Journal: ACS Sustainable Chemistry & Engineering

Article Title: Optimization of Biocatalytic Rhododendrol Production from Biogenic Rhododendrol Glycosides

doi: 10.1021/acssuschemeng.4c05889

Figure Lengend Snippet: Reaction of rhododendrol glycoside hydrolysis catalyzed by β-glucosidase and RAPIDASE.

Article Snippet: Rhododendrol (racemic mixture) was purchased from TCI (Japan).

Techniques:

Journal: ACS Sustainable Chemistry & Engineering

Article Title: Optimization of Biocatalytic Rhododendrol Production from Biogenic Rhododendrol Glycosides

doi: 10.1021/acssuschemeng.4c05889

Figure Lengend Snippet: Hydrolysis of betuloside and apiosylrhododendrin mixture ( T = 40 °C; 100 mM phosphate buffer, pH 6). Correlation of experimental data and model through changes in the concentration of betuloside, apiosylrhododendrin, and rhododendrol over time in a batch reactor: (A) c betuloside = 64.5 mM, c apiosylrhododendrin = 16.6 mM, γ RAPIDASE = 20.0 mg mL –1 , (B) c betuloside = 62.3 mM, c apiosylrhododendrin = 17.2 mM, γ RAPIDASE = 20.0 mg mL –1 , γ β-Glu = 2.0 mg mL –1 , (C) c betuloside = 45.5 mM, c apiosylrhododendrin = 84.6 mM, γ RAPIDASE = 100.0 mg mL –1 , (D) c betuloside = 51.3 mM, c apiosylrhododendrin = 98.0 mM, γ RAPIDASE = 100.0 mg mL –1 , γ β-Glu = 2.0 mg mL –1 . Legend: ● betuloside concentration in experiment, ○ apiosylrhododendrin concentration in experiment, rhododendrol concentration in experiment, – – – betuloside concentration by model, ····· apiosylrhododendrin concentration by model, - - - rhododendrol concentration by model.

Article Snippet: Rhododendrol (racemic mixture) was purchased from TCI (Japan).

Techniques: Concentration Assay

Journal: ACS Sustainable Chemistry & Engineering

Article Title: Optimization of Biocatalytic Rhododendrol Production from Biogenic Rhododendrol Glycosides

doi: 10.1021/acssuschemeng.4c05889

Figure Lengend Snippet: Hydrolysis of crude betuloside ( T = 40 °C; 100 mM phosphate buffer, pH 6). Correlation of experimental data and model through changes in the concentration of betuloside and rhododendrol over time in (A) repetitive batch reactor ( c betuloside = 5 × 62.3 mM, γ β-Glu = 4 mg mL –1 ), (B) batch reactor with a higher substrate concentration ( c betuloside = 275.0 mM, γ β-Glu = 4 mg mL –1 ), and (C) ultrafiltration membrane reaction ( c betuloside = 62.3 mM, γ β-Glu = 4 mg mL –1 , q v = 180 μL min –1 ). Legend: ● betuloside concentration in experiment, ○ rhododendrol concentration in experiment, – – – betuloside concentration by model, - - - rhododendrol concentration by model.

Article Snippet: Rhododendrol (racemic mixture) was purchased from TCI (Japan).

Techniques: Concentration Assay, Membrane

Journal: ACS Sustainable Chemistry & Engineering

Article Title: Optimization of Biocatalytic Rhododendrol Production from Biogenic Rhododendrol Glycosides

doi: 10.1021/acssuschemeng.4c05889

Figure Lengend Snippet: Dependence of process metrics on enzyme concentrations for a mixture of rhododendrol glycosides ( x betuloside = 0.5, c rhod. glyc . = 300 mM). The results for each enzyme’s initial concentration were taken at the time when X rhod.glyc . = 99%. (A) Conversion of rhododendrol glycosides, (B) productivity, (C) final rhododendrol concentration (in g L –1 ), (D) biocatalyst yield for RAPIDASE, and (E) biocatalyst yield for β-glucosidase from almonds.

Article Snippet: Rhododendrol (racemic mixture) was purchased from TCI (Japan).

Techniques: Concentration Assay

Journal: ACS Sustainable Chemistry & Engineering

Article Title: Optimization of Biocatalytic Rhododendrol Production from Biogenic Rhododendrol Glycosides

doi: 10.1021/acssuschemeng.4c05889

Figure Lengend Snippet: Optimal initial concentrations of the enzymes RAPIDASE and β-glucosidase for the hydrolysis of rhododendrol glycoside mixtures ( c 0 = 300 mM), ensuring a substrate conversion of 99% within 24 h determined by simulation.

Article Snippet: Rhododendrol (racemic mixture) was purchased from TCI (Japan).

Techniques:

Journal: ACS Sustainable Chemistry & Engineering

Article Title: Optimization of Biocatalytic Rhododendrol Production from Biogenic Rhododendrol Glycosides

doi: 10.1021/acssuschemeng.4c05889

Figure Lengend Snippet: Estimated Kinetic Parameter, Kinetic Model, and Reactor Models for Rhododendrol Glycoside Hydrolysis Catalyzed by β-Glucosidase from Almonds

Article Snippet: Rhododendrol (racemic mixture) was purchased from TCI (Japan).

Techniques:

Journal: ACS Sustainable Chemistry & Engineering

Article Title: Optimization of Biocatalytic Rhododendrol Production from Biogenic Rhododendrol Glycosides

doi: 10.1021/acssuschemeng.4c05889

Figure Lengend Snippet: Estimated Inactivation Constants and Productivity for Rhododendrol Glycoside Hydrolysis Catalyzed by β-Glucosidase from Almonds in Different Reactors

Article Snippet: Rhododendrol (racemic mixture) was purchased from TCI (Japan).

Techniques: Membrane

Journal: ACS Sustainable Chemistry & Engineering

Article Title: Optimization of Biocatalytic Rhododendrol Production from Biogenic Rhododendrol Glycosides

doi: 10.1021/acssuschemeng.4c05889

Figure Lengend Snippet: Estimated Kinetic Parameters, Kinetic Models, and Reactor Models for Rhododendrol Glycoside Hydrolysis Catalyzed by RAPIDASE

Article Snippet: Rhododendrol (racemic mixture) was purchased from TCI (Japan).

Techniques:

Journal: ACS Sustainable Chemistry & Engineering

Article Title: Optimization of Biocatalytic Rhododendrol Production from Biogenic Rhododendrol Glycosides

doi: 10.1021/acssuschemeng.4c05889

Figure Lengend Snippet: Estimated Inactivation Constants for Rhododendrol Glycoside Hydrolysis Catalyzed by β-Glucosidase from Almonds and Polygalacturonase from RAPIDASE in a Batch Reactor

Article Snippet: Rhododendrol (racemic mixture) was purchased from TCI (Japan).

Techniques:

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: HDAC inhibitory activity of ( R )-, ( S )-, and rac -α-lipoic acid, and the reduced racemic form rac -dihydro-lipoic acid. Enzyme HDAC assays were performed with HDAC2, 4, 6, and 8. Cellular HDAC assay was performed with the class I/IIb selective HDAC substrate Boc-Lys-AC-AMC in T47D cells. Panobinostat, vorinostat, and tubastatin A served as references. Shown are IC 50 values ± SEM [µM]. HDAC enzyme assays were performed three times, each carried out in duplicates. Cellular HDAC assays are based on one experiment, carried out in triplicates. ND = not determined.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Activity Assay, Histone Deacetylase Assay

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Effect of ( R )-α-lipoic acid on acetylation level of a -tubulin and histone H3. Representative immunoblot analysis of histone H3, ac-histone H3, a -tubulin, and ac- a -tubulin in ER+ breast cancer cell lines MCF-7 and T47D. Cells were treated with 1 mM (R)-α-lipoic acid, 1 µM exemestane, as well as a combination of 1 mM (R)-α-lipoic acid and 1 µM exemestane for 48 h. ß-actin served as loading control. Uncropped and labeled immunoblots are presented in .

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Western Blot, Control, Labeling

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: IC 50 values ± SEM [µM] of ( R )-α-lipoic acid and exemestane in MCF-7, T47D, and MDA-MB-231, determined by a 72 h MTT assay. Presented are IC 50 values ± SEM [µM]. Data shown are means of pooled data of at least 2 experiments, all carried out in triplicates.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: MTT Assay

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: IC 50 ± SEM [µM] of exemestane and ( R )-, ( S )- and rac -α-lipoic acid in MCF-7, T47D, and MDA-MB-231 cell lines, determined by a 120 h MTT assay. Data shown are means of pooled data of at least 2 experiments, all carried out in triplicates.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: MTT Assay

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Concentration–effect curve of exemestane in the absence and presence of 1 mM ( R )-α-lipoic acid. Cell viability is measured using MTT assay after 72 h incubation in MCF-7 ( a ) and T47D ( b ). Data are the mean of at least two different experiments ± SD, each carried out in triplicates. Exe = exemestane. ( R )-LA = ( R )-α-lipoic acid.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Concentration Assay, MTT Assay, Incubation

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Cell proliferation of MCF-7 (a) and T47D cells (b) measured via Hoechst 33342 staining. Hoechst 33342-stained nuclei were counted after 72 h incubation with 1 µM exemestane or/and 1 mM ( R )-α-lipoic acid. Shown is one representative experiment out of a series of at least three experiments each performed with 3 replicates. Data are mean ± SD. Statistical comparison was performed using a t-test. Levels of significance: ** ( p ≤ 0.01); **** ( p ≤ 0.0001). Exe = exemestane. ( R )-LA = ( R )-α-lipoic acid.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Staining, Incubation, Comparison

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Concentration–effect curves of exemestane in the absence and presence of 100 µM and 300 ( R )-α-lipoic acid. Cell viability is measured using MTT assay after 120 h incubation in MCF-7 ( a ) and T47D cells ( b ). Data are mean of the of two different experiments ± SD, each carried out in triplicates. Exe = exemestane. ( R )-LA = ( R )-α-lipoic acid.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Concentration Assay, MTT Assay, Incubation

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Combination treatment of 1 µM exemestane and ( R )-α-lipoic acid. ( a , b ) show cell viability of MCF-7 ( a ) and T-47D ( b ) normalized to untreated control estimated via MTT assay after 120 h incubation. ( c ) Inhibition of cell viability based on data from ( a , b ): black bars represent the effects of the sum of single treatments, white bars illustrate the effect of the combination treatments. Data shown are mean ± SD of at least two independent experiments, carried out in 6 replicates. Statistical analysis was performed using a t -test. Levels of significance: **** ( p < 0.0001). ( d ) Combination index (CI) values from the Chou–Talalay analysis of data are shown in and a,b [ , ]. Fractions affected were between 0.25 and 0.8. Exe = exemestane. ( R )-LA = ( R )- a -lipoic acid. ns = not significant.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Control, MTT Assay, Incubation, Inhibition

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Combination treatment of 1 µM exemestane with 1 mM of ( R )-, ( S )-, and rac -α-lipoic acid. ( a , b ) show cell viability of MCF-7 ( a ) and T-47D ( b ) normalized to untreated control estimated via MTT assay after 120 h incubation. ( c ) Inhibition of cell viability based on data from ( a , b ): black bars represent the effects of the sum of single treatments, white bars illustrate the effect of the combination treatments. Data shown are mean ± SD of a representative experiment out of a series of 2 experiments, each carried out in triplicates. Statistical analysis was performed using a t-test. Levels of significance: * ( p = 0.0108, 0.0268), ** ( p = 0.0029), *** ( p = 0.0002), **** ( p < 0.0001). Exe = exemestane. ( R )-LA, ( S )-LA, (RS)-LA = ( R )-, ( S )-, and rac -α-lipoic acid. ns = not significant.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Control, MTT Assay, Incubation, Inhibition

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Cell proliferation of MCF-7 cells over 10 days. ( a ) Growth kinetics were analyzed of MCF-7 cells untreated (control) or treated with the respective compounds at the designated time points after staining with calcein AM and Hoechst 33342 using fluorescence microscopy. Data shown are percentage of cells stained by both calcein AM and Hoechst 33342 from 5 microscopic images per treatment and time point of one representative experiment out of a series of at least three experiments. ( b ) Doubling time was calculated for each treatment. Shown is mean and 95% confidence interval. Exe = exemestane. ( R )-LA = ( R )-α-lipoic acid.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Control, Staining, Fluorescence, Microscopy

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Fluorescence microscopic images of MCF-7 on day 2 (upper row) and day 10 (lower row). Shown are representative images from one experiment out of a series of at least 3 experiments. Cells are stained with calcein AM (green) and Hoechst 33342 (blue). Treatment conditions are ( a ) untreated control, ( b ) 1 µM exemestane, ( c ) 1 mM ( R )-α-lipoic acid, ( d ) 1 µM exemestane and 1 mM ( R )-α-lipoic acid. Magnification: 40×. Scale bar is shown in the upper left image and applies to all images.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Fluorescence, Staining, Control

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Cell proliferation of T47D cells over 10 days. ( a ) Growth kinetics were analyzed of T47D cells untreated (control) or treated with the respective compounds at the designated time points after staining with calcein AM and Hoechst 33342 via fluorescence microscopy. Data shown are the percentage of cells stained by both calcein AM and Hoechst 33342 from 5 microscopic images per treatment and time point of one representative experiment out of a series of at least three experiments. ( b ) Doubling time was calculated for each treatment. Shown is the mean and 95% confidence interval. Exe = exemestane. ( R )-LA = ( R )-α-lipoic acid.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Control, Staining, Fluorescence, Microscopy

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Fluorescence microscopic images of T47D on day 2 (upper row) and day 10 (lower row). Shown are representative images from one experiment out of a series of at least 3 experiments. Cells are stained with calcein AM (green) and Hoechst 33342 (blue). Treatment conditions are ( a ) untreated control, ( b ) 1 µM exemestane, ( c ) 1 mM ( R )-α-lipoic acid, ( d ) 1 µM exemestane and 1 mM ( R )-α-lipoic acid. Magnification: 40×. Scale bar is shown in the upper left image and applies to all images.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Fluorescence, Staining, Control

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Caspase 3/7-activation by exemestane, ( R )-α-lipoic acid, and their combination. MCF-7 ( a ) and T47D ( b ) cells were incubated with the given compounds for 24 h. Then, caspase 3/7-activation was monitored. A sample of 100 µM cisplatin for 24 h incubation served as positive control. Data shown are mean ± SD, n = 4. Statistical analysis was performed using t-test. Levels of significance: * ( p ≤ 0.04); ** ( p ≤ 0.01). Fluorescence images can be found in (MCF-7) and (T-47D). Exe = exemestane. ( R )-LA = ( R )-α-lipoic acid.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Activation Assay, Incubation, Positive Control, Fluorescence

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Effects of ( R )-α-lipoic acid and exemestane on protein expression levels of apoptosis- and proliferation-related proteins in MCF-7 and T47D cells. Shown are representative immunoblots of survivin, c-myk, BCL-2, p21, FOXO1, BIM, APAF-1, and ß-actin (as loading control) in MCF-7 and T47D cells. Cells were treated for 48 h with the given compounds and concentrations. Uncropped and labeled immunoblots are presented in .

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Expressing, Western Blot, Control, Labeling

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Densitometric analysis of the protein bands of p21 and ß-actin in MCF-7 ( a ) and T47D cells ( b ). Cells were treated 48 h with 1 µM exemestane, 1 mM ( R )-α-lipoic acid, or the combination of both. Analysis was performed using ImageJ software version 1.54g/Java 1.8.0_345 (NIH, Bethesda, MD, USA). Data are mean ± SD, n = 3. All values have been normalized to MCF-7 or T-47D control. Statistical analysis was performed using a t-test. Levels of significance: *** ( p = 0.0002); **** ( p ≤ 0.0001). Exe = exemestane. ( R )-LA = ( R )-α-lipoic acid. ns = not significant.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Software, Control

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Kinetics of mitochondrial potential in MCF-7 cells upon treatment with ( R )-α-lipoic acid. Displayed are representative fluorescence images (out of two independent experiments) of untreated control and 1 mM ( R )-α-lipoic acid-treated MCF-7 cells after 2 h, 6 h, 24 h, and 48 h. Positive control with 20 µM CCCP is displayed in the . First column shows brightfield microscope image of cells. Second column shows mitochondrial potential analyzed by TMRE (green) and third column, nuclei stained by Hoechst 33342 (blue). Fourth column: merged mitochondrial potential and nuclei. Magnification: 40×. Scale bar is shown in lower left image and applies to all images. ( R )-LA = ( R )-α-lipoic acid.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Fluorescence, Control, Positive Control, Microscopy, Staining

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Docking scores of ( R )-α-lipoic acid (( R )-α-LA), ( S )-α-lipoic acid (( S )-α-LA), ( R )-dihydro-lipoic acid (( R )-DHA), and ( S )-dihydro-lipoic acid (( S )-DHA). The HYBRID Chemgauss4 scores for the fully deprotonated molecules are shown. The differences between R- and S-forms are marginal, for either the oxidized or reduced forms.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques:

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Predicted binding poses of ( A ) ( R )- and ( B ) ( S )-α-lipoic acid. The best docking pose of each structure (blue) out of 100 docking poses in human HDAC 6 (dark pink) is shown. Residues in close vicinity to the bound α-lipoic acid are shown as sticks. The grey sphere indicates the zinc ion, the magenta sphere, the potassium ion.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Binding Assay

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: HDAC inhibitory activity of ( R )-, ( S )- and rac -α-lipoic acid and the reduced racemic form rac -dihydro-lipoic acid from our group versus Lechner et al. [ 21 ] at HDAC2, 6, and 8. Shown are IC 50 values [µM]. Our data are taken from Table 1 , which also contains reference HDACi controls. IC 50 values from Lechner et al. were obtained by fitting their source data to a sigmoidal concentration–effect model. n.e. = no effect.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Activity Assay, Concentration Assay

Journal: International Journal of Molecular Sciences

Article Title: The Antioxidant and HDAC-Inhibitor α-Lipoic Acid Is Synergistic with Exemestane in Estrogen Receptor-Positive Breast Cancer Cells

doi: 10.3390/ijms25158455

Figure Lengend Snippet: Mechanistic effects of the combination treatment of exemestane and α-lipoic acid in ER-positive breast cancer cells. Illustrated are the structures of exemestane and α-lipoic acid including its intracellular reduction to dihydro-lipoic acid with their effects on mitochondria and cell proliferation/survival, eventually leading to synergistic activation of apoptosis and cell death.

Article Snippet: The enantiomer ( S )-α-lipoic acid (CAS 1077-27-6), the racemic mixture rac -α-lipoic acid (CAS 1077-28-7), and ras -dihydro-lipoic acid (CAS 462-20-4) were purchased by Biosynth (Biosynth s.r.o., Bratislava, Slovakia).

Techniques: Activation Assay