Abstract. Realgar (As 4 S 4 ) has been used in traditional Chinese medicines for treatment of malignancies. However, the poor water solubility of realgar limits its clinical application. To overcome this problem, realgar quantum dots (RQDs; 5.48±1.09 nm) were prepared by a photoluminescence method. The mean particle size was characterized by high-resolution transmission electron microscopy and scanning electron microscopy. Our recent studies revealed that the RQDs were effective against tumor growth in tumor-bearing mice without producing apparent toxicity. The present study investigated their anticancer effects and mechanisms in human hepatocellular carcinoma (HepG2) cells. The HepG2 cells and human normal liver (L02) cells were used to determine the cytotoxicity of RQDs. The portion of apoptotic and dead cells were measured by flow cytometry with Annexin V-fluorescein isothiocyanate/propidium iodide double staining. Apoptosis-related proteins and genes were examined by western blot analysis and reverse transcription-quantitative polymerase chain reaction, and the mitochondrial membrane potential was assayed by confocal microscope with JC-1 as a probe. RQDs exhibited cytotoxicity in a concentration-dependent manner and HepG2 cells were more sensitive compared with normal L02 cells. At 15 µg/ml, 20% of the cells were apoptotic, while 60% of the cells were necrotic at 30 µg/ml. The anti-apoptosis protein Bcl-2 was dose-dependently decreased, while pro-apoptotic protein Bax was increased. There was a loss of mitochondrial membrane potential and expression of the stress genes C/EBP-homologous protein 10 and glucose-regulated protein 78 was increased by RQDs. RQDs were effective in the inhibition of HepG2 cell proliferation and this effect was due to induction of apoptosis and necrosis through endoplasmic reticulum stress. IntroductionThe use of arsenic in China can be traced back thousands of years. Arsenic and arsenic salts, including orpiment, realgar and arsenolite, were fundamental ingredients in certain cancer treatments (1). The Fowler's solution (1% potassium arsenite) was used in the treatment of malignant diseases, such as leukemia and Hodgkin's disease, by numerous physicians in the 19-20th centuries (1). Arsenic trioxide (As 2 O 3 ) has emerged as the first-line therapy in the treatment of acute promyelocytic leukemia (APL); however, the toxicity hinders its clinical applications (2,3).Realgar contains >90% arsenic sulfide and is widely used externally and internally in a number of traditional medicine recipes in China (4). For example, realgar in combination with Indigo naturalis and Salvia miltiorrhiza is effective against APL (5), and targets RING-type E3 ligase c-CBL to induce degradation of BCR-Abl in chronic myelogenous leukemia (6). Realgar also enhances the antitumor effects of imatinib (7). Results from multicenter clinical trials using oral realgar formulations plus intravenous As 2 O 3 against hematological malignancy are promising (8).However, realgar is insoluble in water, resulting in poor ...
Thieno[2,3‐d]pyrimidinones were reported to act as potent anticancer agents; in this work, a series of new substituted thieno[2,3‐d]pyrimidinone (6) were synthesized via the aza‐Wittig reaction in satisfactory yields. The structures of these compounds were confirmed by elemental analysis, IR, 1H‐NMR, and mass spectral data, and compound 6h was further analyzed by single crystal X‐ray diffraction. Cytotoxic effect of all the compounds was carried out on human breast and lung cancer cell lines (MCF‐7 and SPC‐A‐1, A459). Compound 6f exhibited the best inhibition activities against A459 with IC50 4.1 μM.
Efficient Synthesis of New Thieno[2,3-d]pyrimidin-4(3H)-one Derivatives for Evaluation as Anticancer Agents. -Some of the new compounds (IV) show good cytotoxicity against human breast and lung cancer cell lines, with compound (IVf) possessing the best inhibitory activity against lung cancer cell line (A459). -(HU*, Y.-G.; ZHENG, A.-H.; LI, G.-J.; DONG, M.-Z.; YE, F.; SUN, F.; LIU, Z.-Y.; LI, W.; J. Heterocycl. Chem. 51 (2014) S1, E84-E88, http://dx.
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