滑石粉炒鱼鳔胶炮制工艺优选

目的优选最佳滑石粉炒鱼鳔胶炮制工艺,为滑石粉炮制药材的工艺筛选及质量评价提供研究思路及方法。方法选用L_9(3~4)正交表设计试验,以粉碎率、蛋白质含量为指标,以膨胀率、浸出物为参考指标,结合实际选择滑石粉炒制时间、滑石粉粒度、滑石粉炒制温度、滑石粉用量4个因素进行考察,筛选滑石粉炒鱼鳔胶炮制工艺。结果选择2倍于药物的200目滑石粉,190℃,翻炒3 min为滑石粉炒鱼鳔胶最佳工艺。验证试验表明,最佳工艺切实可行,结果稳定。结论采用客观、可靠的评价指标,对传统滑石粉炒鱼鳔胶"翻炒至鼓起、酥脆"的工艺进行了研究,为进一步制订滑石粉炒鱼鳔胶饮片的质量标准提供依据。

Mechanisms of Dihuang(Rehmanniae Radix)in treating diabetic nephropathy complicated with depression based on network pharmacology

Objective To predict the molecular mechanism of Dihuang(Rehmanniae Radix)in the treatment of diabetic nephropathy(DN)complicated with depression based on network pharmacology.Methods The components of Dihuang(Rehmanniae Radix)were identified from the Integrated Pharmacology-based Research Platform of Traditional Chinese Medicine(TCMIP),Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP),and relevant literature.The component targets were detected by combining the SwissTargetPrediction and Pub Chem databases.Disease targets were collected from the Therapeutic Target Database(TTD),Dis Ge NET,and Ensembl databases with“diabetic nephropathy”and“depression”as keywords.The disease-component targets were mapped using Venny 2.1.0 to obtain potential targets.A protein-protein interaction(PPI)network was constructed using the Search Tool for the Retrieval of Interacting Genes/Proteins(STRING)database and Cytoscape 3.7.2.The co-expression genes of the key targets were collected based on the COXPRESdb 7.3.Gene Ontology(GO)and Kyoto Encyclopedia of Genes and Genomes(KEGG)enrichment analysis were performed for potential targets using R language.Target-component docking was verified and evaluated using Discovery Studio 4.5.Results According to the databases and literature reports,Dihuang(Rehmanniae Radix)contained 65 active components,and had 155 related targets for the treatment of DN complicated with depression.PPI screening showed that the key targets included serine/threonine protein kinase 1(AKT1),signal transducer and activator transcription 3(STAT3),interleukin 6(IL-6),mitogen-activated protein kinase 1(MAPK1),and vascular endothelial growth factor A(VEGFA),etc.GO enrichment analysis mainly involved biological processes,such as lipid metabolism,protein secretion regulation,cell homeostasis,and phosphatidylinositol 3 kinase activity.KEGG pathway enrichment analysis included the role of the AGE-RAGE signaling pathway in diabetic complements,insulin resistance(IR),neurotrophin signal path,Toll-like receptor signaling pathway,relaxin signaling pathway,epidermal growth factor receptor tyrosine kinase inhibitors(EGFR-TKIs),etc.Molecular docking showed that the target had high affinity for stachyose,manninotriose,verbascose,nigerose,etc.Conclusion Based on network parmacology,this study preliminarily predict the effects of Dihuang(Rehmanniae Radix)in treating DN complicated with depression by regulating inflammation,glucose metabolism,nution nerve,etc.

Ancient and modern medication laws of aromatic Chinese medicines in treating angina pectoris based on data mining

Objective To explore ancient and modern medication laws of aromatic Chinese medicines in treating angina pectoris, and to provide new ideas for the clinical treatment.Methods With “angina pectoris” as the key word, ancient books prescriptions and Chinese patent medicines related to angina pectoris were collected from China National Knowledge Infrastructure(CNKI), Traditional Chinese Medicine Database System, Chinese Medicine Prescription Database, New National Proprietary Chinese Medicine(2 nd edition), and Chinese Pharmacopoeia(2020 edition) from January 1, 2015 to December 31, 2021. Core highfrequency aromatic Chinese medicines were defined, and their potential medication rules were analyzed and summarized. Microsoft Access 2010 was used for data management. Data analysis software, including Excel and IBM SPSS Modeler 18.0 were used for drug association rule analysis, and Cytoscape 3.7.2 for visual display.Results There were 67 ancient books prescriptions and 258 Chinese patent medicines containing aromatic Chinese medicines treating angina pectoris collected from relevant databases. In ancient books prescriptions, there were nine aromatic Chinese medicines with the frequency ≥10, and the most commonly used medicine was Danggui(Angelicae Sinensis Radix), followed by Chenpi(Citri Reticulatae Pericarpium). There were 33 aromatic Chinese medicines with the frequency ≥10 in Chinese patent medicines, and the most commonly used medicine was Danshen(Salviae Miltiorrhizae Radix et Rhizoma), followed by Chuanxiong(Chuanxiong Rhizoma) and Sanqi(Notoginseng Radix et Rhizoma). In ancient books prescriptions, the medicines mainly belonged to intenal-warming medicines, Qi-regulating medicines, and blood circulation promoting and blood stasis removing medicines.There were eight medicine pairs with confidence equal to 100% in ancient books prescriptions, the most frequently used pairs were Chuanxiong(Chuanxiong Rhizoma) +Danggui(Angelicae Sinensis Radix), and Xiangfu(Cyperi Rhizoma) + Chenpi(Citri Reticulatae Pericarpium). In Chinese patent medicines, the aromatic Chinese medicine Chuanxiong(Chuanxiong Rhizoma) could be combined with many other Chinese medicines, among which the Confidence and Support of Chuanxiong(Chuanxiong Rhizoma) + Danshen(Salviae Miltiorrhizae Radix et Rhizoma) were at a high level.Conclusion Aromatic Chinese medicines for the treatment of angina pectoris of coronary heart disease are mainly warm, and the flavors are mainly pungent, sweet, and bitter. They mainly access to the liver, gallbladder, and pericardium meridians. The treatment of angina pectoris of coronary heart disease mainly focuses on warming heart pulse, and promoting blood circulation and removing blood stasis.

Identification of major compounds of total flavonoids from Smilax china and evaluation of anti-inflammatory effect on phenol mucilage-induced pelvic inflammation in rats

As a Chinese medicinal plant,Smilax china is traditionally used in the treatment of pelvic inflammatory disease(PID).Flavonoids have been identified as the anti-inflammatory bioactive fraction.However,the high content of total flavonoids has not been extracted from S.china.The therapeutic effects and mechanisms of total flavonoids are still unknown.In the present study,we aimed to obtain the effective parts of flavonoids in S.china,and elucidate the mechanism of action on PID.The anti-inflammatory effect was evaluated on phenol mucilage-induced pelvic inflammation in rats.This was the first time that total flavonoids in high concentration(up to 55.6%)were obtained in S.china.A total of 15 compounds were separated and identified by NMR,and the total flavonoids were detected with HPLC.TFSC caused a reduction in serum levels of IL-6 and IL-1β.These results suggested that TFSC had a significant anti-PID effect,probably due to inhibition of the inflammatory reaction.

The multiple mechanisms of tripterygium wilfordii-induced acute kidney injury based on network pharmacology and molecular docking

Acute kidney injury(AKI)is a common and serious health issue with a growing incidence and mortality rate.Tripterygium wilfordii(TW)is a traditional Chinese medicine that has been reported to cause kidney damage.However,the associated mechanism of TW-induced AKI remains unclear.Therefore,we aimed to uncover the associated mechanisms of AKI induced by TW using network pharmacology and bioinformatics.The candidate compounds of TW and the potential targets were screened using TCMSP and CTD database,and the AKI-related targets were identified from the Dis Ge NET database.The disease targets were intersected with the drug targets,and the Wayne diagram was drawn by Venny 2.1.0 software.We developed proteinprotein interactions(PPI)network and the“disease-compound-target-pathway”network through the Cytoscape software.By using the DAVID database,GO and KEGG enrichment analysis was carried out to reveal the potential signaling pathways of the compound-TW-induced AKI.Meanwhile,the Auto dock vina 1.1.2 was used for molecular docking to verify the active compound and key targets’binding ability.Critical compounds and key targets of TW-induced AKI were identified,including triptolide,kaempferol,β-sitosterol,nobiletin,stigmasterol,TNF,and so on.The GO analysis showed that potential genes’biological function was mainly involved in apoptosis,oxidative stress,and inflammation.Moreover,eight signaling pathways were found,including the HIF-1 signaling pathway,VEGF signaling pathway,apoptosis,and so on.The molecular docking results proved that the core compound’s affinity with the corresponding protein of the gene targets was good.This study preliminarily predicted the core toxic compounds,targets,and related pathways of TW-induced AKI,providing a theoretical basis for the follow-up clinical rational drug use and related research work of TW.

In vitro metabolism and inhibitory effects of atractylenolideⅡon various hepatic CYPs in HLMs

In the present study,we aimed to investigate the interaction between atractylenolideⅡ(AT-Ⅱ)and CYP450 enzyme in human liver microsomes,and to lay a theoretical foundation for predicting the possible interaction of AT-Ⅱin combination with drugs.The chemical inhibition experiment was carried out with specific inhibitors to clarify the CYP450 subtypes affecting the metabolism of AT-Ⅱ,and the mechanism,kinetics,and type of inhibition of CYP450 enzyme by AT-Ⅱwere studied by using the probe-based determination method of human liver microsome system with the related data of IC50 and Ki as evaluation indexes.The metabolism of AT-Ⅱwas affected by CYP1A2,CYP2C9 and CYP3A4 inhibitors,and the highest inhibition rates were41.35%,41.97%and 82.45%,respectively.The IC50 values of AT-Ⅱto five subtypes of P450 CYP2C9,CYP1A2,CYP2C19,CYP3A4 and CYP2D6 were 69.7,84.3,92.4,173.8 and 190.1μmol/L,respectively.The Ki values of AT-Ⅱto five subtypes of P450 CYP2C9,CYP1A2,CYP2C19,CYP3A4 and CYP2D6 were 190.6,179.1,>200,72.2 and 66.8,respectively.Among these enzymes,AT-Ⅱexhibited non-competitive inhibition on CYP1A2,showed competitive inhibition on CYP2C9 and CYP3A4,and displayed mixed AT-Ⅱinhibition on CYP2C19 and CYP2D6.CYP1A2,CYP2C9 and CYP3A4 were involved in the AT-Ⅱmetabolism,and AT-Ⅱexhibited different inhibitory mechanisms and strengths for the five subtypes of CYP450.

Study ofβ-cyclodextrin differential encapsulation of essential oil components by using mixture design and NIR:Encapsulation ofα-pinene,myrcene,and 3-carene as an example

The encapsulation of essential oil components in cyclodextrins(CDs)to form inclusion complexes(ICs)is an effective strategy for improving their stability and bioaccessibility.The aim of the present study was to obtain a deeper understanding of the encapsulation behavior of multi-components inβ-CD.Guest molecules ofα-pinene,myrcene,and 3-carene,having the same molecular weight,formed ICs withβ-CD by a freeze-drying method.A simplex lattice mixture design with 28 experiments was carried out.Statistical analysis was applied to analyze the encapsulation behavior of guest components,and quantitative models of guest components in ICs were constructed by coupling with near-infrared(NIR)spectroscopy and chemometrics analysis.Besides,the molecular docking technique was used to obtain the optimal conformation and explain the binding behavior of inclusion.The results suggested that the spatial structure and ratio of guest molecules were the key factors affecting the encapsulation effect.A non-destructive and rapid NIR analytical model for the guest component in ICs could be obtained by second derivative(2nd der)pretreatment.Collectively,the encapsulation of guest components inβ-CD was differentiated,and NIR could be used as a rapid and non-destructive tool for quantitative analysis of ICs.