Fluorinated pyrrole incorporated 2-thiazolyl hydrazone motifs: a new class of antimicrobial and anti tuberculosis agents.

In aim of obtaining novel bio-active compounds, a new series of fluorinated 1-(4-(aryl)thiazol-2-yl)-2-((1-(aryl)-2,5-dimethyl-1H-pyrrol-3-yl)methylene)hydrazines (5a-t) and 1-(4-(4-aryl)thiazol-2-yl)-2-((3-(2,4-dichlorophenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)hydrazines (8a-d) were synthesized and screened for their antibacterial and antifungal activities. The potent compounds were further screened in vitro for anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv strain. Compounds 5a, 5c-5h and 5m were found to be good inhibitors of B. subtilis with MIC ranging from 0.2 to 0.8 µg mL-1, which are nearly three to ten times more potent than the standard drug Ciprofloxacin. Compounds 5a, 5h-5k and 5o exhibited potent antifungal activity against C. albicans strain with MIC ranging from 0.4 to 1.6 µg mL-1. Compounds 8a-8c were found to be excellent inhibitors of A. niger. Compounds 5a and 5k showed significant anti tubercular activity with MIC 3.12 and 6.25 µg mL-1 respectively. Furthermore, highly active compounds were tested for their preliminary toxicity profile by hemolytic assay and were found to be non hemolytic at higher concentration with good selectivity index. Cytotoxicity of the potent compounds 5a, 5d, 5g, 5i and 5k was checked by MTT assay using normal embryonic kidney cell line HEK 293 and found to be non-toxic up to 50-200 times the MIC for antibacterial activity.

Phytochemically Functionalized Cu and Ag Nanoparticles Embedded in MWCNTs for Enhanced Antimicrobial and Anticancer Properties.

Nanomedicine is an emerging field concerned with the use of precision engineered nanomaterials, which leads to the development of novel remedial and diagnostic modalities for human use. In this study, Cu(NO3)2 and AgNO3 precursors were reduced to copper nanoparticles (CuNPs) and silver nanoparticles (AgNPs) using Terminalia arjuna bark extracts under microwave irradiation in the presence of well-dispersed multi-walled carbon nanotubes (MWCNTs) in aqueous medium. The formation of CuNPs or AgNPs and their functionalization with MWCNTs via bioactive molecules of plant extract were evidenced from UV-Vis spectra, XRD, FTIR, FESEM, EDX, and TEM images. The phytochemically functionalized Cu-MWCNTs and Ag-MWCNTs nanomaterials showed enhanced biocide activity, and the inhibitory activity for bacteria was higher than that of fungus. Furthermore, these biohybrid nanomaterials are non-toxic to normal epithelial cells (Vero), whereas they are highly toxic for tested human cancer cells of MDA-MB-231, HeLa, SiHa, and Hep-G2. The cell viability was found to decrease with the increasing dose from 10 to 50 µg mL-1, as well as incubation time from 24 to 72 h. For instance, the cell viability was found to be ~91 % for normal Vero cells and ~76 % for cancer cells for lower dose of 10 µg mL-1.

Phytosynthesis of gold nanoparticles using Mappia foetida leaves extract and their conjugation with folic acid for delivery of doxorubicin to cancer cells.

Mappia foetida leaves extract is used as bioreductant for the synthesis of gold nanoparticles and their application in the efficient delivery of doxorubicin to human cancer cells is reported here. The formation of gold nanoparticles is evident from their characteristic optical absorption at ~560 nm. X-ray diffraction pattern of gold nanoparticles confirmed their fcc structure. Fourier transform infrared spectroscopy shows the bioactive molecules from plant extract capped on the surface of gold nanoparticles and conjugation of doxorubicin along with activated folic acid as navigational molecules for targeted drug delivery. Such a conjugation of gold nanoparticles is characterized by their weight loss, ~35-40 %, due to thermal degradation of plant biomass and conjugated drug along with receptor, as observed in thermogravimetric analysis. The spherical shaped gold nanoparticles (Φ 10-20 nm) are observed by field emission scanning electron microscopy and transmission electron microscopy images and the expected elemental composition by energy dispersive X-ray spectroscopy. Gold nanoparticles conjugated with activated folic acid and doxorubicin complex is found to be toxic for human cancer cells viz., MDA-MB-231, HeLa, SiHa and Hep-G2. Furthermore, the amount of drug released was maximum at pH 5.3 (an ambient condition for intravenous cancer drugs) followed by pH 7.2 and pH 6.8.