Significant Activity Effect Research Articles

Unravelling the multiple effects of H2O on the NH3-SCR over Mn2Cu1Al1Ox-LDO by transient kinetics and in situ DRIFTS

Understanding detrimental effects of water in the low-temperature NH3-SCR is very important for advancing the design of novel catalytic materials. Herein, the effects of 5 vol% H2O on the performance of NH3-SCR over Mn2Cu1Al1Ox-LDO were investigated through steady-state and transient kinetic analysis of step-gas switching experiments, in-situ DRIFTS and 15NO-SSITKA-DRIFTS operando. Water exhibited a significant negative activity effect at T<180 °C. Slightly positive activity (200–300 °C) and N2-selectvity (120–300 °C) effects were observed due to suppression of NH3 oxidation and NH4NO3 decomposition to N2O. The decline in activity at 140 °C by ∼ 45 % in the presence of water was found to be related to the decrease of the site activity (k) and not of surface coverage (θ) of active species formed in the NH3-SCR reaction paths of N2/N2O formation. An increase in the concentration of inactive NOx-s might also contribute to the inhibitive effect of water.

Phenolic Compound Characterization and Biological Activities of Mistletoe (Viscum album L.) Ethanol Macerates Used in Herbal Spirit Production

Biska, a traditional Istrian herbal spirit, is produced by macerating mistletoe leaves and twigs in a water–ethanol base, usually grape marc spirit. The aim of this study was to determine the optimal mistletoe maceration parameters (ethanol content, concentration of plant material, and duration) for the production of biska, which have not yet been the subject of scientific research. The prepared mistletoe macerates and the collected biska samples were subjected to phenolic compound characterization, including total phenolic content (TPC), total flavonoid content (TFC), and polyphenolic profile, by ultra-high-performance liquid chromatography coupled with mass spectrometry (UPLC-ESI-MS2). In addition, the macerates and the biska samples were analyzed for their biological properties: antioxidant and antiproliferative activity. The results showed that both the macerates and the biska samples contain phenolic compounds of mistletoe such as phenolic acids, flavonoids, and coumarins, which contribute to the observed biological activities—significant antioxidant activity and antiproliferative effect. By applying the maceration parameters, which yielded the highest content of phenolic compounds as well as volatile aromatic compounds (40–80 g/L of mistletoe, 40–55% v/v ethanol, and 21 days’ maceration time), the production process can be improved to produce biska with better aromatic and biological properties.

Effects of dietary binder sources on growth, digestive enzymes activity, and gut barrier function and microbial composition of larval largemouth bass (Micropterus salmoides)

A 4-week feeding trail was conducted to explore the impacts of dietary binder sources on growth performance, digestive enzymes activities, intestinal microbiota, and expression of genes involved in tight junctions and nutrient sensing pathway of larval largemouth bass with initial body weight of 8.43 ± 0.01 mg (13 day after hatching). Five isolipidic micro-diets were formulated with different binder sources including sodium alginate (SA), carrageenan (CG), hydroxypropyl methyl cellulose (HPMC), gelatin (GT), and starch (SC). The results revealed that the highest growth performance was observed in the CG group, and meanwhile, the promotion effects of SA and GT was statistically higher than that of HPMC and SC groups. SA, CG and GT had positive effects on digestive enzymes activity compared to other groups. Gene expression results showed that SA, CG and GT groups up-regulated the expression of tight junction genes, zo-1, claudin-4 and claudin-7, and activated the genes involved in the TOR signaling pathway, including tor, akt1, s6kβ1 and s6. Among all the groups, the CG had the most significant activation effect on TOR signaling pathway. Bacterial 16S rRNA V3–4 region analysis showed that the addition of different dietary binders influenced the diversity of intestinal microbial communities. The inclusion of SA and CG groups reduced the relative abundance of Proteobacteria and Actinobacteria at the phylum level, while at the genus level, the relative abundance of Rhodococcus and Achromobacter increased and the abundance of Plesiomonas was inhibited. In summary, dietary binder sources affected the growth, digestive function, gut barrier function and microbial composition, and nutrient sensing, and SA and CG could be suggested as the optimal dietary binders for formulation of micro-diets for largemouth bass larvae.

In situ regulation of the oxygen vacancy concentration of Bi4Ti3O12 by β-particles to activate peroxydisulfate

The key to enhancing the activation efficiency of peroxydisulfate (PDS) lies in facilitating the adsorption of PDS and accelerating the rate of electron transfer at the interface. In this work, the oxygen vacancy (Ovs) concentration of ultrathin Bi4Ti3O12 (BTO) was controlled in situ by high-energy electron beam bombardment. BTOV-300 exhibited a significant activation effect on PDS. The degradation rate constant (kobs) for the removal of ciprofloxacin (CIP) was measured to be 0.2080 min−1 under visible light irradiation, which was 3.71 times greater than that of the original BTO. Density functional theory calculations uncovered the principal role of oxygen vacancies as active sites for PDS activation. Introducing OVs significantly boosted the adsorption energy of PDS on BTO and lengthened the OO bond of PDS. This study represents the potential mechanism behind the activation of PDS by BTOV and provides valuable insights for enhancing the photoactivation efficiency of PDS.

Study on chemical composition and α‐glucosidase inhibitory activity from the leaves of Muntingia calabura

Abstract“Trứng cá” (Muntingia calabura) is a special species of the genus Muntingia. Phytochemical studies on the leaves of M. calabura showed that seven compounds were isolated, including R‐(+)‐5‐(δ‐tocopherol‐5'‐yl)‐δ‐tocopherol (1), trans‐phytol (2), ergosta‐4,6,8(14),22‐tetraen‐3‐one (3), ergosterol peroxide (4), stigmasta‐4‐ene‐3,6‐dione (5), 6β‐hydroxystigmast‐4‐en‐3‐one (6), and β‐sitosterol (7). The structures of the compounds were elucidated by mass spectrometry, nuclear magnetic resonance spectroscopy (NMR), and compared to the literature. The biological test result for all isolated compounds showed that compounds 1‐3, and 5‐7 have the ability to inhibit moderately α‐glucosidase with IC50 values ranging from 57.9 to 249.5 μM. Compound 3 processed a significant inhibitory activity effect with an IC50 value of 57.9 μM, more potent than the positive control, acarbose (IC50, 214.5 μM). This is the first time compounds 1‐5 have been reported for the Muntingia genus.

Nanomolar range of FAM237B can activate receptor GPR83.

Our recent study confirmed that the mature neuropeptide FAM237A, also known as neurosecretory protein GL (NPGL), is an efficient agonist for GPR83. The paralog FAM237B was previously reported as a weak agonist for GPR83. In the present study, we prepared mature human FAM237B via an intein-fusion approach and demonstrated that it could cause a significant activation effect at the nanomolar range (1‒10nM) in a NanoBiT-based β-arrestin recruitment assay. Thus, FAM237B appears to be another endogenous agonist for GPR83 and future in vivo studies will be required to confirm this.

Ginsenoside Rg1 alleviates ANIT-induced cholestatic liver injury by inhibiting hepatic inflammation and oxidative stress via SIRT1 activation

Ethnopharmacological relevanceGinseng (Panax ginseng C. A. Mey) is a common traditional Chinese medicine used for anti-inflammation, treating colitis, type 2 diabetes, diarrhea, and recovering hepatobiliary function. Ginsenosides, the main active components isolated from ginseng, possess liver and gallbladder diseases therapeutic potential. Aims of the studyCholestatic liver injury (CLI) is a liver disease induced by intrahepatic accumulation of toxic bile acids and currently lacks clinically effective drugs. Our previous study found that ginsenosides alleviated CLI by activating sirtuin 1 (SIRT1), but the effective ingredients and the underlying mechanism have not been clarified. This study aimed to identify an effective ingredient with the most significant activation effect on SIRT1 from the five major monomer saponins of ginsenosides: Rb1, Rd, Rg1, 20s-Rg3, and Rc further explore its protective effects on CLI, and elaborate its underlying mechanism. Materials and methodsDiscovery Studio 3.0 was used to conduct molecular docking between monomer saponins and SIRT1, and further detect the influence of monomer saponins on SIRT1 activity in vitro. Finally, it was determined that Rg1 had the most significant stimulative effect on SIRT1, and the hepatoprotective activity of Rg1 in CLI was explored in vivo. Wild-type mice were intragastrically α-naphthylisothiocyanate (ANIT) to establish an experimental model of intrahepatic cholestasis and Rg1 intervention, and then liver injury and cholestasis related indexes were detected. In addition, Liver-specific SIRT1 gene knockout (SIRT1-/-) mice were administered with ANIT and/or Rg1 to further investigate the mechanism of action of Rg1. ResultsThe results of molecular docking and in vitro experiments showed that all the five ginsenoside monomers could bind to the active site of SIRT1 and promote SIRT1 activity in HepG2 cells. Among them, Rg1 exhibited the most significant stimulation of SIRT1 activity in cholestasis. Besides, it could ameliorate ANIT-induced inflammation and oxidative stress in HepG2 cells. Therefore, we investigated the hepatoprotective effect and mechanism of Rg1 on CLI. Results showed that Rg1 reversed the ANIT-induced increase in biochemical parameters, improved liver pathological injury, and decreased liver lipid accumulation, reactive oxygen species and pro-inflammatory factor levels. Mechanistically, Rg1 induced SIRT1 expression, followed by promoted the activity of Nrf2 and suppressed the activation of NF-κB. Interestingly, the hepatoprotective effect of Rg1 was blocked in SIRT1-/- mice. ConclusionRg1 mitigated ANIT-induced CLI via upregulating SIRT1 expression, and our results suggested that Rg1 is a candidate compound for treating CLI.

Effect of auricular acupuncture on neuroplasticity of stroke patients with motor dysfunction: A fNIRS study

Cerebral Stroke is an acute cerebrovascular disease, a disease of brain tissue damage caused by the sudden rupture or blockage of blood vessels in the brain that prevents blood flow to the brain. Acupuncture has become a popular treatment for stroke, with auricular acupuncture providing a new idea for stroke treatment. However, the neuromodulatory mechanism of auricular acupuncture in the brain is still unclear. The aim of this study was to investigate the effect of auricular acupuncture in the treatment of upper limb dysfunction and the activation of specific brain regions in stroke patients. Forty patients with stroke hemiplegia who met the nerf criteria were included in the experiment and randomly assigned into two groups (20 patients in each group): the auricular acupuncture group and the control group. Fugl-Meyer score (FMA) assessment of upper limb motor function, motor evoked potential (MEP) measurement, and functional near-infrared brain function imaging (fNIRS) data acquisition in the primary motor M1 area of the brain at rest were performed before and after treatment, respectively. It was found that: 1) after auricular acupuncture treatment, the patients in the auricular acupuncture group showed significantly greater peak MEP and significantly higher oxyhemoglobin content in the M1 region of the brain compared with the control group, with a significant activation effect (MEP: P-value = 0.032, t = -2.22; HbO2; f = 4.225, p = 0.046); 2) in the clinical efficacy assessment, the FMA score in the auricular acupuncture group after treatment (p = 0.0122, t = 2.769). The results suggest that auricular acupuncture has an ameliorative effect on upper limb motor deficits after stroke and that activation of the M1 region of the brain may be a key node in auricular acupuncture for treating upper limb dysfunction in stroke patients, a finding that emphasizes the potential for clinical application of auricular acupuncture therapy for stroke patients with potential mechanisms influencing the outcome.

Chemical Constituents from the Fruits of Amomum kravanh and Their Role in Activating Alcohol Dehydrogenase.

Alcoholism is a worldwide health problem, and diseases caused by alcoholism are killing people every year. Amomum kravanh is a traditional Chinese medicine used to relieve hangovers. However, whether its bioactive components improve alcohol metabolism is not clear. In this study, ten new (amomumols A-J, 1-10) and thirty-five known (11-45) compounds were isolated from the fruits of Amomum kravanh by an activity-guided separation. Ten novel compounds were identified as four sesquiterpenoids (1-4), three monoterpene derivatives (5-7), two neolignans (8, 9), and a novel norsesquiterpenoid (10) with a new C14 nor-bisabolane skeleton. Their structures were determined by the comprehensive analysis of high-resolution electrospray ionization mass spectrometry (HRESIMS), nuclear magnetic resonance (NMR), and electronic circular dichroism (ECD) calculation. The effects of all isolated compounds on the activity of alcohol dehydrogenase were evaluated in vitro, and it was found that eight compounds (11, 12, 15, 18, 26, and 36-38) exhibited significant activation effects on the alcohol dehydrogenase at 50 μM.

Formation characteristics of algal-bacteria granular sludge under low-light environment: From sludge characteristics, extracellular polymeric substances to microbial community

In this study, the formation characteristics of algal-bacteria granular sludge (ABGS) under low-light environment (80, 110, and 140 μmol/m2/s) were investigated. The findings revealed that the stronger light intensity favored the improvement of sludge characteristics, nutrient removal performances, and extracellular polymeric substance (EPS) secretion at the growing stage, which were more preferential to facilitate the formation of ABGS. However, after the mature stage, the weaker light intensity ensured more stable operation of the system, as shown by contributing to sludge settlement performance, denitrification, and EPS secretion. According to the results of high-throughput sequencing, the dominant bacterial genus of the mature ABGS cultured under low light intensity were all Zoogloe, while the dominant algal genus was different. For the mature ABGS, the 140 and 80 μmol/m2/s light intensity had the most significant activation effect to the functional genes related to carbohydrate metabolism and amino acid metabolism, respectively.

Anticancer, Antioxidant Activity and Molecular Docking Studies of Saccharumoside-B

Objectives: The present study reports antioxidant potential, the in-vitro antiproliferative activity of saccharumoside-B, and molecular docking studies on the binding affinity of saccharumoside-B towards various proteins involved in breast cancer pathogenesis. Methods: The in-vitro antioxidant activity of saccharumoside-B was determined by DPPH, superoxide and nitric oxide free radical scavenging assays. The antiproliferative activity was evaluated in-vitro by MTT assay. The binding affinity of saccharumoside-B towards the HSP90, HER2, human estrogen receptor and tyrosine-protein kinase C-SRC were determined by the molecular docking studies. Results: Saccharumoside-B showed a significant dose-dependent antioxidant activity and potent dose-dependent antiproliferative effect on the MCF-7 breast cancer cell line (IC50 = 22.57±0.39µM) among all other cell lines studied. Tamoxifen was used as a positive control for MCF-7 cell line (IC50 = 27.97±1.07µM). The IC50 of saccharumoside-B on normal MCF-10A cell line (IC50&gt;1000µM) showed a promising safety profile, whereas tamoxifen’s IC50 on MCF-10A normal cell line was found to be 29.6 ± 0.84 µM. The molecular docking analysis revealed that saccharumoside-B was inserted into the active site pockets of all the tested proteins involved in the breast cancer pathogenesis with varying binding affinities. Conclusion: The antioxidant studies revealed the potential antioxidant effect of saccharumoside-B. The in-vitro and in-silico studies are indicating the safe and multiple target protein inhibitory potential of saccharumoside-B against breast cancer. This study suggests that saccharumoside-B can be developed into a new class of anticancer drugs with a high safety profile in the future.

Cognitive and motor cortex activation during robot-assisted multi-sensory interactive motor rehabilitation training: An fNIRS based pilot study.

This study aimed to evaluate the effects of multiple virtual reality (VR) interaction modalities based on force-haptic feedback combined with visual or auditory feedback in different ways on cerebral cortical activation by functional near-infrared spectroscopy (fNIRS). Methods: A modular multi-sensory VR interaction system based on a planar upper-limb rehabilitation robot was developed. Twenty healthy participants completed active elbow flexion and extension training in four VR interaction patterns, including haptic (H), haptic + auditory (HA), haptic + visual (HV), and haptic + visual + auditory (HVA). Cortical activation changes in the sensorimotor cortex (SMC), premotor cortex (PMC), and prefrontal cortex (PFC) were measured. Four interaction patterns all had significant activation effects on the motor and cognitive regions of the cerebral cortex (p < 0.05). Among them, in the HVA interaction mode, the cortical activation of each ROI was the strongest, followed by HV, HA, and H. The connectivity between channels of SMC and bilateral PFC, as well as the connectivity between channels in PMC, was the strongest under HVA and HV conditions. Besides, the two-way ANOVA of visual and auditory feedback showed that it was difficult for auditory feedback to have a strong impact on activation without visual feedback. In addition, under the condition of visual feedback, the effect of fusion auditory feedback on the activation degree was significantly higher than that of no auditory feedback. The interaction mode of visual, auditory, and haptic multi-sensory integration is conducive to stronger cortical activation and cognitive control. Besides, there is an interaction effect between visual and auditory feedback, thus improving the cortical activation level. This research enriches the research on activation and connectivity of cognitive and motor cortex in the process of modular multi-sensory interaction training of rehabilitation robots. These conclusions provide a theoretical basis for the optimal design of the interaction mode of the rehabilitation robot and the possible scheme of clinical VR rehabilitation.

In-vitro antioxidant potential and acetylcholinesterase inhibitory effect of Ficus benghalensis aerial root extract.

The aim of the current study was to evaluate the antioxidant effect, acetylcholinesterase (AChE) inhibitory effect and phytochemical screening of different extracts of aerial root extract of Ficus benghalensis using in-vitro methods. The aerial root extract was prepared by successive extraction method using different organic solvents having increasing order of polarity. FB aerial root extract was screened for preliminary phytochemical analysis. FB aerial root extracts were evaluated for in-vitro acetylcholinesterase inhibitory effect by the Ellman's method and anti-oxidant potential by DPPH assay and hydroxyl radical neutralizing assay. Preliminary phytochemical screening of FB extracts indicate the existence of the phytochemicals such as phenols, alkaloids, flavonoids, glycosides, anthraquinones, tannins and steroids. The results of the DPPH assay, hydroxyl radical scavenging assay and AChE inhibitory assay show that chloroform and ethyl acetate extracts are having significant antioxidant activity and acetylcholinesterase inhibitory effect as compared to the other extracts, respectively. The results of the current study suggest that the aerial root extract of FB might be a potential drug source for treatment of neurodegenerative disorders like Alzheimer disease.

Combination Azacitidine and Lenalidomide: A Novel Relapse Prophylaxis Option in Patients after Allogeneic Stem-Cell Transplantation for Acute Myeloid Leukemia

Introduction: Some patients with acute myeloid leukemia (AML) will still relapse after receiving allogeneic hematopoietic stem cell transplantation (allo-SCT). Once relapse, the salvage options are limited and difficult. Therefore, novel drug regimens to prevent relapse after transplantation are required. Both azacitidine (AZA) and lenalidomide (LEN) possess significant antitumor activity effect in myeloid neoplasms. LEN as maintenance or pre-emptive therapy in the first 3 months post-transplantation was reported to induce severe graft-versus-host disease (GVHD), but AZA has been shown to ameliorate GVHD in transplantation. We therefore examined the efficacy and safety of combined AZA/LEN prophylactic regimen after transplantation. Patients and Methods: AML patients who had received allo-SCT were treated with AZA (75 mg/m2 for 7 days) followed by low dose of LEN on days 10 to 28. The above is one cycle, a total of 8-10 cycles. The course of treatment can be appropriately changed according to the patient's tolerance and condition. The primary endpoint is cumulative incidence of relapse (CIR), the secondary endpoints are Overall survival (OS), Disease-free survival (DFS), adverse events (AEs). Results: A total of 28 patients received azacytidine and low-dose lenalidomide prophylaxis after allo-SCT. According to risk stratification, 71% (20/28) patients were at high risk and 29% (8/28) were at intermediate risk. Median chemotherapy numbers before transplantation were 4 (3-8) cycles. The transplantation model includes Haplo-identical (46%), HLA-identical sibling (14%), and Unrelated donor (40%). With a median follow-up of 387 (94-1073) days, 9 patients relapsed (including molecular relapse and cytological relapse), among them, 4 patients had molecular relapse and MRD was changed into negative again after treatment with this AZA/LEN regimen, and other 5 patients developed cytologically relapsed, so this program was terminated, and they received new treatment, but all still alive now. The remaining 23 have survived so far, with disease free. The 1-year CIR is 26 %, and 2-year CIR is 41 %. The 1-year DFS is 74%, and the 2-year DFS is 59%. OS is 100%. Sequential AZA and LEN prophylaxis therapy was well tolerated. About adverse events: a total of 8 patients had grade 3-4 neutropenia, none had agranulocytosis with fever; 3 patients had grade 3-4 thrombocytopenia; Grade 3 transaminase elevations occurred in 2 patients. Four patients developed chronic GVHD after AZA/LEN regimen with a score of 1-2, and no patient developed acute GVHD.

Optimization of clofibrate with O-desmethyl anetholtrithione lead to a novel hypolipidemia compound with hepatoprotective effect

Oxidative stress and inflammation were considered to be the major mechanisms in liver damage caused by clofibrate (CF). In order to obtain lipid-lowering drugs with less liver damage, the structure of clofibrate was optimized by O-desmethyl anetholtrithione and got the target compound clofibrate-O-desmethyl anetholtrithione (CF-ATT). CF-ATT significantly reduced the levels of plasma triglycerides (TG), total cholesterol (TC) in hyperlipidemia mice induced by Triton WR-1339. In addition, CF-ATT has a significantly protective effect on the liver compared with CF. The liver weight and liver coefficient were reduced. The hepatic function indexes were also decreased, such as aspartate aminotransferase (AST), alanine aminotransferase (ALT), and alkaline phosphatase (ALP). Histopathological examination of the liver revealed that inflammatory cell infiltration, nuclear degeneration, cytoplasmic loosening and hepatocyte necrosis were ameliorated by administration with CF-ATT. The hepatoprotective mechanism showed that CF-ATT significantly up-regulated Nrf2 and HO-1 protein expression and down-regulated p-NF-κB P65 expression in the liver. CF-ATT has obviously antioxidant and anti-inflammatory activity. These findings suggested that CF-ATT has significant hypolipidemia activity and exact hepatoprotective effect possibly through the Nrf2/NF-κB-mediated signal pathway.

Oxidative removal of gaseous hydrogen sulfide by a dual ions-dual oxidants coupling activation system

A gaseous hydrogen sulfide (H2S) oxidative removal technology by a dual ions-dual oxidants coupling activation system (i.e., Cu2+/Fe2+/persulfate(PS)/H2O2 coactivation system) was put forward. The fundamental issues, mainly including H2S removal performance, process parameters optimization, products, free radicals, synergy mechanism and desulfurization mechanism were studied systematically in a bubble column reactor. The study indicates that compared with Fenton system and non-coupling activation systems, the new dual ions-dual oxidants coupling coactivation system shows much higher free radical yield and H2S removal efficiency owing to significant synergistic activation effect. Higher concentrations of Cu2+ or Fe2+ greatly increase the H2S removal efficiency. With the increase of PS concentration, H2O2 concentration or reagent pH value, the H2S removal efficiency is first enhanced, and afterwards slightly declined. The H2S removal efficiency is declined via increasing operating temperature, gas flow rate and contents of H2S, SO2, NO and CO, and is almost not affected by content of Hg0. Sulfate, CuS and elemental sulfur are determined to be the products of H2S removal, and no by-products are produced after the reaction. Oxidation via ·OH and SO4-· plays a crucial role in H2S removal, which is proved to be the primary pathways of H2S removal. Finally, the recovery strategy of the products is discussed preliminarily.

Mangiferin Ameliorates HFD-Induced NAFLD through Regulation of the AMPK and NLRP3 Inflammasome Signal Pathways.

Nonalcoholic fatty liver disease (NAFLD) is closely related to glycolipid metabolism and liver inflammation. And there is no effective drug approved for its clinical therapy. In this study, we focused on mangiferin (Man) and explored its effects and mechanisms on NAFLD treatment based on the regulation of glycolipid metabolism and anti-inflammatory in vivo and in vitro. The results exhibited that Man can significantly attenuate liver injury, insulin resistance, and glucose tolerance in high-fat diet- (HFD-) induced NAFLD mice and significantly reduce fat accumulation and inflammation in hepatic tissue of NAFLD mice. The transcriptome level RNA-seq analysis showed that the significantly different expression genes between the Man treatment group and the HFD-induced NAFLD model group were mainly related to regulation of energy, metabolism, and inflammation in liver tissue. Furthermore, western blots, real-time PCR, and immunohistochemistry experiments confirmed that Man significantly activated the AMPK signal pathway and inhibited NLRP3 inflammasome activation and pyroptosis in NAFLD mice. In in vitro cell experiments, we further confirmed that Man can promote glucose consumption and reduce intracellular triglyceride (TG) accumulation induced by free fatty acids in HepG2 cells and further that it can be blocked by AMPK-specific inhibitors. Western blot results showed that Man upregulated p-AMPKα levels and exhibited a significant AMPK activation effect, which was blocked by compound C. At the same time, Man downregulated the expression of NLRP3 inflammasome-related proteins and inhibited the activation of NLRP3 inflammasome, alleviating cell pyroptosis and inflammation effects. These results indicate that Man anti-NAFLD activity is mediated through its regulation of glucolipid metabolism by AMPK activation and its anti-inflammatory effects by NLRP3 inflammasome inhibition. Our study indicates that Man is a promising prodrug for the therapy of NAFLD patients.

THE EFFECT OF COPPER OXIDE AND SELENIUM NANOPARTICLES ON VITAMIN D LEVELS IN WOMEN WITH INFERTILITY

The nanoparticles of both copper oxide (CuO NPs) and selenium (Se NPs) were synthesized by a laser ablation method that is fast and safe in biological applications. It was Characterization by atomic force microscopy (AFM), Xray diffraction (XRD), field emission scanning electron microscopy (FESEM) and atomic force microscopy (AFM), which showed that the size of the nanoparticles was 20-23 nm for Se NPs and 19-23 nm for CuO NPs. The effectiveness of these nanoparticles was examined on vitamin D levels in the group of women with primary infertility (PP) and the group of women with secondary infertility (SP). The results showed a highly significant activation effect of the copper oxide nanoparticles, with an activation rate equal to 13% for the primary sterility group (P = 0.003) and 23% for the secondary sterility group (P = 0.00)

Aqueous Tuber Extracts of Tylosema fassoglense (Kotschy ex Schweinf.) Torre and Hillc. (Fabaceae). Possess Significant In-Vivo Antidiarrheal Activity and Ex-Vivo Spasmolytic Effect Possibly Mediated by Modulation of Nitrous Oxide System, Voltage-Gated Calcium Channels, and Muscarinic Receptors.

Tylosema fassoglense (TFG) is used as an antidiarrheal traditional medicine in Western Kenya. This study aimed to investigate the antidiarrheal activity of its aqueous extracts in-vivo and the putative mechanism (s) of action ex-vivo using Sprague-Dawley rats and New Zealand white rabbits respectively. The in-vivo antidiarrheal effects of the extract were evaluated in castor oil-induced diarrhea, the castor oil-induced enteropooling, and phenol red gastric motility tests. On the other hand, isolated rabbit’s jejunal segments were used to evaluate the spasmolytic effect of TFG on spontaneous contraction, in acetylcholine-induced contraction, in presence of 80mMK+, calcium chloride-induced contraction as well as in presence of the following antagonists: naloxone, methylene blue, L-NAME, prazosin, and propranolol in the ex-vivo studies. The data were express as Mean ± S.E.M and analyzed by one-way ANOVA and Tukey’s post hoc test in cases of significance which was set at p < 0.05. The extract was phytochemically characterized using Liquid chromatography Mass spectroscopy (LC-MS).The extract possessed significant inhibitory effect in the in-vivo experiments. The extract exhibited significant spasmolytic effect on both spontaneous contraction and in jejunal segment pre-contracted acetylcholine as well as in presence of 80mMK+ solution. It also attenuated the spasmogenic effect of various concentration of calcium chloride. The extract’s spasmolytic effect was, however, significantly attenuated in presence of several antagonists (methylene blue and L-NAME) but the adrenergic blockers (prazosin and propranolol) had no significant effect in the ex-vivo studies. LC-MS identified thirty compounds where Proathocyanidin (11.54%), Syringic acid (7.30%), and 4-Hydroxybenzoic acid (6.19%) had the highest percentage abundance. In conclusion, the results obtained in this study partially validate the traditional uses of the tubers of this plant species as an antidiarrheal. These antidiarrheal effects are probably mediated via modulation of nitrous oxide pathway, voltage gated calcium channels, and muscarinic receptors.

Formononetin Activates the Nrf2/ARE Signaling Pathway Via Sirt1 to Improve Diabetic Renal Fibrosis.

Oxidative stress is the main factor responsible for the induction of diabetic renal fibrosis. Thus, improving the state of oxidative stress can effectively prevent the further deterioration of diabetic nephropathy (DN). Previous research has shown that formononetin (FMN), a flavonoid with significant antioxidant activity and Sirt1 activation effect, can improve diabetic renal fibrosis. However, the exact mechanisms underlying the effect of FMN on diabetic renal fibrosis have yet to be elucidated. In this study, we carried out in vivo experiments in a db/db (diabetic) mouse model and demonstrated that FMN activated the nuclear factor E2-related factor 2 (Nrf2)/antioxidant response element (ARE) signaling pathway and improved oxidative stress by increasing levels of sirtuin-1 (Sirt1) protein level in renal tissue. We also found that this process reversed the up-regulation of fibronectin (FN) and intercellular adhesion molecule 1 (ICAM-1) and led to an improvement in renal insufficiency. In vitro results further showed that FMN significantly reversed the upregulation of FN and ICAM-1 in glomerular mesangial cells (GMCs) exposed to high glucose. FMN also promoted the expression of Nrf2 and widened its nuclear distribution. Thus, our data indicated that FMN inhibited hyperglycemia-induced superoxide overproduction by activating the Nrf2/ARE signaling pathway. We also found that FMN up-regulated the expression of Sirt1 and that Sirt1 deficiency could block the activation of the Nrf2/ARE signaling pathway in GMCs induced by high glucose. Finally, we found that Sirt1 deficiency could reverse the down-regulation of FN and ICAM-1 induced by FMN. Collectively, our data demonstrated that FMN up-regulated the expression of Sirt1 to activate the Nrf2/ARE signaling pathway, improved oxidative stress in DN to prevent the progression of renal fibrosis. Therefore, FMN probably represents an efficient therapeutic option of patients with DN.