Plants are considered rich attractive sources for producing new bioactive compounds which exhibit a wide range of pharmacological activities. Family Aizoaceae is considered to be one of the South Africa largest succulent plant families, and it consists of four subfamilies named Sesuvioideae, Aizooideae, Ruschioideae, and Mesembryanthemoideae. Genus Aptenia consists of four species such as Aptenia cordifolia, Aptenia geniculiflora, Aptenia haeckeliana, and Aptenia lancifolia. Along Aptenia species are rich sources of natural metabolites from diverse chemical classes including oxyneolignans, flavonoids, sterols, lignans, amides and alkaloids with powerful anti-inflammatory activity. This review covers the literature until December 2018, providing a complete survey of all compounds isolated from genus Aptenia with their corresponding biological activities whenever applicable.