ABSTRACT
To explore the suitable fertilizing pattern for Saposhnikovia divaricata in the genuine producing area, a field trial was carried out to investigate the changes in the yield and quality of medicinal materials and soil in different fertilization patterns, such as organic fertilizer substitution(organic fertilizer+NPK fertilizer) and chemical fertilizer reduction(organic fertilizer+NPK fertilizer decrement and organic fertilizer+NPK fertilizer decrement+soil conditioner). The comprehensive analysis of all treatments was based on the medicine quality evaluation data set and soil quality evaluation data set, respectively, by CRITIC weight method. The results showed that(1) the yield of S. divaricate increased by 4.93%-12.67% under the organic fertilizer substitution mode, and the yield increased by 44.43% under the treatment of chemical fertilizer reduction YHT15, which was higher than that of the organic fertilizer substitution mode.(2) The quality of S. divaricate under the two fertilization modes was superior to the standard in the Chinese Pharmacopoeia, and the application of biochar was helpful to improve the quality of S. divaricate quality, with an increase of 82.83%-181.54%. CRITIC method analysis showed that fertilization treatments with high comprehensive scores were YHT15, YH30, and YH15.(3) Soil quality under the two fertilization modes was higher than that under the control. The fertilization treatments with higher comprehensive scores of soil quality were YHT15, YHT30, and YHT. The fertilization mode of adding biochar as soil conditioner, applying an appropriate amount of organic fertilizer, and reducing part of chemical fertilizer is the appropriate way to develop ecological plantation of S. divaricata in the Baicheng area in the western Jilin province. The specific fertilization mode is as follows. The basic fertilizer was 361 kg·hm~(-2) superphosphate+110 kg·hm~(-2) potassium sulfate+82 kg·hm~(-2) organic fertilizer+10 000 kg·hm~(-2) rice husk biochar, and urea was applied as top fertilizer three times, 29, 29, and 20 kg·hm~(-2), respectively.
Subject(s)
Agriculture , Apiaceae , Fertilizers/analysis , Soil , Nitrogen/analysisABSTRACT
A supramolecular complex may be formed by two solutes via a weak intermolecular interaction in a solution. The spectrum of the complex is often inundated by the spectra of the solutes that are not involved in the intermolecular interaction. Herein, a novel spectral analysis approach is proposed to retrieve the spectrum of the supramolecular complex. First, a two-dimensional (2D) asynchronous spectrum is constructed. Then, a genetic algorithm is used to obtain a heuristic spectrum of the supramolecular complex. The heuristic spectrum is a linear combination of the spectrum of the complex and the spectrum of a solute. The coefficients of the linear combination are then obtained, according to which the equilibrium constants are invariant among the sample solutions used to construct the 2D asynchronous spectrum. We have applied the approach to a supramolecular system formed by benzene and I2. In the analysis, several binding models are evaluated, and a benzene molecule interacting with two iodine molecules via halogen bonding turns out to be the only possible model. Hence, the characteristic band of the benzene/I2 supramolecular complex around 1819 cm-1 in the Fourier transform infrared (FTIR) spectrum and the corresponding equilibrium constant are obtained. The above results indicate that the novel approach provides a chance to get new insight into various intermolecular interactions studied by spectroscopy.
Subject(s)
Algorithms , Research Design , Protein Structure, Secondary , Solutions , Spectroscopy, Fourier Transform Infrared/methodsABSTRACT
RHBDD1 overexpression is found in various malignancies, including non-small cell lung cancer (NSCLC), and it is correlated with NSCLC patients' poor overall survival. This study aims to explore the function of RHBDD1 in regulating the progression of NSCLC and its potential molecular basis. qPCR, immunohistochemistry, and/or western blotting were used to evaluate the expression of RHBDD1 in NSCLC tissues and cell lines. RHBDD1 knockdown and overexpression were performed, CCK-8 assay and cell clone formation were applied to study the function of RHBDD1 in cell proliferation in vitro. Flow cytometry and immunofluorescence tests were employed to determine the regulation of apoptosis, cell cycle, and endoplasmic reticulum stress by RHBDD1. As a result, RHBDD1 was found significantly upregulated in NSCLC tissues and cells and associated with pathological tumor staging. RHBDD1 knockdown inhibited the proliferation of NSCLC cells both in vitro and in vivo, promoted their apoptosis, caused cell cycle arrest at G0/G1 phase, characterized with reduced CDK2, suppressed TGF-α secretion, and inhibited the EGFR/Raf/MEK/ERK signaling pathway. In contrast, RHBDD1 overexpression showed the opposite effects. These effects of the manipulated expression of RHBDD1 on NSCLC were restored by EGFR or MEK inhibitor. Additionally, RHBDD1 knockdown and overexpression resulted in decreased and increased BIK cleavage, respectively, but the effects could be blocked by a proteasome inhibitor. In conclusion, our research shows that RHBDD1 promotes the progression of NSCLC through enhancement of proliferation and induction of apoptosis by regulating the EGFR/Raf/MEK/ERK signaling pathway and the level of BIK protein level.
Subject(s)
Apoptosis Regulatory Proteins , Carcinoma, Non-Small-Cell Lung , ErbB Receptors , Lung Neoplasms , Mitochondrial Proteins , Serine Endopeptidases , Apoptosis , Apoptosis Regulatory Proteins/metabolism , Carcinoma, Non-Small-Cell Lung/genetics , Carcinoma, Non-Small-Cell Lung/pathology , Cell Line, Tumor , Cell Proliferation , ErbB Receptors/genetics , ErbB Receptors/metabolism , Gene Expression Regulation, Neoplastic , Humans , Lung Neoplasms/genetics , Lung Neoplasms/pathology , Mitochondrial Proteins/metabolism , Serine Endopeptidases/geneticsABSTRACT
PURPOSE: This national study aimed to investigate the lung ultrasound (LUS) training and practice of respiratory therapists (RTs) in mainland China. METHODS: A cross-sectional multicenter survey was conducted from May 22, 2021 to August 12, 2021, through online platforms. This survey included RTs in mainland China. The survey was divided into four sections: (1) demographic characteristics and basic information; (2) basic information about LUS training and practice; (3) LUS practice details; and (4) Other ultrasound training and practice. RESULTS: A total of 514 responses were received, and 494 valid responses were included in the analysis. 81.2% (401/494) participants' highest degree of education was a bachelor's degree, and 43.1% (213/494) participants were at level II in terms of job ranking. 99.2%(490/494) participants agreed that the RTs needed to learn lung ultrasound, but only 12.3% (61/494) participants had received a LUS training course. Further, 66.2% (327/494) experienced participants responded to Sect. 3. Most of RTs used LUS when the patient had hypoxia (265/327, 81%) or dyspnea (260/317, 79.5%); they also used it during spontaneous breathing trial(SBT) (191/327, 58.4%) or in prone position (177/327, 54.1%). The A-line (302/327, 92.4%), B-line (299/327, 91.4%), lung slide (263/327, 80.4%), and bat sign (259/327, 79.2%) were well known as LUS signs. Also, 30.6% (100/327) participants did not use the LUS protocol in their clinical practice, and only 25.4%(83/327) participants said they had used LUS scores. Moreover, 55.7% (182/327) participants frequently changed the respiratory therapy strategy according to LUS results. CONCLUSIONS: We should improve the number and workplace of RTs in mainland China in the future. We should also standardize the application of LUS practice and training for RTs in mainland China and establish corresponding certification pathways.
Subject(s)
Lung Diseases , Lung , Humans , Cross-Sectional Studies , Ultrasonography/methods , Lung/diagnostic imaging , Respiratory TherapyABSTRACT
Arctigenin (ARG), a natural lignans compound isolated from Arctium lappa L. In this study, the anti-tumor effect of ARG on prostate cancer cell PC-3M and the mechanism of apoptosis and autophagy induced by phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) signaling pathway were discussed, and further confirmed by the joint treatment of ARG and PI3K inhibitor LY294002. Here, the effect of ARG on cell viability was evaluated in PC-3M cells by Cell Counting Kit-8 reagent (CCK-8) assay. After the treatment of ARG, colony formation assay was used to detect the anti-proliferation effect. Annexin V-fluoresceine isothiocyanate/propidium iodide (FITC/PI) kit and 4',6-diamidino-2-phenylindole (DAPI) staining were used to detect the apoptosis level, and cell cycle changes were analyzed by flow cytometry. The expression of autophagy was detected by acridine orange staining. In addition, the expression levels of apoptosis and autophagy-related proteins were analyzed by Western blot. The result showed that different concentrations of ARG inhibited the proliferation of PC-3M cells. DAPI staining and flow cytometry showed that ARG induced PC-3M cell apoptosis and arrested cell in G0/G1 phase. Acridine orange staining showed that ARG induced autophagy in PC-3M cells. Western blot experiments showed that ARG inhibited the expression of Bcl-2, promoted the expression of Bax and cleaved caspase-3. At the same time, the expression of autophagy-related proteins LC3B-II and Beclin-1 increased after ARG treatment, but P62 decreased. In addition, further studies have shown that treatment with LY294002 enhanced the effects of ARG on the expression of proteins associated with apoptosis and autophagy, indicating that ARG may induce apoptosis and autophagy through PI3K/Akt/mTOR pathway.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Apoptosis/drug effects , Autophagy/drug effects , Furans/pharmacology , Lignans/pharmacology , Protein Kinase Inhibitors/pharmacology , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Arctium/chemistry , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Furans/chemistry , Furans/isolation & purification , Humans , Lignans/chemistry , Lignans/isolation & purification , Molecular Conformation , Phosphatidylinositol 3-Kinase/metabolism , Protein Kinase Inhibitors/chemistry , Protein Kinase Inhibitors/isolation & purification , Proto-Oncogene Proteins c-akt/antagonists & inhibitors , Proto-Oncogene Proteins c-akt/metabolism , TOR Serine-Threonine Kinases/antagonists & inhibitors , TOR Serine-Threonine Kinases/metabolism , Tumor Cells, CulturedABSTRACT
The effects of water regulation on the biosynthesis of calycosin-7-O-ß-D-glucoside in 2-year-old Astragalus membranaceus var. mongholicus were studied,and the mechanism was explained from the aspects of key enzyme gene expression and antioxidant enzyme system. The content of calycosin-7-O-ß-D-glucoside was determined by HPLC,and the expression levels of six key enzyme genes( PAL,4 CL,CHS,CHI,IFS,13'H) in the synthesis pathway were analyzed by q RT-PCR. The activities of protective enzymes and contents of osmoregulation substances and malondialdehyde were also determined. In the water deficit group,the maximum concentration of calycosin-7-O-ß-D-glucoside was 0. 49 mg·g-1 on the 24 th day of treatment. In the whole water regulation,the water deficit group outweighed the water adequate group in osmoregulation substance and MDA contents. The activities of A. membranaceus var.mongholicus antioxidant enzymes SOD,POD,and CAT increased during the initial period of water regulation,but decreased with time.The expression of PAL,CHS,and 13'H in the water deficit group was at a low level,and the 4 CL had active expression,slightly lower than that in the water adequate group. The expression of CHI and IFS elevated rapidly when water deficit occurred. Correlation analysis showed that the content of calycosin-7-O-ß-D-glucoside was positively correlated with CHI expression( P<0. 01) and IFS expression( P<0. 05). Therefore,water regulation can change the accumulation pattern of calycosin-7-O-ß-D-glucoside,and water deficit may be an effective way to increase its content. CHI and IFS are the key genes in response to water deficit.
Subject(s)
Astragalus propinquus , Isoflavones , Astragalus propinquus/genetics , Biosynthetic Pathways , Glucosides , WaterABSTRACT
Ginseng (G) and Prepared Rehmannia Root (PRR) are commonly used in traditional Chinese medicine for blood supplementation. This study aimed to study G and PRR with different compatibility ratios changes in chemical composition and inhibition of cyclophosphamide-induced myelosuppression. HPLC was used to determine the chemical constituents of 13 ginsenosides, 5-hydroxymethylfurfural (5-HMF) and verbascoside in different proportions of G-PRR. Balb/c mice were injected intraperitoneally with cyclophosphamide (CTX) to induce bone marrow suppression. The effects of different proportions of G-PRR on peripheral blood, bone marrow nucleated cells, thymus and spleen index of myelosuppressed mice were analyzed. The results showed that the compatibility of G and PRR can promote the dissolution of ginsenosides, and the content of conventional ginsenosides decreased, and the content of rare ginsenosides increased. Different proportions of G-PRR increased the number of peripheral blood and bone marrow nucleated cells in cyclophosphamide-induced bone marrow suppression mice (p < 0.01), increased thymus index (p < 0.01), decreased spleen index (p < 0.01). Different proportions of G-PRR can improve the myelosuppression induced by cyclophosphamide in mice, and the combined effect of G-PRR is better than the single decoction of G and PRR. Among them, G-PRR 2 : 3 and G-PRR 1 : 2 were better than the other groups. These results indicate that different proportion of G-PRR can improve bone marrow suppression, and the combined decoction of G-PRR is better than the separate Decoction in improving bone marrow suppression. This improvement may be related to the changes of the substance basis and active ingredients of G-PRR.
Subject(s)
Bone Marrow/drug effects , Furaldehyde/analogs & derivatives , Ginsenosides/pharmacology , Glucosides/pharmacology , Panax/chemistry , Phenols/pharmacology , Rehmannia/chemistry , Animals , Antineoplastic Agents, Alkylating/administration & dosage , Cyclophosphamide/administration & dosage , Disease Models, Animal , Dose-Response Relationship, Drug , Furaldehyde/chemistry , Furaldehyde/pharmacology , Ginsenosides/chemistry , Glucosides/chemistry , Injections, Intraperitoneal , Male , Medicine, Chinese Traditional , Mice , Mice, Inbred BALB C , Molecular Structure , Phenols/chemistry , Plant Roots/chemistry , Structure-Activity RelationshipABSTRACT
The study is aimed to explore the effect of different water on the content of total saponins,astragaloside â £ and gene expression in the growth of Astragalus membranceus. In this study, one-year-old A. membranaceus was used as the experimental material, by pot culture different water treatments were simulated at herbal garden in Jilin Agricultural University. The content of astragaloside â £ was determined by HPLC and the total saponins by UV spectrophotometry. With 18 S RNA as a reference gene, fluorescent quantitative PCR was applied to analyze the eight key enzymes in astragalus saponin synthesis pathway AACT,HMGS,HMGR,IDI,FPS,SS,SE,CAS expression. With the decrease of soil water, the content of astragaloside â £ in the root tissue of A. membranaceus showed an increasing trend, up to 1.46 mg·g~(-1). The total saponin content tended to increase, up to 6.80 mg·g~(-1). The results of relative expression of genes showed that the eight genes showed different effects at different water. With the change of soil water content, the amount of(AACT,IDI,SS) relative expression in drought stress group firstly increased and then decreased, then increased, and then decreased. The amount of(HMGS,HMGR,FPS) relative expression in drought stress group increased firstly and then decreased. The amount of(SE,CAS) relative expression in drought stress group increased firstly and then decreased, and continued to decrease after rehydration. The expression of key enzyme genes involved in the synthesis of astragaloside was influenced by each other, and the expression of key enzyme in roots showed a correlation with the content of astragaloside. Correlation analysis showed that there was a very significant positive correlation between HMGR gene and total saponins content in drought stress group and a significant negative correlation between content of CAS and total saponins. The contents of FPS,SE,CAS and astragaloside â £ were very significantly and negative correlated. The relationship between other genes and quality was positive. Therefore, HMGR, FPS, SE and CAS genes have significant effects on the regulation of saponin content under water control. On the 15 th day after water regulation, the total amount of astragaloside and total saponins reached the highest value and could be harvested.
Subject(s)
Astragalus Plant/metabolism , Saponins/biosynthesis , Water , Chromatography, High Pressure Liquid , Droughts , Stress, Physiological , TriterpenesABSTRACT
The study is aimed to explore the effect of soil moisture content on ginsenoside biosynthesis and explain its mechanism from the perspectives of antioxidant enzyme system and gene expression of key enzymes in the pathway of ginsenoside synthesis. In the study,two years old Panax ginseng was used as the experimental material and three moisture gradient,40% of saturated water content( W1),60%( W2),80%( W3) were set up. The content of 11 monomeric saponins were determined by HPLC. With GAPDH as a reference gene,six key enzymes( HMGR,SS,ß-AS,CYP716 A47,CYP716 A52 v2,CYP716 A53 v2) in ginseng saponin synthesis pathway expression were analyzed by fluorescent quantitative PCR and the activities of superoxide dismutase( SOD),peroxidase( POD),catalase( CAT) activity and MDA content were also determined. With the increase of soil water,the content of ginseng saponin and biomass showed an increasing trend. PPD( Rb1,Rc,Rb2,Rd,Rh2,Rb3,Rg3),PPT( Rg1,Re,Rf) ginsenoside,Ro and total ginsenoside reached the maximum value on August 30,were 9.92,5.48,0.63 mg·g-1,respectively. During the whole regulation period,the antioxidant activity of W3 was greater than that of W1,and the MDA content was less than that of W1. At W3,expression levels of ß-AS,CYP716 A47 and CYP716 A53 v2 showed an increasing trend,while HMGR and SS genes showed relatively stable expression levels under various water conditions. According to the correlation analysis,HMGR and SS genes in the W3 treatment group were significantly positively correlated with PPD,PPT ginsenoside and Ro,CYP716 A52 v2 gene was significantly positively correlated with Ro,and CYP716 A47 gene was significantly positively correlated with PPD ginsenoside. There was a significant positive correlation between ß-AS gene and PPD ginsenoside in W1 and W2 treatment. Therefore,W3 is the optimum moisture content,ginseng total saponins and monomer saponin content is the highest,the gene closely correlation with content of saponins and more conducive to the accumulation of ginsenosides.
Subject(s)
Ginsenosides/biosynthesis , Panax/physiology , Water/physiology , Chromatography, High Pressure LiquidABSTRACT
MscL is a bacterial mechanosensitive channel that serves as a cellular emergency release valve, protecting the cell from lysis upon a drop in external osmolarity. The channel has an extremely large pore (30 Å) and can be purified and reconstituted into artificial membranes. Moreover, MscL is modified to open in response to alternative external stimuli including changes in pH. These properties suggest this channel's potential as a triggered "nanopore" for localized release of vesicular contents such as magnetic resonance imaging (MRI) contrast agents and drugs. Toward this end, several variants of pH-triggered MscL nanovalves are engineered. Stealth vesicles previously been shown to evade normal in vivo clearance and passively accumulate in inflamed and malignant tissues are reconstituted. These vesicles are loaded with 1,4,7,10-tetraazacyclododecane tetraacetic acid gadolinium complex (Gd-DOTA), an MRI contrast reagent, and the resulting nanodevices tested for their ability to release Gd-DOTA as evidenced by enhancement of the longitudinal relaxation rate (R1 ) of the bulk water proton spins. Nanovalves that are responsive to physiological pH changes are identified, but differ in sensitivity and efficacy, thus giving an array of nanovalves that could potentially be useful in different settings. These triggered nanodevices may be useful in delivering both diagnostic and therapeutic agents.
Subject(s)
Escherichia coli Proteins/metabolism , Ion Channels/metabolism , Liposomes/chemistry , Magnetic Resonance Imaging , Hydrogen-Ion Concentration , Ion Channel Gating , Kinetics , NanoporesABSTRACT
PURPOSE: Esophageal carcinoma (EC) is one of the most aggressive type cancers and dysregulation of retinoid X receptor α (RXRα) involves various tumors. However, the relationship of RXRα with the clinicopathological factors of EC, particularly prognostic characteristics, remains unclear. This present study was to evaluate the effect of RXRα expression in the development of EC. METHODS: The mRNA and protein expression level of RXRα in EC and normal esophageal tissues using reverse transcription-polymerase chain reaction (RT-PCR) and Western blot, respectively. The subcellular localization was detected by immunohistochemistry (IHC) analysis. The clinicopathological parameters were included age, sex, tumor size, differentiation, TNM stages and lymph node metastasis. Kaplan-Meier method and Cox's regression analyses were performed to evaluate the prognosis of 60 patients with EC. RESULTS: RXRα was elevated in EC tissues comparing with normal esophageal tissues at both mRNA and protein levels. The overexpression level of RXRα was closely associated to the tumor differentiation, TNM stage and lymph node metastasis of patients with EC. In addition, EC patients with RXRα high expression had significantly lower disease-free survival (DFS) and overall survival (OS). Multivariate analysis showed RXRα expression as an independent predictor for the DFS and OS rate of patients with EC. CONCLUSIONS: Our results showed that overexpression of RXRα was correlated with unfavorable prognosis, suggesting that RXRα may serve as a potential targeted therapeutic marker in the treatment of EC.
Subject(s)
Biomarkers, Tumor/metabolism , Esophageal Neoplasms/diagnosis , Retinoid X Receptor alpha/metabolism , Biomarkers, Tumor/genetics , Disease-Free Survival , Esophageal Neoplasms/metabolism , Esophageal Neoplasms/pathology , Female , Humans , Immunohistochemistry , Kaplan-Meier Estimate , Lymphatic Metastasis , Male , Middle Aged , Prognosis , Retinoid X Receptor alpha/geneticsABSTRACT
The study is aimed to explore the effect of different temperature on the content of baicalin and gene expression in the growth of Scutellaria baicalensis. Four culture temperatures were used to establish the callus culture of S. baicalensis under dark conditions for 40 days and once every 5 days. The growth and baicalin contents were determined. 18S RNA was used as a reference gene to analyze the five key factors in baicalin biosynthesis pathway (PAL), cinnamic acid 4-hydroxylase (C4H), chalcone synthase (CHS), ß-glucuronidase (GUS), baicalein-7-O-glucuronosyltransferase (UBGAT) gene expression levels. The results showed that biomass, baicalin content and accumulation increased with the increase of temperature. 25 °C and 30 °C were more suitable for the growth of S. baicalensis. The content and accumulation of baicalin at 25 °C reached the highest level at 30 days, reaching 2.75% and 12.44 mg, respectively. The relative expression levels of C4H, CHS, GUS and UGBAT genes at 15 °C were higher than those at other treatments. The correlation between the relative expression levels of each key enzyme and the content of baicalin was negatively correlated with the increase of incubation temperature. The relative expression levels of PAL, C4H and CHS genes at 25 °C and 30 °C were significantly correlated with the contents of baicalin and reached a highly significant or significant level. Relative low temperature conditions were not conducive to the growth of S. baicalensis and the accumulation of baicalin. The accumulation of baicalin by PAL and C4H in the upstream of the synthetic pathway was significant.
Subject(s)
Scutellaria baicalensis , Flavonoids , Temperature , Trans-Cinnamate 4-MonooxygenaseABSTRACT
Although cisplatin is an anticancer drug that has activity against malignant tumor, it often causes nephrotoxicity. Previous reports have confirmed that the saponins from the leaves of P. quinquefolium (PQS) exerted many pharmacological activities. However, the renoprotective effects of PQS were still unknown. The purpose of the present research was to discuss renoprotective effect of PQS in a mouse model of cisplatin-induced acute kidney injury (AKI). The levels of blood urea nitrogen (BUN) and serum creatinine (CRE) were evidently increased in cisplatin-intoxicated mice, which were reversed by PQS. Renal oxidative stress, evidenced by increased malondialdehyde (MDA) level and decline of glutathione (GSH) and superoxide dismutase (SOD) activities, was significantly alleviated by PQS pretreatment. The suppression of inflammatory response by PQS was realized through the decrease the mRNA expression levels of tumor necrosis factor-α (TNF-α) and interleukin-1ß (IL-1ß) in kidney tissues, which were measured by quantitative real-time polymerase chain reaction (qRT-PCR). Simultaneously, the overexpression of cytochrome P450 E1 (CYP2E1) and heme oxygenase-1 (HO-1) were attenuated by PQS. Furthermore, the effects of Western blotting demonstrated that PQS administration significantly suppressed the protein expression levels of nicotinamide adenine dinucleotide phosphate oxidase type 4 (Nox4), cleaved Caspase-3, cleaved Caspase-9, Bax, nuclear factor-κB (NF-κB), cyclooxygenase-2 (COX-2), and inducible nitric oxide synthase (iNOS), suggesting the inhibition of apoptosis and inflammation response. Overall, PQS may possess protective effects in cisplatin-induced AKI through suppression of oxidative stress, inflammation and apoptosis.
Subject(s)
Acute Kidney Injury/chemically induced , Acute Kidney Injury/drug therapy , Cisplatin/adverse effects , Neuroprotective Agents/therapeutic use , Panax/chemistry , Plant Leaves/chemistry , Saponins/therapeutic use , Acute Kidney Injury/pathology , Acute Kidney Injury/physiopathology , Animals , Apoptosis/drug effects , Cytokines/metabolism , Glutathione/metabolism , Inflammation/pathology , Kidney/drug effects , Kidney/enzymology , Kidney/pathology , Kidney/physiopathology , Male , Malondialdehyde/metabolism , Mice, Inbred ICR , Neuroprotective Agents/pharmacology , Oxidative Stress/drug effects , Saponins/pharmacology , Superoxide Dismutase/metabolismABSTRACT
The use of arctigenin (ARG), a traditional medicine with many pharmacological activities, has been restricted due to its poor solubility in water. Five amino acid derivatives of ARG have been synthesized using glycine, o-alanine, valine, leucine, and isoleucine, which have t-butyloxy carbonyl (BOC) as a protective group. In this study, we examined the effects of removing these protective groups. The results showed that the amino acid derivatives have better solubility and nitrite-clearing ability than ARG. Among the compounds tested, the amino acid derivatives without protective group were the best. Based on these results, ARG and its two amino acid derivatives without protective group (ARG8, ARG10) were selected to evaluate their anti-tumor activity in vivo at a dosage of 40 mg/kg. The results indicated that ARG8 and ARG10 both exhibit more anti-tumor activity than ARG in H22 tumor-bearing mice. The tumor inhibition rates of ARG8 and ARG10 were 69.27 and 43.58%, which was much higher than ARG. Furthermore, the mice treated with these compounds exhibited less damage to the liver, kidney and immune organs compared with the positive group. Furthermore, ARG8 and ARG10 improved the serum cytokine levels significantly compared to ARG. In brief, this study provides a method to improve the water solubility of drugs, and we also provide a reference basis for new drug development.
Subject(s)
Amino Acids/pharmacology , Antineoplastic Agents/pharmacology , Esters/pharmacology , Furans/pharmacology , Lignans/pharmacology , Neoplasms, Experimental/drug therapy , Amino Acids/chemical synthesis , Amino Acids/chemistry , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Esters/chemical synthesis , Esters/chemistry , Furans/chemical synthesis , Furans/chemistry , Lignans/chemical synthesis , Lignans/chemistry , Mice , Molecular Structure , Neoplasms, Experimental/pathology , Structure-Activity RelationshipABSTRACT
The ß-Glucuronidase gene (sbGUS) cDNA firstly from Scutellari abaicalensis leaf was cloned by RT-PCR, with GenBank accession number KR364726. The full length cDNA of sbGUS was 1 584 bp with an open reading frame (ORF), encoding an unstable protein with 527 amino acids. The bioinformatic analysis showed that the sbGUS encoding protein had isoelectric point (pI) of 5.55 and a calculated molecular weight about 58.724 8 kDa, with a transmembrane regions and signal peptide, had conserved domains of glycoside hydrolase super family and unintegrated trans-glycosidase catalytic structure. In the secondary structure, the percentage of alpha helix, extended strand, ß-extended and random coil were 25.62%, 28.84%, 13.28% and 32.26%, respectively. The homologous analysis indicated the nucleotide sequence 98.93% similarity and the amino acid sequence 98.29% similarity with S. baicalensis (BAA97804.1), in the nine positions were different. The expression level of sGUS was the highest in root based on a real-time PCR analysis, followed by flower and stem, and the lowest was in stem. The results provide a foundation for exploring the molecular function of sbGUS involved in baicalcin biosynthesis based on synthetic biology approach in S. baicalensis plants.
Subject(s)
Cloning, Molecular , Glucuronidase/chemistry , Glucuronidase/genetics , Plant Proteins/chemistry , Plant Proteins/genetics , Scutellaria baicalensis/enzymology , Amino Acid Sequence , Base Sequence , Computational Biology , Glucuronidase/metabolism , Molecular Sequence Data , Open Reading Frames , Phylogeny , Plant Proteins/metabolism , Protein Structure, Secondary , Scutellaria baicalensis/chemistry , Scutellaria baicalensis/genetics , Sequence AlignmentABSTRACT
MscL, the highly conserved bacterial mechanosensitive channel of large conductance, is one of the best studied mechanosensors. It is a homopentameric channel that serves as a biological emergency release valve that prevents cell lysis from acute osmotic stress. We previously showed that the periplasmic region of the protein, particularly a single residue located at the TM1/periplasmic loop interface, F47 of Staphylococcus aureus and I49 of Escherichia coli MscL, plays a major role in both the open dwell time and mechanosensitivity of the channel. Here, we introduced cysteine mutations at these sites and found they formed disulfide bridges that decreased the channel open dwell time. By scanning a likely interacting domain, we also found that these sites could be disulfide trapped by addition of cysteine mutations in other locations within the periplasmic loop of MscL, and this also led to rapid channel kinetics. Together, the data suggest structural rearrangements and protein-protein interactions that occur within this region upon normal gating, and further suggest that locking portions of the channel into a transition state decreases the stability of the open state.
Subject(s)
Escherichia coli Proteins/metabolism , Ion Channels/metabolism , Lipid Metabolism , Periplasm/metabolism , Amino Acid Sequence , Cysteine , Escherichia coli Proteins/chemistry , Escherichia coli Proteins/genetics , Ion Channels/chemistry , Ion Channels/genetics , Kinetics , Models, Molecular , Molecular Sequence Data , Mutagenesis , Mutation , Protein Binding , Protein Structure, Tertiary , Protein Subunits/chemistry , Static ElectricityABSTRACT
Using the field sampling and indoor soil cultivation methods, the dynamic of ginseng rhizosphere soil microbial activity and biomass with three cultivated ages was studied to provide a theory basis for illustrating mechanism of continuous cropping obstacles of ginseng. The results showed that ginseng rhizosphere soil microbial activity and biomass accumulation were inhibited observably by growing time. The soil respiration, soil cellulose decomposition and soil nitrification of ginseng rhizosphere soil microorganism were inhibited significantly (P <0.05), in contrast to the control soil uncultivated ginseng (R0). And the inhibition was gradual augmentation with the number of growing years. The soil microbial activity of 3a ginseng soil (R3) was the lowest, and its activity of soil respiration, soil cellulose decomposition, soil ammonification and soil nitrification was lower than that in R0 with 56.31%, 86.71% and 90. 53% , respectively. The soil ammonification of ginseng rhizosphere soil microbial was significantly promoted compared with R0. The promotion was improved during the early growing time, while the promotion was decreased with the number of growing years. The soil ammonification of R1, R2 and R3 were lower than that in R0 with 32.43%, 80.54% and 66.64% separately. The SMB-C and SMB-N in ginseng rhizosphere soil had a decreased tendency with the number of growing years. The SMB-C difference among 3 cultivated ages was significant, while the SMB-N was not. The SMB of R3 was the lowest. Compared with R0, the SMB-C and the SMB-N were significantly reduced 77.30% and 69.36%. It was considered by integrated analysis that the leading factor of continuous cropping obstacle in ginseng was the changes of the rhizosphere soil microbial species, number and activity as well as the micro-ecological imbalance of rhizosphere soil caused by the accumulation of ginseng rhizosphere secretions.
Subject(s)
Bacteria/growth & development , Panax/microbiology , Soil Microbiology , Soil/chemistry , Agriculture , Ammonium Compounds/metabolism , Biomass , Cellulose/metabolism , Nitrification , Panax/growth & development , Plant Roots/growth & development , Plant Roots/microbiology , Rhizosphere , Time FactorsABSTRACT
To discuss the effect of environmental factors and photosynthesis on the growing of plant and the content of active components in Scutellaria baicalensis, the photosynthetic physiology index and diurnal changes of flavonoid constituent of S. Baicalensis were observed and tested in flowering and fruiting stages, and in the meantime environmental parameters were recorded. The obtained data were analyzed data by using path analysis and gray correlation analysis. The results showed that PAR and SWC were important environmental factors impacting on photosynthesis of S. baicalensis. SWC, RH and Ca were important environmental factors impacting on baicalin content. PAR, Po and Ta were important environmental factors impacting on baicalein content.
Subject(s)
Flavonoids/analysis , Photosynthesis , Plant Extracts/analysis , Scutellaria baicalensis/chemistry , Scutellaria baicalensis/metabolism , Environment , Flavonoids/metabolism , Plant Extracts/metabolism , Plant Roots/chemistry , Plant Roots/growth & development , Plant Roots/metabolism , Scutellaria baicalensis/growth & developmentABSTRACT
Two-dimensional correlation spectroscopy is used to investigate the intermolecular interaction between two substances dissolved in the same solutions, where the intermolecular interaction is described by two reversible reactions producing two supramolecular aggregates. The severe overlappings expected among the characteristic peaks of the original solute and aggregates make conventional one-dimensional spectra difficult to accurately reflect the physiochemical nature of the intermolecular interaction. The double asynchronous orthogonal sample design (DAOSD) approach is utilized to analyze the simulated data for proof-of-principle demonstration. The patterns of cross-peaks are much more complex compared with the intermolecular interaction described by only a single reaction. Four major groups of cross-peaks with characteristic patterns observed in the pair of DAOSD asynchronous spectra are systematically analyzed and classified. Further analysis of the spectral feature of the cross-peaks of the DAOSD asynchronous spectra is helpful to exact additional information concerning the variation of the peak position and peak width of the aggregates compared with those of the original solute. The result is important to reveal the physicochemical nature of intermolecular interaction between the solutes (e.g., changes in conformation, dynamical behavior, etc.). The pattern of cross-peaks in the corresponding 2D asynchronous spectra may become rather complex when the peak position, peak width, and peak intensity of two supramolecular aggregates change simultaneously. Further work using artificial intelligence techniques to interpret the complex cross-peaks is still being carried out.
ABSTRACT
The strong coupling between society and ecosystem makes socio-ecological risks become the main object of risk management. As the link between ecological and social processes, ecosystem services (ESs) are the core variable in deconstructing the social-ecological risks and the crucial point in resolving the risks. We explored the concept and the internal formation mechanisms of socio-ecological risk combining ESs, and further put the cascade logic and evolution process of "real risk-risk perception-risk behavior". Based on driver-pressure-state-impact-response framework (DPSIR), we proposed a framework for analyzing socio-ecological risk, and expanded the content and methodology system of research and management practices related to socio-ecological risks. We proposed that socio-ecological risk research coupled with ESs should focus on: 1) exploring the transmission mechanism between ecosystem processes, ecosystem services, and human well-being; 2) exploring the response mechanism of social subject behavior and its impacts on ecosystem services and human well-being; 3) construction of a multi-scale assessment model for social ecological risks coupled with ESs. The socio-ecological risk analysis framework for coupled ecosystem services was based on the mutual feedback between human and nature to explore the logic of risk formation, evolution, and governance, which could provide ideas for clarifying the deep meaning of ecological problems and selecting pathways to resolve socio-ecological risks.