artemisinin art  (MedChemExpress)

Journal: Malaria Journal

Article Title: CYP3A4-mediated metabolism of artemisinin to 10β-hydroxyartemisinin with comparable anti-malarial potency

doi: 10.1186/s12936-024-05163-y

Figure Lengend Snippet: Selected ion chromatograms and MS/MS spectra of artemisinin (ART) and its hydroxylated metabolites, when ART (1 μM) was incubated in human liver microsomes (1 mg/mL) for 30 min. I: total ion chromatogram (TIC); II: ART ( m/z 283.1540); III: hydroxylated metabolites of ART ( m/z 316.1755). ART-M: 10β–hydroxyartemisinin

Article Snippet: Artemisinin (ART) was purchased from Kunming Pharmaceutical Co. (Yunnan, China; purity > 99.0%).

Techniques: Tandem Mass Spectroscopy, Incubation

Journal: Malaria Journal

Article Title: CYP3A4-mediated metabolism of artemisinin to 10β-hydroxyartemisinin with comparable anti-malarial potency

doi: 10.1186/s12936-024-05163-y

Figure Lengend Snippet: Enzyme phenotyping for the formation of ART-M (10β–hydroxyartemisinin) from artemisinin (ART; 1 µM) using human liver microsomes (HLM, 1 mg/mL) in the presence of (non)selective inhibitors of total P450 enzymes (1-ABT), CYP1A2 ( α -naphthoflavone, NAPH), CYP2B6 (ticlopidine, TCL), CYP2C8 (quercetin, QUER), CYP2C9 (sulfaphenazole, SULF), CYP2C19 (ticlopidine, TCL), CYP2D6 (quinidine, QUIN) or CYP3A4 (ketoconazole, KTZ), or using recombinant P450 isoforms (100 pmol/mL). A ART-M in HLMs; B ART-M in rCYPs

Article Snippet: Artemisinin (ART) was purchased from Kunming Pharmaceutical Co. (Yunnan, China; purity > 99.0%).

Techniques: Recombinant

Journal: Malaria Journal

Article Title: CYP3A4-mediated metabolism of artemisinin to 10β-hydroxyartemisinin with comparable anti-malarial potency

doi: 10.1186/s12936-024-05163-y

Figure Lengend Snippet: Antiplasmodial activity of artemisinin (ART) and its metabolite 10β–hydroxyartemisinin (ART-M) against two reference Plasmodium strains ( Pf 3D7 and Pf Dd2)

Article Snippet: Artemisinin (ART) was purchased from Kunming Pharmaceutical Co. (Yunnan, China; purity > 99.0%).

Techniques: Activity Assay

Journal: Malaria Journal

Article Title: CYP3A4-mediated metabolism of artemisinin to 10β-hydroxyartemisinin with comparable anti-malarial potency

doi: 10.1186/s12936-024-05163-y

Figure Lengend Snippet: Mean (+ S.D.) plasma concentration–time profiles of artemisinin (ART) and its metabolite 10β–hydroxyartemisinin (ART-M) in healthy Chinese subjects (n = 6) after a recommended two-day oral dose of Artequick (125 mg/dose of ART plus 750 mg/dose of piperaquine), and individual AUC 0-t values

Article Snippet: Artemisinin (ART) was purchased from Kunming Pharmaceutical Co. (Yunnan, China; purity > 99.0%).

Techniques: Concentration Assay

Journal: Malaria Journal

Article Title: CYP3A4-mediated metabolism of artemisinin to 10β-hydroxyartemisinin with comparable anti-malarial potency

doi: 10.1186/s12936-024-05163-y

Figure Lengend Snippet: The pharmacokinetic/pharmacodynamic indices for in vivo anti-malarial potency of artemisinin (ART) and its metabolite 10β-hydroxyartemisinin (ART-M)

Article Snippet: Artemisinin (ART) was purchased from Kunming Pharmaceutical Co. (Yunnan, China; purity > 99.0%).

Techniques: In Vivo

Journal: Parasites & Vectors

Article Title: Artemisitene shows superiority over artemisinin in preventing Schistosoma japonica -induced liver disease

doi: 10.1186/s13071-024-06426-y

Figure Lengend Snippet: Differential effect of ATT and ART on S. japonicum infection‑induced liver inflammation and fibrosis in mice. a Experimental flowchart depicting the treatment of mice infected with S. japonicum cercariae. After a 6-week infection period, mice received intraperitoneal injection of ART or ATT (5 mg/kg body weight) from day 3 to 14 post-infection. b Serum levels of ALT and AST were measured and analyzed in the indicated mouse groups using a t -test ( n = 4 for uninfected; n = 5 or 6 for infected). c , d Liver sections were stained with H&E. The granuloma area percentages, encompassing pre-, early, mature, and late stages around a single egg in each liver section, were quantified using ImageJ and analyzed by two-way ANOVA ( c ). Representative images of granulomas at different stages around a single egg from each mouse group are presented ( d ). e α-SMA levels in mouse liver tissues were assessed by western blotting (WB) (left panel), and semiquantitative analysis of this protein was performed using ImageJ software (right panel, t -test). f Liver sections were stained with Sirius red (200 μm) to visualize S. japonicum egg granulomas. Images show representative staining from mice with and without ART or ATT treatment (left panel). The morphometric analysis of collagen areas around a single egg (stained in strong red) was conducted, and the results are presented (right panel, t -test). Data represent mean ± SD from different group experiments. Significant differences are indicated as * P < 0.05 and ** P < 0.01

Article Snippet: ART was purchased from MedChemExpress (HY-B0094), and ATT was produced and identified the research group led by Professor Zhong-jin Yang at the College of Pharmacy, Guangzhou Medical University [ ].

Techniques: Infection, Injection, Staining, Western Blot, Software

Journal: Parasites & Vectors

Article Title: Artemisitene shows superiority over artemisinin in preventing Schistosoma japonica -induced liver disease

doi: 10.1186/s13071-024-06426-y

Figure Lengend Snippet: Enhanced anti- S. japonicum activity of ATT compared with ART in mice. a The total number of S. japonicum adult worms and individual male worms present in the hepatoportal and mesenteric veins of mice with 6 weeks of S. japonicum infection, with either ART or ATT treatment ( n = 4–6). Data were thoroughly counted and analyzed using a t -test. b Enumeration of eggs in liver section (2 mm) from mice subjected to 6 weeks of S. japonicum infection, with or without ART or ATT treatment, was conducted and analyzed by t -test. Representative liver section (2 mm or 400 μm) post- H&E staining from these groups are exhibited in c . d Scanning electron microscopy (SEM) was employed to examine the surface morphology of adult worms extracted from the livers of infected mice, treated with or without ATT. Detailed views include the tegument of adult worms' mid-body without (a1) or with (a2) ATT treatment. ATT’s impact is evident in the altered appearance of regular prominent spines (b1 versus b2), crests (c1 versus c2) in the mid-body tegument and prominent spines (e1 versus e2) on the gynecophoral canal of adult males (d1 versus d2). e , f Volcano plots illustrate the differential expression of genes (DEGs) in S. japonicum female ( e ) and male ( f ) adult worms from mice with or without ATT treatment, as analyzed by RNA-seq analysis (FDR ≤ 0.001 and log 2 ≥ 1). The X axis represents the log 2 fold change, and the Y axis represents the log 10 (adjusted P value). In these plots, red and green represent up- and downregulated genes, respectively, while gray dots denote genes without significant changes. The threshold was set at adjusted P value < 0.05 and |log 2 fold change| > 1. g , h Significant Gene Ontology (GO) categories for DEGs in S. japonicum female ( h ) and male ( i ) adult worms from mice treated with or without ATT. The X axis denotes the log 10 ( P value), and the Y axis lists the GO term names

Article Snippet: ART was purchased from MedChemExpress (HY-B0094), and ATT was produced and identified the research group led by Professor Zhong-jin Yang at the College of Pharmacy, Guangzhou Medical University [ ].

Techniques: Activity Assay, Infection, Staining, Electron Microscopy, Quantitative Proteomics, RNA Sequencing

Journal: Parasites & Vectors

Article Title: Artemisitene shows superiority over artemisinin in preventing Schistosoma japonica -induced liver disease

doi: 10.1186/s13071-024-06426-y

Figure Lengend Snippet: Neutrophil, eosinophil and macrophage redistribution in the liver or spleen of S. japonicum -infected mice following ART or ATT treatment. Flow cytometry was used for these cells analysis. Nucleated cells were initially gated on the basis of size and complexity, as indicated by forward scatter area (FSC-A) and side scatter area (SSC-A). Subsequently, single cells were distinguished from doublets using a combination of FSC-A and FSC-H. a Within this single cell population, live immune cells were identified as CD45 + . Neutrophils (Neu) were further defined using CD45 + CD11b + Ly6G + markers, and eosinophils (Eos) were gated as CD45 + CD11b + SiglecF + . Macrophages (MA) were identified as CD45 + Ly6G − F4/80 + . These MA were further classified into M0 (CD206 − iNOS − ), M1 (iNOS + ), and M2 (CD206 + ) subpopulations. b The proportion of neutrophils within CD45 + cell population in both liver and spleen of infected mice, with or without ART or ATT treatment, was evaluated and analyzed by two-way ANOVA ( n = 4–6). c The proportion of eosinophils among CD45 + cells in both the liver and spleen of infected mice, treated with or without ART or ATT, was evaluated and analyzed by two-way ANOVA. d , e The proportions of total macrophages and their M0, M1, and M2 subpopulations in the CD45 + Ly6G − liver cells of infected mice, treated with or without ART or ATT, were evaluated and analyzed by one-way or two-way ANOVA, respectively. f The M1/M2 ratio (index) was presented and analyzed by one-way ANOVA. Data represent mean ± SD from different experimental groups. Significant differences are denoted by * P < 0.05, ** P < 0.01, *** P < 0.001 and **** P < 0.0001

Article Snippet: ART was purchased from MedChemExpress (HY-B0094), and ATT was produced and identified the research group led by Professor Zhong-jin Yang at the College of Pharmacy, Guangzhou Medical University [ ].

Techniques: Infection, Flow Cytometry

Journal: Parasites & Vectors

Article Title: Artemisitene shows superiority over artemisinin in preventing Schistosoma japonica -induced liver disease

doi: 10.1186/s13071-024-06426-y

Figure Lengend Snippet: Altered Th1/Th2 index in the livers of infected mice treated with ATT compared with ART. a Flow cytometry was used to assess the proportion of Th1 and Th2 cells in the liver of indicated mice. The gating strategy involved identifying CD45 + CD3 + cells, then subdividing them into CD45 + CD3 + CD4 + IFN-γ + (Th1) and IL-4 + (Th2) populations. b , c The amount of Th1 and Th2 cells in the liver of infected mice, with or without ART or ATT treatment, were evaluated. a and b display the typical cell populations for Th1 and Th2, and panel ( b ) providing their quantification, which was analyzed by two-way ANOVA. d The Th1/Th2 ratio (index) was analyzed by t -test. Data represent mean ± SD from different experimental groups. Significant differences are indicated by * P < 0.05 and ** P < 0.01

Article Snippet: ART was purchased from MedChemExpress (HY-B0094), and ATT was produced and identified the research group led by Professor Zhong-jin Yang at the College of Pharmacy, Guangzhou Medical University [ ].

Techniques: Infection, Flow Cytometry

Journal: Parasites & Vectors

Article Title: Artemisitene shows superiority over artemisinin in preventing Schistosoma japonica -induced liver disease

doi: 10.1186/s13071-024-06426-y

Figure Lengend Snippet: Correlation analysis of the frequency of host immune cells in the liver or spleen with the extent of liver inflammation or fibrosis, the size of granuloma area and the count of parasites. a , b Correlation plot of the frequency of neutrophils, eosinophils in the liver or spleen, the frequency of macrophages or their subsets M0, M1 or M2, M1/M2 index, and the frequency of Th1, Th2 and Th1/Th2 index in the liver with ALT and AST concentration, α-SMA expression folds (/GAPDH), area of collagen, pregranuloma, early granuloma, mature granuloma, late granuloma, and average granuloma, and count of worms, single males, and eggs from S. japonica at 6 weeks with or without ART ( a ) or ATT ( b ) treatment ( Sj 6w/NC, Sj 6w/ART or Sj 6W/ATT, n = 5–6) through OriginPro 2021. Significant correlation are indicated by * P < 0.05 and ** P < 0.01

Article Snippet: ART was purchased from MedChemExpress (HY-B0094), and ATT was produced and identified the research group led by Professor Zhong-jin Yang at the College of Pharmacy, Guangzhou Medical University [ ].

Techniques: Concentration Assay, Expressing

Journal: Molecules

Article Title: Differential Anti-Fibrotic and Remodeling Responses of Human Dermal Fibroblasts to Artemisia sp., Artemisinin, and Its Derivatives

doi: 10.3390/molecules29092107

Figure Lengend Snippet: ( Left ) artemisinin (ART), artemisinin derivatives (DHA, AS, AM), and an artemisinin liver metabolite, deoxyartemisinin (dART); ( right ) Artemisia annua and afra .

Article Snippet: A. annua tea was diluted in a growth media to 50 µM ART; A. afra tea was diluted with water to 1/2, 1/4, or 1/8 strength of the A. annua tea on a dry-weight basis as needed; artemisinin (ART; Cayman Chemical, Ann Arbor, MI, USA, 11816), artesunate (AS; Cayman Chemical 11817), artemether (AM; gift from Prof. J. Plaizier-Vercammen (Brussels, Belgium)), dihydroartemisinin (DHA; Cayman Chemical 19846), and deoxyartemisinin (dART; Toronto Research Chemicals, Toronto, Ontario, Canada, D232150) were dissolved in DMSO as 1000× stock solutions, filter sterilized, and added to a final concentration of 50 μM.

Techniques:

Journal: Molecules

Article Title: Differential Anti-Fibrotic and Remodeling Responses of Human Dermal Fibroblasts to Artemisia sp., Artemisinin, and Its Derivatives

doi: 10.3390/molecules29092107

Figure Lengend Snippet: Relative viability responses of human dermal fibroblasts via resazurin assay at 1 and 4 days after exposure to artemisinin, each of the artemisinic derivatives, artemisinin’s liver metabolite deoxyartemisinin, and hot-water extracts of A. annua , all normalized to 50 µM of the relevant artemisinic compound. Control = 100%; N ≥ 12; * = p ≤ 0.05 for samples to solvent control; # = p ≤ 0.05 for 1 day compared to 4 days using Student’s t -test.

Article Snippet: A. annua tea was diluted in a growth media to 50 µM ART; A. afra tea was diluted with water to 1/2, 1/4, or 1/8 strength of the A. annua tea on a dry-weight basis as needed; artemisinin (ART; Cayman Chemical, Ann Arbor, MI, USA, 11816), artesunate (AS; Cayman Chemical 11817), artemether (AM; gift from Prof. J. Plaizier-Vercammen (Brussels, Belgium)), dihydroartemisinin (DHA; Cayman Chemical 19846), and deoxyartemisinin (dART; Toronto Research Chemicals, Toronto, Ontario, Canada, D232150) were dissolved in DMSO as 1000× stock solutions, filter sterilized, and added to a final concentration of 50 μM.

Techniques: Resazurin Assay, Control, Solvent