Blood Root Base, Baicalin, Celandine Red Alkaline, Baicalin Ion Activity Of Compound Preparation Technology And Research

In recent years, due to bacterial resistance to various types antibiotics showed rapid upward trend, the development of new antibacterial and anti-inflammatory drugs is becoming an important issue of the medical profession.Sanguinarine/chelerythrine, which the main components of Macleaya cordata, and Baicalin, the main components of Radix scutellariae, both have antibiotic, anti-inflammation and other aspects of the pharmacological action. Our study make a single compound by using intermolecular electrostatic attraction of C=N+ionic bond from sanguinarine/chelerythrine and COO-from baicalin. We name the compound as the sanguinarine-baicalin ion-pair-compound, and the chelerythrine-baicalin ion-pair-compound respectively. The antibacterial activity and acute toxicity of the two ion-pair-compounds were also studied.1. The preparation study of sanguinarine-baicalin ion-pair-compounWe use the single factor exploration and orthogonal experiments to determine the optimum preparation process of sanguinarine-baicalin ion-pair-compound. The optimum conditions were as follows:the molar ratio of the sanguinarine hydrochloride to baicalin was1:1, and pH value of baicalin is5.5, after reaction time of1.5h at temperature90℃, the molar ratio of sanguinarine to baicalin were close to1in ion-pair-compound after HPLC detection under the condition of ensuring higher yields.2. Structural elucidation of sanguinarine-baicalin ion-pair-compound and chelerythrine-baicalin ion pair compoundTwo strong peaks of ion-pair-compound which measured by IR are corresponding to the strong peaks of two alkaloids. There is no absorption of carboxyl groups in peak1727cm-1of ion pair compound, and there is no telescopic and symmetric stretching absorption appeared in the ion-pair-compound, which shows that the carboxyl from baicalin can form ion pair compound with sanguinarine or chelerythrine.The profile comparison of1H-NMR,13C-NMR of these two kinds of ion pair compound to those of alkaloids and baicalin are made. All Hydrogen produce very big chemical shifts and splitting except littler chemical shifts of C6-H in alkaloids and C3-H, C8-H and C5-OH and hydrogen on hydroxyl carbon of glucuronic acid hydroxyl group in Baicalin Ion-pair-compound. The results show that the alkaloids and baicalin in ion-pair-compound are quite closed to each other and show shield and shielding effect eliminate with each other due to the electrostatic attraction. This part can be freely rotated are fixed up due to the steric, hydrogen nuclei which chemical and magnetically identical were changed into different. NMR of the ion-pair-compound can not be superimposed by NMR of chelerythrine and baicalin, all which caused the complex of the NMR profile of the ion-pair-compound.EI-MS analysis of two kinds of ion-pair-compound shows that, m/z value of cationic and anion molecular ion peaks of this two ion-pair-compound are equal to the calculation values. The spectral analysis also shows that the structures of two ion-pair-compound are as follows:3. In vitro antibacterial activity study on two ion-pair-compoundsThe minimum inhibitory concentration(MIC) and minimal bactericidal concentration(MBC) of two ion pair compound are being tested on Escherichia Coli, Staphylococcus aureus, chicken Staphylococcus, and Salmonella, within two methods of test tube dilution and agar diffusion. The results show that:the MIC and MBC values of two ion-pair-compounds group are both lower than that of the alkaloid and Baicalin group.4. Acute toxicity study on two ion-pair-compoundsThe test data shows that, the toxicity of both two on-pair-compounds are smaller than that of sanguinarine and chelerythrine.