RESUMO
Objective Aiming at the problem that mechanical properties for the continuum of muscle tissues cannot be considered in active and passive behaviors of different structurally coupled muscles, a method of passive and active coupling in the same constitutive equation was proposed to construct ahyperelastic active and passive constitutive model of skeletal muscle continuum. Methods In order to calibrate parameters of the passive constitutive model, the uniaxial tensile experiment method and conditions were given, and through theoretical derivation, the specific method of using experimental data to solve the passive model parameters was introduced. In order to verify effectiveness of the active model, the model was verified with an example. Results The curves predicted by the model were in good agreement with the experimental output stress-stretch ratio curves. At the same strain, the maximum error of passive stress and total stress were only 20 kPa and 40 kPa. Conclusions The continuum hyperelastic constitutive model can better simulate active and passive behavior of skeletal muscles, which is beneficial for modeling and simulation of human muscles in further study.
RESUMO
Objective To establish an infrared spectroscopic method for the rapid qualitative and quantitative analysis of caffeine and sodium benzoate in Annaka samples. Methods Qualitative and quantitative modeling samples were prepared by mixing high-purity caffeine and sodium benzoate. The characteristic absorption peaks of caffeine and sodium benzoate in Annaka samples were determined by analyzing the infrared spectra of the mixed samples. The quantitative model of infrared spectra was established by partial least squares (PLS). Results By analyzing the infrared spectra of 17 mixed samples of caffeine and sodium benzoate (the purity of caffeine ranges from 10% to 80%), the characteristic absorption peaks for caffeine were determined to be 1 698, 1 650, 1 237, 972, 743, and 609 cm-1. The characteristic absorption peaks for sodium benzoate were 1 596, 1 548, 1 406, 845, 708 and 679 cm-1. When the detection of all characteristic absorption peaks was the positive identification criteria, the positive detection rate of caffeine and sodium benzoate in 48 seized Annaka samples was 100%. The linear range of PLS quantitative model for caffeine was 10%-80%, the coefficient of determination ( R2) was 99.9%, the root mean square error of cross validation (RMSECV) was 0.68%, and the root mean square error of prediction (RMSEP) was 0.91%; the linear range of PLS quantitative model for sodium benzoate was 20%-90%, the R2 was 99.9%, the RMSECV was 0.91% and the RMSEP was 1.11%. The results of paired sample t test showed that the differences between the results of high performance liquid chromatography method and infrared spectroscopy method had no statistical significance. The established infrared quantitative method was used to analyze 48 seized Annaka samples, the purity of caffeine was 27.6%-63.1%, and that of sodium benzoate was 36.9%-72.3%. Conclusion The rapid qualitative and quantitative analysis of caffeine and sodium benzoate in Annaka samples by infrared spectroscopy method could improve identification efficiency and reduce determination cost.
Assuntos
Cafeína , Cromatografia Líquida de Alta Pressão , Análise dos Mínimos Quadrados , Benzoato de Sódio , Espectroscopia de Luz Próxima ao InfravermelhoRESUMO
Objective:The methods of network pharmacology were adopted to predict Multi-component Chinese Medicine (MCCM) with anti-tumor activity from Shuanghuanglian (SHL). Furthermore, the pharmaceutical activity of CT26 colon cancer was verified in vitro and in vivo. Method:Based on the Traditional Chinese Medicine Systems Pharmacology Database (TCMSP), the Handbook of Active Components Analysis of Traditional Chinese Medicine, the Drugbank database, the Reactome database, and the Human protein reference database (HPRD), the protein-protein interactions network (PPI) and the drug target network were built and resolved. The data was mined to discover the pharmacological effect. The anti- tumor activity of components from SHL was determined based on the nearest distance rule between the compounds and the nodes of network. And then, the anti-tumor effect of the MCCM was verified in vitro and in vivo. Result:The 3 combined compounds, baicalin, forsythoside A and chlorogenic acid with the anti-tumor activity from SHL were predicted and discovered. The verification results showed that the combination of baicalin-forsythoside A-chlorogenic acid could significantly inhibit the cell proliferation and migration compared with the control group in vitro (P<0.01). Among CT26 bearing mice, the tumor volume and weight were significantly decreased after the combined administration of baicalin-forsythoside A-chlorogenic acid compared with the model group in vivo (P<0.01). Conclusion:By the methods of network pharmacology, the anti-tumor activities of component of from SHL were discovered. According to the verification in vitro and in vivo, the combination of baicalin-forsythoside A-chlorogenic acid could play better anti-CT26 tumor activity.
RESUMO
Objective:To evaluate the clinical efficacy of Xuanfei Huazhuo prescription in the treatment of coronavirus disease-2019 (COVID-19). Method:A total of 40 patients with COVID-19 were selected and treated with Xuanfei Huazhuo prescription. The changes of body temperature, clinical symptoms, computed tomography (CT), blood routine and biochemical indexes were observed before and after treatment. Result:The 40 patients included 15 males and 25 females, with a male to female ratio of 1∶1.7. They were aged between 20-94 years old, with the average age of (43.9±16.3) years old. The course of disease was 8-23 days, with the average of (14±4.4) days. Compared with before administration, the patients' clinical symptoms, such as cough, fever, sputum, diarrhea, loss of appetite and fatigue, were all improved (P<0.05). Before treatment the traditional Chinese medicine (TCM) syndromes of patients were mainly cold dampness lung (57.5%) and cold dampness Lung (42.5%), and the tongue coating was mainly white greasy coating (52.9%). After adjuvant treatment with Xuanfei Huazhuo prescription, the fever removal time was (2.48±2.56) days; white blood cell (WBC), lymphocyte percentage (LYM%), neutrophil percentage (NEUT%), absolute value of lymphocytes (LYM #) indexes of C-reactive protein (CRP), erythrocyte sedimentation rate (ESR), total bilirubin (TBIL), ratio of glutamic oxaloacetic transaminase to glutamic pyruvic transaminase (AST/ALT) and lactate dehydrogenase (LDH) were basically restored to the normal range (P<0.05) compared with before administration. After adjuvant treatment with Xuanfei Huazhuo prescription, the results of three pharyngeal test virus nucleic acid tests were negative, and the lung CT showed that infected lesions were absorbed and all met the discharge criteria. All 40 patients met the discharge criteria and were all cured and discharged, with a cure rate of 100%. There has been no case of recurrence with a positive result of nucleic acid detection so far. The score of symptom and clinical index of patients after administration was (1.62±1.90), which was significantly lower than that before administration (7.65±4.08, P<0.05). Conclusion:In the adjuvant treatment of COVID-19, Xuanfei Huazhuo prescription can reduce body temperature, promote the absorption of pulmonary inflammation, and improve clinical symptoms, such as fever and cough.
RESUMO
The components of traditional Chinese medicine(TCMCs) are the basic unit of raw materials for Chinese medicines, and their physical and chemical properties directly affect the choice of dosage forms and the optimization of prescriptions. However, most of TCMCs are multi-component complex systems, and the characterization of their overall properties is still in the exploration stage. On the basis of biological activity, the representative components are determined, and then the individual characteristics are fitted with the weight coefficient of efficacy contribution rate, which may provide reference for characterizing the overall properties of TCMCs. In this study, with the pharmacological effects of isoproterenol(ISO)-induced myocardial ischemia in rats as the indicators, the pharmacodynamic contribution rates of three representative components of chishao terpene glucoside components(CSTGCs) were evaluated by the normalization weighting method. The contribution rates of paeoniflorin, paeoniflorin and benzoylpaeoniflorin were 54.87%, 32.46% and 12.67%, respectively. The oil-water partition coefficients of paeoniflorin, albiflorin, benzoylpaeoniflorin in water and buffer solutions with different pH values were measured, and the oil-water partition coefficients of CSTGCs were characterized by the weight of their pharmacodynamics contribution rate. The results showed that the apparent oil-water partition coefficient(log P) of CSTGCs in the phosphate buffer system such as n-octanol-water(pH 2.0, 2.5, 5.0, 5.8, 6.8) were 0.18-0.22, indicating that CSTGCs have common absorption and low permeability, providing basis for the preparation of CSTGCs.
Assuntos
Animais , Ratos , Doença da Artéria Coronariana , Glucosídeos , Medicina Tradicional Chinesa , Isquemia Miocárdica , Terpenos , ÁguaRESUMO
Preformulation research, an in-depth research for pharmacological and pharmaceutical properties of raw materials, has been widely used in the field of chemical drugs. Although traditional Chinese medicine components (TCMCs) are the basic units in Chinese medicine preparation, the properties characterization of these components is still in an exploratory stage, because empiricism and blindness are still present in the development of the Chinese medicine preparations. TCMCs, a complex multi-component system, is very difficult to be analyzed in details. Herein, a research idea is put forward for the characterization of overall properties by using representative compositions. Firstly, various composition groups were set up for screening the representative components by in vitro and in vivo efficacy evaluation according to the original proportion. Then the equilibrium solubility, oil/water (O/W) partition coefficient and apparent permeability coefficient of the representative components were detected. Subsequently, the similarity assessment and discrete analysis were performed for the subdivision of TCMCs. The overall properties of TCMCs were fitted by mass fraction or efficacy contribution of each representative component, so as to characterize the overall properties of components/sub-components.
Assuntos
Medicamentos de Ervas Chinesas , Medicina Tradicional Chinesa , SolubilidadeRESUMO
Epimedii Folium, a famous traditional Chinese medicine made of dried leaves of Epimedium brevicomu, E. pubescens, E. sagittatum or E. koreanum, has been applied in China for several thousand years as a medicine. It has the function of reinforcing kidney Yang, strengthening muscles and bones and dispelling rheumatism. Modern studies have shown that baohuoside Ⅰ has a low content in Herba Epimedii, but it has a wide range of pharmacological effects, such as anti-osteoporosis, anti-tumor, improving cognitive dysfunction, cerebral ischemia-reperfusion injury protection, and neuroprotection. More and more attention has been paid to the preparation methods and pharmacological effects of baohuoside Ⅰ due to its many biological activities and pharmacological effects. In this present research, in order to provide references for the better mass preparation and rational exploitation of baohuoside Ⅰ, we summarized and sorted out the preparation methods and pharmacological effects of baohuoside Ⅰ which were published in recent years.
RESUMO
The discovery and verification of components are prerequisites for developing of component preparations. The molecular docking technique and pharmacodynamic activity evaluation provide effective methods for the discovery and verification of the representative components of Chishao terpene glucoside components (CSTGCS) against ischemia and hypoxia injury. The chemical constituents of CSTGCS were analyzed qualitatively by UPLC-TOF/MS/MS. Main chemical constituents were docked with key receptor proteins of myocardial ischemia to preliminarily screen anti-ischemia active ingredients, and screening for main active ingredients with Libdockscore. Then a H9c2 cell hypoxia injury model was established, and creatine kinase (CK), lactate dehydrogenase (LDH), superoxide dismutase (SOD), malondialdehyde (MDA) were determined to screen the representative combinations in CSTGCS. In addition, apoptosis index, apoptotic protein expression and mitochondria-associated mRNA levels were determined to verify the inhibition of the representative components (RCS) on the apoptosis of hypoxic cells. Eventually, the representative components of CSTGCS were determined. The results showed that paeoniflorin, albiflorin, benzoyl paeoniflorin and oxypaeoniflorin were considered to be the main active components because of their high matching with target proteins (4TWT, 3O4O, 4KZN, 1M9J) in space and energy. There was no statistical difference in regulating CK, LDH, SOD, MDA levels and maintaining mitochondrial function as well as inhibiting cell apoptosis between CSTGCS group and RCS group (paeoniflorin + albiflorin + benzoyl paeoniflorin combination). Therefore, paeoniflorin, albiflorin and benzoyl paeoniflorin were selected as the most representative ingredients of CSTGCS against ischemia and hypoxia injury, providing a basis for the overall properties of the components and formulation of CSTGCS.
RESUMO
Ligusticum chuanxiong is one of the common traditional Chinese medicinal herbs for treating various cardiovascular and cerebrovascular diseases, and a number of previous studies have demonstrated that the extract of L. chuanxiong has strong antioxidative activity. This paper was mainly aimed to investigate the effects and possible mechanisms of L. chuanxiong extraction on oxidative stress induced by myocardial ischemia injury in rats. The rats were subcutaneously injected with isoprenaline hydrochloride to induce myocardial ischemia injury and treated for 2 weeks. Then the cardiac indexes of the rats were recorded. The concentration of malondialdehyde (MDA) and activities of serum creatine kinase (CK), lactate dehydrogenase (LDH), aspartate transaminase (AST), superoxide dismutase (SOD) and total antioxidant capacity (T-AOC) were measured by colorimetry. Light microscope was used to observe the morphological changes of myocardium, and the protein expressions of nuclear factor E2 related factor 2 (Nrf2), quinone oxidoreductase (NQO1) and hemeoxygenase-1 (HO-1) in cardiac tissue were evaluated by Western blot. The results showed that L. chuanxiong extraction could decrease cardiac indexes and the values of CK, LDH and AST in blood serum, increase activities of serum SOD and T-AOC, reduce serum MDA concentration, improve myocardium structure after ischemia injury, and up-regulate the protein expressions of Nrf2, NQO1 and HO-1 in cardiac tissue. These findings revealed that the cardioprotective effects of L. chuanxiong extraction may be related to inhibiting oxidative stress through the activation of Nrf2 signaling pathway.
RESUMO
Idiosyncratic drug-induced liver injury (IDILI) is a kind of unique adverse drug reaction with relative high morbidity compared with other idiosyncratic diseases. Its occurrence, however, has nothing to do with pharmacological effects and clinical dosage of drugs administered, and only a small number of susceptible individuals will suffer from it. Especially to deserve to be mentioned, the proportion of TCM-induced IDILI showed an ascending trend year by year. So in this article, the author has reviewed some facts related with TCM-induced IDILI, including the predisposing causes and occurrence mechanism, and tries to provide reference for the prevention, diagnosis and treatment of TCM-induced IDILI through the analysis of characteristics and research status of TCM-induced IDILI and exploration of the internal relationship between Chinese medicine constitution type and IDILI.
RESUMO
The pharmaceutical materials are divided into coarse and fine types in the development of traditional Chinese medicine preparations. Fine materials with clear composition, stable content and high quality control conform to the international development trend of traditional Chinese medicine preparations. In this paper, the status of fine materials was analyzed, and the development ideas were tentatively put forward. On the one hand, the study on simple methods and efficient equipment shall be strengthened for the simultaneous separation of multiple components of traditional Chinese medicine; on the other hand, the knowledge for traditional Chinese medicine shall be broadened to further develop the scientific compatibility of monomers under the guidance of the theory of traditional Chinese medicine.
RESUMO
In order to clarify the effect of intestinal flora on the absorption and metabolism of paeoniflorin in vivo, the metabolism of paeoniflorin by rat intestinal flora was studied under the in vitro anaerobic condition. Paeoniflorin was incubated with rat anaerobic intestinal flora for 48 h, and UPLC was used to detect the changes of paeoniflorin at different incubation time points under the following chromatographic conditions:WelchromTM C₁₈ chromatographic column (4.6 mm×100 mm, 5 μm), with 0.1% formic acid(A)-acetonitrile(B) as the mobile phase for gradient elution. The flow rate was 0.4 mL•min⁻¹, and column temperature was 30 ℃. UPLC-Q-TOF-MS with positive ion mode(ESI ion source) was applied to investigate the structural characterization of metabolic products. The structures of the metabolites were identified by accurate molecular weight, TOF-MS/MS fragmentation information, combined with retention time and literature data review, and the intestinal metabolic rules were then analyzed. After incubation for 24 h, the paeoniflorin was metabolized completely, and the resulting metabolites(albiflorin, albiflorinaglycone, deacylate albiflorin, deacylate albiflorin aglycone and paeonilactone-B) were detected in rat intestinal flora. The metabolic pathway analysis showed that the isolated rat intestinal flora first transformed peoniflorin into albiflorin, and then further metabolized by glucose removal, phenyl group removal, or four-membered ring pyrolysis and rearrangement. Paeoniflorin was gradually transformed into more hydrophobic metabolites with smaller molecular mass, which were better absorbed by the intestinal tract.
RESUMO
Exquisite materials and excellent excipients are the key parts of modern Chinese medicine development. Long-term clinical researches indicate that the meridian guided medicine has the property of carriers. In this paper, the status of the meridian guided medicine was analyzed, and the research ideas were tried to be put forward. On the one hand, to take advantage of the meridian guided action, the screening of active ingredients should be strengthened. On the other hand, the material basis and mechanism of meridian guided action were clearly explained. In summary, deep research of the meridian guided medicine can exploit the excellent excipients to promote the rapid development of modern Chinese medicine.
RESUMO
In the past several years, prevention and treatment of diabetes has become a hotspot in the research field, but there is blindness in the prevention and treatment of diabetes by Chinese materia medica (CMM). The research advances in anti-hyperglycaemic ingredients of CMM and their mechanism of action according to kinds of these compounds were summarized in this article. As the idea of application of CMM was proposed for the treatment of diabetes, the rationality of the application of CMM could be improved, the high activity of modern hypoglycemic CMM preparation could be developed.
RESUMO
OBJECTIVE: To establish an UPLC-MS/MS method for the determination of linezolid in human plasma. METHODS: The analytical column was packed with Acquity BEH C18(2.1 mm × 50 mm, 1.7 μm, Waters). The mobile phase A consisted of water(containing 0.1% formic acid), the mobile phase B consisted of acetonitrile. The analytes were eluted from the column with a linear gradient. The flow rate was 0.4 mL · min-1. A tandem mass spectrometer equipped with electrospray ionization source was used as detector multiple reaction monitoring(MRM) using the precursor to production pairs of m/z 338.2→296.2 (for linezolid) and m/2: 237.1→-194.2(for carbamazepin) were used to quantification. RESULTS: The liner range of linezolid in human plasma was 20-20 000 μg · L (r=0.9979). The limit of detection was 20 μg · L-1. Intra-day and inter-day RSD for assaying the plasma sample of linezolid were both lower than 6.26%, absolute recovery were more than 80%. CONCLUSION: The method is proved to be highly sensitive, selective, and suitable for pharmacokinetic investigations of linezolid.
RESUMO
This research is to study the relationship between HPLC fingerprints of Moutan Cortex, Paeoniae Radix Rubra and Paeoniae Radix Alba and their activity on lipopolysaccharide-induced acute lung injury. HPLC fingerprints of each extract of Moutan Cortex,Paeoniae Radix Rubra and Paeoniae Radix Alba were established by an optimized HPLC-MS method. The activities of all samples against protein and tumor necrosis a factor were tested by the model of lipopolysaccharide-induced acute lung injury. The possible relationship between HPLC-MS fingerprints and the activitieswere deduced by the Partial least squares regression analysis method. Samples were analyzed by HPLC-MS/MS to identify the major peaks. The results showed that each sample had some effect on acute lung injury. Four components with a lager contribution rate of efficacy were calculated by the research of spectrum-effect relationship. Moutan Cortex exhibited good activity on acute lung injury, and gallic acid, paeoniflorin, galloylpaeoniflorin and paeonol were the main effective components.
Assuntos
Animais , Masculino , Ratos , Acetofenonas , Química , Farmacologia , Lesão Pulmonar Aguda , Tratamento Farmacológico , Compostos Bicíclicos Heterocíclicos com Pontes , Química , Farmacologia , Cromatografia Líquida de Alta Pressão , Métodos , Medicamentos de Ervas Chinesas , Química , Farmacologia , Ácido Gálico , Química , Farmacologia , Glucosídeos , Química , Farmacologia , Lipopolissacarídeos , Farmacologia , Monoterpenos , Química , Farmacologia , Paeonia , Química , Raízes de Plantas , Química , Ratos Wistar , Espectrometria de Massas em Tandem , MétodosRESUMO
<p><b>OBJECTIVE</b>The aim of the present study was to prepare uniform-sized silybin loaded poly (lactic-co-glycolic acid) (PLGA) microspheres in study of silybin with stainless steel membrane.</p><p><b>METHOD</b>Silybin PLGA microspheres were prepared by stainless steel membrane emulsification. The preparation conditions were optimized by single-factor test and orthogonal experiment, and evaluating the mean diameters, the particle size distribution, drug loading, entrapment efficiency and morphology of microsphere.</p><p><b>RESULT</b>Prepared microspheres were round and surface was smooth. The mean diameter was (4.961 +/- 0.56) microm. The span was (1.75 +/- 0.18). The entrapment efficiency was (54.997 +/- 4.05)% and the average drug loading was (23.6 +/- 1.70)%.</p><p><b>CONCLUSION</b>The stainless steel membrane emulsification can be used to prepare the silybin PLGA microspheres. The mean diameters of the silybin PLGA microspheres can be controlled in certain level. Stainless steel membrane emulsification has great potentiality exploitation and utilization.</p>
Assuntos
Composição de Medicamentos , Métodos , Emulsões , Química , Ácido Láctico , Química , Microesferas , Tamanho da Partícula , Ácido Poliglicólico , Química , Silimarina , Química , Aço Inoxidável , QuímicaRESUMO
Chemotherapeutic drug resistance is a frequent cause of treatment failure in colon cancer patients. Several mechanisms have been implicated in drug resistance. However, they are not suffi cient to exhaustively account for this resistance emergence. In this study, two-dimensional gel electrophoresis (2-DE) and the PDQuest software analysis were applied to compare the differential expression of irinotecan-resistance-associated protein in human colon adenocarcinoma LoVo cells and irinotecan-resistant LoVo cells (LoVo/irinotecan). The differential protein dots were excised and analysed by ESI-Q-TOF mass spectrometry (MS). Fifteen proteins were identifi ed, including eight proteins with decreased expression and seven proteins with increased expression. The identifi ed known proteins included those that function in diverse biological processes such as cellular transcription, cell apoptosis, electron transport/redox regulation, cell proliferation/differentiation and retinol metabolism pathways. Identifi cation of such proteins could allow improved understanding of the mechanisms leading to the acquisition of chemoresistance.