| Researches have shown that angiogenesis is positively correlated with the growth and metastasis of malignant tumor. In the recent years, oncologists have been focusing on the study of angiogenesis inhibitors. As a result, more than 35 types of angiogenesis inhibitors have been applied clinically overseas. However, in China, few studies on the angiogenesis inhibitors have been performed, let alone the clinical studies with sole property right of the angiogenesis inhibitors.Turmeric, Radix Curcumae and zedoary, belonging to the turmeric genus, are three kinds of traditional Chinese medicines. The active components of these three plants are curcumin, curcuminoids and volatile oil with the effects of anti-tumor, anti-inflammation and drop of blood-lipid. As to the effect of anti-tumor, oversea studies have been focusing on the studies of curcumin and curcuminoids while Chinese studies on the volatile oil. In addition, new drug of national class has been developed based on the elemene, one of the components of volatile oil, and has stepped into the stage of clinical application. Preliminary studies have shown that the active components of turmeric genus traditional Chinese medicines are of clear effect of anti-angiogenesis.To screen the active component with clear effect of anti-angiogenesis and to perform further studies of the mechanism of anti-angiogenesis, we designed our study based on the following three steps: 1) extracting and separating the main active components from turmeric, Radix Curcumae and zedoary by distillation, ethanol precipitation, column chromatography, etc. 2) analyzing and comparing the inhibitory effects of the active components on humanendothelial cell lines by MTT trial, flow cytometry and electron microscope, etc.Main results:1. The content of curcumin, curcuminoids and volatile oil in turmeric was significantly higher than in Radix Curcumae and zedoary.2. The molecular weight curcumin and two of curcuminiods were in coincidence with the theoretical values, identified by the techniques of mass spectrum.3. Hydrogens of -OH, -CH2- and -OCHs in the molecular structure of curcumin and curcuminoids are active .4. The volatile oils from the three plants of turmeric genus, turmerol extractive substance and the monome of the three turmeric yellows were able to inhibit the growth of endothelial cells. The bioactivity of turmeric volatile oil was remarkably higher than that of Radix Curcumae and zedoary while the bioactivity of the monome of the three turmeric yellows was significantly higher than that of turmerol extractive substance but lower than curcumin-1, curcumin-2 and curcumin-3. The ICso values of inhibitory effect of curcumin-1, curcumin-2 and curcumin-3 on HUVEC growth were 0.525fj.g/ml, 0.399fag/ml and 0.125ug/ml, respectively.5. At the concentration of 4ng/ml, curcumin-1, curcumin-2 and curcumin-3 were able to inhibit effectively the proliferation of endothelial cell at 48 hours post-treatment while the effect reached the peak at 72 hours post-treatment.6. At the concentration of 4(ig/ml, curcumin-3 could effectively retard the endothelial cell at S phase at 24 hours post-treatment. But when the concentration was increased to S^g/ml or more, curcumin-3 could also induce obvious apoptosis of endothelial cell.7. At the concentration of 4(j.g/ml, curcumin-3 could effectively inhibit theproduct of MMP-2 and MMP-9 as well as the mRNA transcription of MMP-1.inConclusions:1. Curcumin-1, curcumin-2 and curcumin-3 may be the main active components of turmeric when used to inhibit angiogenesis in malignant tumor.2. -OH - -OCHs and-CH2-in the molecular constructure of curcumin and curcuminoids are active mass .3. The bioactivity of curcumin-3 is significantly higher than that of curcumin-1 and curcumin-2, respectively.4. Affecting the proliferation cycle of endothelial cell, inducing the apoptosis of endothelial cell and inhibiting the product of MMPs may be the main mechanism of anti-angiogenesis...
|
PDF Full Text Request