Diabetes mellitus (DM) is commonly known as Xiaokezheng ([Chinese characters: see text]) with respect to the sign of imbalance of yin, yang and qi in the traditional Chinese medical system. This review is mainly focused on peer-reviewed international journals in chemistry, pharmacological and clinical research of Chinese medicines (CM) used in therapeutic treatments of DM and its complications. This article will also discuss the advantages and future perspectives of anti-diabetic CM.