Spectrum-effect relationship of total anthraquinone extract of Cassia seeds against fluorouracil-induced liver injury in mice / 南方医科大学学报

OBJECTIVE@#To investigate the spectrum-effect relationship between the total anthraquinone extract of Cassia seeds and fluorouracil (5-Fu)-induced liver injury in mice and identify the effective components in the extract.@*METHODS@#A mouse model of liver injury was established by intraperitoneal injection of 5-Fu, with bifendate as the positive control. The serum levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) and myeloperoxidase (MPO), superoxide dismutase (SOD) and total antioxidant capacity (T-AOC) in the liver tissue were detected to investigate the effect of the total anthraquinone extract of Cassia seeds (0.4, 0.8 and 1.6 g/kg) on liver injury induced by 5-Fu. HPLC fingerprints of 10 batches of the total anthraquinone extracts were established to analyze the spectrum- effectiveness of the extract against 5- Fu- induced liver injury in mice and screen the effective components using the grey correlation method.@*RESULTS@#The 5- Fu- treated mice showed significant differences in liver function parameters from the normal control mice (P < 0.05), suggesting successful modelling. Compared with those in the model group, serum ALT and AST activities were decreased, SOD and T- AOC activities significantly increased, and MPO level was significantly lowered in the mice treated with the total anthraquinone extract (all P < 0.05). HPLC fingerprints of the 31 components in the total anthraquinone extract of Cassia seeds showed good correlations with the potency index of 5-Fu-induced liver injury but with varying correlation strengths. The top 15 components with known correlations included aurantio-obtusina (peak 6), rhein (peak 11), emodin (peak 22), chrysophanol (peak 29) and physcion (peak 30).@*CONCLUSION@#The effective components in the total anthraquinone extract of Cassia seeds, including aurantio-obtusina, rhein, emodin, chrysophanol, and physcion, are coordinated to produce protective effects against 5-Fu-induced liver injury in mice.

Screening the effective components in treating dampness stagnancy due to spleen deficiency syndrome and elucidating the potential mechanism of Poria water extract / 中国天然药物

Poria is an important medicine for inducing diuresis to drain dampness from the middle energizer. However, the specific effective components and the potential mechanism of Poria remain largely unknown. To identify the effective components and the mechanism of Poria water extract (PWE) to treat dampness stagnancy due to spleen deficiency syndrome (DSSD), a rat model of DSSD was established through weight-loaded forced swimming, intragastric ice-water stimulation, humid living environment, and alternate-day fasting for 21 days. After 14 days of treatment with PWE, the results indicated that PWE increased fecal moisture percentage, urine output, D-xylose level and weight; amylase, albumin, and total protein levels; and the swimming time of rats with DSSD to different extents. Eleven highly related components were screened out using the spectrum-effect relationship and LC-MS. Mechanistic studies revealed that PWE significantly increased the expression of serum motilin (MTL), gastrin (GAS), ADCY5/6, p-PKAα/β/γ cat, and phosphorylated cAMP-response element binding protein in the stomach, and AQP3 expression in the colon. Moreover, it decreased the levels of serum ADH, the expression of AQP3 and AQP4 in the stomach, AQP1 and AQP3 in the duodenum, and AQP4 in the colon. PWE induced diuresis to drain dampness in rats with DSSD. Eleven main effective components were identified in PWE. They exerted therapeutic effect by regulating the AC-cAMP-AQP signaling pathway in the stomach, MTL and GAS levels in the serum, AQP1 and AQP3 expression in the duodenum, and AQP3 and AQP4 expression in the colon.

Effect of Rhizophagus intraradices on growth of Salvia miltiorrhiza / 中国中药杂志

The study aimed to explore the effects of inoculation of Rhizophagus intraradices on the biomass, effective component content, and endogenous hormone content of Salvia miltiorrhiza through pot experiments. The number of leaves, plant height, dry weight of aboveground and underground parts, branch number, root number, root length, root diameter, and other biomass were mea-sured by weighing and counting methods. The content of salvianolic acid B, caffeic acid, rosmarinic acid, tanshinone Ⅰ, tanshinone Ⅱ_A, cryptotanshinone, and other effective components was determined by ultra-high performance liquid chromatography. The content of ABA and GA_3 was determined by triple quadrupole mass spectrometry. The correlations between biomass and effective components and between effective components and plant hormones ABA and GA_3 were analyzed. The results showed that R. intraradices significan-tly increased the aboveground dry weight, leaf number, and root number of S. miltiorrhiza by 0.24-0.65 times, respectively. The content of salvianolic acid B and rosmarinic acid in the aboveground part and the content of salvianolic acid B, caffeic acid, rosmarinic acid, tanshinone Ⅰ, and tanshinone Ⅱ_A in the underground part were significantly increased by 0.44-1.78 times, respectively. R. intraradices infection significantly increased the GA_3/ABA values of aboveground and underground parts by 3.82 and 76.47 times, respectively. The correlation analysis showed that caffeic acid, the effective component of the aboveground part, was significantly positively correlated with plant height, tanshinone Ⅱ_A, the effective component of the underground part, was significantly positively correlated with biomass root number, cryptotanshinone, and dry weight, while rosmarinic acid was significantly negatively correlated with dry weight. There were significant positive correlations between cryptotanshinone and ABA, tanshinone Ⅱ_A and ABA and GA_3, and caffeic acid and GA_3. In conclusion, R. intraradices can promote the accumulation of biomass and secondary metabolites of S. miltiorrhiza and regulate the balance between plant hormones ABA and GA_3, thereby promoting the growth of S. miltiorrhiza.

Analysis on Material Basis of Anti-COPD Effect of Euphorbia helioscopia Based on Serum Pharmacochemistry and Network Pharmacology / 中国实验方剂学杂志

ObjectiveTo analyze the migrating components absorbed into blood of the aqueous extract of Euphorbia helioscopia， and to explore the pharmacodynamic material basis of the aqueous extract of E. helioscopia against chronic obstructive pulmonary disease（COPD）. MethodUltra-performance liquid chromatography-quadrupole-time-of-flight mass spectrometry（UPLC-Q-TOF-MS/MS） was used to detecte the migrating components absorbed into blood of rats after intragastric administration of aqueous extract of E. helioscopia. An Agilent RRHD SB-C18 column（3 mm×100 mm， 1.8 μm） was used with 0.1% formic acid aqueous solution（A）-acetonitrile（B） as the mobile phase for gradient elution（0-15 min， 5%-30%B； 15-20 min， 30%-50%B； 20-30 min， 50%-95%B； 30-35 min， 95%-5%B）， and the detection wavelength of 190-800 nm， column temperature of 40 ℃， flow rate of 0.3 mL∙min-1 and injection volume of 4 μL. The electrospray ionization（ESI） was used in positive and negative ion modes， and the detection range was m/z 50-1 250. Network pharmacology was used to screen out the key components and the key targets of COPD through the interaction analysis. Metascape database was used to predict the molecular function， biological process， cellular composition and signal pathways mainly involved in the anti-COPD effect of E. helioscopia. Molecular docking technique was used to determine the affinity of key targets with key components. ResultA total of 29 migrating components absorbed into blood of rats were identified after intragastric administration of aqueous extract of E. helioscopia， 9 of which were prototype components and 20 were metabolites. Network pharmacological analysis showed that luteolin， quercetin， apigenin， naringenin and helioscopinolide C were the key components of E. helioscopia against COPD， and vascular endothelial growth factor A（VEGFA）， albumin（ALB）， protein kinase B1（Akt1）， tumor necrosis factor（TNF） and interleukin-6（IL-6） were the key targets. Molecular docking results showed that one diterpene lactone（helioscopinolide C） and three flavonoids（naringenin， luteolin， apigenin） in the migrating components absorbed into blood all had strong binding activity to the key targets of E. helioscopia against COPD. ConclusionNaringenin， helioscopinolide C， luteolin and apigenin may be the main anti-COPD active substances of E. helioscopia.

Research progress on effective components，pharmacological mechanisms and clinical use of Polyporus umbellatus in diuresis-promotion and dampness-clearance / 中国药房

Polyporus umbellatus， as a traditional Chinese medicine for promoting diuresis and clearing dampness， mainly contains steroids and polysaccharides. It is usually used to treat diseases of urinary system. In this paper， the research progress of the effective components， pharmacological mechanisms and clinical use of P. umbellatus in diuresis-promotion and dampness- clearance is reviewed. Steroids such as ergosterone， peroxyergosterone， ergosta-7，22-dien-3-one and P. umbellatus polysaccharide PPS1， PPS2， PPS3， GUMP-1-1 and GUMP-1-2 promote diuresis and eliminate dampness through diuresis， renal protection， anti- inflammatory， bacteriostatic and immunomodulatory effects. Traditional Chinese medicine compound preparations such as P. umbellatus powder， P. umbellatus decoction， and Wuling powder have significant effects in treating urinary tract infections， lithiasis， renal edema and lesions， which providing reference for the further development and application of P. umbellatus.

Lipid-lowering Effect of Active Components in Common Chinese Medicine： A Review / 中国实验方剂学杂志

Dyslipidemia is a common metabolic disease caused by abnormal lipoprotein metabolism in human body. According to pathogenesis， it is divided into primary dyslipidemia and secondary dyslipidemia. The former is caused by genetic defects， and the latter is caused by diseases， drugs， unhealthy diets， and lifestyle. The clinical manifestations are xanthoma， arteriosclerosis， and other symptoms of coronary heart disease and peripheral vascular disease. Dyslipidemia can cause a variety of diseases， such as cardiovascular disease， diabetes， and cancer， seriously threatening people's quality of life and life safety， so the research on drugs against dyslipidemia is more urgent. In spite of manifest efficacy， chemical antilipemic agents such as lovastatin are accompanied by some adverse reactions， and there is recurrence after drug withdrawal. Compared with chemical drugs， Chinese medicine has the advantages of multi-pathway， multi-target， multi-level regulation of dyslipidemia， with few side effects. Modern medical research has shown that Chinese medicine can affect lipid synthesis， decomposition， and absorption and improve liver lipid and bile acid metabolism by regulating the peroxisome proliferator-activated receptor （PPAR） signaling pathway， AMP-activated protein kinase （AMPK） signaling pathway， cyclic adenosine monophosphate （cAMP） signaling pathway， adipocytokine signaling pathway， farnesoid X receptor （FXR）/small heterodimer partner （SHP） signaling pathway， phosphatidylinositol 3-kinase （PI3K）/protein kinase B （Akt） signaling pathway， etc.， thereby exerting a role in lowering lipid. Therefore， this paper summarized the mechanism of effective components in Chinese medicine in lowering blood lipid to provide new ideas and a theoretical basis for the prevention and treatment of lipid metabolic diseases by Chinese medicine in clinical practice.

Content Difference of Effective Components of Cynomorii Herba Between Different Producing Areas and Its Response to Environmental Factors / 中国实验方剂学杂志

ObjectiveTo explore the content difference of gallic acid，protocatechuic acid，catechin，total flavonoids， and total polysaccharides in Cynomorii Herba between different producing areas and the correlation between effective components and environmental factors. MethodNinety-five batches of Cynomorii Herba samples were collected from 12 major producing areas in five provinces （autonomous regions）， including Gansu，Inner Mongolia，Xinjiang，Qinghai， and Ningxia，and the geographical-climatic factors such as altitude，longitude and latitude，climate type，annual average frost-free period，annual rainfall，annual sunshine hours，annual average temperature， and annual average evaporation were recorded. The content of gallic acid，protocatechuic acid， and catechin in Cynomorii Herba was determined by high-performance liquid chromatography （HPLC），and the mathematical model of the correlation between the content of chemical components and environmental factors was optimized and established. ResultPearson correlation analysis showed that protocatechuic acid content in Cynomorii Herba increased with the increase in annual average frost-free period and annual average temperature， and catechin content increased with the increase in the annual average frost-free period，annual sunshine hours， and annual average evaporation，while total polysaccharides content decreased with the increase in altitude. Redundancy analysis （RDA） showed that the annual average frost-free period， annual average evaporation，annual sunshine hours， and altitude had great influences on the content of effective components in Cynomorii Herba. Curve fitting showed that the optimal conditions for the growth of Cynomorii Herba were as follows： altitude of 800-2 000 m，annual average frost-free period of 80-110 d， annual rainfall of 110-300 mm，annual sunshine hours of 2 400-3 000 h， annual average temperature of 2.2-8.8 ℃，and annual average evaporation of 1 700-2 500 mm. ConclusionThe content of effective components in Cynomorii Herba is diverse in terms of producing areas and shows a clear response rule to environmental factors. The areas suitable for growing and artificial cultivation introduction are those with high altitude，short annual average frost-free period，low annual rainfall，large average evaporation，long sunshine hours， and low annual average temperature.

Research progress on effective components and mechanisms of anti-depressive Chinese medicine / 中国中药杂志

Since the pathogenesis of depression is complicated, the therapeutic effects of western medicine are poor accompanied by severe side effects. Chinese medicine has unique advantages in the treatment based on syndrome differentiation and contains many effective components against depression, including flavonoids, terpenes, phenylpropanoids, quinones, and alkaloids. These chemical components can delay the course of the disease, improve the curative effect, and reduce side effects of western medicine by regulating the biochemical abnormalities of monoamine neurotransmitters, brain tissue protein content, and internal environment as well as energy metabolism to make the treatment of Chinese medicine highlighted and recognized. This study systematically reviewed the effective components and mechanisms of anti-depressive Chinese medicine to inspire the rational development and utilization of new Chinese medicines against depression.

"Six-step strategy" for effective compounds in Chinese medicinal prescriptions based on in vitro-in vivo integration and its application in research on component-based Chinese medicine / 中国中药杂志

The discovery and identification of effective components are pivotal in the research on Chinese medicinal prescriptions. Given two basic conditions for effective components in Chinese medicinal prescriptions, i.e., active structure and a certain level of drug exposure in the body(including the intestine), a "six-step strategy" for the effective compounds in Chinese medicinal prescriptions based on in vitro-in vivo integration(SSS for short) has been proposed and established, as well as the key technologies. SSS contains qualitative and quantitative analyses of components in five steps, including those in Chinese medicinal extract, intestinal contents, portal vein blood, liver, and peripheral blood. The components(prototype components and metabolites) with a certain exposure level(including in the intestine) and those with large differences between in vitro content and in vivo exposure or in exposure among various parts in the body are selected as the minority prioritized candidates. The sixth step is to screen the pharmacological activity of candidate components specifically extracted from Chinese medicinal materials or artificially synthesized. SSS can significantly narrow the screening range, enhance the hit rate, and speed up the identification of effective components specifically targeting indications. Based on the effective components identified by the SSS, the "upstream" can be linked(mechanism research based on the effective components with clear structures) and the "downstream" can be combined(development of innovative component-based Chinese medicine with definite pharmacodynamic composition). In this study, the concept of component-based Chinese medicine and specific applications of SSS in the development of component-based Chinese medicine are also introduced.

Screening of effective antioxidant components from Trichosanthes extract and assessment of their antioxidant activity / 南方医科大学学报

OBJECTIVE@#To screen the effective antioxidant components in Trichosanthes extract based on the mean value of Deng's correlation degree and assess the antioxidant activity of the identified components.@*METHOD@#High-performance liquid chromatography (HPLC) was used to obtain the fingerprints of Trichosanthes extract, and the clearance rates of DPPH · and O2-· by 3, 9 and 27 mg/mL Trichosanthes extract were determined. The antioxidant spectrum effect of Trichosanthes extract was analyzed by calculating the mean value of Deng's correlation degree to screen the effective antioxidant component group. According to the contents of each known components in the antioxidant effective component group, mixed solutions of the components were prepared and tested for their clearance rates of DPPH · and O2-·.@*RESULTS@#The 36 common peaks in HPLC fingerprints of Trichosanthes extract showed different degrees of correlation with DPPH · and O2-· clearance. The common peaks with a correlation degree greater than the median value included peaks 21, 36, 8, 31, 14, 5, 27, 2, 24, 15, 18, 33, 22, 34, 35, 19, 28 and 25. The 5 components, namely kaempferol (peak 36), isoquercitrin (peak 8), luteolin (peak 31), rutin (peak 5) and apigenin (peak 35), were tentatively identified to constitute the effective antioxidant component group with a mass ratio 3∶2∶2∶ 1∶1 in Trichosanthes extract. The prepared mixed solutions of antioxidant effective component group (6.12, 2.04, and 0.68 μg/mL) showed clearance rates of DPPH · of 65.4%, 64.0% and 61.0%, and clearance rates of O2-· of 12.9%, 9.5% and 8.3%, respectively.@*CONCLUSION@#We identified the material basis for the antioxidant activity of Trichosanthes and screened the antioxidant effective component group in Trichosanthes extract.

New Progress in Mechanism of Salviae Miltiorrhizae Radix et Rhizoma in Treatment of Diabetes and Its Complications / 中国实验方剂学杂志

Diabetes is a worldwide public health problem that seriously threats human health. Long-term metabolic disorders， as the main cause of multi-system complications and death in the later stage of diabetes， can cause multi-system damage， leading to chronic progressive lesions in the eyes， kidneys， nerves， heart， blood vessels and other tissues and organs， as well as functional decline and failure. The low risk of side effects and new treatment strategies remain an area to be explored in clinical treatment of diabetes. Salviae Miltiorrhizae Radix et Rhizoma （SM） is one of the commonly used herbs in traditional Chinese medicine （TCM）， with the main effect of activating blood circulation and removing blood stasis. In recent years， it has been found that SM shows good performance in lowering blood sugar and treating diabetes complications. Data mining information has also shown that the drugs of activating blood circulation and removing blood stasis are now common drugs in clinical treatment of diabetes， and SM has the highest use frequency， with significant curative effect. In addition， TCM is a kind of treatment with composite components and multiple targets， and so people are increasingly interested in its effective components and carry out extensive researches. This article summarized the experimental verification of SM extract and its components （tanshinone A， tanshinone B， tanshinone ⅡA， tanshinone I， protocatechuic aldehyde， polysaccharide， and total polyphenol acid） in various diabetes models in improving glucolipid metabolism， improving heart function in patients with diabetes， alleviating the motor and sensory deficits caused by diabetes， preventing the occurence of the diabetic retinopathy， recovery of liver and kidney structure and function damage in diabetic patients， and helping to resist high sugar-induced atrophic cavitation potential. It may inhibit hyperglycemia-induced vascular injury with polyol pathway activation， reduce the formation of advanced glycation end products， inhibit protein kinase C pathway activation and hexosamine pathway activation， and alleviate oxidative stress caused by excessive production of peroxides in mitochondrial electron transport chain during hyperglycemia to play a role of treatment， and provide reference for clinical application.

Anti-inflammatory effect, plasma effective components and therapeutic targets of Huanglian Jiedu Decoction on ulcerative colitis mice / 中国中药杂志

This paper was to investigate the effect of Huanglian Jiedu Decoction(HLJD) on ulcerative colitis(UC) in mice, and determine the effective components in plasma, and virtually screen its therapeutic target, and predict its mechanism. Sixty Balb/c mice were randomly divided into blank group, model group, mesalazine treatment group(0.3 g·kg~(-1)), and HLJD treatment groups(24.66, 12.33, 6.17 g·kg~(-1)). Excepted for the blank group, all the mice in HLJD and mesalazine treatment groups were gavage administration. All mice freely drank 2.5% DSS solution for seven days to induce UC. The disease activity index(DAI) was detected each day. At the end of the experiment, HE staining was used to observe the pathological changes in colon. The content of IL-1β, IL-6 and TNF-α in colon were determined by ELISA. The effective components in plasma were determined by UPLC-Q-TOF-MS. The reverse docking in PharmMapper was used to screen the component targets. The disease targets of UC were collected by searching TTD, OMIM and GeneCards databases. The intersection of the component targets and disease targets was selected as the therapeutic targets. Then the therapeutic targets were imported into the STRING for GO and KEGG enrichment analysis. Discovery Studio was used to simulate the docking between the components and the targets. RESULTS:: showed that the DAI in the model group increased significantly(P<0.05), and the number of inflammatory cells and infiltration degree increased significantly compared with the blank group. The DAI in HLJD treatment group was significantly reduced(P<0.05), and the number and infiltration degree of inflammatory cells were reduced compared with the model group. The ELISA results showed that the levels of IL-1β, IL-6 and TNF-α were increased significantly in the model group(P<0.01) compared with the blank group, and significantly down regulated in the HLJD treatment group(P<0.05) compared with the model group. After UPLC-Q-TOF-MS analyse, ten components were identified. The network pharmacology analysis showed that the action targets were significantly enriched in 129 of biological processes, such as response to organic substance, chemical and oxygen-containing compound, etc., as well as 16 of signal pathways, such as IL-17, TNF and hepatitis B signal pathways, were enriched too. The results of molecular docking showed that limonin, palmatine and berberine could bind to CASP3 and MMP9 by hydrogen bond. In conclusion, HLJD could alleviate the colonic mucosal inflammatory infiltration and mucosal damage in UC mice. The mechanism may be related to the anti-inflammatory effect on UC mice by reducing the levels of IL-1β, IL-6 and TNF-α in colon through limonin, palmatine and berberine regulating IL-17 signal pathway and TNF signal pathway via CASP3 and MMP9 meditated.

Effect of Zengmian Yiliu Formula and Its Effective Components on Notch/Jagged1 Signaling Pathway of Ovarian Cancer Stem Cell Transplanted Tumor in Nude Mice / 中国实验方剂学杂志

Objective:To observe the effect of Zengmian Yiliu （ZMYL） formula and its effective components （PAWU） on the growth inhibition of ovarian cancer stem cell transplanted tumor in nude mice and the Notch signal receptor （Notch） / Notch signal ligand 1 （Jagged1） signal pathway in tumor tissue. Method:Ovarian cancer stem cells were cultured in serum-free suspension to establish the transplanted tumor model of ovarian cancer stem cells in nude mice， and then divided into model group， ZMYL group （36 g·kg-1）， PAWU group （5.8 g·kg-1）， cisplatin （DDP） group （2.5 g·kg-1）， and PAWU （5.8 g·kg-1） + DDP group （2.5 mg·kg-1）.After successful modeling， the drugs were given by gavage for 21 days.To observe the effect of Zengmian Yiliu decoction and its effective components on tumor weight in nude mice， the morphological changes of tumor cells were observed under light microscope， immunohistochemistry and real-time fluorescence quantitative polymerase chain reaction（Real-time PCR）were used to detect the expressions of Notch 1， Jagged1， Hairy and enhancer of split 1 （Hes1） protein and mRNA in tumor tissues. Result:The tumor inhibition rates of ZMYL， PAWU， DDP and combination groups were 35.91%， 32.94%， 57.65% and 69.05%， respectively.Compared with the model group， the tumor weight of ZMYL group， PAWU group， DDP group and combination groups decreased significantly （P<0.05）.Compared with PAWU group， the tumor weight of combination groups decreased significantly （P<0.05）.Immunohistochemistry showed that compared with the model group， the positive expressions of Notch1， Jagged1 in ZMYL group， PAWU group， DDP group and combination groups were down-regulated （P<0.05），and the positive expressions of Hes1 in ZMYL group， DDP group and combination groups were down-regulated （P<0.05）.Compared with combination groups， the positive expressions of Notch1， Jagged1 and Hes1 in ZMYL group， PAWU group， DDP group were up-regulated （P<0.05）. Real time PCR showed that compared with the model group， the expressions of Notch1 mRNA in ZMYL group， PAWU group， DDP group and combination groups decreased significantly （P<0.05）.Compared with model group， the expressions of Jagged1 and Hes1 mRNA in ZMYL group， PAWU group and combination groups decreased significantly （P<0.05）.Compared with DDP group， the expressions of Notch1， Jagged1 and Hes1 mRNA in combination groups decreased significantly （P<0.05）. Conclusion:The growth of ovarian cancer stem cells transplanted in nude mice can be inhibited by Zengmian Yiliu formula and its effective components.The effective components have a significant synergistic effect in the combination with cisplatin.Its mechanism is correlated to the inhibition of Notch/Jagged1 signaling pathway activation.

Review on factors influencing separation and purification of Chinese materia medica components by macroporous adsorption resin / 中草药

In recent years, macroporous adsorption resin has been widely used in the purification and separation of natural medicine and effective components of Chinese materia medica, the purification of compound Chinese medicine preparations, the removal of harmful impurities due to the advantages of stable physical and chemical properties, high selectivity, strong adsorption capacity and easy elution, recyclable use and regeneration treatment, economic and environmental protection, convenient preparation molding and so on. By summarizing the preparation, properties, classification and working principle of macroporous adsorption resin, the influencing factors and purification process of Chinese materia medica components were reviewed. The purpose of this paper is to explore the important factors affecting the purification of Chinese materia medica components by macroporous adsorption resin, and provide reference for improving the purification effect of Chinese materia medica components.

Influences of ancient processing method steaming with black bean and drying and pharmacopoeia processing method continuous steaming with black bean decoction on 12 components of Polygoni Multiflori Radix / 中草药

Objective: To explore the influence of ancient processing method black bean "nine cycles of steaming and drying" and modern pharmacopoeia processing method continuous steaming with black bean decoction on the main components of Polygoni Multiflori Radix (PMR). Methods: Simulating the time arrangement of "nine cycles of steaming and drying", samples were prepared using three processing methods: ancient method that raw PMR (rPMR) and black bean were steamed in layers and then dried, modern method that rPMR were steamed with black bean decoction and then dried, the method recorded in Chinese Pharmacopoeia that rPMR were steamed continuously with black bean decoction; The determination method of 12 components in rPMR and processed PMR (pPMR) was established using ultra-performance liquid chromatography with triple quadrupole mass spectrometry (UPLC-QqQ-MS/ MS), and 12 components in all samples processed by different methods were determined; The results was analyzed combining with t test, principal component analysis (PCA) and orthogonal partial least square-discriminant analysis (OPLS-DA). Results: A reliable UPLC-QqQ-MS/MS method was established for the determination of emodin, physcion, rhein, emodin-8-O-β-D-glucoside, physcion-8-O-β-D-glucoside, cis-2,3,5,4'-tetrahydroxylstilbene-2-O-β-D-glucoside (cis-THSG), trans-2, 3,5,4'-tetrahydroxylstilbene- 2-O-β-D-glucoside (trans-THSG), polydatin, resveratrol, epicatechin, rutin and hyperoside. With the prolongation of steaming time, the content of 12 effective components changed obviously: the content of free anthraquinone was decreased first and then increased; The content of anthraquinone glycoside, cis-THSG, polydatin and hyperoside was increased first and then decreased; The content of trans-THSG, resveratrol, epicatechin and rutin was decreased; The components content were closely related to the auxiliary materials, steaming operation methods and processing time, the influence of operation methods was greater than that of auxiliary materials on the quality of pPMR. Conclusion: The ancient processing method steaming with black bean and drying could not be equated with the modern pharmacopoeia processing method continuous steaming with black bean decoction in terms of the content of effective components. The result provides experimental basis for inheriting and developing the traditional processing method of PMR.

Research progress on effective components of Chinese materia medica in regulating autophagy / 中国中药杂志

Autophagy is a highly conservative and multi-component activated energy metabolism and self-renewal mechanism, which plays a crucial regulatory role in maintaining the normal physiological state of cells and is involved in various pathological processes. In recent years, the mechanism study has made great progress in regulating autophagy with effective components of Chinese materia medica(CMM),which are reported to prevent and treat cancers, neurodegenerative diseases, cardiovascular diseases and metabolic and immune-related diseases. This review outlines the molecular regulation mechanisms of cell autophagy with CMM components in controlling the above-mentioned diseases. There are many relevant reports on the regulatory mechanisms of autophagy in tumor and cardiovascular cells with CMM monomers. The main chemical structural types are alkaloids, saponins, polyphenols, flavonoids and terpenes. And m-TOR pathway is the main mechanism relating to the regulatory mechanisms of autophagy with CMM. Therefore, the regulatory mec-hanisms of cell autophagy become a new research targeting strategy of therapies with CMM. This review provides evidences for the effectiveness and scientificity of CMM in regulating autophagy, in the expectation of providing references for the in-depth studies of CMM in the field of autophagy and the development of natural autophagy regulators.

Study on Potential Mechanism of the Seed of Draba nemorosa Based on Network Pharmacology / 中国药房

OBJECTIVE： To investigate the potential pharmacological mechanism of the seed of Draba nemorosa， and to provide reference for further development， utilization and clinical application. METHODS： Effective components and related target proteins of D. nemorosa were screened and identified by using TCMSP and STRING database. Cytoscape 3.7.0 software was used to construct a visual network of effective components and target proteins for the seed of D. nemorosa， and the network topology analysis was performed. The targeting protein-protein interaction （PPI） network was constructed and analyzed by STRING database and Cytoscape 3.7.0 software. KEGG pathway enrichment of target proteins was analyzed by DAVID bioinformatics resource database. RESULTS： A total of 9 effective components were screened from the seed of D. nemorosa， including quercetin， kaempferol， β-sitosterol， etc. Totally 174 target proteins were obtained， mainly including PTGS2， NCOA2， PGR， etc. Among them， JUN and MAPK1 were core proteins in PPI network. KEGG enrichment pathway included PI3K/Akt signaling pathway， TNF-α signaling pathway， HIF-1 signaling pathway， Toll-like receptor signaling pathway and thyroid hormone signal pathway， etc. CONCLUSIONS： Effective components from the seed of D. nemorosa such as quercetin， kaempferol and β-sitosterol may act on PTGS2， JUN and MAPK1 target proteins through PI3K-Akt signaling pathway and TNF-α signaling pathway， thus exert the effects of purging lung， relieving asthma， promoting edema and reducing edema.

Study on Potential Effective Components and Mechanism of Achyranthes bidentata in the Treatment of Osteoporosis Based on Network Pharmacology / 中国药房

OBJECTIVE： To investigate the potential effective components and mechanism of Achyranthes bidentata in the treatment of osteoporosis （OP）. METHODS： The effective components of A. bidentata were retrieved from the TCMSP database， and corresponding targets of them were collected. The targets related to OP were retrieved from DisGeNET database. TBtools 1.0 mapping software was used to draw the Wayne diagram， and screen the intersecting targets of effective components of A. bidentata and disease OP. Cytoscape 3.6.1 software and STRING database were used to construct and analyze the “drug-component- disease-target” network and protein-protein interaction （PPI） network； KEGG pathway enrichment analysis was conducted by using DAVID bioinformatics resource database. RESULTS： A total of 19 effective components were screened from A. bidentata， and there were 32 intersecting targets between effective components and disease OP. In “drug-component-disease-target” network， there were 45 nodes [1 for A. bidentata， 1 for OP， 11 for effective components （8 of the 19 effective components had no corresponding OP target）， 32 for intersecting targets] and 119 edges between nodes； quercetin， kaempferol， wogonin， baicalein and palmatine were important effective components. In PPI network， there were 31 nodes （1 of 32 intersecting targets was not associated with other proteins） and 212 edges， among which IL6， ESR1， MAPK1， IL8 and MAPK14 were the core targets of the network. There were 67 KEGG enrichment pathways， including rheumatoid arthritis， hepatitis B， Toll-like receptor signaling pathway， PI3K/Akt signaling pathway， JAK/STAT signaling pathway， NF-κB signaling pathway and so on. CONCLUSIONS： The main potential effective components of A. bidentata in the treatment of OP are quercetin， kaempferol， wogonin， baicalein and palmatine， the mechanism of which may be associated with cell differentiation and apoptosis， metabolism， inflammation reaction， etc. It     has multi-component， multi-target and multi-system chara- cteristics.

Establishment of an antibacterially effective components fingerprint for quality evaluation of Scutellariae Radix (Huangqin) / 药学学报

A chemical fingerprint is an important mean for quality control of traditional Chinese medicine (TCM); however, there is much redundant information in a conventional fingerprint that can affect its availability and accuracy. In this work, the antibacterial biopotency of Scutellariae Radix (Huangqin, HQ) was determined according to the parallel line method of quantitative response. HPLC was adopted to detect the chemical fingerprint of HQ; Grey relational analysis (GRA) was used to identify the primary effective components. The results showed that the antibacterial biopotency of 15 batches of HQ ranged from 0 to 1 000 U·g-1 and the average potency was 556.29 ± 258.57 U·g-1 (1 U is equivalent to the bacteriostatic activity of 2.25 μg gentamicin). There were 34 characteristic peaks in the fingerprints of the samples and their similarities were 0.255-0.991. Eight components (P33, P30/baicalein, P19/baicalin, P15, P29, P34, P31/wogonin and P28) are positively related to antibacterial biopotency and selected from the top ten components of the grey correlation sequence to define the antibacterially effective components fingerprint of HQ. This fingerprint can clearly distinguish the commodity specification and grade, and can also characterize the morphology, components and the bacteriostatic potency differences of HQ. In summary, we established an antibacterially effective components fingerprint which provides simplified information on the antibacterial activity of Scutellariae Radix and could significantly improve the efficacy, specificity, and discriminative ability of the fingerprint for HQ, and could be a useful reference for the comprehensive quality evaluation of other TCM.

Effective components of traditional Chinese medicine for regulating TGF-Beta1/Smads signaling pathway in hepatic fibrosis / 中国中药杂志

Hepatic fibrosis is a liver damage healing response affected by a variety of factors; its formation is associated with multiple cytokines and a variety of signaling pathways. Transforming growth factor beta1( TGF-β1) is one of the strongest fibrosis cytokines known,and involves almost all the key links in hepatic fibrosis. TGF-β1/Smads signal pathway is the most classical pathway for TGF-β1 to play its role in promoting fibrosis as well as one of the most important signaling pathways of hepatic fibrosis formation. Studies for the signal pathway have made a series of scientific research achievements in recently years. Traditional Chinese medicine has the advantages of " multiple ingredients,multiple targets and less side effects",and is widely used in the clinical treatment of hepatic fibrosis.Effective components of traditional Chinese medicine are monomer compounds,which are extracted and purified from traditional Chinese medicine. Nowadays,the molecular biology studies of effective traditional Chinese medicine have become a hotspot. Modern advanced technology and methods can be used to directly clarify the targets and the signaling pathways,reveal the mechanism of traditional Chinese medicine in treating diseases,and promote the modernization and international development of traditional Chinese medicine industry. This review summarized the structure,function and application of TGF-β1/Smads signaling pathway in the progress of anti-hepatic fibrosis,and analyzed the action mode and possible mechanism of various effective components of traditional Chinese medicine in regulating TGF-β1/Smads signaling pathway and intervening the treatment of hepatic fibrosis in the past five years,so as to put forward new ideas for innovating new targeted traditional Chinese medicine for hepatic fibrosis.