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INTRODUCTION: To investigate the inhibition properties and structure-activity relationship between monoamine oxidase (MAO) and selected monoamine oxidase inhibitors (MAOIs, including selegiline, rasagiline and clorgiline). METHODS: The inhibition effect and molecular mechanism between MAO and MAOIs were identified via the half maximal inhibitory concentration (IC50) and molecular docking technology. RESULTS: It was indicated that selegiline and rasagiline were MAO B inhibitors, but clorgiline was MAO-A inhibitor based on the selectivity index (SI) of MAOIs (0.000264, 0.0197 and 14607.143 for selegiline, rasagiline and clorgiline, respectively). The high-frequency amino acid residues of the MAOIs and MAO were Ser24, Arg51, Tyr69 and Tyr407 for MAO-A and Arg42 and Tyr435 for MAO B. The MAOIs and MAO A/B pharmacophores included the aromatic core, hydrogen bond acceptor, hydrogen bond donor-acceptor and hydrophobic core. CONCLUSION: This study shows the inhibition effect and molecular mechanism between MAO and MAOIs and provides valuable findings on the design and treatment of Alzheimer's and Parkinson's diseases.
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ObjectiveIn order to understand the quality differences between wild and cultivated Bupleurum chinense(BC), modern analytical techniques were used to systematically compare the quality of wild and cultivated BC in terms of appearance characteristics, primary and secondary metabolites. MethodSamples of wild and cultivated BC were collected from the main production areas of Shanxi, Shaanxi and Hebei, and images of BC were collected and their length and diameter were measured using vernier caliper to compare and analyze the characteristics of the two. Referring to the method under extract of CP in the 2020 edition of Chinese Pharmacopoeia, the extract contents of the two species were determined. The cellulose, hemicellulose and lignin compositions of both were determined using fiber analyzer. Quantitative determination of representative saikosaponins, flavonoids and saccharides in BC by ultra performance liquid chromatography(UPLC), headspace gas chromatography-mass spectrometry(HS-GC-MS) was used to determine the types and relative contents of volatile components, and UPLC-quadrupole-time-of-flight mass spectrometry(UPLC-Q-TOF-MS) coupled with multivariate statistical analysis was used to screen and identify the differential compounds between wild and cultivated BC. ResultThere were significant differences in the appearance characteristics between wild and cultivated BC, the wild BC had a large root head, twisted and thick axial root, rough epidermis, and often had a stem base and lateral root with dark color and strong odor. However, the cultivated BC has long and straight taproots, delicate epidermis, few lateral roots, light root color and light smell. In terms of primary and secondary metabolites, the contents of alcohol-soluble extract and lignin of wild BC was significantly higher than those of cultivated BC, while the contents of water soluble extract and quercitrin was higher than those of cultivated BC, but the difference was not significant. The contents of cellulose, five saikosaponins, rutin, narcissoside and isorhamnetin-3-O-glucoside in cultivated BC were significantly higher than those of wild BC, and the total water-soluble polysaccharides, sucrose, hemicellulose and starch of cultivated BC were higher than those of wild BC, but the difference was not significant. The results of HS-GC-MS identification showed that a total of 67 volatile components were identified in wild and cultivated BC, 59 in wild BC and 51 in cultivated BC, with a total of 43 compounds in both, and the screening based on variable importance in the projection(VIP) value>1 revealed that the differential components were mainly concentrated in the aromatic and fatty acid compounds. The results of UPLC-Q-TOF-MS-based non-targeted metabolomics combined with multivariate statistical analysis showed that the two were significantly different in saikosaponins and the differential compounds had higher response values in cultivated BC. ConclusionThere are significant differences in the appearance, primary and secondary metabolite contents between wild and cultivated BC. At present, the quality evaluation system of cultivated BC is not perfect, and this study provides theoretical references for updating and revising the quality evaluation standard of cultivated BC and guiding the production of high-quality BC.
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By reviewing the research history on quality comparison between wild and cultivated Chinese crude drugs, this paper systematically combed the relevant research reports since the 1950s, and summarized and analyzed the results of existing comparative studies, and found that the existing comparative research on the quality of wild and cultivated Chinese crude drugs were mainly focused on several aspects, including characteristics, microstructures, chemical compositions, pharmacodynamic effects, and genetic diversity. Among these, comparative studies of chemical compositions have been the dominant approach, with a particular emphasis on comparing the contents of index components. However, research on pharmacodynamic effects remained relatively limited. Due to various factors such as sample quantity, sample origin, growth period and cultivation methods, the differences in quality between wild and cultivated Chinese crude drugs vary significantly. In general, most wild Chinese crude drugs exhibited higher quality than cultivated products, with significant differences in their characteristics. The contents and proportions of some chemical components underwent noticeable changes, particularly with a marked increase in the proportion of primary metabolites after cultivation. The quality of cultivated Chinese crude drugs is closely related to the cultivation practices employed. Chinese crude drugs produced through wild nurturing, simulated wild planting, ecological cultivation, and other similar methods demonstrate quality levels comparable to those of wild Chinese crude drugs. Based on the analysis results, it is recommended to explicitly specify the cultivation practices and cultivation period of cultivated Chinese crude drugs in comparative studies of the quality between wild and cultivated Chinese crude drugs. Multiple technical approaches, including characteristics, microscopy, non-targeted metabolomics combined with quantitative analysis of differential components, and bioefficacy evaluation, should be employed to comprehensively assess the quality disparities between wild and cultivated Chinese crude drugs. Moreover, research efforts should be intensified to investigate the changes in pharmacodynamic effects resulting from differences in plant cell wall composition, primary metabolites, and secondary metabolites, in order to guide the production of high-quality Chinese crude drugs.
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Objective To explore the therapeutic effect of combined endoscopic embelization and variceal ligation (EVL) for management in cirrhotic patients with gastroesophageal variceal bleeding. Meth-otis One hundred and fifty-six cases of active gastric fundal variceal bleeding combined with esophageal var-ices of over degree Ⅱ, and with other causes leading to upper digestive tract bleeding excluded, were ran-domized into therapeutic group (n = 80) and control group (n = 76). For the therapeutic group, endoscopic cyanoacrylate injection for embelization of gastric fundal varices and EVL for esophageal varices were per-formed simultaneously. For the control group, EVL was performed 2 months after embolization. Results There was no complication in beth groups. The rate of hemostasis in therapy group was 96. 3% (77/80), and that in control group was 97. 4% (74/76, P >0.05). There was significant difference between two groups, regarding the rates of early re-bleeding [6. 4% (5/78) vs 21.3% (16/75), P < 0. 05] and re-bleeding at 6 months [13.0% (9/69) vs 25. 4% (17/67), P < 0. 05]. There was no significant difference between two groups, regarding the effective rate in disappearance of gastric fundus varices (61.6% vs 59. 1%), and in that of esophageal varices (74. 0% vs 67.9%). Conclusion Endescopic embelisation of gastric fundus vaxices, combined with EVL for esophageal varices, is a safe and effective procedure for the treatment of gastroesophageal variceal bleeding, and it can reduce the rate of re- bleeding.
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The force of hospital culture is a kind of flexible spiritual productivity.First,it can improve in a comprehensive way the quality of a team and the ideological level of all the employees,make the cultural content permeate the various layers within the organizational framework,and ensure that the employees fulfill quality and quantity requirements in completing their tasks.Second,it can impel people to have a sense of identification,mission and pride concerning the hospital's overall objectives,increase the initiative of both individuals and the organization,and result in the exercise of self-control and self-management on the basis of mechanisms and ideology.Third,it can create a life-learning environment for the employees,raise their awareness of and capability for innovation and the hospital's mechanisms for innovation,and bring about enduring spiritual support to the core values of the hospital.Finally,it can make patients associate the hospital with a unique image of service,create a unique culture of service,and increase patients' trust in the hospital.
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Objective To evaluate gastric varices embolization by endoscopic ultrasonography (EUS). Methods One hundred and eighty-five hepatic cirrhosis patients complicated with gastric varices were divided into two groups, the EUS group, 109 patients and the control group, 76 patients. Ninty-nine patients with confirmed gastric varices by EUS in the EUS group were treated by Histoacryl. All of the patients were examined by EUS soon after the embolization and at three months later. While 76 cases confirmed by endoscopy in the control group were treated by Histoacryl who only examined by EUS three months later. Results The rate of hemostasic both were 100% and rebleeding never occurred within three weeks in EUS group while the rate of the early rebleeding in the control group was 11. 8% (9/76). There was significant difference between the two groups (P