Analysis and Identification of Chemical Constituents of Citri Sarcodactylis Fructus by UPLC-Q-Orbitrap HRMS / 中国实验方剂学杂志

Objective::To analyze and identify the chemical constituents of Citri Sarcodactylis Fructus by an ultra-high performance liquid chromatography coupled with hybrid quadrupole-orbitrap high-resolution mass spectrometry (UPLC-Q-Orbirap HRMS) method. Method::Compounds were separated on Thermo Scientific Accucore™ C18 column (3 mm×100 mm, 2.6 μm). The mobile phase was 0.1% formic acid solution and 0.1% formic acetonitrile solution. The flow rate was 0.3 mL·min-1, and the column temperature was set at 30 ℃. HRMS was performed using an electrospray ion source (ESI), and scanned in a positive ion mode by means of full scan/data dependent secondary scan (Full MS/dd-MS2). Compound Discoverer 3.0 software that could be linked to mzCloud network database and local high-resolution mass spectrometry database of traditional Chinese medicine components was used to analyze the data, based on accurate molecular mass, retention behaviors and characteristic ion fragmentation of the compounds, as well as literature information and relevant reference materials. Result::Totally 54 chemical constituents in Citri Sarcodactylis Fructus were identified, including 16 flavonoids, 17 coumarins, 3 limonoids, 6 nucleosides and nucleobases, 2 organic acids, 3 aromatic aldehydes, 1 amino acid and 6 other components. Conclusion::The established UPLC-Q-Orbitrap HRMS method can be used to effectively and rapidly identify main chemical constituents of Citri Sarcodactylis Fructus. The findings provide a methodological reference and theoretical foundation for defining the pharmacodynamic material base and optimizing quality control index of Citri Sarcodactylis Fructus, which is of guiding significance for further development and utilization of the resources.

Design, synthesis and antifungal activity evaluation of coumarin-3-carboxamide derivatives.

A series of coumarin-3-carboxamides/hydrazides have been designed and synthesized, all the target compounds were evaluated in vitro for their antifungal activity against Botrytis cinerea, Alternaria solani, Gibberella zeae, Rhizoctorzia solani, Cucumber anthrax and Alternaria leaf spot, some of the designed compounds 4a-4g exhibited potential activity in the primary assays, this highlighted by the compounds 4a, 4d, 4e and 4f, EC50 values of which against Rhizoctorzia solani were as low as 1.80 µg/mL, 2.50 µg/mL, 2.25 µg/mL and 2.10 µg/mL, respectively, exhibiting more effective control with that of the positive control than Boscalid. Furthermore, compounds 4a and 4e represented equivalent antifungal activity with Boscalid against Botrytis cinerea.

Novel bis-cyclic guanidines as potent membrane-active antibacterial agents with therapeutic potential.

We designed a class of small dimeric cyclic guanidine derivatives which display potent antibacterial activity against both multidrug-resistant Gram-negative and Gram-positive bacteria. They could compromise bacterial membranes without developing resistance, inhibit biofilms formed by E. coli, and exhibit excellent in vivo activity in the MRSA-infected thigh burden mouse model.

Exploration and Discussion on Mechanisms of Different Proportional Compatibility ofBai-Zhu Fu-Ling Decoction Interfering Spleen-QiDeficiency Crohn's Disease by Intestinal Nerve-immune Network / 世界科学技术-中医药现代化

s: The onset of Crohn’s disease (CD) is the interaction of environment, heredity, infection, immune and other factors. It is also closely related to abnormal immune functions. Without special treatment, CD is identified as a modern refractory disease. By syndrome differentiation and treatment, traditional Chinese medicine (TCM) can effectively relieve disease conditions, improve the quality of life and reduce side effects of modern medication. The core compatibility ofBai-Zhu andFu-Ling can reinforce spleen-qi and dispel dampness, which met the common pathogenesis of CD. Therefore, the combination is comprehensively used in the compound prescription. Our previous study found thatBai-Zhu Fu-Ling decoctioncan reduce the vasoactive intestinal peptide (VIP) of animal model of spleen-qi deficiency, downregulate VIP receptors, decrease the affinity of VIP receptors and improve animal model’s sIgA. To further clarify the effects about neurotransmitters and their correlation with the immune system in the pathogenesis of CD and the intervention mechanism treated by different proportional compatibility ofBai-Zhu Fu-Ling decoction, we studied influences of the decoction on related transmitters of nerve- immune network and functions of receptors, as well as cytokine secretion and signal transduction of TLR4-NF-κB. Our studies can provide references and foundations to further explore TCM treatment of CD.

Oxymatrine protects against myocardial injury via inhibition of JAK2/STAT3 signaling in rat septic shock.

Oxymatrine (OMT), an alkaloid extracted from Sophora japonica (kushen), is used to treat inflammatory diseases and various types of cancer in traditional Chinese medicine. However, the cellular and molecular mechanisms underlying the anti­inflammatory activity of OMT remain poorly understood. The present study explored the protective effect of OMT on myocardial injury in rats with septic shock by inhibiting the activation of the janus kinase­signal transducer and activator of transcription (JAK/STAT) signaling pathway. OMT treatment was found to significantly inhibit the activation of JAK2 and STAT3 in myocardial tissue. It also attenuated the expression of pro­inflammatory cytokines, including interleukin­1ß and tumor necrosis factor­α. In addition, OMT exhibited anti­inflammatory properties as heart function and myocardial contractility was improved and pathological and ultrastructural injury was prevented in myocardial tissue induced by septic shock. The results indicate that OMT exhibits substantial therapeutic potential for the treatment of septic shock­induced myocardial injury through inhibition of the JAK2/STAT3 signaling pathway.