pH-Responsive Charge-Reversal Smart Nanoparticles for Co-Delivery of Mitoxantrone and Copper Ions to Enhance Breast Cancer Chemo-Chemodynamic Combination Therapy.

Purpose: The poor delivery and limited penetration of nanoparticles into breast cancer tumors remain essential challenges for effective anticancer therapy. This study aimed to design a promising nanoplatform with efficient tumor targeting and penetration capability for effective breast cancer therapy.

Methods: A pH-sensitive mitoxantrone (MTO) and copper ion-loaded nanosystem functionalized with cyclic CRGDfK and r9 peptide (TPRN-CM) was rationally designed for chemo-chemodynamic combination therapy.

[Research progress on processing history evolution, chemical constituents, and pharmacological action of Scorpio].

Scorpio is a valuable Chinese animal medicine commonly used in clinical practice in China. It is the main drug in the treatment of liver wind internal movement caused by various reasons throughout the history of traditional Chinese medicine(TCM), with the effects of relieving wind and spasm, dredging collaterals, relieving pain, and eliminating toxin and mass. Scorpio is poisonous and often used as medicine after processing.

Development and evaluation of a Chinese herbal gel for analgesic and anti-inflammatory effects.

This study aimed to develop a film-forming gel containing three Chinese herbal extracts, an extracted mixture of Corydalis yanhusuo, Cynanchum paniculatum and Armadillidium vulgare (Latreille) (MCCA) and evaluate its analgesic and anti-inflammatory activities. Using the Box Behnken Design, the optimal prescription for the MCCA gel was determined. The analgesic effects were tested through acid writhing and formalin pain models.

[Research progress on processing history evolution, chemical constituents, and pharmacological effects of Hirudo].

As a traditional animal drug, Hirudo is slightly toxic and has the effects of breaking blood stasis, dredging meridians, expelling stasis, and resolving mass. It has a long history of processing, and the early boiling records can be traced back to the Han Dynasty. More than ten processing methods such as frying, roasting, and lime processing appeared later.

The prebiotic properties of polysaccharides obtained by differentiated deproteinization methods from on .

The polysaccharides derived from various deproteinization methods were prepared from (FSI) to investigate the prebiotic efficacy of ( ). The implications of polysaccharides from FSI (PFSI) gained after purification performed by non-deproteinization and different deproteinization processes (Savage method, papain method, and TCA method) one-factor optimization were firstly investigated for the influences on the growth of . The utilization of carbohydrate sources and the synthesis of protein and lactate during its growth were analyzed, as well as the variations of LDH, SOD, and GSH- Px enzyme dynamics.

The Chemical Profiling and Anticancer Potential of Functional Polysaccharides from Flos Sophorae Immaturus.

Polysaccharides from Flos Sophorae Immaturus (FSI) are one of its pharmacological compounds that can perform effective activities. Aiming to extract the most effective polysaccharides against hepatocellular carcinoma (HCC), the polysaccharides were separated from FSI through ultrasonic microwave extraction, and the first comparison was carried out on the characterization of the structure and its cytotoxic properties on HCC SMMC 7721 cells of undeproteinized purified polysaccharides (PFSI-1) and papain-deproteinized polysaccharides (PFSI-2) from FSI. The findings indicated that PFSI-1 and PFSI-2 had characteristic absorption peaks of polysaccharides; PFSI-1 contained three monosaccharides and PFSI-2 contained ten; and SEM, AFM, and NMR were consistent with the verification of IR polysaccharide characteristics, suggesting probable additional latent activities.

Antibacterial effect and mechanism of anthocyanin from .

The inhibitory effects of the anthocyanin obtained from were tested against several food-borne pathogens were evaluated, such as (), (, and In general, anthocyanin had different antibacterial effect on different bacteria, and the best antibacterial effect on , with minimal inhibitory concentration (MIC) of 3.125 mg/mL. Anthocyanin increased the surface hydrophobicity of , discharged the intracellular K, and reduced the total soluble protein, affecting protein synthesis.

A PBPK Model of Ternary Cyclodextrin Complex of ST-246 Was Built to Achieve a Reasonable IV Infusion Regimen for the Treatment of Human Severe Smallpox.

ST-246 is an oral drug against pathogenic orthopoxvirus infections. An intravenous formulation is required for some critical patients. A ternary complex of ST-246/meglumine/hydroxypropyl-β-cyclodextrin with well-improved solubility was successfully developed in our institute.

Comparative Analysis of Physiological, Enzymatic, and Transcriptomic Responses Revealed Mechanisms of Salt Tolerance and Recovery in .

Salt stress results in the severe decline of yield and quality in wheat. In the present study, salt-tolerant ("Y1805") and salt-sensitive wheat "Chinese Spring" ("CS") were selected from 121 wheat germplasms to test their physiological, antioxidant enzyme, and transcriptomic responses and mechanisms against salt stress and recovery. 56 chromosomes were identified in "Y1805" that comprised A, B, and D chromosomes from wheat parent and E chromosomes from , adding to salt-tolerant trait.

Comparable Intestinal and Hepatic First-Pass Effect of YL-IPA08 on the Bioavailability and Effective Brain Exposure, a Rapid Anti-PTSD and Anti-Depression Compound.

YL-IPA08, exerting rapid antidepressant-like and anxiolytic-like effects on behaviors by translocator protein (TSPO) mediation, is a novel compound that has been discovered and developed at our institute. Fit-for-purpose pharmacokinetic properties is urgently needed to be discovered as early as possible for a new compound. YL-IPA08 exhibited low bioavailability (∼6%) during the preliminary pharmacokinetics study in rats after oral administration.

Procyanidin B2 mitigates endothelial endoplasmic reticulum stress through a PPARδ-Dependent mechanism.

Hyperglycemia-induced endothelial endoplasmic reticulum (ER) stress is implicated in the pathophysiology of diabetes and its vascular complications. Procyanidins are enriched in many plant foods and have been demonstrated to exert several beneficial effects on diabetes, cardiovascular and other metabolic diseases. In the present study, we investigated the effect of procyanidin B2 (PCB2), the most widely distributed natural procyanidin, on ER stress evoked by high glucose in endothelial cells (ECs) and the underlying mechanisms.

Assessment and Confirmation of Species Difference in Nonlinear Pharmacokinetics of Atipamezole with Physiologically Based Pharmacokinetic Modeling.

Atipamezole, an -adrenoceptor antagonist, displayed nonlinear pharmacokinetics (PK) in rats. The aim of this study was to understand the underlying mechanisms of nonlinear PK in rats and linear PK in humans and develop physiologically based PK models (PBPK) to capture and validate this phenomenon. In vitro and in vivo data were generated to show that metabolism is the main clearance pathway of atipamezole and species differences exist.

APC/Cdh1 targets PECAM-1 for ubiquitination and degradation in endothelial cells.

Platelet endothelial cell adhesion molecule-1 (PECAM-1) is a member of the immunoglobulin superfamily and is expressed by hematopoietic and endothelial cells (ECs). Recent studies have shown that PECAM-1 plays a crucial role in promoting the development of the EC inflammatory response in the context of disturbed flow. However, the mechanistic pathways that control PECAM-1 protein stability remain largely unclear.

Procyanidin B2 Activates PPARγ to Induce M2 Polarization in Mouse Macrophages.

Procyanidins, a subclass of flavonoids found in commonly consumed foods, possess potential anti-inflammatory activity. Manipulation of M1/M2 macrophage homeostasis is an effective strategy for the treatment of metabolic inflammatory diseases. The objective of this study was to determine the effect of procyanidins on macrophage polarization.

Hybrid micelles containing methotrexate-conjugated polymer and co-loaded with microRNA-124 for rheumatoid arthritis therapy.

: Methotrexate (MTX) is a first-line drug for rheumatoid arthritis (RA)therapy. However, MTX monotherapy often results in irreversible joint damage due to its slow onset of action and long duration. microRNA-124 (miR-124) has shown direct bone protection activity against RA.

Stachydrine Mediates Rapid Vascular Relaxation: Activation of Endothelial Nitric Oxide Synthase Involving AMP-Activated Protein Kinase and Akt Phosphorylation in Vascular Endothelial Cells.

Stachydrine (STA) is a constituent of citrus fruits and Sweet. In the present study, we established that STA caused acute endothelium-dependent relaxation. The vascular action of STA was mediated by nitric oxide (NO) via cyclic guanosine monophosphate.

PPARδ agonist prevents endothelial dysfunction via induction of dihydrofolate reductase gene and activation of tetrahydrobiopterin salvage pathway.

Background And Purpose: Impaired endothelium-dependent relaxation (EDR) is a hallmark of endothelial dysfunction. A deficiency of tetrahydrobiopterin (BH ) causes endothelial NOS to produce ROS rather than NO. PPARδ is an emerging target for pharmacological intervention of endothelial dysfunction.

Targeted and Efficient Delivery of siRNA Using Tunable Polymeric Hybrid Micelles for Tumor Therapy.

Background/aim: Effective and targeted delivery of siRNA to tumor cells is a prerequisite to achieving their therapeutic effects. Survivin is up-regulated in tumor cells and is associated with resistance to therapy. Therefore, siRNA-mediated silencing of survivin is a potential therapeutic strategy for cancer.

Targeted Co-Delivery of siRNA and Methotrexate for Tumor Therapy via Mixed Micelles.

A combination of chemotherapeutic drugs and siRNA is emerging as a new modality for cancer therapy. A safe and effective carrier platform is needed for combination drug delivery. Here, a functionalized mixed micelle-based delivery system was developed for targeted co-delivery of methotrexate (MTX) and survivin siRNA.

Influences of graphene oxide on biofilm formation of gram-negative and gram-positive bacteria.

In this study, we evaluated the influences of graphene oxide (GO) on biofilm formation. Escherichia coli MG1655 and Bacillus subtilis 168 were used as models for Gram-negative and Gram-positive bacteria. The growth profiles and viability assays indicated that GO exhibited a high antibacterial activity, of which the negative effects on bacteria growth raised with the increasing GO concentration.