Application of curcumin derivative in preparation of drug for treating prostate cancer disease

A technology of curcumin derivatives and prostate cancer, applied in the fields of biology and pharmacy, can solve the problems of low bioavailability and low absorption rate of curcumin, and achieve the effect of good tumor inhibition and good water solubility.

Inactive Publication Date: 2012-09-19
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Curcumin has very low bioavailability due to its low absorption rate, rapid metabolism and rapid clearance mechanism in the body

Method used

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  • Application of curcumin derivative in preparation of drug for treating prostate cancer disease
  • Application of curcumin derivative in preparation of drug for treating prostate cancer disease
  • Application of curcumin derivative in preparation of drug for treating prostate cancer disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Embodiment 1, curcumin and its derivative Ca 37 are to the inhibitory effect of human androgen-independent prostate cancer cell PC-3

[0068] From figure 1 It can be seen that compared with curcumin, the derivative Ca 37 has a shorter carbon chain and one less keto group, two less methoxy groups on the benzene rings on both sides, and the position of the hydroxyl group is also different.

[0069] Human androgen-independent prostate cancer PC-3 treated with (0, 1.25, 2.5, 5, 10 μmol / L) curcumin derivative Ca 37, (0, 10, 20, 40, 60 μmol / L) curcumin After 24 hours, the change of cell viability was detected by MTT method. As can be seen from Figure 2, curcumin derivatives have a concentration-dependent proliferation inhibitory effect on PC-3 cells in a lower concentration range relative to curcumin, and the effective half-inhibitory concentration (IC) of 24 hours is calculated. 50 ) (see Table 1, Ca 374.77±0.19 μmol / L), which is about 1 / 6 of curcumin (33.83±1.83 μmol / L), ...

Embodiment 2

[0070] Embodiment 2, curcumin derivative Ca 37 induces the production capacity function decline of prostate cancer cells

[0071] Mitochondria provide a large amount of energy support for the life activities of cells, and the abnormality of mitochondrial function will lead to the decline of physiological functions of cells. Such as Figure 3a , as shown in 3b, 5, 10 μmol / L curcumin derivative Ca 37 treated PC-3 cells for 12 hours and caused the enzymes (mitochondrial respiratory chain complex enzymes --- I, II, III, IV) associated with ATP generation in the cells And tricarboxylic acid cycle enzyme --- a-ketoglutarate dehydrogenase complex, malate dehydrogenase) activity decreased. Warburg effect has been found in many tumor cells, specifically manifested in the fact that under aerobic conditions, cells mainly rely on glycolysis to produce ATP and other essential growth elements. Aerobic glycolysis terminal regulator enzyme --- lactate dehydrogenase mainly converts pyruvate ...

Embodiment 3

[0072] Embodiment 3, curcumin derivative Ca 37 induced the apoptosis of PC-3 cells

[0073] We believe that the growth inhibition of PC-3 cells induced by curcumin derivatives may be promoted by the induction of apoptosis. Chromatin condensation is a hallmark of apoptosis. Using Hoechst33342 staining, it was found that PC-3 cells showed nuclear condensation after 12 hours of treatment with 5 μmol / L derivatives, while cells treated with 10 μmol / L derivatives showed very significant nuclear condensation, see the results Figure 4a . Mitochondrial apoptosis pathway often involves Bcl-2 family proteins. With the prolongation of treatment time, the anti-apoptotic protein Bcl-2 protein showed a significant down-regulation, while the Bcl-xL protein did not change significantly. Relatively speaking, the pro-apoptotic proteins Bad and Bak both significantly increased the protein expression. see results Figure 4b .

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Abstract

The invention relates to application of a curcumin derivative Ca 37 in preparation of a drug for treating a prostate cancer disease, and relates to the field of biology and pharmacy. The object is to provide a use of the curcumin derivative in treatment of the prostate cancer disease. The application provided by the invention is mainly characterized in that the proliferation of prostate cancer cells PC(Prostate Cancer)-3 which are independent of male hormones is inhibited by the curcumin derivative, and the effect is obviously better than that of curcumin itself, the decrease of the capacity function of the PC-3 cells, i.e., oxygen glycolysis and oxidative phosphorylation, apoptosis starting and autophagy defects are induced, and the growth inhibition function mainly depends on the generation of reactive oxygen species.

Description

technical field [0001] The invention relates to the fields of biology and pharmacy, in particular to the application of curcumin derivatives in the preparation of drugs for treating prostate cancer. Background technique [0002] Based on the global statistical data in 2008, it can be clearly seen that the incidence and mortality of tumors in Western countries (Western Europe, North America) are much higher than those in Eastern countries (East Asia). According to the statistics of the Cancer Society of the United States in 2010, among the new tumor cases, prostate cancer is as high as 28%; among the expected deaths, it also reaches 11%, and the difference in eating habits between the East and the West has deeply affected this process. Through the change of dietary habits, intake of more vegetables and fruits rich in antioxidants may effectively reduce the incidence and mortality of tumors, and at the same time have relatively low negative effects, which indicates that good ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/12A61P35/00A61P13/08
Inventor 刘健康罗成周波
Owner XI AN JIAOTONG UNIV
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