许多天然产物通过干扰细胞表观遗传机制来发挥抗癌或化学预防活性。虽然大量研究表明影响DNA甲基化和组蛋白乙酰化的相关性，但往往忽视了相关于组蛋白甲基化的机制的影响。这可能与迟滞的证据相关，即组蛋白甲基化编写酶和抹消酶作用的改变以及随后的组蛋白甲基化图谱的变化与癌变有因果关系。然而，最近的动物研究表明，靶向组蛋白甲基化/去甲基化会影响实验性致癌的进程。现有数据表明，许多不同化学类别的天然化合物，包括绿茶多酚和其他黄酮类、姜黄素类、二苯乙烯衍生物、酚酸类、异硫氰酸酯、生物碱和萜烯，可以影响参与组蛋白赖氨酸和精氨酸甲基化和去甲基化的关键酶的表达和活性。这些活性已与调节与癌症相关的基因表达和功能变化相关，包括在各种癌症模型中减少细胞增殖和迁移，并增强细胞凋亡。大多数研究集中在调节两种蛋白质的表达和/或活性上 - EZH2（H3K27甲基转移酶）和LSD1（H3K4/9去甲基酶），或通过植物化学物质对全局组蛋白甲基化标记的影响，但有关其他组蛋白甲基转移酶或去甲基酶的数据很少。虽然该领域仍然相对未开发，本综述旨在探讨天然产物对与组蛋白甲基化/去甲基化相关的酶的影响，展示其与癌症发生和癌症进展的相关性。本文受版权保护，版权所有。

Many natural products can exert anticancer or chemopreventive activity by interfering with the cellular epigenetic machinery. While a plethora of studies indicate the relevance of affecting DNA methylation and histone acetylation, the influence on the mechanisms related to histone methylation is often overlooked. This may be associated with the lagging evidence that changes in the action of histone methylation writers and erasers and subsequent alterations in the profile of histone methylation are causally related with carcinogenesis. However, recent animal studies have shown that targeting histone methylation/demethylation affects the course of experimentally induced carcinogenesis. Existing data suggest that numerous natural compounds from different chemical groups, including green tea polyphenols and other flavonoids, curcuminoids, stilbene derivatives, phenolic acids, isothiocyanates, alkaloids and terpenes, can affect the expression and activity of crucial enzymes involved in the methylation and demethylation of histone lysine and arginine residues. These activities have been associated with the modulation of cancer-related gene expression and functional changes, including reduced cell proliferation and migration, and enhanced apoptosis in various cancer models. Most studies focused on the modulation of the expression and/or activity of two proteins - EZH2 (a H3K27 methyltransferase) and LSD1 (a H3K4/9 demethylase), or the effects on the global levels of histone methylation marks by the phytochemicals, but data regarding other histone methyltransferases or demethylases are scarce. While the field still remains relatively unexplored, this review aims to explore the impact of natural products on the enzymes related to histone methylation/demethylation, showing their relevance to carcinogenesis and cancer progression.This article is protected by copyright. All rights reserved.