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。

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。

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。

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。