Activity of methylgerambullin from Glycosmis species (Rutaceae) against Entamoeba histolytica and Giardia duodenalis in vitro.
Acrylamides
/ chemical synthesis
Amides
/ chemical synthesis
Antiprotozoal Agents
/ chemical synthesis
Entamoeba histolytica
/ drug effects
Entamoebiasis
/ drug therapy
Giardia lamblia
/ drug effects
Giardiasis
/ drug therapy
Humans
Plant Extracts
/ chemistry
Rutaceae
/ chemistry
Sulfur Compounds
/ chemical synthesis
Aglafoline
Entamoeba histolytica
Giardia duodenalis
Glycosmis spp.
Methylgerambullin
Sulphur-containing amide
Journal
International journal for parasitology. Drugs and drug resistance
ISSN: 2211-3207
Titre abrégé: Int J Parasitol Drugs Drug Resist
Pays: Netherlands
ID NLM: 101576715
Informations de publication
Date de publication:
08 2019
08 2019
Historique:
received:
16
11
2018
revised:
06
08
2019
accepted:
09
08
2019
pubmed:
1
9
2019
medline:
19
2
2020
entrez:
1
9
2019
Statut:
ppublish
Résumé
Entamoeba histolytica and Giardia duodenalis are widespread intestinal protozoan parasites which both spread via cysts that have to be ingested to infect a new host. Their environment, the small intestine for G. duodenalis and the colon for E. histolytica, contains only very limited amounts of oxygen, so both parasites generate energy by fermentation and substrate level phosphorylation rather than by oxidative phosphorylation. They both contain reducing agents able to reduce and activate nitroimidazole drugs such as metronidazole which is the gold standard drug to treat Entamoeba or Giardia infections. Although metronidazole works well in the majority of cases, it has a number of drawbacks. In animal models, the drug has carcinogenic activity, and concerns about a possible teratogenic activity remain. In addition, the treatment of G. duodenalis infections is hampered by emerging metronidazole resistance. Plant-derived drugs play a dominant role in human medicine, therefore we tested the activity of 14 isolated plant compounds belonging to seven different classes in vitro against both parasites. The tests were performed in a new setting in microtiter plates under anaerobic conditions. The compound with the highest activity was methylgerambullin, a sulphur-containing amide found in Glycosmis species of the family Rutaceae with an EC
Identifiants
pubmed: 31472356
pii: S2211-3207(18)30171-4
doi: 10.1016/j.ijpddr.2019.08.001
pmc: PMC6722286
pii:
doi:
Substances chimiques
Acrylamides
0
Amides
0
Antiprotozoal Agents
0
Plant Extracts
0
Sulfur Compounds
0
methylgerambullin
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
109-117Informations de copyright
Copyright © 2019 The Authors. Published by Elsevier Ltd.. All rights reserved.
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