Interaction of Antimalarial Components Combination from Artemisia annua L. with Bovine Serum Albumin†

doi:10.7503/cjcu20130748

Abstract

Abstract:

The interaction of arteannuin, arteannuic acid and scopoletin on the binding of artemisinin with bovine serum albumin(BSA) was investgated by fluorescent spectrometry. BSA fluorescence quenching effect was strengthened after the interaction of BSA with antimalarial components combination[AAAS, m(artemisinin)∶m(arteannuin B)∶m(arteannuic acid)∶m(scopoletin)=1∶1∶1∶1] from Artemisia annua L. compared to that of BSA with artemisinin alone, and the fluorescence quenching effect was staitc quenching. The binding constant, binding point numbers and thermodynamic parameters at three temperature levels, for example, 298, 303 and 310 K were calculated, and the results revealed that the binding of AAAS with BSA had strong electrostatic attraction and the process was a spontaneous molecular interaction procedure in which entropy was increased. Compared with artemisinin, the quenching constants and the binding constant of AAAS with BSA were also increased. These results confirmed that arteannuin, arteannuic acid and scopoletin could significantly increased the binding of artemisinin with BSA, and the interaction of AAAS with BSA might be a key factor that improved the antimalarial efficacy of artemisinin in vivo.

Key words: Artemisinin, Antimalarial components combination, Bovine serum albumin, Fluorescence spectrum, Drug interaction

CLC Number:

TrendMD:

WANG Manyuan, ZHANG Chao, LI Jing, LI Zhaoxia, GONG Muxin. Interaction of Antimalarial Components Combination from Artemisia annua L. with Bovine Serum Albumin^†[J]. Chem. J. Chinese Universities, 2014, 35(2): 309.

Figures/Tables 4

References 17

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System	10^-12K_q/(L·mol^-1·s^-1)			10^-4K_sv/(L·mol^-1)			r
System	298 K	303 K	310 K	298 K	303 K	310 K	298 K	303 K	310 K
ART-BSA	4.35	3.17	2.52	4.35	3.17	2.52	0.9994	0.9996	0.9995
ARTB-BSA	4.06	1.82	1.29	4.06	1.82	1.29	0.9985	0.9986	0.9986
ARTC-BSA	2.46	1.55	1.22	2.46	1.55	1.22	0.9987	0.9988	0.9994
SCP-BSA	3.59	2.84	2.62	3.59	2.84	2.62	0.9995	0.9987	0.9990
AAAS-BSA	11.25	9.91	5.82	11.25	9.91	5.82	0.9984	0.9995	0.9993

System	10^-12K_q/(L·mol^-1·s^-1)			10^-4K_sv/(L·mol^-1)			r
System	298 K	303 K	310 K	298 K	303 K	310 K	298 K	303 K	310 K
ART-BSA	4.35	3.17	2.52	4.35	3.17	2.52	0.9994	0.9996	0.9995
ARTB-BSA	4.06	1.82	1.29	4.06	1.82	1.29	0.9985	0.9986	0.9986
ARTC-BSA	2.46	1.55	1.22	2.46	1.55	1.22	0.9987	0.9988	0.9994
SCP-BSA	3.59	2.84	2.62	3.59	2.84	2.62	0.9995	0.9987	0.9990
AAAS-BSA	11.25	9.91	5.82	11.25	9.91	5.82	0.9984	0.9995	0.9993

System	K/(L·mol^-1)			n						ΔG/(kJ·mol^-1)					ΔH/ (kJ·mol^-1)	ΔS/(J· K^-1·mol^-1)
System	298 K	303 K	310 K	298 K		303 K		310 K		298 K		303 K		310 K
ART-BSA	7.24×10⁴	6.27×10⁴	5.26×10⁴	1.04	1.05		1.06		-27.72		-27.83		-28.02		-20.33	24.78
ARTB-BSA	4.63×10³	1.24×10³	3.97×10²	0.82	0.75		0.70		-20.91		-17.94		-15.42		-155.55	-452.66
ARTC-BSA	3.62×10⁴	2.29×10⁴	1.09×10⁴	1.04	1.04		0.99		-26.01		-25.29		-23.95		-77.30	-171.95
SCP-BSA	1.23×10⁵	1.04×10⁵	8.49×10⁴	1.11	1.12		1.10		-29.03		-29.10		-29.25		-23.54	18.40
AAAS-BSA	1.65×10⁵	1.42×10⁵	1.20×10⁵	1.04	1.03		1.06		-29.76		-29.89		-30.15		-20.11	32.35

System	K/(L·mol^-1)			n						ΔG/(kJ·mol^-1)					ΔH/ (kJ·mol^-1)	ΔS/(J· K^-1·mol^-1)
System	298 K	303 K	310 K	298 K		303 K		310 K		298 K		303 K		310 K
ART-BSA	7.24×10⁴	6.27×10⁴	5.26×10⁴	1.04	1.05		1.06		-27.72		-27.83		-28.02		-20.33	24.78
ARTB-BSA	4.63×10³	1.24×10³	3.97×10²	0.82	0.75		0.70		-20.91		-17.94		-15.42		-155.55	-452.66
ARTC-BSA	3.62×10⁴	2.29×10⁴	1.09×10⁴	1.04	1.04		0.99		-26.01		-25.29		-23.95		-77.30	-171.95
SCP-BSA	1.23×10⁵	1.04×10⁵	8.49×10⁴	1.11	1.12		1.10		-29.03		-29.10		-29.25		-23.54	18.40
AAAS-BSA	1.65×10⁵	1.42×10⁵	1.20×10⁵	1.04	1.03		1.06		-29.76		-29.89		-30.15		-20.11	32.35