Substitution mode of rare and endangered Chinese medicinal materials and research strategy of multi-component replacement / 中国中药杂志

Rare and endangered Chinese medicinal materials are the material basis for innovation and development of Chinese medicinal materials and their curative effects are remarkable. However, the resources are in shortage due to various man-made or natural factors such as rising demand, overexploitation and environmental degradation. Therefore, finding alternatives is a feasible and effective solution. This study systematically sorted out the list of rare and endangered Chinese medicinal materials, and combed relevant policies and regulations. According to existing research, the substitution model of rare and endangered Chinese medicinal materials was constructed from the theoretical level. In view of the slow search for substitutes, the failure to follow the basic theory of traditional Chinese medicine in the process of research and development, the difficulty in breaking through technologies and the incomplete guarantee of the clinical efficacy of substitutes, a multi-component replacement was proposed to replace the originals with more effective components from a wide range of sources. This study was expected to promote the study on the substitutes of rare and endangered Chinese medicinal materials to step into a new stage.

Acetylation of Rehmannia glutinosa polysaccharides and antioxidant activity of acetylated derivatives / 中国中药杂志

This study aims to acetylate Rehmannia glutinosa polysaccharides by acetic anhydride method, optimize process parameters and evaluate their antioxidant activity. With the degree of substitution(D_s) as a criterion, the effects of reaction time, acetic anhydride-to-polysaccharides ratio and temperature were investigated. Process parameters were optimized by single-factor experiment and response surface methodology. The infrared spectroscopy(IR) and scanning electron microscopy(SEM) proved the successful acetylation and were employed to preliminarily analyze the structural characteristics of acetylated derivatives. The results showed that the D_s was 0.327 under the optimal technological conditions, including m(acetic anhydride):m(R. glutinosa polysaccharides)=2.70, reaction time 3.0 h and temperature 48 ℃. Further, the antioxidant properties of acetylated derivatives were investigated in vitro and acetylation was found effective to improve the antioxidant activity of R. glutinosa polysaccharides. This study provides a reference for the further development and application of R. glutinosa polysaccharides.

Twenty years in the 21st century: temporal and spatial evolution of Chinese medicinal processing equipment / 中国中药杂志

Against the backdrop of "Internet+" and Made in China 2025, Chinese medicinal processing equipment embraces various opportunities and develops to an unprecedented level. In the 20 years of the new century, the processing equipment has gradually developed in the direction of high efficiency, energy saving, environmental protection, integration, and automation, and this field has tended to highlight the establishment and application of the linkage production line for the processing of Chinese medicinal decoction pieces. Integrating automation control technology, online detection technique, and the internet of things technology, the online detection system of Chinese medicinal processing equipment and the computer information management system of Chinese medicinal proces-sing are the mainstream development trends of Chinese medicinal processing equipment. Standard Chinese medicine processing equipment is the prerequisite for the standardization of processing parameters. A standard system for processing equipment and processing parameters is the key to the modernization of Chinese medicinal decoction pieces. This paper summarized the research and application of Chinese medicinal processing equipment in the 20 years of the 21 st century and predicted the development trend, which is expected to serve as a reference for the technological innovation and development of the processing equipment.

Twenty years in the 21st century: research approaches and techniques in modern system biology for mechanisms of Chinese medicinal processing / 中国中药杂志

Clarifying the mechanisms of Chinese medicinal processing is pivotal to the modernization of Chinese medicine. Research on Chinese medicinal processing gives priority to the mechanisms of the processing in enhancing efficacy, reducing toxicity, and repurposing medicinals. During the past 20 years, scholars have carried out in-depth studies on the mechanisms of Chinese medicinal processing via modern system biology. They mainly focused on the changes of medicinal properties and efficacy caused by processing using techniques of modern pharmacology and molecular biology, spectrum-efficacy correlation, and biophoton emission. However, these techniques fail to reflect the holistic view of traditional Chinese medicine. With the introduction of system biology, multi-omics techno-logies(genomics, transcriptomics, proteomics, and metabolomics) have surged, which have been applied to the research on the mec-hanisms of Chinese medicinal processing. These multi-omics technologies have advantages in the research on holism. This study aims to summarize the research techniques and approaches in system biology for mechanisms of Chinese medicinal processing in the past 20 years and analyze the limitations and advantages of them. It is concluded that the multi-omics techniques of system biology can reconstruct the mechanisms of Chinese medicinal processing. This study provides a new direction for further research on the mechanisms of Chinese medicinal processing.

Twenty years in the 21st century: research hotspots and frontier analysis on Chinese medicine processing mechanism / 中国中药杂志

The research on the processing mechanism of Chinese medicine is the key and core foundation to improve processing technologies of Chinese medicine, formulate the quality standards of Chinese medicinal pieces, enhance the clinical efficacy of Chinese medicine, enrich Chinese medicine processing theories, and promote the development of Chinese medicine processing. Many researc-hers have conducted in-depth exploration on the processing mechanism of Chinese medicine in the 20 years in the 21 st century. Significant progress has been made in the transformation of chemical components during the processing, the change of active components in the body, the law of toxicity attenuation in the processing of toxic Chinese medicine, the mechanism of efficacy enhancement and toxicity attenuation of processing with auxiliary materials, and the application of new biomedical technologies. At present, the processing mechanism of multiple Chinese medicines has been preliminarily clarified, which has greatly promoted the development of Chinese me-dicine processing. The development of the processing mechanism of Chinese medicine reveals that the in vitro transformation of chemical components is combined with the in vivo absorption, transport, and metabolism, and the macroscopic biological effects of the organism are combined with the cells, molecules, targets, and pathways in the study of the processing mechanism of Chinese medicine. More attention has been paid to exploring the processing mechanism from the overall level, and a modern systematic research system on the processing mechanism of Chinese medicine has been initially formed. To further promote the scientific development of Chinese me-dicine processing, the present study proposed that the research on the processing mechanism of Chinese medicine should take Chinese medicine properties into account, focus on the influence of disease condition on the mode of action and effect strength of the drugs, comply with the characteristics of clinical compound compatibility of Chinese medicine, use the holistic view research strategies of systems bio-logy, and deeply explore the processing mechanism of Chinese medicine from traditional Chinese medicine theories and the characteristics of clinical medication of Chinese medicine.

Twenty years in the 21st century: identification technologies for and multimodal research on chemical changes in exploration of processing mechanism of Chinese medicine / 中国中药杂志

Chinese medicine undergoes complex chemical changes during processing and identifying these changes is the key to the processing mechanism. In the past 20 years of the 21 st century, research on the chemical changes in Chinese medicine after processing has focused the changes in the biopharmaceutical process in addition to the variation during processing. With the surging of information technologies, various identification technologies(instrumental analysis techniques, molecular biological techniques, data mining techniques, and biotransformation techniques) have developed rapidly and been widely applied to the research on processing mechanism. Thus, based on the chemical changes in the processing and biopharmaceutical process, the author suggested a research tactic of multimodal identification as the core by reorganizing key technologies for chemical identification from studies of the processing mechanism of Chinese me-dicine, aiming at establishing an interdisciplinary multi-dimensional research model for the processing mechanism of Chinese medicine.

Nomenclature standardization of Chinese medicine extracts and components / 中国中药杂志

Chinese medicine extracts are the important pharmaceutical materials of Chinese medicinal preparations, but their nomenclature still needs improvement in the field of traditional Chinese medicine(TCM). By the analysis of the evolution rules of names of Chinese medicine extracts recorded in the Chinese Pharmacopoeia, this study proposed a three-level nomenclature of "Chinese medicine name+chemical information+extract" based on the standardization problems involved in the existing nomenclature, striving to accurately suggest the material basic information on extract names. Meanwhile, the basic elements of Chinese medicine components, the special case from Chinese medicine extracts, were clarified, and the core connotations of the professional names were discriminated to arouse attention and discussions of researchers, facilitate the standardization of Chinese medicine terminology, and promote the scienti-fic development of Chinese medicinal preparations, and the modernization and internationalization of Chinese medicine.

Protective effects of Moutan Cortex polysaccharides components on renal injury in diabetic nephropathy rats / 中国中药杂志

This study investigated the protective effects of Moutan Cortex polysaccharides components(MCPC) on the renal tissues of diabetic nephropathy(DN) rats and explored their regulation effect on inflammatory response and oxidative stress. The DN rat model was induced by high-glucose and high-fat diet combined with streptozotocin(STZ), and then the rats were randomly divided into control group, model group, positive group and MCPC high(120 mg·kg~(-1)·d~(-1)), low(60 mg·kg~(-1)·d~(-1)) dose groups. After 12 weeks treatment, blood was taken from the orbit of the rats, and then they were sacrificed before the kidney tissues were collected. The serum and tissues were detected for related biochemical indicators and pathological changes of the kidney. Immunohistochemical methods were used to determine the expression of FN and ColⅣ in the kidney tissue of DN rats. Compared with the model group, blood glucose, serum creatinine, blood urea nitrogen and 24 h urine protein in the MCPC high-dose group were significantly reduced(P<0.01). The results of HE, PAS, Masson staining showed that glomerular basement membrane thickening, Bowman's capsule narrowing and inflammatory cell infiltration in DN rats were improved in the MCPC high-dose group; the activity of T-SOD and GSH-Px in serum significantly increased(P<0.001), and the expression level of FN significantly decreased(P<0.001). The high-dose MCPC treatment could effectively inhibit the abnormal expression of Col Ⅳ(P<0.001) and significantly reduce the levels of AGEs and RAGE in serum(P<0.001), the content of VCAM-1 and IL-1β in serum(P<0.001), and the levels of IL-1β mRNA in kidney tissue(P<0.001), but failed to effectively reduce VCAM-1 mRNA levels in kidney tissues. The high-dose MCPC could significantly improve pathological injury of renal tissue and related renal indicators in DN rats, and achieve renal protection in DN rats mainly by regulating oxidative stress and inflammatory factors.

Dynamic two-dimensional characterization technique and influencing factors analysis of the hygroscopicity of Chinese medicine extracts / 药学学报

This study aims to construct a dynamic two-dimensional characterization technique for the hygroscopicity of traditional Chinese medicine extracts and investigate the effect of material properties of powders on hygroscopicity. The dynamic hygroscopicity-time curves of the powders were measured at 25 ℃ and 75% humidity, and the semi-equilibrium hygroscopicity time (t1/2) and equilibrium hygroscopicity (F∞) were derived as two-dimensional evaluation indicators. Finally, the correlation between the material properties and the hygroscopic behavior was analyzed by principal component analysis (PCA) and partial least squares analysis (PLS). The results showed that the dynamic two-dimensional characterization system of hygroscopicity constructed with 1/t1/2 = 0.1 h-1 and F∞ = 15% as the center can classify the hygroscopic behavior of traditional Chinese medicine extracts into four categories: fast hygroscopicity with strong hygroscopicity, slow hygroscopicity with strong hygroscopicity, fast hygroscopicity with weak hygroscopicity and slow hygroscopicity with weak hygroscopicity. The moisture absorption was negatively correlated with D50, D90, ρb and ρt; the moisture absorption rate was negatively correlated with D10, D50, D90, ρb, ρt, and positively correlated with moisture content. The hygroscopicity dynamic two-dimensional characterization indicators of Chinese medicine extracts (CMEs) constructed in this study matched with the physical properties. The method of dynamic multi-dimensional characterization technology is feasible and scientific, and the idea has strong promotional value.

Literature Analysis and Textual Research on Huaihuasan / 中国实验方剂学杂志

Huaihuasan， first recorded in Puji Benshifang by XU Shu-wei from the Southern Song dynasty， consists of four herbs， namely Sophorae Flos （fried）， Platycladi Cacumen （smashed with pestle and baked）， Schizonepetae Spica， and Aurantii Fructus （cut into pieces after the removal of pulp and then fried yellow with wheat bran）. At present， Huaihuasan and its modified formulas vary in clinical usages and dosages， and the resulting outcomes have been investigated. However， there are few reviews uncovering its historical evolution. On this basis， this review systematically combed and verified the historical evolution， dose conversion between ancient and modern times， efficacy， and indications of Huaihuasan， as well as the origin and processing of the contained herbs. The findings have demonstrated that Huaihuasan is composed of four herbs， with the original plants and medicinal parts basically the same as those recorded in the 2020 edition of Chinese Pharmacopoeia. Sophorae Flos refers to the dried flower and bud of Sophora japonica in family Leguminosae， Platycladi Cacumen the dried branch and leaf of Platycladus orientalis in family Cupressaceae， Schizonepetae Spica the dried flower spike of Schizonepeta tenuifolia in family Labiatae， and Aurantii Fructus the dried immature fruit of Citrus aurantium in family Rutaceae or its cultivated varieties. On account of the efficacy in clearing intestine， stopping bleeding， dispersing wind， and moving Qi， Huaihuasan has been mainly used to treat intestinal diseases such as bloody defecation and perianal abscess. In modern clinical practice， it is mainly applicable to patients with hematochezia and bleeding due to internal hemorrhoid， ulcerative colitis， or anal fissure. It was suggested that the raw medicinal materials should be decocted and processed according to the methods described in the 2020 edition of Chinese Pharmacopoeia. Following the conversion formula of one Qian=4 g， this paper determined the dosages of Sophorae Flos （fried）， Platycladi Cacumen （smashed with pestle and baked）， Schizonepetae Spica， and Aurantii Fructus （cut into pieces after the removal of pulp and then fried yellow with wheat bran） all to be 2 g， with the total dosage being 8 g. Such comprehensive analysis based on ancient books and modern literature has provided a more scientific reference for the clinical application， research， and development of this classical formula.

The overview of the property system and characterization techniques of Chinese medicine materials before the pharmaceutical / 药学学报

At present, the modernization of Chinese medicine preparations (CMPs) is still a challenging task. The 3 typical Chinese medicine materials (CMMs) used for preparing CMPs are the powders, extracts, and components of Chinese medicine and their properties of CMMs are important for designing CMPs. Basing on our long term research, we have established a property system for CMMs according to the state of CMMs under an exactly condition and according to the interaction characteristics between substances. The property system could be divided into 5 categories: material composition, spatial structure, body property, surface property, physicochemical properties, and they could also be divided into 18 subcategories. Furthermore, we also established the corresponding index and characterization system, where the 61 indexes and characterization techniques were systematically summarized. At last, we hope that the article will promote the modernization of CMPs.

Micro-particulate Ganoderma lucidum spore β-glucanin enhances the antitumor activity of gemcitabin via remodeling immunosuppressive microenvironment in Lewis lung cancer / 药学学报

Gemcitabine (GEM) is a commonly used drug in the clinical treatment of non-small cell lung cancer. Due to the accumulation of cells mediating immune escape and T cell depletion after chemotherapy, tumor microenvironment (TME) tends to be immunosuppressive status, which ultimately leads to tumor metastasis. The experimental protocol was approved by the Medical Laboratory Animal Ethics Committee of Jiangsu Provincial Academy of Chinese Medicine. Therefore, we observed the immunomodulatory effects of micro-particulate Ganoderma lucidum spore β-glucan (PGSG) on macrophages in vitro experiments. Next, mice subcutaneous Lewis lung cancer models were established to observe the anti-tumor effects of PGSG through oral administration of PGSG combined with GEM. Flow cytometry analysis was used to analyze the ratio of anti-tumor T cells in tumors and spleen, as well as the proportion of myeloid-derived suppressor cells (MDSC), tumor-associated macrophages (TAM) and regulatory cells (Tregs). The results showed that PGSG can up-regulate the expression of major histocompatibility antigens (MHC-II), CD40, CD86 and CD80 on the surface of macrophages, enhance the ability to phagocytosis of neutral red and further mediate the release of interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), interleukin-4 (IL-4) and interleukin-10 (IL-10). In vivo experiments, combined administration can significantly decrease the volume and weight of tumors, reduce the ratio of MDSC (CD11b+Gr-1+), M-MDSC (CD11b+Ly6G-Ly6Chigh) and Treg (CD4+Foxp3+). At the same time, PGSG promoted the conversion of M2 (F4/80+CD206+) to M1 (F4/80+MHC-II+) and enhanced the response of helper T cell-1 (Th1) (CD4+IFN-γ+) and cytotoxic T lymphocyte (CTL) (CD8+IFN-γ+), which is of great significance for killing tumors. These results suggest that PGSG can regulate innate and adaptive antitumor immune responses, reshape the immunosuppressive microenvironment and enhance the anti-lung cancer effect of GEM.

Powder modificationfor improving content uniformity of Ziyin Yiwei Capsules / 中国中药杂志

Based on the defects in powder properties of the contents of Ziyin Yiwei Capsules, this study screened out the main medicinal slice powders causing the poor powdery properties, and introduced the powder modification process to improve the powdery properties of these slice powders, the pharmaceutical properties of the capsule contents, and the content uniformity of Ziyin Yiwei Capsules, so as to provide a demonstration for the application of powder modification technology to the preparation of Chinese medicinal solid preparations. Through the investigation on the powder properties of the contents of Ziyin Yiwei Capsules, it was clarified that the pulverized particle size of the capsule contents had a good correlation with the pulverization time. According to the measurement results of the powder fluidity and wettability, the quality defects of the capsule contents were caused by the fine powders of Taraxaci Herba and Lungwortlike Herba. "Core-shell" composite particles were prepared from medicinal excipients magnesium stearate and fine powders of Taraxaci Herba and Lungwortlike Herba slices after ultra-fine pulverization to improve the powder properties of the problematic fine powders. Powder characterization data including fluidity and wettability were measured, followed by scanning electron microscopy(SEM) and infrared ray(IR) detection. It was determined that the optimal dosage of magnesium stearate was 2%, and the compositing time was 3 min. The composite particles were then used as content components of the Ziyin Yiwei Capsules. The powder characteristics between the original capsule and the modified composite capsule including the particle size, fluidity, wettability, uniformity of bulk density, and uniformity of chromatism as well as the content uniformity and in vitro dissolution were compared. The results showed that the powder characteristics and content uniformity of the prepared composite capsule were significantly improved, while the material basis of the preparation was not changed before and after modification. The preparation process was proved to be stable and feasible. The powder modification technology solved the pharmaceutical defects that were easy to appear in the preparation of traditional capsules, which has provided experimental evidence for the use of powder modification technology for improving the quality of Chinese medicinal solid preparations and promoting the secondary development and upgrading of traditional Chinese medicinal dosage forms such as capsules.

Particle design for improving content uniformity of Hewei Jiangni Capsules / 中国中药杂志

Targeting the poor powder characteristics of the contents in Hewei Jiangni Capsules, this study characterized the powder properties of the contents and employed particle design technique for improving the content quality. The content composite particles of Hewei Jiangni Capsules prepared by the particle design technique were evaluated by scanning electron microscopy(SEM), followed by infrared ray(IR), content uniformity, and in vitro dissolution detection. It was found that there was a good correlation between the crushed particle size of slices and the crushing time, and the calcined Haematitum was responsible for the poor content uniformity. After the fine powder of calcined Haematitum was super-finely ground for 8.5 min and those of the other contents in the capsule for 1 min, they were prepared into the composite particles, whose property characterizations were compared with those of the physical mixtures. The content uniformity of the prepared composite particles was significantly improved, and the preparation process was stable and reliable. The adoption of particle design technology to correct the poor uniformity of the physical mixture, solve the pharmaceutical defects of Hewei Jiangni Capsules, and improve the quality of prescriptions has provided important reference for the clinical application and development of Chinese medicinal preparations.

Particle design for improving taste and homogeneity of traditional Chinese medicinal powder: taking Zhuhuang Chuihou Powder as an example / 中国中药杂志

Due to the complex source and different physical and chemical properties of traditional Chinese medicines(TCM) powder, there are many common pharmaceutical problems in its preparation, such as large particle size difference, poor mixing uniformity, and poor compliance with oral intake, which has directly affected the quality of solid preparations as well as their clinical efficacy and safety. This study observed the property of Zhuhuang Chuihou Powder and extract its pharmaceutical defects. It was found that realgar and calcined Borax in Zhuhuang Chuihou Powder were heavy in texture and toxic, and they were easy to be isolated, indicating the potential safety hazard. At the same time, Coptidis Rhizoma and Phellodendri Chinensis Cortex were the main sources of its bitterness. Therefore, based on the idea of "drug-excipients unity", the particle design technology was used to prepare core/shell-type composite particles with bitter medicines as the core and mineral medicines as shell. Both infrared spectroscopy and scanning electron microscopy results indicated the formation of composite particles, and the taste of these composite particles were improved. Compared with the physical mixtures, the composite particles exhibited significantly decreased RSD values in the content uniformity of berberine hydrochloride, arsenic disulfide, and sodium tetraborate and appearance uniformity. The introduction of particle design technology solved the problem of uneven dispersion of Zhuhuang Chuihou Powder, thus ensuring its uniform dispersion, stability, and control and improving the quality of the original preparation. This has provided a scientific basis for the quality control of TCM powder.

Application of design technology for preparing Lingzhu Powder particles based on solvent evaporation method / 中国中药杂志

Targeting the deficiencies of Lingzhu Powder, this study introduced the particle design technology to improve its quality. Based on the mechanism of particle design for powder and the characteristics of solvent evaporation method, composite particles consisting of Succinum, Cinnabaris, and artificial Bovis Calculus were prepared. And the powder properties of composite particles and physical mixtures as well as the content uniformity of toxic components were investigated for exploring the technological advantages of particle design in improving the quality of Lingzhu Powder. The results showed that the composite particles prepared using solvent evaporation method and particle design technology were micro-particles, and the stable agglomerate structure could be observed under SEM. Composite particles exhibited better fluidity and compliance in oral intake than physical mixtures. The differences in chromatism, bulk density, and content uniformity of the composite particles were smaller than those of physical mixtures, and the corresponding RSD values \[4.8%, 1.8%, 3.4%(bilirubin), and 0.63%(HgS), respectively\] were smaller. The solvent evaporation combined with particle design technology can be utilized to significantly improve the quality of Lingzhu Powder, which has provided new ideas for the optimization of the quality of traditional Chinese medicinal powder.

Study on anti-hygroscopic technology based on correlations between particle spatial properties and hygroscopicity of Chinese medicinal extracts / 中国中药杂志

This study was designed to investigate the correlations of the spatial structure properties of Chinese medicinal extracts with hygroscopicity and the anti-hygroscopic techniques. With Poria extract used as the model drug, pregelatinised starch and microcrystalline cellulose at different ratios were added into Poria fluid extract for preparing powder particles with diverse spatial structures using different drying processes. Then, their hygroscopic behaviours were characterized by equilibrium hygroscopicity(F~∞) and semi-hygroscopic time(t_(1/2)). The correlations of the hygroscopicity of each powder with the spatial structure properties such as particle size(D_(90)), porosity(ε), true density(ρ_t), and surface element distribution were analyzed using partial least-squares method. The F~∞ and t_(1/2) values of Poria extract prepared by three drying methods were sorted in a descending order as follows: F~∞(spray drying>drying at ordinary pressure>drying at reduced pressure); t_(1/2)(drying at reduced pressure>drying at ordinary pressure>spray drying). The powder obtained by spray drying showed a spherical structure with the smallest particle size and intra-particle ε but relatively stronger hygroscopicity. The large-scale surface element enrichment of the powders dried by reduced pressure effectively reduced their hygroscopicity. F~∞ and t_(1/2) were negatively correlated with ε but positively with D_(90), and the interactive influence of each spatial structural properties was not significant. There existed a correlation between the spatial structure of the powder particles of Chinese medicine extracts and their hygroscopicity, and the hygroscopicity could be improved by designing the spatial structure. This study has provided some practical basis for developing the moisture-proof technology of Chinese medicinal preparations.

Application of particle design technology in field of traditional Chinese medicine powder / 中国中药杂志

Solid preparations account for more than 50% of traditional Chinese medicines(TCM). TCM powder is an important raw material for solid preparations of TCM. Its powder properties directly affect the quality of solid preparations, and even clinical safety and effectiveness. Particle design technology based on the characteristics of powder in TCM is an important means to improve and enhance the quality of solid preparations. This study summarized the relevant principles, methods, characteristics, classification, equipment, and other elements of particle design technology in recent years, analyzed the difficulties in its application in the field of TCM powder, and proposed the strategies in conjunction with the development of computer data mining. The present study is expected to provide a reference for the suitability of particle design in the field of TCM powder.

Effects and mechanism of epimedium polysaccharide on solubility of icariin and baohuoside Ⅰ / 中国中药杂志

This study evaluated the effects of epimedium polysaccharide(EPS) on the solubility of icariin and baohuoside Ⅰ so as to preliminary explore its solubilization function and the underlying mechanism. The solubility of these two insoluble flavonoids in water and polysaccharide solutions was compared by high performance liquid chromatography, and the mechanism was investigated by diffe-rential scanning calorimetry(DSC) and critical micelle concentration determination. The results indicated that their solubilization in crude EPS solutions was concentration-dependent. The solubility of icariin and baohuoside Ⅰ in 20 mg·mL~(-1) EPS-1-1 was 9.05 times and 5.76 times that in water, respectively; while their solubility in 20 mg·mL~(-1) EPS-2-1 was 10.55 and 8.39 times that in water, respectively. The change of the DSC thermograms suggested the formation of new complexes from icariin and baohuoside Ⅰ with polysaccharides. The critical micelle concentrations proved the micellar properties of both EPS-1-1 and EPS-2-1. In short, EPS can significantly increase the solubility of icariin and baohuoside Ⅰ, the mechanism of which may be related to the formation of micellar complexes between EPS and insoluble flavonoids.

Virtual screening of components of safflower against myocardial ischemia based on molecular docking technology / 中国中药杂志

The screening of active components of traditional Chinese medicine has always been the focus and difficulty in modern research of Chinese medicine preparations. With the continuous development of life science, omics and computer technology, the virtual screening technology for active components of traditional Chinese medicine has gradually come into people's vision. Molecular docking technology is an important method for screening active components of traditional Chinese medicine. It not only has a short cycle and strong operability, but also avoids the disadvantage of poor stability in pharmacological experiments. Safflower extract can effectively alleviate the symptoms of myocardial ischemia, but its active components are not clear. In this study, with use of the molecular docking technology, the active components in safflower against myocardial ischemic were virtually screened based on the screening method of active components. Forty-six chemical components and 5 target proteins which showed high correlation with myocardial ischemia were obtained from the existing database and related literature reports. With the molecules of three commercially available drugs diltiazem, trimetazidine and verapamil as positive control molecules, the compomnents were docked with 5 target proteins. Active components were screened according to docking scores and interactions between molecules and targets, and then the active ingredients can be inferred. Fourteen chemical components were screened to have the most potential anti-myocardial ischemic activity, and all of them were flavonoids. Therefore, it can be inferred that the flavonoid components are the most potential anti-myocardial ischemic components in safflower. The screening of active anti-myocardial ischemia components in safflower was completed in this study, laying the foundation for subsequent researches.