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In-vitro screening method for antineoplastic activity of artemisinin and derivatives of artemisinin

A technology for anti-tumor activity and in vitro screening, applied in the field of in vitro screening of anti-tumor activity of artemisinin and its derivatives, can solve the problems of high cost and long time, and achieve the effects of low cost, short time and simple operation.

Inactive Publication Date: 2015-09-09
NANJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the anti-tumor activity screening of artemisinin and its derivatives mainly adopts the direct in vivo and in vitro anti-tumor activity comparison method, which has the advantage of being direct and accurate, but it is costly and time-consuming

Method used

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  • In-vitro screening method for antineoplastic activity of artemisinin and derivatives of artemisinin
  • In-vitro screening method for antineoplastic activity of artemisinin and derivatives of artemisinin
  • In-vitro screening method for antineoplastic activity of artemisinin and derivatives of artemisinin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] In the concentration range of 1.0×10 -6 ~1×10 -4 Configure transferrin solution in mol / L, fix the concentration of transferrin, add artemisinin, dihydroartemisinin and 9-OH artemisinin respectively, in the concentration range of 1.0×10 -6 ~1×10 -3 Gradually increase the concentration of artemisinin, dihydroartemisinin (DHA) and 9-OH artemisinin (9-OH QHS) in the solution within mol / L, and scan at 298K and 310K with an excitation wavelength of 280nm. The fluorescence emission spectrum of the system is shown in Figure 1.

[0029] The binding constant K can be calculated from the following equation b And the number of binding sites n

[0030] log[(F 0 -F) / F]=log K b +n log[Q]

[0031] Where: F 0 And F respectively represent the fluorescence intensity of transferrin in the absence and presence of the quencher; [Q] is the concentration of artemisinin derivatives.

[0032] Linear regression method can be used, artemisinin derivatives quench the fluorescence of transferrin lg[(F 0 -F)...

Embodiment 2

[0039] Example 2 is basically the same as Example 1, but the artemisinin derivative is artemether or ether.

Embodiment 3

[0040] Example 3 is basically the same as Example 1, but the artemisinin derivatives are artesunate, artemisinin carbonate and artemisinin carboxylate.

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Abstract

The invention discloses an in-vitro screening method for antineoplastic activity of artemisinin and derivatives of the artemisinin. The method comprises the following steps: analyzing the interaction between the artemisinin or the derivatives of the artemisinin and transferrin by adopting ultraviolet-visible absorption spectra or fluorescence spectra; calculating the combining factor Kb of the artemisinin or the derivatives of the artemisinin and the transferring; comparing the combining factor Kb of the artemisinin or the derivatives of the artemisinin and the transferring, or sequencing according to the combining factor Kb, and inferring the strength sequence of the antineoplastic activity of the artemisinin or the derivatives of the artemisinin; and verifying screening results by adopting antineoplastic activity tests. According to the method, a spectroscopic method is used for detecting the combining factor Kb of the artemisinin or the derivatives of the artemisinin and the transferring, and the in-vitro screening is carried out on the antineoplastic activity of the artemisinin and the derivatives of the artemisinin according to the sequence of the combining factor Kb. By using the method, the antineoplastic activity of the derivatives of the artemisinin can be fast and effectively judged, the method can be used for providing the base for designed synthesis of artemisinin-based drugs and clinical application of the artemisinin-based drugs, and promoting the application of the artemisinin-based drugs in the antineoplastic field.

Description

Technical field [0001] The invention relates to an in vitro screening method for antitumor drug activity, in particular to an in vitro screening method for antitumor activity based on the strength of the binding ability of artemisinin and its derivatives with transferrin as a judgment basis. Background technique [0002] Artemisinin is a sesquiterpene lactone compound with a unique peroxy bridge structure first isolated from the traditional Chinese medicine-Artemisia annua in my country. Artemisinin and its derivatives such as dihydroartemisinin and artesunate It has high antimalarial activity and good safety, and has been widely used in clinical practice. In recent years, a large number of studies have shown that artemisinin compounds also have a variety of important pharmacological effects such as anti-tumor, anti-virus and immunomodulation. In particular, the anti-tumor effect of artemisinin and its derivatives has attracted increasing attention from researchers. [0003] Beekma...

Claims

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Application Information

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IPC IPC(8): G01N33/50G01N21/31G01N21/64
CPCG01N33/5011G01N21/31G01N21/64
Inventor 周家宏周林魏少华肖梦思袁秀雪
Owner NANJING NORMAL UNIVERSITY
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