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Pueraria lobata (Willd.) Ohwi, known as kudzu and used as a "longevity powder" in China, is an edible plant which is rich in flavonoids and believed to be useful for regulating blood sugar and treating diabetes, although the modes of action are unknown. Here, a total of 53 flavonoids including 6 novel compounds were isolated from kudzu using multidimensional preparative liquid chromatography. The flavonoid components were found to lower blood sugar levels, promote urine sugar levels in mice, and reduce the urine volume. Molecular docking and in vitro assays suggested that the antidiabetic effect of kudzu was attributed to at least three targets: sodium-dependent glucose transporter 2 (SGLT2), protein tyrosine phosphatase-1B (PTP1B), and alpha-glucosidase (AG). This study suggests a possible mechanism for the antidiabetic effect that may involve the synergistic action of multiple active compounds from kudzu.
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Flavonoides , Hipoglucemiantes , Extractos Vegetales , Proteína Tirosina Fosfatasa no Receptora Tipo 1 , Pueraria , Pueraria/química , Hipoglucemiantes/química , Hipoglucemiantes/farmacología , Flavonoides/química , Animales , Ratones , Proteína Tirosina Fosfatasa no Receptora Tipo 1/antagonistas & inhibidores , Proteína Tirosina Fosfatasa no Receptora Tipo 1/metabolismo , Humanos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Simulación del Acoplamiento Molecular , Masculino , alfa-Glucosidasas/metabolismo , alfa-Glucosidasas/química , Glucemia/metabolismo , Plantas Comestibles/químicaRESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Prostatitis and benign prostatic hyperplasia (BPH) are inflammations of the prostate gland, which surrounds the urethra in males. Jinqiancao granules are a traditional Chinese medicine used to treat kidney stones and this medicine consists of four herbs: Desmodium styracifolium (Osbeck) Merr., Pyrrosia calvata (Baker) Ching, Plantago asiatica L. and stigma of Zea mays L. AIM OF THE STUDY: We hypothesized that Jinqiancao granules could be a potential therapy for prostatitis and BPH, and this work aimed to elucidate active compounds in Jinqiancao granules and their target mechanisms for the potential treatment of the two diseases. MATERIALS AND METHODS: Jinqiancao granules were commercially available and purchased. Database-driven data mining and networking were utilized to establish a general correlation between Jinqiancao granules and the two diseases above. Ultra-performance liquid chromatography-mass spectrometry was used for compound separation and characterization. The characterized compounds were evaluated on four G-protein coupled receptors (GPCRs: GPR35, muscarinic acetylcholine receptor M3, alpha-1A adrenergic receptor α1A and cannabinoid receptor CB2). A dynamic mass redistribution technique was applied to evaluate compounds on four GPCRs. Nitric acid (NO) inhibition was tested on the macrophage cell line RAW264.7. Molecular docking was conducted on GPR35-active compounds and GPR35 crystal structure. Statistical analysis using GEO datasets was conducted. RESULTS: Seventy compounds were isolated and twelve showed GPCR activity. Three compounds showed potent GPR35 agonistic activity (EC50 < 10 µM) and the GPR35 agonism action of PAL-21 (Scutellarein) was reported for the first time. Docking results revealed that the GPR35-targeting compounds interacted at the key residues for the agonist-initiated activation of GPR35. Five compounds showed weak antagonistic activity on M3, which was confirmed to be a disease target by statistical analysis. Seventeen compounds showed NO inhibitory activity. Several compounds showed multi-target properties. An experiment-based network reflected a pharmacological relationship between Jinqiancao granules and the two diseases. CONCLUSIONS: This study identified active compounds in Jinqiancao granules that have synergistic mechanisms, contributing to anti-inflammatory effects. The findings provide scientific evidence for the potential use of Jinqiancao granules as a treatment for prostatitis and BPH.
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Hiperplasia Prostática , Prostatitis , Masculino , Humanos , Prostatitis/tratamiento farmacológico , Prostatitis/metabolismo , Hiperplasia Prostática/tratamiento farmacológico , Hiperplasia Prostática/metabolismo , Simulación del Acoplamiento Molecular , Próstata , Receptores Acoplados a Proteínas G/metabolismoRESUMEN
Basalt fiber (BF) has a high mechanical strength, excellent temperature resistance, good chemical stability, low energy consumption, and an environmentally friendly production process. In addition, BF-reinforced polymers (BFRPs) have good corrosion resistance and designability; thus, they meet the application requirements of electrical equipment, such as new conductors, insulating pull rods, and composite cross-arms. However, there are still a series of technical issues in the mass production of BF, and the stability of the products needs to be further improved. Therefore, the research on the production, modification, and application of BF is necessary. This paper discusses the chemical composition and production technology of BF, describes the morphology and properties of BF, summarizes the interface problems and modification methods of composites, and finally, introduces the application prospects of BF in the field of electrical materials, which is expected to provide a reference for the application and promotion of BFRP in the future.
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In order to promote the application of composite insulators in coastal areas with high temperature, high humidity and high salt, it is of great importance to develop matrix resin with salt corrosion resistance for composite core rods. In this study, bisphenol A epoxy resin was modified by blending with alicyclic epoxy resin (2021P). Three different proportions of 2021P/DGEBA blend resins (0% 2021P/DGEBA, 10% 2021P/DGEBA and 20% 2021P/DGEBA) were prepared, and the high salt medium corrosion test was carried out. The physicochemical (FTIR, DMA, TGA) and electrical properties (dielectric loss, leakage current and breakdown field strength) of the blend resin before and after aging were tested and analyzed, and the optimal blend proportion was determined. The results showed that after salt aging, the Tg of 0% 2021P/DGEBA decreased to 122.99 °C, while the Tg of 10% 2021P/DGEBA reached 134.89 °C; The leakage current of 0% 2021P/DGEBA increased to 48.994 µA, while that of 10% 2021P/DGEBA only increased to 44.549 µA; The breakdown field strength of 0% 2021P/DGEBA dropped to 40.36 kv/mm, while that of 10% 2021P/DGEBA only dropped to 43.63 kv/mm. The introduction of 2021P enhanced the salt corrosion resistance of the blend resin, which could hinder the penetration, diffusion and erosion of external media (such as Na+, Cl-, H2O, etc.) to the matrix resin. The comprehensive properties of 10% 2021P/DGEBA blend system reached the best, which was better than other blending resins, showing great application potential.
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With the application of the composite cross-arm in power systems, comprehensive anti-aging performance is a key factor to determine whether it can operate safely. In order to study the influence of the operating environment on the external insulation characteristics of composite cross-arms of distribution networks, various aging conditions such as voltage, rain, temperature, humidity, salt fog and ultraviolet light were simulated in a climate chamber based on the real operation conditions of the 10-kV composite cross-arm. A multi-factor aging test of composite cross-arms with two kinds of cross-section shapes (T-shaped and square) was carried out for 5000 h. The change trends of leakage current and flashover voltage of the composite cross-arms before and after aging were analyzed. Finally, the aging mechanism of the silicone rubber sheaths was analyzed to further explain the reasons for the change of external insulation performance of composite cross-arms. The results show that the leakage current rising rate of T-shaped and square composite cross-arms after aging increases significantly, and the minimum flashover voltage decreases to 58.3 kV and 49.502 kV, respectively. The results of FTIR, SEM and hydrophobic angle tests show that, after aging, the performance of the silicone rubber outer sheath material decreases in varying degrees. In general, UV aging has the greatest influence on the external insulation characteristics of composite cross arms. Generally speaking, after 5000 h of multi factor aging, although the external insulation characteristics of the 10-kV composite cross-arm decreases to a certain extent, there is still enough margin to meet the normal operation.
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Cardiac glycosides from fresh leaves of Nerium indicum were evaluated for its molluscicidal activity against Pomacea canaliculata (golden apple snail: GAS) under laboratory conditions. The results showed that LC(50) value of cardiac glycosides against GAS was time dependent and the LC(50) value at 96 h was as low as 3.71 mg/L, which was comparable with that of metaldehyde at 72 h (3.88 mg/L). These results indicate that cardiac glycosides could be an effective molluscicide against GAS. The toxicological mechanism of cardiac glucosides on GAS was also evaluated through changes of selected biochemical parameters, including cholinesterase (ChE) and esterase (EST) activities, glycogen and protein contents in hepatopancreas tissues of GAS. Exposure to sublethal concentrations of cardiac glycosides, GAS showed lower activities of EST isozyme in the later stages of the exposure period as well as drastically decreased glycogen content, although total protein content was not affected at the end of 24 and 48 h followed by a significant depletion at the end of 72 and 96 h. The initial increase followed by a decline of ChE activity was also observed during the experiment. These results suggest that cardiac glycosides seriously impair normal physiological metabolism, resulting in fatal alterations in major biochemical constituents of hepatopancreas tissues of P. canaliculata.
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Glicósidos Cardíacos/toxicidad , Moluscocidas/toxicidad , Nerium/química , Extractos Vegetales/toxicidad , Caracoles/efectos de los fármacos , Acetaldehído/análogos & derivados , Acetaldehído/toxicidad , Animales , Colinesterasas/metabolismo , Glucógeno/metabolismo , Isoenzimas/metabolismo , Dosificación Letal Mediana , Nerium/anatomía & histología , Extractos Vegetales/química , Hojas de la Planta/química , Caracoles/anatomía & histología , Caracoles/fisiologíaRESUMEN
OBJECTIVE: To study the attraction effect of the food attractants on Oncomelania hupensis. METHODS: Oncomelania snail food was prepared with the fermented kelp (Laminaria japonica) mixed with corn starch. Snails were fed with the food and kept for 12, 24, 36, and 48 h at 15, 25, 35 degrees C respectively. Meanwhile, snail-killing effect was tested by granules containing jack-in-the-pulpit (Arisama heterophyllum) with or without the fermented kelp under the condition of 25 degrees C, 30% or 60% soil humidity. RESULTS: The snail-attracting rate of the fermented kelp was affected by the temperature, highest under 25 degrees C and lowest under 35 degrees C at any time point, with a rate of 80.3% in 48 h at 25 degrees C which was higher than that of the control (17.0%) (P<0.01). The snail mortality rate in the group using jack-in-the-pulpit with fermented kelp (85.3%) was higher than that of the group without fermented kelp (26.8%) (P<0.05). The mortality under 60% of soil humidity was higher than that under 30% humidity (P<0.01). CONCLUSION: The fermented kelp shows a strong luring effect to the Oncomelania snails.
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Laminaria/química , Moluscocidas/farmacología , Caracoles/efectos de los fármacos , Animales , Fermentación , Schistosoma japonicum , Caracoles/parasitologíaRESUMEN
OBJECTIVE: To determine the visible light-induced photodegradation kinetics of two xanthene photosensitizers, phloxine B and uranine, in solution and on the surface of silica TLC plates, and to examine the phototoxicity of residues of degradation, which could provide valuable safety data on the two photosensitizers and other xanthene chemicals when applied in the environment. METHODS: UV-Vis absorption during photodegradation was monitored with a Unico 2102 spectrophotometer. Organic content of samples was measured with a Shimadzu TOC 4100. Phototoxicity tests were carried out using Saccharomyces cerevisiae with the methods modified from Daniels. RESULTS: When phloxine B and uranine degraded in solution, their apparent rate constant k was 0.0019 and 0.0027 min(-1), respectively. The total organic carbon (TOC) content decreased by approximately 50% during the 8 h irradiation period, which led to a gradual decrease in phototoxicity of the residues. The photodegradation of photosensitizers on the surface of silica TLC plates was much faster than that in the solution. The apparent rate constant k and the half life of phloxine B were 0.0073 min(-1) and 95 min, respectively. CONCLUSION: Visible light can rapidly induce photodegradation of phloxine B and uranine. The phototoxicity of residues is also decreased. The environmental risk of applications of phloxine B and uranine is minimal.
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Eosina I Azulada/toxicidad , Fluoresceína/toxicidad , Fármacos Fotosensibilizantes/toxicidad , Saccharomyces cerevisiae/efectos de los fármacos , Saccharomyces cerevisiae/efectos de la radiación , Eosina I Azulada/química , Fluoresceína/química , Cinética , Estructura Molecular , FotólisisRESUMEN
OBJECTIVE: To evaluate the molluscicidal activities of three Chinese plants N. indicum Mill, R stenoptera DC, and R. japonicum Houtt, and to clarify the molluscicidal mechanism. METHODS: N-butanol extracts and water extracts of the three plants were obtained. The reactions of EST isozyme, glycogen and total protein of snails to the plant extracts were studied. RESULTS: EST electrophoresis showed that EST was an important antidotal enzyme system and reacted strongly to environment. EST changed greatly during the whole exposure period so that it could be viewed as a pathological index of toxicity. Extracts decreased the glycogen content of the snails' soft tissues greatly, and also the protein content. CONCLUSION: All extracts show strong molluscicidal activity. The LD50 value of the water extract of N. indicum Mill is as low as 13.2 mg/L. EST can be viewed as a pathological index of toxicity. The energy metabolism abnormity is the key reason for the molluscicidal activities. The biochemical mechanism needs further research.