Demethoxydeacetoxypseudolaric acid B analog 是由 Pseudolaric acid B 半合成得到,能够有效抑制 HMEC-1、HL-60、A-549、MB-MDA-468、BEL-7402、HCT116、Hela 细胞,且 IC50值范围为 0.136-1.162 μM。
Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated oncogene 1 (Gli1) and cytosolic MMP-9, pERK1, and pERK2 proteins in a dose-dependent manner. Cyclopamine-KAAD also increases TRAIL-mediated cell death in NCH82 and NCH89 human glioblastoma cultures and upregulates expression of the death receptors DR4 and DR5 in LN229 and U251 glioma cells.
CAY10773 is a derivative of the ferroptosis inducer sorafenib .1It selectively inhibits proliferation of BEL-7402, MGC803, and T24 bladder cancer cells (IC50s = 5.77, 5.21 and 3.97 μM, respectively) over non-cancerous HCV-29 cells (IC50= 23.19 μM). CAY10773 induces apoptosis in T24 cells when used at concentrations ranging from 2 to 6 μM but induces ferroptosis at concentrations greater than or equal to 6 μM with 10 hour or longer incubation times. It increases the production of reactive oxygen species (ROS) and decreases the mitochondrial membrane potential in T24 cells. CAY10773 (≥6 μM) also induces autophagy with incubation times longer than eight hours. 1.Chen, J.-N., Li, T., Cheng, L., et al.Synthesis and in vitro anti-bladder cancer activity evaluation of quinazolinyl-arylurea derivativesEur. J. Med. Chem.205112661(2020)
Ursonic acid methyl ester, an esterified derivative of Ursolic acid, exhibits growth inhibitory activity against four tumor cell lines: HL-60, BGC, Bel-7402, and Hela, and the ED50 values for inhibition are >100 μg ml.
Flemiphilippin A has antioxidant activity, it shows DPPH radical scavenging activity with effective half maximal concentration (EC50) of 18.36 ug mL. Flemiphilippinin A (5 ug mL) exhibits some level of antitumor activity against human hepatocellular carci
Aphagranin A exhibits strong antiproliferative activity against the growth of six lines of human cancer cells (MCF-7, A549, HepG2, Bel-7402, SGC-7901, and BGC-823.
Chlorovaltrate K shows moderate cytotoxicity against lung adenocarcinoma (A 549), metastatic prostate cancer (PC-3M), colon cancer (HCT-8) and hepatoma (Bel7402) cell lines with IC50 values of 0.89-9.76 uM.
Marginatoxin may be a promising chemopreventive agent for treating hepatocellular carcinoma, it induces human hepatoma BEL-7402 cells apoptosis in vitro and in vivo via activation of Fas FasL-mediated apoptotic pathway.