Spinosin,　a　flavone　C-glycoside　commonly　found　in　the　Fabaceae　family　and　other　flowering　plants,　has　gained　increasing　attention　for　its　diverse　bioactivities　and　therapeutic　potential.　Spinosin　biosynthesis　likely　follows　the　shikimic　acid　pathway,　involving　key　enzymes　such　as　phenylalanine　ammonia-lyase,　cinnamate　4-hydroxylase　(C4H),　4-coumarate-CoA　ligase　(4CL),　and　chalcone　synthase.　The　primary　source　of　spinosin　is　Ziziphus　jujuba　Mill.　var.　spinosa,　chief　traditional　Chinese　medicine　recognized　for　its　sedative　and　hypnotic　properties,　with　increasing　evidence　supporting　its　role　in　treating　neurological　disorders.　Recent　studies　reveal　spinosin’s　potential　as　an　Alzheimer’s　disease　drug　alongside　its　anti-inflammatory,　hypoglycemic,　cardioprotective,　pigmentation,　and　anti-liver　fibrosis　effects.　In　vitro　bioassays　have　highlighted　its　pharmacological　properties,　with　less　evidence　from　in　vivo　research,　focusing　on　its　effects　on　insulin　resistance,　sedation,　cognitive　improvement,　and　anti-cancer　activity.　This　review　provides　a　comprehensive　exploration　of　spinosin　in　the　context　of　its　plant　sources,　biosynthesis,　pharmacokinetics,　bioactivity,　toxicity,　and　safety.　Such　a　compilation　of　literature　identifies　future　prospects　for　the　medicinal,　agricultural,　and　biotechnological　applications　of　spinosin　to　aid　in　maximizing　its　broader　therapeutic　effects.　©　The　Author(s)　2025.