Benzophenone (BP) UV-filters have been extensively used for the prevention of UV-induced adverse effects in personal care products. Their potential to interfere with steroidogenesis in the female reproductive system remains uncertain. 17β-Hydroxysteroid dehydrogenase 1 (17β-HSD1) facilitates the conversion of estrone to estradiol, playing a key role in estrogen activation. This study delves into the effects of eleven BPs on human and rat 17β-HSD1, while also analysing the 3D-quntitative structure-activity relationship (3D-QSAR) and the underlying mechanisms. The inhibitory potency of inhibiting human placental 17β-HSD1 was found to be in the order of BP-2 (IC₅₀, 11.42 μM) > BP-1 (14.17 μM) > BP-4 (49.05 μM) > BP-6 (63.49 μM) = BP-8 (63.46 μM) > others. BP-1 and BP-2 markedly inhibited estradiol secretion by human placental BeWo cells at ≥ 1 μM. In contrast, the inhibitory strength of suppressing rat ovarian 17β-HSD1 activity was found to be in the order of BP-2 (IC₅₀, 13.33 μM) > BP-1 (15.09 μM) > BP-4 (22.68 μM) > BP-12 (31.12 μM) > BP-3 (97.11 μM) > BP (119.99 μM) > others. Mode action analysis revealed that these BP compounds acted as mixed inhibitors of both human and rat 17β-HSD1. The introduction of a 4-hydroxyl substitution in the benzene ring was found to markedly increase the inhibitory potency against human and rat 17β-HSD1. BP-1 and BP-2 demonstrated the ability to penetrate human BeWo cells and inhibit estradiol secretion at ≥ 1 μM. Docking analysis revealed that the 2-hydroxyl group of BP-1 and BP-2 forms a hydrogen bond with catalytic residue Ser142 of human 17β-HSD1. 3D-QSAR pharmacophore analysis showed that there are hydrophobic regions and hydrogen bond donor can interact with BPs. In conclusion, this study establishes that BP-2 is the most potent inhibitors of human 17β-HSD1 among the BPs under investigation, highlighting a significant difference in the structure-activity relationship.

01 Dec 2022·Marine Pollution Bulletin

The significance of trophic transfer of microplastics in the accumulation of plastic additives in fish: An experimental study using brominated flame retardants and UV stabilizers

Article

Author: Mizukawa, Kaoruko ; Takada, Hideshige ; Sekioka, Tomonori ; Hasegawa, Takaaki ; Yeo, Bee Geok ; Nakaoka, Masahiro

Marine organisms ingest microplastics directly from water and indirectly from food sources. Ingesting microplastics can lead to the accumulation of plastic-derived chemicals. However, the relative contributions of the two exposure routes to the accumulation of plastic-derived chemicals in organisms are unknown. Using microplastics containing two brominated flame retardants (BFRs; BDE209 and DBDPE) and three UV stabilizers (UVSs; UV-234, UV-327, and BP-12), we performed exposure experiments to compare chemical accumulation patterns in fish (Myoxocephalus brandti) between exposure from water and prey (Neomysis spp.). We found significantly higher concentrations of BFRs in fish fed microplastic-contaminated prey than fish exposed to microplastics in the water. However, we observed similar concentrations of UVSs in fish exposed to both sources. As BFRs are more hydrophobic than UVSs, the differences may reflect the hydrophobic nature of the additives. Our findings indicate that both exposure routes are crucial to understanding the accumulation of plastic additives in fish.

01 Jan 2017·Journal of Materials Science: Materials in Medicine

An easy-to-use wound dressing gelatin-bioactive nanoparticle gel and its preliminary in vivo study

Article

Author: Zhu, Feiyan ; Ren, Huihui ; Li, Ailing ; Xie, Yue ; Cui, Yang ; Wang, Chen ; Ji, Lijun ; Yang, Zhenzhong ; Qu, Xiaozhong ; Qiu, Dong

Beyond promoting hard tissue repairing, bioactive glasses (BGs) have also been proved to be beneficial for wound healing. Nano-scale BGs prepared by sol-gel method were found to have a better performance as they have a larger specific surface area. In this work, bioactive nanoparticles (nBPs) with mean diameter of 12 nm (BP-12) instead of conventional BGs were mixed with gelatin to form an easy-to-use hydrogel as a dressing for skin wound. It was found that the composite of BP-12 and gelatin could form a hydrogel (BP-12/Gel) under 25 °C, which showed pronounced thixotropy at a practically accessible shear rate, therefore become easy to be used for wound cover. In vitro, the composite hydrogel of BP-12 and gelatin had good biocompatibility with the fibroblast cells. In vivo, rapid cutaneous-tissue regeneration and tissue-structure formation within 7 days was observed in the wound-healing experiment performed in rats. This hydrogel is thus a promising easy-to-use wound dressing material.

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