34446-64-5Relevant articles and documents
Organic-inorganic hybrid polysilsesquioxane nanospheres as UVA/UVB absorber and fragrance carrier
Kidsaneepoiboon, Punnipa,Wanichwecharungruang, Supason Pattanaargson,Chooppawa, Tianchai,Deephum, Ratthakan,Panyathanmaporn, Thammarat
, p. 7922 - 7930 (2011)
To avoid the photocatalysis property of inorganic UV absorbers, such as TiO2 and ZnO nanoparticles, and to utilize the minimal transdermal penetration and non-sticky nature of particulate silica particles, whilst at the same time fully harnessing the UV absorption characteristics of organic chromophores, hybrid organic-silica particles with UVA/UVB absorptive chromophores as part of their network structures were synthesized. Two UV absorptive hybrid nanospheres, poly[propyl-4-methoxycinnamamide silsesquioxane] (PTES4C) and poly[propyl-2,4-dimethoxycinnamamide silsesquioxane] (PTES24C), were synthesized through the hydrolysis-polycondensation of triethoxysilylpropyl-4-methoxycinnamamide (TES4C) and triethoxysilylpropyl-2,4- dimethoxycinnamamide (TES24C), respectively. Optimization of the catalyst type (acid, base or self-catalysis) and solvent (ethanol) and monomer concentrations, led to a high yield (71-73%) preparation of the two nanospheres. The two spheres displayed good sun protection factor (SPF) and UVA protection factor (UVA-PF) when used in a gel based formulation. The labile and volatile fragrant citronellal could be effectively loaded into the PTES4C spheres at 35-48% (w/w) via the in situ hydrolysis-polycondensation reaction under self-catalysis conditions, and the obtained citronellal-loaded nanospheres demonstrated clear sustained controlled release of the citronella characteristics.
In quest of small-molecules as potent non-competitive inhibitors against influenza
Malbari, Khushboo,Saha, Priyanka,Chawla-Sarkar, Mamta,Dutta, Shanta,Rai, Swita,Joshi, Mamata,Kanyalkar, Meena
, (2021/07/19)
A series of scaffolds namely aurones, 3-indolinones, 4-quinolones and cinnamic acid-piperazine hybrids, was designed, synthesized and investigated in vitro against influenza A/H1N1pdm09 virus. Designed molecules adopted different binding mode i.e., in 430-cavity of neuraminidase, unlike sialic acid and oseltamivir in molecular docking studies. All molecules reduced the viral titer and exhibited non-cytotoxicity along with cryo-protective property towards MDCK cells. Molecules (Z)-2-(3′-Chloro-benzylidene)-1,2-dihydro-indol-3-one (2f), (Z)-2-(4′-Chloro-benzylidene)-1,2-dihydro-indol-3-one (2g) and 2-(2′-Methoxy-phenyl)-1H-quinolin-4-one (3a) were the most interesting molecules identified in this research, endowed with robust potencies showing low-nanomolar EC50 values of 4.0 nM, 6.7 nM and 4.9 nM, respectively, compared to reference competitive and non-competitive inhibitors: oseltamivir (EC50 = 12.7 nM) and quercetin (EC50 = 0.56 μM), respectively. Besides, 2f, 2g and 3a exhibited good neuraminidase inhibitory activity in sub-micromolar range (IC50 = 0.52 μM, 3.5 μM, 1.3 μM respectively). Moreover, these molecules were determined as non-competitive inhibitors similar to reference non-competitive inhibitor quercetin unlike reference competitive inhibitor oseltamivir in kinetics studies.
Quorum sensing and nf-κb inhibition of synthetic coumaperine derivatives from piper nigrum
Baruch, Yifat,Gopas, Jacob,Kadosh, Yael,Kumar, Rajendran Saravana,Kushmaro, Ariel,Muthuraman, Subramani,Yaniv, Karin
, (2021/05/28)
Bacterial communication, termed Quorum Sensing (QS), is a promising target for virulence attenuation and the treatment of bacterial infections. Infections cause inflammation, a process regulated by a number of cellular factors, including the transcription Nuclear Factor kappa B (NF-κB); this factor is found to be upregulated in many inflammatory diseases, including those induced by bacterial infection. In this study, we tested 32 synthetic derivatives of coumaperine (CP), a known natural compound found in pepper (Piper nigrum), for Quorum Sensing Inhibition (QSI) and NF-κB inhibitory activities. Of the compounds tested, seven were found to have high QSI activity, three inhibited bacterial growth and five inhibited NF-κB. In addition, some of the CP compounds were active in more than one test. For example, compounds CP-286, CP-215 and CP-158 were not cytotoxic, inhibited NF-κB activation and QS but did not show antibacterial activity. CP-154 inhibited QS, decreased NF-κB activation and inhibited bacterial growth. Our results indicate that these synthetic molecules may provide a basis for further development of novel therapeutic agents against bacterial infections.
