Evaluation of 3-(3-chloro-phenyl)-5-(4-pyridyl)-4,5-dihydroisoxazole as a Novel Anti-Inflammatory Drug Candidate

BACKGROUND: 3-(3-chloro-phenyl)-5-(4-pyridyl)-4,5-dihydroisoxazole (DIC) is a five-membered heterocyclic compound containing a N-O bond. The anti-inflammatory effects of this compound were studied both in vitro and in vivo. PRINCIPAL FINDINGS: DIC effectively decreased TNF-α and IL-6 release from LPS-stimulated macrophages in a dose dependent manner. DIC diminished the levels of COX-2 with subsequent inhibition of PGE(2) production. DIC also compromised HMGB1 translocation from the nucleus to the cytoplasm. Moreover, DIC prevented the nuclear translocation of NF-κB and inhibited the MAPK pathway. In vivo, DIC inhibited migration of neutrophils to the peritoneal cavity of mice. CONCLUSIONS: This study presents the potential utilization of a synthetic compound, as a lead for the development of novel anti-inflammatory drugs

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Not AvailableThis aim of this study was to assess the relationship, if any, of scrotal surface temperature gradient (SSTG), scrotal circumference (SC) and testicular covering thickness (TCT) with semen quality in Murrah buffalo breeding bulls. For this, buffalo breeding bulls (n = 130) were selected from four different semen centres. The ejaculates of each bull were evaluated for ejaculate volume (EV), mass motility (MM); concentration (SPC), motility (SM), viability and abnormalities (SA). The SSTG, SC and TCT of individual bulls were quantified using digital infrared thermography, measuring tape and ultrasonography, respectively. The bulls were divided into three groups on the basis of SSTG (≤ 4 °C, 4.1 to 6.4 °C and ≥ 6.5 °C), and SC (< 31, 31 to 35 and > 35 cm) and into two groups on the basis of TCT (5 to 7.2 and 7.4 to 10.4 mm). Results indicated the bulls with a larger temperature gradient and larger SC produced greater quality semen than those with a lesser temperature gradient. The MM (P < 0.01) and SPC (P < 0.05) varied among the groups along with SSTG. Among the SC groups the EV, MM, SPC and SM (P < 0.01), and viability (P < 0.05) varied as did the SC. The bulls with a lesser TCT had a lesser SA (P < 0.05) as compared to the group with the greater TCT. Buffalo bulls having a greater SSTG, SC and lesser TCT produced semen of greater quality and these variables may be used as criteria for breeding soundness evaluationNot Availabl

Design and development of hydrogel beads for targeted drug delivery to the colon

The purpose of this research was to develop and evaluate a multiparticulate system of chitosan hydrogel beads exploiting pH-sensitive property and specific biodegradability for colon-targeted delivery of satranidazole. Chitosan hydrogel beads were prepared by the cross-linking method followed by enteric coating with Eudragit S100. All formulations were evaluated for particle size, encapsulation efficiency, swellability, and in vitro drug release. The size of the beads was found to range from 1.04±0.82 mm to 1.95±0.05 mm. The amount of the drug released after 24 hours from the formulation was found to be 97.67%±1.25% in the presence of extracellular enzymes as compared with 64.71%±1.91% and 96.52%±1.81% release of drug after 3 and 6 days of enzyme induction, respectively, in the presence of 4% cecal content. Degradation of the chitosan hydrogel beads in the presence of extracellular enzymes as compared with rat cecal and colonic enzymes indicates the potential of this multiparticulate system to serve as a carrier to deliver macromolecules specifically to the colon and can be offered as a substitute in vitro system for performing degradation studies. Studies demonstrated that orally administered chitosan hydrogel beads can be used effectively for the delivery of drug to the colon