IntroductionThe quality of traditional Chinese medicine (TCM) guarantees clinical efficacy. At present, although chemical quality evaluation methods can reflect the quality of TCMs to a certain extent, there are still many problems. This study proposes a new strategy for the quality innovation evaluation of the TCM “target combined quality evaluation” (TCQE) theory and method. Taking the “disease-target-medicine” combination as the main fusion strategy, using drug components/ components to achieve the overall intervention of disease targets, and establishing the TCQE strategy of TCM to improve the pertinence and accuracy of the quality evaluation of TCM, the clinical efficacy and safety of TCM is improved, and precision clinical medication is achieved.MethodsTaking safflower as the research object, due to its main efficacy in the treatment of primary dysmenorrhea (PD), the potential targets and mechanism of action of safflower in the treatment of PD were analyzed by a network pharmacology method and combined with a metabolomics method. The pathway and mechanism of action of safflower in the treatment of PD were analyzed from multiple dimensions. The network pharmacology and metabolomics results were analyzed, the key targets of safflower in the treatment of PD were screened. Finally, a method for the biological evaluation of safflower quality was established based on the selected targets, which could provide a reference for the precise evaluation of safflower treatment and a scientific basis for the clinical application of safflower in the prevention and treatment of PD.Results and discussionThe pharmacodynamic results showed that Safflower significantly improved Prostaglandin E2 (PGE2) and Prostaglandin F2 α (PGF2 α) levels, the PGF2 α/PGE2 ratio and the analgesic rate in PD rats. The results of network pharmacology combined with metabolomics analysis showed that Prostaglandin G/H synthase 2 (PTGS2) and arachidonic acid (AA)were important targets and pathways of Safflower in the treatment of PD. A biological evaluation method was established around PTGS2. The results of the methodological investigation showed that the method was stable and reliable. In vivo validation experiments showed that the results of this method were consistent with the pharmacodynamic results, which proved its accuracy. PTGS2 is an important target of safflower in the treatment of PD. The biological evaluation method established around PTGS2 can accurately evaluate the quality of Safflower in the treatment of PD, which also proves that the target discrimination theory proposed in this study is scientific.
Angelica dahurica (Hoffm.) Benth. & Hook.f. ex Franch. & Sav (A. dahurica) is widely used in food, medicine and other applications due to its rich content of starch and secondary metabolites and is grown on a large scale in southwestern and northern China, where it is one of the commonly used traditional Chinese medicines(TCM). Modern studies have pointed out that the effect of soil compactness on plant root development as well as secondary metabolite synthesis is extremely significant, and auxin may play an important role in this process. However, the effect of soil compactness on coumarins synthesis in A. dahurica and the reasons for the changes in coumarins content are unknown in the current actual cultivation, which is extremely unfavorable for A. dahurica, which is dependent on the content of secondary metabolites. In this study, A. dahurica was planted in soil environments with low (5 kPa), medium (15 kPa) and high (25 kPa) soil compactness and harvested at 80, 100 and 120 d, respectively. The plant development process was quantified and the indole-3-acetic acid(IAA) content of the corresponding root tips and the total coumarins content of the primary and lateral roots were examined. We aimed to (i) clarify the effects and patterns of soil compactness on the morphology and coumarins synthesis of A. dahurica, and (ii) explore the effects of IAA on coumarins synthesis in the roots of A. dahurica in response to soil compactness stress. It was found that both too low and too high soil compactness resulted in low biomass accumulation of A. dahurica, but the latter showed a higher rate of coumarins accumulation. IAA was positively correlated (p < 0.1) with various morphological parameters and total coumarins content, suggesting that IAA may be associated with coumarins synthesis. Thereafter, we confirmed through validation experiments that IAA positively regulates coumarins synthesis in the roots of A. dahurica, and that it is intrinsic to the positive correlation between root morphology parameters and total coumarins content (p < 0.001) in A. dahurica. The results of the study showed that in response to soil compactness stress, the root system of A. dahurica regulates root morphology by secreting IAA to resist soil compactness stress, while at the same time IAA stimulates the signaling pathway for coumarins biosynthesis. This study has significant practical implications for the cultivation and quality improvement of A. dahurica.
IntroductionWith the onset of the COVID-19 pandemic, the incidence and prevalence of acute pharyngitis (AP) have increased significantly. Tinosporae Radix (TR) is a vital medication utilized in the treatment of pharyngeal and laryngeal ailments, especially AP. The study endeavors to explore unclear molecular mechanisms of TR in addressing AP.MethodsNetwork pharmacology and metabolomics analyses of effect of TR on AP were conducted, and apossible pathway was validated both in vivo using the acute pharyngitis rat model and in vitro using the LPS-induced RAW264.7 cells model, through techniques such as histopathological examinations, immunohistochemical technology, ELISA, RT-qPCR, and Western blotting to systematically explore the possible mechanisms underlying the inhibition of AP by TR.Results and discussionNetwork pharmacology analysis identified several key targets, including PIK3CA, IL6, AKT1, TNF, and PTGS2, alongside pivotal signaling pathways such as IL-17, TNF, Hepatitis B, nuclear factor kappa B (NF-κB), Influenza A, and the PI3K-Akt pathway. Most of them are closely associated with inflammation. Then, wide-target metabolomics analysis showed that TR downregulated substances within the glycerophospholipid metabolic pathway, and modulated the PI3K-Akt pathway. The integrated findings from network pharmacology and metabolomics underscored the pivotal role of the PI3K-Akt signaling pathway and the attenuation of inflammatory responses. Finally, in vitro and in vivo experiments have shown that TR can inhibit inflammatory factors such as IL-6, TNF - α, and COX-2, downregulate targets such as PI3K and AKT on the PI3K-Akt signaling pathway, and thereby alleviate the inflammatory response of AP. Our study demonstrated that TR exerts an anti-AP effect through suppression of release of inflammatory factors and modulation of glycerophospholipid metabolism via suppressing the PI3K-Akt signaling pathway.
Abstract The Tinosporae Radix is favored as a treatment for pharyngitis and is now regarded as the first choice of traditional Chinese medicine as an alternative to antibiotics. However, its wild resources are on the verge of extinction due to over-excavation by human beings, and the quality of the cultivated products varies, so it is urgent to search for the key biological factors affecting the growth and development process of Tinosporae Radix as well as the suitable ecological zones. In this study, we used MaxEnt model and Arcgis spatial analysis technology to predict the suitable growing area of Tinosporae Radix, and found four key environmental factors affecting the quality of Tinosporae Radix. In this paper, we used UPLC analysis to obtain the fingerprints of Tinosporae Radix, and found that the most relevant components for the anti-inflammatory effect of Tinosporae Radix included columbin and several alkaloids, and the correlation analysis with the relevant biotic factors revealed that Tinosporae Radix is suitable for growing in Southwest China, and that Tinosporae Radix with higher content of columbin is suitable for growing in the region of the Yunnan-Guizhou Plateau, and that Tinosporae Radix with higher content of alkaloids is suitable for growing in the borders between Guangxi, Yunnan, Guizhou, and Hunan, which are all characterized by karst landscapes. And all these places are dominated by karst landscape. In vitro analysis of anti-inflammatory efficacy showed that the anti-inflammatory efficacy was good regardless of the high content of either type of components. In this paper, we evaluated the quality of Tinosporae Radix herbs in the suitable habitat obtained by model prediction through the method of "chemical evaluation" associated with "anti-inflammatory" efficacy, and obtained an innovative "ecological-chemical-pharmacological efficacy" evaluation method, which is a good method to evaluate the quality of Tinosporae Radix herbs in the suitable habitat. The results of this method can be used to guide the production of Tinosporae Radix with a high content of columbin or alkaloids, laying the foundation for the establishment of standardized artificial cultivation of Tinosporae Radix, and at the same time, providing theoretical support for the delineation of Tinosporae Radix's suitable areas, the utilization of its resources, and the extension of the industrial chain.
Cardio-cerebrovascular diseases are the leading cause of death worldwide and there is currently no optimal treatment plan. Chinese herbal medicine injection (CHI) is obtained by combining traditional Chinese medicine (TCM) theory and modern production technology. It retains some characteristics of TCM while adding injection characteristics. CHI has played an important role in the treatment of critical diseases, especially cardio-cerebrovascular diseases, and has shown unique therapeutic advantages. TCMs that promote blood circulation and remove blood stasis, such as Salvia miltiorrhiza, Carthami flos, Panax notoginseng, and Chuanxiong rhizoma, account for a large proportion of CHIs of cardio-cerebrovascular disease. CHI is used to treat cardio-cerebrovascular diseases and has potential pharmacological activities such as anti-platelet aggregation, anti-inflammatory, anti-fibrosis, and anti-apoptosis. However, CHIs have changed the traditional method of administering TCMs, and the drugs directly enter the bloodstream, which may produce new pharmacological effects or adverse reactions. This article summarizes the clinical application, pharmacological effects, and mechanism of action of different varieties of CHIs commonly used in the treatment of cardio-cerebrovascular diseases, analyzes the causes of adverse reactions, and proposes suggestions for rational drug use and pharmaceutical care methods to provide a reference for the rational application of CHIs for cardio-cerebrovascular diseases.
Pulmonary fibrosis is a chronic progressive interstitial lung disease caused by a variety of etiologies. The disease can eventually lead to irreversible damage to the lung tissue structure, severely affecting respiratory function and posing a serious threat to human health. Currently, glucocorticoids and immunosuppressants are the main drugs used in the clinical treatment of pulmonary fibrosis, but their efficacy is limited and they can cause serious adverse effects. Traditional Chinese medicines have important research value and potential for clinical application in anti-pulmonary fibrosis. In recent years, more and more scientific researches have been conducted on the use of traditional Chinese medicine to improve or reduce pulmonary fibrosis, and some important breakthroughs have been made. This review paper systematically summarized the research progress of pharmacological mechanism of traditional Chinese medicines and their active compounds in improving or reducing pulmonary fibrosis. We conducted a systematic search in several main scientific databases, including PubMed, Web of Science, and Google Scholar, using keywords such as idiopathic pulmonary fibrosis, pulmonary fibrosis, interstitial pneumonia, natural products, herbal medicine, and therapeutic methods. Ultimately, 252 articles were included and systematically evaluated in this analysis. The anti-fibrotic mechanisms of these traditional Chinese medicine studies can be roughly categorized into 5 main aspects, including inhibition of epithelial-mesenchymal transition, anti-inflammatory and antioxidant effects, improvement of extracellular matrix deposition, mediation of apoptosis and autophagy, and inhibition of endoplasmic reticulum stress. The purpose of this article is to provide pharmaceutical researchers with information on the progress of scientific research on improving or reducing Pulmonary fibrosis with traditional Chinese medicine, and to provide reference for further pharmacological research.
Liver fibrosis refers to a complex inflammatory response caused by multiple factors, which is a known cause of liver cirrhosis and even liver cancer. As a valuable medicine food homology herb, saffron has been widely used in the world. Saffron is commonly used in liver-related diseases and has rich therapeutic and health benefits. The therapeutic effect is satisfactory, but its mechanism is still unclear. In order to clarify these problems, we planned to determine the pharmacological effects and mechanisms of saffron extract in preventing and treating liver fibrosis through network pharmacology analysis combined with in vivo validation experiments. Through UPLC-Q-Exactive-MS analysis, a total of fifty-six nutrients and active ingredients were identified, and nine of them were screened to predict their therapeutic targets for liver fibrosis. Then, network pharmacology analysis was applied to identify 321 targets for saffron extract to alleviate liver fibrosis. Functional and pathway enrichment analysis showed that the putative targets of saffron for the treatment of hepatic fibrosis are mainly involved in the calcium signaling pathway, the HIF-1 signaling pathway, endocrine resistance, the PI3K/Akt signaling pathway, lipid and atherosclerosis, and the cAMP signaling pathway. Based on the CCl4-induced liver fibrosis mice model, we experimentally confirmed that saffron extract can alleviate the severity and pathological changes during the progression of liver fibrosis. RT-PCR and Western blotting analysis confirmed that saffron treatment can prevent the CCl4-induced upregulation of HIF-1α, VEGFA, AKT, and PI3K, suggesting that saffron may regulate AKT/HIF-1α/VEGF and alleviate liver fibrosis.
Quality consistency of Glycyrrhiza formula granules is essential for guaranteeing clinical efficacy. However, a suitable method to accurately and conveniently evaluate the consistency of the clinical efficacy of Glycyrrhiza formula granules is currently not available. This study established a method for the simultaneous determination of 12 active components in Glycyrrhiza formula granules using ultra-high-performance liquid chromatography coupled with quadrupole-time-of-flight tandem mass spectrometry. The rate of inhibition of cyclooxygenase-2 by different batches of Glycyrrhiza formula granules was determined. Near-infrared spectra were collected for different batches of Glycyrrhiza formula granules to detect their biological activity in the inhibition of cyclooxygenase-2. The quality consistency of the 11 batches of Glycyrrhiza formula granules was evaluated using principal component and correlation analyses. The results showed significant differences in the formula granules of Glycyrrhiza uralensis produced by the different manufacturers. Some differences were also observed among batches of formula granules produced by the same manufacturer. Correlation analysis of the chemical components and cyclooxygenase-2 activity showed that glycyrrhizic acid, liquiritin, and isoliquiritin were the main active components of Glycyrrhiza. Correlation analysis of the near-infrared spectra and cyclooxygenase-2 inhibition activity showed a high correlation between the active components and three characteristic bands: 3383-3995, 4227-4651, and 5315-5878 cm-1 . In this study, the main active anti-inflammatory components of Glycyrrhiza granules were screened. Thus, the near-infrared spectrum and characteristic active band of multi-index active components can be used to quickly detect the quality consistency of Glycyrrhiza formula granules, thereby improving the ability to control the quality and consistency of these granules.
The quality of traditional Chinese medicine (TCM) guarantees its clinical efficacy. Although advanced analytical techniques and methods can accurately determine the content of chemical components in TCM, it is difficult to accurately determine its clinical efficacy. In addition, the current analytical methods and technologies are complex and have difficulty meeting the requirements of a rapid, accurate and convenient determination of TCM quality. In this study, we first propose the concept of "indistinct" evaluation of the quality of TCM, that is, combining biological potency with character evaluation, quantifying the character evaluation, and preparing the safflower quality grade evaluation card based on the character analysis, which provides research ideas and methods for the rapid and accurate evaluation of the quality of TCM. We determined the biological potency of different batches of safflower based on the in vitro antiplatelet aggregation model and divided the safflower samples into two grades based on the biological potency. We further collected the color information of different grades of safflower samples, quantified the color information of different grades of safflower, drew a quality grade evaluation card for the rapid judgment of safflower quality grade and verified its accuracy by pharma-codynamic evaluation. To further analyze the differences in the material basis of different grades of safflower, the LC-MS method was used to simultaneously determine the contents of 19 chemical components, such as myr-icetin, in different grades of safflower samples to analyze the differences in the material basis of different grades of safflower. The result shows that the different grades of safflower exhibited significant differences in color. The pharmacodynamic results show that the quality evaluation card prepared based on color information can accurately evaluate quality, and the effect of first-class safflower is significantly better than that of second-class safflower. The chemical analysis results of different grades of safflower show that there are also significant differences between them, among which hypericin, 6-hydroxyapin-6-O-glucose-7-O-glucuronide, 6-hydrox-ykaempferol-3,6-O-diglucoside-7-O-glucuronic acid glycoside, 6-hydroxykaempferol-3,6,7-tri-O-glucoside and hydroxysafflower yellow A exhibit significant differences, which may be the main differentiating components of different grades of safflower. This study preliminarily confirmed that the "indistinct" evaluation of the quality of TCM based on character analysis is accurate and scientific, and the quality evaluation card prepared can accu-rately judge the quality of TCM, providing a reference for the rapid application of TCM character evaluation.
目的 应用星点设计-响应面法优化厚朴Magnolia officinalis产地趁鲜加工与炮制一体化工艺.方法 通过CRITIC法计算厚朴饮片外观性状和主要有效成分厚朴酚、和厚朴酚含量3个指标的权重系数,采用Box-Behnken响应面法,以综合评分作为评价指标,考察干燥温度、干燥时间和切丝宽度3个因素对厚朴饮片的影响,优化厚朴产地趁鲜加工与炮制一体化工艺.结果 利用CRITIC法确定厚朴饮片外观性状、和厚朴酚含量、厚朴酚含量的权重系数分别为0.4221、0.2410、0.3369,优选的厚朴饮片炮制工艺为厚朴药材去粗皮后,切7mm厚的丝装入内膜袋于烘箱内40 ℃发汗16h后,平铺在烘箱内65 ℃干燥14.5h.验证结果与预测值之间的RSD为1.76%,说明模型具有良好的预测性.结论 优化的厚朴产地趁鲜加工与炮制一体化工艺简便易行,稳定性好,可为以厚朴为代表的"发汗"类皮类饮片规范化生产和质量标准提高提供参考.
Objective To compare the effects of different processing methods and drying temperatures on the appearance and coumarins of Baizhi(Angelicae Dahuricae Radix, ADR) decoction pieces, determine the appropriate drying temperatures for different processing methods, and select the appropriate processing methods for ADR in the production area. Methods Three processing methods(steamed-cut, semi-fresh-cut, fresh-cut) combined with three drying temperatures(40, 50, and 60 ℃) were set to process ADR decoction pieces. The contents of five coumarins(bergapten, oxypeucedanin, imperatorin, phellopterin and isoimperatorin) were determined based on HPLC, and colorimeter was used to quantify the appearance parameters of ADR decoction pieces. The system clustering method was applyed to determine the color difference between samples, and the gray correlation method was used to explore the correlation between color and composition. Rank sum ratio comprehensive evaluation method(RSR)was adopt to evaluate the quality of ADR, and the cyclooxygenase-2(COX-2) inhibitor screening kit was used to verify the quality evaluation results. Combining the color and quality evaluation results of the ADR decoction to compare different processing methods and dry temperature. The color of ADR decoction pieces was quantified by colorimeter, and the contents of five coumarins were determined by HPLC. The systematic clustering method was used to determine the difference of color and composition of samples.The gray correlation method was used to explore the correlation between color and composition. The RSR method was used to evaluate the quality of samples, and the COX-2 inhibitor screening kit was used to determine the anti-inflammatory activity of different samples. Results The brightness value(L * ) of the samples dried at 50 ℃ was the highest, followed by the samples dried at 60 ℃, the samples dried at 40 ℃ were the lowest, and the yellow-blue(b * ) value was opposite. The total amount and oxypeucedanin increased with the increase of the drying temperature. Among them, the content of C3 had the highest component content, and A1 was the lowest. The color and composition clustering results showed that the samples A1 and C3 were significantly different from other samples. The analysis of the gray correlation showed that L * value had the strongest correlation with oxypeucedanin, followed by imperatorin, b * value had the strongest correlation with phellopterin, followed by imperatorin, a * value had low correlation with each index component. The quality evaluation results showed that the top three samples are C3, C2 and B3,and A1 ranks the lowest. The results of IC 50 determination are similar to quality evaluation, and IC 50 is negatively correlated with coumarins except bergapten. Conclusion The processing method and drying temperature had significant effects on ADR decoction pieces, the 60 ℃ semi-fresh-cut decoction pieces and 50 ℃ fresh-cut decoction pieces had great color, high anti-inflammatory activity and production efficiency, which is worthy of popularization.
Background: Cardiovascular disease is one of the most concerning chronic diseases in the world. Many studies have shown that platelet overactivation is a very important factor in the occurrence and development of cardiovascular diseases. At present, the widely used antiplatelet drugs have some defects, such as drug resistance and adverse reactions. Purpose: The purpose of this article is to summarize the main mechanisms and pathways of platelet activation, the main targets of antiplatelet aggregation, and the antiplatelet aggregation components of natural drugs and their mechanisms of action to provide new research ideas for the development and application of antiplatelet drugs. Study design and Methods: In this review, we systematically searched the PubMed, Google Scholar, Web of Science, and CNKI databases and selected studies based on predefined eligibility criteria. We then assessed their quality and extracted data. Results: ADP, AA, THR, AF, collagen, SDF-1 alpha, and Ca2+ can induce platelet aggregation and trigger thrombosis. Natural drugs have a good inhibitory effect on platelet activation. More than 50 kinds of natural drugs and over 120 kinds of chemical compounds, including flavonoids, alkaloids, saponins, terpenoids, coumarins, and organic acids, have significantly inhibited platelet activation activity. The MAPK pathway, cGMP-PKG pathway, cAMP-PKA pathway, PI3K-AKT pathway, PTK pathway, PLC pathway, and AA pathway are the main mechanisms and pathways of platelet activation. Conclusion: Natural drugs and their active ingredients have shown good activity and application prospects in antiplatelet aggregation. We hope that this review provides new research ideas for the development and application of antiplatelet drugs.
Insomnia is a very common disease worldwide. It seriously affects the quality of human life and even endangers health. Traditional Chinese medicine (TCM) has unique advantages in the intervention and treatment of insomnia. However, its underlying mechanism has yet to be elucidated. This study was performed to explore the potential biomarkers and mechanisms of insomnia, and treatment TCM and classical prescriptions. The gene microarray data of insomnia is downloaded and preprocessed. Differentially expressed genes (DEGs) and GO and KEGG enrichment analyses were performed. The protein-protein interaction network (PPI) was constructed. Small molecule drugs for curing insomnia were identified using cMap and CTD databases. We searched the TCM corresponding to small molecule drugs and the classic prescriptions corresponding to TCM by the TCMSP database. We constructed a network of "ingredient-TCM-classic prescriptions". The molecular docking was performed to validate the screening results. We obtained a total of 124 DEGs, including 78 up-regulated genes, 46 down-regulated genes, 10 Hub genes and 3 key modules. A total of 125 significant GO entries and 15 significant KEGG were enriched (P < 0.05). The main biological processes involve neuronal apoptosis, autophagy, cell growth and apoptosis, etc. These signaling pathways may be involved in molecular regulatory mechanisms of insomnia, such as autophagy regulation, Alzheimer's disease, pathways to neurodegenerative diseases and neurotrophic factor signaling pathways. We identified 10 traditional Chinese medicines and 2 classical prescriptions of potential value. In addition, the molecular docking results indicated that small molecule ligands were nicely bound to the Hub gene, and the binding affinity ranged from -7.6 to -9.7 kcal/mol. This study provides a foundation for the clinical treatment of insomnia, explains the molecular mechanisms, and efficiently develops TCM and classical prescriptions.
Ethnopharmacological relevance: Keguan-1, a new traditional Chinese medicine (TCM) prescription contained seven Chinese herbs, is developed to treat coronavirus disease 19 (COVID-19). The first internationally registered COVID-19 randomised clinical trial on integrated therapy demonstrated that Keguan-1 significantly reduced the incidence of ARDS and inhibited the severe progression of COVID-19. Aim of the study: To investigate the protective mechanism of Keguan-1 on ARDS, a lipopolysaccharide (LPS)induced acute lung injury (ALI) model was used to simulate the pathological state of ARDS in patients with COVID-19, focusing on its effect and mechanism on ALI. Materials and methods: Mice were challenged with LPS (2 mg/kg) by intratracheal instillation (i.t.) and were orally administered Keguan-1 (low dose, 1.25 g/kg; medium dose, 2.5 g/kg; high dose, 5 g/kg) after 2 h. Bronchoalveolar lavage fluid (BALF) and lung tissue were collected 6 h and 24 h after i.t. administration of LPS. The levels of inflammatory factors tumour necrosis factor alpha (TNF-alpha), interleukin (IL)-6, IL-1 beta, keratinocyte-derived chemokine (KC or mCXCL1), macrophage inflammatory protein 2 (MIP2 or mCXCL2), angiotensin II (Ang II), and endothelial cell junction-associated proteins were analysed using ELISA or western blotting. Results: Keguan-1 improved the survival rate, respiratory condition, and pathological lung injury; decreased the production of proinflammatory factors (TNF-alpha, IL-6, IL-beta, KC, and MIP2) in BALF and the number of neutrophils in the lung tissues; and ameliorated inflammatory injury in the lung tissues of the mice with LPS-induced ALI. Keguan-1 also reduced the expression of Ang II and the adhesion molecule ICAM-1; increased tight junction proteins (JAM-1 and claudin-5) and VE-cadherin expression; and alleviated pulmonary vascular endothelial injury in LPS-induced ALI. Conclusion: These results demonstrate that Keguan-1 can improve LPS-induced ALI by reducing inflammation and pulmonary vascular endothelial injury, providing scientific support for the clinical treatment of patients with COVID-19. Moreover, it also provides a theoretical basis and technical support for the scientific use of TCMs in emerging infectious diseases.
金果榄为喉科要药,民间常用于治疗炎症和胃痛等,疗效显著,为苗、壮、瑶族等少数民族习用药物;同时被《中国药典》收载,具有清热解毒、利咽止痛等功效.现代药理学研究表明金果榄具有抗炎、镇痛、抑菌、抗溃疡、抗肿瘤、降血糖、抗氧化等药理作用,化学成分以二萜类、生物碱类和甾体类为主,其中克罗烷型二萜如古伦宾、异喹啉类生物碱如巴马汀为主要活性成分.对金果榄的化学成分、药理作用和安全性评价进行综述,并从植物亲缘学及成分特异性、成分与中药有效性的关联、成分可测性等方面对金果榄的质量标志物(qualitymarker,Q-Marker)进行预测分析,并预测古伦宾、巴马汀、药根碱、非洲防己碱、木兰花碱等可作为其Q-Marker,为建立和完善其质量标准提供参考.
目的 基于附子强心组分去甲乌药碱、去甲猪毛菜碱和棍掌碱共有的肾上腺素类似结构,构建了以邻二酚羟基基团与茜素红S-苯硼酸体系置换反应为核心的光化学比色传感器,用于整体评价附子配方颗粒的强心作用.方法 以传感器的响应强度为评价指标,对超声提取时间、料液比、提取液浓度和乙二胺四乙酸二钠(EDTA-2Na)浓度等供试品的制备条件进行优化;并对该方法的精密度、重复性和稳定性进行考察;用平板扫描仪获取23批附子配方颗粒的|ΔG|值(绿色G,|ΔG|=|G后-G前|),同时采用LC-MS/MS测定附子配方颗粒中3种生物碱的含量,将|ΔG|与强心成分总含量进行相关性分析.结果 供试品制备方法优选为取附子配方颗粒粉末0.5 g,加10 mL甲醇,300 W、60 kHz超声提取15 min,将上清液全部转移至蒸发皿中,80℃C挥干,4mL0.13g/mL的EDTA-2Na溶液洗脱蒸发皿上物质,离心,取上清液,调pH至8.0左右,缓冲溶液稀释3倍.方法 学考察表明该方法精密度、重复性和稳定性良好.23批样品的强心成分总含量的差异较大,为127.83~6 928.27 μg/g;|ΔG|的范围为0~12.5,两者的相关系数(r)高达0.96,表明强心成分总含量与|ΔG|高度相关.结论 该方法具有一定的科学性与准确性,可整体性评价附子配方颗粒强心药效.
δ-Chymotrypsin, subtilopeptidase and crude extracellular proteases from Pseudomonas aeruginosa have been separated by isoelectric focusing in thin layers of polyacrylamide gel. Ampholine was removed by soaking the gel in buffer, prior to overlaying with casein-containing agar to detect proteolysis. The technique described is simple and has a high resolving power. It should have general application for the analysis of enzymes.
目的:通过整合分析甘草抗炎活性与性状特征数据,研究感官评价的科学性.方法:基于核苷酸结合寡聚化结构域样受体蛋白3(NLRP3)炎症小体细胞模型,建立甘草的抗炎生物效价测定方法,根据测定生物效价将采集的甘草样品分级.通过电子鼻、色彩色差仪等采集不同等级甘草样品的性状信息,通过主成分分析(PCA)、正交偏最小二乘法-判别分析(OPLS-DA)分析不同等级甘草的差异性,并进一步考察性状特征与甘草抗炎活性的关联性.结果:实验结果显示,甘草提取物对尼日利亚菌素诱导的小鼠原代骨髓巨噬细胞NLRP3炎症小体的激活具有明显抑制作用,根据甘草的抗炎生物效价,可将10批次甘草分为两个等级,一等甘草的生物效价为5.949~11.418 U·mg-1,二等甘草的生物效价为1.575~1.887 U·mg-1;PCA结果显示,两等级甘草可以聚成两类;OPLS-DA结果显示,R2X=0.534,R2Y=0.863,Q2=0.75,模型的拟合能力较好,预测能力较强,并且发现色度值b*和断面直径(2R)的变量重要性投影(variable important inprojection,VIP)分别为1.54294、1.26011,均大于1,两者可能是导致两等级甘草药效差异的关键参数,经过实测值比较,两等级甘草在b*上的差异有统计学意义(P<0.01).结论:研究表明,甘草的b*与甘草抗炎活性具有显著的相关性,是其质量评价的一个重要指标,也佐证了甘草传统评价具有一定的科学性.
Safflower (Carthamus tinctorius L.) is cultivated in various countries for the flavonoid compounds it contains. These flavonoids have been used in many industries as drugs and/or dyes. Over 60 flavonoids have been isolated from safflower. These flavonoids can be divided into two groups: special and common, both of which are active pharmaceutical ingredients efficacious in the treatment of cardiovascular and cerebrovascular diseases. Gene functions have been studied to figure out the biosynthesis of flavonoids in safflower. However, there is no comprehensive summary of the flavonoids in safflower. Research was recognised through systematic searches of ScienceDirect, PubMed, Web of Science, and CNKI databases by searching terms of “Carthamus tinctorius L.”, “safflower”, “flavonoid”, “pharmacology”, and “gene”. More than 200 research reports were included after eligibility checks. This study summarizes the application of flavonoids in medicine and other industries. Comprehensively collects the chemical structure information of the two groups of flavonoids, and organic acids, alkaloids, spermidine, polyacetylene, and polysaccharides. The mechanism of two groups of flavonoids in treatment of cardiovascular and cerebrovascular diseases was describe in detail, and pharmacological mechanisms of protecting liver, lung and bone, and anti-cancer and anti-inflammatory were also summarised. Besides, the study updated the latest information on the molecular biology of safflower flavonoids. It is found that two groups of flavonoids in safflower have obvious differences in application, chemical structure, pharmacological mechanism, and biosynthetic pathway. It is hoped that this summative research will provide a new insight to flavonoids research in safflower.
人体的免疫功能是维持身体健康的重要生理性功能,在免疫系统的功能受损或低下时,会对人的身体健康产生严重影响.甘草作为一种补益类中药,有补脾益气之功,对人体的免疫功能具有增强作用,在开发成免疫增强新药方面具有独特优势和发展潜力.通过对近期国内外甘草免疫增强作用的相关文献进行收集和整理,从所含化合物的结构特点、分类及药理作用等方面阐述了甘草增强免疫的物质基础,并以甘草的药效成分为基础综述了甘草促进免疫细胞增殖、影响体内细胞因子和抗体水平以及调控相关酶表达等增强免疫的分子机制,以期为免疫增强药物的研发提供新的思路,为甘草免疫作用的进一步研究提供参考.