Recognition of antitussive components in Farfarae Flos based on grey relational analysis and partial least squares regression. / åŸºäºŽç°è‰²å ³è”åº¦åˆ†æžå’Œåæœ€å°äºŒä¹˜å›žå½’è¾¨è¯†æ¬¾å†¬èŠ±æ­¢å’³æ´»æ€§æˆåˆ†.

OBJECTIVES: Farfarae Flos has the effect of cough suppression and phlegm elimination, with cough suppression as the main function. Studies have revealed that certain components of Farfarae Flos may be related to its cough suppressant effect, and some components have been confirmed to have cough suppressant activity. However, the antitussive material basis of Farfarae Flos has not been systematically elucidated. This study aims to elucidate the group of active ingredients in Farfarae Flos with cough suppressant activity by correlating the high performance liquid chromatography (HPLC) fingerprint of Farfarae Flos extract with its cough suppressant activity. METHODS: HPLC was used to establish the fingerprint profiles of 10 batches of Farfarae Flos extract and obtain their chemical composition data. Guinea pigs were selected as experimental animals and the citric acid-induced cough model was used to evaluate the antitussive efficacy data of 10 batches of Farfarae Flos extract. SPF-grade healthy male Hartley guinea pigs were randomly divided into the S1 to S10 groups, a positive control group, and a blank control group (12 groups in total), with 10 guinea pigs in each group. The S1 to S10 groups were respectively administered Farfarae Flos extract S1 to S10 (4 g/kg), the positive control group was administered pentoverine citrate (10 mg/kg), and the blank control group was administered purified water. Each group received continuous oral administration for 5 days. The guinea pigs were placed in 5 L closed wide-mouth bottles, and 17.5% citric acid was sprayed into the bottle with an ultrasonic atomizer at the maximum spray intensity for 0.5 minutes. The cough latency period and cough frequency in 5 minutes were recorded for each guinea pig. Grey relational analysis (GRA) and partial least squares regression (PLSR) were used to conduct spectral-effect correlation analysis of the chemical composition data of Farfarae Flos extract and the antitussive efficacy data, and predict the group of active ingredients in Farfarae Flos with antitussive activity. The bioequivalence verification was conducted to verify the predicted group of active ingredients in Farfarae Flos with antitussive activity: SPF-grade healthy male Hartley guinea pigs were randomly divided into a S9 group, an active ingredient group, a positive control group, and a blank control group (4 groups in total), with 10 guinea pigs in each group. The S9 group was administered Farfarae Flos extract S9 (4 g/kg), the active ingredient group was administered the predicted combination of antitussive active ingredients (dose equivalent to 4 g/kg of Farfarae Flos extract S9), the positive control group was administered pentoverine citrate (10 mg/kg), and the blank control group was administered purified water. Each group received continuous oral administration for 5 days, and animal modeling and observation of efficacy indicators were the same as above. RESULTS: The HPLC fingerprint of 10 batches of Farfarae Flos extract was established, and the peak area data of 14 main common peaks were obtained. The antitussive effect data of 10 batches of Farfarae Flos extract were obtained. Compared with the blank control group, the cough latence in the positive control group and S1, S2, S3, S4, S6, S7, S8, S9, S10 groups was prolonged (all P<0.01), while the cough frequency in 5 minutes in the positive control group and S1, S2, S4, S6, S8, S9, S10 groups was decreased (all P<0.05). The analysis of spectrum-effect relationship revealed that isochlorogenic acid C, isochlorogenic acid A, chlorogenic acid, isochlorogenic acid B, isoquercitrin, and rutin had high contribution to the antitussive effect of Farfarae Flos, and the 6 components were predicted to be the antitussive component group of Farfarae Flos. The verification of bioequivalence showed that there were no statistically significant differences in the antitussive effect between the S9 group and the antitussive component composition group(all P>0.05), which confirmed that isochlorogenic acid C, isochlorogenic acid A, chlorogenic acid, isochlorogenic acid B, isoquercetin, and rutin were the antitussive component group of Farfarae Flos. CONCLUSIONS: The analysis of spectrum-effect relationship combined with the verification of bioequivalence could be used to study the antitussive material basis of Farfarae Flos. The antitussive effect of Farfarae Flos is the result of the joint action of many components.

Novel α7 nicotinic acetylcholine receptor modulators as potential antitussive agents.

A novel series of α7 nicotinic acetylcholine receptor (nAChR) modulators was designed and evaluated for antitussive activity in an in vivo guinea pig model of chemically induced cough. Compound 16 at all tested doses (9.5, 3 and 1 mg/kg) significantly (p < 0.01) reduced the cumulative number of coughs and showed similar results to a positive control (codeine at 30 mg/kg). Among three different administration routes (intraperitoneal, oral and inhalation), compound 16 exerted a significant antitussive effect in guinea pigs at an inhaled dose as low as 0.4 mg/kg (p < 0.05). α7 nAChR modulators may provide a novel, non-narcotic approach to therapy in patients with acute and chronic cough.

Analysis of active components in aboveground and underground parts of Pinellia ternata and comparison of antitussive effect / 中国药房

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.

Analysis of inter-individual variability of antitussive effect of Farfarae Flos and its fecal metabolites based on gut microbiota.

In this study, the inter-individual variability of antitussive effect of Farfarae Flos was observed, and then the Farfarae Flos treated mice were divided into the mice with good or poor antitussive effect. Then a UHPLC-Q TOF-MS method was developed and validated to quantify 13 fecal metabolites of Farfarae Flos, and the results showed concentrated differences between the two subgroups. The results of 16 S rRNA gene sequencing analysis showed that mice with good or poor antitussive effects were also different at the structure of gut microbiota in phylum and genus, as well as the related 6 pathways. In addition, the differential fecal metabolites of Farfarae Flos between the two subgroups were probably related with 5 bacterial that participating in the CQAs and flavonoids metabolism. This study explained the inter-individual variability of the antitussive effect of Farfarae Flos from the perspective of gut microbiota. However, the specific bacterial that participate in the metabolism of Farfarae Flos as well as the antitussive effects of Farfarae Flos need to be further validated.

Optimization of Naringenin Nanoparticles to Improve the Antitussive Effects on Post-Infectious Cough.

Naringenin (NRG) is a natural compound with several biological activities; however, its bioavailability is limited owing to poor aqueous solubility. In this study, NRG nanoparticles (NPs) were prepared using the wet media milling method. To obtain NRG NPs with a small particle size and high drug-loading content, the preparation conditions, including stirring time, temperature, stirring speed, and milling media amount, were optimized. The NRG (30 mg) and D-α-tocopherol polyethylene glycol succinate (10 mg) were wet-milled in deionized water (2 mL) with 10 g of zirconia beads via stirring at 50 °C for 2 h at a stirring speed of 300 rpm. As a result, the NRG NPs, with sheet-like morphology and a diameter of approximately 182.2 nm, were successfully prepared. The NRG NPs were stable in the gastrointestinal system and were released effectively after entering the blood circulation. In vivo experiments indicated that the NRG NPs have good antitussive effects. The cough inhibition rate after the administration of the NRG NPs was 66.7%, cough frequency was three times lower, and the potential period was 1.8 times longer than that in the blank model group. In addition, the enzyme biomarkers and histological analysis results revealed that the NRG NPs can effectively regulate the inflammatory and oxidative stress response. In conclusion, the NRG NPs exhibited good oral bioavailability and promoted antitussive and anti-inflammatory effects.

Physicochemical properties and in vitro digestion behavior of a new bioactive Tremella fuciformis gum.

A new easy-dissolved Tremella fuciformis gum (TFG) from fruiting body was investigated in detail from three aspects: physicochemical characteristics, rheological behavior and in vitro digestion behavior. The results showed that TFG consisted of 73.9% polysaccharides, exhibiting easy solubility in water and good colloidal characteristics and stability. The physical and chemical treatments could decrease the apparent viscosity of TFG solution. The antioxidation activity of TFG remained constant at each static in vitro digestion phase, revealing that this gum could be used as a potential food thickener and antioxidant. The digestion behavior of TFG was also determined using a dynamic in vitro digestive system, DIVRS-II. The results demonstrated that the digestion behavior of TFG should be attributed to the morphology of digestive tracts, continuous secreting and continuous emptying. The antitussive effect of TFG was related to the increase in serum IL-10 content.

Preparation of Naringenin Nanosuspension and Its Antitussive and Expectorant Effects.

Naringenin (NRG) is a natural flavonoid compound abundantly present in citrus fruits and has the potential to treat respiratory disorders. However, the clinical therapeutic effect of NRG is limited by its low bioavailability due to poor solubility. To enhance the solubility, naringenin nanosuspensions (NRG-NSps) were prepared by applying tocopherol polyethylene glycol succinate (TPGS) as the nanocarrier via the media-milling method. The particle size, morphology, and drug-loading content of NRG-NSps were examined, and the stability was evaluated by detecting particle size changes in different physiological media. NRG-NSps exhibited a flaky appearance with a mean diameter of 216.9 nm, and the drug-loading content was 66.7%. NRG-NSps exhibited good storage stability and media stability. NRG-NSps presented a sustainable release profile, and the cumulative drug-release rate approached approximately 95% within 7 d. NRG-NSps improved the antitussive effect significantly compared with the original NRG, the cough frequency was decreased from 22 to 15 times, and the cough incubation period was prolonged from 85.3 to 121.6 s. Besides, NRG-NSps also enhanced expectorant effects significantly, and phenol red secretion was increased from 1.02 to 1.45 µg/mL. These results indicate that NRG-NSps could enhance the bioavailability of NRG significantly and possess a potential clinical application.

Components study on antitussive effect and holistic mechanism of Platycodonis Radix based on spectrum-effect relationship and metabonomics analysis.

The antitussive effect of Platycodonis Radix is closely related to the components in saponins fraction of Platycodonis Radix extract (SFPRE); however, these active components and their holistic mechanism remain unknown. Hence, a new method by integrating spectrum-effect relationship analysis with metabolomics analysis was applied to study the active components and their holistic mechanism simultaneously. For spectrum-effect relationship analysis, chemical fingerprints of ten batches of SFPRE were developed using UHPLC-LTQ-Orbitrap MSn; antitussive effect were evaluated using a classic mice-cough model induced by ammonia liquor. Spectrum-effect relationship was analyzed by partial least squares regression (PLSR) analysis. For metabolomics analysis, the altered metabolites related to cough in serum were identified by UHPLC-Q-TOF/MS and orthogonal partial least squares-discriminant analysis (OPLS-DA); metabolic pathway analysis was depended on MetaboAnalyst 4.0, KEGG database, METLIN database and HMDB database. Our findings showed that 10 identified components of Polygalacin D (peak 26), Deapio-platycodin D (peak 21), Platycodin D (peak 23), ß-Gentiotriosyl platycodigenin (peak 37), Platycoside G3 (peak 17), Platycoside C (peak 25), Platycodin D3 (peak 16), 3-O-ß-D-glucopyranosyl platycodigenin (peak 33), Platycoside F (peak 19) and 3″-O-acetyl platycodin D3 (peak 15), and 2 unidentified components (peak 45 and 44) possessed antitussive effects. The metabolomics analysis result showed that 19 metabolites were potential biomarkers related to the cough, 16 of which could be restored to normal levels by SFPRE. These biomarkers were involved in arachidonic acid metabolism, linoleic acid metabolism and glycerophospholipid metabolism. The current study may facilitate the development of antitussive medicines with fewer side-effects based on Platycodonis Radix.

Analysis of Antitussive Active Ingredients of Asplenium sampsoni / 中国药房

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.

δ Opioid Receptor Inverse Agonists and their In Vivo Pharmacological Effects.

The discovery of δ opioid receptor inverse agonist activity induced by ICI-174,864, which was previously reported as an δ opioid receptor antagonist, opened the door for the investigation of inverse agonism/constitutive activity of the receptors. Various peptidic or non-peptidic δ opioid receptor inverse agonists have since been developed. Compared with the reports dealing with in vitro inverse agonist activities of novel compounds or known compounds as antagonists, there have been almost no publications describing the in vivo pharmacological effects induced by a δ opioid receptor inverse agonist. After the observation of anorectic effects with the δ opioid receptor antagonism was discussed in the early 2000s, the short-term memory improving effects and antitussive effects have been very recently reported as possible pharmacological effects induced by a δ opioid receptor inverse agonist. In this review, we will survey the developed δ opioid receptor inverse agonists and summarize the possible in vivo pharmacological effects by δ opioid receptor inverse agonists. Moreover, we will discuss important issues involved in the investigation of the in vivo pharmacological effects produced by a δ opioid receptor inverse agonist.

Analysis of Excretion Behavior of GK-A from Ginkgo Semen in Urine and Bile of Rats / 中国实验方剂学杂志

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.

Development of Novel δ Opioid Receptor Inverse Agonists without a Basic Nitrogen Atom and Their Antitussive Effects in Mice.

Our previous results showed that naltrindole (NTI) derivatives with certain types of electron-withdrawing groups as an N-substituent showed δ opioid receptor (DOR) inverse agonistic activities. We therefore synthesized N-acylated NTI derivatives 3a-e and observed that N-benzoyl and N-cyclopropanecarbonyl derivatives SYK-736 (3b) and SYK-623 (3c) were DOR full inverse agonists and the N-acryloyl derivative 3d was a DOR partial inverse agonist. SKY-623 was over 110-fold more potent than the reference compound ICI-174,864. Both naltriben (NTB) and 7-benzylidenenaltrexone (BNTX) derivatives with N-benzoyl and N-cyclopropanecarbonyl groups were also DOR full inverse agonists. These N-acylated inverse agonists are interesting compounds because they have no basic nitrogen atom, which has been demonstrated to be an important pharmacophore. NTI and BNTX-type DOR inverse agonists SYK-623 and SYK-723 (12c) showed dose-dependent antitussive effects in a mouse cough model induced by citric acid exposure. The antitussive effects by SYK-623 and SYK-723 were significantly attenuated by pretreatment with DOR agonist SNC80.

Antitussive effect and mechanism study of effective fractions from Sauropus rostratus / 中草药

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.

Spectrum-effect Relationship in Antitussive Effect of Different Polar Parts of Huabei Zhike Recipe / 中国实验方剂学杂志

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.

Comparative Study on Antitussive, Antiasthmatic, Phlegm-resolving and Anti-inflammatory Effects of Fritillaria cirrhosa and Fritillaria unibracteate / 中国药房

OBJECTIVE:To investigate antitussive,antiasthmatic,phlegm-resolving and anti-inflammatory effects of Fritillaria cirrhosa and Fritillaria unibracteata. METHODS:Mice and guinea pig were randomly divided into blank control group (distilled water),ethanol extract groups,water extraction groups and powder groups of F. cirrhosa and F. unibracteata(1.13 g/kg for mice, 0.42 g/kg for guinea pig,calculated by crude drug),positive control group,with 10 mice(guinea pig)in each group. Each group was given relevant medicine intragastrically once a day for consecutive 5 d. Relative indicators were detected 30 min after last medication. The ammonia water induced cough method was used to investigate antitussive effect (dextromethorphan hydrobromide as positive drug,0.013 g/kg)by determining coughing latent period and coughing times within 3 min. After inducing asthma with 2％ histamine phosphate for 15 s, antiasthmatic effect (aminophylline as positive drug, 0.033 g/kg) was investigated by determining coughing latent period and the number of guinea pig with convulsive fall. The phenol red injection method was used to investigate phlegm-resolving effect (ambroxol as positive drug,21.304 g/kg) by determining the content of phenol red in the trachea of mice in phenol red expectoration test. The anti-inflammatory effect(dexamethasone acetate as positive drug,9.225×10-4 g/kg)was investigated by determining ear swelling degree and inhibition rate of ear swelling mice in xylene-induced inflammation test. RESULTS:Compared with blank control group, coughing latent period and cough induction latent period prolonged significantly in ethanol extract of F. cirrhosa and F. unibracteata groups,F. cirrhosa and F. unibracteata powder groups,positive control group, and coughing time decreased significantly within 3 min. The number of mice with convulsive fall decreased significantly in F. cirrhosa powder group, F. unibracteata ethanol group,F. unibracteata powder group and positive control group. The content of phenol red in the trachea of mice increased significantly,while ear swelling and inhibitory rate of ear swelling decreased significantly,with statistical significance (P<0.05 or P<0.01). There was no statistical significance in each index of mice between powder group and positive control group (P>0.05). Compared with corresponding groups of F. cirrhosa,coughing latent period of mice prolonged significantly in F. unibracteata ethanol extract group (P<0.05), other indexes had no statistical significance(P>0.05). CONCLUSIONS:The antitussive,antiasthmatic,phlegm-resolving and anti-inflammatory effects of F. cirrhosa are similar to or worse than those of F. unibracteata.

Spectrum-effect relationship of antitussive effect by total organic acids in crude and four processed Pinellia ternate based on gray relative analysis method / 中草药

Objective: To investigate the HPLC fingerprint of the total organic acids in Pinelliae Rhizoma (the rhizomes of Pinelliae ternate), Pinelliae Rhizoma Praeparatum cum Alumine, Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine, Pinelliae Rhizoma Praeparatum and Pinelliae Rhizoma Praeparatum cum Glycyrrhizae et Alumine, and the its relationship with antitussive effect, and to establish the spectrum-effect relationship of the total organic acids in crude and processed P. ternate and antitussive effect, so as to elucidate their material basis of antitussive effect. Methods: The gray relative analysis method was used to make correspond analysis of the HPLC fingerprints of total organic acids in Pinelliae Rhizoma and processed products related with three antitussive indexes (the latent period, coughing times in 3 min, and inhibitatory rate), establishing the spectrum-effect relationship between them. Results: The total organic acids of crude Pinelliae Rhizoma and its processed products showed the antitussive activity against the ammonium hydroxide-induced mice cough, consist with arresting cough of Pinelliae Rhizoma. The HPLC data demonstrated that the chemical composition represented by peak 4, 6 (succinic acid), and 12 had strong relevancy with anti-tussive activity and made a great contribution to this activity, especially peak 4, which had bigger area and stronger relevancy. Conclusion: This paper reveals that there exists the correlations between the HPLC fingerprints of total organic acids and antitussive effect of crude and processed Pinelliae Rhizoma, elucidating the material basis of antitussive effects in crude and processed P. ternate by the spectrum-effect study, and could provide a theory basis for the quality control and analysis of Pinelliae Rhizoma.

Effect of various factors such as habitat, growth period, and commercial specification on antitussive effect of Siraitia grosvenorii / 中草药

Objective: To observe the effects of various factors on the antitussive effect of Siraitia grosvenorii. Methods: According to the sequential method (i.e., up and down method) for the principle of median effective dose, the antitussive effect of S. grosvenorii was observed and the median effective time (EDT50) of cough induced by NH3 aq. in mice was calculated. Results: S. grosvenorii from Hunan-Hengyang, Nanning-Tanluo, Yongfu-Longjiang, and Baishou have the antitussive effect, especially in Yongfu-Longjiang and Baishou (R>150%). The fruits obtained from cuttage seedlings and tissue culture seedlings have the antitussive effect, while the immature fruits have not (R130%) have the significant antitussive effect, and so first class fruit and ringing fruit do (R>130%). However secondary class fruit does not have the antitussive effect (R<130%). Conclusion: The factors, except the habitat, breeding technology, and whether drying or not, such as growth period and commercial specification may influence the antitussive effect of S. grosvenori.

Study on Species Characteristics of Chinese Patent Medicines for Antitussive Effect / 世界科学技术-中医药现代化

This study was aimed to reveal the species characteristics of Chinese patent medicines for antitussive ef-fect and provide references for developing new drugs. This research targeted Chinese patent medicines for antitussive effect which were included in the Pharmacopoeia of the People's Republic of China and the New National Chinese Patent Medicines as well as those characterized by keywords such as cough cure, cough alleviating, antitussive effect, cough, persistent cough. The analysis was made on the species characteristics, such as the number of Chinese patent medicines for antitussive effect, license number, ethnomedicine patent medicines, drugs for children use, protection of varieties of traditional Chinese medicine, the number of drugs, the generic names of drug, and drug forms. The results showed that 684 Chinese patent medicines for antitussive effect collected in this research had ac-counted for 8.60% of the total 7 260 of Chinese patent medicines. A total of 7 450 license numbers were approved, and 33% of the Chinese patent medicines shares one license number. One Chinese patent medicine owns 16.6 li-cense numbers on average. Ethnomedicine patent medicines had 3 Tibetan prescriptions such as the Shiwuwei Chenxiang pill and 4 Mongolian prescriptions, such as the Siwei Tumuxiang powder. Drugs for children accounted for 14%, including 9 forms. The type of the generic names of drug reached 16 and most of them originate from abbrevia-tions of the main drug in prescription. The number of drugs in prescription ranges from 8 to 16. Chinese patent medicines for antitussive effect involved 16 forms, of which the proportion of the use of solid preparation was higher than the liquid preparation. It was concluded that Chinese patent medicines for antitussive effect were characterized by such advantages such as a variety of species, various forms, the reasonable number of drugs, considerable medicine retail market share and drug for children use which can meet the clinical needs, and meanwhile some prob-lems, such as a lack of criteria for the generic names of drug, the homogenization of fierce competition, and inade-quacy of ethnomedicine patent medicines.

Study on Prescription Characteristics of Chinese Patent Medicines for Antitussive Effect / 世界科学技术-中医药现代化

This study was aimed to reveal characteristics of functions, main indications and applications of Chinese patent medicines in order to provide references for development of new Chinese patent medicines for antitussive ef-fect. Chinese patent medicines recorded in the Pharmacopoeia of the People's Republic of China and the New Na-tional Chinese Patent Medicines were taken as research subjects. Chinese patent medicines classified in the function and indication with key words of cough-relieving, cough-suppressing, cough and chronic cough were col-lected. Analysis was made on the prescription characteristics, such as functions, main indications and applications. The results showed that there were 684 Chinese patent medicines and 462 terms, which were used for a total of 1533 times. The frequently-used terms are antitussive effect with expectorant, antitussive effect, expectorant, heat-clearing and exterior-releasing, antiasthmatic, wind-expelling and antipyretic, antitussive effect with antiasthmatic, purging lung heat, relieving exterior syndrome and moistening the lungs. All 684 Chinese patent medicines were used 48 ma-jor treatments for a total of 1107 times. The main indications include acute and chronic trachitis / bronchitis, exoge-nous wind-heat type of common cold, exogenous wind-cold type of common cold, cough with abundance of phlegm due to phlegm-heat obstructing the lung, acute upper respiratory tract infection, asthma, acute and chronic pharyngi-tis, lung heat cough, and etc. All 684 Chinese patent medicines used a total of 537 kinds of herbs and chemical medicines, including 441 kinds of herbal medicine, 36 kinds of animal medicine, 25 kinds of mineral medicine and 35 kinds of chemical medicine. The top ten herbs in terms of using frequency are Glycyrrhizae radix et rhizoma, Platycodonis radix, Armeniacae semen amarum, Menthae haplocalycis herba, Citri reticulatae pericarpium, Ephedrae herba, Scutellariae radix, Perilla frutescens (L.) Britt, Pinelliae rhizoma, Fritillariae cirrhosae bulbus. Among them, 1/4 of Chinese patent medicines used extract. Five kinds of food or fruits were also used, which were orange, fresh gin-ger, pear, watermelon and dried mushroom. It was concluded that Chinese patent medicines for antitussive effect can be adopted in the treatment of various kinds of diseases, especially for the treatment of cough(heat cough in partic-ular), abundance of phlegm, asthma, pharyngitis, laryngitis, and etc. The treatment methods of clearing heat, dis-pelling wind and relieving exterior syndrome played an important role in the realization of antitussive effect. However, the expression of functions and main indications is far from standardized and clear. Drugs commonly used are herbal medicine plus animal medicine, mineral medicine and chemical medicine as well as food and fruit. The discovery of preparations with certain clinical curative effect from ethnomedicine and the using of their extracts as a major ingre-dient are one important way to develop new Chinese patent medicines with antitussive effect.

Antitussive and Antiasthmatic Effect of Compound Liquor from Tremella Aurantialba / 医学研究杂志

Objective To study the antitussive and antiasthmatic effect of compound liquor from Tremella aurantialba. Methods The mice cough model induced by ammonia, guinea pig cough model induced by acitric acid,guinea pig asthma model induced by histamine and acetylcholine, guinea pig asthma model induced by ovalbumin were used in this experiment. Results The compound liquor from Tremella aurantialba could significantly prolong the tussive delitescence,decreas the tussive times of mice and guinea pigs;could significantly prolong the asthmatic delitescence. Conclusions The antitussive and antiasthmatic effects of compound liquor from Tremella aurantialba was obvious.