Inhibition of nitric oxide biosynthesis by anthocyanin fraction of blackberry extract.

Anthocyanins are natural colorant belonging to the flavonoid family, widely distributed among flowers, fruits, and vegetables. Some flavonoids have been found to possess anticarcinogenic, cytotoxic, cytostatic, antioxidant, and anti-inflammatory properties. Since increased nitric oxide (NO) plays a role in inflammation, we have investigated whether the pharmacological activity of the anthocyanin fraction of a blackberry extract (cyanidin-3-O-glucoside representing about 88% of the total anthocyanin content) was due to the suppression of NO synthesis. The markedly increased production of nitrites by stimulation of J774 cells with lipopolysaccharide (LPS) for 24 h was concentration-dependently inhibited by the anthocyanin fraction (11, 22, 45, and 90 μg/ml) of the extract. Moreover, this inhibition was dependent on a dual mechanism, since the extract attenuated iNOS protein expression and decreased the iNOS activity in lungs from LPS-stimulated rats. Inhibition of iNOS protein expression appeared to be at the transcriptional level, since the extract and similarly cyanidin-3-O-glucoside (10, 20, 40, and 80 μg/ml, amounts corresponding to the concentrations present in the extract) decreased LPS-induced NF-κB activation, through inhibition of IκBα degradation, and reduced ERK-1/2 phosphorylation in a concentration-dependent manner. In conclusion, our study demonstrates that at least some part of the anti-inflammatory activity of blackberry extract is due to the suppression of NO production by cyanidin-3-O-glucoside, which is the main anthocyanin present in the extract. The mechanism of this inhibition seems to be due to an action on the expression/activity of the enzyme. In particular, the protein expression was inhibited through the attenuation of NF-κB and/or MAPK activatio

On the exhaustive generation of convex permutominoes

A permutomino of size n is a polyomino determined by a pair of permutations of size n+1, such that they differ in each position. In this paper, after recalling some enumerative results about permutominoes, we give a first algorithm for the exhaustive generation of a particular class of permutominoes, the convex permutominoes, proving that its cost is proportional to the number of generated objects.Comment: 15 pages, 14 figure

Studi Bibliometri Media Komunikasi Ilmiah Berkala Ilmu Perpustakaan dan Informasi

Kajian ini bertujuan untuk mengetahui pola kepenulisan artikel dan usia literatur Berkala Ilmu Perpustakaan dan Informasi (BIPI) periode 2003-2015. Kajian ini juga merupakan kajian kuantitatif deskriptif, dengan sumber data BIPI 2003-2015, dan objek kajiannya meliputi: artikel, penulis, literatur, dan tahun penerbitan literatur. Dalam Penganalisisan digunakan metode kuantitatif deskriptif. Hasilnya menunjukkan bahwa periode 2003-2015 telah diterbitkan 23 nomer, yang memuat 99 artikel. Penulis yang terlibat sebanyak 108 penulis, terdiri dari 55 penulis perempuan dan 53 penulis laki-laki. Menurut asalnya ada 56 penulis eksternal, dan 52 penulis internal. Meskipun demikian jumlah artikel karya penulis internal lebih tinggi yaitu sebesar 51 artikel, dan artikel karya penulis eksternal sebanyak 48 artikel. Tingkat kolaborasi 0,39 menunjukkan sebagian besar artikel ditulis secara individual (non-kolaborasi). Menurut jenis kolaborasi, kolaborasi dosen-mahasiswa menduduki peringkat tertinggi. Literatur pendukung artikel sebanyak 1.830 literatur, dan jenis buku teks menempati posisi tertinggi (62,02%). Sekitar 60% lebih, usia literatur berkisar antara 0-10 tahun

Structural optimization and biological evaluation of 2-substituted 5-hydroxyindole-3-carboxylates as potent inhibitors of human 5-lipoxygenase.

Pharmacological suppression of leukotriene biosynthesis by inhibitors of 5-lipoxygenase (5-LO) is a strategy to intervene with inflammatory and allergic disorders. We recently presented 2-amino-5-hydroxy-1H-indoles as efficient 5-LO inhibitors in cell-based and cell-free assays. Structural optimization led to novel benzo[g]indole-3-carboxylates exemplified by ethyl 2-(3-chlorobenzyl)-5- hydroxy-1H-benzo[g]indole-3-carboxylate (compound 11a), which inhibits 5-LO activity in human neutrophils and recombinant human 5-LO with IC50 values of 0.23 and 0.086 μM, respectively. Notably, 11a efficiently blocks 5-LO product formation in human whole blood assays (IC50 = 0.83-1.6 μM) and significantly prevented leukotriene B4 production in pleural exudates of carrageenan-treated rats, associated with reduced severity of pleurisy. Together, on the basis of their high potency against 5-LO and the marked efficacy in biological systems, these novel and straightforward benzo[g]indole-3-carboxylates may have potential as anti-inflammatory therapeutics