Comparative Toxicity of Bis-pyridinium Acetamide Derivatives in Human Cell Lines and their Acute Toxicity in Swiss Albino Mice

Having established the antidotal efficacy of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide (HNK oximes) against Diisopropylphosphorofluoridate (DFP) and sarin poisoning. Toxicity of HNK series and 2-PAM oximes on Human cell lines and Swiss male mice i.e. in vitro and in vivo to reported. Toxicity of the oximes was investigated in Hela, Hep G2 and HEK 293 cell lines and compared with most commonly used 2-PAM. Median lethal doses (LD50) of the oximes (2-PAM, HNK-102, HNK-106, and HNK-111) were also determined following intramuscular, intraperitoneal, intravenous and oral routes of administration. All tested oximes showed no cytotoxic effect on all three cell lines in concentrations up to 0.05 mg/mL. At higher dose (0.5 mg/mL), HNK-102 found to be less toxic thus safer than 2-PAM and other oximes in all the three cell lines. In corroboration with in vitro finding, HNK-102 was found to be least toxic compared to other oximes via intra-peritoneal and intravenous routes of administration. Also, HNK-102 was found to be unequivocally safer compared to that of 2-PAM through i.m. and i.p. routes. For all tested oximes, toxicity following oral route, was found to be lower compared to injections, signifying that these are safer and convenient compounds for administration. These finding also suggested that HNK-102 is safer and better lead as an antidote compared to 2-PAM, against OP intoxicants

In-vitro Evaluation of Bis-pyridinium Oximes Connected by Xylene Linkers as Reactivators of DFP-inhibited Electric EEL Acetylcholinesterase

Bis-pyridinium oximes connected by xylene linkers were synthesised and their in-vitro reactivation efficacy was evaluated for DFP inhibited AChE. The reactivation efficacy data were compared with those of 2-PAM and obidoxime. However, it was observed that none of these oximes were able to surpass the reactivation efficacy of 2-PAM and obidoxime in reactivating DFP inhibited AChE. 2-PAM and obidoxime respectively exhibited52 per cent and 43 per cent reactivation of DFP inhibited AChE, where as the synthesised oximes 3a, 3d, and 3f showed 37 per cent, 30 per cent, and 31 per cent reactivation, respectively within 10 min at 10-3 M

COMPARATIVE IN-VITRO ANTIBACTERIAL AND ANTIFUNGAL ATTRIBUTES OF DIFFERENT SOLVENT EXTRACTS FROM LEAF, BARK, ROOT AND INFLORESCENCE OF MEMECYLON UMBELLATUM BURM.

This paper describes the antibacterial and antifungal activities and Minimum Inhibitory Concentration (MIC) of different solvent (pet. ether, chloroform, ethyl acetate, acetone, methanol and water) extracts of leaves, bark, root and inflorescence of Memecylon umbellatum burm. The percent yields from leaves, bark, root and inflorescence was found to be 0.2062 to 2.836, 0.0601 to 0.5142, 0.050 to 1.425, 0.0210 to 0.717 respectively. Overall, acetone extract produced from the leaves exhibited significantly (P < 0.05) higher antibacterial activity along with superior antifungal activity. MIC for acetone and ethyl acetate extract of leaf was found to be 0.5 mg for the entire organisms compared to 3-15 mg for other extracts. Such study will explore pharmacological activity of the tested parts of Memecylon umbellatum burm especially, the leaves which might be valuable for therapeutic applications

Phytochemical screening and In Vitro Antioxidant potential of Memecylon umbellatum Burm leaf extracts

Objective: Different dry extracts of Memecylon umbellatum Burm leaf obtained by various solvents such as petroleum ether, chloroform, ethyl acetate, acetone, methanol and chloroform water (IP) was screened to reap the benefits of its antioxidant and free radical scavenging properties using ascorbic acid as standard antioxidants. Methods: The in vitro free radical scavenging activity was evaluated using diphenyl picryl hydrazyl (DPPH) radical method using various concentrations of dry extract in distilled water (1, 2, 4, 8, 16, 20 μg/ml) against blank with ascorbic acid as a standard in same concentrations. Results: Among the all extracts, Methanol leaf extract has showed higher Antioxidant activity (84.65 ± 0.064 %) having IC50 Value 11.81 ± 0.033 μg/ml at 20 μg/ml. While, IC50 value for ascorbic acid was found to be 8.91 ± 0.084 μg/ml. Conclusion: The results clearly indicate that Methanol leaf extract of Memecylon umbellatum is effective in free radical scavenging. So in future, this may emerge as promising natural herbal source of powerful antioxidant. Keywords: Memecylon umbellatum, DPPH reagent, Antioxidant activity, Ascorbic acid, IC50

Synthesis of 4-Aryl Substituted 3,4-Dihydropyrimidinones Using Silica-chloride Under Solvent Free Conditions

This paper describes an improved procedure for the efficient and facile synthesis of 4-aryl substituted 3, 4-dihydropyrimidinones under mild reaction conditions with excellent yields using inexpensive silica chloride under solvent free conditions

Synthesis of 4-Aryl substituted 3,4-dihydropyrimidinones using silica-chloride under solvent free conditions

Abstract: This paper describes an improved procedure for the efficient and facile synthesis of 4-aryl substituted 3, 4-dihydropyrimidinones under mild reaction conditions with excellent yields using inexpensive silica chloride under solvent free conditions