Methyl brevifolincarboxylate
(Synonyms: 短叶苏木酚酸甲酯) 目录号 : GC61052
Methylbrevifolincarboxylate(Brevifolincarboxylicacidmethylester)是一种有效的流感病毒PB2帽结合抑制剂。Methylbrevifolincarboxylate对流感病毒A/PuertoRico/8/34(H1N1)和A/Aichi/2/68(H3N2)具有抑制作用,IC50值分别为27.16μM和33.41μM。具有抗氧化活性。
Cas No.:154702-76-8
Sample solution is provided at 25 µL, 10mM.
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Methyl brevifolincarboxylate (Brevifolincarboxylic acid methyl ester) is a potent influenza virus PB2 cap-binding inhibitor. Methyl brevifolincarboxylate exhibits inhibitory activity against influenza virus A/Puerto Rico/8/34 (H1N1) and A/Aichi/2/68 (H3N2) with IC50s of 27.16 μM and 33.41 μM. Anti-oxidant activity[1][2].
Methyl brevifolincarboxylate exhibits significant DPPH radical scavenging activity with an IC50 value of 8.9 μM.
[1]. Wu QY, et al. Chromatographic fingerprint and the simultaneous determination of five bioactive components of geranium carolinianum L. water extract by high performance liquid chromatography. Int J Mol Sci. 2011;12(12):8740-8749. [2]. Fang SH, et al. Anti-oxidant and inflammatory mediator's growth inhibitory effects of compounds isolated from Phyllanthus urinaria. J Ethnopharmacol. 2008;116(2):333-340.
Cas No. | 154702-76-8 | SDF | |
别名 | 短叶苏木酚酸甲酯 | ||
Canonical SMILES | O=C(C1CC(C2=C1C3=C(O)C(O)=C(O)C=C3C(O2)=O)=O)OC | ||
分子式 | C14H10O8 | 分子量 | 306.22 |
溶解度 | 储存条件 | Store at -20°C | |
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1 mg | 5 mg | 10 mg |
1 mM | 3.2656 mL | 16.3281 mL | 32.6563 mL |
5 mM | 0.6531 mL | 3.2656 mL | 6.5313 mL |
10 mM | 0.3266 mL | 1.6328 mL | 3.2656 mL |
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Methyl brevifolincarboxylate, a novel influenza virus PB2 inhibitor from Canarium Album (Lour.) Raeusch
Chem Biol Drug Des 2020 Nov;96(5):1280-1291.PMID:32519462DOI:10.1111/cbdd.13740.
Methyl brevifolincarboxylate (MBC) was isolated from ethyl acetate extract of Canarium album (Lour.) Raeusch. The structure was identified, and the effect on influenza A virus infection was evaluated. MBC exhibited inhibitory activity against influenza virus A/Puerto Rico/8/34 (H1N1) and A/Aichi/2/68 (H3N2) with IC50 values of 27.16 ± 1.39 μM and 33.41 ± 2.34 μM. Mechanism studies indicated that MBC inhibited the replication of influenza A virus by targeting PB2 cap-binding domain. Our results demonstrated MBC was a potent PB2 cap-binding inhibitor and represented as a new type of promising lead compound for the development of anti-influenza virus drugs from natural products.
Methyl brevifolincarboxylate Attenuates Free Fatty Acid-Induced Lipid Metabolism and Inflammation in Hepatocytes through AMPK/NF-κB Signaling Pathway
Int J Mol Sci 2021 Sep 17;22(18):10062.PMID:34576229DOI:10.3390/ijms221810062.
The prevalence of non-alcoholic fatty liver disease (NAFLD) is one of the leading causes of chronic liver diseases worldwide. This study examined the potential protective effects of a naturally occurring polyphenolic compound, Methyl brevifolincarboxylate (MBC) on fatty liver injury in vitro. The results showed that MBC at its non-cytotoxic concentrations, reduced lipid droplet accumulation and triglyceride (TG) levels in the oleic acid (OA)-treated human hepatocarcinoma cell line, SK-HEP-1 and murine primary hepatocytes. In OA-treated SK-HEP-1 cells and primary murine hepatocytes, MBC attenuated the mRNA expression levels of the de novo lipogenesis molecules, acetyl-coenzyme A carboxylase (Acc1), fatty acid synthase (Fasn) and sterol regulatory element binding protein 1c (Srebp1c). MBC promoted the lipid oxidation factor peroxisome proliferator activated receptor-α (Pparα), and its target genes, carnitine palmitoyl transferase 1 (Cpt1) and acyl-coenzyme A oxidase 1 (Acox1) in both the SK-HEP-1 cells and primary murine hepatocytes. The mRNA results were further supported by the attenuated protein expression of lipogenesis and lipid oxidation molecules in OA-treated SK-HEP-1 cells. The MBC increased the expression of AMP activated protein kinase (AMPK) phosphorylation. On the other hand, MBC treatment dampened the inflammatory mediator's, tumor necrosis factor (TNF)-α, interleukin-6 (IL-6), IL-8, and IL-1β secretion, and nuclear factor (NF)-κB expression (mRNA and protein) through reduced reactive oxygen species production in OA-treated SK-HEP-1 cells. Taken together, our results demonstrated that MBC possessed potential protective effects against NAFLD in vitro by amelioration of lipid metabolism and inflammatory markers through the AMPK/NF-κB signaling pathway.
Inhibitory effects of Methyl brevifolincarboxylate isolated from Phyllanthus niruri L. on platelet aggregation
Biol Pharm Bull 2007 Feb;30(2):382-4.PMID:17268086DOI:10.1248/bpb.30.382.
A platelet-aggregatory inhibitor was isolated from the 50% MeOH extract of Phyllanthus niruri L. leaf. Its structure was determined to be Methyl brevifolincarboxylate on the basis of the 1H-, 13C-NMR, and high-resolution mass spectral data. We compared the antiplatelet aggregatory effects of the constituent with adenosine, a well-known inhibitor of platelet aggregation. Platelet aggregation was induced by collagen or adenosine 5'-diphosphate as an activating agent; the extent of inhibition was monitored with a platelet aggregometer employing a laser-scattering method. The inhibitory effects of Methyl brevifolincarboxylate were found to be as potent as adenosine that is known to act on an A2A subtype receptor.
Vasorelaxant effects of Methyl brevifolincarboxylate from the leaves of Phyllanthus niruri
Biol Pharm Bull 2006 Jan;29(1):177-9.PMID:16394535DOI:10.1248/bpb.29.177.
Methyl brevifolincarboxylate (1) isolated from the leaves of Phyllanthus niruri L. showed a vasorelaxant effect on rat aortic rings. Compound 1 exhibited slow relaxation activity against norepinephrine (NE)-induced contractions of rat aorta with or without endothelium. The compound did not affect contractions induced by a high concentration (60 mM) of K+, whereas it inhibited NE-induced vasocontraction in the presence of nicardipine. These results suggest that the inhibition of NE-induced vasocontraction by compound 1 is in part attributable to a decrease in [Ca2+]i through receptor-operated Ca2+ channels.
[Phenols from Euphorbia humifusa]
Zhongguo Zhong Yao Za Zhi 2010 Mar;35(5):613-5.PMID:20506823DOI:10.4268/cjcmm20100516.
The investigation on the herbal of Euphorbia humifusa Wild. was carried out to find its anti-HBV constituents. The isolation and purification were performed by chromatography such as macroporous resin, polyamide, Sephadex LH-20, MCI GEL CHP 20P and so on. Based on the spectral analysis, seven phenols were identified as brevifolin (1), brevifolin carboxylic acid (2), Methyl brevifolincarboxylate (3), phyllanthussin E methyl ester (4), sanguisorbic acid dilactone (5), 3,3'-2-di-O-methyl ellagic acid (6), ellagic acid (7). Among them, Compounds 2-6 were isolated from this plant for the first time.