In recent years, the over use of wide-spectrum antibiotics, long and repeated treatment have caused pathogenic fungi resistant to antifungal agents, especially to fungistatic drugs, and thereby more effective therapeutic drugs or alternative treatments are needed to alleviate the situation. Studies have demonstrated that filamentation plays a crucial role in the pathogenic process. The transition from yeast to hyphae could improve the virulence of C. albicans during the course of infection. Filaments generate strong top pressure for permeation into host body and have the advantage to escape from immune cells. In addition, hyphae serving as the skeleton of biofilms play a critical role for the Silicristin formation of highly heterogeneous architecture, which protects microorganisms from antibiotic treatment and also creates a source of persistent infection. Therefore, prevention of the hyphae formation could be an effective means to reduce the biofilm formation and virulence in the pathogenesis of C. albicans. As the earliest land plants, bryophytes grow in an unfavorable environment and inevitably produce secondary metabolites against different surviving stresses. Among those diverse suite of fungi interacts with bryophytes as pathogens, which exhibit different methods of host cell disruption such as invading the host cell by hyphae formation or causing host protoplast degeneration. Previous studies suggest these plants could biosynthesize some aurantiamide-acetate chemicals to control the plant diseases caused by fungi or bacteria. C. albicans, as a pathogenic fungal, switches from yeast morphotype to filaments and develop the formation of biofilm to colonize in the host. Based on the aforementioned property of bryophytes, we evaluated the antifungal activity of their extracts. Our lab previously reported that bisbibenzyls including plagiochin E and riccardin D derived from bryophytes displayed a moderate antifungal action. We presume bisbibenzyls are the active agents in bryophytes to combat fungal invasion. In our present study, 26 bisbibenzyls isolated from liverworts and chemical synthesizes were screened for antifungal activities. Among them three compounds showed a good effect in inhibiting the transition of yeast-to-hypha and biofilm formation. The effects of these compounds against biofilm formation were observed at or above their MICs. And they were the combination result of inhibitory growth and retarded the yeast to hyphal transition. Farnesol, a QSM, was found to regulate the morphogenesis switch and the inhibitory effect was positively correlated with farnesol formation as detected by HPLC-MS.