si-2

SI-2是类固醇受体辅激活因子-3（SRC-3或 AIB1）的抑制剂（SMI）。SI-2可选择性降低细胞中 SRC-3的转录活性和蛋白浓度，并选择性诱导低纳摩尔范围（3-20 nM）内的乳腺癌症细胞死亡，但不影响正常细胞存活率。

(E)-SI-2 是类固醇受体 coactivator-3（SRC-3 或 AIB1）的有效小分子抑制剂，可选择性抑制 SRC-3 的内在转录活性，也抑制 SRC-1 和 SRC-2。它选择性地降低 SRC-3 的细胞蛋白水平，但不降低 CARM-1 的细胞蛋白水平，阻断 MDA-MB-468 细胞生长，IC50 值为 3.4 nM，但不影响正常细胞。

SI-2 hydrochloride (EPH 116 hydrochloride) 是 SRC-3 的抑制剂，诱导乳腺癌细胞死亡的 IC50 值为 3-20 nM。SI-2 hydrochloride 具有良好的药代动力学特征和改善的毒性，以及可接受的口服可用性。

Beauveriolide I is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.78 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide I also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 6 μM).2 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)

Beauveriolide III is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.41 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide III also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 5.5 μM).2Beauveriolide III (25 and 50 mg kg) reduces the size of aortic atherosclerotic lesions inLdlr- -andApoE- -mouse models of atherosclerosis. 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)

Caffeoylcalleryanin demonstrated potent inhibitory activity against 15-lipoxygenase (15-LOX), with an IC50 value of 1.59 μM. Furthermore, ethanol extract from A. pulchra leaves (EEAPL) was found to contain compounds exhibiting antiviral properties, particularly effective against Dengue virus type 2 (DENV-2). Among these compounds, Caffeoylcalleryanin emerged as the most potent anti-DENV-2 agent, achieving a selectivity index (SI) of 20.0.