Expectorant Effects Research Articles

Discovering the Major Antitussive, Expectorant, and Anti-Inflammatory Bioactive Constituents in Tussilago Farfara L. Based on the Spectrum-Effect Relationship Combined with Chemometrics.

Farfarae Flos (FF) is the dried flower bud of Tussilago farfara L, which has antitussive, expectorant, and anti-inflammatory effects. However, little research on the main active composition of FF has been reported. The purpose of this study is to find the main active compounds responsible for the three pharmacological effects (i.e., antitussive, expectorant, and anti-inflammatory effects) of Farfarae Flos, based on the spectrum–effect relationship combined with chemometrics. First, this study uses the UPLC-QDA method to establish the chromatography fingerprint of Farfarae Flos, which is combined with chemometrics to analyze 18 batches of samples. Then, we study the antitussive, expectorant, and anti-inflammatory effects of Farfarae Flos. Finally, the spectrum–effect relationship between the fingerprint and the three pharmacological effects are studied by grey correlation analysis and partial least squares regression. The results show that four, four, and three main active constituents were found for the antitussive, expectorant, and anti-inflammatory pharmacological effects, respectively. In conclusion, we found the main active compounds corresponding to the main pharmacodynamic effects of Farfarae Flos. To our knowledge, this is the first time that spectrum–effect relationships in FF have been established using both raw and processed samples, which provides an experimental basis for further studies on the pharmacodynamic material basis of Farfarae Flos, as well as providing reference for the comprehensive evaluation of Farfarae Flos quality and the development of substitute resources.

Characterization, in Vitro and in Vivo Evaluation of Naringenin-Hydroxypropyl-ß-Cyclodextrin Inclusion for Pulmonary Delivery.

Naringenin, a flavonoid compound which exists abundantly in Citrus fruits, is proven to possess excellent antitussive and expectorant effects. However, the clinical applications of naringenin are restricted by its poor solubility and low local concentration by oral administration. The aim of the present study is to prepare a naringenin-hydroxypropyl-β-cyclodextrin (naringenin-HPβCD) inclusion as an inhalation solution for pulmonary delivery. The naringenin-HPβCD inclusion was characterized by phase solubility study, XRD, differential scanning calorimetry (DSC), proton nuclear magnetic resonance (1HNMR), and two-dimensional rotating frame Overhauser effect spectroscopy (2D ROESY). The in vitro permeability of the inclusion was evaluated on Calu-3 cells and the pharmacokinetic profile of pulmonary delivery was investigated in Sprague-Dawley (SD) rats. Based on the linear model of phase solubility study, the relationship between naringenin and HPβCD was identified as AL type with a 1:1 stoichiometry. XRD, DSC, and NMR studies indicated that the entire naringenin molecule is encapsulated into the cavity of HPβCD. HPβCD could increase the concentration of naringenin in the epithelium-lining fluid (ELF) of Calu-3 cells and act as a sustained release system for naringenin. The pharmacokinetic profile of naringenin-HPβCD inclusion showed rapid response and higher local concentration by pulmonary delivery. In conclusion, pulmonary delivery of naringenin-HPβCD inclusion is a promising formulation strategy, which could provide a new possibility for the clinical application of naringenin.

Development and Validation of Salbutamol, Bromhexine, Ambroxol and Guauaifenesin Determination in Human Plasma by HPLC-MS/MS Method

Introduction. Multicomponent oral drugs containing salbutamol, bromhexine, ambroxol and guaifenesin have a mucolytic, expectorant and bronchodilator effect. The development method for determination substances in biological fluids is a main procedure for performing the analytical part of pharmacokinetic studies and bioequivalence studies of multicomponent drugs. There is no published data of the determination of bromhexine, ambroxol and guaifenesin, but there a lot of published methods for divided determination analytes in a biological fluid. This study presents the development and validation of a method of the determination of salbutamol, bromhexine, ambroxol and guaifenesin in human blood plasma by high performance liquid chromatography with tandem mass spectrometric detection. A sample preparation was perfomed by solid-phase extraction. Deuterated derivatives were used as internal standards.Aim. The aim of the study is to develop a method for the quantitative determination of salbutamol, bromhexine, ambroxol and guaifenesin in human plasma by HPLC with tandem mass spectrometric detection for performing the analytical part of pharmacokinetic studies.Materials and methods. Determination of salbutamol, bromhexine, ambroxol and guaifenesin in human plasma by HPLC with tandem mass spectrometric detection. A sample was prepared using solid-phase extraction.Results and discussion. The method was validated by next validation parameters: selectivity, matrix effect, calibration curve, accuracy, precision, limit of quantification, carry-over and stability.Conclusion. The method of the determination of salbutamol, bromhexine, ambroxol and guaifenesin in human plasma was developed and validated by HPLC-MS/MS. The analytical range of the was 0.1–20 ng/mL in plasma for salbutamol, 0.25–25 ng/mL in plasma for bromhexine, 0.075–3 ng/mL in plasma for ambroxol, and 10–2000 ng/mL in plasma for guaifenesin. Method could be applied to determination of salbutamol, bromhexine, ambroxol and guaifenesin in plasma for PK and BE studies.

Chinese star anise and anise, magic herbs in traditional Chinese medicine and modern pharmaceutical science

Star anise (Illicium verum Hook. f.) is an important herb in traditional Chinese medicine as well as traditional Asian medicine. The fruit is aromatic and has a strong, pungent and mildly sweet taste. Star anise is one of the many species that contain bioactive compounds as well as a number of phenolic and flavonoid compounds, having antioxidant, preservative and antimicrobial properties. All relevant papers in the English language from researchers of different countries were collected. The keywords of Chinese star anise, anise, traditional Chinese medicine and modern pharmaceutical science were searched in Google Scholar, Scopus, Research Gate and PubMed. Its seeds are good source of minerals like calcium, iron, copper, potassium, manganese, zinc, and magnesium. The essential oil of Chinese star anise contains anethole which has shown several functional properties including antimicrobial, antioxidant, hypoglycemic, hypolipidemic and oestrogenic properties. Due to all positive characteristics, such as antidiabetic, hypolipidemic, antioxidant activities, anticancer and antimicrobial properties, both seeds and essential oils of anise is promising for safe use as super food supplements and raw constituents in the both pharmaceutical and food industries. Anise seed oil contains anethol, estragole, eugenol, pseudisoeugenol, methyl chavicol and anisaldehyde, coumarins, scopoleting, umbelliferon, estrols, terpene hydrocarbons, and polyacetylenes as the major compounds. The plant oil has both pharmacological and clinical effects. The pharmacological effects consist of antimicrobial, hepatopreotective, anticonvulsant, anti-inflammatory, antispasmodic, bronchodilator, estrogenic, expectorant and insecticidal effects, and clinical effects such as nausea, constipation, menopausal period, virus, diabetes, obesity and sedative action. Combined with a nutritious diet, other traditional Chinese and Asian medicine, Chinese star anise and ansie seed may improve various aspects of health. More clinical studies are necessary to uncover the numerous substances and their effects in ginseng that contribute to public health.
 Asian J. Med. Biol. Res. June 2019, 5(3): 162-179

The modern view of mucolytic therapy

In the article represents modern scientific data about complex therapeutic effect of the new unique release form of ambroxol – Respix® Spray. It has high mucolytic and mucokinetic activity with pronounced expectorant, anti-inflammatory and antioxidant effects. The scientific rationale for clinical usage prospects of this drug is given: it can stimulate ability for synthesis of surfactant and stimulate local immunity of respiratory tract mucous membranes, as well as significantly reduce the intensity of pain in the throat.

Antitussive, expectorant, and anti-inflammatory effects of Adenophorae Radix powder in ICR mice

Ethnopharmacological relevanceAdenophora triphylla var. japonica is frequently used as an oriental medicinal plant in Korea, China, and Japan for its anti-inflammatory, antitussive, and hepatoprotective effects. Aim of the studyIn the present study, the antitussive, expectorant, and anti-inflammatory effects of AR powder were investigated using animal models to evaluate their potential to treat respiratory disorders. Materials and methodsAR powder was administered orally to mice once daily for 11 days, at dose levels of 400, 200, and 100 mg/kg. Theobromine (TB), ambroxol (AM) and dexamethasone (DEXA) were used as standard drugs for antitussive effects, expectorant effects and anti-inflammatory effects, respectively. Evaluations of antitussive effects were based on changes in body weight, the number of cough responses and the histopathology of the lung and trachea. Expectorant effects were based on changes in the body weight, macroscopic observations of body surface redness, the mucous secretion of the trachea and histopathology of lung (secondary bronchus). Anti-inflammatory effects were based on changes in the body weight, macroscopic observations involving redness and edema of the treated ear, absolute and relative ear weights and histopathology of the treated ears. ResultsAllergic acute inflammation and coughing induced by exposure to NH4OH and symptoms of xylene-induced contact dermatitis were significantly inhibited by treatment with AR powder in a dose-dependent manner. Histological analyses revealed that AR powder decreased the OD values in trachea lavage fluid, reduced body surface redness, thicknesses of intrapulmonary secondary bronchus mucosa, and the number of PAS-positive mucous producing cells. Overall, AR powder administered at 200 mg/kg displayed superior antitussive and expectorant effects as compared to TB (50 mg/kg), and AM (250 mg/kg). At the highest concentration (400 mg/kg) AR powder displayed only moderately improved anti-inflammatory activities as compared to DEXA (1 mg/kg). ConclusionThe results obtained in this study suggest that AR powder exerts dose-dependent, favorable antitussive, expectorant, and anti-inflammatory activities achieved through modulation of the activity of mast cells and respiratory mucous production. Therefore, AR powder may serve as a therapeutic agent in various respiratory disorders, especially those that occur as a result of environmental toxicants.

A comparative assessment of acute oral toxicity and traditional pharmacological activities between extracts of Fritillaria cirrhosae Bulbus and Fritillaria pallidiflora Bulbus

Ethnopharmacological relevanceFritillariae Bulbus (“Beimu” in Chinese) is a famous traditional Chinese medicine used to treat cough, expectoration and asthma for more than 2000 years, which belongs to the Fritillaria genus in Liliaceae family. Bulbs of Fritillaria cirrhosa D.Don (BFC) and bulbs of Fritillaria pallidiflora Schrenk (BFP) are two important drugs of Beimu. Due to the significant similarities in their outward appearance characters and chemical profiles, BFC has often been adulterated with BFP in Chinese Traditional Medicine markets. Aim of the studyThis study aims to compare the oral acute toxicity and the traditional pharmacological activities including antitussive, expectorant and anti-inflammatory effects between the extract of BFC and BFP, to clear and definite if the BFP can be used as a substitute of the BFC in the application of traditional medicine. Materials and methodsThe extracts were prepared through refluxing with 80% ethanol solvent. For the acute toxicity tests, graded doses of BFP extracts and the maximum dose of BFC extracts were administered orally to mice. The animals were observed for toxic symptoms and mortality daily for 14 days. For the pharmacological activities tests, graded doses of BFP and BFC extracts were administered orally to mice. To observe the effects relieving cough, expelling phlegm and lessening the ear swelling of BFC extracts and BFP extracts through ammonia liquor inducing cough, phenol red apophlegmating in mice and the xylene-induced auricular swelling of mouse, respectively. ResultsIn the acute toxicity study, the LD50 value of BFP in mice was calculated to be 213.57 g/kg body weight, and the maximum feasible dose (MFD) value of BFC in mice was 452.14 g/kg. Histopathological analysis has shown inflammatory cells infiltration and cells edema in liver, multinucleated giant cell proliferation in spleen, perivascular exudate and hemorrhage in lung, glomerulus atrophy in kidney of mice after oral administrations of BFP extracts. But only liver cells edema was observed in BFC group. Both BFC extract and BFP extract significantly increased latent period of cough and inhibited cough frequency in mice induced by ammonia. Besides, the two extracts also obviously enhanced mice's tracheal phenol red output in expectorant assessment and inhibited the development of ear edema in anti-inflammatory evaluation assay. ConclusionTo summarize, the BFP has the significant similarities in morphological characteristics, chemical profiles and traditional pharmacological activities compared with the BFC. The result of this study provide some valid scientific support for using BFP as a plant substitute of the BFC, but considering the toxicity of BFP is much higher than BFC, we don't recommend long-term oral administration of BFP or exceeding recommended dosage of Chinese Pharmacopoeia 2015.

Individually orientated choice of mucolytic drug for coughing in a child with acute respiratory viral infections

Coughing in acute respiratory infections, regardless of the level of infection: upper or lower respiratory tract is a frequent clinical symptom in childhood. The analysis of the modern literature and the data of the authors’ own researches testify to the fact that the prescription of mucoactive therapy in a complex of therapeutic measures (etiotropic, basic therapy, bronchopulmonary drainage, etc.).) should be differentiated and determined not only by the nature and severity of coughs, separated sputum, but also by individual characteristics of the patient, the severity and course of bronchopulmonary pathology, the age of the child, the presence of adverse environmental factors (in particular, passive smoking), the level of compliance with the patient. The use of combined medications simultaneously influencing various pathogenetic mechanisms of inflammation and coughing becomes a promising direction of mucoactive therapy. One of them is Eucabal® syrup containing liquid extracts of thyme and plantain. Due to the synergy of its components, Eucabal® syrup has an expectorant and anti-inflammatory effect, which is important in the initial period of acute respiratory viral infections (tracheitis, bronchitis tracheobronchitis), especially in dry, painful cough with hard-to-remove sputum. In case of acute respiratory viral infections accompanied by a wet cough with a viscous, difficult to separate sputum, mucolytic agents are shown first of all. One of the modern widely used drugs of this group is acetylcysteine (ESPA-NAC®) in a convenient dosage form.

Identification and quantitative determination of steroidal compounds in the plant material of cabbage

Vegetable crops are inexhaustible source of biologically active compounds. Cabbage (Brassica oleracea L.) – is a plant that has been extensively used in folk medicine of different countries of the world for the treatment of various disorders, and has anti-inflammatory, expectorant, broncholytic, diuretic, and genera tonic effect. The plant material of cabbage in not officinal in Ukraine, thus it requires a complex pharmacognostic research to be carried out. The aim of the research. Identification and quantitative determination of steroidal compounds in the leaves, seeds and heads of cabbage. Materials and methods. Identification of steroidal compounds and determination of their quantity in the plant material of cabbage was carried out using gas chromatography/mass-spectrometry (GC/MS) method. The results of the study and their discussion . As a result of the carried out experiment 3 compounds of steroidal nature were identified in the leaves of cabbage of “Snow-white” variety, and 4 – of “Ukrainian autumn” and “Yaroslavna” varieties, 4 compounds in the seeds of cabbage of “Snow-white” variety, 3 – of “Ukrainian autumn” and “Yaroslavna” varieties, and 3 steroidal compounds in the heads of cabbage of all the varieties. β-Sitosterol was the dominating compound by the content in all studied samples. Its highest content was found in the leaves (2499 mg/kg) and seeds (1728 mg/kg) of cabbage of “Yaroslavna” variety, as well as in the heads (1148 mg/kg) of cabbage of “Ukrainian autumn” variety. Conclusion . Results of the experiment can be used at the quality control methods for the cabbage plant material development as well as obtaining prospective biologically active substances from the studied plant material

NMR based metabolomic comparison of the antitussive and expectorant effect of Farfarae Flos collected at different stages

Farfarae Flos (FF) is widely used for the treatment of cough, bronchitis, and asthmatic disorders in the Traditional Chinese Medicine (TCM). According to the experience of TCM, only the flower bud can be used as herbal drug, and its medicinal quality becomes lower after blooming. However, the underlying scientific basis for this phenomenon is not fully understood. In this study, the chemical components and the bioactivities of the FF collected at three different development stages were compared systematically. NMR based fingerprint coupled with multivariate analysis showed that the flower buds differed greatly from the fully opened flower both on the secondary and primary metabolites, and the animal experiments showed that the fully opened flower exhibited no antitussive or expectorant effect. In addition, the endogenous metabolites correlated with the antitussive and expectorant effect of FF were also identified. These findings are useful for understanding the rationality of the traditional use of FF, and also suggested the components responsible for the antitussive and expectorant effect of FF.

EFFECT OF THE LEAF Pettiveria alliacea EXTRACT ACTIVE COMPOUND ON Mycobacterium tuberculosis

Indonesia has a variety of herbal plants used as herbal/traditional medicines. Singawalang (Petiveria alliacea) is one of the herbal plants usually used in the United States as a cough medicine because of its expectorant effect. Singawalang plants are also widely used to cure tuberculosis. However, the investigations on the effects of toxicity on this plant leaf extract has not been done. This study aims to investigate the effects of active compounds in singawalang against Mycobacterium tuberculosis using a variety of solvents. The active compound of ethanol extract was obtained by maceration using ethanol solvent. The extract was then fractionated using column chromatography method, and using gradual eluent to produce fraction. The doses used were 0.5 mg/ml; 1 mg/ml; 2 mg/ml; 70% ethanol, h-hexane, benzene, chloroform, ethylacetate, silica gel 60GF254, Middlebrook 7H9, and 7H10. The reactions using Singawalang leaf extract with various solvents resulted in a reduction of the Mycobacterium tuberculosis colony growth, compared with the reaction on control treatment, treatment using DMSO 1%, and treatment using 70% ethanol. As a conclusion, the various solvents used did not make a significant difference. However, control treatment, treatment using DMSO 1%, and treatment using 70% ethanol had significant results.

Inhibition of airway remodeling and inflammation by isoforskolin in PDGF-induced rat ASMCs and OVA-induced rat asthma model

Isoforskolin (ISOF) has been reported to play an important role in many illnesses including respiratory, cardiovascular and ophthalmologic diseases. In our study, we aimed to investigate how ISOF regulates airway remodeling and inflammation in asthma. Based on SO2-stimulated mouse cough model, we assessed the role of ISOF in cough and secretion of phlegm. Afterwards, platelet derived growth factor (PDGF)-induced primary rat airway smooth muscle cell (ASMC) model and ovalbumin (OVA)-induced rat asthma model were used to continue our following research. Our results showed that ISOF could prolong the cough latent period, reduce the cough times in two minutes, and increase the excretion of red phenol, which suggested the antitussive and expectorant effects of ISOF. Besides, ISOF pretreatment reversed the hypotonicity and cytoskeleton remodeling in PDGF-induced ASMCs, and reduced mucus hypersecretion and collagen overdeposition in OVA-induced rat asthma model, which indicated its inhibition on airway remodeling in vitro and in vivo. Moreover, ISOF reduced the invasion of inflammatory cells into bronchoalveolar lavage fluid (BALF) and lungs, which revealed its inhibitory role in airway inflammation. The down-regulation of transforming growth factor β1 (TGF-β1) and interleukin-1β (IL-1β) upon ISOF treatment might be responsible for its anti-remodeling and anti-inflammation roles. In conclusion, ISOF can reduce cough and sputum, as well as inhibit airway remodeling and inflammation by regulating the expression of TGF-β1 and IL-1β. These data indicate the potency of ISOF in treating asthma and also provide insights into the development of new anti-asthma agent.

Effects of the fermentation products of endophytes from Glycyrrhiza uralensis on inflammation-associated factors and Aquaporin in rat models with phlegm blocking in lung

To filtrate the effective fermentation products of endophytes from Glycyrrhiza uralensis by comparing expectorant effects. Ninety Wistar rats with half males and half females were randomly divided into 9 groups(n=10):including normal control group, model group, positive control group, Glycyrrhiza decoction group, 5 groups of the fermentation products of endophytes(JTZB005,JTZB006,JTZB043,JTZB060,JTZB063). The model of phlegm blocking in lung was induced by inhaling SO2 for 30 minutes and cold wind for 10 minutes twice per day for ten days. Ten days later, 10 ml/kg normal saline was administrated in normal control group and model group, 0.08 mg/kg Fufang Beimu Lvhuaan tablets was administrated in positive control group, 0.95 g/kg Glycyrrhiza water decoction and the fermentation products of endophytes were respectively administrated in Glycyrrhiza decoction group and 5 groups of the fermentation products of endophytes. All groups were given the corresponding dose by intragastric administration once a day for seven days. The changes of rats' general activities were observed during the experimental time. Two hours after the last gavage, rats were sacrificed. The upper lobe of the right lung was removed for HE and immunohistochemical staining. Pathological of lung tissues and the expressions of aquaporin-1(AQP1)and aquaporin-5(AQP5) in lung tissue were measured. In addition, the lung tissue of middle lobe of right lung were accurately weighed, and 10% homogenate were made. The supernatant was removed by centrifugation at 3 000 r/min for ten minutes. The levels of nitric oxide (NO) was determined by nitric acid reductase method. The content of tumor necrosis factor(TNF-α) and intercellular adhesion molecule 1(ICAM-1) and the concentration of cyclooxygenase-2(COX-2) in lung tissue were measured by enzyme-linked immunosorbent(ELISA) method. After modeling,the levels of NO, TNF-α, ICAM-1, and the concentration of COX-2 in lung tissue were increased significantly, the expressions of AQP1 and AQP5 were decreased significantly (P<0.01). Compared with the model group, the levels of NO,TNF-α,ICAM-1 and the concentration of COX-2 in lung tissue were decreased significantly, and the expressions of AQP1 and AQP5 were increased significantly in Glycyrrhiza decoction group, JTZB005,JTZB006 and JTZB063 group(P<0.05, P<0.01). By filtrating, JTZB005、JTZB006、JTZB063 have expectorant effects.

Study on the expectoration effect of improved nursing intervention of infants' pneumonia

Objective To explore the expectoration effect of improved nursing intervention of infants' pneumonia. Methods A total of 237 cases of children with pneumonia were divided into intervention group (119 cases )and control group (118 cases )according to random number table method.The patients of the two groups were given routine therapy care in accordance with the doctor's advice.On the basis of this, the intervention group implemented the improved all-in-one nursing intervention mode, including oxygen-driven intermittent inhalation, new-style chest percussion, postural improved drainage and audio-visual training therapy.The control group were given the traditional routine nursing method. Results After the elimination of sputum, the breathing, heart rate and blood oxygen of the two groups were compared and the differences were statistically significant(P<0.01). The effective duration of sputum, dyspnea remission time, sputum rale disappearance time, pulmonary rales disappeared time, the normal temperature time and hospitalization time of the two groups were compared and the differences were statistically significant(P<0.01). The total effectiveness rate of the intervention group was significantly higher than that of the control group, and the difference between the two groups was statistically significant(P<0.05). The incidence of complications of the intervention group was significantly lower than that of the control group, and the differences were statistically significant(P<0.05). Conclusions Improved nursing intervention model can effectively remove respiratory obstruction, improve the function of gas exchange and reduce the complications, so as to improve the effect of treatment of infant pneumonia. Key words: Infant pneumonia; Nursing intervention; Sputum elimination; Effect evaluation

Anti-Aging Implications of Astragalus Membranaceus (Huangqi): A Well-Known Chinese Tonic.

Owing to a dramatic increase in average life expectancy and the Family Planning program of the 1970s - 1990s, China is rapidly becoming an aging society. Therefore, the investigation of healthspan-extending drugs becomes more urgent. Astragalus membranaceus (Huangqi) is a major medicinal herb that has been commonly used in many herbal formulations in the practice of traditional Chinese medicine (TCM) to treat a wide variety of diseases and body disorders, or marketed as life-prolonging extracts for human use in China, for more than 2000 years. The major components of Astragalus membranaceus are polysaccharides, flavonoids, and saponins. Pharmacological research indicates that the extract component of Astragalus membranaceus can increase telomerase activity, and has antioxidant, anti-inflammatory, immunoregulatory, anticancer, hypolipidemic, antihyperglycemic, hepatoprotective, expectorant, and diuretic effects. A proprietary extract of the dried root of Astragalus membranaceus, called TA-65, was associated with a significant age-reversal effect in the immune system. Our review focuses on the function and the underlying mechanisms of Astragalus membranaceus in lifespan extension, anti-vascular aging, anti-brain aging, and anti-cancer effects, based on experimental and clinical studies.

ДОСЛІДЖЕННЯ АНАТОМІЧНОЇ БУДОВИ НАДЗЕМНИХ ОРГАНІВ PRIMULA JULIAE KUSN

Вперше здійснено дослідження особливостей анатомічної будови надземних органів первоцвіту (примули) Юлії родини первоцвіті, в результаті якого виявлено їх характерні мікроскопічні діагностичні ознаки. Встановлені мікродіагностичні ознаки дають можливість ідентифікувати лікарську рослинну сировину і можуть бути використані для розробки проекту АНД.

Standardization of the manufacturing procedure for Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine

Ethnopharmacological relevancePinelliae Rhizoma (PR), the dried tuber of Pinellia ternata (Thunb.) Breit., is a traditional Chinese medicinal herb. It is commonly used for treating cancer, cough and phlegm. To treat cancer, Chinese medicine practitioners often use raw PR; while to treat cough and phlegm, they usually use Pinelliae Rhizoma Praeparatum cum Zingibere et Alumine (PRZA, raw PR processed with ginger juice and alumen as adjuvant materials). Currently, the producing protocol of PRZA varies greatly among different places in China. This study aims to standardize the manufacturing procedure for PRZA. We also evaluated the impact of processing on the bioactivities and chemical profile of raw PR. Materials and methodsWe used the orthogonal design to optimize the manufacturing procedure of PRZA at bench scale, and validated the optimized procedure in pilot-scale production. The MTT assay was used to compare the cytotoxicities of raw PR and PRZA in hepatocellular carcinoma HepG2 cells. Animal models (ammonia liquor-induced cough model and phenol red secretion model) were used to compare the antitussive and expectorant effects of raw PR and PRZA, respectively. The chemical profiles of raw PR and PRZA samples were compared using a newly developed ultra-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry (UPLC/Q-TOF-MS) method. ResultsThe standardized manufacturing procedure for PRZA is as follows: soak raw PR in water until the center of the cut surface is devoid of a dry core, after that, boil the herb in water (for each 100kg raw PR, 12.5kg alumen and 25L freshly squeezed ginger juice are added) for 6h, and then take out and dry them. The cytotoxicity of PRZA was less potent than that of raw PR. Intragastric administration of raw PR or PRZA demonstrated antitussive and expectorant effects in mice. These effects of PRZA were more potent than that of raw PR at the dose of 3g/kg. By comparing the chemical profiles, we found that six peaks were lower, while nine other peaks were higher in PRZA than in raw PR. Six compounds corresponding to six individual changed peaks were tentatively identified by matching with empirical molecular formulae and mass fragments. ConclusionThe manufacturing procedure for PRZA was standardized. This protocol can be used for PRZA industrial production. The bioactivity assay results of raw PR and PRZA (produced using the standardized protocol) support the common practice for the clinical applications of these two decoction pieces. Moreover, raw PR and PRZA showed different chemical profiles. Further studies are warranted to establish the relationship between the alteration of chemical profiles and the changes of medicinal properties caused by processing.

Spiralosides A-C, Three New C27-Steroidal Glycoalkaloids from the Fruits of Solanum spirale.

Three new C27-steroidal glycoalkaloids, spiralosides A–C (1–3), were obtained from the total alkaloids of Solanum spirale by chromatographic methods. On the basis of spectroscopic evidence, spiralosides A–C were elucidated as (22R,25S)-22,26-epiminocholest-5-ene-3β,16α-diol-N-acetyl-3-O-α-l-rhamnopyranosyl-(1→4)-β-d-glucopyranosyl (1), (22R,25S)-22,26-epiminocholest-5-ene-3β,16α-diol-N-acetyl-3-O-β-d-glucopyranosyl (2), (22R,25S)-22,26-epiminocholest-3β,16α-diol-N-acetyl-3-O-β-d-glucopyranosyl (3), respectively. The total alkaloids of S. spirale have been screened for their antitussive and expectorant effects in intact animal model.Graphical Electronic supplementary materialThe online version of this article (doi:10.1007/s13659-016-0103-9) contains supplementary material, which is available to authorized users.

Nutraceutical Properties and Safety Evaluation of Fruits and Arrope of Geoffroea decorticans (Chañar)

Context: Geoffroea decorticans (chanar) fruits and its derivate product (arrope) have been traditionally used as food and in folk medicine for the treatment of a wide variety of diseases including bronchopulmonary disorder. Objective: The objective of this study is to evaluate the antitussive, expectorant and anti-inflammatory effects and safety of aqueous extract (AE) and arrope (Ar) of chanar. Materials and methods: The anti-inflammatory activity of AE and Ar was evaluated through carrageenan induced edema and cotton pellet-induced granuloma formation in rats. The antitussive activity was evaluated using model against ammonia induced cough in rats. The expectorant activity was evaluated by volume of phenol red in rat’s tracheas. The tested doses of extracts were of 250, 500 and 1000 mg/kg, (p.o.). For the safety evaluation of AE and Ar, was conducted the subchronic toxicity test in rats (1 g/kg and 2 g/kg, p.o.). Results: The results showed that AE (1000 mg/Kg) significantly reduced the edema (100%) induced by carrageenan 3 h post-dosing and granuloma formation (47.76%) induced by cotton pellets. In the ammonia liquor induced cough and the amount of phenol red secretion, AE and Ar of chanar (1000 mg/kg) significantly enhanced the latent period of cough, inhibited the cough frequency and significantly enhance tracheal phenol red compared with that negative control. The result of toxicity assays suggested that AE and Ar did not induce or cause any damage to the liver and kidney of the rats and can be considered nontoxic for these animals at tested doses. Discussion and conclusion: This study has shown that the AE and Ar possess antitussive and expectorant significant effect. Also AE possess significant anti-inflammatory effects, both extracts were nontoxic. These findings seem to justify use of the plant in traditional medicine and are proposed, the chanar fruits as an excellent nutraceutical.

Antitussive and expectorant activities of Potentilla anserina

Context The root of Potentilla anserina L. (Rosaceae) is an herbal medicine that has been used as an antitussive and expectorant drug for thousands of years in Chinese folk medicine.Objective: This study estimated the antitussive and expectorant effects of P. anserina extract to validate its traditional use.Materials and methods The antitussive and expectorant activities of the ethanol extract, aqueous extract, and polysaccharides from P. anserina were evaluated using classical animal models.Results The results showed that in three antitussive tests, the aqueous extract and polysaccharides at high and low doses significantly inhibited the frequency of cough induced by ammonia and sulfur dioxide in mice and by citric acid in guinea pigs, and increased the latent period of cough in guinea pigs. Similarly, the aqueous extract and polysaccharides also showed significant expectorant activity compared with the control in phenol red secretion experiments. Polysaccharides at dose of 600 mg/kg enhanced tracheal phenol red output by 121.1%, the ammonium chloride (positive control) at dose of 1000 mg/kg by 117.4%. However, the ethanol extract at a high dose (600 mg/kg) has antitussive activity only in the sulfur dioxide induced coughing test. Moreover, the polysaccharides at the same dose showed better bioactivity than the aqueous extract in all tests.Discussion and conclusion The results of the present study provide evidence that P. anserina can be used as an antitussive and expectorant herbal medicine and that polysaccharides may be the main active ingredients of P. anserina responsible for its bioactivities.