Effect of gallic acid on pirarubicin transport kinetics in living leukemic K562 and K562/Dox cell lines

1. EFFECT OF GALLIC ACID ON PIRARUBICIN TRANSPORT KINETICS
IN LIVING LEUKEMIC K562 AND K562/DOX CELL LINES
Presenter :
Miss Khin TheNu Aye
Khin TheNu Aye1,2,3* and Montree Tungjai1,2
1 Department of Radiologic Technology, Faculty of Associated Medical Sciences,
Chiang Mai University, Chiang Mai, Thailand
2 Center of Radiation Research and Medical Imaging, Department of Radiologic Technology,
Faculty of Associated Medical Sciences, Chiang Mai University, Chiang Mai, Thailand
3 Ph.D. degree program in biomedical sciences, Faculty of Associated Medical Sciences, Chiang Mai University,
under the CMU Presidential Scholarship
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2. Introduction
Leukemia : Multidrug Resistant Cancer
Source: Globocan 2020 https://gco.iarc.fr/today/
Cancer Treatment
• Chemotherapy : Pirarubicin
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3. https://www.mdpi.com
Gallic Acid (3,4,5- Trihydroxy benzoic acid)
Introduction
• Antioxidant activity
• Anticancer activity
• Anti-inflammation
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4. Objective
 To investigate effect of gallic acid (GA) on pirarubicin (Pira) transport kinetics
in living leukemic K562 and K562/Dox cell lines
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5. Complete Media
(RPMI 1640 + 10% FBS + Penicillin-Streptomycin 1%)
K562 K562 /DOX
Cell lines and culture media
K562 = Myelogenous leukemia cell line
K562/DOX = Doxorubicin resistant derivative of K562 cell line, P-glycoprotein expression
Cell lines
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6. Kinetic transport of Pirarubicin in K562 and K562/Dox cells
K562 cells K562/Dox cells
Non-invasive Functional Spectrofluorometric Method
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7. F0 : Fluorescence intensity (FI) of Pirarubicin
Fn : FI of steady state before GA
FnGA: FI of steady state after GA
FN : FI of steady state after Triton-X
Kinetic Parameter of Pirarubicin Transportation
Computerized
Calculation
Kinetic parameters such as :
V- : Pirarubicin, passive efflux
V+ : Pirarubicin, passive influx
Va : P-glycoprotein-mediated
Pirarubicin efflux
ki
a /k0
a : the potentiality of GA for
inhibition of P-glycoprotein function
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8. The potentiality of GA for inhibition of P-glycoprotein function;
Where; ki
a = the P-glycoprotein-mediated active efflux of Pira in the presence of GA.
k0
a = the P-glycoprotein-mediated active efflux of Pira in the absence of GA
ki
a /k0
a
1 Not Inhibit
0 Completely inhibit
ki
a /k0
a
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9. Kinetic parameters of Pira transport into K562
GA, µM
K562 cells
V+ , nM.s-1 k+ ×10-12 l.cell-1.s-1 Cn, µM
0 2.2±0.2 2.24±0.21 0.41±0.003
10 1.7±0.1 1.86±0.09 0.41±0.010
50 1.5±0.2* 1.47±0.20* 0.40±0.013
100 1.5±0.1* 1.48±0.06* 0.42±0.013
200 0.9±0.2* 0.94±0.02* 0.42±0.017
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V+ = Pirarubicin passive influx
Cn = intracellular accumulation of Pirarubicin

10. Kinetic parameters of Pira transport into K562/Dox
Higher concentration of Gallic Acid ---> Higher intracellular Pirarubicin Accumulation
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Cn = intracellular accumulation of Pirarubicin

11. Conclusion
Gallic
Acid
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