Antitussive activity of alcoxyphenyl carbamic acid analogues.

In this study we report pharmacological evaluation of four newly synthetized analogues of alcoxyphenyl carbamic acid, structurally related to butamirate citrate that is frequently used as cough suppressing drug, and marked as ATK 231, ATK 241, ATK 251 and ATK 261. These agents with various modifications of the molecular structure have been tested for antitussive activity in cough induced by inhalation of aerosol of citric acid (0.3 M) over 3 minutes using conscious guinea pigs. Results revealed significant cough suppressing activity without significant influence on specific airways resistances in all tested substances. ATK 231 and ATK241 showed significantly higher total antitussive activities when compared to both codeine phosphate and butamirate citrate, while ATK 251 only comparing to butamirate citrate. We did not observe any notable adverse effects and these compounds could thus potentially represent promising new non-narcotic antitussives suitable for further studies.

Beneficial effects of an alkaline topical treatment in patients with mild atopic dermatitis.

BACKGROUND: Atopic dermatitis (AD) is the most common cause of eczema. The skin condition affects millions of people worldwide. Severe cases of AD demand systemic treatment, but most AD cases rely on local therapy with topical corticosteroids, emollients, and moisturizing agents to alleviate eczema. Commonly, derma-cosmetics with a pH around 5.5 are used to treat eczematous lesions (EL). However, evidence is currently amassing that the use of mildly alkaline topical creams is beneficial for AD-related eczema treatment because of its effect on the inflammation in the skin. AIMS: To test an alkaline two-phase care concept for the treatment of eczema. PATIENTS/METHODS: An open-label study of 25 patients with eczema associated with mild AD. Patients were treated with Alkaline Build Up Caring Cream INTENSIVE and Alkaline Build Up Caring Cream PLUS+ (both Siriderma® ) for eight weeks. Dermatological, biochemical, and questionnaire-based examinations were conducted prior to the trial and after its completion. RESULTS: Topical administration of slightly alkaline creams led to small and statistically insignificant increases of skin pH. Clinical examination at the end of the observation period revealed a significant decrease of total eczematous-affected skin area, a significant decrease in average severity scores of EL, and significant improvements in patient-reported outcome parameters. Blood tests did not reveal any significant changes, except for small but significant increases in IL-8 and monocytes. CONCLUSION: Mildly alkaline topical creams seem to provide soothing effects on eczema-related skin inflammation and thus might contribute to treatment of local symptoms of eczema in patients with mild AD.

Antitussive arabinogalactan of Andrographis paniculata demonstrates synergistic effect with andrographolide.

Traditional Indian medicines have been used in humans for thousands of years. While the link to a particular indication has been established in man, the active principle of the formulations often remains unknown. In this study, we aim to investigate the structural features and antitussive activity of fractions from Andrographis paniculata leaves. In vivo investigations of water extract (WE), and both ethanol-soluble (WES) and precipitated (WEP) fractions from WE on the citric-acid induced cough efforts and airways smooth muscle reactivity in guinea pigs were performed. Chemical, chromatographic and spectroscopic analysis revealed the existence of a highly branched pectic arabinogalactan (109kDa) in WEP and andrographolide in WES. WEP showed significant antitussive activity while the potencies of WE and WES are even higher. Neither WE nor WES significantly alter specific airway smooth muscle reactivity. Remarkably, the antitussive activity of arabinogalactan could be increased by synergistic action with andrographolide. Finally, traditional aqueous extraction method provides an arabinogalactan from A. paniculata, which stimulate biological response but without addiction.

Herbal polysaccharides and cough reflex.

In the last decades plant substances have become a leading form of treatment of many respiratory symptoms, including cough. It has been shown that compounds purified form polysaccharides from Adhatoda vasica, Withania somnifera, and Glycyrrhiza glabra have various biological activities, such as antioxidant, anti-inflammatory, immunomodulating, antispasmodic action, or antiallergic properties, and they often act as cough suppressants. This work demonstrates new natural substitutes for synthetic antitussives whose application is associated with numerous adverse effects. We investigated pharmacodynamic characteristics of arabinogalacatan samples extracted from A. vasica, W. somnifera, and G. glabra. These extracts showed the ability to reduce citric acid-induced cough in awake guinea pigs after oral administration in a dose of 50mg/kg. The strongest antitussive effect (81%) was found after application of the extract from G. glabra. There was a 67% cough suppression with A. vasica and 61% with W. somnifera, which was comparable with the antitussive activity of codeine (62%).

Antitussive Activity of the Water-Extracted Carbohydrate Polymer from Terminalia chebula on Citric Acid-Induced Cough.

Terminalia chebula, a medicinal plant, is widely used in the management of various diseases. As the water extract of its dried ripe fruit is a frequently used preparation, we decided to look for bioactive polysaccharide in this extract. We demonstrate that the obtained polysaccharide fraction, CP, contained a highly branched arabinogalactan protein having a (1 → 3)-, (1 → 6)- and (1 → 3, 6)-linked ß -D-Galp together with (1 → 5)- and (1 → 3)-linked α -L-Araf and nonreducing end units of α -L-Araf. This polymer possesses strong antitussive property. Our results showed that the number of citric acid-induced cough efforts decreased significantly after the oral application of polysaccharide fraction in a dose of 50 mg kg(-1) body weight. Its antitussive efficacy was higher than cough suppressive effect of standard drug codeine. Therefore, traditional aqueous extraction method provides a major polysaccharide, which induces a pharmacological effect: this could represent an attractive approach in phytotherapeutic managements.

Antitussive activity of an extracellular Rhodella grisea proteoglycan on the mechanically induced cough reflex.

A mucilagineous extracellular proteoglycan (EPG) composed of xylose and its 3-O-and 4-O-methyl-derivates (55%), glucuronic acids (17%), rhamnose (14%), galactose (8%), glucose (4%) and minor amounts of other sugars (∼2%) has been isolated from culture medium of Rhodella grisea. A white fluffy algal biopolymer of molecular mass over 8.1×105 contained protein (13%), methoxyl (6%), acetyl and succinyl groups. EPG was tested in vivo on mechanically induced cough in non-anaesthetized cats as a test system. The biopolymer showed a cough suppressing effect on laryngopharyngeal type of cough while the cough from tracheobronchial mucous area was slightly or not affected. Further, the intensity of maximal cough efforts from laryngopharyngeal and tracheobronchial parts in expirium and inspirium were influenced slightly only indicating that the expectoration effect was not suppressed by biopolymer application.