This paper reviewed updated research progresses of caffeoylquinic acids both in phytochemical and pharmacological aspects. The resources, distribution as well as the chemical structures of monocaffeoylquinic acids, dicaffeoylquinic acids, tricaffeoylquinic acids and multicaffeoylquinic acids are conclusively analyzed. The reviewed pharmacological investigations indicated that the caffeoylquinic acids exhibited significant activities such as anti-oxidation, anti-inflammation, enzyme inhibition, hypatoprotective and anti-PAF effects. The broad distribution and the remarkably pharmacological activities of these natural phenolic acids indicated their potential in the discovery and development of new natural drugs.