Integrative analysis of bone-formation associated genes and immune cell infiltration in osteoporosis, and the prediction of active ingredients in targeted traditional Chinese medicine

Objective To explore the differential expression and mechanisms of bone formation-related genes in osteoporosis(OP)leveraging bioinformatics and machine learning methodologies;and to predict the active ingredients of targeted traditional Chinese medicine(TCM)herbs.Methods The Gene Expression Omnibus(GEO)and GeneCards databases were employed to conduct a comprehensive screening of genes and disease-associated loci pertinent to the pathogenesis of OP.The R package was utilized as the analytical tool for the identification of differentially expressed genes.Least absolute shrinkage and selection operator(LASSO)logis-tic regression analysis and support vector machine-recursive feature elimination(SVM-RFE)algorithm were employed in defining the genetic signature specific to OP.Gene Ontology(GO)and Kyoto Encyclopedia of Genes and Genomes(KEGG)pathway enrichment analyses for the selected pivotal genes were conducted.The cell-type identification by estimating rela-tive subsets of RNA transcripts(CIBERSORT)algorithm was leveraged to examine the infiltra-tion patterns of immune cells;with Spearman’s rank correlation analysis utilized to assess the relationship between the expression levels of the genes and the presence of immune cells.Coremine Medical Database was used to screen out potential TCM herbs for the treatment of OP.Comparative Toxicogenomics Database(CTD)was employed for forecasting the TCM ac-tive ingredients targeting the key genes.AutoDock Vina 1.2.2 and GROMACS 2020 softwares were employed to conclude analysis results;facilitating the exploration of binding affinity and conformational dynamics between the TCM active ingredients and their biological targets.Results Ten genes were identified by intersecting the results from the GEO and GeneCards databases.Through the application of LASSO regression and SVM-RFE algorithm;four piv-otal genes were selected:coat protein(CP);kallikrein 3(KLK3);polymeraseγ(POLG);and transient receptor potential vanilloid 4(TRPV4).GO and KEGG pathway enrichment analy-ses revealed that these trait genes were predominantly engaged in the regulation of defense response activation;maintenance of cellular metal ion balance;and the production of chemokine ligand 5.These genes were notably associated with signaling pathways such as ferroptosis;porphyrin metabolism;and base excision repair.Immune infiltration analysis showed that key genes were highly correlated with immune cells.Macrophage M0;M1;M2;and resting dendritic cell were significantly different between groups;and there were signifi-cant differences between different groups(P<0.05).The interaction counts of resveratrol;curcumin;and quercetin with KLK3 were 7;3;and 2;respectively.It shows that the interac-tions of resveratrol;curcumin;and quercetin with KLK3 were substantial.Molecular docking and molecular dynamics simulations further confirmed the robust binding affinity of these bioactive compounds to the target genes.Conclusion Pivotal genes including CP;KLK3;POLG;and TRPV4;exhibited commendable significant prognostic value;and played a crucial role in the diagnostic assessment of OP.Resveratrol;curcumin;and quercetin;natural compounds found in TCM;showed promise in their potential to effectively modulate the bone-forming gene KLK3.This study provides a sci-entific basis for the interpretation of the pathogenesis of OP and the development of clinical drugs.

Study on Skin Care Efficacy of the Active Ingredients in Camellia Japonica Flowers at High and Low Altitudes

The active ingredients of Camellia japonica flowers(CJF)at high and low altitudes,as well as their skin care efficacy were compared.The dried red CJF at high and low altitudes were ultrasonically extracted with 70%ethanol,and these extracts were concentrated and then diluted to a constant volume.The content of total flavonoids,total polyphenols and total proteins was tested and analyzed.In addition,DPPH free radical scavenging,inhibition of the formation of advanced glycation end products,and inhibitory activity against elastase was measured to compare their skin care efficacy in anti-oxidation,anti-glycation,anti-wrinkling and firming.The results showed that,based on the dry weight of CJF,the content of total flavonoids and total proteins of the CJF at high altitude was approximately 1.5 times of the CJF at low altitude,while the content of total polyphenols was approximately 2.4 times that of the CJF at low altitude.The skin care efficacy of CJF at high altitude was significantly better than that of the CJF at low altitude.This work could provide theoretical basis for the selection and application of Camellia japonica flowers in the field of cosmetics.

Screening of Anti-inflammatory Active Ingredients from Gancao Qinlian Extract and Study of Its Efficacy

[Objectives]To establish the chromatographic fingerprint of Gancao Qinlian Extracts(GQE)and reveal the possible material basis of the anti-inflammatory effect of GQE by the correlation analysis between the fingerprint chromatographic peaks of different components of GQE and its anti-inflammatory activity.[Methods]Ultra-performance liquid chromatography(UPLC)was used to detect the different ingredients of GQE to establish its chromatographic fingerprint and analyze the differences among the three medicine components;LPS stimulated RAW264.7 cells to construct an inflammatory cell model.The NO secretion of cells was detected by the Griess method.ELISA was used to detect the changes in TNF-αand IL-10 contents.RT-qPCR tested the mRNA expression levels of TNF-αand IL-10.Grey relational analysis was carried out by combining fingerprint chromatographic peak data and anti-inflammatory activity data.[Results]The GQE fingerprint was established,34 fingerprint characteristic peaks were calibrated,and 33 related chromatographic peaks were screened out.The corresponding chromatographic peaks in the three components were obtained,and the content of the components was calculated;the anti-inflammatory results showed that the content of NO,TNF-α,and the expression of TNF-αmRNA in the high and medium-dose groups of GQE were significantly lower than those in the blank group(P<0.01).The NO content and TNF-αmRNA expression in the high-dose group of GQE I was considerably lower than those in the blank group(P<0.01).The secretion of NO,TNF-α,and the expression of TNF-αmRNA in the high,medium,and low dose groups of GQE II were significantly lower than those in the blank group(P<0.01);the results of grey relational analysis showed that the correlation degree of the three components was GQE II>GQE>GQE I,and the characteristic fingerprint peaks 12,15,22,23,28,31,33 may be closely related to the anti-inflammatory effect.[Conclusions]The best component of the anti-inflammatory effect in GQE is water-soluble component,and its main components are flavonoids and alkaloids.These components can alleviate cellular inflammatory damage by inhibiting the excessive secretion of NO and reducing the expression of TNF-αmRNA.

Research Progress of Active Ingredients and Pharmacological Action of Honeysuckle

Honeysuckle, the dry flower bud or with open flower of Lonicerajaponica in caprifoliaceae, has been touted as a cure-all for heat-clearing and detoxifying effect. Honeysuckle contains abundant components such as volatile oil, flavonoids and organic acids, playing the role of antibiosis, antivirus, antiphlogosis, immunopotenfiation and antioxidation. The active ingredients and pharmacological action of honeysuckle are reviewed in the paper, so as to lay the foundation for further application of honeysuckle in veterinary clinic.

Structural similarity-based prediction of the potential active ingredients and mechanism of action of traditional Chinese medicine formulations used to anti-aging

Objective:To predict the potential active ingredients (PAIs) and mechanism of action of traditional Chinese medicine formulations used to delay aging.Methods:We incorporated the use of quantum-chemistry calculations and machine learning to predict the active ingredients of some Chinese herbal medicines used to delay aging.Then,a network-pharmacology approach was used to uncover how these PAls delayed aging.Results:Twelve PAls with anti-aging effects were discovered:androsterone,MHP,cortisone,propyl methyl trisulfide,retinol,retinal,cortisol,11-cis-Retinol (2R,3R)-3-hydroxyproline,4,5alpha-Dihydrocortisone (2S)-2-ammonio-6-ureidohexanoate and17alpha,21-Dihydroxy-5beta-pregnane-3,11,20-trione.Enrichment analyses indicated that a putative compound target and aging target were significantly associated with:regulation of the immune system;insulin receptor signaling pathway;regulation of the mitotic cell cycle;response to nutrient levels;response to oxidative stress;release of cytochrome c from mitochondria;learning or memory;inflammatory response.Conclusions:A novel method was proposed to predict the PAls of anti-aging herbal medicines by incorporating quantum-chemistry calculations and machine learning.Then,a network-pharmacology approach was used to uncover how these PAls delay aging.The information provided by our study on PAls may aid the discovery of anti-aging drugs.

Studies on Insecticidal Activities and Active Ingredients of Stephania kwangsiensis Lo.

Insecticidal activities and active ingredients of Stephania kwangsiensis Lo. were studied for the first time. The results showed that all parts of S. kwangsiensis Lo. had contact activity against brown planthoppers, Nilaparvata lugens Stal, and the contact activity of methanol extract from root tubers was the highest, with a LD50 value being 1.5794 lag/female. l-roemerine was isolated from root tubers of S. kwangsiensis Lo. and identified, and it was the main active ingredient. l-roemerine had high contact toxicity to brown planthoppers, with a LD50 value being 0.0443 lag/female. Contact toxicity of l-roemerine to brown planthoppers was 7.48 times that of malathion, the convientional chemical insecticide used for controlling brown planthoppers.l-roemerine also had stomach poison activity against brown planthoppers.

“ACTIVE”英语学科育人模式构建与应用

本研究以“立德树人”为核心理念,构建“ACTIVE”英语学科育人模式。该模式通过六个关键维度--学科育人(AIM)、文化浸润(Culture)、思维可见(Thinking)、技术融合(Integration)、美德根植(Virtue)和情感共鸣(Empathy)--全面激发学生英语学习的热情,培养他们的语言能力,同时注重道德品质的熏陶和文化素养的提升,促进英语学科素养落地。本研究不仅为英语教学实践提供了新的视角,也为其他学科育人模式的构建提供了有益的参考和借鉴。

Antifeedant Activity and Active Ingredients Against Plutella xylostella from Momordica charantia Leaves

With the bioguided fractionation of the ethanol extracts from the leaves of Momordica charantia, we obtained two most active compounds against the feeding of the diamondback moth, Plutella xylostella larvae. The antifeedant activity of momordicine Ⅰ and momordicine Ⅱ against the second and the third instar larvae of Plutella xylostella were tested using leaf discs of cabbage in the laboratory. The results showed that momordicin Ⅰ and momordicin Ⅱ had significant antifeedant activity on the larvae of P. xylostella, and momordicin Ⅱ was more active than momordicin Ⅰ. The concentrations for 50% antifeedant effects （AFC50） of momordicin Ⅱ against the second and the third instar larvae of P. xylostella were 76.69 and 116.24μg mL^-1, whereas that of momordicin I was 144.08 and 168.42μg mL^-1, respectively. In addition, momordicin Ⅰ and momordicin Ⅱ had significant inhibitive effect on the rate of weight gain and survival of P. xylostella larvae.

Research Progress of Anti-tumor Active Ingredients in Dandelion

As a traditional Chinese herb,dandelion,containing complicated active ingredients which includes polysaccharide,flavonoid,terpene,pigment,phytosterol,coumarin,organic acid and etc,plays significant roles in various physiological activities in organisms.The active ingredients generally interfere in signal transduction of cancer cells,regulate cell cycle and apoptotic protein expression,inhibit cancer cells proliferation and migration and etc,which effectively restrains tumor development and deterioration.This article summarizes the anti-tumor mechanism of five active ingredients in dandelion through paper reading which provides thoughts and references for anti-tumor research.

Chinese medicine active ingredients or monomers increase neuronal synaptic plasticity

Totally three articles focusing on Schisandra N-butanol extract effects on hippocampal CA1 synaptic morphology and plasticity in ovarectomized mice, as well as catalpol and GBE50 effects on neuronal synaptic plasticity in the motor cortex following cerebral ischemia were published in three issues. We hope that our readers find these papers useful to their research.

Impacts of Active Ingredients of Three Traditional Chinese Medicine on Immune Effect of PCV2 Vaccine

[ Objective ] The paper was to screen the active ingredients of traditional Chinese medicine （ TCM）, which significantly enhanced the immune effect of porcine circovirus type 2 （PCV2） vaccine. [Method]Sixty-six 14-day-old piglets were randomly divided into 11 groups, including immune control group, blank control group and nine drug groups. Piglets that were reared for 21 d were intramuscularly injected with 2 mL of inactivated vaccine in cervical region expect for blank control group. Piglets in nine drug groups were administrated with 5 mL of matrine, scutellarin and astragalus polysaecharide （ASP） at three doses （ high dose 12 mg, medium dose 8 nag, low dose 4 mg） three days before and after immunization; piglets in blank control group and irmnune control group were administrated with equal volume of normal saline. Five piglets were randomly selected from each group to collect venous blood at 7, 14, 21 and 28 d post immunization, and the PCV2 antibody level, the concentration of specific immunoglobulin [gG, the changes in peripheral blood lymphocyte subsets, and the content of serum IL-2 and IFN-γ were determined. [ Result] The immunological effects of active ingredients of three TCM on PCV2 vaccine all enhanced at different degree. The effects of scutellarin middle dose group was the best. [ Conclusion ] Scutellarin could be used as a candidate drug for PCV2 vaccine immunoenhancer.

A review on cocrystal of active ingredients in traditional Chinese medicine

In the development of new drugs products,especially the development of traditional Chinese medicine active ingredients,solubility and oral bioavailability are the main factors which are restricting the development of new drugs,whereas the physicochemical properties of active ingredients are the key element to affecting these factors.Pharmaceutical cocrystal provides an excellent opportunity to develop new drugs with excellent physical and chemical properties such as melting point,solubility,stability and bioavailability while retaining the pharmacological properties of individuals active pharmaceutical ingredients among pharmaceutical cocrystal compounds.Traditional Chinese herbal medicine has the characteristics of multiple pathways and multiple targets,mainly because it contains many active ingredients,like cocrystals thereof with many components.The active ingredients extracted from traditional Chinese herbal medicine have a wide range of pharmacological activities,but most of the active ingredients affect the development of traditional Chinese medicine active ingredients due to their physical and chemical properties such as solubility.Traditional Chinese medicine pharmaceutical cocrystals can not only improve the physical and chemical properties of drugs without changing the internal structure of drugs,so as to provide a new scheme for the development of traditional Chinese medicine active ingredients.This paper reviews the research progress of active ingredients of traditional Chinese medicine pharmaceutical cocrystal.The preparation methods of cocrystals are summarized and the advantages of cocrystals are illustrated with examples.

Study on the Anti-aging Efficacy of the Active Ingredients in Aqueous Extract of Ganoderma lucidum

[ Objective ] The research aimed to develop anti-aging masks with aqueous extracts of Ganoderma lucidum and to study the clinical efficacy on the delaying of skin aging. [Method] The anti-aging efficacy of the aqueous extract of C.anoderrna luciclum was evaluated by sensory evaluation, safety evaluation, instrumental measurements, etc. [ Result] The results of sensory evaluation showed that after continuous application of the test materials for 12 weeks, the skin dryness, elasticity, surface sheen, fine wrinkles and smoothness were well improved, and the improvement rates were 9l. 17%, 91.17% , 94.12% , 11.76% and 91.18% , respectively. The measurement results by specialized instrument showed that the skin hydration on the target site increased continuously with the prolonging of the using time. Significant differences existed between each time point after using the products and the time before using. There was no signiScant difference existed in elasticity index 112 and R5 compared with before using. [Result] Clinical data showed that the active ingredients in aqueous extract of Ganoderma lucidum had a certain effect on the delaying of skin aging.

Effect of Different Drying Processes on Active Ingredients of Rheum officinale Baill.

[Objectives]To determine the drying process of different functional rhubarbs.[Methods]The contents of tannins,bianthrone,free anthraquinones and combined anthraquinones in medicinal rhubarb were determined by HPLC.The results were analyzed by two-way analysis of variance.[Results]Under different drying conditions,the contents of tannins,bianthrone,free anthraquinones and combined anthraquinones in medicinal rhubarb were significantly different.Taking the tannins content as the index,the optimum drying condition of the rhizome is 1 cm thick,dried at 60℃,the root is cut 1 cm thick,and dried at 30℃;the bianthrone content is used as an indicator,the rhizome is optimally dried.The condition is to cut 1 cm thick,dry at 60℃,the root is cut to 5 cm thick,and dried at 40℃;the free anthraquinones content is used as an index,and the optimum drying condition of the rhizome is 3 cm thick and dried at 50℃.The root is cut to a thickness of 3 cm and dried at 30℃.The combine anthraquinones content is used as an indicator.The optimum drying conditions for the rhizome are 5 cm thick,dried at 40℃,and the root is cut to 5 cm thick and dried at 70℃.[Conclusions]Different functional components of rhubarb have different directional processing methods.The drying process can reduce the drying temperature or increase the thickness of the slice,and the directional processing of the diarrhea-type rhubarb can be processed.The drying process can be carried out by increasing the drying temperature or reducing the thickness of the slice directed processing of heat-clearing and purging-fire rhubarb.

Model evaluation for the prediction of solubility of active pharmaceutical ingredients(APIs) to guide solid–liquid separator design

The assumptions and models for solubility modelling or prediction in systems using nonpolar solvents, or water and complex triterpene and other active pharmaceutical ingredients as solutes aren't well studied. Furthermore, the assumptions concerning heat capacity effects(negligibility, experimental values or approximations) are explored, using non-polar solvents(benzene), or water as reference solvents, for systems with solute melting points in the range of 306–528 K and molecular weights in the range of 90–442 g/mol. New empirical estimation methods for the Δ_(fus)C_(pi) of APIs are presented which correlate the solute molecular masses and van der Waals surface areas with Δ_(fus)C_(pi). Separate empirical parameters were required for oxygenated and non-oxygenated solutes. Subsequently, the predictive capabilities of the various approaches to solubility modelling for complex pharmaceuticals,for which data is limited, are analysed. The solute selection is based on a principal component analysis, considering molecular weights, fusion temperatures, and solubilities in a non-polar solvent, alcohol, and water, where data was available. New NRTL-SAC parameters were determined for selected steroids, by regression. The original UNIFAC, modified UNIFAC(Dortmund), COSMO-RS(OL), and COSMO-SAC activity coefficient predictions are then conducted, based on the availability of group constants and sigma profiles. These are undertaken to assess the predictive capabilities of these models when each assumption concerning heat capacity is employed. The predictive qualities of the models are assessed, based on the mean square deviation and provide guidelines for model selection, and assumptions concerning phase equilibrium, when designing solid–liquid separators for the pharmaceutical industry on process simulation software. The most suitable assumption regarding Δ_(fus)C_(pi) was found to be system specific, with modified UNIFAC(Dortmund) performing well in benzene as a solvent system, while original UNIFAC performs better in aqueous systems.Original UNIFAC outperforms other predictive models tested in the triterpene/steroidal systems,with no significant influence from the assumptions regarding Δ_(fus)C_(pi).

Research progress on antidepressive active ingredients and mechanism of Xiaoyaosan

The antidepressive effect of Xiaoyaosan is doubtless by researches while the potential antidepressive ac- tive ingredients and their mechanisms remain unclear. In order to explain the antidepressive effect of Xiaoyaosan, all of the recent reports were sought out on the current situation of the antidepressive monomer compositions of Xi- aoyaosan and their mechanism. By exploring the relationship between the effects and the active ingredients, the mechanism and the active ingredients, the antidepressive active ingredients such as quercetin, isorhamnetin, isoliquiritigenin, saikosaponinA, saikosaponinD, glycyrrhiz- kaempferol, liquiritin, isoliquiritin, liquiritigenin, inate, paeoniflorin, albiflorin, ferulic acid, curcumin and their mechanism of antidepressive such as regulating the monoamine neurotransmitter systems, regulating the neuroendocrine system, affecting the neural plasticity and neu- affecting the cytokines level, anti-oxidative stress were rotrophic, affecting the cellular and molecular mechanisms , summarized. By the overview in the level of monomer rather than formulae, we uncovered the antidepressive mech- anism of Xiaoyaosan and further confirmed that Xiaoyaosan, as a classic antidepressive Chinese prescription, had many characteristics, such as multi-level , multi-channel, multi-target and so on .

Multiple Emulsions Able to Be Used for Oral Administration of Active Pharmaceutical Ingredients: Physico-Chemical Parameters Study of Different Phases

Multiple emulsions are of great therapeutic interest especially in the administration of medicines which can be inactivated by digestive enzymes;moreover the researches of formulation not being often easy, a control of the different phases physicochemical parameters would be of great interest in rapid formulations and at low cost. When formulating emulsions, the preliminary tests, also known as formulation tests, constitute a step which can be long and expensive because of the quantity of reagents that can be used. A rigorous methodology could thus be of great interest, which is at the aim of our study which consists of evaluating the physico-chemical parameters of different phases used to make thus multiple emulsions. In our study, physico-chemical parameters such as conductivity, pH, density, viscosity, and surface tension have been studied by direct measurement using equipment and also by means of suitable mounting. The results showed that the pH and the surface tension have an important role in the prediction of the stability of emulsions, these latter must be of the same order of magnitude. For all phases conductivity does not have too much interest apart from helping to determine the type of the emulsion.

Application of Caenorhabditis elegans in screening active ingredients of traditional Chinese medicine

People continue to recognize the important role of Chinese medicine in the treatment of diseases,and there is an urgent need to clarify the mechanism of Chinese medicine.Because of the multi-target and multi-component characteristics of traditional Chinese medicine,it is difficult to elaborate from a single perspective.As a high-quality animal model,Caenorhabditis elegans with the characteristics of small size and fast reproduction,has been widely used in traditional Chinese medicine activity experiments.In this article,Caenorhabditis elegans,as model organisms used to screen the active components of traditional Chinese medicine were reviewed.

Research Progress of Anti-tumor Effects of Curcuma zedoaria and its Active Ingredients Through Immune Regulation Mechanism

The continuous increase in the incidence rate of various fatal malignant tumors in the recent years warrants an imperative search for medications or drugs with obvious anti-tumor eflects and reliable curative effects.Previous studies have found that Curcuma zedoaria and its active ingredients,such as turmeric oil,curcumol,and P-elemene,have obvious antitumor effects,and they do not have the adverse reactions and side effects seen in the anti-tumor drugs of Western medicine.Based on the review and inductive analysis of related literature,we summarize in the present article the results of some researchers who investigated the anti-tumor effects of Curcuma zedoaria and its active ingredients through the immune regulation mechanism.

Liquid crystal-integrated metasurfaces for an active photonic platform

Metasurfaces have opened the door to next-generation optical devices due to their ability to dramatically modulate electromagnetic waves at will using periodically arranged nanostructures.However,metasurfaces typically have static optical responses with fixed geometries of nanostructures,which poses challenges for implementing transition to technology by replacing conventional optical components.To solve this problem,liquid crystals(LCs)have been actively employed for designing tunable metasurfaces using their adjustable birefringent in real time.Here,we review recent studies on LCpowered tunable metasurfaces,which are categorized as wavefront tuning and spectral tuning.Compared to numerous reviews on tunable metasurfaces,this review intensively explores recent development of LC-integrated metasurfaces.At the end of this review,we briefly introduce the latest research trends on LC-powered metasurfaces and suggest further directions for improving LCs.We hope that this review will accelerate the development of new and innovative LC-powered devices.