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Lilium brownii var. viridulum (Longya lily) is an edible vegetable and medicinal plant with the effects of moistening lungs, relieving coughs, and removing phlegm. In this study, a homogenous mannoglucan LLP11 was purified from Longya lily using membrane ultrafiltration followed by ion exchange chromatography. The Mw of LLP11 was 12.0 kDa. LLP11 exhibited a backbone of →4)-α-D-Glcp-(1 → and →4)-β-D-Manp-(1 → with a branch of T-α-D-Glcp-(1 → substituted at C-6 of →4,6)-α-D-Glcp-(1→. During the simulated digestion, LLP11 remained indigestible to digestive enzymes. Furthermore, through its interaction with the gut microbiota, LLP11 was able to significantly boost Bifidobacterium and decrease the harmful bacteria Klebsiella, that was linked to pneumonia. Additionally, LLP11 promoted the growth of B. pseudocatenulatum and B. longum and was utilized to produce acetic acid. Our findings introduced an alternative approach for the investigation of microbiota-targeted polysaccharides and underscored the potential of LLP11 as a prebiotic for supplementary treatment in respiratory diseases.

Evapotranspiration is a key driver of water and energy exchanges between terrestrial surfaces and the atmosphere, significantly influencing ecosystem balances. This study focuses on the Yellow River Basin (YRB), where evapotranspiration impacts both ecological dynamics and human activities. By analyzing actual evapotranspiration data from 1982 to 2017, this research provides insights into its spatial and temporal patterns within the YRB. Furthermore, a comprehensive assessment and comparative analysis were performed on four distinct evapotranspiration product datasets: GLDAS-Noah, ERA5-Land, GLEAM v3.8a, and MOD16A2. Employing the Geodetector model, the research identified seven key influencing factors—the digital elevation model (DEM), slope, aspect, precipitation, temperature, soil moisture, and normalized difference vegetation index (NDVI)—and analyzed their impact on evapotranspiration variations, yielding the following insights: (1) Based on the monthly-scale actual evapotranspiration dataset from 1982 to 2017, the annual average evapotranspiration in the YRB fluctuated between 375 and 473 mm, with an average value of 425 mm. A declining trend in the region’s overall evapotranspiration was discerned using the Theil–Sen median slope estimator and Mann–Kendall trend test. (2) The datasets from GLDAS-Noah, ERA5-Land, and GLEAM exhibited the highest correlation with the observed datasets, all exceeding a correlation coefficient of 0.96. In contrast, the MOD16A2 dataset showed the least favorable performance. The ERA5-Land dataset was particularly noteworthy for its close alignment with observational benchmarks, as evidenced by the lowest recorded root mean square error (RMSE) of 5.09 mm, indicative of its outstanding precision. (3) Employing the Geodetector model, a thorough analysis was conducted of the interactions between evapotranspiration and seven critical determinants. The findings revealed that precipitation and the NDVI were the most significant factors influencing evapotranspiration, with q-values of 0.59 and 0.42 in 2010, and 0.71 and 0.59 in 2015, respectively. These results underscore their pivotal role as the main drivers of evapotranspiration variability within the YRB. Conversely, the q-values for slope in 2010 and 2015 were only 0.01 and nearly zero, respectively, indicating their minimal impact on the dynamics of evapotranspiration in the YRB.

As a major grain-producing province in China’s Central Plains, Henan Province is severely impacted by drought, making the study of agricultural drought characteristics in the region crucial. Theil–Sen (Sen) trend analysis, the Mann–Kendall (M-K) test and the Hurst index method were used to systematically analyze the spatial variation characteristics of agricultural drought based on the Temperature Vegetation Dryness Index (TVDI). The results show that: (1) The drought occurs in central, northwestern and southern Henan on an annual scale. The drought situation will continue to increase in northern, eastern northeastern and central Henan. (2) The drought in spring, summer and winter showed an increasing trend, but the opposite trend was observed in autumn. The increasing trend of drought in each season is mainly distributed in northern, central and eastern Henan. (3) The drought in January, February, April, July, September and December showed an increasing trend, while the drought in the other 6 months showed a decreasing trend. The increase in drought during July and August was not pronounced, while the drought situation in September remained largely unchanged. The distribution of drought across the other months exhibited varying patterns across different regions. Overall, the drought trend in Henan Province is on the rise, displaying distinct seasonal and regional patterns in its temporal and spatial distribution. The results can provide a reference for Henan Province to formulate effective measures of drought resistance and disaster reduction to ensure grain production.

Drought, as a recurring extreme climatic event, inflicts diverse impacts on ecological systems, agricultural productivity, water resources, and socio-economic progress globally. Discerning the drought patterns within the evolving environmental landscape of the Yellow River Basin (YRB) is imperative for enhancing regional drought management and fostering ecological conservation alongside high-quality development. This study utilizes meteorological drought indices, the Standardized Precipitation Evapotranspiration Index (SPEI) and the self-calibrating Palmer Drought Severity Index (scPDSI), for a detailed spatiotemporal analysis of drought conditions. It examines the effectiveness of these indices in the basin’s drought monitoring, offering a comprehensive insight into the area’s drought spatiotemporal dynamics. The findings demonstrate the following: (1) SPEI values exhibit distinct fluctuation patterns at varying temporal scales, with more pronounced fluctuations at shorter scales. Drought years identified via the 12-month SPEI time scale include 1965, 1966, 1969, 1972, 1986, 1997, 1999, 2001, and 2006. (2) A modified Mann–Kendall (MMK) trend test analysis of the scPDSI time series reveals a worrying trend of intensifying drought conditions within the basin. (3) Correlation analysis between SPEI and scPDSI across different time scales yields correlation coefficients of 0.35, 0.54, 0.69, 0.76, and 0.62, highlighting the most substantial correlation at an annual scale. Spatial correlation analysis conducted between SPEI and scPDSI across various scales reveals that, within diverse temporal ranges, the correlation peaks at a 12-month time scale, with subsequent prominence observed at 6 and 24 months. This observed pattern accentuates the applicability of scPDSI in the monitoring of medium- to long-term drought phenomena.

A novel bis-γ-butyrolactone grifolamine A (1), the first γ-butyrolactone dimer from nature, together with three known γ-butyrolactones (2–4), was isolated from the byproduct from Grifola frondosa polysaccharides preparation process. The structure and stereochemistry of grifolamine A (1) were elucidated by extensive spectroscopic analysis combined with quantum chemical calculation. The biosynthetic origin of compound 1, as well as 2–4 was proposed. Grifolamine A (1) showed an intense inhibition against α-glucosidase in vitro. The underlying inhibitory mechanism was revealed by surface plasmon resonance (SPR), molecular docking, molecular dynamics (MD) simulation and binding free energy calculation. SPR revealed that grifolamine A exhibited a strong affinity to α-glucosidase with an equilibrium dissociation constant (KD) value of 1.178 × 10−4 M. Molecular docking manifested that grifolamine A sat at the active pocket of α-glucosidase by van der Waals force, alkyl interaction and carbon hydrogen bonds, and consequently changed the micro-environmental structure of α-glucosidase. MD simulation revealed that grifolamine A had high binding affinity to α-glucosidase with average free energy of −25.2 ± 3.2 kcal/mol. Free energy decomposition indicated amino acid residues including PHE298, PHE308, PHE309, PHE155 and ARG310 at the binding pocket played a strongly positive effect on the interaction between grifolamine A and α-glucosidase. Our findings provide valuable information for the design and development of novel α-glucosidase inhibitors based on γ-butyrolactone skeleton.

In this paper, we reported the hypouricemic effect of 2,4-dihydroxybenzoic acid methyl ester (DAE), a component of Ganoderma applanatum, in hyperuricemic mice through inhibiting XOD and down-regulating URAT1. Computationally, DAE showed a high similarity to allopurinol and depicted a high affinity in docking to XOD. In vitro, DAE exhibited an inhibitory effect against XOD. Importantly, DAE demonstrated a remarkable hypouricemic effect, decreasing serum uric acids (SUAs) of hyperuricemic mice (407 ± 31 μmol/L) to 195 ± 23, 145 ± 33 and 134 ± 16 μmol/L (P

The chemical structure of GLP-1, a novel water-soluble heteropolysaccharide purified Ganoderma leucocontextum fruiting bodies, has been characterized in our previous study. This study aimed to investigate the immunostimulatory activity of GLP-1 in vitro and in vivo by using RAW264.7 macrophages and cyclophosphamide-induced immunosuppressed mice model. Results showed that GLP-1 was able to enhance phagocytic activity and promote the production of reactive oxygen species, nitric oxide, tumor necrosis factor-α, interleukin-6, and monocyte chemoattractant protein-1 in RAW264.7 macrophages. Moreover, GLP-1 could activate mitogen-activated protein kinase, phosphatidylinositol-3-kinase/protein kinase B, and nuclear factor-kappa B signaling pathways through toll-like receptor 2 and dectin-1 receptors. Furthermore, GLP-1 increased the thymus index, serum immunoglobulin levels, and percentage of CD3+ T lymphocytes in cyclophosphamide-induced immunosuppressed mice. These results demonstrated that GLP-1 possessed significant immunostimulatory effects in vivo and in vitro and could be developed as an effective immunomodulator for application in functional foods.

Context Poria coco F.A.Wolf (Polyporaceae) dispels dampness and promotes diuresis implying hypouricaemic action. Objective To examine hypouricaemic action of Poria coco. Materials and methods Ethanol extract (PCE) was prepared by extracting the sclerotium of P. cocos with ethanol, and the water extract (PCW) was produced by bathing the remains with water. PCE and PCW (50, 100 and 200 mg/kg, respectively) were orally administered to hyperuricemic Kunming mice (n = 8) to examine its hypouricaemic effect. Also, molecular docking was performed. Results P. cocos showed excellent hypouricaemic action, decreasing the serum uric acid of hyperuricaemia (HUA) control (526 ± 112 μmol/L) to 178 ± 53, 153 ± 57 and 151 ± 62 μmol/L (p

In this study, Ganoderma lucidum crude polysaccharide (GLP) was found to have protective effect on liver damage in mice caused by restraint stress through improving oxidative status. Two polysaccharides, including a neutral β-glucan (GLPB2) and an acidic β-glucan (GLPC2) were purified from GLP through anion-exchange chromatography (AEC) combined with gel permeation. GLPC2, with an average molecular weight of 20.56 kDa, exhibited stronger hepatoprotective effect against H2O2-induced liver injury in HepG2 cells compared to GLPB2. Glycosidic residues and NMR analysis comprehensively revealed that GLPC2 contained d-Glcp-(1→, →3)-d-Glcp-(1→, →4)-d-Glcp-(1→, →6)-d-Glcp-(1→, →3, 6)-d-Glcp-(1 → and → 4)-d-GlcpA-(1 → . AEC can be an effective technique for separating β-glucans into neutral and acidic fractions by different ionic strength buffer. The findings provided a theoretical basis for the potential application of G. lucidum polysaccharides as a hepatoprotective in food and pharmaceutical industry.

A water-soluble heteropolysaccharide (SGP2-1) was purified from Suillus granulatus fruiting bodies by anion-exchange chromatography and gel permeation chromatography. The structural characteristics were analyzed by high-performance gel permeation chromatography, high-performance liquid chromatography, Fourier transform infrared spectroscopy, gas chromatography-mass spectrometry, and nuclear magnetic resonance spectroscopy. The immunostimulatory activity was investigated using RAW 264.7 macrophages. Results showed that SGP2-1 with weight average molecular weight of 150.75 kDa was composed of mannose, glucose, and xylose. The backbone of SGP2-1 was mainly composed of → 4)-α-Glcp-(1→, and the terminal group α-d-Glcp → was linked to the main chain by O-6 position. SGP2-1 could significantly enhance pinocytic capacity, reactive oxygen species production, and cytokines secretion. SGP2-1 exerted immunomodulatory effects through interacting with toll-like receptor 2, and activating mitogen-activated protein kinase, phosphatidylinositol-3-kinase/protein kinase B, and nuclear factor-kappa B signaling pathways. These findings indicated that SGP2-1 could be explored as a potential immunomodulatory agent for application in functional foods.

Abstract Ganoderma leucocontextumGanoderma leucocontextumG. leucocontextumG. leucocontextum and Ganoderma lucidumGanoderma leucocontextumG. lucidumG. leucocontextumG. leucocontextum

Ganoderma lucidum is an important medicinal mushroom widely cultured in Asian countries. Exopolysaccharides are bioactive compounds of G. lucidum with health benefits. Limited exopolysaccharide content hinders its extraction from G. lucidum. The addition of Tween80 had an enhanced effect on G. lucidum exopolysaccharide production in submerged fermentation. However, the mechanism of this effect remains unclear. In this study, we report on a high-quality assembly of G. lucidum strain yw-1-5 to lay the foundation for further transcriptome analysis. The genome sequence was 58.16 Mb and consisted of 58 scaffolds with an N50 of 4.78 Mb. A total of 13,957 protein-coding genes were annotated and Hi-C data mapped to 12 pseudo-chromosomes. Genes encoding glycosyltransferases and glycoside hydrolases were also obtained. Furthermore, RNA-seq was performed in a Tween80-treated group and control group for revealing the enhanced effect of Tween80 on exopolysaccharide production. In total, 655 genes were identified as differentially expressed, including 341 up-regulated and 314 down-regulated. Further analysis of differentially expressed genes showed that groups of MAPK, amino sugar and nucleotide sugar metabolism, autophagy, ubiquitin-mediated proteolysis, peroxisome, starch and sucrose metabolism, TCA cycle, glycolysis/gluconeogenesis KEGG pathway, glycosyltransferases and glycoside hydrolases played important roles in the enhanced effect of Tween80 on exopolysaccharide production. This work provides a valuable resource for facilitating our understanding of the synthesis of polysaccharides and accelerating the breeding of new strains with a high content of exopolysaccharides.

Inhibiting the intestinal α-glucosidase can effectively control postprandial hyperglycemia for type 2 diabetes mellitus (T2DM) treatment. In the present study, we reported the binding interaction of betulinic acid (BA), a pentacyclic triterpene widely distributed in nature, on α-glucosidase and its alleviation on postprandial hyperglycemia. BA was verified to exhibit a strong inhibitory effect against α-glucosidase with an IC50 value of 16.83 ± 1.16 μM. More importantly, it showed a synergistically inhibitory effect with acarbose. The underlying inhibitory mechanism was investigated by kinetics analysis, surface plasmon resonance (SPR) detection, molecular docking, molecular dynamics (MD) simulation and binding free energy calculation. BA showed a non-competitive inhibition on α-glucosidase. SPR revealed that it had a strong and fast affinity to α-glucosidase with an equilibrium dissociation constant (KD) value of 5.529 × 10−5 M and a slow dissociation. Molecular docking and MD simulation revealed that BA bound to the active site of α-glucosidase mainly due to the van der Waals force and hydrogen bond, and then changed the micro-environment and secondary structure of α-glucosidase. Free energy decomposition indicated amino acid residues such as PHE155, PHE175, HIE277, PHE298, GLU302, TRY311 and ASP347 of α-glucosidase at the binding pocket had strong interactions with BA, while LYS153, ARG210, ARG310, ARG354 and ARG437 showed a negative contribution to binding affinity between BA and α-glucosidase. Significantly, oral administration of BA alleviated the postprandial blood glucose fluctuations in mice. This work may provide new insights into the utilization of BA as a functional food and natural medicine for the control of postprandial hyperglycemia.

Side effects of chemotherapy are burning questions for physicians and patients involved in cancers. Ganoderma lucidum is a widely consumed traditional Chinese medicine and edible mushroom with multiple functional properties. The present study aims to investigate the potential of polysaccharides from spore of G. lucidum (SGP) on small intestinal barrier function recovery against paclitaxel (PTX) challenge in a breast cancer mice model and IEC-6 cell line. The 4T1 tumor-bearing mice were treated with PTX together with four-week daily oral administration of SGP. Results indicated that combination of PTX and SGP reversed body weight lost and remolded the histology of small intestine, accompanied with promoted proliferation but suppressed apoptosis in intestinal cells. Intestinal barrier function was enhanced by the combination as indicated by reduced endotoxemia and the up-regulation of tight junction proteins, including Zonula occludens-1 (ZO-1), E-cadherin, β-catenin and Occludin. The protection of SGP was further confirmed in IEC-6 cells affected by PTX in vitro. The combination treatment prevented PTX-induced apoptosis in IEC-6 by inhibiting microtubule polymerization, and the aforementioned tight junction proteins were also upregulated. These findings suggest a promising protective effect of SGP against small intestinal barrier injury caused by PTX, highlighting its clinical implication against the chemotherapy side effects.

Inflammatory bowel disease (IBD) is a chronic relapsing inflammation involving the gut system, and disequilibrium of T helper (Th) cell paradigm has been recognized as critical pathogenesis. Pycnoporus sanguineus (L.) Murrill is a species of the white-rot basidiomycetes listed as food- and cosmetic-grade microorganisms. In this study, anti-inflammatory activity of the ethanol extract from P. sanguineus (PSE) was investigated in dextran sulfate sodium (DSS)-induced experimental colitis model. PSE recovered the DSS-caused weight loss, reversed the colon shortening, and ameliorated the histopathological lesion in colon, resulting in lower disease activity index (DAI). Levels of serumal lipopolysaccharide (LPS), colonic myeloperoxidase (MPO) in the colitis-suffering mice were declined by PSE treatment. PSE also improved the mucosal integrity by enhancing the expression of tight junction and adherens junction proteins in the colon, including ZO-1, occludin, claudin-1, and E-cadherin. Besides, PSE reduced helper T cells (Th) in the colon, together with an evident decrease of several Th cell-related cytokines. Moreover, it was found that in vitro, PSE suppressed T cells and the Th subset upon Concanavalin A (ConA)-stimulation by inducing apoptosis. In summary, PSE displayed a remission on the colitis-related inflammation, which would possibly rely on the epithelial barrier restoration by suppressing Th cells via apoptosis induction, highlighting a promising potential in the treatment for IBD.

Triple-negative breast cancer (TNBC) is an aggressive disease with worst prognosis than other subtypes of breast cancer. Owing to the lack of hormone receptors and HER2 expression on TNBC cells, patients do not have targeted therapy options available with other breast cancer subtypes. Extensive efforts have been made to identify novel therapeutics against TNBC. Interestingly, recent studies had shown that plant-derived natural products could modulate the autophagy and induce the breast cancer cells death. Seed of Brucea javanica has been used as an important traditional Chinese medicine against cancers. In the present study, the anti-breast cancer potential of ethanol crude extracts from B. javanica seed (BJE) was explored. Data demonstrated that BJE could inhibit the TNBC cell line MDA-MB-231 proliferation and induced apoptosis. In the cells exposed to BJE, protein expressions of UNC-51-like kinase-1 (ULK1) and Beclin-1 and the ratio of light chain 3 II/I (LC3 II/I) were reduced, while the expression of p62 was increased, indicating an inhibition on autophagy. Moreover, BJE promoted the phosphorylation of mammalian target of rapamycin (mTOR), phosphatidylinositol 3-kinase (PI3K), and Akt in MDA-MB-231. BJE also suppressed the MDA-MB-231 tumor growth in vivo. Coincide with the results in vitro, autophagy in the tumor tissue was weakened as indicated by decreased ratio of LC 3 II/I and Beclin-1 accompanied by enhanced phosphorylation of mTOR, which confirmed that autophagy restraint via the PI3K/Akt/mTOR signaling pathway contributes to the suppression by BJE. Notably, no noticeable toxicity in non-targeted organs was found, including small intestine, liver, and kidney. Taken together, this study revealed anti-breast cancer activity of BJE based on autophagy restraint, highlighting its clinical importance as a novel natural agent against TNBC.

Previously, polysaccharides with hypoglycemic effects from G. frondosa were reported by us. To explore compounds against α-glucosidase and human tumor cells, three extractive fractions (GF-1–GF-3) were prepared from G. frondosa ethanol extraction (GF) by chromatographic column. Rather than GF-1 and GF-2, the fraction GF-3 demonstrated inhibitory actions against α-glucosidase and proliferation of human tumor cells dominantly. To identify the bioactive compounds in GF-3, one new compound named pyrrolefronine together with 19 known ones, which included seven pyrrole alkaloids, nine ergosterols and three others, were isolated and characterized from GF-3. Significantly, pyrrole alkaloids were found in G. frondosa for the first time, showing potent inhibition against α-glucosidase. Obtained ergosterols displayed inhibition against proliferation of tumor cells. This study provides a basis for further development and utilization of G. frondosa as natural nutraceuticals and functional food ingredients.

Grifola frondosa (GF) has been exploited as herb medicine for metabolic diseases and also as tasty food in Asia. Water (GFW) and ethanol (GFE) extracts produced remarkable hypouricemic effects, thereby decreasing the levels of serum uric acid from 240 μmol/L (hyperuricemia control, P

Two low-molecular-weight polysaccharides (GLP-1 and GLP-2) were purified from Ganoderma leucocontextum fruiting bodies, and their physicochemical properties and antioxidant activities were investigated and compared in this study. The results showed that GLP-1 and GLP-2 were mainly composed of mannose, glucose, galactose, xylose, and arabinose, with weight-average molecular weights of 6.31 and 14.07 kDa, respectively. Additionally, GLP-1 and GLP-2 had a similar chain conformation, crystal structure, and molecular surface morphology. Moreover, GLP-1 exhibited stronger antioxidant activities than GLP-2 in five different assays: 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), hydroxyl radical, superoxide anion radical, ferric reducing antioxidant power (FRAP), and oxygen radical antioxidant capacity (ORAC). The main linkage types of GLP-1 were found to be →4)-α-D-Glcp-(1→, →4)-β-D-Glcp-(1→, →3)-β-D-Glcp-(1→, →6)-β-D-Galp-(1→, →6)-α-D-Glcp-(1→, →4,6)-α-D-Glcp-(1→, and Glcp-(1→ by methylation analysis and nuclear magnetic resonance (NMR) spectroscopy. In addition, GLP-1 could protect NIH3T3 cells against tert-butyl hydroperoxide (tBHP)-induced oxidative damage by increasing catalase (CAT) and glutathione peroxidase (GSH-Px) activities, elevating the glutathione/oxidized glutathione (GSH/GSSG) ratio, and decreasing the malondialdehyde (MDA) level. These findings indicated that GLP-1 could be explored as a potential antioxidant agent for application in functional foods.

Agrocybe aegerita has long been utilized for promoting diuresis in traditional Chinese medicine (TCM) with a close correlation to hypouricemia. Ethanol (AAE) and water (AAW) extracts of the compound led to a remarkable decrease in serum uric acid levels (SUA) in hyperuricemia mice, approaching that of the normal control. Both AAE and AAW exhibited suppression effects on hepatic xanthine oxidase (XOD) activities and elevation effects on renal OAT1 (organic anion transporter 1). However, only little negative impact was observed on the inner organ functions. The molecular docking was used to screen our in-home compound database for A. aegerita, and four compounds including 2-formyl-3,5-dihydroxybenzyl acetate, 2,4-dihydroxy-6-methylbenzaldehyde, 2-(6-hydroxy-1H-indol-3-yl)acetamide, and 6-hydroxy-1H-indole-3-carbaldehyde (HHC) were identified as potential active compounds. Their inhibitory mechanism on XOD might be attributed to their localization in the tunnel for the entrance of substrates to XOD active site, preventing the entrance of the substrates. To confirm the activity of the screened compounds experimentally, HHC was selected due to its high ranking and availability. The assaying result suggested the significant inhibitory activity of HHC on XOD. Also, these compounds were predicted to carry good ADME (absorption, distribution, metabolism, and excretion) properties, thereby necessitating further investigation. The current results provided an insight into the hypouricemic effects of macrofungi and their bioactives, which might provide the significant theoretical foundation for identifying and designing novel hypouricemia compounds.

Ganoderma applanatum (G. applanatum) dispels wind to eliminate dampness and exhibited nephron- and liver-protective effects as noted in Chinese herbal classic literature; it might also affect hyperuricemia. Therefore, we examined the hypouricemia effects and mechanisms underlying G. applanatum on chemical-induced hyperuricemia in mice. Ethanol (GAE) and water (GAW) extracts were prepared by extracting G. applanatum in ethanol (GAE), followed by bathing the remains in water to yield GAW. GAE and GAW were administered orally at different doses to hyperuricemia mice, while allopurinol and benzbromarone served as positive controls. Both GAE and GAW showed remarkable hypouricemia activities, rendering a substantial decline in the SUA (serum uric acid) level in hyperuricemia control (P < 0.01). Moreover, the urine uric acid (UUA) levels were enhanced by GAE and GAW. In contrast to the evident renal toxicity of allopurinol, GAE and GAW did not show a distinct renal toxicity. Almost no suppressing effect was observed on the XOD activities. However, compared to the hyperuricemia control, OAT1 was elevated remarkably in mice drugged with GAE and GAW, while GLUT9 was significantly decreased. Similar to benzbromarone, GAE decreased the URAT1 protein levels significantly (P < 0.01), while GAW did not display a similar effect. GAE and GAW downregulated the level of CNT2 proteins in the gastrointestinal tract of hyperuricemia mice. Thus, G. applanatum produced outstanding hypouricemic effects, mediated by renal OAT1, GLUT9, and URAT1 and gastrointestinal CNT2 that might elevate urine uric secretions and decline in the absorption of purine in the gastrointestinal tracts. G. applanatum showed little negative influence on inner organs. By docking screening, four top-ranked compounds were identified that necessitated further investigation.Compounds: potassium oxonate, hypoxanthine, allopurinol, benzbromarone.

Droughts represent the most complex and damaging type of natural disaster, and they have taken place with increased frequency in China in recent years. Values of the standardized precipitation evapotranspiration index (SPEI) calculated using station-based meteorological data collected from 1961 to 2013 in the middle and lower reaches of the Yangtze River Basin (MLRYRB) are used to monitor droughts. In addition, the SPEI is determined for different timescales (1, 3, 6, and 12 months) to characterize dry or wet conditions in this study area. Moreover, remote sensing methods can cover large areas, and multispectral and temporal observations are provided by satellite sensors. The temperature vegetation dryness index (TVDI) is selected to permit assessment of drought conditions. In addition, the correlation between the SPEI and TVDI values is calculated. The results show that the SPEI values over different timescales reflect complex variations in drought conditions and have been well applied in the MLRYRB. Droughts occurred on an annual basis in 1963, 1966, 1971, 1978, 1979, 1986, 2001, 2011, and 2013, particularly 2011. In addition, the regional average drought frequency in the study area during 1961–2013 is 30%, as determined using the SPEI. An analysis of the correlation between the monthly values of the TVDI and the SPEI-3 shows that a negative relationship exists between the SPEI-3 and the TVDI. That is, smaller TVDI values are associated with greater SPEI-3 values and reduced drought conditions, whereas larger TVDI values are associated with smaller SPEI-3 values and enhanced drought conditions. Therefore, this study of the relationship between the SPEI and the TVDI can provide a basis for government to mitigate the effects of drought.

Recently, we've reported the anti-hyperuricemic effects of Cordyceps militaris. As a characteristic compound of C. militaris, we hypothesized that cordycepin may play a role in preventing hyperurecimia. Remarkably, cordycepin produced important anti-hyperuricemic actions, decreasing SUA (serum uric acid) to 216, 210, and 203 μmol/L (P < 0.01) at 15, 30, and 60 mg/kg in comparison of hyperuricemic control (337 μmol/L), closing to normal control (202 μmol/L). Elisa, RT-PCR and western blot analysis demonstrated that the actions may be attributed to its downregulation of uric acid transporter 1 (URAT1) in kidney. Serum creatinine levels and blood urine nitrogen and liver, kidney, and spleen coefficients demonstrated that cordycepin may not impact liver, renal, and spleen functions. In addition, we used computational molecular simulation to investigate the binding mechanism of cordycepin. Of which, van der Waals interaction dominated the binding. Residues TRP290, ARG17, ALA408, GLY411, and MET147 contributed mainly on nonpolar energy. This provided the theoretical guidance to rationally design and synthesis novel URAT1 inhibitors.

This study was carried out to isolate chemical constituents from the lipid enriched fraction of Ganoderma lucidum extract and to evaluate their anti-proliferative effect on tumor cells and human umbilical vein endothelial cells (HUVECs). Ergosterol derivatives (1–14) were isolated and purified from the lipid enriched fraction of G. lucidum. Their chemical structures were established by spectroscopic analyses or by comparison of mass and NMR spectral data with those reported previously. Amongst, compound 1 was purified and identified as a new one. All the compounds were evaluated for their anti-proliferative effect on human tumor cells and HUVECs in vitro. Compounds 9–13 displayed inhibitory activity against two types of human tumor cells and HUVECs, which indicated that these four compounds had both anti-tumor and anti-angiogenesis activities. Compound 2 had significant selective inhibition against two tumor cell lines, while 3 exhibited selective inhibition against HUVECs. The structure–activity relationships for inhibiting human HepG2 cells were revealed by 3D-QASR. Ergosterol content in different parts of the raw material and products of G. lucidum was quantified. This study provides a basis for further development and utilization of ergosterol derivatives as natural nutraceuticals and functional food ingredients, or as source of new potential antitumor or anti-angiogenesis chemotherapy agent.

Soil moisture is an important indicator that is widely used in meteorology, hydrology, and agriculture. Two key problems must be addressed in the process of downscaling soil moisture: the selection of the downscaling method and the determination of the environmental variables, namely, the influencing factors of soil moisture. This study attempted to utilize machine learning and data mining algorithms to downscale the Advanced Microwave Scanning Radiometer-Earth Observing System (AMSR-E) soil moisture data from 25 km to 1 km and compared the advantages and disadvantages of the random forest model and the Cubist algorithm to determine the more suitable soil moisture downscaling method for the middle and lower reaches of the Yangtze River Basin (MLRYRB). At present, either the normalized difference vegetation index (NDVI) or a digital elevation model (DEM) is selected as the environmental variable for the downscaling models. In contrast, variables, such as albedo and evapotranspiration, are infrequently applied; nevertheless, this study selected these two environmental variables, which have a considerable impact on soil moisture. Thus, the selected environmental variables in the downscaling process included the longitude, latitude, elevation, slope, NDVI, daytime and nighttime land surface temperature (LST_D and LST_N, respectively), albedo, evapotranspiration (ET), land cover (LC) type, and aspect. This study achieved downscaling on a 16-day timescale based on Moderate Resolution Imaging Spectroradiometer (MODIS) data. A comparison of the random forest model with the Cubist algorithm revealed that the R2 of the random forest-based downscaling method is higher than that of the Cubist algorithm-based method by 0.0161; moreover, the root-mean-square error (RMSE) is reduced by 0.0006 and the mean absolute error (MAE) is reduced by 0.0014. Testing the accuracies of these two downscaling methods showed that the random forest model is more suitable than the Cubist algorithm for downscaling AMSR-E soil moisture data from 25 km to 1 km in the MLRYRB, which provides a theoretical basis for obtaining high spatial resolution soil moisture data.

Precipitation plays an important role in the global water cycle, in addition to material and energy exchange processes. Therefore, obtaining precipitation data with a high spatial resolution is of great significance. We used a geographically weighted regression (GWR)-based downscaling model to downscale Tropical Rainfall Measuring Mission (TRMM) 3B43 precipitation data over the middle and lower reaches of the Yangtze River Basin (MLRYRB) from a resolution of 0.25° to 1 km on an annual scale, and the downscaled results were calibrated using the geographical differential analysis (GDA) method. At present, either the normalized difference vegetation index (NDVI) or a digital elevation model (DEM) is selected as the environmental variable in the downscaling models. However, studies have shown that the relationship between the NDVI and precipitation gradually weakens when precipitation exceeds a certain threshold. In contrast, the enhanced vegetation index (EVI) overcomes the saturation shortcomings of the NDVI. Therefore, this study investigated the performances of EVI-derived and NDVI-derived downscaling models in downscaling TRMM precipitation data. The results showed that the NDVI performed better than the EVI in the annual downscaling model, possibly because this study used the annual average NDVI, which may have neutralized detrimental saturation effects. Moreover, the accuracy of the downscaling model could be effectively improved after correcting for residuals and calibrating the model with the GDA method. Subsequently, the downscaled rainfall was closer to the actual weather station rainfall observations. Furthermore, the downscaled results were decomposed into fractions to obtain monthly precipitation data, showing that the proposed method by utilizing the GDA method could improve not only the spatial resolution of remote sensing precipitation data, but also the accuracy of data.

As the water source area for the middle route of China’s South-to-North Water Diversion Project, the upper Hanjiang basin is of central concern for future management of the country’s water resources. The upper Hanjiang is also one of the most flood-prone rivers in China. This paper explores the process of extreme floods by using multivariate analysis to characterize flood and precipitation event data in combination, for historical data and simulated data from global climate models. The results suggested that the generalized extreme value and Gamma models better simulated the extreme precipitation and flood volume sequence than the generalized Pareto model for the annual maximum series, while the generalized Pareto distribution model was the best-fit model for peaks over threshold series. For the two-dimensional joint distributions of precipitation and flood volume, the Frank Copula was preferred in simulation of the annual maximum flood series whereas the Gumbel Copula was the most appropriate function to simulate the points over threshold flood series. We concluded that, compared with the traditional univariate approach, multivariate statistical analysis produced flood estimates that were more physically based and statistically sound and carried lower risk for flood design purposes.

Precipitation is the core data input to hydrological forecasting. The uncertainty in precipitation forecast data can lead to poor performance of predictive hydrological models. Radar-based precipitation measurement offers advantages over ground-based measurement in the quantitative estimation of temporal and spatial aspects of precipitation, but errors inherent in this method will still act to reduce the performance. Using data from White Lotus River of Hubei Province, China, five methods were used to assimilate radar rainfall data transformed from the classified Z-R relationship, and the postassimilation data were compared with precipitation measured by rain gauges. The five sets of assimilated rainfall data were then used as input to the Xinanjiang model. The effect of precipitation data input error on runoff simulation was analyzed quantitatively by disturbing the input data using the Breeding of Growing Modes method. The results of practical application demonstrated that the statistical weight integration and variational assimilation methods were superior. The corresponding performance in flood hydrograph prediction was also better using the statistical weight integration and variational methods compared to the others. It was found that the errors of radar rainfall data disturbed by the Breeding of Growing Modes had a tendency to accumulate through the hydrological model.

Inonotus obliquus is an edible mushroom and also a remedy against various diseases, especially metabolic syndrome. In this paper we report the actions of an ethanol extract of I. obliquus (IOE) against hyperuricemia in hyperuricemic mice, and the screen of bioactives. The extract (IOE) was prepared by extracting I. obliquus at 65 °C with ethanol, and characterized by HPLC. IOE at low, middle, and high doses reduced serum uric acid (SUA) of hyperuricemic mice (353 μmol/L) to 215, 174, and 152 μmol/L (p < 0.01), respectively, showing similar hypouricemic effectiveness to the positive controls. IOE showed a non-toxic impact on kidney and liver functions. Of note, IOE suppressed xanthine oxidase (XOD) activity in serum and liver, and also down-regulated renal uric acid transporter 1 (URAT1). Four compounds hit highly against XOD in molecular docking. Overall, the four compounds all occupied the active tunnel, which may inhibit the substrate from entering. The IC50 of betulin was assayed at 121.10 ± 4.57 μM, which was near to that of allopurinol (148.10 ± 5.27 μM). Betulin may be one of the anti-hyperuricemia bioactives in I. obliquus.

Conventionally, benzophenone-type molecules are beneficial for alleviating the UV exposure of humans. More importantly, various compounds with this skeleton have demonstrated various biological activities. In this paper, we report the anti-hyperuricemic effect of the benzophenone compound 2-hydroxy-4-methoxybenzophenone-5-sulfonic acid (HMS). Preliminarily, its molecular docking score and xanthine oxidase (XOD) inhibition suggested a good anti-hyperuricemic effect. Then, its anti-hyperuricemic effect, primary mechanisms and general toxicity were examined on a hyperuricemic mouse model which was established using potassium oxonate and hypoxanthine together. HMS demonstrated a remarkable anti- hyperuricemic effect which was near to that of the control drugs, showing promising perspective. General toxicity was assessed and it showed no negative effects on body weight growth and kidney function. Moreover, anti-inflammatory action was observed for HMS via spleen and thymus changes. Its anti-hyperuricemic mechanisms may be ascribed to its inhibition of XOD and its up-regulation of organic anion transporter 1 (OAT1) and down-regulation of glucose transporter 9 (GLUT9).

Searching novel hypouricemic agents of high efficacy and safety has attracted a great attention. Previously, we reported the hypouricemic effect of Ganoderma applanatum, but its bioactives, was not referred. Herein, we report the hypouricemic effect of 2,5-dihydroxyacetophenone (DHAP), a compound screened from Ganoderma applanatum computationally. Serum parameters, such as uric acid (SUA), xanthine oxidase (XOD) activity, blood urea nitrogen (BUN), and creatinine were recorded. Real-time reverse transcription PCR (RT-PCR) and Western blot were exploited to assay RNA and protein expressions of organic anion transporter 1 (OAT1), glucose transporter 9 (GLUT9), uric acid transporter 1 (URAT1), and gastrointestinal concentrative nucleoside transporter 2 (CNT2). DHAP at 20, 40, and 80 mg/kg exerted excellent hypouricemic action on hyperuricemic mice, reducing SUA from hyperuricemic control (407 ± 31 μmol/L, p < 0.01) to 180 ± 29, 144 ± 13, and 139 ± 31 μmol/L, respectively. In contrast to the renal toxic allopurinol, DHAP showed some kidney-protective effects. Moreover, its suppression on XOD activity, in vivo and in vitro, suggested that XOD inhibition may be a mechanism for its hypouricemic effect. Given this, its binding mode to XOD was explored by molecular docking and revealed that three hydrogen bonds may play key roles in its binding and orientation. It upregulated OAT1 and downregulated GLUT9, URAT1, and CNT2 too. In summary, its hypouricemic effect may be mediated by regulation of XOD, OAT1, GLUT9, URAT1, and CNT2.