RESUMO
The aim of the present study is to synthesize cationic salts from a relatively toxic compound named 2-mercaptobenzimidazole and to evaluate some of their pharmacological properties. The acute toxicity of these salts is evaluated according to OECD 423 Guidelines at the doses of 300 and 2000 mg/kg; their peripheral analgesic effect is studied using the Koster test at the therapeutic dose of 200 mg/kg and their sedative action is evaluated using Traction, Chimney, Hole-board, and Rotarod tests at the doses of 200 and 400 mg/kg. All synthesized molecules show no acute toxicity according to OECD Code 423 guidelines at doses ranging from 300 to 2000 mg/kg and do not cause any obesity or anorexia. Also, the results of the Koster test show that the studied compounds have an average analgesic effect at the dose of 200 mg/kg compared to acetylsalicylic acid. In addition, the elaborated compounds have shown a moderate sedative effect at the dose of 400 mg/kg, in comparison to 2-mercaptobenzimidazole (400 mg/kg) and Bromazepam (20 mg/kg). These compounds have no cataleptic and hypnotic effects on the central nervous system at the doses of 200 and 400 mg/kg. These results argue in favor of a possible integration of the most active salts tested in the pharmaceutical industry owing to their analgesic and sedative effects.
RESUMO
The objective of our work is to make a pharmacological study of molecules derived from 4-phenyl-1,5-benzodiazepin-2-one carrying long chains so that they have a structure similar to surfactants, with the benzodiazepine as a hydrophilic head and a carbon chain as a hydrophobic tail. First, we studied the acute toxicity of the above mentioned 4-phenyl-1,5-benzodiazepin-2-one derivatives. This study was conducted according to OECD 423 guidelines in female mice and revealed that these compounds are nontoxic. We then assessed the psychotropic effects of our products on the central nervous system (CNS). The results obtained show that 4-phenyl-1,5-benzodiazepin-2-one has no sedative effect at therapeutic doses of 100 and 200 mg/kg. On the other hand, its long-chain derivatives possess them. Moreover, all these products have no cataleptic and hypnotic effects at the doses studied. But at 100 mg/kg, these compounds all have the ability to significantly prolong the hypnotic effect of thiopental sodium.
RESUMO
Melissa officinalis L. (Lamiaceae) had been reported in traditional Moroccan medicine to exhibit calming, antispasmodic, and strengthening heart effects. Therefore, this study is aimed at determining the anti-inflammatory activities of M. officinalis L. leaves. The effect of the essential oil of the leaves of this plant was investigated for anti-inflammatory properties by using carrageenan and experimental trauma-induced hind paw edema in rats. The essential oil extracted from leaves by hydrodistillation was characterized by means of gas chromatography-mass spectrometry (GC-MS). M. officinalis contained Nerol (30.44%), Citral (27.03%), Isopulegol (22.02%), Caryophyllene (2.29%), Caryophyllene oxide (1.24%), and Citronella (1.06%). Anti-inflammatory properties of oral administration of essential oil at the doses of 200, 400 mg/kg p.o., respectively, showed significant reduction and inhibition of edema with 61.76% and 70.58%, respectively, (P < 0.001) induced by carrageenan at 6 h when compared with control and standard drug (Indomethacin). On experimental trauma, M. officinalis L. essential oil showed pronounced reduction and inhibition of edema induced by carrageenan at 6 h at 200 and 400 mg/kg with 91.66% and 94.44%, respectively (P < 0.001). We can conclude that the essential oil of M. officinalis L. possesses potential anti-inflammatory activities, supporting the traditional application of this plant in treating various diseases associated with inflammation and pain.
