Marine　bis-indole　alkaloids　comprise　a　large　and　increasingly　growing　class　of　secondary　metabolites,　and　continue　to　deliver　a　great　variety　of　structural　templates　for　diverse　biological　targets.　The　alkaloids　derived　from　marine　resources　play　a　crucial　role　in　medicinal　chemistry　and　as　chemical　agents.　In　particular,　bis-indole　alkaloid　caulerpin　which　has　been　isolated　from　marine　green　algae　Caulerpa　and　a　red　algae　Chondria　armata　at　various　places　around　the　world,　was　tested　for　several　therapeutic　potentials　such　as　anti-diabetic,　antinociceptive,　anti-inflammatory,　anti-tumor,　anti-larvicidal,　anti-herpes,　anti-tubercular,　anti-microbial　and　immunostimulating　activities　as　well　as　a　means　of　other　chemical　agents.Herein,　we　summarized　the　discovery　and　isolation　of　caulerpin,　and　its　potential　medicinal　and　chemical　applications　in　chronological　order　with　various　aspects.　Additionally,　synthesis　of　caulerpin　and　its　functional　analogues　have　also　been　reviewed.