anti-glioma

trans-AUCB (t-AUCB) 是口服具有活力的、选择性的可溶性环氧水解酶 (sEH) 抑制剂，对人，小鼠和大鼠的 sEH 的IC50分别为 1.3 nM，8 nM，8 nM。它具有抗神经胶质瘤特性。

Hydroxygenkwanin (Luteolin 7-methylether) 是一种丁香达芙妮的主要成分，是一种天然的类黄酮化合物。它具有抗氧化，抗神经胶质瘤能力和抗癌作用。

U-83836E (lazaroid ) 具有神经保护活性和抗肿瘤活活性，抑制神经胶质瘤细胞增殖，抑制肿瘤坏死因子并逆转内毒素诱导的休克。

(±)-α-Bisabolol (Bisabolol) 是一种从洋甘菊、念珠菌树等植物精油中提取的倍半萜烯醇，是一种天然防腐剂，具有舒缓、抗刺激、抗炎、抗氧化和抗癌活性。(±)-α-Bisabolol 通过诱导细胞周期停滞、线粒体死亡和抑制 PI3K/Akt 信号通路来发挥作用，对 A549 NSC-LC 细胞产生抗癌作用 (IC50 = 15 μM)。(±)-α-Bisabolol 能强效诱导胶质瘤细胞凋亡。

Cycloartenol (Handianol) 是一种广泛存在于植物中的植物甾醇类化合物，具有抗炎、抗肿瘤、抗氧化和抗菌活性，抑制胶质瘤细胞的迁移，抑制 p38 MAPK 的磷酸化，可用于研究植物生长发育。

USL311 是选择性 CXCR4拮抗剂，可防止基质细胞衍生因子 1（SDF-1 或 CXCL12）与 CXCR4 结合。它抑制 CXCR4 活化并减少表达 CXCR4 的肿瘤细胞的增殖和迁移，具有抗肿瘤活性。

Imipramine Blue chloride 是一种有效抑制神经胶质瘤侵袭的化合物。它能够抑制 NADPH 氧化酶介导的活性氧 (reactive oxygen species) 生成，从而发挥其抗侵袭作用。

NG 52 (NG-52) 是可逆和 ATP 相容性且具有口服活性的Cdc28p 和Pho85p 激酶抑制剂，IC50分别为 7 μM 和 2 μM。它还抑制磷酸甘油酸激酶 1 的活性，IC50值为 2.5 μM。

Germacrone 提取自莪术，具有抗炎、抗雄激素和抗病毒活性。 它还通过促进细胞凋亡来抑制胶质瘤细胞的增殖。

Adenosine 5’-methylenediphosphate is an inhibitor of ecto-5’-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5’-monophosphate , adenosine 5’-diphosphate , or adenosine 5’-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5’-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) cells in a migration assay.2,3It increases tumor infiltration of CD3+CD8+T cells and reduces tumor growth in a K1735 murine melanoma model when administered at a dose of 400 μg/mouse.4 1.Bruns, R.F.Adenosine receptor activation by adenine nucleotides requires conversion of the nucleotides to adenosineNaunyn Schmiedebergs Arch. Pharmacol.315(1)5-13(1980) 2.Braganhol, E., Tamajusuku, A.S.K., Bernardi, A., et al.Ecto-5′-nucleotidase/CD73 inhibition by quercetin in the human U138MG glioma cell lineBiochim. Biophys. Acta1770(9)1352-1359(2007) 3.Shali, S., Yu, J., Zhang, X., et al.Ecto\5′\nucleotidase (CD73) is a potential target of hepatocellular carcinomaJ. Cell Physiol.234(7)10248-10259(2018) 4.Forte, G., Sorrentino, R., Montinaro, A., et al.Inhibition of CD73 improves B cell-mediated anti-tumor immunity in a mouse model of melanomaJ. Immunol.189(5)2226-2233(2021)

CP681301 是CDK5的有效抑制剂，具有抗增殖活性。CP681301 在果蝇中表现出抗肿瘤活性。CP681301 降低神经胶质瘤干细胞中 CD133、OLIG2、SOX2、KI67、pCDK5 蛋白水平的表达。CP681301 减少小鼠胶质瘤异种移植物的自我更新。

KCN1, a novel synthetic sulfonamide, is a HIF pathway inhibitor with potential anticancer activity in vitro and in vivo anti-pancreatic cancer activities and preclinical pharmacology. KCN1 specifically inhibited HIF reporter gene activity in several glioma cell lines at the nanomolar level. KCN1 also downregulated transcription of endogenous HIF-1 target genes, such as VEGF, Glut-1, and carbonic anhydrase 9, in a hypoxia-responsive element (HRE)-dependent manner. KCN1 potently inhibited the growth of subcutaneous malignant glioma tumor xenografts with minimal adverse effects on the host.

Norswertianin，一种氧杂蒽酮类化合物，有效抗神经胶质瘤化合物(anti-glioma compound)。通过氧化应激和Akt/mTOR依赖自噬，诱导GBM细胞分化。

Chol-CTPP是针对血脑屏障(BBB)与胶质瘤(glioma)细胞展现双重靶向性的配体，可以与Chol-TPP合成为Lip-CTPP。Lip-CTPP作为一种潜在载体，可用于联合阿霉素(DOX)和氯胺达明(LND)发挥抗胶质瘤(anti-glioma)效果。此载体能够增强对肿瘤细胞的增殖、迁移及侵袭抑制，同时促进细胞凋亡(apoptosis)与坏死(necrosis)，并干扰线粒体功能。

NEO214, an autophagy inhibitor and a covalent conjugate of the PDE4 inhibitor Rolipram and perillyl alcohol, exhibits anti-cancer activity and blood-brain barrier (BBB) permeability. It prevents autophagy-lysosome fusion, blocking autophagic flux and triggering glioma cell death via mTOR activation and TFEB (Transcription Factor EB) aggregation. NEO214 inhibition of Macroautophagy/autophagy in glioblastoma cells may overcome chemotherapy resistance in glioblastoma [1].

Mitraphylline 是一种绒毛钩藤中主要的五环吲哚类生物碱，可阻碍脂多糖介导的原代人中性粒细胞活化。