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A multifunctional integrated microfluidic biochip device was engineered to estimate the activity-toxicity and composition principle of medicine in a cell model in vitro. This biochip could be used for disease cells and healthy cells in two modules of “Yin-Yang” on the same chip for detecting the medicine efficacy-toxicity simultaneously, as well as adjust different gradient ratios of concentration through the Christmas tree structure in both “Yin-Yang” modules autonomously for detecting the best compatibility of medicine in maximum efficacy and minimal toxicity. In the applicability experiment, the best concentration of three chemical compounds including dinatin, diosmetin and cisplatin, were detected using the biochip and traditional 96-cell plate. Biochip assays showed perfect positive correlation compared with the results of traditional 96-cell plate, in addition presented advantages as less detection time and much lower price than the traditional 96-cell plate, which indicated the biochip is both convenient and feasible. Thus, the novel microfluidic chip-based multifunctional integrated system congregated the virtues of high throughput, rapid, sensitive, specific, cost-effective, and similar to the physical environment of the human body, which was especially suitable for the medicine efficacy-toxicity and compatibility evaluation.