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In this paper, the antitussive and expectorant activity of platycodin D (PD) were studied by constructing a mouse cough induced by concentrated ammonia water and a mouse trachea phenol red excretion model. The mechanism of antitussive and expectorant effect of PD was studied by metabolomics. The animal experiment was approved by the Animal Ethics Committee of Jiangxi University of Chinese Medicine (approval number: JZLLSC-20220739). Then mice were randomly divided into the normal, model, positive drug, PD low-dose, PD medium-dose and PD high-dose group. The antitussive and expectorant effects of PD were evaluated using a cough mouse model induced by concentrated ammonia water and a mouse tracheal phenol red excretion model, respectively. UHPLC-LTQ-Orbitrap-MS was used to identify the metabolites of mouse lung tissue, and multivariate statistical analysis method of orthogonal partial least squares discriminant analysis (OPLS-DA) was used for metabolites profile analysis. The differential metabolites were screened by variable projected importance value (VIP) and t-test results. Pathways for enrichment of differentiated metabolites were analyzed using the MetaboAnalyst platform. The comparative method was applied to analyze the differences in mechanisms of PD, Deapio-platycodin D (DPD) and total platycosides fraction. The results showed that PD at different concentrations could significantly prolong (P < 0.05) the incubation period of cough mice induced by ammonia water, reduce the coughs frequency, and significantly increase (P < 0.05) the amount of phenol red excretion in phenol red excretion model mice. PD could regulate 6 metabolic pathways of phenylalanine, tyrosine and tryptophan biosynthesis, linoleic acid metabolism, phenylalanine metabolism, glycerophospholipid metabolism, and tyrosine metabolism to exert antitussive effect. It could also regulate 8 metabolic pathways of linoleic acid metabolism, glyoxylic acid and dicarboxylic acid metabolism, glycerol phospholipid metabolism, citric acid cycle and arachidonic acid metabolism to exert an expectorant effect. However, only linoleic acid metabolism and glycerophospholipid metabolism could be regulated by the PD, total platycosides fraction and DPD, which may be ascribed to the structural difference of the platycosides and the interaction between platycosides and the intestinal microbiota. Functional analysis showed that these metabolic pathways are closely related to the regulatory mechanisms of anti-inflammatory response, immune function regulation, neurotransmitter release, cell signal transduction, energy metabolism and cell apoptosis. This study shows that PD possesses good antitussive and expectorant activities. In addition, the mechanism difference of PD, total platycosides fraction and DPD imply that the apiose in PD and the interaction between PD and intestinal microbiota could exert an important effect on the antitussive and expectorant mechanism of the platycosides.
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OBJECTIVE To understand the information labeling of children’s medication in the instructions of antitussive and expectorant drugs commonly used in children’s medical institutions， analyze the existing problems， and propose relevant suggestions. METHODS The instructions for 100 antitussive and expectorant drugs commonly used in 20 tertiary children’s hospitals （centers） and 14 maternal and child health hospitals （centers） with regional representativeness in China were collected， and the information labeling of children’s medication in the instructions was investigated and analyzed. RESULTS There were only 7 kinds of antitussive and expectorant drugs for children， and the others were non-specific drugs for children. Among antitussive and expectorant drugs， tablets accounted for 18.00%， injections for 18.00%， and capsules for 4.00%. Among 100 antitussive and expectorant drugs， 72 （72.00%） labeled the usage and dosage for children， 63 （63.00%） labeled the medication items for children， 59 （59.00%） indicated the information of children in the precautions， and pharmacokinetic parameters for children were absent. Compared with imported antitussive and expectorant drugs or the drugs manufactured by joint ventures， there were many missing labeling of medication information for children with Chinese drugs. Among 63 kinds of drug instructions labeled with medication items for children， various instructions information had little guiding significance. CONCLUSIONS There is a lack of labeling in the instructions of antitussive and expectorant drugs for children， and the proportion of special drugs for children remains low. Pediatric drug information in the instructions has little guiding significance for pediatric medication. Relevant departments should further promote the completeness of pediatric medication information in the instructions of antitussive and expectorant drugs to ensure the rational use of children’s medication.
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OBJECTIVE To study active components and antitussive effect of aboveground part of Pinellia ternata （non- medicinal stems and leaves）， and compare them with the underground part of P. ternata （medicinal underground tubers）， providing scientific basis for the comprehensive utilization and product development of P. ternata. METHODS TLC， GC， HPLC and UPLC- MS/MS were used for qualitative and quantitative analysis of amino acids， volatile oil， total flavonoids and succinic acid from the aboveground and underground parts of P. ternata. The antitussive effects of the aboveground and underground parts of P. ternata were compared and studied through cough inducing experiment with concentrated ammonia water. RESULTS Results of TLC showed that at the corresponding positions on the chromatograms of the reference substances of P. ternata， and arginine， alanine， valine， leucine and rutin control， the aboveground and underground parts of P. ternata showed spots of the same color. Results of GC showed that the similarity among characteristic chromatograms of volatile oil from aboveground and underground parts of P. ternata was 0.767； results of HPLC and UPLC-MS/MS showed that compared with underground parts of P. ternata， the contents of succinic acid， quercetin， kaempferol and isorhamnetin increased by 0.15%， 0.15%， 0.09% and 0.03%， and aspartate content decreased by 2.5 mg/g. Pharmacodynamics results showed that compared with model control group， the cough incubation period of rats was prolonged significantly in administration groups （P＜0.05）， and the cough frequency within 3 min was significantly decreased （P＜0.05）； there was no statistical significance in the cough frequency within 3 min among administration groups （P＞0.05）. CONCLUSIONS The composition of amino acids， volatile oils and total flavonoids in aboveground part of P. ternata are similar to underground part of P. ternata， while the content of aspartic acid is lower than that in underground part. The aboveground part of P. ternata can prolong the cough incubation period of rats and reduce the number of coughs， which has a certain antitussive effect， but the effect is slightly weaker than that of the underground part.
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UHPLC-Q-TOF/MS metabonomics technology was used to clarify the metabolic regulation pathways by which Platycodon total saponins (PTS) exert antitussive and expectorant effects in a mouse cough model, in which coughing is induced by concentrated ammonia, and in a phenol red excretion model. After approval by the Experimental Animal Ethics Committee of Jiangxi University of Chinese Medicine (Approval No. JZLLSC-20190235), the mice were randomly divided into a normal group, a model group, a positive drug group and a PTS group. Endogenous metabolites in mouse serum were identified by UHPLC-Q-TOF/MS. Principal component analysis (PCA) and orthogonal partial least squares discriminant analysis (OPLS-DA) were used for multivariate analysis. Metabolic pathways were analyzed by the Metaboanalyst platform. The results show that PTS can significantly prolong the cough latent period and cough frequency of mice, and significantly increase phenol red excretion. UHPLC-Q-TOF/MS identified 19 metabolites related to cough, and PTS significantly decreased 16 of them; 17 metabolites related to expectoration were identified, and PTS decreased the levels of all. Metabolic pathway analysis showed that linoleic acid metabolism, arachidonic acid metabolism and glycerophospholipid metabolism were the main pathways involved in serum metabolite changes in this mouse cough model. Linoleic acid metabolism, phenylalanine, tyrosine and tryptophan biosynthesis, arachidonic acid metabolism, phenylalanine metabolism and α-linolenic acid metabolism were the main pathways involved in serum metabolite changes in the phenol red excretion model. This study is the first to elucidate the regulation of antitussive and expectorant metabolic pathways and the effect of PTS on these pathways.
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Daturae Flos is a traditional antitussive and antiasthmatic medicine， its flowers and leaves are rich in a variety of compounds， including withanolides， alkaloids， terpenes， flavonoids and amides. Because of its antiasthmatic， antitussive， antispasmodic and analgesia effect， it is traditionally used for the treatment of asthma， cough， cold pain in abdominal cavity， rheumatic arthralgia， infantile chronic eclampsia， and can also be used as raw material for surgical anesthesia. Modern pharmacological studies have shown that in addition to the traditional efficacy， Daturae Flos also has anti-inflammatory， immunosuppression， anti-convulsion and other effects， and is often used in the treatment of psoriasis， Parkinson's disease， epilepsy， rheumatoid arthritis and other diseases. At present， the chemical constituents of Daturae Flos are mainly focused on withanolides and alkaloids. At the same time， there is a lack of clear classification of chemical components and the distribution of chemical components in medicinal parts of this medicine， and little information is available for the pharmacological effects of polysaccharides. Based on this， this paper systematically searched relevant literature of Daturae Flos， and summarized and analyzed its chemical composition， pharmacological effect and clinical application， in order to provide reference for further development and utilization of Daturae Flos.
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Asari Radix et Rhizoma （ARR） is a traditional Chinese medicine for relieving exterior syndrome， and its roots and stems contain rich chemical components， including volatile oils （terpenoids， aromatics and aliphatics）， lignans， flavonoids， etc. Clinically， it has been traditionally used for the treatment of diseases such as phlegm and cough， anemofrigid cold， rheumatic arthralgia due to its ability to spread cold. Modern pharmacological studies have shown that ARR played beneficial roles in analgesic， anti-inflammatory， antitussive， antiasthmatic， antiviral， antibacterial， sedative， antioxidative， and antidepressant responses， antihypertension， as well as tumor suppression. The current studies on the chemical composition of ARR mainly focused on volatile components， and little information is available for the occurrence and pharmacological effects of non-volatile components. In addition， there is a lack of clear classification of chemical components and the distribution of chemical components in medicinal parts and the origin of species. Therefore， in this study， the authors reviewed a large number of literature on the chemical compositions and pharmacological effects of ARR， and hoping to provide a reference for further pharmacological research and the new drug development of ARR.
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OBJECTIVE：To study chemical constitue nts of Asplenium sampsoni ，and to investigate its antitussive effects preliminarily. METHODS ： The 75％ ethanol extract was isolated from A. sampsoni and purified by silica gel column chromatography. The structures of the compounds were identified by physicochemical properties and spectral data （mass spectrum ， hydrogen spectrum and carbon spectrum ）. Kunming mice were randomly divided into negative control group ，test group （the doses of 7 monomers were 0.12 g/kg），and positive control group （same dose of benproperine phosphate ），with 10 mice in each group. The antitussive effect of each compound was evaluated by the method of inducing cough with concentrated ammonia water. RESULTS：Totally 13 compounds were isolated and identified from ethyl acetate and petroleum ether parts of 75％ ethanol extract of A. sampsoni ，i.e. 4-hydroxy-acetophenone（Ⅰ），4-hydroxy-ethyl phenylacetate （Ⅱ），luteolin（Ⅲ），apigenin（Ⅳ），quercetin （Ⅴ），formononetin（Ⅵ），acacetin（Ⅶ），protocatechuic acid （Ⅷ），isorosmarinoside（Ⅸ），quercetin-3-O-β-D-glucopyranoside （Ⅹ），isorhamnetin-3-O-β-D-glucopyranoside（Ⅺ），methyl palmitate （Ⅻ）and imperatorin （XⅢ）. Luteolin could significantly prolong the cough latency and reduce the times of cough in mice （P＜0.05）. CONCLUSIONS ：Thirteen compounds are isolated from this plant for the first time ；luteolin has certain antitussive effect ，and may be the antitussive active component of the plant.
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OBJECTIVE：To explore the medication rul e of Glycyrrhiza uralensis -containing antitussive prescriptions （GUAP）， and to provide reference for the research and development of new antitussive drugs. METHODS ：The GUAP were collected from 2015 edition of Chinese Pharmacopoeia （part Ⅰ）. The information of prescription name ，composition，flavor and meridian tropism，and functional indications were input into Excel 2018 software to establish the database. The frequency of traditional Chinese medicine （TCM）was analyzed statistically. Cluster analysis was performed for high frequency TCM （frequency≥15）in GUAP by using SPSS Statistics 23.0 software；Apriori algorithm and association rules of SPSS Modeler 18.0 software were used to analyze the drug combination of high-frequency TCM in GUAP （support degree ≥15％，confidence degree ≥70％，lift degree ≥1）. New GUAP was sorted. Totally 60 mice were divided into model group （normal saline ），positive group （Codeine phosphate tablet ， 5 mg/kg），New prescription low-dose ，medium-dose and high-dose groups （1.17，5.83，11.67 g/kg，by extractum ），with 12 mice in each group. They were given relevant medicine intragastricaaly once a day ，for consecutive 7 d. 1 h after last medication ，cough was induced by ammonia in mice for 30 seconds；the latent period of cough and the frequency of cough within 2 min were recorded，and the cough inhibition rate was calculated. RESULTS ：Totally 73 prescriptions involved 194 kinds of TCM ，with 11 ingredients of high-frequency TCM （G. uralensis ，Platycodon grandiflorus ，Semen Armeniacae ，Citrus reticulate ，Ephedra sinica ， Gypsum fibrosum ，Scutellaria baicalensis ，Mentha haplocalyx ，Pinellia ternate ，Poria cocos ，Peucedanum praeruptorum ），which were mainly pungent and mostly belonged to lung meridian. High-frequency TCM could be grouped into 5 categories. There were 7 two-item association rules （such as E. sinica →Semen Armeniacae ，G. fibrosum →Semen Armeniacae ）and 10 three-item association rules （such as G. fibrosum -Semen Armeniacae →E. sinica ，C. reticulate -P. grandiflorus →Semen Armeniacae ）. New GUAP contained G. uralensis ，P. grandiflorus ，Semen Armeniacae ，E. sinica ，C. reticulate ，G. fibrosum （mass ratio 1 ∶ 2 ∶ 2 ∶ 2 ∶ 3 ∶ 4）. Compared with model group ，the latent period of cough was prolonged and the frequency of cough within 2 min was decreased significantly in positive group and new prescription low-dose ，medium-dose and high-dose groups （P＜0.01）. Compared with positive group ，latent period of cough was shortened significantly in new prescription low-dose and medium-dose groups ，while the frequency of cough within 2 min was increased （P＜0.05 or P＜0.01）；but there was no significant difference in latent period of cough， the frequency of cough within 2 min， cough inhibitory rate of new prescription high-dose group （P＞0.05）. CONCLUSIONS：The new antitussive prescription was summarized by analyzing the medication rule of GUAP ，and was verified to have good antitussive effect ，which can provide reference for the development of new antitussive drugs.
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Objective::To investigate excretion of GK-A, a antitussive compound separated from Ginkgo Semen, in the urine and bile of rats. Method::UPLC-MS/MS was used to determine the concentration of GK-A in rat urine and bile samples. The separation was performed on a C18 column, the mobile phase consisted of 0.1%formic acid aqueous solution (A) and acetonitrile (B) for gradient elution (0-1 min, 95%A; 1-3 min, 95%-85%A; 3-7.5 min, 85%-40%A; 7.5-8 min, 40%A). The detection was carried out by a triple quadrupole mass spectrometer in the positive ion mode with an electrospray ionization (ESI). Multiple reaction monitoring (MRM) mode was employed. After intragastric administration of GK-A, the urine and bile samples were collected at different time points, and the contents of GK-A in the samples were determined, and the cumulative excretion and cumulative excretion rate were calculated. Result::After 72 h of administration, the cumulative excretion of GK-A in urine was (12.35±2.69) μg, and the cumulative excretion rate was (0.58±0.13)%. Meanwhile, after 24 h of administration, the cumulative excretion of GK-A in bile was (55.16±29.22) μg, and the cumulative excretion rate was (1.57±0.83)%. Only a small amount of GK-A was excreted from urine and bile of rats with a slow speed. Conclusion::After intragastric administration, the excretion of GK-A in rat urine and bile is not the main elimination pathway.
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Objective: Using network pharmacology analysis method to explore the efficacy network and mechanism of Pediatric Xiaoji Zhike Oral Liquid (PXZOL) in treating children with food accumulation cough. Methods: We collected main components in PXZOL and their targets by using Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP) and Traditional Chinese Medicine Information Database (TCM-ID) combined with literature. Functional constipation related targets were searched from Comparative Toxicogenomics Database (CTD), PubMed, Drugbank, and other databases combined with literature. The herb-component-target network and ingredient-target-disease interaction Protein-protein interaction (PPI) network of PXZOL were constructed by Cytoscape 3.6.0 software. A core target network was constructed by screening targets in the PPI network. Gene Ontology (GO) analysis and Pathway analysis of the core target network were performed by using the ClueGO plugin. Organ localization of core targets was detected using the BioGPS database. Results: GO analysis showed that PXZOL exerted antitussive effect mainly by regulating nuclear transcription factor-κB (NF-κB) signaling. The role of depletion is mainly achieved by the synthesis and regulation of related proteins. Pathway results showed that PXZOL exerts antitussive effects mainly through mitogen-activated protein kinase (MAPK) signaling pathway, retinoic acid-inducible gene-I (RIG-I)-like receptor signaling pathway, interleukin 17 (IL-17) signaling pathway, and TNF receptor associated factor 6 (TRAF6)-mediated NF-κB activation. The role of elimination is mainly achieved through a variety of immune and inflammatory signaling pathways. In terms of organ localization, nearly 50% of target sites for antitussive targets, targets for elimination, and common targets have more expression in the lungs and large intestine. Conclusion: PXZOL is based on the theory of traditional Chinese medicine "lung and large intestine phase" and the prescription of latent medicine, modern pharmacology research showed that the effect of "resolving accumulation and relieving cough" mostly concentrated on immunity and inflammation, and network pharmacology research found that the target and its common target have nearly 50% more expression in the lungs and large intestine. From the infective disease and the network of action, we suggest that the efficacy of PXZOL is manifested by mucosal immunity and inflammation-mediated pathways. The scientific nature of the theory with the large intestine also lays the foundation for further in-depth research and verification of the model and clinical practice of pediatric food accumulation cough.
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Objective: To investigate and analyze anticomplement and antitussive activities and the active ingredients of the extract of Chimonanthus nitens leaf. Methods: The classical anti-complement pathway and the concentrated ammonia-induced cough model was used to compare the activity of the different polar parts of C. nitens leaf, and the polar parts with anti-complement and antitussive activity were determined. A preliminary analysis of the chemical composition in activity extract was identified by high performance liquid chromatography-mass spectrometry. The main chemical components in the C. nitens leaf of antitussive and antibody activity were also evaluated. Results: The ethyl acetate extract of C. nitens leaf had both anti-complement and antitussive effects. A total of 28 compounds were initially identified through mass spectrometry analysis. Kaempferol-3-O-rutinoside and kaempferol had both antitussive and anti-complement activities. Conclusion: The ethyl acetate extract of C. nitens leaf has good anti-complement and antitussive activities, and the mainly active ingredients in it were kaempferol-3-O-rutinoside and kaempferol that could be used as quality-controlling chemical markers.
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OBJECTIVE： To establish the quality standard of Compound Platycodon grandiflorum antitussive tablets. METHODS： TLC was used to identify the P. grandiflorum， Polygala tenuifolia and Glycyrrhiza uralensis qualitatively in Compound P. grandiflorum antitussive tablets. HPLC-ELSD method was used to measure the content of platycodin D in Compound P. grandiflorum antitussive tablets. The determination was performed on Agilent C18 column with mobile phase consisted of acetonitrile-water （26 ∶ 74， V/V） at the flow rate of 1.0 mL/min. ELSD was used with drift tube temperature of 105 ℃， gas flow rate of 3.0 L/min and column temperature at 35 ℃. RESULTS： TLC chromatograms of P. grandiflorum， P. tenuifolia and G. uralensis had clear spots with good separation and no same spot from negative samples. The linear range of platycodin D was 0.421 9- 5.062 8 μg （r＝0.999 9）. The quantitative limit and detection limit were 0.364， 0.109 μg， respectively. RSDs of precision， stability， reproducibility and durability tests were all lower than 3.0％. The recovery rates were 87.32％-91.96％ （RSD＝1.73％，n＝6）. The platycodin D contents of 178 samples ranged from 0.004 to 0.73 mg/tablet. The content of platycodin D in 55 batches （30.9％） of samples was lower than the content limit （0.10 mg/tablet） proposed in this study. CONCLUSIONS： Established method is accurate and reliable， and can be used for the quality control of Compound P. grandiflorum antitussive tablets.
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Objective: To study the antitussive effect of Sauropus spatulifolius, screen the active part of its antitussive effect, and study its antitussive mechanism. Methods The acute toxicity of different extraction sites of S. spatulifolius were studied by modified Karber’s method; The model was made with ammonia liquor to induce cough. The spray time that caused half of the mice to cough was calculated by sequential method with aim to screen the active sites. Capsaicin was used to induce cough, and the mechanism of action of extracts from various parts of S. spatulifolius on opioid receptor and ATP-sensitive potassium channel (KATP) of mice was explored. Results The LD50 of 75% ethanol, ethyl acetate, n-butanol, and 95% ethanol extracts was 7.30, 17.00, 69.68, and 75.88 g/kg, respectively; The maximum tolerance dose (MTD) of petroleum ether extracts was 117.71 g/kg; Extracts from 75% ethanol and ethyl acetate had antitussive effects, and its antitussive effect was related to opioid receptor and KATP pathway. Conclusion The fractions from 75% ethanol and ethyl acetate are the active parts of S. spatulifolius for relieving cough, and its antitussive mechanism is related to the KATP pathway and opioid receptors in the excited central system.
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Objective: To clarify the antitussive, expectorant, antipyretic and anti-inflammatory effects of Tanreqing inhalation solution, and provide basis and data support for further research and development of this preparation. Method: The methods of cough induced by ammonia and tracheal phenol red excretion were used to observe the antitussive and expectorant effects of Tanreqing inhalation solution in mice. The fever model of rats was established by intraperitoneal injection of bacterial lipopolysaccharide(LPS) to observe the antipyretic effect of the Tanreqing inhalation solution, the acute pneumonia model of rats was established by atomizing LPS inhalation, and the anti-inflammatory effect of Tanreqing inhalation solution was observed. Result: Tanreqing inhalation solution could reduce the number of coughs in mice induced by ammonia water, increase the amount of phenol red excretion in mouse trachea, decrease the levels of body temperature and its related regulatory factors of prostaglandin E2(PGE2) and cyclic adenosine monophosphate(cAMP) of rats induced by LPS, decrease the white blood cell(WBC) count and the neutrophil ratio(NEUT) in bronchoalveolar lavage fluid(BALF) of rats with LPS-induced acute pneumonia, and reduce the levels of nuclear transcription factor-κB(NF-κB) and interleukin-1β(IL-1β) in lung tissue. Conclusion: Tanreqing inhalation solution has obvious antitussive, expectorant, antipyretic and anti-inflammatory effects, which is worthy of further development and promotion.
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Objective: To study the correlation between the fingerprint of different polar parts of Huanbei Zhike recipe and its antitussive effect,identify the chromatographic peaks greatly contributing to its pharmacological effect,and ascribe the chromatographic peaks. Method: Gradient elution method was used to establish the chromatographic peaks of different polar parts of Huanbei Zhike recipe. The common peaks and corresponding peak areas of each part were obtained by referring to the water extract chromatogram and after being processed by chromatographic workstation. The cough frequency,the latent period of cough and the contents of interleukin (IL)-4,interferon-γ(IFN-γ),immunoglobulin (Ig)E and IL-5 in lung lavage fluid of mice were used as the detection indexes to investigate the antitussive effect of different polar parts of Huanbei Zhike recipe. The correlation analysis among cough frequency,cough latent period and common peak area was carried out,and the peaks greatly contributing to the effect of medicine were pointed out,which were assigned according to the fingerprint of single drug. Result:Bivariate correlation analysis showed that seven chromatographic peaks, i.e. No.12,13,29,32,33,35 and 39,contributed significantly to the antitussive effect. The higher the content of the compounds represented by these peaks,the stronger the antitussive effect. There was a significant correlation between No. 32 peak and the latent period of cough,while No. 13 and No. 32 peaks were significantly correlated with cough frequency. These chromatographic peaks were assigned and found to be present in Scutellaria baicalensis,Crepis Herba, Aurantii Fructus,Glycyrrhiza uralensis,etc. Conclusion:The chromatographic peaks of No.13 and No.32 peaks contribute greatly to the antitussive effect of Huanbei Zhike recipe,while Crepis turczaniowii,S. baicalensis and Aurantii Fructus are of significant significance for the whole recipe.
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Mori Cortex is the dry root bark of Moras alba L. and usually used in clinical practice. It is sweet and cold in nature, and enters the lung meridian. With effects in purging lung and relieving asthma, and inducing diuresis to reduce edema, it is mainly used to treat lung heat, asthma, cough, swelling, urine deficiency and facial skin edema. In clinic, it is mainly used for the treatment of respiratory system, urinary infection and diabetes mellitus. In recent years, great progress has been made in studies on the pharmacological effects of Mori Cortex. The literatures on the pharmacological effects of Mori Cortex in recent years were reviewed and summarized in this paper. Mori Cortex has antitussive, anti-inflammatory, hypoglycemic, cardiovascular, antiviral, anticancer, immunoregulatory, antioxidation and anti-allergy and other pharmacological effects, in addition to antitussive, expectorant, antiasthmatic and other traditional effects. Total flavones have a strong pharmacological activity. These extended studies provide valuable reference for the further development of Mori Cortex. This paper summarizes the pharmacological effects of Mori Cortex, proposes the key directions of further studies, and provides the beneficial reference for better development and utilization of Mori Cortex.
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ABSTRACT Folium Eriobotryae, the dried leaves of loquat (Eriobotrya japonica, (Thunb.) Lindl., Rosaceae), is a traditional Chinese medicine used to treat cough with phlegm in China. Fallen and growing loquat leaves were tested for their effect on coughing and expectoration in mice. HPLC-ELSD and HPLC-MS analyses of aqueous and ethanol extracts of fallen or growing leaves were used to identify the chemical components responsible for this effect. Both the aqueous and ethanol extracts of growing and fallen leaves of loquat contained antitussive and expectorant activities. Moreover, an aqueous extract of growing loquat leaves with a higher flavonoid content displayed a stronger expectorant activity while the ethanol extract of fallen loquat leaves that contained a higher content of triterpenoid acids induced a stronger antitussive activity.
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Objective To predict the action targets of antitussive and expectorant active ingredients of Farfarae Flos (FF) to understand the “multi-components, multi-targets, and multi-pathways” mechanism. Methods Using network pharmacology, the main components in FF [chlorogenic acid, 3,5-O-dicaffeoylquinic acid, 3,4-O-dicaffeoylquinic acid, 4,5-O-dicaffeoylquinic acid, rutin, caffeic acid, quercetin, kampferol, hyperoside, β-sitosterol, tussilagone, and 7β-(3-Ethyl-ciscrotonoyloxy)-1α-(2-methylbutyryloxy)-3(14)- dehydro-Z-notonipetranone] reported in previous studies, were used to predict the targets of main active ingredients of FF according to the PharmMapper method. The prediction was made by screening of the antitussive and expectorant targets approved by the CooLGeN database and annotating the information of targets with the aid of MAS 3.0 biological molecular function software. Based on the molecular docking, the tight binding of active ingredients with potential protein targets was explored by Systems Dock Web Site. The Cytoscape software was used to construct the FF ingredients-targets-pathways network. Results The network analysis indicated that the active ingredients in FF involve 18 targets, such as IL-2, COX-2, and RNASE3, as well as the signal transduction-inflammation-energy metabolism relevant biological processes and metabolic pathways. Conclusion The antitussive and expectorant effect of FF showed the characteristics of traditional Chinese medicine in multi-components, multi-targets, and multi-pathways. This research provides a scientific basis for elucidation of the antitussive and expectorant pharmacological mechanism of FF.
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Objective: To investigate the molecular mechanism and potential active components of Jiegeng Decotion (JD) with the antitussive and expectorant effects. Methods: Target proteins related with phlegm and cough were selected through mining literature and retrieving in DrugBank and TTD database, and the main active components and potential target proteins from JD were computed and analyzed by DOVIS 2.0 and Cytoscape 3.0 to build a molecular-protein regulatory network. Results: A total of 38 target proteins and 472 small molecules were initially screened based on the pathological mechanism which is related with phlegm and cough. Molecular docking results showed that 78 molecules (five from Platycodi Radix and 73 from Glycyrrhizae Radix et Rhizoma, and their structural characteristics analysis were in accordance with the “rules of generic drugs”) were found in JD with higher docking score (Score ≥ 7) of target protein. According to the results of molecular docking, 128 molecular-target protein data pairs with high docking scores (Score ≥ 7) were selected, and then 26 major active components of JD (saponins and flavonoids, etc.) and 13 target proteins were identified by using Network analyzer. Conclusion: The active components of JD could regulate over-inflammatory response on the respiratory tract, improve the lung function, inhibit the over-expression of mucin, and reduce the reaction of the stimulation on cough center through acting on the main target proteins (TLR4, MMP9, IKK2, etc), thereby achieving the antitussive and expectorant effects.
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Objective To study the chemical constituents and effects of crude and processed Pinelliae Rhizoma. Methods The contents of inosine, guanosine, adenosine, succinic acid, ephedrine hydrochloride, liquiritin, glyeyrrhizie acid, and 6-gingerol of Pinelliae Rhizoma, Pinelliae Rhizoma Praeparatum cum Alumine, Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine, and Pinelliae Rhizoma Praeparatum were detected by HPLC. The pharmacodynamics of the traditional efficacy of expectorant and cough relieving was studied by stimulating mice with phenol red and concentrated ammonia in the trachea of mice. Results The contents of inosine, guanosine, adenosine, succinic acid, and ephedrine hydrochloride decreased significantly after processing, and inosine was not detected in Pinelliae Rhizoma Praeparatum cum Alumine. Compared with the three processed products, the content of inosine, guanosine, adenosine and succinic acid was the highest in the Pinelliae Rhizoma Praeparatum cum Alumine, the lowest was in Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine, and in consistent with the effect of resolving phlegm. The four components were the active components of resolving phlegm effect. Adding alumen during Pinelliae Rhizoma Praeparatum cum Alumine processing has also enhanced its effectiveness. Pinelliae Rhizoma Praeparatum has the strongest antitussive effect, followed by Pinelliae Rhizoma, Pinelliae Rhizoma Praeparatum cum Alumine and Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine. Adding licorice and lime water during Pinelliae Rhizoma Praeparatum processing, licorice (peak 6: liquiritin, peak 7: ammonium glycyrrhizinate) had a powerful antitussive effect and enhanced its antitussive effect. After processing by ginger and white peony, ginger (peak 8: 6-gingerol) is good at warming middle energizer to arrest vomiting, thus enhance antiemetic effect and weaken phlegm, cough effect of Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine. Conclusion The chemical composition and efficacy of Pinelliae Rhizoma have changed after being processed, and different processing methods have different effects on its chemical composition and efficacy.