The invention discloses a gambogic acid cyclized analog, a preparation method and application thereof. The semi-synthesized gambogic acid cyclized analog is obtained by the extracted and purified gambogic acid through chemical synthesis and has a structural general formula I-III as the right formula, wherein substituent groups of A ring, B ring, C ring, R1, R2, R3, R4, R5, R6, R7, R7, R8, R9, R10, R11 or/and R12 contain glycosyl group, polyhydroxy, amino acid group, acyloxy group, phosphoric acid oxygen group, sulphonic acid oxygen group, alkoxyl group, aromatic oxygen group, heterocyclic oxygen group, mercapto group, substituted mercapto group, primary amine and secondary amines groups or/and substituted primary amine and secondary amines groups, and chain hydrocarbon or and cyclic group containing oxygen, sulphur, nitrogen, carbon or/and phosphor atoms, and one or combination of the substitution groups. The gambogic acid cyclized analog has anti-tumor, antivirus, antibacterial and antifungal pharmacology activities, can be used as anti-tumor, antivirus, immune, antibacterial and antifungal medicaments, and can be applied together with the known anti-tumor, antivirus, immune, antibacterial and antifungal medicaments.