Apicidin，一种天然真菌代谢物，是HDAC的选择性抑制剂。

组蛋白去乙酰酶（HDAC）移除组蛋白ε-N-乙酰赖氨酸的乙酰基。据悉，通过对组蛋白赖氨酸残基的可逆性乙酰化作用，组蛋白乙酰转移酶和组蛋白去乙酰化酶在转录激活或抑制基因表达方面起着重要的作用。

Apicidin对顶复门寄生虫具有强效而广泛的活性[1]。实验还表明，它在人类和小鼠肿瘤细胞株中具有强效的抗血管生成活性以及降低HIF-1α的水平[2]。

Apicidin也被广泛地用于体内研究，以明确HDAC在不同生理过程中的作用。Apicidin对小鼠中的不同癌细胞系显现出抗增殖活性[3]。在人结肠癌HCT-116异种移植肿瘤模型中，Apicidin抑制肿瘤生长[4]。同时，它在Ishikawa细胞异种移植肿瘤模型中也显现出抗肿瘤活性[5]。

参考文献：
1.  Darkin-Rattray SJ, Gurnett AM, Myers RW, Dulski PM, Crumley TM, Allocco JJ, et al. Apicidin: a novel antiprotozoal agent that inhibits parasite histone deacetylase. Proc Natl Acad Sci U S A 1996, 93:13143-13147.
2.  Kim SH, Jeong JW, Park JA, Lee JW, Seo JH, Jung BK, et al. Regulation of the HIF-1alpha stability by histone deacetylases. Oncol Rep 2007, 17:647-651.
3.  Han JW, Ahn SH, Park SH, Wang SY, Bae GU, Seo DW, et al. Apicidin, a histone deacetylase inhibitor, inhibits proliferation of tumor cells via induction of p21WAF1/Cip1 and gelsolin. Cancer Res 2000, 60:6068-6074.
4.  Jones P, Altamura S, De Francesco R, Paz OG, Kinzel O, Mesiti G, et al. A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo. J Med Chem 2008, 51:2350-2353.
5.  Ahn MY, Chung HY, Choi WS, Lee BM, Yoon S, Kim HS. Anti-tumor effect of apicidin on Ishikawa human endometrial cancer cells both in vitro and in vivo by blocking histone deacetylase 3 and 4. Int J Oncol 2010, 36:125-131.