A review on the in vitro and in vivo screening of α-glucosidase inhibitors.

As a global metabolic disease, the control and treatment of diabetes have always been the focus of medical research. α-Glucosidase is a key enzyme in regulating blood glucose levels and has important applications in the treatment of diabetes. This review aims to explore the enzyme activity of α-glucosidase and its inhibition mechanism and evaluate the efficacy and limitations of existing inhibitor screening methods. First, the chemical structure, biological activity, and influencing factors of α-glucosidase on diabetes are discussed in detail. Then, the various methods that have been used to screen α-glucosidase inhibitors in recent years are reviewed, including in vivo animal experiments, in vitro experiments, and virtual molecular docking. The experimental principles, advantages, and limitations of each method and their application in discovering new inhibitors are also discussed. Finally, this review emphasizes the importance of developing efficient and safe α-glucosidase inhibitors, summarizes the advantages and disadvantages of various screening models, and proposes future research directions. This review comprehensively examines the enzyme activity of α-glucosidase and the screening methods for α-glucosidase inhibitors, provides an important perspective in the field of diabetes drug discovery and development, and provides a reference for future research.

Investigation of Transmission and Evolution of PEDV Variants and Co-Infections in Northeast China from 2011 to 2022.

Porcine epidemic diarrhea virus (PEDV) is a rapidly evolving virus that causes outbreaks in pig herds worldwide. Mutations in the S protein of PEDV have led to the emergence of new viral variants, which can reduce vaccine immunity against prevalent strains. To understand the infection and variation pattern of PEDV in China, an extensive epidemiological survey was conducted in northeast China from 2015 to 2022. The genetic diversity of enteroviruses co-infected with PEDV and the PEDV S gene was analyzed, common mutation patterns that may have led to changes in PEDV virulence and infectivity in recent years were identified, and structural changes in the surface of the S protein resulting from mutations in the PEDV S gene from 2011 to 2022 were reviewed. Of note, two distinct mutations in the emerging 2022 HEB strain were identified. These findings provide a basis for a better understanding of PEDV co-infection and genetic evolution in northeast China.

Role of fibroblast autophagy and proliferation in skin anti-aging.

Skin, as the outermost protective barrier of the body, becomes damaged with age and exposure to external stimuli. Dermal fibroblasts age and undergo apoptosis, which decreases collagen, collagen fibers, elastic fibers, hyaluronic acid, etc., leading skin to loss of elasticity and appearance of wrinkles. Skin aging is complex, involving several biological reactions，and various treatment methods are used to treat it. This review focuses on the importance of autophagy and cell proliferation in skin anti-aging, summarizes research progress on skin anti-aging by regulating autophagy and promoting the proliferation of dermal fibroblasts, and discusses future directions on skin anti-aging research.

Impaired serological response to COVID-19 vaccination following anticancer therapy: A systematic review and meta-analysis.

Owing to the high coronavirus disease 2019 (COVID-19)-related morbidity and fatality rate among patients with cancer, the introduction of COVID-19 vaccines is of profound significance in this fragile population. Accumulating data suggested that oncologic patients, especially those with anticancer therapy have an impaired immune response to COVID-19 vaccination. However, the exact effect of anticancer treatments on postvaccination response has not been elucidated yet. We, therefore, conducted a meta-analysis to evaluate the impact of treatments on response to COVID-19 vaccination in patients with cancer. A total of 39 studies were finally included comprising 11 075 oncologic patients. Overall, we found the humoral response was significantly decreased in patients undergoing anticancer treatments (odds ratio [OR] = 2.55, 95% confidence interval [CI]: 2.04-3.18) compared with those without active treatment. The seroconversion rates were significantly lower in patients with chemotherapy (OR = 3.04, 95% CI: 2.28-4.05), targeted therapy (OR = 4.72, 95% CI: 3.18-7.01) and steroid usage (OR = 2.19, 95% CI: 1.57-3.07), while there was no significant association between immunotherapy or hormonal therapy and seroconversion after vaccination. Subgroup analyses showed therapies with anti-CD20 antibody (OR = 11.28, 95% CI: 6.40-19.90), B-cell lymphoma 2 inhibitor (OR = 5.76, 95% CI: 3.64-9.10), and Bruton tyrosine kinase inhibitor (OR = 6.86, 95% CI: 4.23-11.15) were significantly correlated with the risk of negative humoral response to vaccination. In conclusion, our results demonstrated that specific oncologic therapies may significantly affect serological response to COVID-19 vaccines in patients with cancer. Thus, an adapted vaccination strategy taking the influence of active treatment into account is in need, and further research on the effect of the third dose of vaccine and the role of postvaccination cellular response in oncologic patients is also needed.

Characteristics and DGT Based Bioavailability of Cadmium in the Soil-Crop Systems from the East Edge of the Dongting Lake, China.

Contamination of heavy metals (including the cadmium, Cd) in agricultural soils has become an increased issue, posing a threat to the crop safety and human health. In order to evaluate the contamination characteristics and bioavailability of Cd in the soil−crop systems from the East edge of the Dongting Lake, four kinds of agricultural products for typical crops (rice, peanut, sweet potato, and corn) and corresponding rhizosphere soils were collected and analyzed for the Cd concentrations. The technique of diffusive gradients in thin-films (DGT) was applied to evaluate the Cd bioavailability in the rhizosphere soils. Concentrations of Cd ranged from 0.04 to 2.95 mg/kg (average 0.24 mg/kg) with 73.9% sites above the background levels, especially for paddy soils. Cd concentrations in the agricultural products ranged from 0.01 to 2.19 mg/kg (average 0.18 mg/kg), with Cd enrichment observed in the peanut samples. No obvious correlations (R2 < 0.25) were observed between the Cd concentrations in the agricultural products and total Cd concentrations in the rhizosphere soils, this indicated that the total Cd concentrations in the soils cannot predict the concentrations in the agricultural products of crops. While the DGT measured Cd concentrations showed good correlations (R2 = 0.64−0.90) with the concentrations in the most agricultural products of crops, which may be used to evaluate the safety of the soil and further safety of the agricultural products of crops. Overall, DGT showed a good potential for prediction of heavy metal bioavailability in soil since the DGT technique can simulate the sustained supply of heavy metals from solid to liquid in the soils.

Venlafaxine, an anti-depressant drug, induces apoptosis in MV3 human melanoma cells through JNK1/2-Nur77 signaling pathway.

Introduction: Venlafaxine is one of the most commonly used anti-depressant and antineoplastic drug. Previous studies have predicted venlafaxine as an anti-cancer compound, but the therapeutic effects of venlafaxine in melanoma have not yet been demonstrated. Nur77 is an orphan nuclear receptor that highly expressed in melanoma cells and can interact with Bcl-2 to convert Bcl-2 from an antiapoptotic to a pro-apoptotic protein. Method: We examined the effects of venlafaxine in MV3 cells in vitro and MV3 xenograft tumor in nude mice. Western-blot, PCR, TUNEL assay and immunofluorescence were used to reveal the growth of melanoma cells. Results: Here, our data revealed that venlafaxine could reduce the growth, and induce apoptosis of melanoma cells through a Nur77-dependent way. Our results also showed that treatment with venlafaxine (20 mg/kg, i.p.) potently inhibited the growth of melanoma cells in nude mice. Mechanistically, venlafaxine activated JNK1/2 signaling, induced Nur77 expressions and mitochondrial localization, thereby promoting apoptosis of melanoma cells. Knockdown of Nur77 and JNK1/2, or inhibition of JNK1/2 signaling with its inhibitor SP600125 attenuated the anti-cancer effects of venlafaxine. Conclusion: In summary, our results suggested venlafaxine as a potential therapy for melanoma.

[Study on the pharmacognosy identification and UV identification of Basella rubra].

OBJECTIVE: To provide reference for identification and development of Basella rubra. METHODS: Microscopic identification and UV spectrometry methods were used. RESULTS: Obvious characteristics were found in the tissue structures of the roots, stems and leaves . And Basella rubra showed some UV spectrometry characteristics. CONCLUSION: The results can be used as the reference for analyzing the quality of the crude drug.

[Microscopic identification and UV-Vis spectrum identification on Sapium sebiferum].

OBJECTIVE: To study the microscopic and UV-Vis spectrum characteristic of Sapium sebiferum. METHODS: The microscopic identification and UV-Vis spectrum identification were adopted. RESULTS: There were cluster crystals in cortical cells of roots and stems and parenchyma cells of the leaves. A few stone cells were found in cortex of the stem. The vascular bundles arranged in the form of a circle in the main vein of the leaves. It could be observed that many crystals and crystal fibers in the powder. Six kinds of solvent of crude drug had absorption peaks between 200 - 800 nm. CONCLUSION: These results can provide the scientific evidence for the establishment of standard for quality control and further study.

[Analysis of essential oil from the leaves and fruits of Eucalyptus tereticornis in Guangxi province by GC-MS].

OBJECTIVE: To Analyze the chemical composition and their relative contents of essential oil from the leaves and fruits of Eucalyptus tereticornis in Guangxi province. METHODS: The column temperature was controlled by a program with a capillary column HP-5 MS, and the MS analysis was performed with EI and quadrupole mass analyzer. The chemical compositions were identified by NIST98 searching and mass spectra comparing, and their relative contents were determined by using normalization method of chromatographic peak areas. RESULTS: 39 compounds constituting 96.69% of the oil of leaves were identified. The major components were eucalyptol (27.93%), 1R-alpha-pinene (22.60%), isopinocarveol (8.71%); 36 compounds constituting 93.50% of the oil of fruits were identified. The major components are 1R-alpha-pinene (32.88%), eucalyptol (13.64%), D-limonene (8.31%). CONCLUSION: The GC-MS is a simple, rapid and sensitive method.