Prediction of the anti-inflammatory mechanisms of curcumin by module-based protein interaction network analysis

Curcumin,the medically active component from Curcuma longa(Turmeric),is widely used to treat inflammatory diseases.Protein interaction network(PIN) analysis was used to predict its mechanisms of molecular action.Targets of curcumin were obtained based on ChE MBL and STITCH databases.Protein–protein interactions(PPIs) were extracted from the String database.The PIN of curcumin was constructed by Cytoscape and the function modules identified by gene ontology(GO) enrichment analysis based on molecular complex detection(MCODE).A PIN of curcumin with 482 nodes and 1688 interactions was constructed,which has scale-free,small world and modular properties.Based on analysis of these function modules,the mechanism of curcumin is proposed.Two modules were found to be intimately associated with inflammation.With function modules analysis,the anti-inflammatory effects of curcumin were related to SMAD,ERG and mediation by the TLR family.TLR9 may be a potential target of curcumin to treat inflammation.

不同加工方法对川明参多糖及欧前胡素含量的影响

目的:研究不同加工方法对川明参多糖及欧前胡素含量的影响,为川明参的科学加工提供资料。方法:采用水回流提取及苯酚-硫酸法显色,紫外分光光度法测定川明参多糖含量;采用甲醇回流提取,高效液相色谱法测定欧前胡素含量。结果:不同方法加工的川明参中多糖及欧前胡素含量差异较大,多糖含量最高者是最低者的2.77倍,欧前胡素含量最高者是最低者的8.4倍。结论:研究结果为科学评价加工方法对川明参质量的影响及优化川明参产地加工方法奠定了基础。

Stems and leaves of Aconitum carmichaelii Debx.as potential herbal resources for treating rheumatoid arthritis： Chemical analysis,toxicity and activity evaluation

According to folk usage of Aconitum carmichaelii Debx., the present study was designed to determine the feasibility of the stems and leaves of Aconitum carmichaelii Debx. as a new medicinal resource. Fourteen alkaloids in mother roots, fibrous roots, stems, and leaves of Aconitum carmichaelii Debx. were measured by HPLC-MS/MS. And multivariate analysis methods, such as clustering analysis and principal component analysis, were applied to analyze the difference among various parts. In addition, the acute toxicity, analgesia, and anti-inflammatory tests were carried out. The results suggested that the contents of alkaloids in mother roots and fibrous roots were approximate, but those of leaves and stems were different from mother roots and fibrous roots. The results of the acute toxicity testing demonstrated the toxicity of fibrous root was strongest, and mother roots were slightly less toxic than fibrous roots. The stems and leaves were far less toxic than mother and fibrous roots. In addition, the analgesia and inflammatory tests showed the effects of the various tissues had no difference each other. These results provided a basis for developing new complementary and alternative treatments for rheumatoid arthritis patients. Simultaneously, the approach may also turn wastes into treasure and promote the development of circular economy.

Rapid determination of pesticide residues in Chinese materia medica using QuEChERS sample preparation followed by gas chromatography-mass spectrometry

Pesticide residue analysis plays an important role in the quality control of Chinese materia medica.This paper reports the development and validation of an analytical method for the quantitative determination of the residues of 39 pesticides in 12 different matrices of Chinese materia medica.Sample preparation utilized the QuEChERS method with acetonitrile:1% aqueous acetic acid(9:1,v/v)as extraction solvent followed by sample clean-up by dispersive solid phase extraction using primary secondary amine sorbent and graphitized carbon black.Extracts were then analysed by gas chromatography coupled with electron impact mass spectrometry in the selected ion monitoring mode.Limit of detection(LOD)and limit of quantitation(LOQ)values were in the ranges 0.5-50 ng/g and 1-100 ng/g,respectively.The recoveries of the 39 pesticides were in the range 75-112% with precision(as relative standard deviation,RSD)<15%.The results show that the modified QuEChERS method allows rapid and sensitive analysis of multiple pesticide residues in Chinese materia medica.

In Vitro and In Vivo Antibacterial Activity of Patchouli Alcohol from Pogostemon cablin

Objective:To investigate the antibacterial activity of patchouli alcohol(PA)against 127 bacteria strains,including the common bacteria and drug-resistant bacteria strains both in the in vitro and in vivo tests.Methods:For the in vitro trial,the antibacterial property of PA against 107 Gram-positive and 20 Gram-negative bacteria strains was screened by agar double dilution method.For the in vivo trial,specific pathogen free Kunming strain of both male and female white mice,were used to test the protective ability of PA after being injected with the median lethal dose of the tested strains.Results:PA possessed antibacterial activity against all the tested 127 strains.In the in vitro test,PA could inhibit both Gram-negative bacteria(25-768μg/m L)and Gram-positive bacteria(1.5-200μg/m L).Particularly,PA was active against some drug-resistant bacteria like methicillin-resistant Staphylococcus aureus(MRSA).PA also exhibited in vivo anti-MRSA activity in mice via intraperitoneal injection.PA could protect mice entirely infected with MRSA at 100 and 200 mg/kg,while 80% mice injected with MRSA could be protected at a low dose of 50 mg/kg.Conclusion:PA might be a potential antibacterial drug from natural sources and might be worthy to explore its mechanism and application in further study.

Recent advances in the development of protein–protein interactions modulators:mechanisms and clinical trials

Protein–protein interactions(PPIs)have pivotal roles in life processes.The studies showed that aberrant PPIs are associated with various diseases,including cancer,infectious diseases,and neurodegenerative diseases.Therefore,targeting PPIs is a direction in treating diseases and an essential strategy for the development of new drugs.In the past few decades,the modulation of PPIs has been recognized as one of the most challenging drug discovery tasks.In recent years,some PPIs modulators have entered clinical studies,some of which been approved for marketing,indicating that the modulators targeting PPIs have broad prospects.Here,we summarize the recent advances in PPIs modulators,including small molecules,peptides,and antibodies,hoping to provide some guidance to the design of novel drugs targeting PPIs in the future.

Active Compounds and Molecular Targets of Chinese Herbal Medicine for Neurogenesis in Stroke Treatment: Implication for Cross Talk between Traditional Chinese Medicine and Biomedical Sciences

Neural stem/progenitor cells (NSCs) could be attractive therapeutic targets for promoting adult neurogenesis, brain plasticity, and repair in stroke and neurodegenerative diseases, raising great potentials for regeneration therapy. In adult ischemic brains, NSCs have limited capacities of growth, differentiation, and generating new neurons for repairing the damaged central nervous system. However, the spontaneous brain repair seems to be insufficient to recover neurological deficits in most stroke cases. To overcome those problems, pharmacological manipulations targeting on endogenous NSCs or transplanted stem cells could be a promoting strategy for regeneration therapy. Chinese herbal medicine has great potentials for developing novel therapeutic strategies for adult neurogenesis and brain repair in poststroke treatment. Chinese herbal medicine has a long history for poststroke treatment. Recent studies create great opportunity for drug discovery for promoting neurogenesis and improving the recovery of neurological fimctions in poststroke treatment. Many active compounds or extracts from medicinal herbs have shown promising effects on regulating proliferation, self-renewal and differentiation of NSCs, and promoting neural network formation as well as neurological functional recovery with in vitro and in vivo experimental evidence. Therefore, targeting neural stem/progenitor cells can be an important opportunity for the studies of Traditional Chinese Medicine in regeneration medicine. Due to the complex interactions of herbal ingredients in network regulation, huge challenge remains to be resolved for further study.

Energy metabolism disorders and potential therapeutic drugs in heart failure

Heart failure(HF)is a global public health problem with high morbidity and mortality.A large number of studies have shown that HF is caused by severe energy metabolism disorders,which result in an insufficient heart energy supply.This deficiency causes cardiac pump dysfunction and systemic energy metabolism failure,which determine the development of HF and recovery of heart.Current HF therapy acts by reducing heart rate and cardiac preload and afterload,treating the HF symptomatically or delaying development of the disease.Drugs aimed at cardiac energy metabolism have not yet been developed.In this review,we outline the main characteristics of cardiac energy metabolism in healthy hearts,changes in metabolism during HF,and related pathways and targets of energy metabolism.Finally,we discuss drugs that improve cardiac function via energy metabolism to provide new research ideas for the development and application of drugs for treating HF.

Asymmetric aza-Henry reaction with α-substituted nitroacetates catalyzed by a bifunctional thiourea-guanidine catalyst

代替的 nitroacetates 和 N-Boc imines 的不对称的 aza-Henry 反应与新型的 thiourea-guanidine bifunctional organocatalyst 被完成。新奇转变展出了忍受邻近的第四级、第三级的 chiral 中心的高 diastereoselectivities，和 adducts 通常被获得在对好 enantioselectivities (多达 88% ee ) 中等。