Swertia plants have been considered to be medicinal plants useful for the treatment of various ailments for thousands of years, especially in Asian countries. This is due to the broad variety of chemical compounds that provide multiple ligands for bonding to different endogenous biomacromolecules for patients. Chemical constituents and pharmacological activities of Swertia plants are summarized in this paper. Approximately 419 metabolites and 40 bioactive compounds have been reported from 30 Swertia species, including xanthones, flavonoids, seco-iridiods, iridiods, triterpenoids, alkaloids, volatiles, and other secondary metabolites. The bioactivities of Swertia plants include anticarcinogenic, hepatoprotective, anti-oxidant, hypoglycemic, anthelmintic, antibacterial, antifungal, anti-diabetic, gut, and airways modulatory, metabolizing isozymes inhibitory, neuroprotective, HIV-I reverse transcriptases inhibitory, anticholinergic, and CNS-depressant activities, etc. In addition, biosynthetic pathways of xanthones, and seco-iridiods, two most important secondary metabolites for Swertia, are elucidated. The xanthones biosynthetic pathway is a mixed biosynthetic pathway involved the shikimate and the malonate routes, and the seco-iridoid pathway starts with geraniol derived from IPP which is produced either via the MEP or the MVA pathway. This review will offer a reference for future researches on the protection of natural resources, the investigation of therapeutic basis, new drug development, and so forth. Metabolic pathways of some crucial active compounds were also discussed in this review.