Recent advances in self-targeting natural product-based nanomedicines.

Natural products, recognized for their potential in disease prevention and treatment, have been integrated with advanced nano-delivery systems to create natural product-based nanomedicines, offering innovative approaches for various diseases. Natural products derived from traditional Chinese medicine have their own targeting effect and remarkable therapeutic effect on many diseases, but there are some shortcomings such as poor physical and chemical properties. The construction of nanomedicines using the active ingredients of natural products has become a key step in the modernization research process, which could be used to make up for the defects of natural products such as low solubility, large dosage, poor bioavailability and poor targeting.

Application of Advanced High-Resolution Mass Spectrometric Techniques for the Analysis of Losartan Potassium Drug Substance Degradation Products: From Nontargeted to Targeted Screening.

Advances in techniques for quality analysis allow for a more detailed examination of drug impurities. High-resolution mass spectrometry (HRMS) contributes to detecting both known and unknown impurities. In this study, a combination of a nontargeted and targeted screening approach was established and applied to the detailed degradation profile of the losartan potassium (LP) drug substance.

An encounter between metal ions and natural products: natural products-coordinated metal ions for the diagnosis and treatment of tumors.

Natural products-coordinated metal ions to form the nanomedicines are in the spotlight for cancer therapy. Some natural products could be coordinated with metal ions forming nanomedicines via simple and green environmental self-assembly, which not only improved the bioavailability of natural products, but also conferred multiple therapeutic modalities and multimodal imaging. On the one hand, in the weak acidity, glutathione (GSH) and hydrogen peroxide (HO) overexpression of tumor microenvironment (TME), such carrier-free nanomedicines could be further enhanced the therapeutic effect via optimizing the species of metal ions.

Modular Design and Scaffold-Synthesis of Multi-Functional Fluorophores for Targeted Cellular Imaging and Pyroptosis.

Fluorophores are essential tools for optical imaging and biomedical research. Their synthetic modification to incorporate new functions, however, remains a challenging task. Conventional strategies rely on linear synthesis in which a parent framework is gradually extended.

A review of L. in the treatment of liver disease: viral hepatitis, liver fibrosis/cirrhosis and hepatocellular carcinoma.

Due to the pathological production of liver disease in utility particularly complexity, the morbidity and mortality of liver disease including viral hepatitis, liver fibrosis/cirrhosis and hepatocellular carcinoma (HCC) are rapidly increasing worldwide. Considering its insidious onset, rapid progression and drug resistance, finding an effective therapy is particularly worthwhile. L.

A Novel Multi-Effect Photosensitizer for Tumor Destruction via Multimodal Imaging Guided Synergistic Cancer Phototherapy.

Background: How to ingeniously design multi-effect photosensitizers (PSs), including multimodal imaging and multi-channel therapy, is of great significance for highly spatiotemporal controllable precise phototherapy of malignant tumors.

Methods: Herein, a novel multifunctional zinc(II) phthalocyanine-based planar micromolecule amphiphile () was successfully designed and synthesized, in which N atom with photoinduced electron transfer effect was introduced to enhance the near-infrared absorbance and nonradiative heat generation. After simple self-assembling into nanoparticles (NPs), would exhibit enhanced multimodal imaging properties including fluorescence (FL) imaging (FLI) /photoacoustic (PA) imaging (PAI) /infrared (IR) thermal imaging, which was further used to guide the combined photodynamic therapy (PDT) and photothermal therapy (PTT).

A SARS-CoV-2 M fluorescent sensor for exploring pharmacodynamic substances from traditional Chinese medicine.

The main protease of SARS-CoV-2 (SARS-CoV-2 M) plays a critical role in the replication and life cycle of the virus. Currently, how to screen SARS-CoV-2 M inhibitors from complex traditional Chinese medicine (TCM) is the bottleneck for exploring the pharmacodynamic substances of TCM against SARS-CoV-2. In this study, a simple, cost-effective, rapid, and selective fluorescent sensor (TPE-S-TLG sensor) was designed with an AIE (aggregation-induced emission) probe (TPE-Ph-In) and the SARS-CoV-2 M substrate (S-TLG).

Self-Assembled Matrine-PROTAC Encapsulating Zinc(II) Phthalocyanine with GSH-Depletion-Enhanced ROS Generation for Cancer Therapy.

The integration of a multidimensional treatment dominated by active ingredients of traditional Chinese medicine (TCM), including enhanced chemotherapy and synergistically amplification of oxidative damage, into a nanoplatform would be of great significance for furthering accurate and effective cancer treatment with the active ingredients of TCM. Herein, in this study, we designed and synthesized four matrine-proteolysis-targeting chimeras (PROTACs) (depending on different lengths of the chains named LST-1, LST-2, LST-3, and LST-4) based on PROTAC technology to overcome the limitations of matrine. LST-4, with better anti-tumor activity than matrine, still degrades p-Erk and p-Akt proteins.

Electrochemical deoxygenative homo-couplings of aromatic aldehydes.

An electrochemical deoxygenative homo-coupling of aromatic aldehydes is achieved to selectively access bibenzyl and stilbene derivatives. The protocol allows the homo-coupling of aldehydes to occur after single-electron-reduction at the cathode. Taking advantage of the oxophilicity of triphenylphosphine, the electrochemical deoxygenation proceeds smoothly to give reductive homo-coupling products.

An aggregation-induced emission sensor combined with UHPLC-Q-TOF/MS for fast identification of anticoagulant active ingredients from traditional Chinese medicine.

Xuebijing injection (XBJ) has a good therapeutic effect on the patients with severe coronavirus disease, but the material basis of XBJ with the anticoagulant effect to improve the coagulopathy and thromboembolism is still unclear. Herein, we developed a new strategy based on aggregation-induced emission (AIE) for monitoring thrombin activity and screening thrombin inhibitors from XBJ. The molecule AIE and the thrombin substrate peptide S-2238 were formed into AIE nanoparticle (AIENP) which emitted notable fluorescence due to the restriction of intramolecular motions.

A Multichannel Fluorescent Array Sensor for Discrimination of Different Types of Drug-Induced Kidney Injury.

The differences in urinary proteins could provide a novel opportunity to distinguish the different types of drug-induced kidney injury (DIKI). In this research, Au nanoparticles-polyethyleneimine (AuNPs-PEI) and the three fluorophore-labeled proteins (FLPs) have been constructed as a multichannel fluorescent array sensor via electrostatic interaction, which was used to detect the subtle changes in urine collected from the pathological state of DIKI. Once the urine from different types of DIKI was introduced, the binding equilibrium between AuNPs-PEI and FLPs would be broken due to the competitive binding of urinary protein, and the corresponding fluorescence response pattern would be generated.

Electrochemical deoxygenative arylation of aldehydes and ketones.

The construction of diaryl alkanes from aromatic aldehydes or ketones with electron-deficient arenes is achieved in the presence of trivalent phosphine under electrochemical conditions. Reductive coupling between electron-deficient arenes and the carbonyl groups of aldehydes or ketones occurs at the cathode to yield diaryl alcohols. At the anode, the trivalent phosphine reagent may undergo single-electron oxidation to generate its radical cation, which reacts with the diaryl alcohols to form dehydroxylated products.

N-Selective β-Thioalkylation of Benzotriazoles with Alkenes.

Herein, N-selective β-thioalkylation of benzotriazoles with unactivated alkenes and styrenes is reported. The N-selective β-thioalkylation of benzotriazoles is highly stereospecific and works under simple and mild conditions, exhibiting excellent functional group tolerance. The high N-selectivity is a consequence of the combination of hydrogen bonding and Lewis acid/base activation, which reverses the N-position to be favored for alkylation.