It review the structure-function relationship of natural anthraquinone derivatives from Radix et Rhizoma Rhei. The anthraquinone derivatives had many identical activities because they have the identical mother nucleus; but the strength of their activities were different, because they have different substitution groups. The anthraquinone derivatives shown the obvious structure-function relationship in many respects, such as antioxygenation, antibiosis, anticancer, the influence of immunity and so on.