生物活性

• 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].
• 临床研究

• 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 ... more >> 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 Collapse <<
  NCT01699711	Down Syndrome (DS)	Phase 2	Completed	-	Spain ... more >> IMIM (Institut Hospital del Mar d'Investigacions Mèdiques) Barcelona, Spain, 08003 Collapse <<
  NCT00917735	-	-	Completed	-	-

• 参考文献

• [1] Baek JM, Kim JY, et al. Methyl Gallate Inhibits Osteoclast Formation and Function by Suppressing Akt and Btk-PLCγ2-Ca(2+) Signaling and Prevents Lipopolysaccharide-Induced Bone Loss. Int J Mol Sci. 2017 Mar 7;18(3). pii: E581.

  [2] Jeon M, Rahman N, Kim YS. Wnt/β-catenin signaling plays a distinct role in methyl gallate-mediated inhibition of adipogenesis. Biochem Biophys Res Commun. 2016 Oct 7;479(1):22-7.

  [3] Kang MS, Oh JS, Kang IC, Hong SJ, Choi CH. Inhibitory effect of methyl gallate and gallic acid on oral bacteria. J Microbiol. 2008 Dec;46(6):744-50

  [4] Noleto Dias C, Nunes TAL, Sousa JMS, Costa LH, Rodrigues RRL, Araújo AJ, Marinho Filho JDB, da Silva MV, Oliveira MR, Carvalho FAA, Rodrigues KADF. Methyl gallate: Selective antileishmanial activity correlates with host-cell directed effects. Chem Biol Interact. 2020 Apr 1;320:109026

  [5] Hsieh TJ, Liu TZ, Chia YC, Chern CL, Lu FJ, Chuang MC, Mau SY, Chen SH, Syu YH, Chen CH. Protective effect of methyl gallate from Toona sinensis (Meliaceae) against hydrogen peroxide-induced oxidative stress and DNA damage in MDCK cells. Food Chem Toxicol. 2004 May;42(5):843-50

  [6] Lee H, Lee H, Kwon Y, Lee JH, Kim J, Shin MK, Kim SH, Bae H. Methyl gallate exhibits potent antitumor activities by inhibiting tumor infiltration of CD4+CD25+ regulatory T cells. J Immunol. 2010 Dec 1;185(11):6698-705

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