Synthesis of propargylic alcohols and biological effects on Echinococcus multilocularis metacestodes.
This study describes the synthesis of propargylic alcohols derived from isatin and their biochemical and morphological effects on Echinococcus multilocularis metacestodes in Meriones unguiculatus. Propargylic alcohols decreased the alkaline phosphatase and the lactate dehydrogenase activities of the metacestode selectively. The most effective compound, 1b, decreased the lactate dehydrogenase enzymatic activity, and the glucose concentration in the parasite increased, whereas the glycogen content was partially decreased. Furthermore, the ultrastructure study revealed several damages. The host-parasite relationships are very important in the intrahepatic cestodes as shown by the biochemical side effects observed in the host's liver during the treatment. An in vitro enzymatic study was performed with alcohols 1b and 1c.
Sarciron
M E
ME
Laboratoire de Parasitologie Comparée, Université des Sciences et Techniques du Languedoc, Montpellier, France.
Audin
P
P
Delabre
I
I
Gabrion
C
C
Petavy
A F
AF
Paris
J
J
D000469:Alkaline Phosphatase / Q000378:metabolism; D000480:Alkynes / Q000138:chemical synthesis* / Q000494:pharmacology*; D000813:Anilides / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D004444:Echinococcosis, Hepatic / Q000188:drug therapy / Q000473:pathology; D004446:Echinococcus / Q000187:drug effects* / Q000201:enzymology / Q000648:ultrastructure; D005260:Female; D005849:Gerbillinae; D005947:Glucose / Q000378:metabolism; D006003:Glycogen / Q000378:metabolism; D007510:Isatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D008099:Liver / Q000469:parasitology / Q000473:pathology; D009682:Magnetic Resonance Spectroscopy; D008297:Male
D000480:Alkynes; D000813:Anilides; C082146:3-(1-hexynyl)-3-hydroxy-2-indolinone; C082144:1-methyl-3-(1-hexynyl)-3-hydroxy-2-indolinone; C082143:3-(1-hexynyl)-3-hydroxy-5-nitro-2-indolinone; C082147:2-(hydroxy)-3-octyn carboxanilide; D007510:Isatin; D006003:Glycogen; D007770:L-Lactate Dehydrogenase; D000469:Alkaline Phosphatase; D005947:Glucose