MicroRNAs, small non-coding RNA molecules, have gained a reputation of the most substantial regulators in gene network with the ability to down-regulate their targets. Accumulating evidence shifted insight toward microRNAs regulation as the key element of cancer initiation, development, and aggression. Recent studies have attached the importance of traditional Chinese medicine (TCM) to the treatment of various cancers, and the functional natural compounds have been considered as novel anticancer agents to directly inhibit tumor progression. In more recent decades, a wide range of biologically active components of TCM has gained increasing attention to their applications in the modulation of microRNAs. This review is on the purpose of demonstrating the significance of TCM bioactive ingredients in microRNAs regulation for cancer treatment according to the reports mainly in the recent six years, providing the evidence of efficient Chinese herbal medicine-based therapy and effective pro-diagnosis focusing on microRNAs expression of cancer patients.