The　Wnt　signaling　is　one　of　the　major　pathways　known　to　regulate　embryonic　development,　tissue　renewal　and　regeneration　in　multicellular　organisms.　Dysregulations　of　the　pathway　are　a　common　cause　of　several　types　of　cancer　and　other　diseases,　such　as　osteoporosis　and　rheumatoid　arthritis.　This　makes　Wnt　signaling　an　important　therapeutic　target.　Small　molecule　activators　and　inhibitors　of　signaling　pathways　are　important　biomedical　tools　which　allow　one　to　harness　signaling　processes　in　the　organism　for　therapeutic　purposes　in　affordable　and　specific　ways.　Natural　products　are　a　well　known　source　of　biologically　active　small　molecules　with　therapeutic　potential.　In　this　article,　we　provide　an　up-to-date　overview　of　existing　small　molecule　modulators　of　the　Wnt　pathway　derived　from　natural　products.　In　the　first　part　of　the　review,　we　focus　on　Wnt　pathway　activators,　which　can　be　used　for　regenerative　therapy　in　various　tissues　such　as　skin,　bone,　cartilage　and　the　nervous　system.　The　second　part　describes　inhibitors　of　the　pathway,　which　are　desired　agents　for　targeted　therapies　against　different　cancers.　In　each　part,　we　pay　specific　attention　to　the　mechanisms　of　action　of　the　natural　products,　to　the　models　on　which　they　were　investigated,　and　to　the　potential　of　different　taxa　to　yield　bioactive　molecules　capable　of　regulating　the　Wnt　signaling.