Garcinol Is an HDAC11 Inhibitor,ACS Chemical Biology

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Garcinol Is an HDAC11 Inhibitor
ACS Chemical Biology ( IF 3.5 ) Pub Date : 2020-10-09 , DOI: 10.1021/acschembio.0c00719
Se In Son ₁ , Dan Su ₁ , Thanh Tu Ho ₁ , Hening Lin _{1,

2}

Affiliation

Garcinol is a natural product from the Garcinia Indica fruit and is well-known as an antioxidant, anti-inflammatory, and anticancer agent. However, the understanding of its mechanism of action is still incomplete. It has been reported to be a histone acetyltransferase (HAT) inhibitor. Here, we surprisingly found that garcinol is a potent histone deacetylase 11 (HDAC11) inhibitor (IC₅₀ ∼ 5 μM in vitro with the HPLC assay and IC₅₀ ∼ 10 μM in the cellular SHMT2 fatty acylation assay), which is comparable to previously reported HDAC11 inhibitors. Additionally, among all the HDACs tested, garcinol specifically inhibits HDAC11 over other HDACs. HDAC11 is the only class IV HDAC, and there are very few inhibitors available for it. Therefore, this study provides a new HDAC11 inhibitor lead from natural products and may help explain the various biological activities of garcinol.

中文翻译：

Garcinol 是一种 HDAC11 抑制剂

Garcinol 是来自Garcinia Indica果实的天然产物，是众所周知的抗氧化剂、抗炎剂和抗癌剂。然而，对其作用机制的了解仍不完全。据报道，它是一种组蛋白乙酰转移酶 (HAT) 抑制剂。在这里，我们令人惊讶地发现，garcinol 是一种有效的组蛋白脱乙酰酶 11 (HDAC11) 抑制剂（体外 HPLC 测定的IC ₅₀ ∼ 5 μM 和 IC ₅₀在细胞 SHMT2 脂肪酰化试验中约为 10 μM），这与之前报道的 HDAC11 抑制剂相当。此外，在所有测试的 HDAC 中，与其他 HDAC 相比，garcinol 特异性抑制 HDAC11。HDAC11 是唯一的 IV 类 HDAC，可用的抑制剂很少。因此，本研究从天然产物中提供了一种新的 HDAC11 抑制剂铅，可能有助于解释 Garcinol 的各种生物活性。

更新日期：2020-11-21

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