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Background: Very few papers covering the anticancer activity of azulenes have been reported, as compared with those of antibacterial and anti-inflammatory activity. This led us to investigate the antitumor potential of fifteen 4,6,8-trimethyl azulene amide derivatives against oral malignant cells. Methods: 4,6,8-Trimethyl azulene amide derivatives were newly synthesized. Anticancer activity was evaluated by tumor-specificity against four human oral squamous cell carcinoma (OSCC) cell lines over three normal oral cells. Neurotoxicity was evaluated by cytotoxicity against three neuronal cell lines over normal oral cells. Apoptosis induction was evaluated by Western blot and cell cycle analyses. Results: Among fifteen derivatives, compounds 7, 9, and 15 showed the highest anticancer activity, and relatively lower neurotoxicity than doxorubicin, 5-fluorouracil (5-FU), and melphalan. They induced the accumulation of a comparable amount of a subG1 population, but slightly lower extent of caspase activation, as compared with actinomycin D, used as an apoptosis inducer. The quantitative structure–activity relationship analysis suggests the significant correlation of tumor-specificity with a 3D shape of molecules, and possible involvement of inflammation and hormone receptor response pathways. Conclusions: Compounds 7 and 15 can be potential candidates of a lead compound for developing novel anticancer drugs., Licensee MDPI, Basel, Switzerland.This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).

A high‐throughput, fully automated antigen detection test for SARS‐CoV‐2 is a viable alternative to reverse‐transcription polymerase chain reaction (RT‐qPCR) for mass screening during outbreaks. In this study, we compared RT‐qPCR for viral load and the VITROS® SARS‐CoV‐2 Antigen Test with reference to the results of the LUMIPULSE® SARS‐CoV‐2 Ag Test. Of 128 nasopharyngeal swab specimens taken from patients suspected of being infected with SARS‐CoV‐2, 49 were positive and 79 were negative according to RT‐qPCR. Consistent dose‐dependent detection with VITROS® assay was successfully achieved when using nasopharyngeal swab specimens with Ct values of 32.0 or lesser, whereas the CLEIA‐based LUMIPULSE® assay was able to detect lower viral loads compared with the VITROS® assay. Our results show that the performance of the VITROS® assay was satisfactory for the diagnosis of contagious COVID‐19 patients in the clinical setting. Highlights The performance of the VITROS® SARS‐CoV‐2 Antigen Test was sufficient for the diagnosis of contagious COVID‐19. This test showed high sensitivity and specificity in the detection of SARS‐CoV‐2 in samples with a Ct value of 32 or less.

Several automated high-throughput immunoassays for detecting anti-SARS-CoV-2 antibodies by a semi-quantitative approach have been commercialized. In this study, we describe the timeline of the antibody response in patients with RT-PCR-confirmed COVID-19. A total of 292 sequential serum samples from 33 Japanese patients were retrospectively analyzed using four test kits for SARS-CoV-2: the Abbott SARS-CoV-2 IgG assay (Abbott), Elecsys® Anti-SARS-CoV-2 assay (Roche Diagnostic), and VITROS® Anti-SARS-CoV-2 Total and IgG assays (Ortho Clinical Diagnostics). All automated immunoassays could equivalently identify positive sera collected within 2 weeks after symptom onset (99.3%-100%). In addition, the S protein-based automated immunoassay, the VITROS® Anti-SARS-CoV-2 Total assay, may play a complementary role in evaluating passive antibody therapies or vaccines against SARS-CoV-2, although further research is required.