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ObjectiveTaking Achyranthis Bidentatae Radix（ABR） from different origins as samples， to quantitatively analyze the chemical composition and chromaticity of ABR with different processing degrees， and clarify the correlation and change law between color and composition in the processing process of ABR， so as to provide reference for the quality evaluation of processed products of ABR. MethodThe colorimeter is used to measure the chromaticity values of three kinds of processing degrees of ABR in different origins to show the color value change trend during the processing process， and the color parameters of wine-processed and salt-processed products of ABR with different processing degrees were analyzed by principal component analysis（PCA）， orthogonal partial least squares-discriminant analysis（OPLS-DA） and other analysis methods. The contents of eight representative components of ABR were measured by high performance liquid chromatography（HPLC）， the correlation between chromaticity and each representative component was analyzed by Pearson correlation analysis， and the applicability of the selected eight representative components was further verified by Fisher linear discriminant analysis， and the wine-processed and salt-processed products of ABR with different processing degrees were grouped according to the degree of processing， and 48 samples of wine-processed and salt-processed products with different processing degrees were used as training samples. Taking the contents of 5-hydroxymethylfurfural， polypodine B， β-ecdysterone， 25R-inokosterone， 25S-inokosterone， ginsenoside Ro， chikusetsusaponin Ⅳa and polysaccharides as variables， the discriminant function was established respectively， and 12 samples of wine-processed and salt-processed products of ABR with different processing degrees were back-tested to verify the discriminant function and test the reliability of the function. ResultPCA and OPLS-DA results showed that ABR samples with different processing degrees were classified into clusters， and the results could significantly distinguish different processed products. During the process of wine and salt processing， the contents of 5-hydroxymethylfurfural， ginsenoside Ro， and chikusetsusaponin Ⅳa gradually increased with the deepening of the processing degree， while the contents of polypodine B， β-ecdysterone， 25R-inokosterone， 25S-inokosterone and polysaccharides showed a gradual decreasing trend， indicating these 8 components increased and decreased to different degrees in the process of wine and salt processing. The results of Pearson correlation analysis showed that the 5-hydroxymethylfurfural content of the samples with different processing degrees of wine-processed and salt-processed products were negatively correlated with the brightness value（L*） and the total color difference value（E*ab）（P<0.01）， and positively correlated with the red-green value（a*） and the yellow-blue value（b*）（P<0.01）， and that the content of polypodine B and polysaccharides were positively correlated with L* and E*ab（P<0.01）. The discriminant functions of wine-processed and salt-processed products of ABR were established by Fisher linear discriminant analysis， and their accuracy rates in the training samples were 93.75% and 95.83%， respectively. Twelve test samples of wine-processed and salt-processed products with different processing degree were back substitution， and the correct rate was 100%. ConclusionThe trend of composition and color changes of ABR with different processing degrees in different production areas is relatively consistent， and the color value can better distinguish ABR with different processing degrees， and the color of ABR is related to some representative components in the processing process， indicating that the color can provide reference for the identification of the processing degree of ABR and the prediction of component content.

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Based on FangNet platform,the data of the prescriptions for the effective cases of post-stroke sequelae treated by national renowned Chinese medical practitioner LIU Mao-Cai were collected for the analysis of medication frequency of the prescribed drugs as well as their properties,flavors and meridian tropism.The medication rules of LIU Mao-Cai for treating post-stroke sequelae was summarized by analyzing the weight scale,co-occurrence and mutual exclusivity of the prescribed drugs and by drug-symptom association rule analysis and drug clustering analysis.The results showed that a total of 105 prescriptions involving 95 Chinese medicines were obtained.The drugs in the prescriptions were mainly warm in nature,sweet in flavor and had the meridian tropism of liver meridian.There were 17 driver herbs,and they were Astragali Radix,Gastrodiae Rhizoma,Corni Fructus,Codonopsis Radix,Eucommiae Cortex,Achyranthis Bidentatae Radix,Chuanxiong Rhizoma,Polygalae Radix,Curcumae Longae Rhizoma,Acori Tatarinowii Rhizoma,Ophiopogonis Radix,Atractylodis Macrocephalae Rhizoma,Salviae Miltiorrhizae Radix et Rhizoma,Poria,Uncariae Ramulus cum Uncis,Pinelliae Rhizoma Praeparatum,and Ligustri Lucidi Fructus.The results of drug co-occurrence analysis yielded 12 drug pairs such as Achyranthis Bidentatae Radix-Eucommiae Cortex,drug-symptom association rule analysis yielded 9 groups of drug-symptom association combinations such as Gastrodiae Rhizoma-dizziness,and cluster analysis yielded 4 drug combinations.The results indicated that the drugs for post-stroke sequelae treated by LIU Mao-Cai are mild in nature and mainly have the actions of supporting healthy-qi and replenishing the deficient,and Astragali Radix and Codonopsis Radix are often used to replenish the vital energy,and Corni Fructus,Achyranthis Bidentatae Radix and Eucommiae Cortex are usually used to tonify the liver and kidney.Moreover,simultaneous treatment of phlegm and blood stasis,and simultaneous application of purging and nourishing therapeutics are also stressed.

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ObjectiveTo investigate the different effects of Yunvjian with or without Achyranthis Bidentatae Radix on glucose and lipid metabolism and inflammatory response in diabetic rats with the syndrome of Yin deficiency and internal heat. MethodThe rat model of diabetes due to Yin deficiency and internal heat was established by feeding with a high-sugar and high-fat diet and injection of thyroxine and streptozotocin. The successfully modeled rats were randomized into model control， Yunvjian without Achyranthis Bidentatae Radix （11.8 g·kg-1）， Yunvjian with Achyranthis Bidentatae Radix （12.8 g·kg-1）， and Achyranthis Bidentatae Radix （1.0 g·kg-1） groups （n=10）， and another 10 rats were taken as the normal control group. Each group was administrated with corresponding drugs or saline by gavage for 28 days. The fasting blood glucose （FBG）， fasting insulin （FINS）， total cholesterol （TC）， triglycerides （TG）， low-density lipoprotein cholesterol （LDL-C）， and high-density lipoprotein cholesterol （HDL-C） in rats were measured. Enzyme-linked immunosorbent assay was employed to determine the levels of cyclic adenosine monophosphate （cAMP）， cyclic guanosine monophosphate （cGMP）， triiodothyronine （T3）， thyroxine （T4）， interleukin （IL）-1β， IL-6， tumor necrosis factor （TNF）-α， and C-reactive protein （CRP） in the serum. The histopathological changes of the liver were observed. The expression of lipoxygenase-2 （COX-2） was detected by immunofluorescence. The mRNA levels of nuclear transcription factors-κB （NF-κB）， monocyte chemotactic protein-1 （MCP-1）， and intercellular adhesion molecule-1 （ICAM-1） were determined by real-time polymerase chain reaction （Real-time PCR）.Western blot was employed to determine the protein levels of NF-κB in hibitory protein（IκB） kinase β （IKKβ）， IκBα， and phosphorylated IκBα （p-IκBα） in the liver and the protein levels of NF-κB in the cytoplasm and nucleus. ResultCompared with the normal group， the model group showed elevated levels of FBG， FINS， insulin resistance index， TC， TG， LDL-C， cAMP， T3， T4， IL-1β， IL-6， TNF-α， and CRP， up-regulated mRNA levels of NF-κB， MCP-1， and ICAM-1， and up-regulated protein levels of COX-2， p-IκBα， and nuclear NF-κB （P<0.01）. Compared with the model group， Yunvjian without Achyranthis Bidentatae Radix lowered the levels of FBG， FINS， insulin resistance index， TC， TG， LDL-C， cAMP， T3， T4， IL-1β， IL-6， TNF-α， and CRP， down-regulated the mRNA levels of NF-κB， MCP-1， and ICAM-1， and down-regulated the protein levels of COX-2， p-IκBα and nuclear NF-κB （P<0.05， P<0.01）. Compared with the Yunvjian without Achyranthis Bidentatae Radix， Yunvjian with Achyranthis Bidentatae Radix showed lowered levels of FBG， FINS， insulin resistance index， and inflammatory cytokines， down-regulated mRNA levels of NF-κB， MCP-1， and ICAM-1， and down-regulated protein levels of p-IκBα and nuclear NF-κB （P<0.05， P<0.01）. ConclusionAchyranthis Bidentatae Radix can enhance the performance of Yunvjian in reducing blood glucose and inhibiting inflammation in diabetic rats with the syndrome of yin deficiency and internal heat by down-regulating the IKK/IκB/NF-κB signaling pathway.

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Objective: To investigate the targets and mechanism of Achyranthis bidentatae radix and Morindae officinalis radix (ABR-MOR) for the treatment of osteoporosis (OP) by utilizing network pharmacology, molecular docking technology (MDT) and molecular dynamics simulation (MDS). Methods: The main drug active ingredients (DAIs) and target genes of ABR-MOR were screened by the TCMSP database. The relevant targets of OP were obtained from GeneCards, DisGeNET, and CTD databases. Venny mapping is used to determine the potential target of ABR-MOR in the treatment of OP. The potential targets were analyzed using a protein‒protein interaction network and the MCODE module, and were subjected to GO and KEGG enrichment analysis. The binding sites and conditions of potential key DAIs and core targets were verified through MDT and MDS. Result: The 32 DAIs and 212 targets of ABR-MOR were screened; 1453 OP-related targets were obtained, and 118 targets were mapped. The results of GO and KEGG enrichment analysis showed that the targets of DAIs-OP were mainly enriched in biological processes such as response to hormones, peptides, oxygen levels and reactive oxygen species, and positive regulation of cell migration. The main signaling pathways enriched in the regulation of the immune-inflammatory response, cell proliferation, senescence, apoptosis, angiogenesis, and estrogen signaling pathway. Additionally, the targets were also enriched in bone metabolism-related cell differentiation biological processes and the osteoclast differentiation signaling pathway. MDT and MDS results showed that wogonin, beta-sitosterol, and americanin A, the core DAIs of ABR-MOR, were able to form good ligand‒protein complexes with key targets such as PTGS2, PTGS1, PRKACA, PGR, MAPK1, AKT1, and RELA. Conclusion: This study preliminarily investigated the key targets, biological processes, and signaling pathways involved in the combined application of ABR and MOR for the treatment of OP. The results revealed that ABR-MOR may play a therapeutic role mainly by regulating immune-inflammatory responses, cellular biological processes, and osteoblast differentiation, which provides a theoretical basis for further experimental validation and a new strategy for the treatment of OP.

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This work aimed to investigate the differences of pharmacokinetics and tissue distribution of four alkaloids in Ermiao Pills and Sanmiao Pills in normal and arthritic model rats. The rat model of arthritis was established by injecting Freund's complete adjuvant, and ultra-high performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS) in the positive ion multiple reaction monitoring(MRM) mode was used for the determination of four alkaloids in plasma and tissues of normal and arthritic rats after administration of Ermiao Pills and Sanmiao Pills, respectively. The differences in pharmacokinetics and tissue distribution of the four active components were compared, and the effect of Achyranthis Bidentatae Radix on the major components of Sanmiao Pills was explored. This study established an UPLC-MS/MS for simultaneous determination of four alkaloids, and the specificity, linearity, accuracy, precision, and stability of this method all met the requirements. Pharmacokinetics study found that as compared with normal rats, the AUC and C_(max) of phellodendrine, magnoflorine, berberine and palmatine in model rats were significantly decreased after administration of Ermiao Pills, the clearance rate CL/F was significantly increased, and the distribution and tissue/plasma concentration ratio of the four alkaloids in the liver, kidney, and joint were significantly reduced. Achyranthis Bidentatae Radix increased the AUC of phellodendrine, berberine, and palmatine, reduced the clearance rate, and significantly increased the distribution of the four alkaloids in the liver, kidney, and joints in arthritic rats. However, it had no significant effect on the pharmacokinetics and tissue distribution of the four alkaloids in normal rats. These results suggest that Achyranthis Bidentatae Radix may play a guiding role in meridian through increasing the tissue distribution of effective components in Sanmiao Pills under arthritis states.

Asunto(s)

Alcaloides , Artritis , Berberina , Medicamentos Herbarios Chinos , Ratas , Animales , Berberina/farmacocinética , Distribución Tisular , Cromatografía Liquida , Espectrometría de Masas en Tándem/métodos , Medicamentos Herbarios Chinos/farmacocinética , Alcaloides/farmacocinética , Cromatografía Líquida de Alta Presión/métodos

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Radiotherapy causes a series of side effects in patients with malignant tumors. Polygonati Rhizoma, Achyranthis Bidentatae Radix, and Epimedii Folium are all traditional Chinese herbs with varieties of functions such as anti-radiation and immune regulation. In this study, the above three herbs were used as a herbal diet to study their effects on the hematopoietic, immune, and intestinal systems of mice exposed to three doses of radiation. Our study showed that the diet had no radiation-protective effect on the hematopoietic and immune systems. However, at the radiation dose of 4 Gy and 8 Gy, the diet showed an obvious radiation-protective effect on intestinal crypts. At the dose of 8 Gy, we also found that the Chinese herbal diet had an anti-radiation effect on reducing the loss of the inhibitory nNOS+ neurons in the intestine. That provides a new diet for relieving the symptoms of hyperperistalsis and diarrhea in patients after radiotherapy.

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This work aimed to investigate the differences of pharmacokinetics and tissue distribution of four alkaloids in Ermiao Pills and Sanmiao Pills in normal and arthritic model rats. The rat model of arthritis was established by injecting Freund's complete adjuvant, and ultra-high performance liquid chromatography-tandem mass spectrometry(UPLC-MS/MS) in the positive ion multiple reaction monitoring(MRM) mode was used for the determination of four alkaloids in plasma and tissues of normal and arthritic rats after administration of Ermiao Pills and Sanmiao Pills, respectively. The differences in pharmacokinetics and tissue distribution of the four active components were compared, and the effect of Achyranthis Bidentatae Radix on the major components of Sanmiao Pills was explored. This study established an UPLC-MS/MS for simultaneous determination of four alkaloids, and the specificity, linearity, accuracy, precision, and stability of this method all met the requirements. Pharmacokinetics study found that as compared with normal rats, the AUC and C_(max) of phellodendrine, magnoflorine, berberine and palmatine in model rats were significantly decreased after administration of Ermiao Pills, the clearance rate CL/F was significantly increased, and the distribution and tissue/plasma concentration ratio of the four alkaloids in the liver, kidney, and joint were significantly reduced. Achyranthis Bidentatae Radix increased the AUC of phellodendrine, berberine, and palmatine, reduced the clearance rate, and significantly increased the distribution of the four alkaloids in the liver, kidney, and joints in arthritic rats. However, it had no significant effect on the pharmacokinetics and tissue distribution of the four alkaloids in normal rats. These results suggest that Achyranthis Bidentatae Radix may play a guiding role in meridian through increasing the tissue distribution of effective components in Sanmiao Pills under arthritis states.

Asunto(s)

Ratas , Animales , Berberina/farmacocinética , Distribución Tisular , Cromatografía Liquida , Espectrometría de Masas en Tándem/métodos , Medicamentos Herbarios Chinos/farmacocinética , Alcaloides/farmacocinética , Cromatografía Líquida de Alta Presión/métodos , Artritis

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In order to realize the rapid and non-destructive detection of SO_2 content in sulphur-fumigated Achyranthis Bidentatae Radix, this paper first prepared the sulphur-fumigated Achyranthis Bidentatae Radix samples with the usage amount of sulphur being 0, 2.5%, and 5% of the mass of Achyranthis Bidentatae Radix pieces. The SO_2 content in different batches of sulphur-fumigated Achyranthis Bidentatae Radix was determined using the method in Chinese Pharmacopoeia, followed by the acquisition of their hyperspectral data within both visible-near infrared(435-1 042 nm) and short-wave infrared(898-1 751 nm) regions by hyperspectral imaging. Meanwhile, the first derivative, AUTO, multiplicative scatter correction, Savitzky-Golay(SG) smoothing, and standard normal variable transformation algorithms were used to pre-process the original hyperspectral data, which were then subjected to characteristic band extraction based on competitive adaptive reweighted sampling(CARS) and the partial least square regression analysis for building a quantitative model of SO_2 content in sulphur-fumigated Achyranthis Bidentatae Radix. It was found that the accuracy of the quantitative model built depending on the visible-near infrared spectra was high, with the determination coefficient of prediction set(R■) reaching 0.900 1. The established quantitative model has enabled the rapid and non-destructive detection of SO_2 content in sulphur-fumigated Achyranthis Bidentatae Radix, which can serve as an effective supplement to the method described in Chinese Pharmacopeia.

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Imágenes Hiperespectrales , Raíces de Plantas , Análisis de los Mínimos Cuadrados , Azufre

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This study aimed to explore the possible mechanism of Achyranthis Bidentatae Radix for the treatment of osteoporosis using tandem mass tag-based proteomics technique combined with mass spectrometry. Proteomics techniques combined with bioinformatics were used to analyze the biological functions of differentially expressed proteins. In addition, western blotting was performed to verify the expression of related proteins. A total of 3,752 proteins were identifiable by proteomic analysis. Furthermore, 93 differentially expressed proteins were identified, of which 61 were upregulated and 32 were downregulated. Differentially expressed proteins were primarily associated with oxidative phosphorylation (p = 4.8 × 10-4 ) pathways and involved in transmembrane transport (p = 3.5 × 10-3 ), exocytic process (p = 1.2 × 10-2 ), cellular developmental process (p = 1.3 × 10-2 ), adenosine triphosphate metabolic process (p = 1.0 × 10-2 ) and other biological processes. Western blotting analysis showed that MT-CYB and NDUFA9 were differentially expressed in the bone microenvironment of rats with osteoporosis. We speculated that they were potential biomarkers linked to osteoporosis. This study employed proteomics to explore the potential therapeutic targets of Achyranthis Bidentatae Radix to treat osteoporosis. This revealed that mitochondria are a new target for the treatment of glucocorticoid-induced osteoporosis.

Asunto(s)

Medicamentos Herbarios Chinos , Osteoporosis , Animales , Biomarcadores , Medicamentos Herbarios Chinos/química , Osteoporosis/tratamiento farmacológico , Raíces de Plantas , Proteómica , Ratas

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Saponins and sterones are two main characteristic components in Achyranthis Bidentatae Radix. In order to control the quality of Achyranthis Bidentatae Radix more effectively, a high-performance liquid chromatography (HPLC) method was established by using double external standards calibration method (DESCM) for simultaneous determination of the contents of achyranthoside C, achyranthoside D, β-ecdysterone, 25R-inokosterone and 25S-inokosterone in Achyranthis Bidentatae Radix. Chromatographic separation was achieved on an Agilent Poroshell 120 EC-C18 (150 mm × 4.6 mm, 2.7 µm) using 0.1% phosphoric acid in water and 0.1% phosphoric acid in acetonitrile as mobile phase. The flow rate was 0.8 mL·min-1 and the column temperature was set as 35 ℃, the injection volume was 5 μL and the total analytical time was 30 min. β-Ecdysterone was used as the reference to calculate the relative correction factors (RCF) and relative retention time (RRT) of 25R-inokosterone and 25S-inokosterone, achyranthoside D was used for achyranthoside C. The RCFs of 25R-inokosterone, 25S-inokosterone, and achyranthoside C were 1.116, 1.056, and 0.888 1, respectively. The double external standards calibration method (DESCM) and external standard method (ESM) were used to calculate the contents of five ingredients in Achyranthis Bidentatae Radix samples from different sources and the variation between the results was within acceptable limits (RE ≤ 5%). The results showed that the contents of two saponins and three sterones of Achyranthis Bidentatae Radix were 0.597%-1.916% and 0.044%-0.150% respectively. The total content of saponins was about 10 times that of sterones. In conclusion, the established DESCM allowed simultaneous determination of five ingredients (achyranthoside C, achyranthoside D, β-ecdysterone, 25R-inokosterone, and 25S-inokosterone) in Achyranthis Bidentatae Radix, providing a scientific and feasible overall quality evaluation method for Achyranthis Bidentatae Radix.

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ObjectiveTo investigate the protective effect and mechanism of Achyranthis Bidentatae Radix-Paeoniae Radix Alba on dopaminergic neurons in Parkinson's disease mouse model with the syndrome of ascendant hyperactivity of liver Yang. MethodThe C57BL/6 mice were randomly assigned into normal group， a model group， low-， medium， and high-dose （3.25， 6.5， 13 g·kg-1） Achyranthis Bidentatae Radix-Paeoniae Radix Alba groups， and a selegiline group （0.01 g·kg-1）. The mouse model of Parkinson's disease with the syndrome of ascendant hyperactivity of liver yang was established by intragastric administration of Fuzitang combined with intraperitoneal injection of 1-methyl-4-phenyl-1，2，3，6-tetrahydropyridine （MPTP）. The behavioral changes were evaluated by rotarod test and pole test. The protein levels of Ras homolog gene family member A （RhoA）， Rho-associated coiled-coil containing protein kinase 2 （ROCK2）， myosin light chain 1 （MLC1）， and α-synuclein in the substantia nigra were determined by Western blot. Real-time fluorescence quantitative PCR （Real-time PCR） was employed to determine the mRNA levels of RhoA， ROCK2， and MLC1 in the substantia nigra. Enzyme-linked immunosorbent assay （ELISA） was used to measure the levels of tumor necrosis factor-α （TNF-α） and interleukin-1β （IL-1β）. The ultrastructural changes of mouse neurons were observed under a transmission electron microscope. ResultCompared with the normal group， the modeling shortened the latency to fall， increased the average total time in the pole test （P<0.01）， and up-regulated the levels of RhoA， ROCK2， MLC1， TNF-α， α-synuclein， and IL-1β in the substantia nigra （P<0.05）. Compared with the model group， different doses of Achyranthis Bidentatae Radix-Paeoniae Radix Alba and selegiline prolonged the latency to fall， shortened the average total time in the pole test （P<0.05， P<0.01）， and down-regulated the levels of ROCK2， MLC1， α-synuclein， TNF-α， and IL-1β in a dose-dependent manner （P<0.05）. Further， the modeling decreased the number of cytoplasmic organelles and caused mitochondrial swelling and abnormal shape of endoplasmic reticulum compared with the normal group. The neurons in high-dose Achyranthis Bidentatae Radix-Paeoniae Radix Alba and selegiline groups showed intact nuclei， clear cell boundary， and normal endoplasmic reticulum shape. ConclusionThe combination of Achyranthis Bidentatae Radix and Paeoniae Radix Alba may improve the motor coordination ability of Parkinson's disease mouse model with the syndrome of ascendant hyperactivity of liver yang by inhibiting the neuroinflammation mediated by the RhoA/ROCK2 signaling pathway in the brain.

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In order to realize the rapid and non-destructive detection of SO_2 content in sulphur-fumigated Achyranthis Bidentatae Radix, this paper first prepared the sulphur-fumigated Achyranthis Bidentatae Radix samples with the usage amount of sulphur being 0, 2.5%, and 5% of the mass of Achyranthis Bidentatae Radix pieces. The SO_2 content in different batches of sulphur-fumigated Achyranthis Bidentatae Radix was determined using the method in Chinese Pharmacopoeia, followed by the acquisition of their hyperspectral data within both visible-near infrared(435-1 042 nm) and short-wave infrared(898-1 751 nm) regions by hyperspectral imaging. Meanwhile, the first derivative, AUTO, multiplicative scatter correction, Savitzky-Golay(SG) smoothing, and standard normal variable transformation algorithms were used to pre-process the original hyperspectral data, which were then subjected to characteristic band extraction based on competitive adaptive reweighted sampling(CARS) and the partial least square regression analysis for building a quantitative model of SO_2 content in sulphur-fumigated Achyranthis Bidentatae Radix. It was found that the accuracy of the quantitative model built depending on the visible-near infrared spectra was high, with the determination coefficient of prediction set(R■) reaching 0.900 1. The established quantitative model has enabled the rapid and non-destructive detection of SO_2 content in sulphur-fumigated Achyranthis Bidentatae Radix, which can serve as an effective supplement to the method described in Chinese Pharmacopeia.

Asunto(s)

Imágenes Hiperespectrales , Análisis de los Mínimos Cuadrados , Raíces de Plantas , Azufre

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Steam explosion technology was employed for the pretreatment of Achyranthis bidentatae radix (ABR) under mild conditions, followed by the polysaccharide extraction. An increase in the extraction yield and uronic acid content of crude polysaccharide were detected, along with a decrease in the protein content induced by the steam explosion. The monosaccharide analysis showed the main compositional modification of polysaccharide is the increase in the proportion of galacturonic acid, galactose, and arabinose. It is consistent with the discriminant analysis of the FT-IR and UV-vis spectra. These structural modifications of crude polysaccharide caused by the steam explosion pretreatment (SEP) resulted in the significant increases in their antioxidant activities in vitro and in vivo. Strong correlations were observed between the pretreatment conditions and the changes in the structural characteristics and antioxidant activities of Achyranthis bidentatae radix polysaccharides (ABPS).

Asunto(s)

Antioxidantes , Vapor , Raíces de Plantas , Polisacáridos , Espectroscopía Infrarroja por Transformada de Fourier

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BACKGROUND AND AIM: Achyranthis Bidentatae Radix plus Semen Vaccariae are traditional Chinese medicines, which have been widely applied in the treatment of migraine and Erectile Dysfunction (ED) for many years. This study verified the effect of Achyranthis Bidentatae Radix plus Semen Vaccariae in improving migraine-induced ED and explored its potential mechanism. METHODS: Key targets and signaling pathways of Achyranthis Bidentatae Radix plus Semen Vaccariae in migraine-induced erectile dysfunction treatment were predicted by network pharmacology. A rat model of migraine was established by nitroglycerin injection. Apomorphine was injected into rats to screen the migraine-induced erectile dysfunction model, Achyranthis Bidentatae Radix-Semen Vaccariae granule suspension administered, and erectile function evaluated. Hematoxylin and eosin staining was used to compare the histological structure of the penile tissue, while RT-qPCR and Western blotting were used to determine mRNA and protein levels, respectively. RESULTS: Screening allowed us to identify common targets for migraine and ED; the signaling pathway exhibiting the greatest change was the Myosin light chain kinase- Calcium (MLCK-CaM) signal pathway. From Western blotting and RT-qPCR, we found that the levels of MLCK mRNA and protein in rats from Group B rats were significantly higher (P <0.05) than those in Groups A and C. Furthermore, the mRNA and protein levels of CaM were significantly higher in Group B (P <0.05) than in Groups A and C. CONCLUSION: Data indicate that the regulatory effects of Achyranthis Bidentatae Radix plus Semen Vaccariae on migraine-induced ED in a rat model are mediated by the MLCK-CaM signaling pathway.

Asunto(s)

Achyranthes , Medicamentos Herbarios Chinos , Disfunción Eréctil , Trastornos Migrañosos , Achyranthes/química , Achyranthes/genética , Animales , Medicamentos Herbarios Chinos/química , Disfunción Eréctil/tratamiento farmacológico , Humanos , Masculino , Trastornos Migrañosos/tratamiento farmacológico , Farmacología en Red , ARN Mensajero , Ratas , Semillas

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OBJECTIVE: To retrieve the core drug of osteoarthritis in clinic using Data Mining, predict the drug molecular action target through the Network Pharmacology, identify the key nodes of the interaction by combining with the related targtes of osteoarthritis, explore the pharmacological mechanism of Traditional Chinese Medicine against osteoarthritis and other possible mechanisms of actions. METHODS: to retrieve the commonly used therapeutic formulations for osteoarthritis patients in clinical with PubMed, CNKI, VIP, CBM, Wan Fang Database and other databases, and screen out the core drugs through the Ancient and Modern Medical Case Cloud Platform and software Gephi, filter out the core drug molecules and targets combined with TCMSP database and the targets of osteoarthritis in Genecard and OMIM database, plunge those data into R project and Cytoscape to construct the intersection model of Drug molecule-osteoarthritis, establish PPI network and GO and conduct KEGG enrichment analysis with String database. Vina molecular docking was finally implemented to draw molecular docking diagram, and the results were analyzed after comprehensive analysis. RESULTS: The core drug pairs were identified as 'Eucommiae Cortex - Achyranthis Bidentatae Radix' through correlation analysis, complex network analysis based on the coefficient. 'Eucommiae Cortex - Achyranthis Bidentatae Radix' can intervene cell behavior through multiple pathways and regulate cell metabolism, cytokine synthesis, oxidative and cellular immunity with the help of topology analysis in String Database. CONCLUSIONS: The core molecules of Quercetin and Kaempferol derived from 'Eucommia bark - achyranthes' can change the spatial conformation of PTGSs by hydrogen bonding with PTGSs, the hydrophobic bonds and van der Waals forces generated by Baicalein, Wogonin and ß-carotene, thereby changing the activity of PTGSs and affecting bone properties the process of osteoarthritis.

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Medicamentos Herbarios Chinos , Osteoartritis , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/uso terapéutico , Humanos , Medicina Tradicional China , Simulación del Acoplamiento Molecular , Farmacología en Red , Osteoartritis/tratamiento farmacológico

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Objective:To screen the active components of sovereign medicinal Achyranthis Bidentatae Radix in Rongjin Niantong formula based on bioinformatics and network pharmacology and observe their effects on therapeutic targets of osteoarthritis （OA） in <italic>in vivo</italic> and <italic>in vitro</italic> animal experiments. Method:The main active components and therapeutic targets of Achyranthis Bidentatae Radix were retrieved from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform （TCMSP）， and the differentially expressed genes relevant to OA from the Gene Expression Omnibus （GEO） database for cross analysis. The effects of main active components in Achyranthis Bidentatae Radix on enriched therapeutic targets of rats with OA <italic>in vivo </italic>and <italic>in vitro</italic> were detected by real-time polymerase chain reaction （Real-time PCR） and Western blot. Result:There were 20 active components for Achyranthis Bidentatae Radix against OA， with quercetin being an important one. Among the three target genes， osteopontin （OPN） and plasminogen activator inhibitor-1（PAI-1） were the key ones in the network. Gene Ontology （GO） analysis yielded 227 related terms， involving the regulation of physiological response to trauma （GO： 1903034）， negative regulation of trauma response （GO： 1903035）， etc. Kyoto Encyclopedia of Genes and Genomes （KEGG） pathway analysis revealed 12 related pathways， involving extracellular matrix receptor interaction （hsa04512） and so on. In animal experiments， compared with the normal group， the model group exhibited increased gene and protein expression of OPN and PAI-1. Compared with the model group， the quercetin group displayed decreased gene and protein expression of OPN and PAI-1 （<italic>P</italic><0.05）. In cell experiments， the OPN and PAI-1 protein expression levels in the model group were increased as compared with those in the normal group， while the Collagen Ⅱ protein expression was decreased. The OPN and PAI-1 protein expression levels in the quercetin group and the inhibitor group were down-regulated in contrast to those in the model group， whereas the Collagen Ⅱ protein expression levels were up-regulated significantly （<italic>P<</italic>0.05）. Conclusion:Achyranthis Bidentatae Radix<italic> </italic>inhibits cartilage degeneration and exerts the preventive and therapeutic effects against OA， which is possibly due to the efficacy of its active component quercetin in down-regulating the expression of OPN and PAI-1 in chondrocytes and up-regulating the Collagen Ⅱ protein expression.

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Objective:To study HPLC fingerprints of Achyranthis Bidentatae Radix from different origins,compare different specifications in the same origin,and explore the effect of origin and specifications on the quality of Achyranthis Bidentatae Radix and relationship between the specifications and the internal quality of Achyranthis Bidentatae Radix, in order to provide basis for the identification of its origin. Method:The HPLC fingerprints of Achyranthis Bidentatae Radix from different origins and with different specifications in the same origin were collected. The similarity analysis,cluster analysis and principal component analysis were adopted to analyze the fingerprints,the differences in fingerprints of Achyranthis Bidentatae Radix from different origins and with different specifications in the same origin were compared. Result:Analysis of different origins and principal component analysis could be used to distinguish Achyranthis Bidentatae Radix from five producing areas,and the identification results of origin analysis was better than those of cluster analysis and similarity analysis. Analysis of different specifications, similarity analysis or principal component analysis could not distinguish Achyranthis Bidentatae Radix with different specifications. Conclusion:There are significant differences in chemical composition and peak height among Achyranthis Bidentatae Radix from different origins,with less differences in chemical composition and peak height of Achyranthis Bidentatae Radix with different specifications, the principal component analysis could be used to identify origins of Achyranthis Bidentatae Radix.

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Objective This study was designed to predict the main targets of Alzheimer’s disease (AD) in Achyranthis Bidentatae Radix based on network pharmacology and molecular docking methods, and to explore its “multi-component, multi-target, and multi- pathway” mechanism. Methods According to the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP), the library of chemical constituents of Achyranthis Bidentatae Radix was established by referring to Chinese and foreign literature reports and collecting targets for treating AD in DrugBank. The Discovery Studio 3.5 software was used to carry out molecular docking, virtual screening of the chemical composition set of Achyranthis Bidentatae Radix combined with AD target, and KEGG database was used to enrich and analyze the key target of virtual screening. The active compounds of Achyranthis Bidentatae Radix with anti-AD activities were yielded to Discovery Studio 3.5 software and molecular docking to predict the poteneial proteins and carry out related KEGG pathways notation separately. Finally, the network of “active compound-target proteins-pathway” was built and analyzed using the Cytoscape 3.2.1 software. Results The 58 active compounds were selected from Achyranthis Bidentatae Radix, of which were mostly small alkanes, esters, and carboxylic acids followed by flavonoids and terpenoids. These active ingredients may regulate 36 potential target proteins such as CaMK-IIα, CaMK-IIβ, CaMK-IIγ, Akt1, and TNF-α to play a role in the pathogenesis of AD. The results also suggested that 12 signaling pathways were involved in the pathogenesis of AD, such as MAPK signaling pathway, Wnt signaling pathways and so on. Conclusion This research method initially revealed that the active ingredients of flavonoids and glycosides in Achyranthis Bidentatae Radix are the material basis for the treatment of AD. Its mechanism of action involved anti-inflammatory, anti-apoptosis and so on.

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ETHNOPHARMACOLOGICAL RELEVANCE: Sanmiao Wan (SMW) has been a basic prescription employed for the treatment for gout in the clinic since Yuan dynasty. Achyranthis bidentatae radix (ABR) is designed as a lower-guiding drug in SMW to augment the articular accumulation of active ingredients and improve the anti-inflammatory effect. AIM OF THE STUDY: Present study was undertaken to investigate the dose-response relationship of berberine in SMW between the articular concentration and anti-inflammatory effect in the knee joint under the lower-guiding of ABR. MATERIALS AND METHODS: Rats were divided into control group, model group and SMW without or with low, medium and high doses of ABR groups. Rat model of acute gouty arthritis (AGA) was established by intra-articular injection of 0.2 mL monosodium urate crystal (20 mg/mL) inside knee joint cavity on day 2 during drug treatment slots. Knee joint swelling, synovial hyperplasia and inflammatory cell infiltration were investigated for anti-inflammatory study. The concentrations of berberine in rat plasma and tissues were determined by UPLC-MS/MS method. The effect of ABR on the expression levels of P-glycoprotein (P-gp) and MDR1 mRNA in the synovial tissues of knee joints in AGA rats was examined by Western blot and RT-qPCR assay, respectively. RESULTS: The distribution of berberine increased by 6.53%, 44.31% and 212.96% in the knee joint and 474.93%, 631.01% and 1063.3% in the ankle for SMW with low, medium and high doses of ABR groups, compared with SMW without ABR group. Similarly, the plasma level of berberine increased by 19.81%, 143.4% and 681.13%. On the contrary, the distribution of berberine evidently decreased 3.23, 10.61 and 46.21-fold in heart and 3.68, 6.74 and 24.78-fold in lung. SMW with different doses of ABR groups exhibited better efficiency than SMW without ABR group on ameliorating knee joint swelling, inhibiting synovial hyperplasia and alleviating inflammatory cell infiltration of AGA rats. The treatment with ABR could down-regulate the MDR1 mRNA and P-gp expressions of synovial tissues of knee joints in AGA rats. CONCLUSIONS: The enhanced articular distribution of berberine in SMW was attributed to the lower-guiding effect of ABR, which could evidently increase the plasma concentration of berberine, improve the supply of blood of inflamed joint, reduce the distribution of berberine in heart and lung and significantly inhibit the MDR1 mRNA and P-gp expression of synovial tissues of knee joints in AGA rats. The dose-response relationship of berberine between the enhanced articular concentration and improved anti-inflammatory effect in the knee joint under the lower-guiding of ABR was observed for the first time.

Asunto(s)

Achyranthes , Antiinflamatorios , Artritis Gotosa/tratamiento farmacológico , Berberina , Medicamentos Herbarios Chinos , Miembro 1 de la Subfamilia B de Casetes de Unión a ATP/genética , Miembro 1 de la Subfamilia B de Casetes de Unión a ATP/metabolismo , Animales , Antiinflamatorios/sangre , Antiinflamatorios/farmacocinética , Antiinflamatorios/uso terapéutico , Artritis Gotosa/inducido químicamente , Artritis Gotosa/metabolismo , Artritis Gotosa/patología , Berberina/sangre , Berberina/farmacocinética , Berberina/uso terapéutico , Modelos Animales de Enfermedad , Medicamentos Herbarios Chinos/farmacocinética , Medicamentos Herbarios Chinos/uso terapéutico , Articulación de la Rodilla/efectos de los fármacos , Articulación de la Rodilla/metabolismo , Articulación de la Rodilla/patología , Masculino , Fitoterapia , Raíces de Plantas , Ratas Sprague-Dawley , Distribución Tisular , Ácido Úrico

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AIM To investigate the correlation between surface features and hygroscopicities of Achyranthis bidentatae Radix extract powders added with different excipients.METHODS Achyranthis bidentatae Radix aqueous extract was added with crospovidone CL-SF,maltodextrin DE11-14,β-cyclodextrin,Arabic gum,dextrin,mannitol,soluble starch and lactose,respectively,after which extract powders were prepared,and hygroscopicities and morphological changes were determined.Then the surface features of various extract powders were compared by double exponential model.RESULTS Compared with other excipients,soluble starch and β-cyclodextrin could reduce the saturated moisture content of the extract powders more obviously,and crospovidone CL-SF exhibited the strongest inhibitory effect on powder synechia after moisture absorption.No direct relationship between hygroscopicities and specific surface area or pore volume was observed,but specific surface area,pore volume and average particle size demonstrated positive correlations with model parameter A1.CONCLUSION Addition of proper excipients can improve the surface features and hygroscopicities of Achyranthis bidentatae Radix extract powders.