| The effective ingredients of traditional Chinese medicine on the organic component have been studied for a long time, and the inorganic part has been ignored. In some cases, the effective components of Chinese herbs have been clarified clearly, but its pharmacological action has not been perfectly illustrated. For example, the soluble components in Chinese materia medica Decoction with single drug have significant biological activity. However when researchers continue to extract them with improvement of purity, their pharmacological activity are decreased. During the refining process of Chinese Herbs, the inorganic components run off, since the inorganic components are thought to be invalid, they are always abandoned. But most of them are trace elements, which play a fundamental role in the pharmacological activity. So the discard of the inorganic components leads to the decrease and even the loss of pharmacological activity and affects the efficacy at the same time. Studies have found that, in the traditional Chinese medicine preparation process, the metal ion with traditional Chinese medicine ingredients such as anthraquinone, flavone, alkaloid formed complexes in the boiling process, and the metal complexes are an existing form in the raw material of compound. Metal ions and chemical constituents forming the complexes tend to change or enhance its activity, such as antimicrobial, antitumor, antioxidant etc. The effective components in Chinese medicine and metal ion coordination to play the role of both, is the effective way to improve the activity of chemical components of traditional Chinese medicine.This study focuses on anthraquinones in rhubarb (Emodin, Aloe emodin). Based on the types and contents of trace metal elements in Rheum offcinale Baillon,18emodin and aloe emodin metal complexes have been synthesized. Using UV, IR and NMR to indicate the structural characterizations of them and then make a contrast research on the structure and biological activities of Emodin, Aloe emodin and various complexes. And this research achieves the following significant results.(1) Using inductively coupled plasma atomic emission spectrometry (ICP-OES) to measure the content of Ca, Mg, Cu, Mn, Fe, Zn, Co and Cr elements in medical rhubarb at the same time. The result shows that there is Ca, Mg, Cu, Mn, Fe, Zn, Co and Cr elements in it; the contents of Ca, Mg reach a record high of27880μg/g and2250μg/g,respectively; while the lowest content of trace elements is Cu,5.1μg/g.(2)Choose Emodin and Aloe emodin as ligand, and then combine them with Ca (II), Mg (Ⅱ), Cu(Ⅱ), Fe(Ⅱ), Mn(Ⅱ),Fe(Ⅲ), Zn(Ⅱ),Co(Ⅱ), Cr(Ⅲ) to synthesize18metal complexes. Ca (Ⅱ),Mg(Ⅱ),Fe(Ⅱ),Mn(Ⅱ),Fe(Ⅲ), Co(Ⅱ),Cr(Ⅲ) complexes were synthesized for the first time. Through the ultraviolet spectrum, infrared spectrum, nuclear magnetic resonance spectra, differential thermal analysis, content of metal ion detection and other modern analysis methods to analyze possible structures of these complexes. The results show that the8phenolic of hydroxyl emodin and aloe emodin molecule looses its proton and combines with9oxygen atoms and metal ions to synthetize complexes. Only the ratio of Calcium complexes and its ligand is1:1, while the proportion of other metal complexes and their ligands is1:2.(3) Make a research on the antioxidant activity of Emodin, Aloe emodin and its metal complexes. Using two generation of benzene bitter hydrazine free radical (DPPH method), nitro blue tetrazolium method (NBT method), Fe2+-H2O2-methylene blue method for its antioxidant activity were studied. The scavenging rate of three kinds of free radical (DPPH, O2-·,·OH) was studyed on ligand and18complexes. Comparison of the ligands and metal complexes between antioxidant activity, results show that in the experiment range, metal complexes with ligands showed high antioxidant activity, and with the antioxidant activity of compounds were higher than that of the ligand. Show the dependence of antioxidant activity and the dose of the ligands and complexes, in the range of experiment, antioxidant activity increased with increasing concentration of the compound.(4) Emodin, Aloe emodin and its metal complexes were studied on antimicrobial activity. Investigated inhibition activity against Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli and18kinds of metal ligand with qualitative and quantitative experiments. The experimental results show that:in the experimental range, metal complexes and ligands have antibacterial activity, and most metal complexes with antibacterial activity were higher than that of the ligand.(5) Emodin, Aloe emodin and its metal complexes were studied the antitumor activity. Using the method of MTT, the ligand of emodin, aloe emodin and18metal complexes on liver cancer HepG2cell lines were screened in vitro cytotoxicity.The proliferation inhibition rate of the ligand and the complexes on human hepatocellular carcinoma HepG2cells was measured, and the half effective concentration (IC50value) of active compounds was measured. The experimental results show that the metal complexes and ligands have antitumor activity, and the antitumor activity of the complexes is higher than that of the ligand.The results of this study provide a train of thought, method and experimental data for the further study of traditional Chinese medicine in the field of coordination chemistry of traditional Chinese medicine theory, provides a valuable reference for anthraquinone metal with the reasonable and effective, to reveal the relationship between the effective chemical components in traditional Chinese medicine and Chinese Medicine, to reveal the essence of traditional Chinese medicine to prevent and cure diseases to provide scientific reference. |
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