ABSTRACT
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.
ABSTRACT
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.
ABSTRACT
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.
ABSTRACT
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.
ABSTRACT
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.
ABSTRACT
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.
ABSTRACT
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.
ABSTRACT
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.
ABSTRACT
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.
ABSTRACT
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.
ABSTRACT
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.
ABSTRACT
Aim To Compare the quality of Pinellia Tubers between Nanchong Sichuan and relevant areas in order to standardize plant and to provide evidence for further exploitation and application. Methods Expectorant experiment was conducted with methods of washing mice's respiratory tract with phenol red and antitussive effect, with ammomia caused mice cough. Results In the experiment of expectorant effect, oral administration of the water or the ethanol extracts of pinellia Tubers showed no obvious expectorant effect, it also showed no significant difference compared with control NS. In the antitussive effect experiment, however the water or the ethanol extracts of pinellia Tuhers prolonged the incubation period and reduced the frequency of coughing. It presented significant difference compared with the control NS and clear time-effect relationship. Conclusion Pinellia Tubers from Nanchong Sichuan and relevant areas showed no apparent expectorant effect and have destinct antitussive effect. As for antitussive effects, water extracts were stronger than those of ethanol extracts, and wild Pinellia Tubers outmatched planted ones. Antitussive effect of wild Pinellia Tubers samples was rather stronger from Nanchong, Guangan, Suining, and Liangshan of Sichuan and Xihe Gansu.
ABSTRACT
Objective: To study the pharmacological action of Mahuang Compound Capsule(MCC) (Herba Ephedrae, Semen Armeniacae Amarum, Fructus Schisandrae, etc.). Methods: The study was carried out through the observation of ammonia induced cough model in mice and acrolein induced cough model in guinea pigs treated with MCC, its effects on asthma model of guinea pigs induced by histamine and acetylcholine mixture and on isolated tracheas smooth muscle of guinea pigs were also studied. Results: MCC administrated orally showed significant antitussive effect in ammonia induced cough model in mice and acrolein induced cough model in guinea pigs. MCC could effectively prevent guinea pigs from asthma induced by histamine and acetylcholine mixture. The water extracts could antagonize histamin phosphate that contract the isolated tracheas of guinea pigs. Conclusions: MCC has antitussive and anti asthma effects.