ArticleAntimicrobial agents and chemotherapy2001
High-affinity binding of silybin derivatives to the nucleotide-binding domain of a Leishmania tropica P-glycoprotein-like transporter and chemosensitization of a multidrug-resistant parasite to daunomycin.
Article in Antimicrobial agents and chemotherapy, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 44 citations in OpenAlex.
- A Comprehensive Review on the Antibacterial, Antifungal, Antiviral, and Antiparasitic Potential of Silybin.Antibiotics (Basel, Switzerland) · 2024Review
- Global distribution of treatment resistance gene markers for leishmaniasis.Journal of clinical laboratory analysis · 2022Review
- Modulation of Skin Inflammatory Response by Active Components of Silymarin.Molecules (Basel, Switzerland) · 2018Article
- In-Vitro Activity of Silybin and Related Flavonolignans againstMolecules (Basel, Switzerland) · 2018Article
- HM015k, a Novel Silybin Derivative, Multi-Targets Metastatic Ovarian Cancer Cells and Is Safe in Zebrafish Toxicity Studies.Frontiers in pharmacology · 2017Article
- Sitamaquine overcomes ABC-mediated resistance to miltefosine and antimony in Leishmania.Antimicrobial agents and chemotherapy · 2011Article
- Use of antimony in the treatment of leishmaniasis: current status and future directions.Molecular biology international · 2011Article
- Synergistic antibacterial effect between silybin and N,N'-dicyclohexylcarbodiimide in clinical Pseudomonas aeruginosa isolates.Journal of microbiology (Seoul, Korea) · 2008Article
- Common dietary flavonoids inhibit the growth of the intraerythrocytic malaria parasite.BMC research notes · 2008Article
- Combination of suboptimal doses of inhibitors targeting different domains of LtrMDR1 efficiently overcomes resistance of Leishmania spp. to Miltefosine by inhibiting drug efflux.Antimicrobial agents and chemotherapy · 2006Article
- Evaluation of silymarin in the treatment on asymptomatic Giardia infections in dogs.Parasitology research · 2005Article
- Alkyl-lysophospholipid resistance in multidrug-resistant Leishmania tropica and chemosensitization by a novel P-glycoprotein-like transporter modulator.Antimicrobial agents and chemotherapy · 2001Article
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Authors and funding
9 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In order to overcome the multidrug resistance mediated by P-glycoprotein-like transporters in Leishmania spp., we have studied the effects produced by derivatives of the flavanolignan silybin and related compounds lacking the monolignol unit on (i) the affinity of binding to a recombinant C-terminal nucleotide-binding domain of the L. tropica P-glycoprotein-like transporter and (ii) the sensitization to daunomycin on promastigote forms of a multidrug-resistant L. tropica line overexpressing the transporter. Oxidation of the flavanonol silybin to the corresponding flavonol dehydrosilybin, the presence of the monolignol unit, and the addition of a hydrophobic substituent such as dimethylallyl, especially at position 8 of ring A, considerably increased the binding affinity. The in vitro binding affinity of these compounds for the recombinant cytosolic domain correlated with their modulation of drug resistance phenotype. In particular, 8-(3,3-dimethylallyl)-dehydrosilybin effectively sensitized multidrug-resistant Leishmania spp. to daunomycin. The cytosolic domains are therefore attractive targets for the rational design of inhibitors against P-glycoprotein-like transporters.
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