Journal: International Journal for Parasitology: Drugs and Drug Resistance

Article Title: High-throughput screen of drug repurposing library identifies inhibitors of Sarcocystis neurona growth

doi: 10.1016/j.ijpddr.2018.02.002

Figure Lengend Snippet: Inhibitory compounds of S. neurona .

Article Snippet: AM-251, artesunate, azelastine HCl, carmofur, clofazimine, dantrolene, disulfiram, hexachlorophene, perphenazine, prazosin, and primaquine phosphate were purchased from TargetMol.

Techniques:

Journal: Antioxidants

Article Title: Syk Kinase Inhibitors Synergize with Artemisinins by Enhancing Oxidative Stress in Plasmodium falciparum -Parasitized Erythrocytes

doi: 10.3390/antiox9080753

Figure Lengend Snippet: Combination index value (CI) 24 and 48 h after treatment.

Article Snippet: Cultures at the ring stage of P. falciparum were treated at 12 h post infection, from 3 to 24 h, with the indicated concentrations of dihydroartemisinin (DHA), artesunate (AS), or artemether (ATH) combined with the desired concentration of one of the following Syk inhibitors: P505-15 (Selleckchem); R406 (Calbiochem, Darmstadt, Germany), entospletinib (Selleckchem), Syk inhibitor II (henceforth abbreviated as SYK II), piceatannol, or imatinib (Santa Cruz Biotechnology).

Techniques:

Journal: Antioxidants

Article Title: Syk Kinase Inhibitors Synergize with Artemisinins by Enhancing Oxidative Stress in Plasmodium falciparum -Parasitized Erythrocytes

doi: 10.3390/antiox9080753

Figure Lengend Snippet: Isobolograms showing the interactions between Syk Inhibitors (P505-15 and R406) and dihydroartemisinin (DHA) and artesunate (AS) in combination with the iron chelator Deferasirox (DFX), after 24 h of incubation in the P . falciparum Palo Alto strain. Synchronized P. falciparum cultures were treated for 24 h with different concentrations (from 0.05 to 2.5 µM) of representative Syk inhibitors (P505-15 and R406) in combination with different concentrations of DHA and AS (from 0.6 to 10 nM) using a fixed concentration (50 µM) of the iron chelator Deferasirox (DFX) at the ring stage.

Article Snippet: Cultures at the ring stage of P. falciparum were treated at 12 h post infection, from 3 to 24 h, with the indicated concentrations of dihydroartemisinin (DHA), artesunate (AS), or artemether (ATH) combined with the desired concentration of one of the following Syk inhibitors: P505-15 (Selleckchem); R406 (Calbiochem, Darmstadt, Germany), entospletinib (Selleckchem), Syk inhibitor II (henceforth abbreviated as SYK II), piceatannol, or imatinib (Santa Cruz Biotechnology).

Techniques: Incubation, Concentration Assay

Journal: Antioxidants

Article Title: Syk Kinase Inhibitors Synergize with Artemisinins by Enhancing Oxidative Stress in Plasmodium falciparum -Parasitized Erythrocytes

doi: 10.3390/antiox9080753

Figure Lengend Snippet: Combination index value (CI) 24 h after treatment. Combination index (CI) (Chow–Talalay) of different SYK inhibitors (P505-15 and R406) at different concentrations (50–500 nM) in combination with different artemisinin derivatives (dihydroartemisinin and artesunate) using a fixed concentration of the iron chelator Deferasirox (DFX) after 24 and 48 h of incubation.

Article Snippet: Cultures at the ring stage of P. falciparum were treated at 12 h post infection, from 3 to 24 h, with the indicated concentrations of dihydroartemisinin (DHA), artesunate (AS), or artemether (ATH) combined with the desired concentration of one of the following Syk inhibitors: P505-15 (Selleckchem); R406 (Calbiochem, Darmstadt, Germany), entospletinib (Selleckchem), Syk inhibitor II (henceforth abbreviated as SYK II), piceatannol, or imatinib (Santa Cruz Biotechnology).

Techniques: Concentration Assay, Incubation

Journal: Animals : an Open Access Journal from MDPI

Article Title: Effect of Artesunate on Leishmania Amazonesis Induced Neuroinflammation and Nociceptive Behavior in Male Balb/C Mice

doi: 10.3390/ani10040557

Figure Lengend Snippet: ( A ) An elevated plus maze test showed a significant decrease in time spent on open arms and number of open arm entries for the infected group compared to the control group. Treatment with artesunate significantly increased time spent on open arms and number of open arm entries compared to infected group. ( B ) An open field test showed a significant decrease in time spent in the center and the number of lines crossed in the infected group compared to control group. Treatment with artesunate significantly decreased the time spent in the center and the number of lines crossed compared to infected group. Data are expressed as mean ± SEM from N = 10 mice for each group. *** p < 0.001 vs. control group; ** p < 0.01 vs. control group; °° p < 0.01 vs. infected group; ° p < 0.05 vs. infected group.

Article Snippet: Artesunate was obtained from Santa Cruz Biotechnology.

Techniques: Infection, Control

Journal: Animals : an Open Access Journal from MDPI

Article Title: Effect of Artesunate on Leishmania Amazonesis Induced Neuroinflammation and Nociceptive Behavior in Male Balb/C Mice

doi: 10.3390/ani10040557

Figure Lengend Snippet: ( A ) Hematoxylin and eosin (H&E) staining and histological score graph of infected paw tissues from control, infected, and artesunate groups. ( B ) Myeloperoxidase (MPO) assay highlights the presence of inflammatory cells. L. amazonensis infection induced a significant increase in MPO, and the artesunate group showed a significant reduction in MPO compared to the infected group. ( C ) qPCR for parasitism in paw tissue evaluation. Data are expressed as mean ± SEM from N = 10 mice for each group. *** p < 0.001 vs. control group; ° p < 0.05 vs. infected group; °°° p < 0.001 vs. infected group.

Article Snippet: Artesunate was obtained from Santa Cruz Biotechnology.

Techniques: Staining, Infection, Control, MPO Assay

Journal: Genes

Article Title: Genomic and Transcriptomic Analysis for Identification of Genes and Interlinked Pathways Mediating Artemisinin Resistance in Leishmania donovani

doi: 10.3390/genes11111362

Figure Lengend Snippet: Analysis of CNV diversity in artesunate-resistant L.donovani (K133AS-R). ( A ) Size distribution of CNVs detected in the K133AS-R genome ( B ) Comparative CNV analysis of K133WT vs. K133AS-R.

Article Snippet: The susceptibility of K133WT and K133AS-R parasites towards artesunate was determined in the presence of the AQP1 inhibitor (Tocris Biosciences, Bristol, UK) and ABC transporter modulator, verapamil (Sigma, St. Louis, MO, USA).

Techniques:

Journal: Genes

Article Title: Genomic and Transcriptomic Analysis for Identification of Genes and Interlinked Pathways Mediating Artemisinin Resistance in Leishmania donovani

doi: 10.3390/genes11111362

Figure Lengend Snippet: Susceptibility of K133WT/K133AS-R isolates in the presence of the AQP1 inhibitor or the modulator to ABC transporter, verapamil. In vitro susceptibility of the sensitive wild-type strain K133 WT/artemisinin-resistant strain K133AS-R isolates towards artesunate in the presence of the AQP1 inhibitor (AQP1 Inh.) and verapamil (Vera) at ( A ) the promastigote stage and ( B ) amastigote stage. IC 50 ± SD of three independent experiments in duplicates is represented here. *** represents p ≤ 0.001, **** represents p ≤ 0.0001, NS represents not significant, Circle represents IC 50 of K133WT, Triangle represents IC 50 of K133AS-R.

Article Snippet: The susceptibility of K133WT and K133AS-R parasites towards artesunate was determined in the presence of the AQP1 inhibitor (Tocris Biosciences, Bristol, UK) and ABC transporter modulator, verapamil (Sigma, St. Louis, MO, USA).

Techniques: In Vitro

Journal: Genes

Article Title: Genomic and Transcriptomic Analysis for Identification of Genes and Interlinked Pathways Mediating Artemisinin Resistance in Leishmania donovani

doi: 10.3390/genes11111362

Figure Lengend Snippet: Transcriptome predicted adaptations contributing artesunate resistance in L. donovani : Genes altered in K133AS-R parasites are represented here. Genes marked with an up and down arrow represent, respectively, the upregulated genes and the downregulated genes in K133AS-R parasites. 1, 2, 3, 4, 5, and 6 are probable adaptations in K133AS-R parasites. (1.) Downregulation of Atg8 and HSP70 leads to increased ROS production, which was compensated by upregulation in the expression of GSH1, (2.) Upregulated expression of enzymes involved in amino acid and lipid metabolism and downregulated expression of the enzyme involved in carbohydrate metabolism, suggesting a dependency on these metabolites for energy generation, (3.) Reduced DNA synthesis that leads to the parasites in the quiescence state may be responsible for artesunate resistance in Leishmania , (4.) Reduced protein synthesis and reduced protein degradation, (5.) Upregulated expression of AQP1 leads to higher nutrient uptake and increased discharge of waste material and metabolic end product from the parasites and (6.) Upregulated expression of ABC transporter (ABCG1) and partial reversion or resistance in the presence of the ABC transporter modulator verapamil suggested probable involvement of the ABC transporter in the efflux of artesunate drug.

Article Snippet: The susceptibility of K133WT and K133AS-R parasites towards artesunate was determined in the presence of the AQP1 inhibitor (Tocris Biosciences, Bristol, UK) and ABC transporter modulator, verapamil (Sigma, St. Louis, MO, USA).

Techniques: Expressing, DNA Synthesis

Journal: Malaria Journal

Article Title: Prognostic indicators in adults hospitalized with falciparum malaria in Western Thailand

doi: 10.1186/1475-2875-12-229

Figure Lengend Snippet: Anti-malarial dr u g treatment and outcome

Article Snippet: Artemisinin-based parenteral treatment: Intravenous artesunate (Guilin Pharmaceutical Factory No. 2, Guangxi, People’s Republic of China); 2.4 mg/kg stat, 1.2 mg/kg at 12 h followed by 1.2 mg/kg every 24 h) or intramuscular artemether (3.2 mg/kg stat followed by 1.6 mg/kg every 24 h) for 7 days alone or with oral doxycycline, tetracycline or mefloquine (alone or combined with SP) with or without primaquine.

Techniques:

Journal: International Journal of Ophthalmology

Article Title: Artesunate inhibits proliferation and migration of RPE cells and TGF-β2 mediated epithelial mesenchymal transition by suppressing PI3K/AKT pathway

doi: 10.18240/ijo.2022.02.02

Figure Lengend Snippet: ARPE-19 cells were left untreated with different concentrations of artesunate (0, 75, 100, 150, and 200 µmol/L) for 24, 48, and 72h. Absorbance at 450 nm showed a significant decrease in the growth of artesunate-treated cells compared with that in the control cells in a dose-and-time-dependent manner. aP<0.05, bP<0.01, cP<0.001, dP<0.0001. The date are presented as the mean±SD (n=3/group).

Article Snippet: Cells were treated with artesunate which had various concentrations (lot#418A024.Solarbio, China).

Techniques: Control

Journal: International Journal of Ophthalmology

Article Title: Artesunate inhibits proliferation and migration of RPE cells and TGF-β2 mediated epithelial mesenchymal transition by suppressing PI3K/AKT pathway

doi: 10.18240/ijo.2022.02.02

Figure Lengend Snippet: ARPE-19 cells are treated with artesunate at 0, 50, and 150 µmol/L for 0, 12, 24, and 36h. A: Scratch assay were measured cell horizontal migration. cP<0.001, dP<0.0001. Data are presented as mean±SD. n=3/group. Scale bar: 250 µm. B: In the Transwell assay, the cells that migrated into the detection zone (the lower chamber) were measured. dP<0.0001. Data are presented as mean±SD. n=3/group. Scale bar: 50 µm.

Article Snippet: Cells were treated with artesunate which had various concentrations (lot#418A024.Solarbio, China).

Techniques: Wound Healing Assay, Migration, Transwell Assay

Journal: International Journal of Ophthalmology

Article Title: Artesunate inhibits proliferation and migration of RPE cells and TGF-β2 mediated epithelial mesenchymal transition by suppressing PI3K/AKT pathway

doi: 10.18240/ijo.2022.02.02

Figure Lengend Snippet: After 48h of pretreatment with TGF-β2, ARPE-19 cells were treated with or without artesunate for 12, 24, and 36h. A: Scratch assay was measured cell horizontal migration. bP<0.01, cP<0.001, dP<0.0001. Data are presented as mean±SD (n=3/group). Scale bar: 250 µm. B: In the Transwell assay, the cells that migrated into the detection zone (the lower chamber) were measured. dP<0.0001. Data are presented as mean±SD (n=3/group). Scale bar: 50 µm.

Article Snippet: Cells were treated with artesunate which had various concentrations (lot#418A024.Solarbio, China).

Techniques: Wound Healing Assay, Migration, Transwell Assay

Journal: International Journal of Ophthalmology

Article Title: Artesunate inhibits proliferation and migration of RPE cells and TGF-β2 mediated epithelial mesenchymal transition by suppressing PI3K/AKT pathway

doi: 10.18240/ijo.2022.02.02

Figure Lengend Snippet: After 48h of pretreatment with TGF, ARPE-19 cells used for EMT assay were treated with or without ART for up to 48h. A: Western blot analysis levels of vimentin, α-SMA and GAPDH in the lysates of ARPE-19 cells after treatment for 48h. NS (P>0.05), aP<0.05, bP<0.01, cP<0.001. The data are presented as the mean±SD. (n=3/group). B: Immunofluorescence staining for vimentin (green) and nuclei (blue) in ARPE-19 cells after treatment for 48h. Scale bar: 50 µm. ART: Artesunate.

Article Snippet: Cells were treated with artesunate which had various concentrations (lot#418A024.Solarbio, China).

Techniques: Western Blot, Immunofluorescence, Staining

Journal: International Journal of Ophthalmology

Article Title: Artesunate inhibits proliferation and migration of RPE cells and TGF-β2 mediated epithelial mesenchymal transition by suppressing PI3K/AKT pathway

doi: 10.18240/ijo.2022.02.02

Figure Lengend Snippet: Vitreous tissue were collected from clinical patients. A: Western blot analysis levels of vimentin, α-SMA and the GAPDH in the lysates of clinical tissue. NS (P>0.05), aP<0.05, bP<0.01. The data are presented as the mean±SD (n=3/group). B: Western blot analysis levels of PI3K, P-PI3K, Akt, P-Akt and the housekeeping protein GAPDH in the lysates of clinical tissue. NS (P>0.05), aP<0.05, bP<0.01, cP<0.001, dP<0.0001. The data are presented as the mean±SD (n=3/group). ART: Artesunate.

Article Snippet: Cells were treated with artesunate which had various concentrations (lot#418A024.Solarbio, China).

Techniques: Western Blot

Journal: International Journal of Ophthalmology

Article Title: Artesunate inhibits proliferation and migration of RPE cells and TGF-β2 mediated epithelial mesenchymal transition by suppressing PI3K/AKT pathway

doi: 10.18240/ijo.2022.02.02

Figure Lengend Snippet: After 48h of pretreatment with TGF, ARPE-19 cells stimulated with or without artesunate for 48h. Western blot analysis levels of PI3K, P-PI3K, Akt, P-Akt and GAPDH in the lysates of ARPE-19 cells after treatment for 48h. NS (P>0.05), aP<0.05, bP<0.01, cP<0.001, dP<0.0001. The data are presented as the mean±SD (n=3/group). ART: Artesunate.

Article Snippet: Cells were treated with artesunate which had various concentrations (lot#418A024.Solarbio, China).

Techniques: Western Blot