The present invention discloses mono- or poly-substituted oil-water amphiphilic hypocrellin derivatives and methods for their preparation and use. The oil-water amphipathic hypocrellin derivative containing substitution of groups such as polyglycol and quaternary ammonium salt prepared in the present invention has a clear red shift of the absorption spectrum and a significant molar absorption coefficient compared to the hypocrellin matrix. Under the photosensitization conditions, reactive oxygen species such as singlet oxygen are efficiently generated, and their hydrophilicity and hydrophobicity are adjusted to impart different oil-water amphipathicity to the derivative, as well as cells or tissues. Such an oil-in-water amphiphilic hypocrellin derivative can improve the biocompatibility with the drug, solve the contradiction of the hydrophilicity and lipophilicity of the drug required for various drug administration methods, meeting the requirements of various clinical drugs. Under the same conditions, the oil-water amphipathic hypocrellin derivative photosensitizer according to the present invention is more photodynamically directed to tumor cells than the first and second generation commercial photosensitizers. It has the ability to activate.本発明は一置換又は多置換の油水両親媒性ヒポクレリン誘導体及びその製造方法と使用を開示する。本発明で製造されたポリグリコール、第四級アンモニウム塩等の基の置換を含む油水両親媒性ヒポクレリン誘導体は、ヒポクレリン母体に比べて、吸収スペクトルが明らかにレッドシフトし且つモル吸光係数が大幅に高まり、光増感条件下で一重項酸素等の反応性酸素種を効率よく発生させ、その親水性及び疎水性を調整して、該誘導体に異なる油水両親媒性を付与するとともに、細胞又は組織との生体適合性を高めることができ、このような油水両親媒性ヒポクレリン誘導体は、さまざまな臨床薬の要件を満たし、各種薬物投与方式に求められる薬物の親水性と親油性の矛盾を解決し、同じ条件では、本発明に係る油水両親媒性ヒポクレリン誘導体光増感剤は、第１世代及び第２世代の市販光増感剤よりも高い腫瘍細胞に対する光線力学的不活性化能力を有する。
