In nature, photosynthetic organisms such as cyanobacteria efficiently capture, transfer, and utilize solar energy in aqueous environments. However, replicating these processes in artificial supramolecular systems to achieve effective light harvesting and photocatalysis in water remains highly challenging. Here, we report a supramolecular light-harvesting system (LHS) constructed from a water-soluble dicarboxylate pillar[5]arene (H2), a triphenylacrylonitrile derivative (TPAN), and the acceptor dye 4,7-di(2-thienyl)benzo[2,1,3]thiadiazole (DBT). Structural optimization of the host enhanced the emission of the H2-TPAN supra-amphiphile by 2.5-fold compared with its fully carboxylated analogue (H1). The resulting ternary LHS exhibited excellent performance, enabling efficient generation of both singlet oxygen (1O2) and superoxide anion radical (O2•-). These reactive oxygen species (ROS) synergistically promoted metal-free oxidative amidation in water, affording methacetin and related derivatives in yields of up to 95%. This work demonstrates how rational supramolecular design can integrate fluorescence amplification, light harvesting, and dual-ROS generation into a single platform for efficient photocatalysis in aqueous media.

The level of phosphodiesterase type 2 (PDE2) in the body is closely associated with human health. From the L6000 natural compound library, the natural coumarin compound coumestrol was identified as possessing PDE2 inhibitory activity. Using computer-aided drug design software, we modified and synthesized coumestrol derivatives and subsequently evaluated their PDE2 inhibitory activity. Among the synthesized compounds, B2-1 exhibited the strongest activity, with an IC₅₀ value of 1.09 ± 0.07 μM, approximately 7 times higher than that of coumestrol. Finally, ADMET prediction of coumestrol and B2-1 found that B2-1’s ability is equal to or better than coumestrol in terms of intestinal absorption, hepatotoxicity, protein binding, and so on.

Artificial systems that efficiently utilize light offer a viable approach for photocatalytic oxidation under mild conditions. Herein, the photocatalytic performance of a tetraphenylethylene-based supramolecular system is investigated. The assembled system (TPEC/CTAB-ESY-SR101) enables multiple oxidation reactions with high efficiency. Aryl sulfides are selectively converted to sulfoxides in up to 99% yield via singlet oxygen (1O2), while phenylboronic acids are oxidized to phenols in up to 90% yield, predominantly mediated by superoxide radicals (O2 center dot-). In addition, lignin photodegradation is significantly enhanced from 35% for TPEC alone to 82% in the assembled system. This work demonstrates a versatile supramolecular platform that integrates efficient reactive oxygen species generation with diverse photocatalytic oxidation reactions, providing a practical strategy for solar-driven oxidation chemistry.

Phosphodiesterase-2A (PDE2A) is a potential therapeutic target for the treatment of ganglion dysfunction-related diseases such as Alzheimer's disease, schizophrenia, cognitive impairment, anxiety, and depression. However, most current PDE2A inhibitors have moderate selectivity compared to other PDEs. In this study, we described the discovery of 6 novel PDE2A inhibitors by bioassays, molecular docking, and molecular dynamics simulations. Six molecules out of 2592 compounds from the L6000-Natural Compound Library inhibited PDE2A with affinity ranging from 4.03 to 39.84 μM. Selective experiments were carried out on PDE4D, PDE5A, PDE9A, and PDE10A, among which 5-5H and 16-2H exhibited good dual inhibition against both PDE2A and PDE4D. Their IC50 values for PDE2A were 4.03 and 9.08 μM, respectively, and for PDE4D they were 3.89 and 10.96 μM, respectively. Molecular docking and molecular dynamics simulation were used to explore the binding modes of active compounds with PDE2A. It is shown that in addition to the common interactions with Gln859 and Phe862 of PDE2A, 6 molecules formed extra hydrogen bonds with Ile826 and Leu809. These molecules may serve as starting points for further optimization of selective PDE2A inhibitors.

Urolithin A (UA) is a dibenzo[b,d]pyran-6-one polyhydroxy derivative produced as intestinal microbe metabolize ellagitannin and ellagic acid. Because of its superior anti-inflammatory and antioxidant effects, it can cure neuronal damage in a variety of ways and play a neuroprotective role. More and more research has revealed that UA is a potential medicine for the treatment of neurodegenerative diseases. Due to UA source limitations, it is insufficient to achieve disease treatment concentrations, and the activity of UA inhibiting PDE2 needs further enhancement. As a result, we used UA as the parent nucleus structure, independently designed and used Discovery Studio software to assist in the structural design and molecular docking screening of the compounds, and tested the in vitro enzyme activity of the synthesized compounds, hoping to obtain UA-based PDE2 inhibitors. The IC50 of 6-18, 6-19, 6-20, 6-22, and 6-29 were 0.62, 0.85, 1.51, 1.09, and 1.58 μM, respectively. In this study, UA derivatives that can bind to the crystal structure of PDE2 protein 4HTX were proposed, which laid a groundwork for further structural modification, lead design, and development of small molecule inhibitors with inhibitory activity of PDE2.

Urolithin A (UA) is a naturally occurring polyphenolic compound.Due to its remarkable efficacy in safeguarding the central nervous system, UA has emerged as a promising candidate for drug development targeting neurodegenerative diseases such as Alzheimer's. However, the source of UA is limited and the activity of UA to inhibit PDE2 needs to be further improved. Therefore, this study will be optimized on the basis of UA to seek PDE2 inhibitors with better activity. In this study, we designed a series of UA derivatives based on 4HTX as the target protein and UA as the lead compound, utilizing the binding crystal structures of 4HTX and BAY60-7550 as references. After thorough screening, we successfully identified the 8-hydroxyl group as the precise site of modification. Utilizing 2-bromo5-hydroxybenzoic acid as our primary raw material, we synthesized a series of the 8-hydroxyl modified UA. Subsequently, we evaluated the inhibitory activity of these synthesized UA derivatives using a phosphodiesterase assay kit. Ultimately, we screened a total of 34 derivatives; among them, compounds 1f, 1q, 2d, and 2j exhibited significant inhibitory activity against PDE2 with half-maximal inhibitory concentrations of 3.05 mu M, 0.67 mu M, 0.57 mu M, and 4.96 mu M, respectively.

Metal-free C(sp3)–S bond cleavage of thioethers was achieved using NCS as a critical additive. A wide range of arylmethyl thioethers were successfully transformed into aryl aldehydes with satisfactory yields in chloroform. Meanwhile, employing fluorobenzene as the solvent enables the selective formation of dithioacetals from arylmethyl thioethers, achieving moderate to good yields. Notably, dithioacetals were first prepared through a metal-free C(sp3)–S bond cleavage and subsequent thioacetalization process. Furthermore, these simple and efficient approaches also provide complementary strategies for accessing important aryl aldehydes and dithioacetals.

Urolithin A (UA), a dietary polyphenol metabolite, exhibits bioactivity across diverse domains, including antioxidant, anti-inflammatory, anticancer, muscle health improvement, and neuroprotective effects. Due to its prominent bioactivity in central nervous system protection, UA has emerged as a promising lead compound for developing therapeutic agents against neurodegenerative disorders. However, limitations such as poor activity, low bioavailability, and instability necessitate targeted structural modifications. In this study, guided by relevant literature, UA was utilized as the core scaffold. Structural modifications involved replacing the 8-hydroxy group with an amino group and etherifying the 3-hydroxy group. Discovery Studio software was employed for compound design and molecular docking screening. Subsequently, the target compounds were synthesized and subjected to in vitro enzymatic activity assays. Our group designed 35 compounds and synthesized them using 2-bromo-5-aminobenzoic acid as the starting material. This yielded 35 intermediate compounds (3-hydroxyl-modified 8-amino-urolithin A series) and 35 final derivatives (3-hydroxyl-modified 8-amino-urolithin A series). The inhibitory activity of the synthesized products was evaluated using a Phosphodiesterase Assay Kit. Among the derivatives, compounds D24, D31, and E31 demonstrated significant inhibitory activity against PDE2, with half-maximal inhibitory concentration (IC₅₀) values of 0.31 μM, 0.018 μM, and 0.7 μM, respectively. Here, we report the design and synthesis of 3-hydroxyl-modified 8-amino-urolithin A derivatives and the biological evaluation of their activity against PDE2.

Deep mucosal and organ infections caused by the infestation of Candida albicans in immunocompromised patients represent a significant cause of mortality in hospitalized patients. The rise in fungal resistance is a consequence of the overuse of antibiotics. Therefore, innovative immunostimulants must be developed to combat pathogenic fungal infections. We used urolithin A (UA), an intestinal metabolite rich in the naturally occurring polyphenolic antioxidants ellagic acid (EA) or ellagitannin (ET), as a lead compound for structural modification. Through liquid screening of 17 synthesized compounds, we discovered compound 1e effectively inhibited C. albicans biofilm formation, thereby reducing its virulence. Furthermore, it protects animals from severe infections by enhancing tolerance to infection by intestinal pathogens and reducing oxidative stress. Moreover, our findings indicate that compound 1e exerts its effects through the p38 mitogen-activated protein kinase (MAPK) innate immune pathway, which is evolutionarily conserved. These observations not only enhance our comprehension of immune mechanisms but also provide a crucial foundation for the development of immune activators with the potential to resist pathogenic bacterial infections.

A selective C(sp3)-S bond cleavage of thioethers mediated by NBS is developed. Various alkyl bromides have been obtained in good yields using N-aryl-3-(methylthio)propanamides and arylmethylene alkylthioethers. Mechanistic studies suggest that the formation of 3-bromo-N-arylpropanamides may involve sulfoxide intermediates, while the arylmethylene bromides are formed through direct bromination process mediated by NBS. The significance of this strategy lies in its pioneering use of NBS for C-S bond cleavage and subsequent bromination reaction.

Inspired by natural photosynthetic systems that feature both sequential energy transfer and temperature response, we herein report an artificial thermosensitive sequential light-harvesting system (LHS) based on an amphiphilic molecule TPEO. It self-assembles into fluorescent nanoparticles in water and shows tunable LCST behavior. By loading ESY as the first acceptor and NiR as the second acceptor into the nanoparticles, an artificial LHS with two-step FRET was successfully constructed. Interestingly, the system exhibits thermosensitive colorimetric fluorescence in both aqueous solution and hydrogel by taking advantage of a combination of LCST and sequential FRET.

Urolithins are the gut microbiota metabolites of ellagitannins which are found in natural plants such as pomegranate, strawberry, and raspberry, and in nuts. Recently, several reports have clarified the underlying mechanism of urolithins in central nervous system inflammation. Therefore, urolithins have become potential therapeutic drug candidate molecules for central nervous system diseases. Derivatives 1–1d, 1–1f, 3–2a, and 3–2b of urolithin A, urolithin B, and methoxyurolithin A were found to have had significant inhibitory activity against phosphodiesterase II with IC50 values of 35.42, 39.96, 25.58, and 13.84 μM, respectively. Herein, we report the design and synthesis of urolithin derivatives along with a biological evaluation of their activity against phosphodiesterase II.

Coumarin and chalcone are two compounds that have been extensively studied for their neuroprotective effects. Coumarin is known for its ability to inhibit MAO activity in the brain and reduce central nervous system damage caused by dopamine degradation. Chalcone, on the other hand, has gained attention due to its potential medicinal value, including free radical scavenging, anti-inflammatory, and neuroprotective properties. Both compounds have shown promise in the development of treatments for neurodegenerative diseases like Alzheimer's disease. In this study, we designed and synthesized 36 coumarin-chalcone heteroderivatives based on the principle of structure hybridization. We then evaluated the inhibitory effects of these compounds on phosphodiesterase II (PDE2) at the enzyme level and analyzed their structure-activity relationship. Among the hybrid derivatives, compounds 2b, 3a, 3i, 3m, and 1l demonstrated significant inhibitory activity on PDE2, with IC50 values of 24.46 mu M, 16.82 mu M, 28.13 mu M, 21.88 mu M, and 29.72 mu M, respectively. This paper presents the design, synthesis, and biological evaluation of coumarin-chalcone hybrid derivatives for their potential as PDE2 inhibitors.

Aging is a natural process, but with the increase of people’s average life expectancy, aging has brought great economic pressure and social burden to many countries and regions. As urolithin B (UB) is a natural metabolite, it has shown positive effects in many disease studies, such as obesity, diabetes, osteoporosis, cancer, learning and memory disorders, and other diseases. This inspired researchers to further study and application of UB as a potential anti-aging drug. In this study, 13 amide derivatives of UB were designed and synthesized, and their anti-aging and biosafety were verified using Caenorhabditis elegans (C. elegans). C. elegans is a powerful model organism for anti-aging research. Finally, our results showed that Cpd. 11 had the best anti-aging activity among the thirteen amide derivatives, and the compound had good biosafety. Therefore, Cpd. 11 has the potential to be used as an anti-aging drug and needs to be further developed and applied.

New media has a strong vitality and its wide application for college students innovation and entrepreneurship education provides a good opportunity, which makes the use of new media to cultivate,train and enhance college students innovation and entrepreneurship education and practical ability become an important part of China’s higher education reform. In view of the current practical problems of the difficulty of employment of college students in China, the favorable factors of new media for college students innovation and entrepreneurship are analyzed, and the new media is used to carry out innovation and entrepreneurship education for college students from the aspects of creating an atmosphere of innovation and entrepreneurship, improving the quality of teachers innovation and entrepreneurship, creating innovation and entrepreneurship teams, building innovation and entrepreneurship platforms, and participating in innovation and entrepreneurship competitions, so as to improve the quality of innovation and entrepreneurship education for college students.

将椰子油、甘氨酸、氢氧化钠、水加入反应容器中,升温搅拌反应,经一步反应得到N-椰油酰基甘氨酸钠表面活性剂,并探索了反应投料比、反应溶剂、反应温度、反应时间等影响因素.结果表明,合成N-椰油酰基甘氨酸钠的较佳条件为:n(椰子油):n(甘氨酸):n(氢氧化钠)=1:3:3.3,反应温度180℃,反应时间12 h.在上述条件下,N-椰油酰基甘氨酸钠收率大于85％.

Thioether skeletons are widely present in drugs, natural products, functional materials, and life science. In the past decade, the selective C–H functionalization of thioethers has been extensively studied to construct novel thioether derivatives. This mini-review systematically introduces the recent advances in the field of the direct α-C(sp3)-H functionalization of thioethers.

专业群建设作为高职院校深化改革的关键,是将多个专业进行有序、互补和共享化的集合.通过科学合理设计专业群结构,有助于凸显院校办学特色,推动高职教育的高水平、高质量发展,促进院校核心竞争力的提升.面对制约高职院校专业群建设的瓶颈及不利因素,为了提升建设的集成、适应和协同效能,以特色性、共享性和竞争性为视角,从组群引导、校企合作规划、健全"双师型"团队、优化教学管理和评价保障机制等方面提出了解决对策.

In the last decade, transition-metal-catalyzed direct C-H bond functionalization has been recognized as one of most efficient approaches for the derivatization of thioethers. Within this category, both mono- and bidentate-directing group strategies achieved the remote C(sp2)-H and C(sp3)-H functionalization of thioethers, respectively. This review systematically introduces the major advances and their mechanisms in the field of transition-metal-catalyzed remote C-H functionalization of thioethers from 2010 to 2021.