Complementary pharmacological and toxicological characterization data on the pharmacological profile of N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl) acetamide

This text presents complementary data corresponding to pharmacological and toxicological characterization of N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide (LIA) compound. These data support our research article entitled “Pharmacological profile of N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide, a novel analog of lidocaine” Déciga-Campos M., Navarrete-Vázquez G., López-Muñoz F.J., Librowski T., Sánchez-Recillas A., Yañez-Pérez V., Ortiz-Andrade R. (2016) [1]. Toxicity was predicted through the ACD/ToxSuite software and evaluated in vivo using brine shrimp larvae (Artemia salina L.) and mice. Also, we used the micronucleus assay to determine genotoxicity. We used the platform admetSAR to predict absorption properties of LIA and lidocaine. Keywords: N-(2,6-dichlorophenyl)-2-(4-methyl-1-piperidinyl)acetamide, Toxicity, Lidocain

Spasmolytic and Antibacterial Activity of Two Citrus sinensis

Antibacterial activity on ATCC strains of Escherichia coli, Salmonella enterica, Salmonella enteritidis, and Salmonella choleraesuis and spasmolytic effect on contraction on rat ileum trips were determinate. Eight organic extracts (hexanic and methanolic) of albedo (mesocarp) and flavedo (pericarp) of two varieties (Valencian and National) of Citrus sinensis (L.) Osbeck of Yucatán, México, were studied. Additionally, chromatographic fingerprints were obtained and correlated with their pharmacological effects. MAN, MAV, and HFN extract caused inhibition against S. choleraesuis (MIC: 1000 µg/mL) and S. enteritidis (MIC: 1000 µg/mL). Regarding the spasmolytic effect, the Valencian extracts variety was more efficient on spontaneous contraction, HAV (Emax = 51.98±1.98%), MAV (Emax = 35.98±1.42%), HFV (Emax = 68.91±4.14%), and MFV (Emax = 51.28±2.59%), versus National variety, HAN (Emax = 43.80±6.32%), MAN (Emax = 14.62±1.69%), HFN (Emax = 64.87 ± 3.04%), and MFN (Emax = 31.01±3.92%). Chromatographic fingerprints of HFV and HFN were found to have some similar signals that belong to monoterpenes, whereas for HAN and HAV similar signals were found belonging to fatty acids and triterpenoids. Methanolic extracts showed signals of (1) furfural, (2) furfural acetone (3) furfuraldehyde and (4) β–sitosterol compounds. Flavedo portion of C. sinensis possessed spasmolytic effect on rat ileum strips and antibacterial activity against Salmonella strains. This species is source for obtaining bioactive compounds with therapeutic potential in the treatment of infectious diarrhea

2-Methyl-2-(4-nitro­phenyl­sulfanyl)­propanoic acid

The title compound, C10H11NO4S, is of inter­est with respect to its biological activity. The mol­ecules are linked into centrosymmetric dimers by inter­molecular O—H⋯O hydrogen bonds and the dimers are further connected into chains by weak C—H⋯O inter­actions

Vasorelaxant activity of Euphorbia furcillata Kunth mainly by activation of NO/cGMP pathway and calcium channel blockade

The aim of current study was to determinate ex vivo and chromatographic fingerprint by HPLC of four extracts of Euphorbia furcillata K. Ethyl acetate extract of Euphorbia furcillata (EaEEf) was the most effective and potent extract (Emax=98.69±1.24%) and its effect was partially endothelium-dependent. Functional vasorelaxant mechanism of action of EaEEf was determinate, EaEEf showed efficient relaxation of KCl [80 mM]-induced contraction and norepinephrine and CaCl2 contraction curves showed diminution of maximal contraction in the presence of EAEEf and EaEEf-relaxation curve was shifted to the right in the presence of L-NAME (nitric oxide synthase inhibitor) and ODQ (guanylate cyclase inhibitor). Chromatographic fingerprints analysis suggests presence of diterpenoid such as abietane, tigliane, and ingenane skeletons. Our experiments suggest the EaEEf vasorelaxant activity could be attributed to diterpenoid molecules whose mechanism involves nitric oxide production and calcium channel blockade

Encapsulation and release characteristics of glibenclamide loaded calcium-alginate beads

The aims of this study were to formulate calcium-alginate beads containing glibenclamide, characterize the resulting microparticles, evaluate the release characteristics of this type of delivery system in an in vitro dissolution test, and compare it with two commercially available trademarks (Daonil® and Glibetab®). We obtained glibenclamide loaded calcium-alginate beads with a rough surface and a particle size between 150-200 µm. For the in vitro dissolution test Daonil® at 45 min showed a Q > 70%, whereas Glibetab® and glibenclamide calcium-alginate beads a Q < 70%; in spite of that glibenclamide calcium-alginate beads showed significant release properties

Spasmolytic and Antibacterial Activity of Two Citrus sinensis Osbeck Varieties Cultivated in Mexico

Antibacterial activity on ATCC strains of Escherichia coli, Salmonella enterica, Salmonella enteritidis, and Salmonella choleraesuis and spasmolytic effect on contraction on rat ileum trips were determinate. Eight organic extracts (hexanic and methanolic) of albedo (mesocarp) and flavedo (pericarp) of two varieties (Valencian and National) of Citrus sinensis (L.) Osbeck of Yucatán, México, were studied. Additionally, chromatographic fingerprints were obtained and correlated with their pharmacological effects. MAN, MAV, and HFN extract caused inhibition against S. choleraesuis (MIC: 1000 g/mL) and S. enteritidis (MIC: 1000 g/mL). Regarding the spasmolytic effect, the Valencian extracts variety was more efficient on spontaneous contraction, HAV ( max = 51.98 ± 1.98%), MAV ( max = 35.98 ± 1.42%), HFV ( max = 68.91 ± 4.14%), and MFV ( max = 51.28 ± 2.59%), versus National variety, HAN ( max = 43.80 ± 6.32%), MAN ( max = 14.62 ± 1.69%), HFN ( max = 64.87 ± 3.04%), and MFN ( max = 31.01 ± 3.92%). Chromatographic fingerprints of HFV and HFN were found to have some similar signals that belong to monoterpenes, whereas for HAN and HAV similar signals were found belonging to fatty acids and triterpenoids. Methanolic extracts showed signals of (1) furfural, (2) furfural acetone (3) furfuraldehyde and (4) -sitosterol compounds. Flavedo portion of C. sinensis possessed spasmolytic effect on rat ileum strips and antibacterial activity against Salmonella strains. This species is source for obtaining bioactive compounds with therapeutic potential in the treatment of infectious diarrhea

Citroflavonoids as Promising Agents for Drug Discovery in Diabetes and Hypertension: A Systematic Review of Experimental Studies

Flavonoids are naturally occurring compounds widely distributed in the Citrus genus. These natural compounds have many health benefits, mainly for metabolic and cardiovascular diseases. In fact, some these compounds are components of drug products with approved indications for peripheral vascular insufficiency and hemorrhoids. However, information on pharmacological effects of these compounds remains disperse and there is scarce comprehensive analysis of whole data and evidence. These kinds of evidence analyses could be necessary in drug design and the development of novel and innovate drug products in diabetes and hypertension. We aimed to systematically search for evidence on the efficacy of citroflavonoids in diabetes and hypertension in in vivo models. We searched four literature databases based on a PICO strategy. After database curation, twenty-nine articles were retrieved to analyze experimental data. There was high heterogeneity in both outcomes and methodology. Naringenin and hesperetin derivates were the most studied citroflavonoids in both experimental models. More investigation is still needed to determine its potential for drug design and development