Improvement effect of arbutin on myocardial fibrosis model rats and its mechanism / 中国药房

OBJECTIVE To study the improvement effects of arbutin on myocardial fibrosis （MF） model rats and its mechanism. METHODS The network pharmacology was used to predict the potential target of arbutin in improving MF and molecular docking was used to validated. Totally 50 SD rats were given isoprenaline subcutaneously （5 mg/kg， once a day， for 14 consecutive days） to induce the MF model. Modeled rats were randomly divided into model group， captopril group （9 mg/kg）， arbutin low-dose， medium-dose and high-dose groups （50， 100， 200 mg/kg）， with 10 rats in each group. Another 10 healthy rats were included as normal group. Each group was given the corresponding drugs， once a day， for 28 consecutive days. Twenty-four hours after the final administration， electrocardiograms and heart-related indexes [heart weight index （HWI）， left ventricular weight index （LVWI）] of rats were detected； the levels of creatine kinase （CK）， lactate dehydrogenase （LDH）， N-terminal pro-brain natriuretic peptide （NT-proBNP） and type Ⅰ collagen （Col Ⅰ） and Col Ⅲ were detected in myocardial tissue of rats； the pathological changes of myocardial tissue were observed， and protein and mRNA expressions of adenosine deaminase （ADA） and adenosine kinase （ADK） were detected in the myocardial tissue of rats. RESULTS The results of network pharmacology showed that the main targets of arbutin improving MF were ADA and ADK. The results of molecular docking showed that arbutin bind stably with ADA and ADK. The results of experimental verification showed that compared with model group， the amplitude of ST and T waves in electrocardiogram were improved in administration groups， and the symptoms of atrial flutter were alleviated； HWI （except for arbutin medium-dose group）， LVWI， the levels of CK， LDH， NT-proBNP， Col Ⅰ and Col Ⅲ in the myocardial tissue of rats were decreased significantly （P＜0.05）； the degree of myocardial fibrosis in rats decreased； protein and mRNA expressions of ADA and ADK in the myocardial tissue were significantly increased （P＜0.05）. CONCLUSIONS Arbutin can improve cardiac fibrosis and cardiac function of MF model rats， the mechanism of which may be associated with up-regulating protein and mRNA expressions of ADA and ADK，influencing the nucleotide metabolism and collagen generation. zhangminghao@hactcm.edu.cn

Q-marker analysis of Kanggongyan soft capsule / 中国药房

OBJECTIVE To analyze quality maker （Q-marker） of Ka nggongyan soft capsule （KSC）. METHODS The fingerprints of 20 batches of KSC were established by ultra high performance liquid chromatography （UPLC）method. Similarity Evaluation System of TCM Chromatographic Fingerprint （2012 edition）were used to evaluate the similarity and confirm common peaks. The contents of norisoboldine ，leonurine hydrochloride ，forsythoside B ，acteoside，poliumoside and isoacteoside were determined by the same UPLC method. Targets and pathways related to KSC in the treatment of cervicitis were screened and analyzed by network pharmacology and molecular docking method to construct a “component-target-pathway”network，and analyze its potential Q-marker. RESULTS Twelve common peaks were identified in the fingerprints of 20 batches of KSC ，and the similarity was greater than 0.99. Six common peaks were identified ，including norisoboldine ，leonurine hydrochloride ，forsythoside B，acteoside，poliumoside and isoacteoside. The contents of the above 6 components were 1.336-1.774，0.093-0.143，4.970-5.888， 0.505-0.623，5.206-6.226 and 0.785-0.895 mg/g，respectively. By network pharmacology analysis ，14 key targets and 94 pathways were obtained ，and their binding energies to the core targets （protein kinase B 1，tumor necrosis factor ）were all less than －6.4 kJ/cal. CONCLUSIONS Six components such as norisoboldine and leonurine hydrochloride are potential Q-marker of KSC.

Exploration of mechanism of Huoxue Jiedu Chinese Herbal Compatibility in anti-atherosclerosis: Based on network pharmacology and molecular docking / 中国药理学通报

Aim To explore the mechanism of Huoxue Jiedu Chinese Herbal Compatibility (angelica sinensis - lonicerae japonicae flos ) in anti-atherosclerosis by means of network pharmacology and molecular rloe- king.Methods The effective eomponents and related targets of angelica sinensis and lonicerae japonicae flos were sereened by the TCMSP database, and the dis¬ease related targets of atheroselerosis were obtained by using the Gene Cards database, DrugBank database and OMIM database.The common targets were ob¬tained by Venny2.1 , an online mapping tool.The pro- tein-protein interaction ( PPI) network was established by String 11.0, and the common target was analyzed by gene ontology(GO) enrichment analysis and kvoto en- cyelopedia of genes and genomes ( KEGG) enrichment analysis using metascape online platform.Cyto- seape3.8.2 was used to construct the " active ingredi¬ent-active target-pathway network map.Finally AutoDock and PyMOL softwares were applied for mo¬lecular docking.Results A total of 31 active compo¬nents of angelica sinensis-lonicerae japonicae flos com¬ patibility and 509 component targets were screened.Hie number of intersection targets with atherosclerosis was 210.GO function enrichment analysis revealed 2 961 biological process items and 242 molecular func¬tion items.KEGG pathway enrichment screened 250 signaling pathways, PI3K-Akt signaling pathway, MAPK signaling pathway, and fluid shear stress and atherosclerosis were the key pathways.Molecular doc¬king results showed that beta-sitosterol, ferulic acid, rutin, luteolin, quercetin could bind stably with MAPK (-1,-3), AKT1, PRKC ( A, B).Conclusions Huoxue Jiedu Chinese Herbal Compatibility ( angelica sinensis -lonicerae japonicae flos) containing multiple active ingredients may play an anti-atherosclerosis role through the signaling pathways of MAPK, P13K-Akt and PRKC, reflecting the advantages of the treatment of activating blood circulation and detoxification of tra¬ditional Chinese medicine in anti-atherosclerosis.