YQ36: A Novel Bisindolylmaleimide Analogue Induces KB/VCR Cell Death

Overexpression of multidrug resistance proteins P-glycoprotein (P-gp, MDR1) causes resistance of the tumor cells against a variety of chemotherapeutic agents. 3-(1-methyl-1H-indol-3-yl)-1-phenyl-4-(1-(3-(piperidin-1-yl)propyl)-1H-pyrazolo[3,4-b]pyridine-3-yl)-1H-pyrrole-2,5-dione (YQ36) is a novel analogue of bisindolylmaleimide, which has been reported to overcome multidrug resistance. Here, we dedicated to investigate the anticancer activity of YQ36 on KB/VCR cells. The results revealed that YQ36 exhibited great antiproliferative activity on three parental cell lines and MDR1 overexpressed cell lines. Moreover, the hypersensitivity of YQ36 was confirmed on the base of great apoptosis induction and unaltered intracellular drug accumulation in KB/VCR cells. Further results suggested that YQ36 could not be considered as a substrate of P-gp, which contributed to its successfully escaping from the efflux mediated by P-gp. Interestingly, we observed that YQ36 could accumulate in nucleus and induce DNA damage. YQ36 could also induce the activation of caspase-3, imposing effects on the mitochondrial function. Collectively, our data demonstrated that YQ36 exhibited potent activities against MDR cells, inducing DNA damage and triggering subsequent apoptosis via mitochondrial pathway

Effects of Different Irrigation Methods on Growth, Fruit Quality and Yield of Apple Trees

Water-saving irrigation is an important way to realize the sustainable development of the apple industry. In order to screen the best irrigation pattern for apple, taking 9-year-old ‘Yanfu 10’ Fuji / Malus robusta apple as the material, the effects of different irrigation methods (drip irrigation, sprinkling irrigation, and flood irrigation) on the growth, fruit quality, and yield of apple trees were studied. The results showed that compared with the flood irrigation, drip irrigation and sprinkling irrigation significantly increased the spring shoot length by 14.8% and 9.1%, respectively, and decreased the autumn shoot length by 11.7% and 8.8%, respectively. Drip irrigation and sprinkling irrigation significantly increased the leaf area, chlorophyll content, and leaf weight, the leaf area increased by 3.0% and 1.9%, respectively, the chlorophyll content increased by 13.9% and 11.5%, respectively, and the leaf weight increased by 5.8% and 5.1%, respectively. Drip irrigation and sprinkling irrigation could slightly increase the single fruit weight and fruit shape index, significantly increase the coloring index and smoothness index. The single fruit weight increased by 3.2% and 1.9%, the coloring index increased by 6.1% and 4.1%, the smoothness index increased by 4.7% and 2.8%, and the proportion of red fruit increased by 4.2% and 2.2%, respectively. The content of soluble solids in drip irrigation and sprinkling irrigation was significantly higher than that in flood irrigation, which was 13.0% and 2.6% higher than CK, respectively. The fruit hardness in drip irrigation and sprinkling irrigation was 7.9% and 2.2% higher than CK, respectively, and that in drip irrigation increased significantly. The yield in drip irrigation and sprinkling irrigation was 12.1% and 8.2% higher than CK, respectively. In conclusion, drip irrigation and sprinkling irrigation could promote the growth of apple trees, improve the fruit quality, and increase the yield of apple trees, and the effect of drip irrigation is better than sprinkling irrigation