Phytochemical screening, antimicrobial, antioxidant, anticancer activities on cervical cancer cell lines and aero-digestive extract of Moringa oleifera.

The phytochemical screening showed that the Moringa oleifera (MO) extract contained many compounds such as polyphenols, polyterpenes, sterols, reducing sugars, and hydrolysates tannins. The MICs of MO extract for microbial strains is 0.73 mg/ml for Escherichia coli, Pseudomonas aeruginosa, 7.5 mg/ml for Enterococcus faecalis, Staphylococcus aureus and 0.5 mg/ml for Candida albicans. The MO extract has an IC50 of 3.403 mg/ml has an antioxidant activity by DPPH radical scavenging. The cytotoxic activity of MO extract was evaluated by determining the content of lactate dehydrogenase released by the lysed cells. MO extract exhibited cytotoxic activity against HeLa and FaDu cell lines with an identical IC50 value of 25 µg/ml. We did not observe any remarkable decrease cytotoxic activity when these lines were exposed to the MO extract after 48 h. Our findings help to support the promising role of MO as anticancer agent and open a new challenge for studying DNA fragmentation.

Access to a Library of 1,3-disubstituted-1,2,3-triazenes and Evaluation of their Antimicrobial Properties.

BACKGROUND: Due to the rapid development of microbial resistance, finding new molecules became urgent to counteract this problem. OBJECTIVE: The objective of this work is to access 1,2,3-triazene-1,3-disubstituted, a class of molecule with high therapeutic potential. METHODS: Here we describe the access to 17 new triazene including six with an imidazole-1,2,3-triazene moiety and eleven with an alkyl-1,2,3-triazene moiety and their evaluation against five strains: two gram (-): Escherichia coli ATCC 25921 and Pseudomonas aeruginosa ATCC 27253; two gram (+) : Staphylococcus aureus ATCC 38213 and Enterococcus faecalis ATCC 29212; and one fungi: Candida albicans ATCC 24433. RESULTS: All strains were sensitive and the best MIC, 0.28 µM, is observed for 4c against Escherichia coli ATCC 25921. Compound 9, 3-isopropynyltriazene, appears to be the most interesting since it is active on the five evaluated strains with satisfactory MIC 0.32 µM against Escherichia coli and Pseudomonas aeruginosa and 0.64 µM against Enterococcus faecalis and Pseudomonas aeruginosa. CONCLUSION: Comparing the structure activity relationship, electron withdrawing groups appear to increase antimicrobial activity.

Targeting bacterial biofilms: design of a terpenoid-like library as non-toxic anti-biofilm compounds.

A new class of anti-biofilm compounds possessing 1,4-disubstituted-(1H)-1,2,3-triazolic cores was designed. Their efficient synthesis was performed by means of click chemistry through 1,3-dipolar cycloadditions. Two compounds were found to act as specific anti-biofilm agents against a gram negative species.

Design, synthesis, and biological activities of conformationally restricted analogs of primaquine with a 1,10-phenanthroline framework.

A series of primaquine analogs was prepared, according to a conformationally restricted conformation of primaquine. In vitro antiplasmodial activities were evaluated and showed that all compounds were active on different strains of Plasmodium falciparum. In particular compounds 5 and 15 possessing a methoxy group were more active than was primaquine. Furthermore, analog 5 displayed good in vitro gametocytocidal activity. In addition selectivity indexes were calculated in respect with cytotoxic activities on Vero cell lines.