Three new scalarane-based sesterterpenes, 1- 3, were isolated from a marine sponge of the genus Spongia, and their chemical structures were elucidated by analysis of HRMS and 2-D NMR spectra. The isolated compounds 1 and 3 showed inhibition against the farnesoid X-activated receptor (FXR) with IC50 values of 2.4 and 24 microM, respectively. In particular, compound 3 directly inhibited the interaction between FXR and a coactivator peptide (SRC-1) as determined by surface plasmon resonance (SPR) spectroscopy.

We have identified and characterized a new amphibian orphan member of the nuclear receptor superfamily and termed it FOR1 (farnesoid X receptor (FXR)-like Orphan Receptor) because it shares the highest amino acid identity with the mammalian FXR. We also identi- The nuclear receptor superfamily comprises a large group of structurally related ligand-dependent transcription factors regulated by a variety of steroid and non-steroid hormones. It also includes a large number of related proteins that do not have known ligands, referred to as orphan nuclear receptors (reviewed in Refs. 1-3). The nuclear receptors modulate target gene transcription by direct binding to specific DNA sequences, called hormone response elements (HRE), 1 which are generally located in the promoter of the specific target genes. In general, both classic nuclear hormone receptors and orphan nuclear hormone receptors consist of four or five different modules or domains; A/B, C, D, E, and F (1). The non-conserved N-terminal region of nuclear receptors (A/B domain) is involved in transactivation in some cases but is of unknown function or is absent in others. The DNA-binding C-domain (DBD) shows the strongest sequence similarity among different nuclear receptors and is engaged in the binding of these receptors to cognate HREs. The C-domain consists of 65-68 amino acids, among which 8 cysteine residues are absolutely conserved and form two zincbinding modules (1, 3, 4). The D-domain, called the hinge region, shows relatively low sequence similarity and contains sequences involved in HRE binding at its N terminus. The E-domain directly binds to ligands or hormones and is also involved in nuclear localization and receptor dimerization. The C terminus of the LBD contains a conserved motif that, together with other portions of the LBD, forms the binding site for transcriptional coactivators (1). The F-domain is an additional C-terminal extension found in only subset of receptors. The function of this non-conserved segment is unclear.A large number of orphan nuclear receptor genes have been discovered by several different approaches. These include 1) screening cDNA libraries with conventional receptor cDNA probes at relaxed stringency (5) or with degenerate oligonucleotides based on the conserved regions (6), 2) performing PCR with degenerate oligonucleotide PCR primers from the DBD (7, 8), 3) screening cDNA libraries using nuclear receptor ligand binding domains (LBD) or receptor interaction domains of coactivators as bait in a yeast two-hybrid system (9, 10).

The nasal tip lifting maneuver helped to guide preformed nasal RAE tubes into the lower pathway during nasotracheal intubation.

A new inhibitor, placotylene A (1), of the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclast differentiation, and a regioisomer of placotylene A, placotylene B (2), were isolated from a Korean marine sponge Placospongia sp. The chemical structures of placotylenes A and B were elucidated on the basis of 1D and 2D NMR, along with MS spectral analysis and revealed as an iodinated polyacetylene class of natural products. Placotylene A (1) displayed inhibitory activity against RANKL-induced osteoclast differentiation at 10 μM while placotylene B (2) did not show any significant activity up to 100 μM, respectively.

Objectives/Hypothesis To compare effect of 1 and 2 mg/kg of sugammadex on the incidence of intraoperative bucking and intraoperative neuromonitoring (IONM) quality in thyroid surgery. Study Design Randomized controlled trial. Methods Patients qualified for thyroid surgery with IONM were eligible for this double‐blind, randomized, controlled trial. After tracheal intubation with 0.6 mg/kg rocuronium, 1 or 2 mg/kg of sugammadex was administered to patients in group I or II, respectively. The quality of the IONM for the external branch of the superior laryngeal nerve (EBSLN) was evaluated (strong/intermediate/weak). The initial amplitude of electromyography for the vagus nerve (V1) and the recurrent laryngeal nerve (R1) were recorded. Intraoperative bucking movements was recorded. Results A total of 102 patients (51 in each group) completed the study. Time from sugammadex administration to initial checking for the EBSLN was not different between group I and II (25.0 ± 7.9 vs. 25.5 ± 9.0 minutes, P = .788). There was no difference in the neuromonitoring quality for the EBSLN between group I and II (strong/intermediate/weak: 46/5/0 vs. 50/1/0, P = .205). The amplitudes of V1 (1,086.3 ± 673.3 μV vs. 1,161.8 ± 727.5 μV, P = .588) and R1 (1,328.2 ± 934.1 μV vs. 1,410.5 ± 919.6 μV, P = .655) were comparable between the groups. Patients who experienced bucking were significantly fewer in the group I than the group II (13.7% vs. 35.3%, P = .020). Conclusion A dose of 1 mg/kg sugammadex induced less bucking than 2 m/kg while providing comparable IONM quality during thyroid surgery. Level of Evidence 2 Laryngoscope, 131:2154–2159, 2021

Two new benzophenones, acredinones A (1) and B (2), were isolated from a marine-sponge-associated Acremonium sp. fungus. Their chemical structures were elucidated on the interpretation of spectroscopic data. The structure of 1 was confirmed by palladium-catalyzed hydrogenation, followed by spectroscopic data analysis. Acredinones A (1) and B (2) inhibited the outward K(+) currents of the insulin secreting cell line INS-1 with IC50 values of 0.59 and 1.0 μM, respectively.

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