ABSTRACT
Leukemia is a common malignant tumor in blood system, and it is one of the 10 high incidence malignant tumors in China. The main reason related to the failure of chemotherapy in leukemia is multidrug resistance (MDR). Chemical reversal agents often have the side effects and the mechanisms of chemical reversal agents are single, which restricts its clinical application. With efficiency, low-level toxicity, and multi-target points, Chinese materia medica shows its unique advantages in reversing MDR of leukemia. This paper summarizes the MDR mechanisms of leukemia and reversal agents in Chinese medicine in order to find more Chinese medicine to reverse leukemia.
ABSTRACT
10 kinds of annonaceous acetogenins were selected for antitumor activity testing against human lung cancer cell line A549/Taxol and the structure activity relationship was analyzed.MTT assay was used to detect the inhibitory activities of 10 kinds of annonaceous acetogenins and positive drugs against A549/Taxol cells, respectively uvariamicin-Ⅲ(1), uvariamicin-Ⅱ(2), annosquacin D(3), desacetyluvaricin(4), annosquatin A(5), squamostatin D(6), bullatacin(7), squamocin(8), motrilin(9), annosquatin B(10), verapamil and cisplatin. Annonaceous acetogenins showed significant inhibitory activities against A549/Taxol cells, and were more potent than the positive drug verapamil and cisplatin.The more carbon atoms between the tetrahydrofuran ring and the lactone ring of annonaceous acetogenins exhibited more potency.Besides,ACGs with two substituted hydroxyl showed more potency than the compounds with three substituted hydroxyl in the bis-adjacent-THF ACGs. Furthermore, ACGs with three substituted hydroxyl showed more potency than the compounds with four substituted hydroxyl among the no bis-adjacent-THF ACGs.