Advances in Targeting Drug Biological Carriers for Enhancing Tumor Therapy Efficacy

Chemotherapy drugs continue to be the main component of oncology treatment research and have been proven to be the main treatment modality in tumor therapy. However, the poor delivery efficiency of cancer therapeutic drugs and their potential off-target toxicity significantly limit their effectiveness and extensive application. The recent integration of biological carriers and functional agents is expected to camouflage synthetic biomimetic nanoparticles for targeted delivery. The promising candidates, including but not limited to red blood cells and their membranes, platelets, tumor cell membrane, bacteria, immune cell membrane, and hybrid membrane are typical representatives of biological carriers because of their excellent biocompatibility and biodegradability. Biological carriers are widely used to deliver chemotherapy drugs to improve the effectiveness of drug delivery and therapeutic efficacy in vivo, and tremendous progress is made in this field. This review summarizes recent developments in biological vectors as targeted drug delivery systems based on microenvironmental stimuli-responsive release, thus highlighting the potential applications of target drug biological carriers. The review also discusses the possibility of clinical translation, as well as the exploitation trend of these target drug biological carriers.     

A novel lipid droplets-targeting fluorescent probe based on dicyanisophorone and carbazole for Cu2+ and its application

A novel fluorescent probe, LCH , based on dicyanisophorone and carbazole, was prepared for the visual detection of Cu²⁺. The probe LCH could recognize Cu²⁺ by fluorescence quenching in EtOH/H₂O (1/4, v/v) solution, which could be easily identified under the 365 nm UV lamp, and the detection limit was as low as 0.785 μM. The recognition mechanism of probe LCH with Cu²⁺ was determined by combining ¹H NMR titration, MS, and theoretical calculations. Practical application experiments showed that probe LCH could be used to detect Cu²⁺ in the test strip experiments. Cell imaging experiments showed that the probe LCH owned good cell permeability and could be applied to the imaging of Cu²⁺ in HepG2 cells. In addition, fluorescence colocalization experiments showed that LCH could target lipid droplets. These results indicate that the probe LCH will have a good application prospect in environmental detection and clinical medicine.     

非衍生化高效液相色谱-串联质谱法快速检测生物体液中草甘膦、草铵膦及代谢物

建立了一种非衍生化高效液相色谱-串联质谱快速检测生物体液中草甘膦、草铵膦及其代谢物等8种极性农药的方法。8种极性农药经Metrosep A Supp 5阴离子色谱柱(150 mm×4.0 mm,5μm)分离,以纯水-200 mmol/L碳酸氢铵溶液(含0.1%氨水)为流动相进行梯度洗脱,负离子多反应监测(MRM)模式进行检测。实验结果表明,8种极性农药在0.5~50 ng/mL范围内线性关系良好(r²>0.99),检出限(S/N≥3)为0.08~0.3 ng/mL,定量下限(S/N≥10)为0.3~1 ng/mL。方法的基质效应为86.5%~106%,目标化合物的回收率为81.5%~114%,日内相对标准偏差(RSD)为0.30%~2.8%,日间RSD为0.50%~5.3%。该方法无需复杂的衍生化过程,简便快速、灵敏度高、稳定性好,适用于生物体液中8种极性农药的检测。     

Bee Venom in Wound Healing

Bee venom (BV), also known as api-toxin, is widely used in the treatment of different inflammatory diseases such as rheumatoid arthritis or multiple sclerosis. It is also known that BV can improve the wound healing process. BV plays a crucial role in the modulation of the different phases of wound repair. It possesses anti-inflammatory, antioxidant, antifungal, antiviral, antimicrobial and analgesic properties, all of which have a positive impact on the wound healing process. The mentioned process consists of four phases, i.e., hemostasis, inflammation, proliferation and remodeling. The impaired wound healing process constitutes a significant problem especially in diabetic patients, due to hypoxia state. It had been found that BV accelerated the wound healing in diabetic patients as well as in laboratory animals by impairing the caspase-3, caspase-8 and caspase-9 activity. Moreover, the activity of BV in wound healing is associated with regulating the expression of transforming growth factor (TGF-β1), vascular endothelial growth factor and increased collagen type I. BV stimulates the proliferation and migration of human epidermal keratinocytes and fibroblasts. In combination with polyvinyl alcohol and chitosan, BV significantly accelerates the wound healing process, increasing the hydroxyproline and glutathione and lowering the IL-6 level in wound tissues. The effect of BV on the wounds has been proved by numerous studies, which revealed that BV in the wound healing process brings about a curative effect and could be applied as a new potential treatment for wound repair. However, therapy with bee venom may induce allergic reactions, so it is necessary to assess the existence of the patient’s hypersensitivity to apitoxin before treatment.     

Biodegradable and Biocompatible Silatrane Polymers

In this study, new biodegradable and biocompatible amphiphilic polymers were obtained by modifying the peripheral hydroxyl groups of branched polyethers and polyesters with organosilicon substituents. The structures of the synthesized polymers were confirmed by NMR and GPC. Organosilicon moieties of the polymers were formed by silatranes and trimethylsilyl blocks and displayed hydrophilic and hydrophobic properties, respectively. The effect of the ratio of hydrophilic to hydrophobic organosilicon structures on the surface activity and biological activity of macromolecules was studied, together with the effect on these activities of the macromolecules’ molecular weight and chemical structure. In particular, the critical micelle concentrations were determined, the effect of the structure of the polymers on their wetting with aqueous solutions on glass and parafilm was described, and the aggregation stability of emulsions was studied. Finally, the effect of the polymer structures on their antifungal activity and seed germination stimulation was examined.     

Structures and Bioactivities of Steroidal Saponins Isolated from the Genera Dracaena and Sansevieria

The species Dracaena and Sansevieria, that are well-known for different uses in traditional medicines and as indoor ornamental plants with air purifying property, are rich sources of bioactive secondary metabolites. In fact, a wide variety of phytochemical constituents have been isolated so far from about seventeen species. This paper has reviewed the literature of about 180 steroidal saponins, isolated from Dracaena and Sansevieria species, as a basis for further studies. Saponins are among the most characteristic metabolites isolated from the two genera. They show a great variety in structural motifs and a wide range of biological activities, including anti-inflammatory, anti-microbial, anti-proliferative effects and, in most case, remarkable cytotoxic properties.     

碳点的性质及其在生物传感器领域的应用

碳点(carbon dots,CDs)作为一种具有优良生物相容性、低毒性和表面功能可调的新型碳基纳米材料,在生物传感领域具有极大的应用潜力.本文对碳点的生物效应、发光性质及其发光机理进行了简述,并根据传感机制的不同,将CDs在生物传感领域的应用分为荧光(fluorescence,FL)传感器、电致发光(electrochemiluminescence,ECL)传感器以及化学发光(chemiluminescence,CL)传感器三类进行综述.最后分析了CDs目前在生物传感器领域应用中存在的问题,并对其发展进行了展望.     

Biosynthesis and Anti-Mycotoxigenic Activity of Zingiber officinale Roscoe-Derived Metal Nanoparticles

Mycotoxigenic fungi have attracted special attention due to their threat to food security and toxicity to human health. Aqueous extract of Zingiber officinale Roscoe was used as reducing and capping agent for the synthesis of silver (AgNPs), copper (CuNPs), and zinc oxide (ZnONPs) nanoparticles. UV-Visible spectra of the AgNPs, CuNPs, and ZnONPs showed absorption peaks at λ_max 416 nm, 472 nm, and 372 nm, respectively. Zeta potential of AgNPs, CuNPs, and ZnONPs were −30.9, −30.4 and −18.4 mV, respectively. ZnONPs showed the highest activity against Aspergillus awamori ZUJQ 965830.1 (ZOI 20.9 mm and MIC 24.7 µg/mL). TEM micrographs of ZnONPs-treated A. awamori showed cracks and pits in the cell wall, liquefaction of the cytoplasmic content, making it less electron-dense. The sporulation and ochratoxin A production of A. awamori was inhibited by ZnONPs in a concentration-dependent pattern. The inhibition percentage of OTA were 45.6, 84.78 and 95.65% for 10, 15, 20 of ZnONPs/mL, respectively.     

An Insight into Kiwiberry Leaf Valorization: Phenolic Composition,Bioactivity and Health Benefits

During kiwiberry production, different by-products are generated, including leaves that are removed to increase the fruit’s solar exposure. The aim of this work was to extract bioactive compounds from kiwiberry leaf by employing microwave-assisted extraction (MAE). Compatible food solvents (water and ethanol) were employed. The alcoholic extract contained the highest phenolic and flavonoid contents (629.48 mg of gallic acid equivalents (GAE) per gram of plant material on dry weight (dw) (GAE/g dw) and 136.81 mg of catechin equivalents per gram of plant material on dw (CAE/g dw), respectively). Oppositely, the hydroalcoholic extract achieved the highest antioxidant activity and scavenging activity against reactive oxygen and nitrogen species (IC₅₀ = 29.10 μg/mL for O₂^•−, IC₅₀ = 1.87 μg/mL for HOCl and IC₅₀ = 1.18 μg/mL for ^•NO). The phenolic profile showed the presence of caffeoylquinic acids, proanthocyanidin, and quercetin in all samples. However, caffeoylquinic acids and quercetin were detected in higher amounts in the alcoholic extract, while proanthocyanidins were prevalent in the hydroalcoholic extract. No adverse effects were observed on Caco-2 viability, while the highest concentration (1000 µg/mL) of hydroalcoholic and alcoholic extracts conducted to a decrease of HT29-MTX viability. These results highlight the MAE potentialities to extract bioactive compounds from kiwiberry leaf.     

Benzodiazepines: Drugs with Chemical Skeletons Suitable for the Preparation of Metallacycles with Potential Pharmacological Activity

The synthesis of organometallic compounds with potential pharmacological activity has attracted the attention of many research groups, aiming to take advantage of aspects that the presence of the metal-carbon bond can bring to the design of new pharmaceutical drugs. In this context, we have gathered studies reported in the literature in which psychoactive benzodiazepine drugs were used as ligands in the preparation of organometallic and metal complexes and provide details on some of their biological effects. We also highlight that most commonly known benzodiazepine-based drugs display molecular features that allow the preparation of metallacycles via C-H activation. These organometallic compounds merit further attention regarding their potential biological effects, not only in terms of psychoactive drugs but also in the search for drug replacements, for example, for cancer treatments.