It has been shown by the results-of HPLC analysis in combination with spectrographicdeterminations that PsD-007 is composed of 7 different porphyrins,In order of the proportion inPsD-007,they are:3 （or 8）-（l-methox...It has been shown by the results-of HPLC analysis in combination with spectrographicdeterminations that PsD-007 is composed of 7 different porphyrins,In order of the proportion inPsD-007,they are:3 （or 8）-（l-methoxyethyl）-8 （or 3）-（l-hydroxyethyl）-deuteroporphyrin Ⅸ（MHD）;3,8-di-（l-methoxyethyl）-deuteroporphyrin Ⅸ（DMD）;3（or 8）-（l-methoxyethyl）-8 （or3）-vinyl-deuteroporphyrin Ⅸ（MVD）;3（or 8）-（l-hydroxyethyl）-8（or 3）-vinyl-deuteroporphyrin Ⅸ（HVD）;hernatoporphyrin Ⅸ （Hp）;protoporphyrin Ⅸ （Pp） and 3（or 8）-（O-aceylethyl）-8（or 3）-（l-hydroxyethyl）-deuteroporphrin Ⅸ （AHD）,which presented only in crude PsD-007 and hasbeen transformed into MHD and Hp,respectively during the separation and preparing the clinicalpreparation of PsD-007.Structures of these porphyrins were further eonfirmed by the corre-sponding anthentic samples obtained by synthetic method.It was found on the basis of the experi-mental data of photosensitizing ability in cell-free systems and photoinactivation of human cancercells in vitro as well as efficacy of photodynamic therapy for sarcoma.S<sub>180</sub> in mice of the ma-jor components MILD,DMD and MVD composed of which more over 85% of the totalamount of PsD-007,that they all exhibited comparatively high photosensitizing ability andphotodynamic effects on cancer cells and tram-planted animal tumor.展开更多
Photocarcinorin was prepared in our Lab and its composition was differentfrom that of any other hematoporphyrin photosensitizers by TLC and HPLC analyses.The 95% fiducial limits of iv LD in mice were 176-236 mg·k...Photocarcinorin was prepared in our Lab and its composition was differentfrom that of any other hematoporphyrin photosensitizers by TLC and HPLC analyses.The 95% fiducial limits of iv LD in mice were 176-236 mg·kg<sup>-1</sup>.The iv MLD indogs was 171 mg·kg<sup>-1</sup>.The acute and subacutc toxic tests in 37 dogs showed that theintoxicated manifestations were characterized by a complex syndrome always seen inporphyrias.The biological,laboratory and histopathologic findings revealed that theliver,kidney and erythroeytic series were the target organs.The damages were dose-related and reversible within 2 wk.he phototoxicity was determined in mice with UV ra-diation and compared with that of HpD.The extent of its phototoxic reactions waslower than that of HpD’s.展开更多
Here is presented a brief review of studies on the home-made photolocalizing andphotochemotherapeutic agent as well as radiosensitizer for human malignancies called photocarcinorin(PsD-007).Experimental data and princ...Here is presented a brief review of studies on the home-made photolocalizing andphotochemotherapeutic agent as well as radiosensitizer for human malignancies called photocarcinorin(PsD-007).Experimental data and principal research conclusions of chemistry,pharmacodynamics,preclinical pharmacology and toxicology as well as phase-Ⅰ-Ⅱ clinical trials are summarized.展开更多
文摘It has been shown by the results-of HPLC analysis in combination with spectrographicdeterminations that PsD-007 is composed of 7 different porphyrins,In order of the proportion inPsD-007,they are:3 （or 8）-（l-methoxyethyl）-8 （or 3）-（l-hydroxyethyl）-deuteroporphyrin Ⅸ（MHD）;3,8-di-（l-methoxyethyl）-deuteroporphyrin Ⅸ（DMD）;3（or 8）-（l-methoxyethyl）-8 （or3）-vinyl-deuteroporphyrin Ⅸ（MVD）;3（or 8）-（l-hydroxyethyl）-8（or 3）-vinyl-deuteroporphyrin Ⅸ（HVD）;hernatoporphyrin Ⅸ （Hp）;protoporphyrin Ⅸ （Pp） and 3（or 8）-（O-aceylethyl）-8（or 3）-（l-hydroxyethyl）-deuteroporphrin Ⅸ （AHD）,which presented only in crude PsD-007 and hasbeen transformed into MHD and Hp,respectively during the separation and preparing the clinicalpreparation of PsD-007.Structures of these porphyrins were further eonfirmed by the corre-sponding anthentic samples obtained by synthetic method.It was found on the basis of the experi-mental data of photosensitizing ability in cell-free systems and photoinactivation of human cancercells in vitro as well as efficacy of photodynamic therapy for sarcoma.S<sub>180</sub> in mice of the ma-jor components MILD,DMD and MVD composed of which more over 85% of the totalamount of PsD-007,that they all exhibited comparatively high photosensitizing ability andphotodynamic effects on cancer cells and tram-planted animal tumor.
文摘Photocarcinorin was prepared in our Lab and its composition was differentfrom that of any other hematoporphyrin photosensitizers by TLC and HPLC analyses.The 95% fiducial limits of iv LD in mice were 176-236 mg·kg<sup>-1</sup>.The iv MLD indogs was 171 mg·kg<sup>-1</sup>.The acute and subacutc toxic tests in 37 dogs showed that theintoxicated manifestations were characterized by a complex syndrome always seen inporphyrias.The biological,laboratory and histopathologic findings revealed that theliver,kidney and erythroeytic series were the target organs.The damages were dose-related and reversible within 2 wk.he phototoxicity was determined in mice with UV ra-diation and compared with that of HpD.The extent of its phototoxic reactions waslower than that of HpD’s.
文摘Here is presented a brief review of studies on the home-made photolocalizing andphotochemotherapeutic agent as well as radiosensitizer for human malignancies called photocarcinorin(PsD-007).Experimental data and principal research conclusions of chemistry,pharmacodynamics,preclinical pharmacology and toxicology as well as phase-Ⅰ-Ⅱ clinical trials are summarized.
