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To improve the information service quality of the online Traditional Chinese Medicine (TCM) community, this study investigated users' information needs, feedback and the relationship between them. Using qualitative content analysis, the basic characteristics of users' needs were obtained. Logistic regression was used to explore the impact of different need characteristics of feedback. The main findings are as follows: 1) Disease consultation, health preservation, professional discussion, knowledge sharing and experience description are the major 5 types of information needs in the online TCM community; 2) Some users provided TCM-related information, such as the tongue image and the TCM four diagnosis; 3) A total of 78.8% of the posts received effective feedback, and the main types of feedback were answering, discussing, inquiring and emotional supporting; 4) Providing enough information can significantly and positively affect whether needs receive effective feedback, suggesting that users can present information about their condition in as many different formats as possible when articulating their needs.
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Medicina Tradicional Chinesa , RetroalimentaçãoRESUMO
Nanoformulations for combining chemotherapy, chemodynamic therapy, and photothermal therapy have enormous potential in tumor treatment. Coating nanoformulations with cell membranes endows them with homologous cellular mimicry, enabling nanoformulations to acquire new functions and properties, including homologous targeting and long circulation in vivo, and can enhance internalization by homologous cancer cells. Herein, we fused multifunctional biomimetic nanoformulations based on Cu-doped zeolitic imidazolate framework-8 (ZIF-8). Hydroxycamptothecin (HCPT), a clinical anti-tumor drug, was encapsulated into ZIF-8, which was subsequently coated with polydopamine (PDA) and red blood cell membrane. The as-fabricated biomimetic nanoformulations showed an enhanced cell uptake in vitro and the potential to prolong blood circulation in vivo, producing effective synergistic chemotherapy, chemodynamic therapy, and photothermal therapy under the 808 nm laser irradiation. Together, the biomimetic nanoformulations showed a prolonged blood circulation and evasion of immune recognition in vivo to provide a bio-inspired strategy which may have the potential for the multi-synergistic therapy of breast cancer.
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Estruturas Metalorgânicas , Nanopartículas , Neoplasias , Humanos , Terapia Fototérmica , Doxorrubicina , Biomimética , Fototerapia , Nanopartículas/uso terapêutico , Neoplasias/tratamento farmacológico , EritrócitosRESUMO
The fruit of Crataegus sp. is known as "Shanzha (SZ)" in China and is widely used in the food, beverage, and traditional Chinese medicine (TCM) industries. SZ usually requires thermal processing to reduce the irritation of its acidity to the gastric mucosa. Different processed products of SZ resulting from thermal processing have different or even opposite functions in clinical applications. In addition, 5-hydroxymethylfurfural (5-HMF) intermediates produced during thermal processing are carcinogenic to humans. Therefore, the aim of this study was to explore a rapid and accurate method by Fourier transform infrared spectroscopy (FT-IR) for the identification of different processed products and the determination of 5-HMF in extracts. In qualitative identification, a three-stage infrared spectroscopy identification method (raw spectra, the second derivative spectra, and two-dimensional correlation (2DCOS) spectra) was developed to distinguish different processed products of SZ step by step. In quantitative determination, partial least squares regression combined with different variable selection methods, especially the 2DCOS method, was applied to determine the 5-HMF content. The results show that temperature-induced 2DCOS synchronous spectra can effectively identify different processed products of SZ by shape, intensity, and position of auto-peaks or cross-peaks, and the variables selected by power spectra from concentration-induced 2DCOS synchronous spectra have better prediction ability for 5-HMF compared to full variables. The above results demonstrate that 2D-COS analysis is a potential tool in qualitative and quantitative analysis, which can improve sample identification accuracy and determination capabilities. This study not only establishes a rapid and accurate method for the identification of different processed products but also provides a practical reference for food safety and the efficient use of TCM.
Assuntos
Crataegus , Frutas , Humanos , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Espectrofotometria Infravermelho/métodos , Medicina Tradicional ChinesaRESUMO
There is an urgent need for research into effective interventions for pain management to improve patients' life quality. Traditional needle and syringe injection were used to administer the local anesthesia. However, it causes various discomforts, ranging from brief stings to trypanophobia and denial of medical operations. In this study, a dissolving microneedles (MNs) system made of composite matrix materials of polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA), and sodium hyaluronate (HA) was successfully developed for the loading of lidocaine hydrochloride (LidH). The morphology, size and mechanical properties of the MNs were also investigated. After the insertion of MNs into the skin, the matrix at the tip of the MNs was swelled and dissolved by absorption of interstitial fluid, leading to a rapid release of loaded LidH from MNs' tips. And the LidH in the back patching was diffused into deeper skin tissue through microchannels created by MNs insertion, forming a prolonged anesthesia effect. In addition, the back patching of MNs could be acted as a drug reservoir to form a prolonged local anesthesia effect. The results showed that LidH MNs provided a superior analgesia up to 8 h, exhibiting a rapid and long-lasting analgesic effects. Additionally, tissue sectioning and in vitro cytotoxicity tests indicated that the MNs patch we developed had a favorable biosafety profile.
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Lidocaína , Polímeros , Humanos , Anestesia Local , Álcool de Polivinil , PovidonaRESUMO
Combinations of different therapeutic strategies, including chemotherapy (CT), chemodynamic therapy (CDT), and photothermal therapy (PTT), are needed to effectively address evolving drug resistance and the adverse effects of traditional cancer treatment. Herein, a camouflage composite nanoformulation (TCBG@PR), an antitumor agent (tubercidin, Tub) loaded into Cu-doped bioactive glasses (CBGs) and subsequently camouflaged by polydopamine (PDA), and red blood cell membranes (RBCm), was successfully constructed for targeted and synergetic antitumor therapies by combining CT of Tub, CDT of doped copper ions, and PTT of PDA. In addition, the TCBG@PRs composite nanoformulation was camouflaged with a red blood cell membrane (RBCm) to improve biocompatibility, longer blood retention times, and excellent cellular uptake properties. It integrated with long circulation and multimodal synergistic treatment (CT, CDT, and PTT) with the benefit of RBCms to avoid immune clearance for efficient targeted delivery to tumor locations, producing an "all-in-one" nanoplatform. In vivo results showed that the TCBG@PRs composite nanoformulation prolonged blood circulation and improved tumor accumulation. The combination of CT, CDT, and PTT therapies enhanced the antitumor therapeutic activity, and light-triggered drug release reduced systematic toxicity and increased synergistic antitumor effects.
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Nanopartículas , Neoplasias , Humanos , Fototerapia/métodos , Terapia Fototérmica , Nanopartículas/uso terapêutico , Neoplasias/tratamento farmacológico , Membrana Celular/metabolismo , Membrana Celular/patologiaRESUMO
INTRODUCTION: The quality evaluation of Coptidis rhizome (CR) is attributed to the origin and processing method, and this strategy of ignoring the bioactive components usually leads to biased quality analysis, which is difficult to indicate the clinical efficacy. OBJECTIVES: In order to evaluate the quality level of different species of CR, we collected 20 batches of CR and investigated the fingerprint-effect relationship. METHODS: High-performance liquid chromatography (HPLC) fingerprints of CR were established, and the fingerprint-effect relationship was explored using cluster analysis, principal component analysis, Pearson correlation analysis, grey relation analysis, and partial least squares regression. RESULTS: We have identified a total of 10 common peaks (1-10) with similarity scores above 0.96. The study on the relationship between spectra and potency further showed that the contents of peaks 8, 9, and 10 are potential key components. And based on a previous study, a method of one measurement and multiple evaluations of CR was established to achieve the goal of simplifying the analytical process and reducing costs. CONCLUSION: Through a combination of fingerprint analysis, antioxidant activity evaluation, fingerprint-efficacy relationship analysis, and simultaneous quantification of multiple components, a CR quality control index and method have been selected and established, which can also provide a more comprehensive quality evaluation for traditional Chinese medicine.
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Medicamentos de Ervas Chinesas , Medicamentos de Ervas Chinesas/química , Rizoma/química , Medicina Tradicional Chinesa , Controle de Qualidade , Antioxidantes/análise , Cromatografia Líquida de Alta Pressão/métodosRESUMO
This study explored the flower visiting behaviors and pollination abilities of mason bees (Osmia excavata Alfken (Hymenoptera: Megachilidae)), bumble bees (Bombus terrestris (Linnaeus, 1758) (Hymenoptera: Apidae)), and Italian honey bees (Apis mellifera ligustica Spinola (Hymenoptera: Apidae)) in apple orchards in early spring in Jinan (located in the central region of Shandong) and Yantai (located in the Peninsula of Shandong). We compared the pollen collection patterns, flower visiting behavior, flying speed, and effects on apple pollination of the 3 types of bees. The frequencies of flower visits were significantly higher for mason bees (12.89/min in Jinan and 10.63/min in Yantai) than bumble bees and Italian honey bees in the 2 regions. The single flower residence times were significantly higher for Italian honey bees (8.22 s in Jinan and 9.43 s in Yantai), but Italian honey bees were most affected by the climate. The 3 bees differed significantly in terms of the amount of apple pollen collected and their effects on the fruit setting rate in apples (mason beesâ >â bumble beesâ >â Italian honey bees). The results showed that the mason bee was the most suitable pollinating species for spring apple orchards; Bumble bees were more suitable as alternative pollinators during cloudy and low temperatures; Italian honey bees were able to take advantage of their large number of worker bees in sunny and warm weather. Compared to individual bee species, a combination of 2 or 3 species of bees might be more advantageous in dealing with complex and variable weather conditions.
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Himenópteros , Malus , Abelhas , Animais , Polinização , Frutas , Pólen , FloresRESUMO
Swertia mussotii Franch. (SMF), a traditional Tibetan medicine, which has miraculous effect on treating hepatitis diseases. However, there is no research on its entire production process, and invisible production process has seriously hindered the SMF modern development. In this study, principal component analysis (PCA), subtractive spectroscopy, and two-dimensional correlation spectroscopy (2D-COS) were used to explain changes of characteristic groups in the extraction process. Four main characteristic peaks at 1884 nm, 1944 nm, 2246 nm and 2308 nm were identified to describe the changes of molecular structure information of total active components in SMF extraction process. In addition, multi critical quality attributes (CQAs) models were established by near-infrared spectroscopy (NIRS) combined with the total quantum statistical moment (TQSM). The coefficients of determination (R2eval and R2ival) were both greater than 0.99. The ratios of the standard deviation of validation to the standard error of the prediction (RPDe and RPDi) were greater than five. The quantitative model of AUCT could save time on primary data measurement by not requiring determination of indicator components compared with others. In conclusion, these results demonstrated that it was feasible to understand the SMF extraction process through AUCT and characteristic groups. These could realize the visual digital characterization and quality stability of the SMF extraction process.
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Swertia , Swertia/química , Espectroscopia de Luz Próxima ao InfravermelhoRESUMO
Apple pomace (AP) from the food industry is a mixture of different fractions containing bioactive polyphenolic compounds. This study provides a systematic approach toward the recovery and evaluation of the physiochemical and biological properties of polyphenolic compounds from AP. We studied subcritical water extraction (SCW) and solvent extraction with ethanol from four different AP fractions of pulp, peel, seed, core, and stem (A), peel (B), seed and core (C), and pulp and peel (D). The subcritical water method at the optimum condition resulted in total polyphenolic compounds (TPC) of 39.08 ± 1.10 mg GAE per g of AP on a dry basis compared to the ethanol extraction with TPC content of 10.78 ± 0.94 mg GAE/g db. Phloridzin, chlorogenic acid, and quercetin were the main identified polyphenolics in the AP fractions using HPLC. DPPH radical scavenging activity of fraction B and subcritical water (SW) extracts showed comparable activity to ascorbic acid while all ethanolic extracts were cytocompatible toward human fibroblast (3T3-L1) and salivary gland acinar cells (NS-SV-AC). Our results indicated that AP is a rich source of polyphenolics with the potential for biomedical applications.
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Antioxidantes , Malus , Humanos , Antioxidantes/química , Malus/química , Resíduos Industriais/análise , Polifenóis/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Etanol/química , Água , Indústria AlimentíciaRESUMO
Xinkeshu tablets (XKST), a traditional Chinese patent medicine (CPM), have served in the clinical treatment of cardiovascular diseases (CVDs) for decades. However, its pharmacodyamic material basis was still unclear, and the holistic quality control has not been well established due to the lack of systematic research on the quality markers. In this experiment, the heart rate recovery rate of a zebrafish larva was used to evaluate the traditional pharmacological effect of XKST i.e., antiarrhythmic effect. The HPLC fingerprints of 16 batches of XKST samples were obtained, and antiarrhythmic components of XKST were identified by establishing the spectrum-effect relationship between HPLC fingerprints and heart rate recovery rate of zebrafish larva with orthogonal signal correction and partial least squares regression (OSC-PLSR) analysis. The anticardiovascular disease components of XKST were identified by mapping the targets related to CVDs in network pharmacology. The compounds of XKST absorbed and exposed in vivo were identified by ultra-high performance liquid chromatography Q-Exactive high-resolution mass spectrometry (UHPLC-Q-Exactive HRMS). Based on the earlier studies, combined with five principles for identifying quality markers and verified by a zebrafish arrhythmia model, danshensu, salvianolic acid A, salvianolic acid B, daidzein, and puerarin were identified as quality markers of XKST. In total, 16 batches of XKST samples were further quantified with the method established in this study. Our study laid the foundation for the quality control of XKST. The integrated strategy used in the study of XKST could be applied for the identification and quantification of quality markers of other CPMs as well.
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Separation power was limited when the conventional high-performance liquid chromatography (HPLC) fingerprinting method based on a single column was used to analyze very complex traditional Chinese medicine (TCM) preparations. In this research, a novel HPLC fingerprinting method based on column switching technology by using a single pump was established for evaluating the quality of Tianmeng oral liquid (TMOL). Twelve batches of TMOL samples were used for constructing HPLC fingerprints. Compared with the 16 common peaks in fingerprinting with a single column, 25 common peaks were achieved with two columns connected through a six-way valve. The similarity analysis combined with bootstrap method was applied to determine the similarity threshold, which was 0.992 to distinguish expired samples and unexpired samples. Principal component analysis (PCA) and hierarchical clustering analysis (HCA) were also applied to classify the TMOL samples, and results revealed that expired and unexpired samples are classified into two categories. The HPLC fingerprinting based on column switching technology with better separation power and higher peak capacity could characterize chemical composition information more comprehensively, providing an effective and alternative method to control and evaluate the quality of TMOL, which would offer a valuable reference for other TCM preparations.
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Selenium-doped nanostructure has been considered as an attractive approach to enhance the antibacterial activity of calcium phosphate (CaP) materials in diverse medical applications. In this study, the selenium-doped biphasic calcium phosphate nanoparticles (SeB-NPs) were first synthesized. Then, silver was in situ incorporated into SeB-NPs to obtain nanostructured composite nanoparticles (AgSeB-NPs). Both SeB-NPs and AgSeB-NPs were characterized by Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), ultraviolet-visible spectroscopy (UV-Vis), X-ray photoelectron spectroscopy (XPS), and Raman spectra. The results confirmed that the SeO32- was doped at the PO43- position and silver nanoparticles were deposited on the surface of SeB-NPs. Next, Transmission Electron Microscopy (TEM) analysis displayed that the prepared AgSeB-NPs had a needle-cluster-like morphology. CCK-8 analysis revealed SeB-NPs and AgSeB-NPs had good cytocompatibility with osteoblasts. The antibacterial activity of the prepared AgSeB-NPs was confirmed by using Gram-negative E. coli and Gram-positive S. aureus. The above results manifested the significance of the final AgSeB-NPs for biomedical applications.
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Antibacterianos/farmacologia , Hidroxiapatitas/química , Hidroxiapatitas/farmacologia , Nanopartículas Metálicas/química , Nanoestruturas/química , Selênio/química , Células Cultivadas , Escherichia coli/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana/métodos , Microscopia Eletrônica de Transmissão/métodos , Tamanho da Partícula , Espectroscopia Fotoeletrônica/métodos , Prata/química , Espectrofotometria Ultravioleta/métodos , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Staphylococcus aureus/efeitos dos fármacos , Difração de Raios X/métodosRESUMO
Traditional Chinese medicine (TCM), especially herbal medicine compound preparation, faces great challenges in its quality control due to a myriad of components involved. How to perform quality control of TCM more effectively has been a research topic. In this study, we used Tianmeng oral liquid (TOL) as a case study and developed a comprehensive strategy based on non-targeted, targeted and bioactive analyses for quality evaluation of TOL from different batches. Firstly, a non-targeted fingerprinting analysis was performed by HPLC-DAD and UHPLC-MS/MS. Twenty-five batches of TOL were clearly discriminated by similarity analysis and hierarchical cluster analysis and components were tentatively identified. Secondly, the targeted quantitative methods based on HPLC-DAD and HPLC-MS were applied to simultaneous quantitative determination of five and eight marker compounds, especially toxic component strychnine, respectively. The quantitative data were processed with principal component analysis for differentiating different batches of samples. Finally, we explored the feasibility of establishing a total antioxidant capacity (TAC) model. How to use the peak area instead of the corresponding concentration to determine the antioxidant activity-related compounds was theoretically explained for the first time, which was of great significance for the study of the fingerprint-efficacy relationship. The orthogonal signal correction-partial least squares model was employed to predict the TAC of TOL from their chromatographic fingerprints and identify three potential antioxidant markers. These results demonstrated that the comprehensive strategy from fingerprinting, chemical composition, multiple-component quantification, and antioxidant activity could be applied to quality evaluation of TOL and discrimination of the expired and unexpired samples.
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Medicamentos de Ervas Chinesas/química , Medicina Tradicional Chinesa , Administração Oral , Compostos de Bifenilo/química , Calibragem , Cromatografia Líquida de Alta Pressão/métodos , Sequestradores de Radicais Livres/química , Análise dos Mínimos Quadrados , Limite de Detecção , Modelos Teóricos , Picratos/química , Análise de Componente Principal , Padrões de Referência , Reprodutibilidade dos Testes , SoluçõesRESUMO
The usage of traditional Chinese medicines has expanded globally, but the data about authentication, efficacy, and safety is far from sufficient to meet the criteria supporting their use worldwide due to complexity in the composition. Fingerprinting describes integral characterization and reflects interactive aspects of complex components; therefore, it can offer the possibility of evaluating quality of traditional Chinese medicines following the overall principle. Chemometric techniques introduce multivariate analytical methods into fingerprinting to obtain more information that is useful, which is consistent with the holistic thought and plays an important role in research on the substantial basis. In this review, we will start with three aspects to expound the quality evaluation of traditional Chinese medicines based on fingerprints. The analytical techniques used in developing fingerprints including chromatographic methods, spectroscopic methods, and capillary electrophoresis are introduced. Strategies for fingerprints analysis usually based on chemometric methods including unsupervised and supervised pattern recognition are described. Applications of fingerprints for multi-component quantification, quality control, screening of bioactive components, and fingerprint-efficacy relationship study are also outlined. Finally, we propose challenges and future perspectives of fingerprints in quality evaluation to promote the development of modernization and internationalization of traditional Chinese medicines.
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Medicamentos de Ervas Chinesas/química , Cromatografia , Eletroforese Capilar , Medicina Tradicional Chinesa , Controle de QualidadeRESUMO
In this study, a useful method of Attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) combined with chemometrics was proposed for rapid quantification of two-indicator components as well as discrimination of Shenzhiling oral liquid in shelf life and over shelf life. Fifteen batches of samples were employed to construct quantitative and discriminant models. Two ingredients (paeoniflorin and cinnamic acid) for quality control were modeled by partial least square regression (PLSR). The discrimination of samples between in shelf life and over shelf life was carried out by using discriminant analysis (DA). The samples were divided into calibration set and validation set according to batches. Different data pre-processing algorithms such as standard-normal-variate (SNV), multiplicative scatter correction (MSC), Savitzkye-Golay (SG) smoothing with derivative methods were applied to reduce the influence of systematic disturbances. Variable selection methods including correlation coefficient (CC), competitive adaptive reweighted sampling (CARS) and interval partial least squares regression (iPLS) were all performed for optimizing the PLSR models and DA model. The results demonstrated that ATR-FTIR combined with chemometrics could be a rapid, convenient and nondestructive approach to evaluate the quality of Shenziling oral liquid.
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Medicamentos de Ervas Chinesas/análise , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Administração Oral , Calibragem , Cinamatos/análise , Análise Discriminante , Glucosídeos , Análise dos Mínimos Quadrados , Modelos Teóricos , Monoterpenos , Análise de Componente Principal , Padrões de ReferênciaRESUMO
OBJECTIVE: To investigate the effects of Pinggan Prescription (, PGP) on hypertension by the associated methods of metabonomic and pharmacodynamic. METHODS: A total of 32 male spontaneously hypertensive rats (SHRs) were randomly divided into two groups by using the random number table method: a treatment group (n=18) and a model group (n=14). The Wistar rats (n=14) were used as the normal group. Different prescription were used to intervene three groups: the treatment group in which PGP extract was administered orally at a dose of 18.336 g/kg (PGP/body weight), and the model group in which physiological saline was administered at the equivalent dose. The same treatment was applied to the normal group as the model group. The blood pressure was measured by tail-cuff method, and pharmacodynamic indexes including cyclic adenosine monophosphate (cAMP) and angiotensin II (Ang II) were tested by enzyme-linked immunosorbent assay. The plasma samples from three groups were detected by gas chromatography-mass spectrometry (GC-MS). RESULTS: Compared with the model group, blood pressure of treatment group was obviously reduced after continuous curing with PGP (P<0.01). The pharmacodynamic results illustrated that the content of Ang II increased with the raised blood pressure and the cAMP expressed the converse trend. After curing with PGP, the content of Ang II decreased, the difference between model group and treatment group was significant (P<0.01), and the cAMP expressed the converse trend. Five potential biomarkers were identified, including arachidonic acid, hexadecanoic acid, elaidic acid, octadecanedioic acid and 9,12-octadecadienoic acid. These metabolites had shown significantly changes as followed: arachidonic acid, hexadecanoic acid and elaidic acid were significantly higher and octadecanedioic acid and 9,12-octadecadienoic acid were lowered in the model group than those in the normal group. After the treatment of PGP, the metabolites had the trends of returning to normal along with the reduced blood pressure. CONCLUSIONS: PGP intervention for hypertension played a major role in the metabolism of arachidonic acid and linoleic acid. Metabonomic with pharmacodynamic methods could be potentially powerful tools to investigate the mechanism of Chinese medicine.
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Medicamentos de Ervas Chinesas/farmacologia , Metabolômica , Modelos Biológicos , Animais , Biomarcadores/sangue , Análise Discriminante , Cromatografia Gasosa-Espectrometria de Massas , Hipertensão/sangue , Hipertensão/tratamento farmacológico , Análise dos Mínimos Quadrados , Masculino , Redes e Vias Metabólicas/efeitos dos fármacos , Análise de Componente Principal , Ratos Endogâmicos SHR , Ratos WistarRESUMO
As a powerful process analytical technology (PAT) tool, near infrared (NIR) spectroscopy has been widely used in real-time monitoring. In this study, NIR spectroscopy was applied to monitor multi-parameters of traditional Chinese medicine (TCM) Shenzhiling oral liquid during the concentration process to guarantee the quality of products. Five lab scale batches were employed to construct quantitative models to determine five chemical ingredients and physical change (samples density) during concentration process. The paeoniflorin, albiflorin, liquiritin and samples density were modeled by partial least square regression (PLSR), while the content of the glycyrrhizic acid and cinnamic acid were modeled by support vector machine regression (SVMR). Standard normal variate (SNV) and/or Savitzkye-Golay (SG) smoothing with derivative methods were adopted for spectra pretreatment. Variable selection methods including correlation coefficient (CC), competitive adaptive reweighted sampling (CARS) and interval partial least squares regression (iPLS) were performed for optimizing the models. The results indicated that NIR spectroscopy was an effective tool to successfully monitoring the concentration process of Shenzhiling oral liquid.
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Medicamentos de Ervas Chinesas/análise , Medicina Tradicional Chinesa , Espectroscopia de Luz Próxima ao Infravermelho/métodos , Calibragem , Cromatografia Líquida de Alta Pressão , Análise dos Mínimos Quadrados , Padrões de Referência , Reprodutibilidade dos Testes , Máquina de Vetores de SuporteRESUMO
The present study was conducted to determine the effects of 1-O-acetylbritannilactone (ABL), a compound extracted from Inula britannica L., on vascular endothelial growth factor (VEGF) signaling and angiogenesis in endothelial cells (ECs). We showed that ABL promotes VEGF-induced cell proliferation, growth, migration, and tube formation in cultured human ECs. Furthermore, the modulatory effect of ABL on VEGF-induced Akt, MAPK p42/44, and p38 phosphorylation, as well as on upstream VEGFR-2 phosphorylation, were associated with VEGF-dependent Matrigel angiogenesis in vivo. In addition, animals treated with ABL (26 mg/kg/day) recovered blood flow significantly earlier than control animals, suggesting that ABL affects ischemia-mediated angiogenesis and arteriogenesis in vivo. Finally, we demonstrated that ABL strongly reduced the levels of VEGFR-2 on the cell surface, enhanced VEGFR-2 endocytosis, which consistent with inhibited VE-cadherin, a negative regulator of VEGF signaling associated with VEGFR-2 complex formation, but did not alter VE-cadherin or VEGFR-2 expression in ECs. Our results suggest that ABL may serve as a novel therapeutic intervention for various cardiovascular diseases, including chronic ischemia, by regulating VEGF signaling and modulating angiogenesis.
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Indutores da Angiogênese/farmacologia , Células Endoteliais da Veia Umbilical Humana/fisiologia , Lactonas/farmacologia , Fator A de Crescimento do Endotélio Vascular/fisiologia , Animais , Antígenos CD/metabolismo , Caderinas/metabolismo , Movimento Celular , Proliferação de Células , Células Cultivadas , Avaliação Pré-Clínica de Medicamentos , Membro Posterior/irrigação sanguínea , Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos , Humanos , Isquemia/fisiopatologia , Camundongos Endogâmicos C57BL , Neovascularização Fisiológica , Transporte Proteico/efeitos dos fármacos , Transdução de Sinais , Receptor 2 de Fatores de Crescimento do Endotélio Vascular/metabolismoRESUMO
To develop a method for the rapid monitoring of five components during the alcohol precipitation process of Shenzhiling oral solution using near infrared spectroscopy(NIRS).The contents of five components detemined by high performance liquid chromatography(HPLC) were used as the reference values, and the NIRS based partial least square regression(PLSR) models were used to monitor the concentrations of paeoniflorin, albiflorin, liquiritin, cinnamic acid and glycyrrhizic acid during the alcohol precipitation process of Shenzhiling oral solution, which were optimized and verified through comparing of different spectral pre-processing and variables selection methods. Determination coefficients(Rcal2 and Rpred2), root mean squares error of prediction (RMSEP), root mean squares error of calibration(RMSEC) and ratiao of performance to deviation(RPD) were applied to evaluate the performance of the models, and the corresponding values were 0.993 3 and 0.997 6, 0.084 9 gâ¢L⻹, 0.073 3 gâ¢L⻹ and 14.7 for paeoniforin; 0.991 4, 0.992 7, 0.028 1 gâ¢L⻹, 0.030 5 gâ¢L⻹ and 10.2 for albiforin; 0.955 3, 0.976 1, 0.012 0 gâ¢L⻹, 0.012 3 gâ¢L⻹ and 5.1 for liquiritin; 0.958 8, 0.990 3, 0.003 89 gâ¢L⻹, 0.002 89 gâ¢L⻹ and 7.1 for cinnamic acid; 0.982 0, 0.986 3, 0.053 8 gâ¢L⻹, 0.059 0 gâ¢L⻹, 7.2 for glycyrrhizic acid, respectively. The results indicated that the presented approach was effectively for the quantitative monitoring of the alcohol precipitation process of Shenzhiling oral solution.
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Medicamentos de Ervas Chinesas/normas , Espectroscopia de Luz Próxima ao Infravermelho , Calibragem , Precipitação Química , Etanol , Análise dos Mínimos QuadradosRESUMO
Evaluation of the batch consistency of traditional Chinese medicines (TCMs) is essential for the promotion of the development and quality control of TCMs. The aim of the present work was to develop a useful strategy via liquid chromatography and chemometrics to evaluate the batch consistency of TCM preparations. Xin-Ke-Shu (XKS) tablet was chosen as a model for this method development. Four types of chromatographic fingerprint approaches were compared by using similarity analysis based on cosine of angel or correlation coefficient. Differences in the fingerprints of 71 batches of XKS tablet were illustrated by hierarchical cluster analysis. Then, Mahalanobis distance was employed for estimating the probability level (P < 0.05) of the differences mentioned above. Additionally, t-test was applied to find out the chromatographic peaks which had significant differences. For XKS tablet, the maximum wavelength fingerprint had the largest range and dispersion degree of similarity as compared with the other three ones. There were two clear clusters in all the batches of samples. And we clearly arrived at the conclusion that higher similarity does not exactly indicate small Mahalanobis distance, while lower similarity indicated larger Mahalanobis distance. Finally, a useful strategy was proposed for evaluation of the batch consistency of XKS tablet.