A monosubstituted or polysubstituted amphiphilic hypocrellin derivative, being represented by general structural formula (IV-a) or (V-a): in formula (IV-a), substituent R is represented by general structural formula: in formula, 0≤m≤12, 0≤n≤500, 0≤p≤12, 0≤q≤12 and 0≤r≤1; the m, n, p, q and r are zero or positive integers; Y is O, S, a carboxylate, an amide, a sulfonate, or a cycloalkane containing 3-12 carbon atoms, optionally substituted with an alkyl containing 1-12 carbon atoms; in formula, the terminal group Z is hydrogen, an alkyl containing 1-12 carbon atoms, an alkoxy containing 1-12 carbon atoms, a phenyl, a heterocycle, a hydroxy, a sulfhydryl, a carboxy, a sulfo or a pyridine salt; in formula, when the terminal group Z is a pyridine salt, the substituent on the pyridine ring of the pyridine salt is at an ortho-position, a meta-position or a para-position; the pyridine salt is prepared by quaternization of pyridine and a halogenated hydrocarbon containing 1-12 carbon atoms of different chain lengths; and the anion of the pyridine salt is an acceptable anion in pharmaceutical preparations; in formula, three substituents R 12, R 13 and R 14 of a quaternary ammonium salt are independently or completely: an alkyl containing 1-12 carbon atoms, an alkenyl containing 2-12 carbon atoms, an alkynyl containing 2-12 carbon atoms, a cycloalkyl containing 3-8 carbon atoms, a cycloalkenyl containing 3-8 carbon atoms, an aryl or an aralkyl containing 6-12 carbon atoms; or an alkyl with a terminal group containing a hydroxy, a carboxy, a sulfo or a carboxylate; or an alkyl, alkenyl, alkynyl, cycloalkyl, aryl or aralkyl having a chain containing a heteroatom of oxygen, nitrogen or sulfur atom and 1-12 carbon atoms; or different combinations of the above substituents and the anion X - of the quaternary ammonium salt is an acceptable anion in pharmaceutical preparations; in formula (V-a), R 6 -R 11 are partially identical, or completely identical, or completely different, and are -H; -CH 3; -C 2 H 5; -C 3 H 7; -C 4 H 9; -C 5 H 11; or -C 6 H 13. in formula (IV-a), substituent R is represented by general structural formula: in formula, 0≤m≤12, 0≤n≤500, 0≤p≤12, 0≤q≤12 and 0≤r≤1; the m, n, p, q and r are zero or positive integers; Y is O, S, a carboxylate, an amide, a sulfonate, or a cycloalkane containing 3-12 carbon atoms, optionally substituted with an alkyl containing 1-12 carbon atoms; in formula, the terminal group Z is hydrogen, an alkyl containing 1-12 carbon atoms, an alkoxy containing 1-12 carbon atoms, a phenyl, a heterocycle, a hydroxy, a sulfhydryl, a carboxy, a sulfo or a pyridine salt; in formula, when the terminal group Z is a pyridine salt, the substituent on the pyridine ring of the pyridine salt is at an ortho-position, a meta-position or a para-position; the pyridine salt is prepared by quaternization of pyridine and a halogenated hydrocarbon containing 1-12 carbon atoms of different chain lengths; and the anion of the pyridine salt is an acceptable anion in pharmaceutical preparations; in formula, three substituents R 12, R 13 and R 14 of a quaternary ammonium salt are independently or completely: an alkyl containing 1-12 carbon atoms, an alkenyl containing 2-12 carbon atoms, an alkynyl containing 2-12 carbon atoms, a cycloalkyl containing 3-8 carbon atoms, a cycloalkenyl containing 3-8 carbon atoms, an aryl or an aralkyl containing 6-12 carbon atoms; or an alkyl with a terminal group containing a hydroxy, a carboxy, a sulfo or a carboxylate; or an alkyl, alkenyl, alkynyl, cycloalkyl, aryl or aralkyl having a chain containing a heteroatom of oxygen, nitrogen or sulfur atom and 1-12 carbon atoms; or different combinations of the above substituents and the anion X - of the quaternary ammonium salt is an acceptable anion in pharmaceutical preparations; in formula (V-a), R 6 -R 11 are partially identical, or completely identical, or completely different, and are -H; -CH 3; -C 2 H 5; -C 3 H 7; -C 4 H 9; -C 5 H 11; or -C 6 H 13.