Active Ingredient Of Chinese Medicine Research Articles

Comparison of different extraction methods of active ingredients of Chinese medicine and natural products.

Like other traditional medicine in the world, Chinese traditional medicine (CTM) has a long history, which is a treasure of the combination of medicine and Chinese classical culture even more than 5000 years. For thousands of years, CTM has made great contributions to the reproduction and health of the Chinese people. It was an efficient therapeutic tool under the guidance of Chinese traditional medical theory, its source is generally natural products, but there are also a small number of it are natural products after some processing methods. In fact, the definition of Chinese medicine (CM) includes both traditional and new CM developed by modern technology. It is well known that the chemical composition of most CM and natural products is very complex, for example, a single herb may contain hundreds of different chemicals, including active ingredients, side effects, and even toxic ingredients. Therefore, the extraction process is particularly crucial for the quality and clinical efficacy of CM and natural products. In this work, a new classification method was proposed to divide the extraction technologies of CM and natural products into 21 kinds in recent years and analyze their status, advantages, and disadvantages. Then put forward a new technical route based on ultra-high-pressure extraction technology for rapid extraction else while removing harmful impurities and making higher utilization of CM and natural products. It is a useful exploration for the extraction industry of medicinal materials and natural products in the world.

Integrative analysis of the molecular signature of target genes involved in the antitumor effects of cantharidin on hepatocellular carcinoma

BackgroundCantharidin (CTD) is the active ingredient of Chinese medicine, which has been traditionally used in multiple cancers treatment, especially in hepatocellular carcinoma (HCC). However, a comprehensive analysis of the CTD-related molecular mechanism is still necessary to understand its functions in HCC treatment. This study aimed to reveal the novel molecular targets and regulatory networks of CTD in HCC.MethodsA model of H22 tumour-bearing mice was constructed, and the function of CTD in tumour growth was evaluated. An integrated approach of CTD associated transcriptional profiling and biological systems analysis was used to identify key regulators involved in antitumour pathways. The identified differential expression patterns were supported by the results of Gene Ontology (GO) term and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyse, and by protein-protein interaction (PPI) network construction. The relationships between gene expression and tumour immunity were evaluated using Tumour Immune Estimation Resource (TIMER). Prognostic value was analyzed with Kaplan-Meier plotter.ResultsIn the present study, the therapeutic effect of CTD on HCC was evaluated in vivo. We obtained the CTD-related transcriptional profiles, systematically and intuitively illustrated its possible pharmacological mechanisms in HCC through multiple targets and signalling pathways. These results revealed that the CTD-related differentially expressed genes were involved in autophagy, transcription factors (TFs) related transcriptional regulation, fatty acid metabolism and immune response in HCC. We found that MAPT, TOP2A, CENPF and MEFV were hub genes of CTD targets involved in autophagy regulation. Totally, 14 TFs have been confirmed to be critical for transcriptional regulation, and 33 TF targets were identified as the hub genes in transcriptional mis-regulation pathway in cancer. These TFs were associated with the immune response and immune cell infiltration. In addition, the downregulated genes were significantly enriched in metabolic regulation pathways, especially fatty acid metabolism after CTD treatment. Furthermore, the network of CTD associated miRNAs with these fatty acid metabolism-related targets was constructed in HCC.ConclusionsTaken together, our results comprehensively elucidated that CTD could act on multiple targets in HCC therapy, affecting autophagy, transcriptional regulation, the immune response and fatty acid metabolism. Our results provide a foundation for the study of the molecular mechanistic of CTD and its clinical application in the treatment of HCC.

Active ingredients of Chinese medicine with immunomodulatory properties: NF-κB pathway and Parkinson's disease

Parkinson's disease (PD) is a neurodegenerative disease with a complex pathogenesis and no cure. Persistent neuroinflammation plays an important role in the development of PD, and activation of microglia and astrocytes within the central nervous system leads to an inflammatory response and production of pro-inflammatory factors, and activation of NF-κB is key to neuroglial activation in chronic inflammation in PD and a hallmark of the onset of neuroinflammatory disease. Therefore, inhibiting NF-κB activation to prevent further loss of dopaminergic nerves is a more effective means of treating PD. It has been found that an increasing number of active ingredients in Chinese medicines, such as flavonoids, alkaloids, saponins, terpenoids, phenols and phenylpropanoids, have anti-inflammatory properties that can regulate neuroglia cell activation and ameliorate neuroinflammation through the NF-κB pathway, and increase dopamine release or protect dopaminergic neurons for neuroprotection to improve behavioural dysfunction in PD. The active ingredients of traditional Chinese medicine are expected to be good candidates for the treatment of PD, as they provide holistic regulation through multi-targeting and multi-level effects, and are safe, inexpensive and readily available. Therefore, this paper summarises that the active ingredients of some relevant Chinese medicines ameliorate the symptoms of PD and delay the development of PD by inhibiting glial cell-mediated neuroinflammation through the NF-κB pathway, which may provide new ideas for exploring the molecular mechanism of PD pathogenesis and developing new anti-PD drugs.

Celastrol alleviated acute kidney injury by inhibition of ferroptosis through Nrf2/GPX4 pathway

Ferroptosis is an important pathological process in acute kidney injury (AKI) which could lead to chronic kidney disease (CKD) and end-stage renal disease (ESRD). As an active ingredient of Chinese medicine Tripterygium wilfordii, celastrol has been reported to alleviate inflammation and preclinical studies have confirmed its anticancer effect. In the present study, we investigated the renal protective effects of celastrol against cisplatin induced AKI. Mice were administrated cisplatin by intraperitoneal injection and we found that celastrol reduced serum levels of BUN and creatinine, inhibited renal dysfunction, inflammation and oxidative stress. In addition, renal iron accumulation and ferroptosis were significantly reduced by celastrol treatment. Further mechanistic analyses suggested that Nrf2 is essential for celastrol upregulated GPX4 to alleviate ferroptosis and reduction of LDH release, intracellular iron accumulation and lipid peroxidation. These findings expand the potential uses of celastrol for treatment of various kinds of AKI associated with ferroptosis.

The preventive effect of secondary metabolites of Dendrobium officinale on acute alcoholic liver injury in mice

Dendrobium officinale (D. officinale) is a valuable Chinese herbal medicine and rich in chemical components. The current research on the pharmacological active ingredients of D. officinale mainly focus on polysaccharides, however, there are very few studies on the activity of its secondary metabolites. Our study aimed to investigate the potential pharmacological activity of secondary metabolites of D. officinale. Firstly, we determined the polysaccharide content of D. officinale from four different origins and analyzed their secondary metabolites using UPLC Q-TOF/MS. We found that the average polysaccharide content of D. officinale from Anlong, Guizhou was the lowest, and the secondary metabolites were also significantly different from those of Dendrobium from the other three origins. Then, ten differential compounds with high content in D. officinale from Anlong, Guizhou were identified using Orthogonal Projection to Latent analysis (OPLS-DA), and the potential targets of these secondary metabolites associated with acute alcoholic liver injury through network pharmacology. Finally, pharmacodynamic experiments verified that only D. officinale from Anlong significantly improved liver damage in mice with acute alcoholic liver injury, confirming the pharmacodynamic activity of D. officinale secondary metabolites in the prevention of acute alcoholic liver injury. The present study found that the preventive effect of D. officinale on acute alcoholic liver injury in mice was not directly correlated with the polysaccharide content, indicating that the polysaccharide content alone cannot be used as a quality indicator to evaluate the medicinal activity of D. officinale. Our study provides more references for the study of the substance basis of the pharmacological effect of D. officinale, and also provides a research idea and method for the discovery of the pharmacological active ingredients of Chinese medicine.

Nanocarriers for Active Ingredients of Chinese Medicine (AIFCM) Used in Gastrointestinal Cancer Therapy

Active ingredients of Chinese medicine (AIFCM) are pharmacological substances taken from traditional Chinese medicine that show promise in treating gastrointestinal cancer. Compared with traditional chemotherapeutic drugs, AIFCM have advantages such as multi-target and multi-level treatment of gastrointestinal cancer. Nanocarriers have the following advantages, better bioavailability, passive or active targeting of tumor sites and responsive release of drugs. The use of nanocarriers for delivery of AIFCM in treatment of gastrointestinal cancer, can overcome the disadvantages of some AIFCM, such as insolubility and low bioavailability. In this review, we first outline the background on gastrointestinal cancer, main curative factors and conventional therapeutic approaches. Then, the mechanisms for AIFCM in gastrointestinal cancer therapy are presented in the following four aspects: gene regulation, immune modulation, cellular pathway transduction, and alteration of intestinal flora. Thirdly, preparation of various nanocarriers and results when combining AIFCM in gastrointestinal cancer are presented. Fourth, application of novel targeted nanocarriers and responsive nanocarriers in gastrointestinal tumors is further introduced. Finally, the application of AIFCM in the treatment of gastrointestinal cancer is summarized and prospected, hoping to shed some light on the nanocarrier-bound AIFCM in the treatment of gastrointestinal cancer.

Anti-photoaging effects and mechanisms of active ingredients of Chinese medicine: a review

Skin photoaging is exogenous aging caused by long-term ultraviolet radiation, which not only affects skin appearance, but also has a close relationship with the development of skin cancer. Saponins, flavonoids, polyphenols, polysaccharides, and extracts of Chinese medicine have been found to have anti-skin photoaging effects in recent studies. Various mechanisms such as anti-oxidative stress damage, inhibition of matrix metalloproteinase expression, promotion of collagen synthesis, inhibition of inflammatory response, DNA damage repair, enhancement of cell autophagy, and inhibition of melanin synthesis can improve the symptoms of skin photoaging and delay the photoaging process. With the active ingredients of Chinese medicine for anti-skin photoaging as the entry point, the study systematically discussed the research progress of the mechanisms underlying the anti-photoaging effects of active ingredients of Chinese medicine in recent years, in order to provide theoretical reference for the development of new anti-photoaging drugs and methods.

Mitophagy mediated by ligustilide relieves OGD/R-induced injury in HT22 cells

Mitochondrion, as the main energy-supply organelle, is the key target region that determines neuronal survival and death during ischemia. When an ischemic stroke occurs, timely removal of damaged mitochondria is very important for improving mitochondrial function and repairing nerve damage. This study investigated the effect of ligustilide(LIG), an active ingredient of Chinese medicine, on mitochondrial function and mitophagy based on the oxygen and glucose deprivation/reperfusion(OGD/R)-induced injury model in HT22 cells. By OGD/R-induced injury model was induced in vitro, HT22 cells were pre-treated with LIG for 3 h, and the cell viability was detected by the CCK-8 assay. Immunofluorescence and flow cytometry were used to detect indicators related to mitochondrial function, such as mitochondrial membrane potential, calcium overload, and reactive oxygen species(ROS). Western blot was used to detect the expression of dynamin-related protein 1(Drp1, mitochondrial fission protein) and cleaved caspase-3(apoptotic protein). Immunofluorescence was used to observe the co-localization of the translocase of outer mitochondrial membrane 20(TOMM20, mitochondrial marker) and lysosome-associated membrane protein 2(LAMP2, autophagy marker). The results showed that LIG increased the cell viability of HT22 cells as compared with the conditions in the model group. Furthermore, LIG also inhibited the ROS release, calcium overload, and the decrease in mitochondrial membrane potential in HT22 cells after OGD/R-induced injury, facilitated Drp1 expression, and promoted the co-localization of TOMM20 and LAMP2. The findings indicate that LIG can improve the mitochondrial function after OGD/R-induced injury and promote mitophagy. When mitophagy inhibitor mdivi-1 was administered, the expression of apoptotic protein increased, suggesting that the neuroprotective effect of LIG may be related to the promotion of mitophagy.

Identification of the potential mechanism of Radix pueraria in colon cancer based on network pharmacology

Radix Puerariae (RP), a dry root of Pueraria lobata (Willd.) Ohwi, is used to treat a variety of diseases, including cancer. Several in vitro and in vivo studies have demonstrated the efficacy of RP in the treatment of colon cancer (CC). However, the biological mechanism of RP in the treatment of colon cancer remains unclear. In this study, the active component of RP and its potential molecular mechanism against CC were studied by network pharmacology and enrichment analysis. The methods adopted included screening active ingredients of Chinese medicine, predicting target genes of Chinese medicine and disease, constructing of a protein interaction network, and conducting GO and KEGG enrichment analysis. Finally, the results of network pharmacology were further validated by molecular docking experiments and cell experiments. Eight active constituents and 14 potential protein targets were screened from RP, including EGFR, JAK2 and SRC. The biological mechanism of RP against CC was analysed by studying the relationship between active components, targets, and enrichment pathways. These findings provide a basis for understanding the clinical application of RP in CC.

Paeoniflorin ameliorates oxidase stress in Glutamate-stimulated SY5Y and prenatally stressed female offspring through Nrf2/HO-1 signaling pathway

BackgroundPrenatal stress (PS) can cause brain retardation, reduce the learning and memory ability of the offspring and significantly increase the incidence of depression in offspring. Paeoniflorin (PF), a kind of monoterpenoid glycoside, is one of the main active ingredients of Chinese Medicine Paeonia lactiflora Pall, has anti-inflammation and potential neuroprotective effects. However, few reports have shown that the neuroprotective effects of PF are exerted through ameliorating Glutamate toxicity in vivo and in vitro. MethodsHere, we used a prenatal restraint stress model and Glu-induced excitotoxic neurotoxicity in SH-SY5Y cells to study the effects of PF. ResultsOur results showed that PF can ameliorate learning and memory impairments and increases the density of hippocampal neurons, typical Golgi-positive pyramidal cells, and neuronal Neurogranin (Ng) expression in PS rat offspring. Furthermore, PF can significantly up-regulate the decrease of Glu-induced SH-SY5Y cell viability. At the same time, PF can significantly reduce apoptosis, ROS, NO levels, and intracellular Ca2+ concentration, and significantly inhibit the increase of mitochondrial membrane potential. Besides, PF significantly increased the expression of Nrf2 and iNOS, decreased p-JNK/JNK, p-P38/P38, Bax/Bcl-2, active-caspase-3, and active-caspase-9. ConclusionsOur results demonstrate that PF may be an effective treatment in preventing the development of PS-induced learning and memory impairment and have therapeutic potential in Glu-related neurological diseases.

Combination of a biopharmaceutic classification system and physiologically based pharmacokinetic models to predict absorption properties of baicalein in vitro and in vivo

To determine the in vitro and in vivo absorption properties of active ingredients of the Chinese medicine, baicalein, to enrich mechanistic understanding of oral drug absorption. The Biopharmaceutic Classification System (BCS) category was determined using equilibrium solubility, intrinsic dissolution rate, and intestinal permeability to evaluate intestinal absorption mechanisms of baicalein in rats in vitro . Physiologically based pharmacokinetic (PBPK) model commercial software GastroPlus™ was used to predict oral absorption of baicalein in vivo . Based on equilibrium solubility, intrinsic dissolution rate, and permeability values of main absorptive segments in the duodenum, jejunum, and ileum, baicalein was classified as a drug with low solubility and high permeability. Intestinal perfusion with venous sampling (IPVS) revealed that baicalein was extensively metabolized in the body, which corresponded to the low bioavailability predicted by the PBPK model. Further, the PBPK model predicted the key indicators of BCS, leading to reclassification as BCS-II. Predicted values of peak plasma concentration of the drug (C max ) and area under the curve (AUC) fell within two times of the error of the measured results, highlighting the superior prediction of absorption of baicalein in rats, beagles, and humans. The PBPK model supported in vitro and in vivo evidence and provided excellent prediction for this BCS class II drug. BCS and PBPK are complementary methods that enable comprehensive research of BCS parameters, intestinal absorption rate, metabolism, prediction of human absorption fraction and bioavailability, simulation of PK, and drug absorption in various intestinal segments across species. This combined approach may facilitate a more comprehensive and accurate analysis of the absorption characteristics of active ingredients of Chinese medicine from in vitro and in vivo perspectives.

Icariin reduces Glu-induced excitatory neurotoxicity via antioxidative and antiapoptotic pathways in SH-SY5Y cells.

Excessive glutamate (Glu) can lead to significant effects on neural cells through the generation of neurotoxic or excitotoxic cascades. Icariin (ICA) is a main active ingredient of Chinese Medicine Berberidaceae epimedium L., and has many biological activities, such as antiinflammation, antioxidative stress, and anti-depression. This study aims to evaluate the effect of ICA on Glu-induced excitatory neurotoxicity of SH-SY5Y cells. The cell viability assay was evaluated by the CCK-8 assay. The apoptosis, reactive oxygen species (ROS), and mitochondrial membrane potential were assessed by flow cytometry. Intracellular Ca2+ concentration was determined by using the fluorescent probe Fluo-3. Protein expression was detected by western blotting analysis. ICA can significantly enhance the SH-SY5Y cell viability reduced by Glu. At the same time, ICA can significantly reduce apoptosis, ROS, nitric oxide (NO) levels, and intracellular Ca2+ concentration, and significantly inhibit the increase of mitochondrial membrane potential. In addition, ICA significantly increased the expression of P47phox and iNOS, decreased p-JNK/JNK, p-P38/P38, Bax/Bcl-2, active caspase-3, and active caspase-9. These results indicate that ICA may reduce the excitatory neurotoxicity of Glu-induced SH-SY5Y cells through suppression of oxidative stress and apoptotic pathways, suggesting that ICA could be a potential therapeutic candidate for neurological disorders propagated by Glu toxicity.

Anti-Tumor Mechanisms Associated With Regulation of Non-Coding RNA by Active Ingredients of Chinese Medicine: A Review.

Cancer has become the second leading cause of death worldwide; however, its complex pathogenesis remains largely unclear. Previous research has shown that cancer development and progression are closely associated with various non-coding RNAs, including long non-coding RNAs and microRNAs, which regulate gene expression. Target gene abnormalities are regulated and engaged in the complex mechanism underlying tumor formation, thereby controlling apoptosis, invasion, and migration of tumor cells and providing potentially effective targets for the treatment of malignant tumors. Chemotherapy is a commonly used therapeutic strategy for cancer; however, its effectiveness is limited by general toxicity and tumor cell drug resistance. Therefore, increasing attention has been paid to developing new cancer treatment modalities using traditional Chinese medicines, which exert regulatory effects on multiple components, targets, and pathways. Several active ingredients in Chinese medicine, including ginsenoside, baicalin, and matrine have been found to regulate ncRNA expression levels, thus, exerting anti-tumor effects. This review summarizes the scientific progress made regarding the anti-tumor mechanisms elicited by various active ingredients of Chinese medicine in regulating non-coding RNAs, to provide a theoretical foundation for treating tumors using traditional Chinese medicine.

Emodin alleviates LPS-induced inflammatory response in lung injury rat by affecting the function of granulocytes

BackgroundAcute lung injury (ALI) and/or acute respiratory distress syndrome (ARDS) are critical life-threatening syndromes characterized by the infiltration of a large number of granulocytes (mainly neutrophils) that lead to an excessive inflammatory response. Emodin (Emo) is a naturally occurring anthraquinone derivative and an active ingredient of Chinese medicine. It is believed to have anti-inflammatory effects. In this study, we examined the impact of Emo on the pulmonary inflammatory response and the granulocytes function in a rat model of lipopolysaccharide (LPS)-induced ALI.ResultsTreatment with Emo protected rat against LPS-induced ALI. Compared to untreated rat, Emo-treated rat exhibited significantly ameliorated lung pathological changes and decreased tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β). However, Emo has no protective effect on the rat model of acute lung injury with granulocyte deficiency. In addition, treatment with Emo enhanced the bactericidal capacity of LPS-induced granulocytes via the up-regulation of the ability of granulocytes to phagocytize bacteria and generate neutrophil extracellular traps (NETs). Emo also downregulated the respiratory burst and the expression of reactive oxygen species (ROS) in LPS-stimulated granulocytes, alleviating the damage of granulocytes to surrounding tissues. Finally, Emo can accelerate the resolution of inflammation by promoting apoptosis of granulocytes.ConclusionOur results provide the evidence that Emo could ameliorates LPS-induced ALI via its anti-inflammatory action by modulating the function of granulocytes. Emo may be a promising preventive and therapeutic agent in the treatment of ALI.

Research progress on mechanism of active ingredients in traditional Chinese medicine for gastric cancer

Gastric cancer is a disease with high mortality, which threatens the health of people for a long time. At present, the main treatment methods are surgery and chemotherapy, but these methods have great harm to the human body. However, it is found that the active ingredients of traditional Chinese medicine have an obvious therapeutic effect in the adjuvant treatment of the tumor. Therefore, the active ingredients of traditional Chinese medicine have become a research hotspot in the anti-tumor field. In recent years, many related researchers have been particularly active in studying the in vitro activity and mechanism of active ingredients of traditional Chinese medicine on human gastric cancer cells. In this paper, the Chinese herbal medicine extracts, polysaccharides, alkaloids, saponins, flavones, terpenes, quinones, volatile oils, esters, phenols, protein components and other active ingredients of Chinese medicine were used as the starting points to investigate the anti-gastric cancer mechanism, such as inhibiting cell proliferation and inducing apoptosis of cancer cells, inhibiting cell invasion and migration; inhibiting over-expression of vascular endothelial growth factor(VEGF); interfering with cell mitosis; and regulating cell signaling pathways. Their in vitro inhibitory activity and mechanism for gastric cancer cells were described in this study, providing a theoretical reference for the development and application of anti-gastric cancer drugs.

Nano-carriers for delivery and targeting of active ingredients of Chinese medicine for hepatocellular carcinoma therapy

Active ingredients from Chinese medicine (AIFCM) are emerging as a class of anticancer agents for treating hepatocellular carcinoma (HCC). AIFCM have unique advantages over traditional chemotherapeutic drugs, such as their multi-target, multi-level, and coordinated intervention effects against HCC. Recent researches demonstrated their potentials in inhibiting HCC initiation, cell proliferation, angiogenesis, and metastasis. With the advantages of nano-carriers including better bioavailability, significant features of passive or active targeting and stimulus-responsive drug release. Formulation of AIFCM and nano-carriers shows great potential in promoting anti-HCC therapeutic development. Here, we critically assess nano-carriers for delivery and targeting of AIFCM for HCC therapy. First, we offer an overview of major pathogenic factors to induce HCC, including virus infection, alcoholic liver disease, mycotoxin, obesity, and type 2 diabetes. Second, the mechanisms of AIFCM for HCC therapy comprising gene regulation and transduction of different molecular pathways are discussed. Third, significant achievements of AIFCM-encapsulated nano-carriers and AIFCM-modified nano-carriers against HCC are presented. Finally, we provide concluding remarks and future perspectives of AIFCM for HCC therapy, hoping to offer some insight on how to improve AIFCM-based HCC therapy.

Celastrol ameliorates cisplatin nephrotoxicity by inhibiting NF-κB and improving mitochondrial function.

BackgroundCelastrol is an active ingredient of Chinese medicine Tripterygium wilfordii which is clinically used to treat the immune diseases. Currently, celastrol is documented as a potent agent for treating cancer and inflammatory disorders. This study was to investigate the effect of celastrol on cisplatin nephrotoxicity and the underlying mechanism.MethodsMale C57BL/6 mice were treated with cisplatin (20 mg/kg) with or without celastrol treatment (1 and 2 mg/kg/day). In vitro, human proximal tubule epithelial cell line (HK−2) and mouse renal tubule epithelial cells (RTECs) were treated with cisplatin (5 μg/mL) with or without celastrol administration. Then renal injury and cell damage were evaluated.FindingsIn vivo, after celastrol treatment, cisplatin-induced kidney injury was significantly ameliorated as shown by the improvement of renal function (BUN, serum creatinine, and cystatin C), kidney morphology (PAS staining) and oxidative stress (MDA) and the suppression of renal tubular injury markers of KIM-1 and NGAL. Meanwhile, the renal apoptosis and inflammation induced by cisplatin were also strikingly attenuated in celastrol-treated mice. In vitro, celastrol treatment markedly inhibited cisplatin-induced renal tubular cell apoptosis, suppressed NF-κB activation, and improved mitochondrial function evidenced by the restored mtDNA copy number, mitochondrial membrane potential, and OXPHOS activity in cisplatin-treated renal tubular epithelial cells.InterpretationThis work suggested that celastrol could protect against cisplatin-induced acute kidney injury possibly through suppressing NF-κB and improving mitochondrial function.FundThe National Natural Science Foundation of China, National Key Research and Development Program, and Natural Science Foundation of Jiangsu Province.

Magnetic core/shell Fe3O4/Au nanoparticles for studies of quinolones binding to protein by fluorescence spectroscopy.

Magnetic core/shell Fe3O4/Au nanoparticles were used in the determination of drug binding to bovine serum albumin (BSA) using a fluorescence spectroscopic method. The binding constants and number of binding sites for protein with drugs were calculated using the Scatchard equation. Because of their superparamagnetic and biocompatible characteristics, magnetic core/shell Fe3O4/Au nanoparticles served as carrier proteins for fixing proteins. After binding of the protein to a drug, the magnetic core/shell Fe3O4/Au nanoparticles-protein-drug complex was separated from the free drug using an applied magnetic field. The free drug concentration was obtained directly by fluorescence spectrometry and the proteins did not influence the drug determination. So, the achieved number of binding sites should be reliable. The binding constant and site number for ciprofloxacin (CPFX) binding to BSA were 2.055 × 10(5) L/mol and 31.7, and the corresponding values for norfloxacin (NOR) binding to BSA were 1.383 × 10(5) L/mol and 38.8. Based on the achieved results, a suitable method was proposed for the determination of binding constants and the site number for molecular interactions. The method was especially suitable for studies on the interactions of serum albumin with the active ingredients of Chinese medicine.

Dissecting active ingredients of Chinese medicine by content-weighted ingredient-target network.

Chinese medicine has been widely used in clinical practice, but its mode of action often remains obscure. This has seriously hindered further development and better clinical applications of Chinese medicine. Among the most critical questions to be addressed, the identification of active ingredients is an important one requiring more research. Existing methods are only concerned the potential pharmacological effects of the individual purified chemical ingredients without consideration of the contents of these ingredients, which is critical to the comprehensive effect of Chinese medicine. A novel approach was proposed here to integrate network pharmacology analysis and ingredient content in Chinese medicine to identify active ingredients. The therapeutic action of Xuesaitong (XST) injection on myocardial infarction was analyzed as an example in this study. Firstly, we built a cardiovascular disease (CVD) related protein-protein interaction (PPI) network. Secondly, the potential targets of the ingredients of XST were identified by integrating microarray data, text mining and pharmacophore model-based prediction. The target-ingredient relationships were then mapped to the network. Topological attributes related to the targets of these ingredients, together with the ingredients' contents, were combined to calculate a composition-weighted index for integrative evaluation of ingredient efficacy. Our results indicated that major active ingredients in XST were notoginsenoside R1, ginsenoside Rg1, Rb1, Rd and Re, which was further validated on myocardial infarction rat models. In conclusion, this study presented a novel approach to identify active ingredients in Chinese medicine.

Separation/Richment Total Flavonoids in Phellinus Igniarius by Ionic Liquid/Salt Aqueous Two-phase Flotation

Ionic liquid/salt aqueous two-phase flotation coupled with UV spectrophotometry was developed for the separation/enrichment and analysis of total flavonoids in Phellinus igniarius(Sanghuang).The method was combined with ionic liquid aqueous two-phase system based on ionic liquid(1-butyl-3-methylimidazolium chloride,Cl) and inorganic salt(K2HPO4) with solvent sublation.The effect on the flotation efficiency was studied.The best conditions were as follows: the concentration of K2HPO4 was 50%;pH of solution was 9.53;the amount of Cl was 3 mL;the flotation time was 50 min;the nitrogen flow rate was 30 mL/min.The flotation efficiency was 85.31%,the enrichment factor was 8.59.These values are higher and larger than those of two-phase extraction.The method is suitable for the separation and enrichment of the active ingredient of Chinese medicine.