Antiulcer Activity of Anthraquinone-Flavonoid Complex of Rumex tianschanicus Losinsk.

The composition of an ethanol extract from the roots of Rumex tianschanicus Losinsk of the Trans-Ili Alatau wild flora was studied in order to determine its antiulcer activity. The phytochemical composition of the anthraquinone-flavonoid complex from (AFC) R. tianschanicus revealed the presence of numerous polyphenolic compounds, the most abundant of which are anthraquinones (1.77%), flavonoids (6.95%), and tannins (13.39%). The use of column chromatography (CC) and thin-layer chromatography (TLC) in conjunction with UV, IR, NMR spectroscopy, and mass spectrometry data allowed the researchers to isolate and identify the major components of the anthraquinone-flavonoid complex's polyphenol fraction: physcion, chrysophanol, emodin, isorhamnetin, quercetin, and myricetin. The gastroprotective effect of the polyphenolic fraction of the anthraquinone-flavonoid complex (AFC) of R. tianschanicus roots was examined in an experimental model of rat gastric ulcer induced by indomethacin. The preventive and therapeutic effect of the anthraquinone-flavonoid complex at a dose of 100 mg/kg was analyzed using intragastric administration per day for 1 to 10 days, followed by a histological examination of stomach tissues. It has been demonstrated that prophylactic and prolonged use of the AFC R. tianschanicus in laboratory animals resulted in significantly less pronounced hemodynamic and desquamative changes in the epithelium of gastric tissues. The acquired results thus offer fresh insight into the anthraquinone and flavonoid metabolite component composition of R. tianschanicus roots, and they imply that the examined extract can be used to develop herbal medicines with antiulcer activity.

Antihypothyroid Effect of Salidroside.

In terms of prevalence, thyroid pathology, associated both with a violation of the gland function and changes in its structure, occupies one of the main places in clinical endocrinology. The problem of developing low-toxic and highly effective herbal preparations for the correction of thyroid hypofunction and its complications is urgent. Salidroside is a glucoside of tyrosol, found mostly in the roots of Rhodiola spp., and has various positive biological activities. The purpose of this study was to study the antihypothyroid potential of salidrosid-containing extract from R. semenovii roots, which was evaluated on a mercazolyl hypothyroidism model. We showed that extract containing salidroside is a safe and effective means of hypothyroidism correction, significantly reducing (p ≤ 0.001) the level of thyroid-stimulating hormone and increasing the level of thyroid hormones. The combined use of R. semenovii extract with potassium iodide enhances the therapeutic effect of the extract by 1.3-times.

Design, synthesis and molecular docking of benzophenone conjugated with oxadiazole sulphur bridge pyrazole pharmacophores as anti inflammatory and analgesic agents.

The prostaglandins (PG) a group of physiologically active lipid compounds having diverse hormone like effects are important mediators of the body's response to pain and inflammation, and are formed from essential fatty acids found in cell membranes. This reaction is catalyzed by cyclooxygenase, a membrane associated enzyme occurring in two isoforms, COX-1 and COX-2. Nonsteroidal anti-inflammatory drugs (NSAIDs) act by inhibiting the activity of COX. In view of this, a series of novel benzophenones conjugated with oxadiazole sulphur bridge pyrazole moiety 8a-l were designed, synthesized, characterized and subsequently evaluated for anti-inflammatory and analgesic property. The investigation of novel analogues 8a-l for potential anti-inflammatory activity showed high levels of COX-1 and COX-2 inhibitory activity. Among the series, compound 8i with electron withdrawing fluoro group at the para position of the benzoyl ring of benzophenone was characterized by highest IC50 values for both COX-1 and COX-2 inhibition, which is comparable to the standard drug. Further, molecular docking studies have been performed for the potent compound.

The Reactions of Photosynthetic Capacity and Plant Metabolites of Sedum hybridum L. in Response to Mild and Moderate Abiotic Stresses.

In this article, for the first time, an experimental study of the effect of mild and moderate osmotic stress, NaCl content and the effect of low positive temperature on photosynthetic activity and composition of metabolites of immature plants Sedum hybridum L. is reported. In this representative of the genus Sedum adapted to arid conditions and having the properties of a succulent, a change in photosynthetic activity and an increase in the level of protective metabolites in the shoots were revealed when exposed to mild and moderate stress factors. The results of this study can be used in work on the adaptation of succulent plants to arid conditions, environmental monitoring and work on the directed induction of valuable secondary metabolites in succulents to obtain new herbal medicines.

Accumulation of Secondary Metabolites of Rhodiola semenovii Boriss. In Situ in the Dynamics of Growth and Development.

Rhodiola semenovii Boriss. (Regel and Herder) might be a promising replacement for the well-known but endangered Rhodiola rosea L. In this research, the metabolic profile of R. semenovii, including drug-active and stress-resistant components, was studied in the context of source-sink interactions in situ in the dynamics of growth and development. Gas chromatography with mass spectrometric detection and liquid chromatography methods were used. The data obtained allow for assumptions to be made about which secondary metabolites determine the level of stress resistance in R. semenovii at different stages of ontogeny in situ. For the first time, an expansion in the content of salidroside in the above-ground organs, with its maximum value during the period of seed maturation, and a significant decrease in its content in the root were revealed in the dynamics of vegetation. These results allow us to recommend collecting the ground component of R. semenovii for pharmaceutical purposes throughout the seed development stage without damaging the root system.

Laryngeal epithelial defenses against laryngopharyngeal reflux: investigations of E-cadherin, carbonic anhydrase isoenzyme III, and pepsin.

OBJECTIVES: This is the third annual report of an international research network studying the cellular impact of laryngopharyngeal reflux (LPR) on laryngeal epithelium. The objective of this study was to investigate the presence of E-cadherin (epithelial cadherin; the intercellular junctional complex protein) in relation to the presence of (intracellular) pepsin and carbonic anhydrase isoenzyme III (CAIII). METHODS: Fifty-four laryngeal biopsy specimens from 18 LPR patients were studied by immunohistochemistry and Western blotting for pepsin, E-cadherin, and CAIII. These data were compared to those from normal control subjects analyzed in another research study. RESULTS: Intracellular pepsin was detected in LPR patients, but not in controls. E-cadherin expression was reduced in patients with LPR. Carbonic anhydrase III expression was not found in the vocal fold or in the majority of samples taken from the ventricle of LPR patients and was inversely associated with E-cadherin membranous expression. CONCLUSIONS: The findings of depleted E-cadherin and CAIII and the presence of pepsin appear to correlate with LPR. The reduced protective response indicated by the reduced expression of CAIII may play an important role in the disruption of the intercellular barrier associated with the down-regulation of E-cadherin.

Cell biology of laryngeal epithelial defenses in health and disease: further studies.

This is the second annual report of an international collaborative research group that is examining the cellular impact of laryngopharyngeal reflux (LPR) on laryngeal epithelium. The results of clinical and experimental studies are presented. Carbonic anhydrase (CA), E-cadherin, and MUC gene expression were analyzed in patients with LPR, in controls, and in an in vitro model. In patients with LPR, we found decreased levels of CAIII in vocal fold epithelium and increased levels in posterior commissure epithelium. The experimental studies confirm that laryngeal CAIII is depleted in response to reflux. Also, cell damage does occur well above pH 4.0. In addition, E-cadherin (transmembrane cell surface molecules, which have a key function in epithelial cell adhesion) was not present in 37% of the LPR laryngeal specimens. In conclusion, the laryngeal epithelium lacks defenses comparable to those in esophageal epithelium, and these differences may contribute to the increased susceptibility of laryngeal epithelium to reflux-related injury.

Clonidine as an adjuvant for lidocaine in axillary brachial plexus block in patients with chronic renal failure.

BACKGROUND: Clonidine is often used as an adjuvant for local anaesthetics in regional anaesthesia; however, its effects on axillary block in chronic renal failure patients have not been investigated. These effects were the focus of this study. METHODS: Twenty-eight adult chronic renal failure patients (ASA physical status III) scheduled for arteriovenous fistula construction were studied in a prospective, randomized, double-blind, controlled design. All axillary block procedures were performed by the same anaesthesiologist using the nerve stimulator technique. The control group received 40 ml of lidocaine (10 mg ml(-1)) combined with 1 ml of saline, and the clonidine group received 40 ml of lidocaine (10 mg ml(-1)) mixed with 150 microg of clonidine. Characteristics of the patients and the blocks were recorded, in addition to data on the nerves stimulated, intraoperative haemodynamic parameters, and sedative and analgesic requirements. RESULTS: The onset time for sensory blockade was longer in the clonidine group than in the controls (P = 0.013), and both motor and sensory blocks lasted longer in the clonidine group (P = 0.004, P < 0.001, respectively). In addition, the clonidine group had lower mean arterial pressures, heart rates and higher sedation scores compared to the controls (P < 0.05 for all). CONCLUSION: Use of clonidine (150 microg) as adjuvant for lidocaine in axillary blocks for arteriovenous fistula construction in chronic renal failure patients prolongs blockade, decreases both heart rates and blood pressures and provides sedative effects.