hepatoma

α-Lipoic Acid (DL-α-Lipoic acid) 是线粒体酶复合物的重要辅助因子，是一种抗氧化剂，可抑制NF-κB 依赖性的HIV-1LTR 活化。它还可诱导内质网应激介导的肝癌细胞凋亡。

Mestranol (Devocin) 是一种雌激素受体激动剂，是一种非活性的前药，在转化为炔雌醇时具有生物活性。动物实验中，它可以与黄体酮联合使用，它可用于更年期激素或月经紊乱的研究。

Matrine (Vegard) 是一种从槐属植物中分离出来的生物碱，可作为一种κ阿片受体激动剂，有抗肿瘤活性。

Isofraxidin (Phytodolor) 是来自刺五加的香豆素成分，抑制MMP-7表达和人肝癌细胞侵袭。它作用于肝癌细胞，抑制ERK1/2磷酸化。它减弱iNOS 和COX-2表达，还抑制TLR4/髓样分化蛋白 2 复合物的形成。

Epirubicin hydrochloride (Pharmorubicin) 是一种阿霉素衍生物，一种拓扑异构酶 (Topo) 抑制剂，也是一种 Forkhead box 蛋白 p3 (Foxp3) 抑制剂。Epirubicin hydrochloride 具有抗肿瘤活性。

1,4-Chrysenequinone (Chrysene-1,4-dione) 是多环芳香烃类，是芳烃受体 (AhR) 的激活剂

(S)-10-Hydroxycamptothecin (10-HCPT) 是一种从喜树中分离的 DNA 拓扑异构酶 I 抑制剂。它显著诱导细胞凋亡，可研究肝癌、胃癌、结肠癌和白血病。

Berberine (Umbellatine) 属于生物碱类天然产物，可以激活 AMPK、抑制 DNA 拓扑异构酶、诱导 ROS 生成。Berberine 具有抗肿瘤、抗菌、降血糖、降血脂等生物学活性。

Nur77 modulator 1 可与Nur77结合，KD 为 3.58 μM。它上调 Nur77 表达，介导Nur77亚细胞定位，诱导Nur77 依赖的内质网应激和自噬，可导致细胞凋亡，Nur77 modulator 1显示出抗肝癌生物活性。

Melatonin-D4 is a hormone produced by the pineal gland,known for its role as a selective ATF-6 inhibitor that promotes apoptosis in human hepatoma cells via COX-2 downregulation. Additionally,it activates melatonin receptors and exhibits antioxidative and anti-inflammatory properties.

Alternariol 是从 Etoac 提取的天然产物，在小鼠肝癌细胞与人血清体系中表现出抗炎活性，并影响 TLR 信号通路及促凋亡蛋白表达。同时研究显示 Alternariol 对甲基转移酶不具抑制作用，为其代谢失活特征提供参考。

Musk tibetine reveals no genotoxicity in the micronucleus test with human lymphocytes and human hepatoma cell lines. Musk tibetene is a nitro musk compound with carcinogenic activity.

HDGFRP2/PSIP1-IN-1 (compound BPP) 为针对HDGFRP2及PSIP1的PWWP结构域的双重抑制剂，有效阻断弥漫性内在脑桥胶质瘤 (DIPG) 的形成与进展。该化合物与HDGFRP2的结合Kd值为7 μM，配体效率为0.47；与PSIP1的PWWP结构域的结合Kd值为27 μM；对HDGFRP3的Kd值为14 μM，证实了其作为HDGFRP2PWWP亚家族抑制剂的潜力。

2,3,4,6,7,8-Hexachlorodibenzofuran (2,3,4,6,7,8-HxCDF) 是一种属于polychlorinated dibenzofuran (PCDF)的化合物。2,3,4,6,7,8-HxCDF 在H-4-II-E大鼠肝癌细胞中诱导芳烃羟化酶 (AHH) 和乙氧基间苯甲素-o-去乙基化酶 (EROD) 基因的表达 (EC50s = 0.687 和 0.575 nM)。

1,2,3,6,7,8-Hexachlorodibenzofuran (1,2,3,6,7,8-HxCDF) 是一种属于多氯二苯并呋喃 (PCDF) 的化合物。它能在 H-4-II-E 大鼠肝癌细胞中诱导芳烃羟化酶 (AHH) 和乙氧基间苯甲素-O-去乙基化酶 (EROD) 基因的表达，EC50s 分别为 1.47 和 1.24 nM。此化合物可降低大鼠体重，导致胸腺萎缩，并诱导细胞色素 P450 (CYP) 亚型 CYP1A1 和 4-chlorobiphenyl hydroxylase 基因表达，EC50s 分别为 3.2、0.9、0.35 和 0.21 µmol/kg。

193 D7 是一种具备口服生物活性的选择性 JMJD1C 抑制剂，其 IC50 为 0.59 μM，Kd 为 1.96 μM。在 HTRF 检测中，193 D7可阻断 JMJD1C 与 H3K9me2 多肽底物的结合，对应 IC50 为 1.47 μM。193 D7通过双重作用机制调控肿瘤微环境中调节性 T 细胞（Treg）的适应性：一方面促进 H3K9me2 富集进而下调 PD1 表达，另一方面抑制 STAT3 去甲基化以提升 STAT3 活化水平。在 MCA205 纤维肉瘤、B16-F10 黑色素瘤、LLC 肺癌、Hepa1-6 肝癌及 CT26 结直肠癌等多种小鼠肿瘤模型中，193 D7均表现出剂量依赖性的抗肿瘤活性，可作为选择性靶向肿瘤内 Treg 细胞的工具分子应用于肿瘤免疫相关机制研究。

Heliotrine leads to apoptosis of the human hepatoma cell line HepaRG.

Galegine hemisulfate是一种胍衍生物，有助于小鼠的体重减轻。它在3T3-L1脂肪细胞、L6肌管、H4IIE大鼠肝癌和HEK293人肾细胞系中激活AMPK。Galegine hemisulfate具备抗菌活性，对金黄色葡萄球菌菌株 (Staphylococcus aureus) 的最低抑菌浓度为4 mg/L。

6-Alkynyl-fucose, a widely used fucosylation probe, acts by strongly inhibiting fucosylation and GDP-fucose synthetase FX and halting hepatoma invasion.

Arcapillin, an anticancer agent, induces apoptosis mediated at least in part by the ERS pathway and inhibits hepatoma tumor growth.

SC-III3 is a novel scopoletin derivative, induces autophagy of human hepatoma HepG2 cells through AMPK/mTOR signaling pathway by acting on mitochondria. SC-III3 reduces the viability of HepG2 cells and tumor growth of HepG2 xenograft mouse model. It induc

Heteroatom-substituted fatty acids have been observed to modulate the extension and desaturating of fatty acids, and to influence their distribution within phospholipids pools. 10-Thiastearic acid inhibits desaturation of radiolabeled stearate to oleate in rat hepatocytes and hepatoma cells by more than 80% at a concentration of 25 μM. This activity is associated with a hypolipidemic effect, making this 10-thiastearic acid a useful tool for evaluating new anti-obesity therapeutics.

Galegine hydrochloride, a guanidine derivative derived from G. officinalis, plays a role in inducing weight loss in mice and has contributed to the development of biguanides, including metformin and phenformin. This compound stimulates AMPK activation in 3T3-L1 adipocytes, L6 myotubes, H4IIE rat hepatoma, and HEK293 human kidney cell lines. Additionally, galegine hydrochloride exhibits antibacterial properties, particularly demonstrating a minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains[1][2].

Destruxin B2 is a cyclic hexadepsipeptide mycotoxin that has been found in M. anisopliae and has antiviral, insecticidal, and phytotoxic activities.1,2,3 It inhibits secretion of hepatitis B virus surface antigen (HBsAg) by Hep3B cells expressing hepatitis B virus (HBV) DNA (IC50 = 1.3 μM).1 Destruxin B2 is toxic to Sf9 insect cells in an electric cell-substrate impedance sensing (ECIS) test with a 50% inhibitory concentration (ECIS50) value of 92 μM.4 It is also phytotoxic to B. napus leaves.3 |1. Yeh, S.F., Pan, W., Ong, G.-T., et al. Study of structure-activity correlation in destruxins, a class of cyclodepsipeptides possessing suppressive effect on the generation of hepatitis B virus surface antigen in human hepatoma cells. Biochem. Biophys. Res. Commun. 229(1), 65-72 (1996).|2. Male, K.B., Tzeng, Y.-M., Montes, J., et al. Probing inhibitory effects of destruxins from Metarhizium anisopliae using insect cell based impedance spectroscopy: Inhibition vs chemical structure. Analyst 134(7), 1447-1452 (2009).|3. Buchwaldt, L., and Green, H. Phytotoxicity of destruxin B and its possible role in the pathogenesis of Alternaria brassicae. Plant Pathol. 41(1), 55-63 (1992).