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                同义名:
                    
                        
                            3,4,5-三羟基苯甲酸甲酯
                            
                             / Gallincin; NSC 363001
                            
                        
                    
                
                
                
                    
                     
                
            
Methyl gallate是一种逆转录酶抑制剂,分离自大戟树(Sapium sebiferum),具有抗氧化、抗癌和抗炎活性,并对 HIV-1 和相关酶具有抑制作用。
 
                                 
                                
                            

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| 描述 | Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. The growth of A. viscosus is inhibited completely by a low dose of Methyl gallate (MIC=1 mg/mL). S. mutans and . sobrinus show intermediate sensitivity to Methyl gallate (MIC=2-4 mg/mL), whereas the growth of Lactobacillus spp. is inhibited completely at a relatively high concentration (MIC=8 mg/mL)[3]. MG (Methyl gallate) effectively inhibited the growth of both promastigote (IC50 5.71 μM) and amastigote-like forms (EC50 5.39 μM), with much higher selectivity indexes than the reference drugs, being more benign towards J774A.1 macrophages than meglumine antimoniate and amphotericin B, at 1631- and 70.92-fold respectively, with respect to the promastigote form. Additionally, MG proved to be even more active against intracellular amastigotes of the parasite (EC50 4.24 μM). In addition, MG induced increased phagocytic capability, and lysosomal volume in macrophages; structural parameters of microbicidal activity[4]. Methyl gallate, in a concentration of 100 mM, could alleviate lipid peroxidation of the cells exposed to a short-term H2O2 treatment. In addition, Methyl gallate-treated cells could prevent intracellular glutathione (GSH) from being depleted following an exposure of H2O2 (8.0 mM) for a 3 h period[5]. Methyl gallate inhibits Treg cell-suppressive effects on effector CD4+ T cells and Treg migration toward tumor environment. Furthermore, forkhead box P3 (Foxp3) expression is also significantly decreased by methyl gallate[6]. | 
| Concentration | Treated Time | Description | References | |
| RAW264.7 cells | 5, 10, 20 µg/mL | 24 hours | MG inhibited LPS-induced NO production, regulated macrophage polarization, and suppressed pro-inflammatory cytokine expression. | Int J Mol Sci. 2022 Nov 14;23(22):14024. | 
| Methicillin-susceptible Staphylococcus aureus (MSSA) | 64 mg/mL | 24 hours | Evaluated antibacterial activity, forming inhibition zones of approximately 19 mm | Polymers (Basel). 2024 Dec 24;17(1):7. | 
| Methicillin-resistant Staphylococcus aureus (MRSA) | 64 mg/mL | 24 hours | Evaluated antibacterial activity, forming inhibition zones of approximately 19 mm | Polymers (Basel). 2024 Dec 24;17(1):7. | 
| Differentiated Caco-2 cells | 30 µg/mL and 90 µg/mL | 48 hours | MG showed no cytotoxic effects on differentiated Caco-2 cells. | Antioxidants (Basel). 2023 Jun 16;12(6):1292. | 
| LO2 cells | 20, 40, 80, 160, 320, 640 µM | 48 hours | MG showed minimal toxicity in human normal hepatocyte LO2 cells. | Front Pharmacol. 2022 Jun 13;13:894285. | 
| Plasmodium falciparum W2 | 0.61 µg/mL | 72 hours | Antimalarial activity with IC50 value of 0.61 µg/mL | Molecules. 2022 Dec 1;27(23):8382. | 
| Plasmodium falciparum D6 | 1.57 µg/mL | 72 hours | Antimalarial activity with IC50 value of 1.57 µg/mL | Molecules. 2022 Dec 1;27(23):8382. | 
| Human peripheral blood mononuclear cells (PBMCs) | 10 and 50 µM | Inhibited IL-1β release in ATP-treated PBMCs | Front Pharmacol. 2021 Dec 20;12:759040. | |
| Ralstonia solanacearum | 25 mg/ml | Evaluate the antibacterial activity of methyl gallate against Ralstonia solanacearum | Front Microbiol. 2021 Feb 4;11:598692. | |
| Administration | Dosage | Frequency | Description | References | ||
| C57BL/6 mice | High-fat diet-induced obesity model | Oral | 0.1% | For 14 weeks | Evaluate the effects of VFP or VFPE on weight gain, fat accumulation, glucose and insulin tolerance, energy expenditure, mitochondrial function, hepatic and renal protection, found that VFP and VFPE prevented obesity, improved metabolic flexibility, increased energy expenditure, and protected liver and kidney | Int J Mol Sci. 2023 Apr 28;24(9):7984 | 
| ICR mice | LPS-induced osteoporosis model | Oral | 10 mg/kg | Every 8 days for 8 days | Methyl gallate restored LPS-induced osteoporotic phenotype by inhibiting osteoclast formation and bone-resorbing activity. | Int J Mol Sci. 2017 Mar 7;18(3):581 | 
| C57BL/6 mice | Hyperuricemia nephropathy (HN) model | Oral | 20 and 40 mg/kg | Once daily for 28 days | Significantly ameliorated HN by inhibiting uric acid production and promoting uric acid excretion as well as ameliorating renal injury induced by NLRP3 activation | Front Pharmacol. 2021 Dec 20;12:759040. | 
| BALB/C nude mice | Xenograft tumor model | Intragastric | 40, 80, 160 mg/kg | Once daily for 21 days | MG significantly inhibited the growth of HCC xenografts, with tumor inhibition rates of 49.94%, 52.66%, and 55.92% respectively. | Front Pharmacol. 2022 Jun 13;13:894285. | 
| C57BL/6J mice | DSS-induced ulcerative colitis model | Oral | 50, 100, 200 mg/kg | Once daily for 6 days | MG alleviated body weight loss, improved colon length and histological damage, modulated gut microbiota, and inhibited TLR4/NF-κB pathway. | Int J Mol Sci. 2022 Nov 14;23(22):14024. | 
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 | 
| NCT00917735 | Breast Cancer | Phase 2 | Completed | - | United States, Minnesota ... 展开 >> Fairview Southdale Breast Center Edina, Minnesota, United States, 55435 Fairview Maple Grove Breast Center Maple Grove, Minnesota, United States, 55369 University of Minnesota Medical Center (UMMC) Breast Clinic Minneapolis, Minnesota, United States, 55455 Park Nicollet Institute St. Louis Park, Minnesota, United States, 55426 Food Science and Nutrition, University of Minnesota St. Paul, Minnesota, United States, 55108 收起 << | 
| NCT01699711 | Down Syndrome (DS) | Phase 2 | Completed | - | Spain ... 展开 >> IMIM (Institut Hospital del Mar d'Investigacions Mèdiques) Barcelona, Spain, 08003 收起 << | 
| NCT00917735 | - | Completed | - | - | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 5.43mL 1.09mL 0.54mL | 27.15mL 5.43mL 2.72mL | 54.30mL 10.86mL 5.43mL | |
| CAS号 | 99-24-1 | 
| 分子式 | C8H8O5 | 
| 分子量 | 184.15 | 
| SMILES Code | O=C(OC)C1=CC(O)=C(O)C(O)=C1 | 
| MDL No. | MFCD00002194 | 
| 别名 | 3,4,5-三羟基苯甲酸甲酯 ;Gallincin; NSC 363001; Gallicin; Gallic acid methyl ester | 
| 运输 | 蓝冰 | 
| InChI Key | FBSFWRHWHYMIOG-UHFFFAOYSA-N | 
| Pubchem ID | 7428 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, room temperature | 
| 溶解方案 | DMSO: 105 mg/mL(570.2 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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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