Latest ArticlesTwo lindenane-type sesquiterpene (LDS) trimers with unprecedented carbon skeletons, holotrichones A (1) and B (2), were obtained from the whole plant of Chloranthus holostegius var. trichoneurus by a ultra performance liquid chromatography-photodiode array detector-mass spectrometry (UPLC-PDA-MS)-guided isolation strategy. Compound 1 represents the first LDS trimer incorporating a unique 3/5/6/6-fused framework, in which a lindenane-type monomer and the 2-methylbutyryl substituent of an LDS dimer is bridged by a six-membered ring system. Compound 2 is the first hetero-trimer fused by an LDS dimer with a p-benzoquinone-meroterpenoid, featuring an unusual 3/5/6/6/3/5/6/6/6 nonacyclic system fused by the sesquiterpenoid unit and a 2-geranyl-6-methyl-2,5-cyclohexadien-1,4-dione moiety. In compound 2, the dimeric LDS moiety is equipped with a rare oxaspiro[4.5]decane system. Their structures, including absolute configurations, were established by spectroscopic methods, GIAO NMR calculations and DP4+ probability analyses, electronic circular dichroism (ECD) calculations, and single-crystal X-ray diffraction analysis. The plausible biogenetic pathway speculation indicated that hetero- and homo-Diels-Alder additions may dominate the formation of these highly fused polycyclic frameworks. Both compounds 1 and 2 induced the human acute myeloid leukemia MV-4–11 cell death via apoptosis induction, which deserves further investigation on this new chemical class of LDS oligomers for their anti-leukemic potential.
Photodynamic therapy has been widely employed as an alternative strategy against bacterial infection. Molecular structure has a profound effect on the antibacterial ability of photosensitizers (PSs). Herein, we designed and synthesized a series of boron dipyrromethene (BODIPY)-based photosensitizers with different alkyl chain lengths, and then their antibacterial activities were compared. Among these BODIPYs, the BODIPY with octyl (BDP-8) exhibits the best antibacterial effect, while the antibacterial performance of BODIPY with dodecyl (BDP-12) is the worst. This work provides instructive information for further development of effective photodynamic antimicrobial agents.
Patients with oral squamous cell carcinoma (OSCC) encounter challenges in achieving efficient antitumor immunity, primarily due to the inherent pathophysiological characteristics of solid tumors affecting drug accumulation and penetration. Insufficient T-cells and immune escape induced by tumor-associated macrophages (TAMs) further exacerbate these issues. This study utilized M1 macrophage membrane-modified spatial dimension conversion drug delivery systems (SDDDSs) and introduced photosensitizers chlorophyll Pyro and the immune agonist R848. This innovative approach enhanced tumor targeting and accumulation by transforming stimulus-responsive size-reductive SDDDSs into smaller-sized iRGD-Pyro and R848 within the extracellular tumor microenvironment (TME). This facilitated effective drug penetration into deep tumor regions and cellular uptake. The synergistic treatment strategy for OSCC, combining photodynamic therapy (PDT) and tumor immunotherapy, induced tumor cell apoptosis, triggered immunogenic cell death (ICD), polarized TAMs towards the M1 phenotype, promoted sufficient T-cell infiltration, and resulted in significant therapeutic outcomes. This approach offers a promising avenue for future OSCC therapeutic interventions.
A copper-catalyzed three-component reaction involving cyclic carbonates, elemental sulfur, and H-phosphonates is presented. It proceeds with excellent yields and provides an attractive approach for the construction of valuable trisubstituted allenyl phosphorothioates using a one-step strategy. Moreover, this method can be easily adapted to large-scale preparation.
Increasing interests of difluorinated amino acids (DFAAs) have been raised in recent years due to their widespread bio-organic and medical applications. However, to date, only few investigations focused on their asymmetric synthesis. Exploring difluoromethyl reagent to tailor a novel pathway and developing efficient catalytic system are highly desirable for constructing structurally diverse chiral DFAAs. Herein, a copper-catalyzed asymmetric difluorobenzylation of aldimine esters is described. By using α,α-difluorinated benzyltriflones as difluoromethyl reagents, this protocol allows the asymmetric synthesis of α-quaternary DFAAs with wide scope, good yields and excellent enantioselectivities (90%-98% ee). Control experiments and DESI-MS analysis demonstrate the reaction probably proceeds via a key difluorocarbocation intermediate. Moreover, polyfluoroarenes are found efficient candidates to polyfluoroaryl amino acids via C-F activation. Gram-scale experiment, late-stage functionalization, synthesis of difluorinated dipeptides and bioactive molecular analogues revealed the utility of the protocol, thereby largely enriching the structural diversity of FAAs and providing more potential opportunities in drug discovery.
Dopamine, a pivotal excitatory neurotransmitter, plays a crucial role in metabolic, cardiovascular, renal, central nervous, and endocrine systems. Abnormal dopamine within the human body can cause various diseases. Therefore, the precise quantification of dopamine levels, both in vivo and in vitro, holds paramount significance for clinical applications and physiological investigations. Carbon dots (CDs) exhibit a plethora of remarkable properties, including a substantial specific surface area, robust electrical conductivity, commendable biocompatibility, minimal toxicity, and high photostability. Considering these unique characteristics, CDs demonstrate substantial potential for fluorescent sensors, colorimetric sensors, and electrochemical sensors for dopamine detection. This review systematically examined the challenges and prospects for the utilization of CDs-based fluorescent sensors, electrochemical biosensors, and colorimetric sensors for monitoring dopamine levels in recent years. These findings unveil promising avenues for further advancements in the field of dopamine detection.
Lymphoma is a hematological malignancy with an increasing mortality rate. Nevertheless, the treatment strategy against lymphoma remains limited. Doxorubicin (DOX) is a broad-spectrum anti-tumor chemotherapeutic drug, the clinical application of which is limited by serious adverse effects and drug resistance. In this work, biodegradable methoxy poly(ethylene glycol)-block-poly(lactic acid) (mPEG-PLA) nanomicelles co-delivering of DOX and apatinib (AP) (DOX-AP/m) was developed for lymphoma therapy. The average particle size of the self-assembled drug-loaded nano-micelle was 31.94 nm. It is revealed that AP can enhance the uptake of DOX by tumor cells. The in vivo and in vitro experimental results revealed that DOX-AP/m combination therapy could inhibit proliferation and promote apoptosis of lymphoma cells, and greatly suppress tumor growth. Our study indicated that DOX-AP/m might provide new insight and hold great potential in the treatment of lymphoma.
Sonodynamic therapy (SDT) exhibits noninvasive and accuracy in cancer treatment, and has aroused widespread attention. However, the low quantum yield of inorganic sonosensitizers under ultrasound (US) stimulation leads to unsatisfactory efficacy. In this work, an urchin-like piezoelectric ZnSnO3/Cu3P p-n heterojunction was constructed as an efficient sonosensitizer for enhanced SDT. The p-n heterojunction formation narrows the band bandgap and increases the piezoelectric property, which contribute to the promotion of carrier separation and suppression of carrier recombination, resulting in enhanced SDT. Moreover, under tumor microenvironment (TME) with over produced H2O2 and glutathione (GSH), Cu3P NNs induce chemodynamic therapy (CDT) by initiating a Fenton-like reaction and depleting GSH, leading to increased cellular oxidative damage. With the combination effect, the ZnSnO3/Cu3P heterojunction demonstrates a 70% tumor growth inhibition rate in 4T1 tumor mice model. This piezoelectric heterojunction achieves the combined treatment of SDT and CDT, and opens new possibilities for the application of SDT in tumor therapy.
Osteoporosis is a disease of bone metabolism homeostasis imbalance with obvious bone loss, damage to bone microstructure, and increased risk of fracture. The occurrence and development of osteoporosis is related to the augmentation of active osteoclasts. Receptor activator of nuclear factor kappa B (RANK) small interfering RNA (siRNA) knockdowns the expression of RANK mRNA to inhibit the osteoclast precursors differentiate into osteoclasts as a treatment in osteoporosis. Salmon calcitonin (sCT) is a commonly used anti-osteoporotic agent that inhibits osteoclast activity and induces osteoclast apoptosis, and it also could promote the osteogenesis by osteoblasts. A cocktail therapy improves the therapeutic effect of osteoporosis between RANK siRNA and sCT. A size-switchable microsphere from micro to nano scale was developed to address the delivery barriers of biomacromolecules with poor stability and frequent administration. RANK siRNA and sCT were incorporated into the microspheres with a nanoparticle/micelle-microsphere double-layer structure to achieve sustained release when the particle size shrunk and dual protection of RANK siRNA and sCT. The size-switchable microspheres MS@(AL-NPs/ARM) had an optimal therapeutic effect and reduced the frequency of administration in glucocorticoid induced osteoporosis (GIOP) mouse model. RANK siRNA and sCT co-delivery system based on size-switchable microsphere is a promising strategy to treat osteoporosis through the controlled release of biomacromolecules.
To efficiently remove perfluorooctanoic acid (PFOA), we developed a composite of magnetic Fe3O4 nanocrystals and MIL-101 (an iron-based metal organic framework). Because of its high surface area, porous structure, and complexation between PFOA as confirmed by experimental results and density functional theory simulation, the magnetic composite showed a Langmuir adsorption capacity of 415 mg/g in the presence of various groundwater components, and thus adsorbed PFOA at environment-relevant concentration within 20 min. The catalyst loaded with PFOA can then be magnetically separated from the synthetic groundwater. This adsorption step concentrated PFOA near MIL-101 and resulted in a fast decomposition rate in the decomposition step, where MIL-101 served as an efficient Fenton agent due to its abundant Fe3+/Fe2+ sites. Meanwhile, the alternative magnetic field was introduced to change the production pathway of reactive oxygen species and superoxide radical anions were produced, which was critical for PFOA degradation. In addition, the inductive heating effect heat the magnetic particles to 445 K through an in-situ approach, which thus further accelerated Fenton reactions rate. In addition, and achieved a complete degradation of PFOA within 30 min. This newly developed Fenton catalyst demonstrates advantages over conventionally heterogeneous and homogeneous catalysts, and thus is promising for practical applications.
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