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.

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.

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 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.

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.

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.

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.

Application of Natural Medicinal Plants Active Ingredients in Oral Squamous Cell Carcinoma

Oral squamous cell carcinoma(OSCC)is the most common malignant cancer of the head and neck,with high morbidity and mortality,ranking as the sixth most common cancer in the world.The treatment of OSCC is mainly radiotherapy,chemotherapy and surgery,however,the prognosis of patients is still poor and the recurrence rate is high.This paper reviews the range of effects of natural medicinal plant active ingredients(NMPAIs)on OSCC cancer,including the types of NMPAIs,anti-cancer mechanisms,involved signaling pathways,and clinical trials.The NMPAIs include terpenoids,phenols,flavonoids,glycosides,alkaloids,coumarins,and volatile oils.These active ingredients inhibit proliferation,induce apoptosis and autophagy,inhibit migration and invasion of OSCC cells,and regulate cancer immunity to exert anti-cancer effects.The mechanism involves signaling pathways such as mitogen-activated protein kinase,phosphatidylinositol 3 kinase/protein kinase B,nuclear factor kappa B,miR-22/WNT1/β-catenin and Nrf2/Keap1.Clinically,NMPAIs can inhibit the growth of OSCC,and the combined drug is more effective.Natural medicinal plants are promising candidates for the treatment of OSCC.

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.

Multi-layered effects of Codonopsis Radix on the immune system

Recent research has highlighted the potential of Codonopsis Radix to modulate the immune system,making it a promising candidate for treating chronic inflammatory and cardiovascular diseases,tumors,and aging.However,because of the complex immune activities of its various components,a comprehensive understanding of Codonopsis Radix immune-regulating properties is still lacking.This knowledge gap hinders its widespread utilization in clinical practice.Therefore,this review aimed to assess the impact of Codonopsis Radix on the immune system and elucidate its underlying mechanisms.Additionally,we compared the immunomodulatory effects of different active ingredients derived from Codonopsis Radix to provide a theoretical basis for future investigations on immunomodulation.

Licorice:comprehensive review of its chemical composition,pharmacodynamics,and medicinal value

Licorice,a perennial herb of Leguminosa,is one of the oldest and most widely used herbal medicines worldwide.Its distinct sweet flavor and rich medicinal value make it an integral component of traditional Chinese medicine(TCM)formulations,which continue to be widely employed.The main chemical constituents of licorice include triterpenoid saponins,flavonoids,and polysaccharides.Experimental and clinical studies have demonstrated that various extracts and pure compounds derived from licorice exhibit a wide range of pharmacological properties including anti-inflammatory,antioxidant,antimicrobial,antiviral,antitumor,immune-regulatory,and neuroprotective activities.The bioactive constituents of licorice offer therapeutic benefits for cardiovascular and cerebrovascular diseases,diabetes mellitus,and liver disorders.This comprehensive review discusses the primary chemical constituents of licorice and their pharmacological activities,describes in vivo and in vitro models employed for studying licorice,and its potential targets and mechanisms of action.Furthermore,we discuss the toxicological profile,side effects,dosage recommendations,and clinical applications of licorice.This review aims to establish a foundation for further research on the safe and effective utilization of licorice while facilitating an in-depth exploration of its properties and fostering the development of novel therapeutic agents.

Research progress in the study of Clinacanthus nutans and treatment of liver diseases

Background:Based on the long history of medicinal value and modern pharmacological research,a systematic collation of the Clinacanthus nutans has been carried out with a view to providing useful references for the clinical application of the Clinacanthus nutans in hepatoprotection and the research and development of new drugs.Methods:The research progress of a large number of domestic and international studies on the therapeutic mechanism of the antiliver diseases of Clinacanthus nutans and its active ingredients is summarized.The aim is to explore the greater value of the herb.Results:The major chemical constituents with pharmacological activities of the Clinacanthus nutans were summarized,and a feasible mechanism of action was compiled and analyzed.Conclusion:Many studies have confirmed the great medicinal value of Clinacanthus nutans and its active monomer components,especially in the prevention and treatment of liver diseases,which is worthy of more in-depth research,development and utilization.Chinese medicine is the treasure of China,therefore,it should be used in more clinical applications.

Pharmacokinetics of Two Ingredients of the Compound Chinese Herbal Medicine Transdermal Preparation in Cows

The topical administration of the compound Chinese herbal medicine transdermal preparation has been widely used in treating the mastitis of cows. In order to understand the metabolic process, four cows suffering from clinical mastitis were selected for the pharmacokinetic study. The transdermal preparation was applied to the diseased part of breast. Then the plasma and milk samples were collected respectively at 0, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, and 36 h, The concentrations of baicalin and phillyrin in plasma and milk were determined by HPLC and the data of time-concentrations were analyzed by the pharmacokinetic software. The results showed that two ingredients in the plasma were not detectable, but they in the milk had linear relationship with the time. The peak concentration of baicalin [（2.84 ±0.15）μg mL^-1] appeared at （4.93 ± 0.35） h, AUC0.1OQ was （27.32 ± 7.91） mg L^-1 h^-1, and the mean retention time was （28.31 ±0.49） h. The peak concentration of phillyrin [（0.49 ± 0.41） μg mL^-1] achieved at （3.68 ± 3.14） h, AUC0-LOQ was （4.10± 0.31） mg L^-1 h^-1, and the mean retention time was （14.52 ± 0.02） h. These suggested that two ingredients had slow absorbing speed and high absorbing degree. They could not be eliminated in a short time, thus exerted the topical curative effect.

Modeling solubility of oxaprozin and irbesartan in biorelevant complex solutions based on a combination of pH-dependent and micellar solubilization models

Biological solubility is one of the important basic parameters in the development process of poorly soluble drugs,but the current measurement methods are mainly based on a large number of experiments,which are time-consuming and cost-intensive.There is still a lack of effective theoretical models to accurately describe and predict the biological solubility of drugs to reduce costs.Therefore,in this study,osaprazole and irbesartan were selected as model drugs,and their solubility in solutions containing surfactants and biorelevant media was measured experimentally.By calculating the parameters of each component using the perturbed-chain statistical associating fluid theory(PC-SAFT)model,combined with pH-dependent and micellar solubilization models,the thermodynamic phase behavior of the two drugs was successfully modeled,and the predicted results were in good agreement with the experimental values.These results demonstrate that the model combination used provides important basic parameters and theoretical guidance for the development and screening of poorly soluble drugs and related formulations.

Research on Extraction of Anti-allergic Active Ingredient from Citrus Peels and Its Anti-allergic Activity

[Objective] This study aimed to determine the optimal process conditions for extraction of anti-allergic active ingredient from citrus peels. [Method] Crude anti- allergic active extracts of citrus peels were extracted. Effects of extraction conditions including extraction temperature, ethanol concentration, extraction time and liquid-to-solid ratio on extraction were explored with single-factor experiment, and the extrac- tion process was optimized with orthogonal experiment. [Result] Based on the single- factor experiment and orthogonal experiment, the optimal extraction condition for crude anti-allergic active extracts of citrus peels were determined to be under extraction temperature of 60℃, ethanol concentration of 70%, extraction time of 60 min, liquid-to-solid ratio of 1：25 and twice extraction. [Concluslon] This process condition is of simple operation and high extraction efficiency, which is environment-friendly and suitable for the extraction of crude anti-allergic active extracts from citrus peels. This study provided a new approach and research ideas for the effective and rapid extraction of anti-allergic active ingredient in citrus peels.

Research Progress on Medicinal Active Components of Endophytes in Plants

Endophytes are a type of microorganisms which live in plant tissues and have no obvious disease symptoms to plants,mainly including fungi,bacteria and actinomycetes.Endophytes can produce the same or similar active substances as host plants,so they have become a hot spot in the research of natural medicinal active products in recent years.Endophytes provide abundant resources for searching medicinal active substances because of their abundant species and huge reserves.In this paper,the species,structural characteristics,separation methods and pharmacological studies of active products of endophytic fungi were reviewed,in order to provide theoretical reference for the research of medicinal active components of endophytic fungi.