Impact of the state of emergency enacted due to the COVID-19 pandemic on the physical activity of the elderly in Japan.

[Purpose] In Japan, the government issued a state of emergency due to the spread of COVID-19 in April 2020. In this study, we measured physical activity before and after the state of emergency, and assessed the factors that affected physical activity. [Participants and Methods] We included thirteen elderly people living in Hiroshima Prefecture, Japan, in the study. The participants wore 3-axis accelerometer on their hips to measure physical activity for a week, before (in October 2019) and after the state of emergency. According to the median rate of decrease in physical activity (23.6%), we divided the participants into two groups: one group had participants with a high rate of decrease (low physical activity) and the other had participants with a low rate of decrease (high physical activity). [Results] The following factors decreased after the state of emergency: total physical activity, amount of moderate-intensity physical activity and activities of daily living, amount of light-intensity physical activity and walking, daily activity time, and daily steps. Statistical analysis showed that engaging in housework was associated with high physical activity. [Conclusion] Elderly people who engaged in household chores had a smaller decrease in physical activity. In order to reduce the decrease in physical activity and the risk of cardiovascular events, the elderly should perform as many daily activities and hobbies as they can while paying attention to the infection control measures.

CJ-15,208, a novel kappa opioid receptor antagonist from a fungus, Ctenomyces serratus ATCC15502.

A novel kappa opioid receptor binding inhibitor CJ-15,208 (I) was isolated from the fermentation broth of a fungus, Ctenomyces serratus ATCC15502. The structure of I was determined to be a cyclic tetrapeptide consisting of one tryptophan, one D-proline, and two L-phenylalanine. Compound I was a selective binding inhibitor for the kappa opioid receptor: 47 nM (IC50) for kappa, 260 nM for mu, and 2,600 nM for delta. In the electrically-stimulated twitch response assay of rabbit vas deferens I recovered the suppression by a kappa agonist asimadoline with an ED50 of 1.3 microM, indicating that it is a kappa antagonist.

Thielavins as glucose-6-phosphatase (G6Pase) inhibitors: producing strain, fermentation, isolation, structural elucidation and biological activities.

High-throughput screening of microbial extracts using rat hepatic microsomal glucose-6-phosphatase (G6Pase) led us to find thielavin B as a G6Pase inhibitor with inhibition of glucose output from glucagon-stimulated hepatocytes. Further searching for more potent analogs identified 11 new thielavins F-P in addition to the known thielavins A and B from a fungus Chaetomium carinthiacum ATCC 46463. Thielavin G showed the strongest activity as a G6Pase inhibitor (IC50=0.33 microM), while the IC50 of thielavin B was 5.5 microM. According to the structure-activity relationship, including authentic thielavins C, D and 3 partial hydrolysates from thielavins A and B, 3 benzoic acid-units and carboxylic acid functions are essential for G6Pase inhibition.

CJ-15,696 and its analogs, new furopyridine antibiotics from the fungus Cladobotryum varium: fermentation, isolation, structural elucidation, biotransformation and antibacterial activities.

CJ-15,696 and 7 novel furopyridine antibiotics were isolated from the fungus Cladobotryum varium CL12284. Their structures were determined by X-ray crystallography and spectral analysis. Three biotransformed analogs were also prepared from CJ-15,696. CJ-15,696 showed moderate activity against various Gram-positive bacteria including some drug resistant strains such as methicillin resistant Staphylococcus aureus (MRSA).