Electrochemically Promoted Three-Component Reaction to N-Sulfonyl Amidines.

In this study, a multicomponent reaction via the Mannich intermediate was developed using methanol, secondary amine, and sulfonamide as starting materials. This method uses methanol as a green C1 source. The substrate scope is wide, and the yield is good. The mechanistic study shows that methanol generates formaldehyde under electrochemical conditions, and sulfonyl amidine as a nucleophile reacts with Schiff base intermediates to form N-sulfonyl amidine in a single step.

Antibacterial oxygenated ergostane-type steroids produced by the marine sponge-derived fungus Aspergillus sp.

Two oxygenated ergostane-type steroids including one new compound, 3ß-hydroxy-5α,6ß-methoxyergosta-7,22-dien-15-one (1) along with a known analogue ergosta-6,22-dien-3ß,5α,8α-triol (2) were isolated from the crude extracts of the marine sponge-derived fungus Aspergillus sp. Their structures were elucidated on the basis of combined NMR and MS spectroscopic methods. Compound 1 was a marine ergostane-type steroid with two methoxy groups at C-5 and C-6, respectively. These oxygenated ergostane-type steroids were evaluated for their antibacterial activities against human or aquatic pathogens. Among them, compound 1 exhibited antibacterial activity against Staphylococcus aureus.

Advances in Photoelectric Therapy for the Early Intervention and Treatment of Traumatic Scars.

Traumatic scar is a disease that affected approximately tens of millions of patients worldwide. According to the histological and morphological properties of scars, the traumatic scar typically includes superficial scar, atrophic scar, hypertrophic scar, and keloid. Its formation is a natural consequence of wound healing, regardless of whether the wound was caused by trauma or surgery. However, the production of scars has considerable impacts on the physical and mental health of patients, even causing substantial aesthetic and functional impairments. Prevention or early treatment of scars is the most suitable therapeutic method, including surgical and non-surgical procedures; nevertheless, the benefits of non-operative therapies for scars are quite limited, and surgical treatments are always hard to achieve satisfying outcomes. Through the application of innovative technologies such as lasers, intense pulsed light, and radiofrequency, significant progress has been made in the treatment of traumatic scars. This review highlights the current advancements of photoelectric therapy for the prevention and treatment of various traumatic scars, which may throw light on innovative therapeutic options for scar therapies.

Ursolic acid-piperazine-dithiocarbamate ruthenium(II) polypyridyl complexes induced necroptosis in MGC-803 cells.

Three ursolic acid-piperazine-dithiocarbamate ruthenium(II) polypyridyl complexes Ru1-Ru3 were designed and synthesized for evaluating antitumor activity. All the complexes exhibited high in vitro cytotoxicity against MGC-803, T24, HepG2, CNE2, MDA-MB-231, MCF-7, A549, and A549/DDP cell lines. Ru1, Ru2, and Ru3 were 11, 8 and 10 times, respectively, more active than cisplatin against A549/DDP. An in vivo study on MGC-803 xenograft mouse models demonstrated that representative Ru2 exhibited an effective inhibitory effect on tumor growth, showing stronger antitumor activity than cisplatin. Biological investigations suggested that Ru2 entered MGC-803 cells by a clathrin-mediated endocytic pathway, initially localizing in the lysosomes and subsequently escaping and localizing in the mitochondria. Mitochondrial swelling resulted in vacuolization, which induced vacuolation-associated cell death and necroptosis with the formation of necrosomes (RIP1-RIP3) and the uptake of propidium iodide. These results demonstrate that the potential of Ru2 as a chemotherapeutic agent to kill cancer cells via a dual mechanism represents an alternative way to eradicate apoptosis-resistant forms of cancer.

High throughput analysis to identify key gene molecules that inhibit adipogenic differentiation and promote osteogenic differentiation of human mesenchymal stem cells.

The present study investigated the key genes, which cause switch from adipogenic to osteogenic differentiation of human mesenchymal stem cells (hMSCs). The transcriptomic profile of hMSCs samples were collected from Array Express database. Differential expression network was constructed by calculating the Pearson's correlation coefficient and ranked according to their topological features. The top 5% genes with degree ≥2 were selected as ego genes. Following the KEGG pathway enrichment analysis and the relevant miRNAs prediction, the miRNA-mRNA-pathway networks were constructed by combining the miRNA-mRNA pairs and mRNA-pathway pairs together. In total, we obtained 84, 119, 94 and 97 ego-genes in B, BI, BT and BTI groups, and DLGAP5, DLGAP5, NUSAP1 and NDC80 were the ego-genes with the highest z-score of each group, respectively. Beginning from each ego-gene, we identified 2 significant ego-modules with gene size ≥4 in group BI, and the ego-genes were PBK and NCOA3, respectively. Through KEGG pathway analysis, we found that most of the pathways enriched by ego-genes were associated with gene replication and repair, and cell proliferation. According to the miRNA prediction results, we found that some of the predicted miRNAs have been validated to be the regulatory miRNAs of these corresponding mRNAs. Finally we constructed a miRNA-mRNA-pathway network by integrating the miRNA-mRNA and mRNA-pathway pairs together. The constructed network gives us a more comprehensive understanding of the mechanism of osteogenic differentiation of hMSCs.

Platinum(ii) complexes with rutaecarpine and tryptanthrin derivatives induce apoptosis by inhibiting telomerase activity and disrupting mitochondrial function.

Four new platinum(ii) complexes, [Pt(Rut)(DMSO)Cl2] (Rut-Pt), [Pt(Try)(DMSO)Cl2] (Try-Pt), [Pt(ITry)(DMSO)Cl2] (ITry-Pt) and [Pt(BrTry)(DMSO)Cl2] (BrTry-Pt), with rutaecarpine (Rut), tryptanthrin (Try), 8-iodine-tryptanthrin (ITry) and 8-bromo-tryptanthrin (BrTry) as ligands were synthesized and fully characterized. In these complexes, the platinum(ii) adopts a four-coordinated square planar geometry. The inhibitory activity evaluated by the MTT assay showed that BrTry-Pt (IC50 = of 0.21 ± 0.25 µM) could inhibit the growth of T-24 tumor cells (human bladder cancer cell line) more so than the other three complexes. In addition, all of these Pt complexes exhibited low toxicity against non-cancerous HL-7702 cells. BrTry-Pt induced cell cycle arrest in the S phase, leading to the down-regulation of cyclin A and CDK2 proteins. BrTry-Pt acts as a telomerase inhibitor targeting the c-myc promoter. In addition, BrTry-Pt also caused mitochondrial dysfunction. Importantly, the in vitro anticancer activity of BrTry-Pt was higher than those of Rut-Pt, Try-Pt and ITry-Pt, and it was more selective for T-24 cells than for non-cancerous HL-7702 cells.

Selective Recognition of Highly Hydrophilic Molecules in Water by Endo-Functionalized Molecular Tubes.

Selective recognition of neutral hydrophilic molecules in water is a challenge for supramolecular chemistry but commonplace in nature. By mimicking the binding pocket of natural receptors, endo-functionalized molecular tubes are proposed to meet this challenge. We found that two molecular tubes with inwardly directed hydrogen-bond donors recognize highly hydrophilic solvent molecules in water with high selectivity. In the complexes, hydrogen bonding occurs in the deep and hydrophobic cavity. The cooperative action between hydrogen bonding and hydrophobic effects accounts for the high affinity and selectivity. The molecular receptor is fluorescent and can detect concentrations of 1,4-dioxane-a known carcinogen and persistent environmental contaminant-in water at a limit of 119 ppb. The method simplifies the analytic procedure for this highly hydrophilic molecule.

Atom-economical chemoselective synthesis of 1,4-enynes from terminal alkenes and propargylic alcohols catalyzed by Cu(OTf)2.

A novel and efficient Cu(OTf)2-catalyzed sp(3)-sp(2) C-C bond formation reaction through the direct coupling of propargylic alcohols with terminal alkenes has been realized under mild conditions. The reaction is tolerant to air and is atom-economical, in accordance with the concept of modern green chemistry. The present protocol provides an attractive approach to a diverse range of 1,4-enynes in high to excellent yields.