Anti-ulcerogenic and anti-ulcerative colitis (UC) activities of seven amines derivatives

The Novel target compounds (CP-1-7) were synthesized and tested at doses up to 1000mg/kg for their entitled activities. They exerted promising results without any behavioral changes and mortality in mice. Therefore, according to the results obtained in our study, it could be categorized as highly safe agents for treating UC since substances possessing LD50 higher than 50mg/kg are considered nontoxic. They also possessed a potent anti-ulcerogenic activity with different potentials. The most effective compound was CP-4, it produced 97.7% ulcer protection of control followed by CP-3, which produced 90.3% protection, while the standard drug ranitidine (100mg/kg) produced 49.2% protection. Compound CP-1 showed lowest activity among the current series, it produced 55.5% protection. The target compounds were significantly more effective than the standard in reducing ulcer index. The anti-ulcerative colitis activity was tested using acetic acid induced colitis model. The curative effect of the tested compounds at a dose of 50mg/kg oral administration on rats showed a potent anti-ulcerative colitis activity with different potentials. They induced a significant decrease in ulcer score, ulcer area, ulcer index and weight/length of the colon specimens.The percent protection of control colitis ranged from 66.8% for CP-7 to 22.3% for CP-5; however the percent protection for dexamesathone (0.1. mg/kg) was 59.3%. The effect of the tested compounds CP-7 and CP-3 at dose 50. mg/kg were significantly more effective than dexamesathone (0.1. mg/kg) in reducing all parameters.Liver functions were not affected as there is no effect on the activity of both AST and ALT in animals that received the compounds, so the compounds didn't reveal hepatotoxic manifestation. Although, the results on kidney functions showed that, CP-1 slightly elevated blood urea concentration and CP-3 & CP-4 slightly elevated serum creatinine; no apparent nephrotoxic manifestations were recorded

Novel quinazoline and acetamide derivatives as safe anti-ulcerogenic agent and anti-ulcerative colitis activity

Two novel quinazoline derivatives named as; 3-[(4-hydroxy-3-methoxy-benzylidene)-amino]-2-p-tolyl3H-quinazolin-4-one (5) and 2-p-Tolyl-3-[3,4,5-trimethoxy-benzylidene-amino]-3H-quinazolin-4-one (6) in addition to one acetamide derivative named as 2-(2-Hydroxycarbonylphenylamino)-N-(4- aminosulphonylphenyl) 11 were synthesized, and evaluated for their anti-ulcerogenic & AntiUlcerative colitis activities. All of the three compounds showed curative activity against acetic acid induced ulcer model at a dose of 50 mg/kg, they produced 65%, 85% & 57.74% curative ratio for compounds 5, 6 & 11 respectively. The effect of the tested compounds 5, 6 & 11 at dose 50 mg/kg were significantly (P < 0.01) more effective than dexamesathone (0.1 mg/kg) in reducing all parameters. Compounds showed curative activity of for peptic ulcer (induced by absolute alcohol (at a dose of 50 mg/kg, it produced Curative of control ulcer 56.00%, 61.70% & 87.1% for compounds 5, 6 & 11 respectively at dose 50 mg/kg, while the standard drug (Omeprazole 20 mg/kg) produced 33.3%. In both tests, the activity of our target compounds were higher than the standard drugs used for treatment of peptic ulcer and ulcerative colitis. No side effects were reported on liver and kidney functions upon prolonged oral administration of this compounds

Development and validation of a high-performance thin-layer chromatographic method for the quantitative analysis of vitexin in Passiflora foetida herbal formulations

© 2019 Dehon et al. Introduction: Formative evaluations of clinical teaching for emergency medicine (EM) faculty are limited. The goal of this study was to develop a behaviorally-based tool for evaluating and providing feedback to EM faculty based on their clinical teaching skills during a shift. Methods: We used a three-phase structured development process. Phase 1 used the nominal group technique with a group of faculty first and then with residents to generate potential evaluation items. Phase 2 included separate focus groups and used a modified Delphi technique with faculty and residents, as well as a group of experts to evaluate the items generated in Phase 1. Following this, residents classified the items into novice, intermediate, and advanced educator skills. Once items were determined for inclusion and subsequently ranked they were built into the tool by the investigators (Phase 3). Results: The final instrument, the Faculty Shift Card, is a behaviorally-anchored evaluation and feedback tool used to facilitate feedback to EM faculty about their teaching skills during a shift. The tool has four domains: teaching clinical decision-making; teaching interpersonal skills; teaching procedural skills; and general teaching strategies. Each domain contains novice, intermediate, and advanced sections with 2-5 concrete examples for each level of performance. Conclusion: This structured process resulted in a well-grounded and systematically developed evaluation tool for EM faculty that can provide real-time actionable feedback to faculty and support improved clinical teaching

Glucosinolates, myrosinase hydrolysis products, and flavonols found in rocket (Eruca sativa and Diplotaxis tenuifolia)

Rocket species have been shown to have very high concentrations of glucosinolates and flavonols, which have numerous positive health benefits with regular consumption. In this review we highlight how breeders and processors of rocket species can utilize genomic and phytochemical research to improve varieties and enhance the nutritive benefits to consumers. Plant breeders are increasingly looking to new technologies such as HPLC, UPLC, LC-MS and GC-MS to screen populations for their phytochemical content to inform plant selections. Here we collate the research that has been conducted to-date in rocket, and summarise all glucosinolate and flavonol compounds identified in the species. We emphasize the importance of the broad screening of populations for phytochemicals and myrosinase degradation products, as well as unique traits that may be found in underutilized gene bank resources. We also stress that collaboration with industrial partners is becoming essential for long-term plant breeding goals through research

Novel essential amino acid-sulfanilamide hybrid as safe anti-ulcerogenic agent with anti-helicobacter pylori activity

A novel and safe essential amino acid (Leucine) incorporating sulfanilamide was synthesized, and evaluated for its anti-ulcerogenic activity and in vitro anti-Helicobacter pylori activity. The new molecule showed a dose dependent activity against absolute ethanol-induced ulcer in rats, it produced percent protection of control ulcer by 66.7 at dose 100 mg/kg. In addition it showed a potent anti-Helicobacter pylori activity in vitro against 7 clinically isolated strains. The minimum inhibitory concentration (MIC) ranged from 12.5 to 50 μg/ml. The preliminary safety studies and toxicity profile are optimistic and encouraging

Comparative profiling of biomarker psoralen in antioxidant active extracts of different species of genus Ficus by validated HPTLC method

Background: A simple but sensitive HPTLC method was developed for the comparative evaluation of psoralen in antioxidant active extracts of leaves of five different species of genus Ficus (Ficus carica, Ficus nitida, Ficus ingens, Ficus palmata and Ficus vasta).Materials and Methods: HPTLC studies were carried out using CAMAG HPTLC system on Glass-backed silica gel 60F254 HPTLC pre-coated plates using selected mobile phase toluene: methanol (9:1). The antioxidant activity was carried out, using DPPH free radical method.Results: Among all the five species of genus Ficus, F. palmata and F. carica exhibited comparatively good antioxidant activity in DPPH assay. The developed HPTLC method was found to give a compact spot for psoralen (Rf = 0.55±0.001) at 305 nm. The regression equation and r2 for psoralen was found to be Y= 4.516X+35.894 and 0.998. The quantification result revealed the presence of psoralen in only two species, F. carica (0.24%, w/w) and F. palmata (1.88%, w/w) which supported their supremacy for anti-oxidant potential over other species. The statistical analysis proved that the developed method was reproducible and selective.Conclusion: The developed method can be used as an important tool to assure the therapeutic dose of active ingredients in herbal formulations as well as for standardization and quality control of bulk drugs and in-process formulations. This method can also be employed for the further study of degradation kinetics and determination of psoralen in plasma and other biological fluids.Key words: Ficus species, psoralen, antioxidant, HPTLC, Validation

3-[(1-Hy­droxy-1-phenyl­propan-2-yl)amino]-5,5-dimethyl­cyclo­hex-2-enone

The asymmetric unit of the title compound, C17H23NO2, consists of two crystallographically independent mol­ecules (A and B). The cyclo­hexene rings in both mol­ecules adopt an envelope conformation. In the crystal, independent mol­ecules, A and B, are each linked by inter­molecular bifurcated (N,O)—H⋯O hydrogen bonds, generating R 2 1(7) ring motifs and forming infinite chains along the b axis

EFFECT OF BETA VULGARIS L. ON CHOLESTEROL RICH DIET-INDUCED HYPERCHOLESTEROLEMIA IN RATS

Abstract The lyophilized aqueous extract of Beta vulgaris L. (beet root) (BVE) was investigated for its possible antihypercholesterolemic and antioxidant potential in cholesterol rich diet-induced hypercholesterolemia in Wistar albino rats. Hypercholesterolemia was induced in rats by feeding 1% cholesterol rich diet for 10 weeks. Lipid profile and glucose were estimated in serum. Malondialdehyde (MDA) and non-protein sulfhydryls (NP-SH) levels were measured in liver and heart. Hypercholesterolemic rats showed a significant increase in total cholesterol and triglycerides and a significant decrease in high-density lipoprotein-cholesterol (HDL-C) levels. BVE at the doses of 250 and 500 mg/kg body weight for 70 consecutive days showed a significant decrease in total cholesterol and triglycerides and significant increase in HDL-C. Furthermore, hypercholesterolemic rats showed free radical generation (lipid peroxidation), evident by a significant increase in MDA level and a significant reduction in NP-SH content in both liver and heart homogenates. BVE treatment significantly decreased MDA level and significantly replenished the reduced NP-SH content in both liver and heart tissue. The acute toxicity test of BVE showed no mortality or morbidity in rats. The findings indicate that BVE has a significant antihypercholesterolemic and antioxidant potential and/or free radical scavenging properties in hypercholesterolemic, rats possibly exerted by the phytoconstituents present in the beet root. Rezumat Studiul experimental evaluează acţiunea antihipercolesterolemiantă şi antioxidantă a extractului apos liofilizat al rădăcinii plantei Beta vulgaris (Chenopodiaceae). Studiul a fost realizat pe şobolani albi de laborator, cărora li s-a indus experimental hipercolesterolemia. A fost evaluat profilul lipidic şi glucidic al animalelor, concentraţia serică a malonildialdehidei. De asemenea, au fost evaluate (ĭn ţesutul hepatic şi cardiac) grupările sulfhidril non-proteice. Rezultatele obţinute indică proprietăţile antihipercolesterolemiante şi antioxidante, datorate fitoconstituenţilor prezenţi în rădăcina plantei studiate