Therapeutic effect of ursodeoxycholic acid-berberine supramolecular nanoparticles on ulcerative colitis based on supramolecular system induced by weak bond / 中国中药杂志

Ulcerative colitis(UC) is a recurrent, intractable inflammatory bowel disease. Coptidis Rhizoma and Bovis Calculus, serving as heat-clearing and toxin-removing drugs, have long been used in the treatment of UC. Berberine(BBR) and ursodeoxycholic acid(UDCA), the main active components of Coptidis Rhizoma and Bovis Calculus, respectively, were employed to obtain UDCA-BBR supramolecular nanoparticles by stimulated co-decocting process for enhancing the therapeutic effect on UC. As revealed by the characterization of supramolecular nanoparticles by field emission scanning electron microscopy(FE-SEM) and dynamic light scattering(DLS), the supramolecular nanoparticles were tetrahedral nanoparticles with an average particle size of 180 nm. The molecular structure was described by ultraviolet spectroscopy, fluorescence spectroscopy, infrared spectroscopy, high-resolution mass spectrometry, and hydrogen-nuclear magnetic resonance(H-NMR) spectroscopy. The results showed that the formation of the supramolecular nano-particle was attributed to the mutual electrostatic attraction and hydrophobic interaction between BBR and UDCA. Additionally, supramolecular nanoparticles were also characterized by sustained release and pH sensitivity. The acute UC model was induced by dextran sulfate sodium(DSS) in mice. It was found that supramolecular nanoparticles could effectively improve body mass reduction and colon shortening in mice with UC(P<0.001) and decrease disease activity index(DAI)(P<0.01). There were statistically significant differences between the supramolecular nanoparticles group and the mechanical mixture group(P<0.001, P<0.05). Enzyme-linked immunosorbent assay(ELISA) was used to detect the serum levels of tumor necrosis factor-α(TNF-α) and interleukin-6(IL-6), and the results showed that supramolecular nanoparticles could reduce serum TNF-α and IL-6 levels(P<0.001) and exhibited an obvious difference with the mechanical mixture group(P<0.01, P<0.05). Flow cytometry indicated that supramolecular nanoparticles could reduce the recruitment of neutrophils in the lamina propria of the colon(P<0.05), which was significantly different from the mechanical mixture group(P<0.05). These findings suggested that as compared with the mechanical mixture, the supramolecular nanoparticles could effectively improve the symptoms of acute UC in mice. The study provides a new research idea for the poor absorption of small molecules and the unsatisfactory therapeutic effect of traditional Chinese medicine and lays a foundation for the research on the nano-drug delivery system of traditional Chinese medicine.

Study on the substance basis of "property-taste-efficacy" of Liquorice and Rhizoma chinensis based on supramolecular system induced by weak bond / 药学学报

It is a common understanding that turbidity and precipitation of traditional Chinese medicine are easy to occur in the process of decocting. At present, our research group found that the cause of "multi-phase of traditional Chinese medicine decoction" mainly came from the interaction between the effective components of traditional Chinese medicine, especially the interaction of acid and base components. For example, the Liquorice and Rhizoma chinensis was a supramolecular system formed by a large number of active components in the decoction (>30%), and could stably exist in the decoction system. In this study, the supramolecular part was extracted, and the morphology of the supramolecular part was characterized by scanning electron microscopy and dynamic light scattering. It was observed that the supramolecular particles were uniform in size and regular in shape. The main components of supramolecular sites were identified by liquid mass spectrometry (LC-MSn). The results of UV and IR spectra showed that the chemical components of Liquorice and Rhizoma chinensis in the co-decocting process collided with each other, and weak bonds were formed between the functional groups of the molecules, which then induced the aggregation to form supramolecules. Thereafter, Through the diarrhea model of mice, sensory evaluation and antibacterial activity evaluation found that Liquorice and Rhizoma chinensis decocted together enhanced the antibacterial activity of Rhizoma, and compatibility "reconcile" Rhizoma "big bitter cold" property compared with single decoction group and interval administration group. All animal experiments were approved by the Animal Ethics Committee of Beijing University of Chinese Medicine, and the relevant regulations of Beijing University of Chinese Medicine on experimental animals were strictly followed. In this study, supramolecular chemistry method was used to preliminarily discuss the scientific connotation of "increasing efficiency and decreasing toxicity" of Liquorice and Rhizoma chinensis combined decoction from three perspectives of "property, efficacy and taste", and provide new ideas for the basic research of "reconcile" compatibility of Liquorice.

Research progress on improvement of functions of small molecular compounds of traditional Chinese medicine based on supramolecular properties of hyaluronic acid / 药学学报

Hyaluronic acid is widely used in biomaterials, cosmetics, clinical medicine and other fields due to its good biocompatibility, degradability, hydrophilicity, tumor targeting, viscosity and other characteristics. Pharmacodynamic activities of natural small molecular products which derived from traditional Chinese medicine (TCM) are significant, but their low solubility and poor targeting limit the clinical application. Based on supramolecular properties of hyaluronic acid, in this review, numerous studies were reviewed on the improvement of solubility, bioavailability, targeting and suitable dosage forms of small molecular compounds in TCM by domestic and foreign scholars using hyaluronic acid as carrier. It provides new ideas and inspirations for exploring the potential application value of small molecule compounds in TCM and even for the research and development of new drugs.

Based on weak bond chemistry, the interaction mechanism between glycyrrhiza protein and berberine in water decocting process of Rhizoma Coptidis and Liquorice was investigated / 药学学报

The purpose of this study was to explore the interaction mechanism between glycyrrhiza protein and berberine in the decocting process of Rhizoma Coptidis and Liquorice and its effect on the pharmacodynamic effect. In this experiment, licorice crude protein was obtained from licorice decoction pieces, and it was found that licorice crude protein and berberine could form spherical supramolecular particles after decocting together. Morphological characterization was carried out by using Malvin particle size analyzer and emission scanning electron microscopy, and the supramolecular particles were observed to be nanoscale, which was significantly different from the morphology of licorice protein and berberine. The results of ultraviolet, infrared and fluorescence spectroscopy showed that the mechanism of molecular interaction was induced by weak bonds such as electrostatic attraction and hydrophobic interaction. Furthermore, the antimicrobial activity of berberine was significantly affected by the supramolecular particles of licorice protein-berberine, which were significantly different from the mechanical mixture. This study reveals the pharmacological value of macromolecular substances such as proteins in the decoction of licorice and Coptis chinensis from a new perspective, which is helpful to promote the secondary development of clinical effective prescriptions, especially the research on the pharmacological substance basis of classic famous prescriptions.

The mechanism of toxicity enhancement with the combination of Flos Genkwa and Radix et Rhizoma Glycyrrhizae based on the solubilization of glycyrrhizic acid / 药学学报

In order to study the contraindications of the compatibility of Flos Genkwa-Radix et Rhizoma Glycyrrhizae, in this study, the solubilizing and poisoning essence were explored. In this experiment, chromatographic assay, field emission scanning electron microscopy, MTT cytotoxicity evaluation, and other methods were used to study the main chemical components, morphology and toxicity of the ethyl acetate part of Flos Genkwa and its co-decoction with glycyrrhizic acid, in order to clarify Flos Genkwa-Radix et Rhizoma Glycyrrhizae incompatibility provides a new idea for the research on incompatibility of Flos Genkwa-Radix et Rhizoma Glycyrrhizae. The results showed that after co-decoction of the ethyl acetate part of Flos Genkwa with glycyrrhizic acid, high performance liquid chromatography (HPLC) detected the dissolution of the toxic component yuanhuacine of 54.8%, while yuanhuacine chromatographic peak was not detected in the Flos Genkwa ethyl acetate part of the single decoction. The increase of co-decoction dissolution rate was observed by scanning electron microscopy, and it was found that glycyrrhizic acid uniformly dispersed the fat-soluble components of Flos Genkwa into nano-scale particles, which improved the solubility and stability in the solution. Furthermore, the results of cytotoxicity evaluation showed that the survival rate of cells decreased after co-decoction, 4',6-diamidino-2-phenylindole (DAPI) staining also gave the same results. In summary, the co-decoction of the ethyl acetate part of Flos Genkwa with glycyrrhizic acid promotes the dissolution of the toxic component yuanhuacine, and makes the part form uniformly distributed nanoparticles, which is conducive to the absorption of the ingredient and increases the toxicity.

Malaria focus investigation and disposal in Tengchong City between 2015 and 2016 / 中国血吸虫病防治杂志

Objective To analyze the results of malaria focus investigation and disposal in Tengchong City,Yunnan Prov-ince between 2015 and 2016,so as to provide evidences for interrupting potential malaria transmission. Methods The malaria foci were investigated and disposed according to the malaria cases reported from"China Information System for Disease Control and Prevention"in Tengchong City between 2015 and 2016. The mosquitoes were captured by mosquito-lured lamp overnight to investigate the malaria vector in local. The peripheral blood samples were collected from the local residents with a febrile history in the foci within two weeks and the accompanists of the cases,and then the rapid malaria diagnosis tests were used to screen the malaria carriers. Results Totally 145 imported malaria cases were reported in Tengchong City between 2015 and 2016,and the focus investigation and disposal rate within 7 d was 100%(145/145). A total of 16186 mosquitoes of 12 species of Anopheles were captured,among which An. sinensis was the predominant,accounting for 64.31%(10410/16186),followed by An. kun-mingensis and An. minimus,with the constituent ratios of 14.15%(2291/16186)and 11.66%(1887/16186),respectively. One person(1.96%,1/51)in the 51 accompanists of the cases was positive in the malaria rapid diagnosis test. Conclusions The malaria transmission vectors such as An. sinensis,An. kunmingensis,An. minimus etc. are still distributed in Tengchong City,and An. sinensis is the predominant species. Therefore,the relevant authorities should continue to strengthen the focus in-vestigation and disposal to interrupt the potential introduced malaria transmission by imported cases in the future.

Alterations of SP-A, SP-D and KL-6 in serum and bronchoalveolar lavage fluid in children with Mycoplasma pneumoniae pneumonia / 中华儿科杂志

<p><b>OBJECTIVE</b>To study the alterations and relationship of surfactant protein (SP)-A, SP-D and KL-6 in serum and bronchoalveolar lavage fluids (BALF) in children with Mycoplasma pneumoniae pneumonia (MPP).</p><p><b>METHOD</b>Self-control method was used for the study on SP-A, SP-D and KL-6 in serum, infected and non-infected BALFs in 32 MMP children with only one side of MPP.</p><p><b>RESULT</b>The contents of SP-A, SP-D and KL-6 in infected BALF were [mg/L;M (IQR) ]: 243 (90-468) , 187 (43-333) , 148 (47-426) ;104 (37-257) , 56 (25-131) , 35 (12-147) in non-infected BALF; 35 (25-69) , 33 (9-149) and 24 (15-62) in serum. The correlation coefficient of KL-6 between serum and infected BALF were -0.534 and -0.378 (P < 0.05).</p><p><b>CONCLUSION</b>There were significant correlation between the alterations of SP-A, SP-D and KL-6 in serum and lung infection in children with CAP. KL-6 in serum may be more sensitive than SP-A and SP-D.</p>