An aza-tryptanthrin derivative represented by Formula, or a geometric isomer, a tautomer, an isotopic label, a hydrate, a solvate or a pharmaceutically acceptable salt thereof: wherein: one of A and B is N and the other is C-R 3; E is N or -C-R 6; Y is -O-, and Z is hydrogen, an unsubstituted or substituted C1-C4 alkyl group, an unsubstituted or substituted C2-C4 alkenyl group, an unsubstituted or substituted C2-C4 alkynyl group, a carboxymethyl group -CH 2 C(=O)OH, a sulfonyl group -S(=O) 2 OH, or a phosphoryl group -P(=O) 2; and alternatively, Y is -N -, and Z is hydrogen, -C(=S)-N(R 8)(R 9), -C(=O)-N(R 8)(R 9), or -C(=N)-N(R 8)(R 9); R 1 to R 5 and R 7 are hydrogen; R 6 is hydrogen, an unsubstituted or substituted C1-C4 alkyl group, an unsubstituted or substituted C1-C4 alkoxy group, halogen, a nitro group, a cyano group, a methylsulfonyl group or a hydroxyl group; and when B is N, Z is hydrogen and Y is -O-, R 6 is not hydrogen; R 8 and R 9 are each independently selected from hydrogen or an unsubstituted C1-C4 alkyl group; each substituted C1-C4 alkyl group is substituted by one of the following groups: halogen, a hydroxyl group, an amino group, or -N(R 10)(R 11), wherein R 10 and R 11 are each independently selected from hydrogen or an unsubstituted C1-C4 alkyl group; each substituted C1-C4 alkoxy group is substituted by one of the following groups: halogen, a hydroxyl group, an amino group, or -N(R 10)(R 11), wherein R 10 and R 11 are each independently selected from hydrogen or an unsubstituted C1-C4 alkyl group; each substituted C2-C4 alkenyl group is substituted by one of the following groups: halogen or a hydroxyl group; and each substituted C2-C4 alkynyl group is substituted by one of the following groups: halogen or a hydroxyl group. one of A and B is N and the other is C-R 3; E is N or -C-R 6; Y is -O-, and Z is hydrogen, an unsubstituted or substituted C1-C4 alkyl group, an unsubstituted or substituted C2-C4 alkenyl group, an unsubstituted or substituted C2-C4 alkynyl group, a carboxymethyl group -CH 2 C(=O)OH, a sulfonyl group -S(=O) 2 OH, or a phosphoryl group -P(=O) 2; and alternatively, Y is -N -, and Z is hydrogen, -C(=S)-N(R 8)(R 9), -C(=O)-N(R 8)(R 9), or -C(=N)-N(R 8)(R 9); R 1 to R 5 and R 7 are hydrogen; R 6 is hydrogen, an unsubstituted or substituted C1-C4 alkyl group, an unsubstituted or substituted C1-C4 alkoxy group, halogen, a nitro group, a cyano group, a methylsulfonyl group or a hydroxyl group; and when B is N, Z is hydrogen and Y is -O-, R 6 is not hydrogen; R 8 and R 9 are each independently selected from hydrogen or an unsubstituted C1-C4 alkyl group; each substituted C1-C4 alkyl group is substituted by one of the following groups: halogen, a hydroxyl group, an amino group, or -N(R 10)(R 11), wherein R 10 and R 11 are each independently selected from hydrogen or an unsubstituted C1-C4 alkyl group; each substituted C1-C4 alkoxy group is substituted by one of the following groups: halogen, a hydroxyl group, an amino group, or -N(R 10)(R 11), wherein R 10 and R 11 are each independently selected from hydrogen or an unsubstituted C1-C4 alkyl group; each substituted C2-C4 alkenyl group is substituted by one of the following groups: halogen or a hydroxyl group; and each substituted C2-C4 alkynyl group is substituted by one of the following groups: halogen or a hydroxyl group.