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The solubility of genistein was measured in the binary system of ethanol and water at temperatures ranging from 288.2 to 328.2 K. The obtained data were correlated with the modified Apelblat model, Yalkowsky model

The different parts of Platycodon grandiflorum were collected from a medicinal herb garden to determine five heavy metal(loid)s (Pb, Cd, As, Hg, and Cu) contents at different growth stages. The data showed that the plant accumulated varying amounts of metal(loid)s in the order Cu > Hg > Pb > As > Cd. Five heavy metal(loid) concentrations decreased in the early growth stage and then increased in the flowering season. The contents of heavy metal(loid)s except Hg in the stem were relatively lower than other tissues. The flower of Platycodon grandiflorum can highly accumulate heavy metal(loid)s, especially for Cu in the flowering period. Pb, Cd, and Cu contents in stem generally increased with growth time, while Cd and Cu in root decreased during growth time. The average daily intake doses of five heavy metal(loid)s in the root of Platycodon grandiflorum were all below the safety guideline and the target hazard quotient was less than 1.

Lovastatin is a typical drug interacting with grapefruit juice and naringin and vitamin C are main active constituents in fruit juice. It is necessary to study the interaction between lovastatin and digestive enzymes and the effect of naringin and vitamin C on the interaction. Pepsin, trypsin and α-chymotrypsin were selected as representatives of digestive tract enzymes, and fluorescence spectroscopy was employed to study the interaction of lovastatin with three digestive enzymes and the effect of naringin and vitamin C on this interaction. The mechanism of interaction between lovastatin and three digestive enzymes was static quenching. Lovastatin bound to trypsin by electrostatic interaction, while bound to pepsin or α-chymotrypsin mainly by hydrophobic interaction. The conformation of three enzymes changed and non-radiative energy transfer occurred with high probability between three digestive enzymes and lovastatin. Both naringin and vitamin C could reduce the binding stability of lovastatin to pepsin and α-chymotrypsin, increasing concentration of free lovastatin. That is, naringin or vitamin C in the fruit or food may increase the blood concentration of lovastatin; perhaps taking frequency or dosage of lovastatin may be reduced.

The interaction mechanisms of nimodipine with pepsin, trypsin, α-chymotrypsin, lysozyme and human serum albumin were investigated by multispectral and molecular docking methods. Vitamin C and naringin were the main active components of grapefruit juice, and nimodipine was the typical drug that interacts with this juice. Fluorescence spectroscopy was used to study the interaction of nimodipine with five proteinases (pepsin, trypsin, α-chymotrypsin, lysozyme and human serum albumin) and the effects of vitamin C and naringin on these interactions. The fluorescence quenching results showed that nimodipine can quench the intrinsic fluorescence of these five proteinases by a static quenching procedure. Nimodipine binds to pepsin and α-chymotrypsin, through hydrogen bonding and van der Waals forces, whereas it binds to trypsin, lysozyme and human serum albumin mainly by hydrophobic interactions. The microenvironment of the five proteinases changed. The probability of nonradiative energy transfer between the five proteinases and nimodipine was high. Both vitamin C and naringin reduced the binding constant of nimodipine to the four proteinases (except α-chymotrypsin) and might increase the concentration of free nimodipine. Thus, vitamin C or naringin in fruits or foods could increase the blood concentration of free nimodipine and perhaps a reduction in nimodipine dose was needed.

We report epidemiologic, laboratory, and clinical findings for 7 patients with 2019 novel coronavirus disease in a 2-family cluster. Our study confirms asymptomatic and human-to-human transmission through close contacts in familial and hospital settings. These findings might also serve as a practical reference for clinical diagnosis and medical treatment.

In this study, UC rat model was established by administration of 5% (w/v) dextran sulfate sodium, and the pharmacokinetics of verapamil and norverapamil were evaluated in normal and UC rats using UPLC-MS/MS after oral administration of 5 mg/kg and 50 mg/kg verapamil.The peak concentration (C

The heavy metals and deleterious element (Pd, Cd, Cu, As, and Hg) in Chinese peony (Paeonia lactiflora Pall.) were determined by Tessier's sequence extraction method. Pb mainly existed in carbonate fraction. The main fraction of Cd in different tissues and different month is quite different. Cu mainly exists as exchangeable carbonate fractions. Five forms of Hg all exist in leaf, stem, and root. The total absorbable fraction of Pd, Cd, Cu, As, and Hg was different in different tissues. The total content of heavy metals can migrate from different tissues and the content of different speciation of heavy metal also can change during the growing period of plants. The results showed that different parts of plants and different elements resulted in different distribution and mobility. Base on this, it is more scientific and reasonable to clarify the migration and enrichment and to analyses the speciation of heavy metals during growing period of plant medicine. It is more scientific and reasonable to clarify the migration and enrichment, and to analyses the speciation of heavy metals during growing period of plant medicine.

Eupatorium fortunei Turcz. is a widely used Chinese herbal medicine in China. In this study, a gas chromatography-triple quadrupole mass spectrometry (GC-MS/MS) method was developed and validated to simultaneously determine the contents of p-cymene, thymol, neryl acetate, and β-caryophyllene in roots, stems, and leaves of Eupatorium fortunei Turcz. harvested at different growth periods. All four constituents could be detected in leaves, three could be detected in stems except β-caryophyllene, and only thymol could be detected in roots. The order of the total contents of four constituents in different parts was leaves > stems > roots. It indicated that the leaves could be the proper medicinal parts of Eupatorium fortunei Turcz. The content of four constituents in leaves varied a lot among different growth periods and showed an M-shaped change trend with the growth of Eupatorium fortunei Turcz. The four constituents accumulated to the highest values in early July followed by mid-September. Accordingly, the best harvest time of Eupatorium fortunei Turcz. is early July and mid-September.

Nitric oxide (NO) dysfunction has been found to be an important factor in both the development and progression of diabetic complications due to its many roles in the vascular system. Multifunctional compounds with hypoglycemic and endothelial protective action will be promising agents for the treatment of diabetes and its complications. In this study, a series of novel NO-donating sitagliptin derivatives and relevant metabolites were synthesized and evaluated as potential multifunctional hypoglycemic agents. All of synthetic compounds shown remarkable inhibitory activity against dipeptidyl peptidase IV (DPP-IV) in vitro and demonstrated excellent hypoglycemic activities in diabetic mice, similar to the activity of sitagliptin, and compounds T1-T4 shown different extents of NO-releasing abilities and potent antioxidant abilities in vivo. By screening in DPP-4, compound T4 was recognized as a potent DPP-4 inhibitor with the IC50 value of 0.060 μM. Docking study revealed compound T4 has a favorable binding mode. Furthermore, compounds T1-T4 exhibited different extents of NO-releasing abilities and excellent anti-platelet aggregation in vitro. The overall results suggested that T4 could help to the amelioration of endothelial dysfunction by reducing blood glucose, lessening oxidative stress and raising NO levels as well as inhibiting platelet aggregation. Based on this research, compound T4 deserves further investigation as potential new multifunctional anti-diabetic agent with antioxidant, anti-platelet aggregation and endothelial protective properties.

Objective To observe the differences in curative effects between prophylactic and therapeutic administrations of Gliclazide (GLZ) or Methylcobalamin (MCA) on diabetic peripheral neuropathy in rats. Methods GLZ (25 mg/kg/day) or MCA (175 μg/kg/day) was orally administrated prophylactically to streptozotocin-induced diabetic rats for 8 weeks before diabetic peripheral neuropathy developed or administrated therapeutically after diabetic peripheral neuropathy developed, respectively. The motor nerve conduction velocities (MNCV), aldose reductase (AR) activities, the polyol contents and antioxidative enzyme activities in the sciatic never tissues were determined. The morphology of sciatic never tissues was observed. Results In comparison to vehicle, most of the changes in the sciatic nerves of the diabetic rats (e. g., delayed MNCV, altered/damaged nerve structure, enhanced AR activity, increased polyol contents, altered Cu, Zn-superoxide dismutase, glutathione-peroxidase activities, and elevated malondialdehyde level) were significantly ameliorated by prophylactic administration with either GLZ or MCA. In contrast, only few of above-mentioned parameters were alleviated in DPN rats by therapeutic administration with GLZ or MCA as compared to vehicle. The curative effects of GLZ or MCA prophylactic administration on MNCV, AR activity, polyol contents and antioxidative enzyme activities were markedly stronger than therapeutic administration. Conclusion Prophylactic administration of GLZ or MCA was superior to the therapeutic administration in alleviation of diabetic neuropathy in STZ-rats, suggesting that pharmacotherapy should be initiated at a much earlier stage before diabetic neuropathy developed, but not at a later stage after never damage reached.

Rationale Xiao Chai Hu Tang (XCHT, Sho-saiko-to in Japanese) is a well-known medicine formula used in Asia for centuries. However, the quality control and the absorption of XCHT components are the major remaining concerns.. The study was to develop a sensitive and robust method to characterize the chemical components in XCHT and evaluate their absorptions. Methods An ultra-high pressure liquid chromatography coupled with electrospray ionization quadrupole time-of-flight mass spectrometry (UHPLC-ESI-QTOF MS/MS) was used to identify the compounds in XCHT. The Caco-2 cell culture model was employed to determine the absorption of the identified components. Results The results showed that 109 compounds were identified including organic acids, flavonoids, saikosaponins, ginsenosides, licoricesaponins and gingerols. The absorption study showed that among those identified, 33 compounds have decent absorption permerbilities ranging from 1.46 ± 0.24×10-7 to 3.10±0.61×10-5 cm/sec. These compounds were classified as classes II and IV in the biopharmaceutical classification system (BCS). Conclusions These identified compounds could be used to characterize quality of XCHT and those absorbed compounds with decent permreabiliteis are the potential active components in XCHT. Future pharmacodynamics studies should focus on these absorbed compounds.

Hydroxytyrosol (HT) is a natural polyphenol antioxidant that exists in olive oil. In the study of multifunctional hypolipidemic of nicotinic derivatives, we found that hydroxytyrosol nicotinate (HT-N) incorporation of niacin with HT displayed ?-glucosidase inhibitory activities in vitro, such as yeast ?-glucosidase (IC50?=?117.72??M) and rat intestinal ?-glucosidases maltase (IC50?=?31.86??M) and sucrase (IC50?=?22.99??M), and had a good control of postprandial blood glucose (PBG). HT-N shown significantly hypoglycemic action by 16.9% and protection of pancreatic tissue in type 2 diabetic mellitus (T2DM) mouse model. HT-N also shown a potent antioxidant activity and property of anti-glycation in vitro, which were benefit for ameliorating diabetic complications. Moreover, HT-N exhibited much significant hypolipidemia, lowering plasma triglyceride (TG), total cholesterol (TC), and malonaldehyde (MDA) by 34.6%, 45.8% and 32.1% respectively, in hyperlipidemic mice induced by Triton WR 1339. The results indicated that HT-N has hypolipidemic, hypoglycemic and antioxidant actions. All these properties could be conducive to amelioration of oxidative stress, hyperlipidemia, and diabetes that HT-N may serve as a multifunctional potential therapeutic strategy in diabetic patients with hyperlipidemia.

Emerging evidence suggests that inflammation plays a pivotal role in Atherosclerosis. Sirtuin 6 (SIRT6), a member of NAD+-dependent protein lysine deacylases of the sirtuin family, plays an important role in the regulation of metabolism, aging and stress resistance. However, the role of SIRT6 in vascular inflammation and its molecular mechanism is unknown. The present study showed that TNF-α significantly reduced the expression of SIRT6 protein and mRNA in a concentration- and time-dependent manner and increased the expression of monocyte chemotactic protein 1 (MCP-1), interleukin (IL) -6 and IL-1β in human umbilical vein endothelial cells (HUVECs). Overexpression of SIRT6 but not its catalytically inactive mutant inhibited TNF-α-induced expression of MCP-1, IL-6 and IL-1β. Knockdown of SIRT6 significantly enhanced TNF-α-induced expression of MCP-1, IL-6 and IL-1β. Moreover, knockdown of SIRT6 reduced TNF-α-induced nuclear factor erythroid 2 related factor 2 (NRF2) nucleus protein expression, whereas knockdown of NRF2 significantly enhanced TNF-α-induced expression of MCP-1, IL-6 and IL-1β. In addition, overexpression of SIRT6 increased NRF2 and its target genes expression, and knockdown of SIRT6 decreased NRF2 and its target genes expression. Meanwhile, knockdown of SIRT6 inhibited NRF2 nucleus protein expression. Further, knockdown of SIRT6 decreased phosphorylation of NRF2, overexpression of SIRT6 increased phosphorylation of NRF2. SIRT6 interacted with NRF2. In vivo, the levels of TNF-α and IL-1β were increased in the serum of hyperlipidemia mice. Hyperlipidemia-induced production of MCP-1, IL-6 and IL-1β was significantly augmented in the endothelium specific SIRT6 knockout mice. In contrast, the expression of NRF2 and its target genes was reduced. Taken together, these results indicate that SIRT6 protects against vascular inflammation via its deacetylase activity and the NRF2-dependent signaling pathway.

Dyslipidemia, oxidative stress and inflammation are major risky factors involved in the pathophysiology of type 2 diabetes mellitus and atherosclerosis. Multifunctional intervene is more meaningful. The aim of this study was to evaluate the multifunctional effects of two new compounds, combination of fenofibric acid (FA) with tyrosol (T) or hydroxytyrosol (HT). Compared with fenofibrate (FF), FF-HT exhibited excellent antioxidant capacities in vitro and much improved hypolipidemia, reducing plasma triglyceride (TG), total cholesterol (TC), and malonaldehyde (MDA) by 76%, 54%, and 28%, while FF-T decreased the plasma parameters by 16%, 10%, and 20% in hyperlipidemic mice induced by Triton WR 1339. Furthermore, compound FF-HT exhibited significant antihyperglycemic, antihyperlipidemic, antioxidant and anti-inflammatory activities as well as attenuating hepatotoxicity in a type 2 diabetes experimental mouse model. The histological findings showed that FF-HT suppressed the development of hepatic lipid accumulation and ameliorated the damage in hepatic and pancreatic tissues compared to model mice. This study indicates for the first time that reasonable optimized drug design produce a compound entity which is conducive to the prevention of type 2 diabetes mellitus and its complications.

Phenylsulfonyfuroxan nitric oxide (NO)-donor phenols were designed, synthesized and evaluated. The compounds were designed through a symbiotic approach using selected phenols and phenylsulfonylfuroxan NO-donor. The antioxidant activities of the hybrid compounds T2-T6 showed to be good in vivo. Compounds T4 and T6 revealed excellent yeast α-glucosidase inhibitory activity and anti-glycosylation activity. All of the compounds exhibited strong NO releasing activity and significant anti-platelet aggregation activity. The inhibition of platelet aggregation was more than 50% at low concentration (1.5μM) and 95% at higher concentration (15μM and 150μM). The vasodilatation experiment demonstrated that the six compounds under test exhibited definite vasodilation activity (pIC50 ranged from 5.698 to 6.383), especially compound T6 (pIC50 was 6.383) which was similar to sodium nitroprusside (pIC50 was 6.786). Both anticoagulant and vasodilatation effects were correlated with their NO releasing activities. These hybrid phenylsulfonyfuroxan-based NO-donor phenols offer a multifunctional prodrug design concept for the development of therapeutic or preventive agents for metabolic syndrome.

Different polymorphic forms can affect the performance of the drug product. In addition, isomorphic crystals show different chemical and physical properties due to the changes in the crystal habit. However, it is unclear whether the crystal habit results in different pharmacological activity. The aim of this study was to investigate whether the pharmacological effect of ibuprofen could be affected due to the variety of the crystal habit. Solvent change technique and conventional fusion method were carried out to modify the characteristics of ibuprofen. The physicochemical properties of each were investigated using powder X-ray diffraction (PXRD), Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC) techniques. Results of scanning electron microscopy (SEM) analysis revealed differences in the surface characteristics of the crystals obtained. Further study revealed that the samples crystallized exhibited the remarkable variation on the dissolution profiles in different dissolution medium. Moreover, in vivo antinociceptive and anti-inflammatory findings demonstrated that the crystal habit modifications resulted in the different therapeutic efficacy. Taken together, these results indicate that the modification of the crystal habit had a great influence on the in vivo pharmacological activity of ibuprofen crystals.

Hydroxytyrosol acetate (HT-AC), a polyphenolic compound in olive oil, exerts an anti-inflammatory effect on murine collagen-induced arthritis. However, the effect of HT-AC on inflammatory response in cardiovascular disease remains unclear. Thus, in this study, we aimed to investigate the effect of HT-AC on the inflammation response of vascular endothelial cells and the related molecular mechanism. Our results showed that HT-AC inhibited the inflammatory response in hypercholesterolemic mice and tumor necrosis factor (TNF)-stimulated HUVECs. Meanwhile, HT-AC also up-regulated SIRT6 expression in hypercholesterolemic mice and HUVECs. To further investigate whether SIRT6 is involved in the regulation of endothelial inflammatory response by HT-AC, endothelium-specific Sirt6 knockout (Sirt6endo-/-) mice were used. Our study found that Sirt6endo-/- abolished the inhibition of inflammatory response by HT-AC in the thoracic aorta of hypercholesterolemic mice. In vitro study also showed that knockdown of SIRT6 reduced the inhibition of inflammatory response by HT-AC, whereas overexpression of SIRT6 augmented the inhibition of inflammatory response by HT-AC in HUVECs. Further study demonstrated that HT-AC exerts its anti-inflammatory effect partly via the SIRT6-mediated PKM2 signaling pathway. In addition, HT-AC inhibited TNF-induced inflammatory response through the TNF receptor superfamily member 1A (TNFRSF1A) signaling pathway. These findings indicate that HT-AC regulates the vascular endothelial inflammatory response partly through the TNFRSF1A/SIRT6/PKM2-mediated signaling pathway.

Traditional Chinese medicines (TCMs) are widely used to treat various diseases in China and some countries, and TCM products are becoming increasingly available and popular worldwide. But TCMs are facing the challenge of heavy metal pollution. In this work, we examined the total contents and fractionations of Pb, Cd, Hg, and Cu in six TCMs (Angelicae Sinensis Radix (ASR), Chuanxiong Rhizoma (CR), Polygonati Rhizoma (PR), Astragali Radix (AR), Carthami Flos (CF), and Paeoniae Radix Rubra (PRR)) and evaluated the health risk of four heavy metals in these TCMs. The results showed that Cd, Pb, and Cu contents were considerably high and the amount of Cd in six TCMs, Pb in CR, ASR, AR, and CF, and Hg in ASR, PR, and PRR exceeded the limit values. The predominant fractions of Pb, Cd, and Cu were exchangeable and carbonate fractions in six TCMs; Hg mainly existed in organic and residual fractions. The average daily intake dose (ADD) and target hazard quotient (THQ) of Pb based on total content and total THQ of four heavy metals based on bioaccessible fractions in AR and PRR exceeded the safety guideline. These results indicated that the potential health risk could occur by taking these TCMs.

The heavy metals and deleterious element (Pd, Cd, Cu, As, and Hg) in

Background The coronavirus disease 2019 (COVID-19) is spreading rapidly across countries and has infected tens of millions of people all over the world. So far, the pandemic is ongoing globally, and the situation is still worsening. Methods In this retrospective, single-center cohort analysis, we included 25 adult inpatients with laboratory confirmed COVID-19 disease from the affiliated hospital of Xuzhou Medical University (Xuzhou, China). Epidemiological characterizations, clinical findings, and medical treatments were all reported. In addition, laboratory markers were investigated in terms of course of treatment. Results Epidemiological features and clinical findings were present for all 25 patients. Laboratory markers were identified due to temporal changes. After medical treatment, all patients were discharged home and recovering from the infection. Conclusions This study provides a comprehensive overview of patients with COVID-19 disease in a single hospital. Some of the laboratory markers were statistically different during the course of the disease, which might serve as indicators in identifying patients with COVID-19 disease at an early stage of the infection.

Emerging evidences indicated that NLRP3 inflammasome initiates inflammatory response involved in cardiovascular disease. Nicotinic acid (NA) has been known to possess potential anti-inflammatory property. The aim of this study was to investigate the effect of NA on the activation of NLRP3 inflammasome and the underlying mechanisms. It was found that lipopolysaccharide (LPS) and adenosine triphosphate (ATP) triggered the activation of NLRP3 inflammasome in human umbilical vein endothelial cells (HUVECs). NA inhibited NLRP3 inflammasome activation and subsequent caspase-1 cleavage as well as interleukin (IL)-1β secretion. Moreover, NA administration up-regulated SIRT1 expression in HUVECs stimulated with LPS plus ATP. Importantly, knockdown of SIRT1 reversed the inhibitory effect of NA on the activation of NLRP3 inflammasome. Further study revealed that NA also decreased the generation of reactive oxygen species (ROS) in HUVECs. In addition, NA inhibited NLRP3 inflammasome activation partly through suppression of ROS. Taken together, these findings indicate that NA is able to regulate the activation of NLRP3 inflammasome in HUVECs, which may be partly mediated by SIRT1 and ROS.

The effect of myricetin (MY) and dihydromyricetin (DMY) on the activity of pepsin was evaluated. The interaction between MY and DMY with pepsin was investigated using multispectroscopic and molecular docking methods. Binding constant, number of binding sites, and thermodynamic parameters at different temperatures were measured. MY and DMY have no significant effect on the activity of pepsin. The results of fluorescence quenching revealed that MY and DMY could strongly quench the intrinsic fluorescence of pepsin through a static quenching procedure. The thermodynamic parameters showed that hydrophobic interactions played main roles in the interaction of MY with pepsin, while the Van der Waals' interactions and hydrogen bonds were mainly interactions between DMY and pepsin. The analysis of UV absorption spectra and molecular docking showed that MY and DMY induced conformational changes of pepsin. The synchronous fluorescence spectra indicated that microenvironment around tyrosine and tryptophan residues of pepsin were not changed obviously. The energy transfer from pepsin molecules to MY or DMY occurs with high probability. Displacement experiments indicated that DMY and MY could bind to the same site of pepsin.

The previous investigation suggested the approach for an in situ formation of Cr2O3 diffusion barrier by annealing the cold-sprayed Ni coatings on 310SS. In this paper, the influences of annealing conditions on the growth kinetics of Cr2O3 and substrate microstructure were investigated. Results show that Cr2O3 formed at the selected annealing temperatures of 850, 900 and 950°C for different durations of 4, 8 and 20 h. Increasing temperature enhanced the growth kinetics of Cr2O3 and the Mn content in the oxide layer. The annealing process for the growth of Cr2O3 improves the coating adhesion compared to the as-deposited coating. However, annealing at 950°C resulted in the precipitation of chromium carbides and enhanced the element inter-diffusion across the substrate/coating interface.

The interaction of pepsin with daidzein (Dai) or genistein (Gen) was investigated using spectroscopic techniques under simulated physiological conditions. Dai and Gen can quench the fluorescence of pepsin and the quenching mechanism was a static process. The binding site number n and apparent binding constant K were measured at different temperatures. The thermodynamic parameters ΔΗ, ΔG and ΔS were calculated. The results indicated that van der Waals forces and hydrogen bond formation played major roles in the interaction of Dai or Gen with pepsin. The binding distance between pepsin and Dai or Gen was calculated according to energy transfer theory. The results of synchronous fluorescence spectra showed that the microenvironment and conformation of pepsin were changed. UV absorption and 3D fluorescence spectra showed that the binding interaction disturbed the microenvironment of amino acid residues and induced conformational changes in pepsin. Molecular docking results showed that Dai and Gen entered into the hydrophobic cavity of pepsin and two hydrogen bonds formed between Dai or Gen and pepsin. The results demonstrated that the interaction behavior between Dai and Gen with pepsin was slightly different, which denoted that the 5-hydroxyl group of Gen, to a certain extent, had an effect on ligand binding to proteins. Copyright © 2016 John Wiley & Sons, Ltd.

The solubility of myricetin (MY) is very important in regard to its extraction and purification, which was performed by an equilibrium method in the binary solvent system of ethanol and water in th...

In this study, a series of salicylic acid derivatives were designed and synthesized as novel non-saccharide α-glucosidase inhibitors. Biological evaluation indicated that when compared to acarbose, compounds T9, T10, and T32 exhibited a higher potency of α-glucosidase inhibitory activity with IC50 values of 0.15 ± 0.01, 0.086 ± 0.01 and 0.32 ± 0.02 mM, respectively. Evaluation of the inhibition kinetics indicated that T9, T10, T32, and acarbose interacted with α-glucosidase in a mixed non-competitive inhibitory manner. Moreover, T9, T10, and T32 statically quenched the fluorescence of α-glucosidase by formation of an inhibitor-α-glucosidase complex. The docking results showed that hydrogen bonds were generated between the test compounds and α-glucosidase. The antioxidant study revealed that compound T10 exhibited a higher antioxidant activity via scavenging 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH), thereby inhibiting lipid peroxidation and the total reduction capacity. In brief, the salicylic acid derivatives identified in this study were promising candidates for development as novel non-saccharide α-glucosidase inhibitors.

The extraction of daidzein and genistein from soybean has been studied and the kinetic modeling was established using four modeling equations. The goodness of fit was evaluated by statistical errors including the standard error of means (SEM), the adjusted correlation coefficient (R

Soybean [Glycine max (Linn.) Merrill] and mung bean [Vigna radiate (Linn.) Wilczek] plants were challenged with 5 kinds of heavy metals [cadmium (Cd), chromium (Cr), copper (Cu), lead (Pb) and mercury (Hg)] in a hydroponic system. We applied 4 different metal treatments to study the effects of heavy metals on several physiological and biochemical parameters in these species, including root length, heavy metal concentrations and allocation in different organs, superoxide dismutase, catalase, and peroxidase activities, the content of malondialdehyde (MDA), protein and chlorophyll. The data showed that the growth of the roots of soybean and mung bean was equally sensitive to external Hg concentrations. Soybean was more sensitive to external Cd concentrations, and mung bean was more sensitive to external Cr, Cu and Pb concentrations. Normal concentrations of heavy metal would not cause visible toxic symptoms, and a low level of heavy metal even slightly stimulated the growth of plants. With the rise of heavy metal concentration, heavy metal stress induces an oxidative stress response in soybean and mung bean plants, characterized by an accumulation of MDA and the alternation pattern of antioxidative enzymes. Meanwhile, the growth of plants was suppressed, the content of chlorophyll decreased and leaves showed chlorosis symptoms at high metal concentrations.

Oxidative stress has been regarded as the leading mechanism of the hepatotoxicity of clofibrate (CF). To achieve multifunctional novel hypolipidemic agents with hypolipidemia, antioxidant, and ameliorating liver injury, clofibric acid derivative hydroxytyrosol-clofibrate (CF-HT) was synthesized by molecular hybridization. CF-HT exhibited significant hypolipidemia, reducing serum triglyceride (TG), total cholesterol (TC), and malonaldehyde (MDA) by 30%, 33%, and 29% in hyperlipidemic mice induced by Triton WR 1339. CF-HT also shown hepatoprotective effect, a significant decrease in hepatic indices toxicity was observed, i.e. aspartate and lactate transaminases (AST and ALT) activities, alkalines phosphatases (ALP), and total bilirubin (TBIL) levels. The liver weight and liver coefficient were also ameliorated. Serum superoxide dismutase (SOD) was significantly elevated, and serum catalase (CAT) and malondialdehyde (MDA) content were remarkably restored. The hepatic glutathione (GSH) content was obviously increased and hepatic oxidized glutathione (GSSG) content was reduced dramatically by CF-HT, as compared to the CF treated mice (p 0.05). Moreover, the histopathological damage that hepatocyte hyperplasia and hypertrophy was also significantly ameliorated by treatment with CF-HT. Therefore, the results indicated that CF-HT exerted more potent hypolipidemic activity and definite hepatoprotective effect which may mainly be associated with its antioxidative property in mice.

Rapid and accurate identification of multiple toxins for clinical diagnosis and treatment of mushroom poisoning cases is still a challenge, especially with the lack of authentic references. In this study, we developed an effective method for simultaneous identification of amanita peptide toxins by liquid chromatography coupled with photodiode array detection and ion trap time-of-flight mass spectrometry. The accuracy and selectivity of the methodology were validated through similar multiple fragmentation patterns and characteristic ions of standard α- and β-amanitin. The developed method could successfully separate and identify major toxic constituents in Amanita mushrooms. Two amatoxins and three phallotoxins were confirmed in a single run through their fragmentation patterns and characteristic ions, which can be used as diagnostic fragment ions to identify mushroom toxins in complex samples. Furthermore, the performance of the developed method was verified by using real biological samples, including plasma and urine samples collected from rats after intraperitoneal administration of toxins. Thus, the development methodology could be crucial for the accurate detection of mushroom toxins without standard references.

Research on extraction of chrysin is crucial for theoretical purposes and for food industrial bioprocesses. Optimization and kinetics of chrysin extraction from seeds of Oroxylum indicum (L.) Vent. were analyzed using agitated solid-liquid extractions with ethanol and water mixtures. The influence of extraction process parameters was investigated. Optimized conditions for chrysin extraction were a 0.2 mole fraction of ethanol as an extraction solvent, a temperature of 318 K, an agitation speed 1,400 rpm, and a solid to solvent ratio of 1:30. The extraction kinetic behavior of chrysin followed first order kinetics. The kinetic expression developed by Spiro and Siddique was used and the model was in agreement with experimental results. The diffusion coefficient ranged from 1.38×10−11 to 19.43×10−11 m2·s−1 and the activation energy for extraction kinetics was 21.85 kJ·mol−1.

Nicotinic acid (NA) has recently been shown to inhibit inflammatory response in cardiovascular disease. Sirtuin1 (SIRT1), a NAD(+)-dependent class III histone deacetylase, participates in the regulation of cellular inflammation. We hypothesized that dietary supplementation of NA could attenuate vascular inflammation via modulation of SIRT1 pathway. New Zealand White rabbits received chow or chow supplemented with 0.6% (wt/wt) NA for 2 weeks. Acute vascular inflammation was induced in the animals by placing a non-occlusive silastic collar around the left common carotid artery. At 24 h after collar implantation, the collar-induced production of C-reactive protein and monocyte chemotactic protein-1 was significantly suppressed in the NA-supplemented animals. Meanwhile, NA also decreased the expression of cluster of differentiation 40 (CD40) and CD40 ligand, but up-regulated SIRT1 expression, both in rabbits and in lipopolysaccharide-stimulated endothelial cells. Moreover, knockdown of SIRT1 reversed the inhibitory effect of NA on CD40 expression. Further study revealed that NA also decreased the expression of CD40 partly through mammalian target of rapamycin. These results indicate that NA protects against vascular inflammation via the SIRT1/CD40-dependent signaling pathway.

The solubility of dihydromyricetin in the binary system of ethanol and water was measured by using UV spectrophotometric method at the maximum absorption wavelength of 290 nm from 288.15 K to 323.15 K. The solubility increases with temperature and mole fraction of ethanol in the binary system. The calculated solubility data of dihydromyricetin were computed by using three models, the modified Apelblat equation, the Buchowski–Ksiązczak λH equation, and the Jouyban–Acree equation. The modified Apelblat equation and λH equation are more suitable for correlating experimental solubility data of dihydromyricetin. The activity coefficients were calculated based on the results of thermal properties of DMY (obtained by DSC), presenting good consistency with the solubility behavior. In this study, the enthalpy and entropy of a solution were evaluated using the van't Hoff equation. The course of dihydromyricetin dissolving in the binary system in the experimental temperature range was endothermic.

The dissociation constants (pKa) of dalbergin and nordalbergin were measured at 298.2 K using ultraviolet (UV) spectroscopy method. The solubilities of dalbergin and nordalbergin in water, methanol, propanone, ethyl ethanoate, trichloromethane, and hexane have been determined by the UV spectrophotometric method from 283.2 to 308.2 K at atmospheric pressure. The experimental solubility values were correlated with a modified Apelblat equation, λh model, and ideal model. The pKa value of dalbergin is 8.91 ± 0.12, and the pKa1 and pKa2 values of nordalbergin are 7.31 ± 0.29 and 9.79 ± 0.39, respectively. The solubilities of dalbergin and nordalbergin in six solvents increase with an increase in temperature. The solubility order of dalbergin in six pure solvents was trichloromethane > propanone > ethyl ethanoate > methanol > hexane > water, whereas that of nordalbergin was propanone > methanol > ethyl ethanoate > trichloromethane > water > hexane. A comparison of the solubility of dalbergin with that of nordal...

The solubility of three types of benzamide derivatives S 1 , S 2 , and S 3 in six pure solvents, with various polarities, including toluene, ethyl acetate, acetone, chloroform, methanol, and water at temperatures ranging from 288.15 to 328.15 K (318.15 K for acetone) was determined by ultraviolet spectrophotometry at atmospheric pressure. The solubility of S 1 , S 2 , and S 3 in the selected solvents increased with the increase in temperature. The mole fraction solubility of S 1 was found to be the highest in methanol (1.2464 × 10 3 at 328.15 K) and the solubility of S 1 in the selected solvents was in the following order: methanol > acetone > chloroform > ethyl acetate > toluene > water. The highest mole fraction solubility of S 2 was found in chloroform (7.6750 × 10 3 at 328.15 K) and the solubility of S 2 in the six solvents followed the order: chloroform > methanol > acetone > ethyl acetate > toluene > water. However, for S 3 the mole fraction solubility was found to be highest in acetone (1.1520 × 10 3 at 318.15 K) and the order was acetone > methanol > ethyl acetate > chloroform > toluene > water. The experimental solubility data were correlated with the modified Apelblat equation, λ h model, and ideal model. The calculated solubility by the three models showed good agreement with the experimental values and the modified Apelblat equation provided the best correlation results. Based on the solubility data, the dissolution enthalpy and entropy of S 1 , S 2 , and S 3 were calculated by using the van't Hoff equation.

The biochemical activities of polydatin and resveratrol have been proven to own considerable medicinal potential. However, the extraction processes are yet to be fully characterized. This study explores particularly the optimization and kinetics of polydatin and resveratrol extraction from Rhizoma Et Radix Polygoni Cuspidati (the root of Polygonum cuspidatum ) in agitation extractions by ethanol and water mixtures. The effects of the parameters on several extraction processes have been fully investigated. The optimized condition for polydatin was found at 0.4 mole fraction of ethanol as the extraction solvents, temperature 323 K, agitation speed 500 rpm and solid to solvent ratio of 1:90. However, the optimized condition for resveratrol was 0.4 mole fraction of ethanol, temperature 323 K, agitation speed 800 rpm, solid to solvent ratio of 1:120. Furthermore, the extraction kinetics behavior of polydatin and resveratrol follows a first order kinetics with diffusion coefficient ranging from 3.59 × 10 −11 to 7.53 × 10 −11 m 2 s −1 and 3.90 × 10 −11 to 10.10 × 10 −11 m 2 s −1 for polydatin and resveratrol respectively. The values of activation energy for the extraction were found to be 3.96 kJ mol −1 for polydatin and 17.83 kJ mol −1 for resveratrol.

The solubility of naringin in the binary system of ethanol and water was measured by using UV spectrophotometric method at the maximum absorption wavelength (UV = 283 nm) from 283.15 K to 318.15 K under atmospheric pressure. The solubility increases with the increasing temperature and in the solvent system it exhibits a synergistic effect. The modified Apelblat model was applied to correlate the experimental solubility data, and the calculated solubilities were in good agreement with the experimental results. The process of the dissolution of naringin was always endothermic, and was influenced by two mechanisms which are enthalpy-driven and entropy-driven. Non-linear enthalpy–entropy compensation was found for naringin in the binary system of ethanol and water.

The solubilities of naringin and naringenin in methanol, isopropanol, ethyl acetate, petroleum ether, n-butanol, and hexane were measured by using UV spectrophotometric methods at the maximum absorption wavelength of (283 and 372) nm from (288.15 to 328.15) K. The solubilities of naringin and naringenin in different solvents increase with an increase of temperature. The solubility of naringin in the six solvents was in the order methanol > ethyl acetate > n-butanol > isopropanol > petroleum ether > hexane, and the solubility of naringenin in these solvents follows the order ethyl acetate > isopropanol > methanol > n-butanol > petroleum ether > hexane. The solubility of naringenin was significantly higher than naringin in all selected solvents because of the more similar polarity of naringenin with solvents. The solubilities of naringin and naringenin are calculated by using the modified Apelblat equation model, ideal model, and the λH equation model. From solubility data, the changes of dissolution enthal...

Saussureae involucratae Flos is the primary component of the jiangu capsule, which also consists of 12 types of natural medicine. It is a traditional Chinese medicine used to treat a number of conditions including arthralgia, cold and sore muscles, stiff limbs, inconvenient flexion and activity limitation caused by different types of osteoarthritis. The present study was performed to assess the safety of the jiangu capsule following acute and chronic administration in mice and rats. In the acute study, mice were treated with the jiangu capsule orally at 16 g/kg/day, the highest dose, for 14 days. In the chronic oral toxicity study, rats were treated with 2, 4 and 8 g/kg/day of the jiangu capsule for 6 months. The general condition, body weight changes, food and water consumption, hematological and biochemical parameters, urinalysis, systematic anatomy and organ weights of the rats were monitored and histopathological examination was performed at the end of 3 and 6 months' daily administration, and following 14 days of withdrawal. There were no signs of toxicity in the general condition and body weight of the mice was not significantly affected by the treatment. Furthermore, necropsy findings for the animals in the acute and chronic toxicity studies demonstrated that no mortalities had occurred. The results of the current study indicate that treatment with the jiangu capsule did not induce mortality or any detectable abnormalities in mice and rats.

α-Amanitin is the main lethal component of amanita mushrooms, and data on its toxicokinetics are few. The aim of this study was to develop a sensitive and cost-effective method to identify α-amanitin and investigate its toxicokinetic parameters using liquid chromatography-triple quadrupole tandem mass spectrometry. The colchicine was used as the internal standard (IS). The compounds were extracted from plasma samples by protein precipitation with acetonitrile (containing 1% formic acid). The analysis was performed through multiple reactions monitoring. The molecular ions and fragment ions of α-amanitin could be used as characteristic ions to perform qualitative analysis of α-amanitin. The assay was successfully validated by selectivity, linearity, matrix effect, precision and accuracy, recovery and stability according to the U.S. Food and Drug Administration Guidance, and applied to study the toxicokinetic profile of α-amanitin in rats after a single intraperitoneal administration.