当前位置： SCI文献检索 > PHOTOCHEMISTRY AND PHOTOBIOLOGY期刊下所有文献 > Structure-activity and mechanism studies on silicon phthalocyanines with Plasmodium falciparum in the dark and under red light.

Structure-activity and mechanism studies on silicon phthalocyanines with Plasmodium falciparum in the dark and under red light.

Abstract：

:Syntheses for the new photosensitizers HOSiPcOSi(CH3)2(CH2)3N(CH1)1 or 3(CH3)2, Pc 34 and Pc 25, have been developed and the order of activity of these photosensitizers and the previously reported photosensitizer Pc 4, HOSiPcOSi(CH3)2(CH2)3N(CH3)2, in the dark and with broad-band red light toward Plasmodium falciparum in red blood cell (RBC) suspensions has been studied. The order of activity has been found to be Pc 4 > Pc 34 > Pc 25. Thus, the activity of the photosensitizers under both sets of conditions is inversely proportional to the length of their terminal amino alkyl chains. The 50% inhibition dye concentration (IC50) in the dark for the parasites in RBC suspension with Pc 4 is 24 nM and the dye concentration and light fluence that yield > or = 3 log10 of parasite inactivation with Pc 4 are 2 microM and 3 J/cm2, respectively. The synthesis of DNA and proteins by the parasites in culture was strongly inhibited by Pc 4 in the dark while parasite lactate dehydrogenase (pLDH) activity was unaffected. With Pc 4 and light, DNA and protein synthesis of the parasites in culture was strongly inhibited, pLDH activity of the parasites was moderately inhibited and ribosome density of the parasite cells was reduced. Gel electrophoresis studies showed that synthesis of all parasite proteins was inhibited to a similar extent. These results suggest that Pc 4 both in the dark and with light inactivates the cells by disturbing their machinery for the synthesis of not just one but a whole series of proteins. It is concluded that Pc 4 and light may be able to serve as a practical sterilization combination not only for HIV and other viruses but also for malaria parasites in RBC concentrates, and that Pc 4 by itself may have potential as a chemotherapeutic agent toward malaria.

journal_name

Photochem Photobiol

journal_title

Photochemistry and photobiology

authors

Zhao XJ,Lustigman S,Li YS,Kenney ME,Ben-Hur E

doi

10.1111/j.1751-1097.1997.tb08656.x

subject

Has Abstract

pub_date

1997-08-01 00:00:00

pages

282-7

issue

eissn

0031-8655

issn

1751-1097

journal_volume

pub_type

杂志文章

在线工具

Structure-activity and mechanism studies on silicon phthalocyanines with Plasmodium falciparum in the dark and under red light.