Synthesis and characterization of some new tebufenozide analogues and study their toxicological effect against Spodoptera littoralis (Boisd.)

Many of mimic analogues synthesized before depending on the change in the structure of aromatic rings. In this work, the carbonyl group in the structure of compounds 1-4 converted to thiocarbonyl group, and then studying the toxicological activity due to chemical change in the active center of mimic analogues was performed for compounds N-tert-butyl-2,4-dichloro-N'-(2,4-dichlorobenzoyl)benzohydrazide (2) and N-tert-butyl-2,4-dichloro-N'-[(2,4-dichlorophenyl)carbonothioyl]benzenecarbothiohydrazide (6). The toxicological study was done by using 2nd and 4th instar larvae of the cotton leaf worm, Spodoptera littoralis (Boisd.). Five concentration levels (600, 300, 150, 75 and 37.5 ppm) of compounds (2) and (6) were applied on the fresh plant food to the newly grown (2nd and 4th) instar larvae.

Toxicological Activity of the Methanolic Leaf Extract of Some Medicinal Plants Used in Sokoto Township and Environs

Inspite of the availability of different antiseptic and antibiotics in most localities in some parts of the world, there is still a number of information on the usage of some local plants in various kinds of treatments of different ill-health conditions. Leaves of Ocimum basilicum, Leptadania hastata and Momordica balsamina are locally used by traditional birth attendants at pre and post-partum periods. The present study investigates the phytochemical compositions and toxicity of the leaf extracts of the plants against isolates of Listeria monocytogenes. Standard microbiological techniques and polymerase chain reaction was used to isolate and identify the bacteria. Phytochemical analysis was done and cytotoxicity of the extracts at different concentrations (MBC, OBC and LHC) were determined using human erythrocytes. Results of the phytochemical analysis revealed the presence of tannins, flavonoids, carbohydrates, alkaloids, terpinoids and glycosides in the studied extracts. Toxicity to erythrocytes, expressed as percentage hemolysis of only 17.27% (MBC1) was seen in one of the plants; M. balsamina. Similarly, the other extracts exhibited minimal toxicity to human erythrocytes (LHC1= 15.45%; OBC1= 7.6%). It was concluded that all the plant leaf extracts are safe for human consumption. Studies on the preparation, effective doses and side effects of these extracts in vivo are hereby recommended.

Advances of enantioselective solid membranes

The enantiomers differ greatly in their pharmacological and toxicological activity, and chirality is closely correlated with many significant biological processes, the separation of racemates is of great importance. Compared with...

Novel N-cyanoguanidyl derivatives: Synthesis and studying their toxicological activity against Spodoptera littoralis and Schizaphis graminum

Reaction of N-cyanoguanidine with acid chlorides and aroylisothiocyanates gave the respective; N-(N-cyanocarbamimidoyl)aryl-2-carboxamides 1-5 and N-[(N-cyanocarbamimidoyl)carbamothioyl]benzamides 6-10, which have a Neonictinoid insecticide’s active group moiety (=N–CN). They have more toxicological activity against wheat Aphid (Schizaphis graminum) than Spodoptera littoralis.

Halogen bonding: an underestimated player in membrane-ligand interactions

<div>Halogen bonds (XBs) are noncovalent interactions where halogen atoms act as electrophilic species interacting with Lewis bases. These interactions are relevant in biochemical systems being increasingly explored in drug discovery, mainly to moduate protein–ligand interactions. In this work, we report evidence for the existence of XB-mediated phospholipid–halogen recognition phenomena as our molecular dynamics simulations support the existence of favorable interactions between halobenzene derivatives and both phosphate or ester oxygen acceptors from model phospholipid bilayers. We also provide insights into the role of XBs in driving the permeation of halogenated small molecules across biological membranes. This represents a relevant molecular mechanism, previously overlooked, eventually determining the pharmacological or toxicological activity of halogenated compounds and hence with implications in drug discovery and development, a place where such species account for a significant part of the chemical space. Our data strongly suggests that, as the ubiquitous hydrogen bond, XBs should be accounted for in the development of membrane permeability models.</div>

Halogen bonding: an underestimated player in membrane-ligand interactions

<div>Halogen bonds (XBs) are noncovalent interactions where halogen atoms act as electrophilic species interacting with Lewis bases. These interactions are relevant in biochemical systems being increasingly explored in drug discovery, mainly to moduate protein–ligand interactions. In this work, we report evidence for the existence of XB-mediated phospholipid–halogen recognition phenomena as our molecular dynamics simulations support the existence of favorable interactions between halobenzene derivatives and both phosphate or ester oxygen acceptors from model phospholipid bilayers. We also provide insights into the role of XBs in driving the permeation of halogenated small molecules across biological membranes. This represents a relevant molecular mechanism, previously overlooked, eventually determining the pharmacological or toxicological activity of halogenated compounds and hence with implications in drug discovery and development, a place where such species account for a significant part of the chemical space. Our data strongly suggests that, as the ubiquitous hydrogen bond, XBs should be accounted for in the development of membrane permeability models.</div>

Chemical Compounds, Pharmacological and Toxicological Activity of Brugmansia suaveolens: A Review

This study investigates updated information in different search engines on the distribution, phytochemistry, pharmacology, and toxicology of Brugmansia suaveolens (Solanaceae) using the extracts or chemical compounds at present. This plant has been used in traditional medicine in different cultures as a hallucinatory, analgesic, aphrodisiac, nematicide, sleep inducer, and muscle relaxant, as well as a treatment for rheumatism, asthma, and inflammation. The flowers, fruits, stems, and roots of the plant are used, and different chemical compounds have been identified, such as alkaloids, volatile compounds (mainly terpenes), coumarins, flavonoids, steroids, and hydrocarbons. The concentration of the different compounds varies according to the biotic and abiotic factors to which the plant is exposed. The toxic effect of the plant is mainly attributed to atropine and scopolamine, their averages in the flowers are 0.79 ± 0.03 and 0.72 ± 0.05 mg/g of dry plant, respectively. Pharmacological studies have shown that an aqueous extract exhibits the antinociceptive effect, at doses of 100 and 300 mg/kg i.p. in mice. On the other hand, the ethanolic extract at 1000 mg/L, showed a nematocidal activity in vitro of 64% against Meloidogyne incognita in 72 h. Likewise, it showed a 100% larvicidal activity at 12.5 mg/L against Ancylostoma spp. In another study, the lethal activity of shrimp in brine from an ethanolic extract showed an LC50 of 106 µg/mL at double serial concentrations of 1000–0 (µg/mL). Although there are pharmacological and phytochemical studies in the plant, they are still scarce, which has potential for the examination of the biological activity of the more than one hundred compounds that have been reported, many of which have not been evaluated.