The search for new antifungal agents was essential because of opportunistic infections in immunocompromised individuals and the development of resistance to currently used agents. Bryophytes offer a rich source of rare and structurally unique molecules and can serve as a reserve of potentially antifungal compounds for further development as pharmaceuticals. This minireview covered the chemical and biological research of Chinese bryophytes recently finished in our laboratory. Totally about 120 compounds have been isolated and identified from 17 bryophyte species collected from North to South of China. The antifungal effect of these isolated compounds and their reversal of resistance of Candida albicans to fluconazole were evaluated. The possible reversal mechanisms were also preliminarily tested.