computational docking were used to examine the mechanism of GST inhibition by CF. Computational docking found that CF could be fully docked into the gorge of GSTP1-1. The further exploration of the mechanisms showed that CF was a reversible noncompetitive inhibitor with respect to GSH and CDNB, and it has much less cytotoxicity. Apoptosis and the expression of P-gp mRNA were evaluated in the MDR positive B-MD-C1 (ADR+/+) cell line to investigate the MDR reversal effect of CF. Moreover, CF showed strong apoptogenic activity and could markedly decrease the overexpressed P-gp. The results demonstrated that CF could inhibit GST activity in a concentration-dependent manner and showed a potential MDR reversal effect for antitumour adjuvant therapy.