Human microsomal prostaglandin E synthase-1 (mPGES-1) is an emerging drug target for inflammatory disorders and cancer suppression. Therefore, it is crucially important to discover mPGES-1 inhibitors with novel structural scaffolds for the development of anti-inflammatory drugs. Here, we report the mPGES-1 inhibitors identified through screening of a chemical library. Initial screening of 1841 compounds out of 200,000 in a master library resulted in 9 primary hits. From the master library, 387 compounds that share the scaffold structure with the 9 primary hit compounds were selected, of which 3 compounds showed strong inhibitory activity against mPGES-1 having IC(50) values of 1-3 μM. Notably, a derivative of sulfonylhydrazide, compound 3b, inhibited the LPS-induced PGE(2) production in RAW 264.7 cells. This compound showed novel scaffold structure compared to the known inhibitors of mPGES-1, suggesting that it could be further developed as a potent mPGES-1 inhibitor.

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BackgroundThe current study evaluated the hemodynamic effects of different types of pneumatic compressions of the lower extremities during anesthesia induction. In addition, the hemodynamic effects were compared between patients older than 65 age years and those aged 65 years or younger.MethodsOne hundred and eighty patients (90: > 65 years and 90: ≤ 65 years) were enrolled. Each age group of patients was randomly assigned to one of three groups; Group 1 (no compression), Group 2 (sequential pneumatic compression), and Group 3 (sustained pneumatic compression without decompression). Invasive blood pressure, cardiac index (CI), and stroke volume variation (SVV) were measured.ResultsIn patients aged ≤ 65 years, mean arterial pressure (MAP) and CI were significantly higher and SVV was lower in Group 3 compared to Group 1 before tracheal intubation, but there were no differences between Groups 1 and 2. However, there were no differences in MAP, CI, and SVV among the three groups in patients aged > 65 years. The number of patients who showed a MAP < 60 mmHg was less in Group 3 than Group 1 in patients aged ≤ 65 years, but not in patients aged > 65 years.ConclusionsSustained pneumatic compression of the lower extremities has more hemodynamic stabilizing effects compared to sequential compression during anesthesia induction in patients aged 65 years or younger. However, no difference between methods of compression was observed in patients older than 65 years.

Injection at the wrong level leads to unwanted effects or no effect for the patients. Many pain physicians use fluoroscopy to identify the segments of the lumbar vertebrae, but it may cause confusion if the lumbar spine has anatomical deformities such as lumbarization or sacralization [1]. Thus, the fifth lumbar vertebra may be fused with the sacrum, or the sacrum may be separated to form the sixth lumbar vertebra.In these circumstances, many clinicians designate the L1 vertebra based upon the location of the 12th rib. The lowest rib attached costal facets would be identified as T12, and the vertebra beneath T12 identified as the first lumbar vertebra. Jagannathan et al. [2] stated that the costal facets are reliable markers for T12 identification, and the lumbar segment can be fairly accurately identified in both the normal and the lumbarization groups. However, this method has a drawback, because up to 8% of normal children have only 11 pairs of ribs [3]. Here, we report a series of cases of interventional procedures on the wrong lumbar segment in patients whose 12th pair of ribs was absent.