Inhibition of SARS-CoV-2 Virus Entry by the Crude Polysaccharides of Seaweeds and Abalone Viscera In Vitro.

Much attention is being devoted to the potential of marine sulfated polysaccharides as antiviral agents in preventing COVID-19. In this study, sulfated fucoidan and crude polysaccharides, extracted from six seaweed species (Undaria pinnatifida sporophyll, Laminaria japonica, Hizikia fusiforme, Sargassum horneri, Codium fragile, Porphyra tenera) and Haliotis discus hannai (abalone viscera), were screened for their inhibitory activity against SARS-CoV-2 virus entry. Most of them showed significant antiviral activities at an IC50 of 12~289 µg/mL against SARS-CoV-2 pseudovirus in HEK293/ACE2, except for P. tenera (IC50 > 1000 µg/mL). The crude polysaccharide of S. horneri showed the strongest antiviral activity, with an IC50 of 12 µg/mL, to prevent COVID-19 entry, and abalone viscera and H. fusiforme could also inhibit SARS-CoV-2 infection with an IC50 of 33 µg/mL and 47 µg/mL, respectively. The common properties of these crude polysaccharides, which have strong antiviral activity, are high molecular weight (>800 kDa), high total carbohydrate (62.7~99.1%), high fucose content (37.3~66.2%), and highly branched polysaccharides. These results indicated that the crude polysaccharides from seaweeds and abalone viscera can effectively inhibit SARS-CoV-2 entry.

Screening of Human CYP1A2 and CYP3A4 Inhibitors from Seaweed In Silico and In Vitro.

Phenolic compounds and carotenoids are potential inhibitors of cytochrome P450s. Sixteen known compounds, phenolic compounds and carotenoids from seaweed were examined for potential inhibitory capacity against CYP1A2 and CYP3A4 in silico and in vitro. Morin, quercetin, and fucoxanthin inhibited the enzyme activity of CYP1A2 and CYP3A4 in a dose-dependent manner. The IC50 values of morin, quercetin, and fucoxanthin were 41.8, 22.5, and 30.3 µM for CYP1A2 and 86.6, 16.1, and 24.4 µM for CYP3A4, respectively. Siphonaxanthin and hesperidin did not show any significant effect on CYP1A2, but they slightly inhibited CYP3A4 activity at high concentrations. In silico modeling of CYP's binding site revealed that the potential inhibitors bound in the cavity located above the distal surface of the heme prosthetic group through the 2a or 2f channel of CYPs. This study presents an approach for quickly predicting CYP inhibitory activity and shows the potential interactions of compounds and CYPs through in silico modeling.

Sex Differences in Pedobarographic Findings and Relationship between Radiographic and Pedobarographic Measurements in Young Healthy Adults.

BACKGROUND: Although pedobarographic measurement is increasingly used for clinical and research purposes, relatively few published studies have investigated normative data. This study examined pedobarographic findings in young healthy adults with regard to sex-related differences and correlations among measurement indices. METHODS: Twenty young healthy adults (mean age, 22.4 years; standard deviation, 1.2 years; and 10 males and 10 females) were included. Weight bearing anteroposterior (AP) and lateral foot radiographs were taken, and dynamic pedobarographic data during treadmill walking and maximum ankle dorsiflexion were obtained. AP talo-first metatarsal angle, naviculocuboid overlap, lateral talo-first metatarsal angle, and plantar soft tissue thickness were measured on foot radiographs. Pedobarographic data including peak pressure and pressure-time integral were measured on five plantar segments: medial forefoot (MFF), lateral forefoot (LFF), medial midfoot (MMF), lateral midfoot (LMF), and heel. RESULTS: Male and female subjects significantly differed in body mass index (BMI, p < 0.001), AP talo-first metatarsal angle (p = 0.018), soft tissue thickness under the metatarsal head (p = 0.040) and calcaneal tuberosity (p < 0.001), maximum dorsiflexion during stance phase (p = 0.041), peak pressure on the MFF (p = 0.005) and LFF (p = 0.004), and pressure-time integral on the MFF (p = 0.018) and heel (p = 0.001). BMI was significantly correlated with soft tissue thickness under the metatarsal head (r = 0.521, p = 0.018) and calcaneal tuberosity (r = 0.585, p = 0.007), peak pressure on the MFF (r = 0.601, p = 0.005) and LFF (r = 0.487, p = 0.029), pressure-time integral on the heel (r = 0.552, p = 0.012), and total pressure-time integral (r = 0.755, p < 0.001). Maximum dorsiflexion demonstrated significant negative correlations with pressure-time integral on the MFF (r = -0.595, p = 0.007) and total pressure-time integral (r = -0.492, p = 0.032). Pressure-time integral varus/valgus index was significantly correlated with pressuretime integral forefoot/heel index (r = 0.472, p = 0.036). CONCLUSIONS: Sex-related differences in pedobarographic examination were observed, which could provide useful information in setting appropriate treatment goals and obtaining appropriate control data. The effects of subtalar motion in distributing plantar pressure should be investigated in a future study.