Journal: Bioengineered

Article Title: An extraction from Trametes robiniophila Murr. ( Huaier ) inhibits non-small cell lung cancer proliferation via targeting to epidermal growth factor receptor

doi: 10.1080/21655979.2022.2066757

Figure Lengend Snippet: Virtual verification of Huaier targets by molecular docking. (a) Maestro 2D interactions between EGFR and gefitinib, adenosine, daucosterol, ergosterol, ergosta-7,22-dien-3β-ol and 3β-hydroxystigmast-5,22-dien-7-one. Residues in green spheres are hydrophobic, blue spheres are polar, red spheres are negatively charged, purple spheres are charged and light yellow spheres are glycine. The purple arrows and their directions represent hydrogen bonds between the ligand and the protein. The green line represents the π-π stacking arrangement seen between the aromatic core. (b) We conducted kinase activity assays to validate Huaier ’s inhibition on EGFR kinase activity. Staurosporine, an effective PKC inhibitor, was chosen as positive control. (c) Cells were conducted by CETSAs, and the protein expression of EGFR was detected by western blot analysis. The line chart showed the relative expression level of EGFR.

Article Snippet: Gefitinib and Daucosterol were both purchased from MCE (HY-50895; HY-N0410).

Techniques: Activity Assay, Inhibition, Positive Control, Expressing, Western Blot

Journal: Molecular Pharmacology

Article Title: Insights into the Structure-Activity Relationship of Glycosides as Positive Allosteric Modulators Acting on P2X7 Receptors

doi: 10.1124/molpharm.120.000129

Figure Lengend Snippet: Structural details of tested glycosides Substitution pattern is derived from Fig. 1C . Maximum response was defined at 1 mM ATP. To calculate the EC 50 ratio, the average EC 50 value for ATP + vehicle was used from each set of experiments. Average EC 50 value is shown with 95% confidence intervals in parentheses.

Article Snippet: Ginsenoside-CK (CAS 39262-14-1), ginsenoside-Rb1 (CAS 41753-43-9), ginsenoside-Rd (CAS 52705-93-8), 20( S )-ginsenoside-Rg3 (CAS 14197-60-5), 20( R )-ginsenoside-Rh2 (CAS 112246-15-8), protopanaxadiol (PPD) (CAS 30636-90-9), glycyrrhizic acid (CAS 1405-86-3), stevioside (CAS 57817-89-7), daucosterol (CAS 474-58-8), esculentoside A (CAS 65497-07-6), mogroside V (CAS 88901-36-4), saikosaponin A (CAS 20736-09-8), and stevenleaf (CAS 80321-63-7) were from Shanghai Richem International Ltd., China (supplier code CDCMANSETE).

Techniques: Derivative Assay

Journal: Molecular Pharmacology

Article Title: Insights into the Structure-Activity Relationship of Glycosides as Positive Allosteric Modulators Acting on P2X7 Receptors

doi: 10.1124/molpharm.120.000129

Figure Lengend Snippet: Screening glycosides containing monosaccharide moieties at P2X7. Dose-response curves to ATP in the presence of vehicle (DMSO), ginsenoside-CK, and the following: daucosterol (10 µM) (A), stevioside (SV; 10 µM) (B), ginsenoside-F1 (F1; 10 µM) (C), ginsenoside-F2 (F2; 10 µM) (D), ouabain (10 µM) (E), or scilliroside (10 µM) (F). Ginsenoside-CK is demonstrated throughout as the reference compound (same data shown in each plot). Data are collated from three independent experiments each performed in triplicate. Error bars represent S.D.

Article Snippet: Ginsenoside-CK (CAS 39262-14-1), ginsenoside-Rb1 (CAS 41753-43-9), ginsenoside-Rd (CAS 52705-93-8), 20( S )-ginsenoside-Rg3 (CAS 14197-60-5), 20( R )-ginsenoside-Rh2 (CAS 112246-15-8), protopanaxadiol (PPD) (CAS 30636-90-9), glycyrrhizic acid (CAS 1405-86-3), stevioside (CAS 57817-89-7), daucosterol (CAS 474-58-8), esculentoside A (CAS 65497-07-6), mogroside V (CAS 88901-36-4), saikosaponin A (CAS 20736-09-8), and stevenleaf (CAS 80321-63-7) were from Shanghai Richem International Ltd., China (supplier code CDCMANSETE).

Techniques: