TLC Identification of Yao Medicine Pileostegia tomentellal and Extraction Technology and Content Determination of Umbelliferone

[Objectives]To establish a TLC and content determination method of Pileostegia tomentellal,with umbelliferone as the indicator component.[Methods]TLC identification was performed by silica gel G thin layer plate with n-hexane-ethyl acetate(4:3)as the developing agent,and the plate was examined by UV lamp(365 nm).The umbelliferone content was determined by HPLC:Inertsil ODS-3 C 18 column(4.60 mm×250 mm,5μm);mobile phase acetonitrile-0.2%phosphoric acid gradient elution;detection wavelength 320 nm,flow rate 1.0 mL/min,column temperature 30℃,injection volume 10μL.[Results]The chromatogram of P.tomentellal showed the same color spot in the same position as that of reference medicinal material,and the spot was clear with good specificity.Umbelliferone showed a good linear relationship when the injection volume was 2.63-131.27μg/mL(R^(2)=0.9997).The average recovery of umbelliferone in the low,middle and high adding groups of P.tomentellal was 99.57%and the RSD was 2.15%.[Conclusions]The method can effectively identify Yao medicine P.tomentellal and accurately determine the content of umbelliferone in medicinal materials,which will provide a scientific basis for the development and utilization of medicinal resources of Yao medicine P.tomentellal.

Renoprotective effect of umbelliferone in high-fat diet/streptozotocin-induced type 2 diabetic rats

Objective:To evaluate the renoprotective effect of umbelliferone in high-fat diet/streptozotocin-induced type 2 diabetic rats.Methods:We established a streptozotocin-induced type 2 diabetic model in male Wistar rats.The rats were fed with high-fat diet(45 kcal%lard fat)and injected with 35 mg/kg streptozotocin.Diabetic rats were treated with umbelliferone for 8 weeks.At the end of the experimental period,the serum and kidney were used for measuring biochemical parameters,protein expression and histological analysis.Results:After 8-week treatment,umbelliferone decreased fasting plasma glucose,concentrations of malondialdehyde and monocyte chemoattractant protein-1 in the plasma and tissues.It also significantly reduced serum creatinine,blood urea nitrogen,serum advanced glycation end products,as well as kidney weight in type 2 diabetic rats(P<0.05).Moreover,umbelliferone reduced the 24-h urine albumin,but increased 24-h urine creatinine excretion(P<0.05).In renal protein expression,umbelliferone decreased the levels of transforming growth factor-β1 and fibronectin while increasing the levels of superoxide dismutase and catalase(P<0.05).Renal histological examination revealed an enlarged glomerular size in diabetic rats,which was smaller in umbelliferone-treated diabetic rats.Conclusions:Umbelliferone alleviates renal dysfunction in diabetes via decreasing hyperglycemia,oxidative stress,inflammation and glycation.

Umbelliferone ameliorates renal function in diabetic nephropathy rats through regulating inflammation and TLR/NF-κB pathway

Diabetic nephropathy(DN) is a leading cause of renal failure, contributing to severe morbidity and mortality in diabetic patients. Umbelliferae(Umb) has been well characterized to exert protective effects in diabetes. However, the action and mechanism of Umb in DN remains unclear. In this work, we studied the effect of Umb in a streptozotocin(STZ)-induced DN rat model and explore its underlying mechanism. DN rats were treated with Umb(20, 40 mg·kg^(-1)) or irbesartan(15 mg·kg^(-1)) for 4 weeks. Levels of serum glucose, insulin, blood uric acid, creatinine, triglycerides(TG) and total cholesterol(TC) were measured by commercial assay kits,respectively. Histopathological changes and inflammatory cytokine levels including IL-6, IL-1β and TNF-α in the kidney were also evaluated. Alterations in the expression of podocin, CD2 AP and TLR/NF-κB were assessed by western blotting. Our results showed that Umb reduced renal injury in DN rat model, as evidenced by the decrease in blood glucose, 24 h urinary protein, serum creatinine,and blood uric acid. Umb also significantly ameliorated the renal histopathological alteration, and down-regulated the expression of epithelial-to-mesenchymal transition-related molecular markers podocin and CD2AP. Moreover, Umb inhibited TLR2, TLR4, MyD88 expressions, NF-κB activation and considerably reduced levels of other downstream inflammatory molecules(TNF-α, IL-6, IL-1β).These findings indicated that Umb improved renal function through regulating inflammation and TLR/NF-κB pathway, suggesting the potential efficacy of Umb in DN treatment.

Anti-Alzheimer's disease potential of coumarins from Angelica decursiva and Artemisia capillaris and structure-activity analysis

Objective: To use structure-activity analysis to study the anti-Alzheimer's disease(anti-AD) activity of natural coumarins isolated from Angelica decursiva and Artemisia capillaries, along with one purchased coumarin(daphnetin). Methods: Umbelliferone, umbelliferone 6-carboxylic acid, scopoletin, isoscopoletin, 7-methoxy coumarin, scoparone, scopolin, and esculetin have been previously isolated; however 2'-isopropyl psoralene was isolated from Angelica decursiva for the first time to evaluate their inhibitory effects against acetylcholinesterase(ACh E), butyrylcholinesterase(BCh E), and β-site amyloid precursor protein cleaving enzyme 1(BACE1) enzyme activity. We scrutinized the potentials of coumarins as cholinesterase and BACE1 inhibitors via enzyme kinetics and molecular docking simulation. Results: Among the test compounds, umbelliferone 6-carboxylic acid, esculetin and daphnetin exhibited potent inhibitory activity against ACh E, BCh E and BACE1. Both esculetin and daphnetin have a catechol group and exhibit significant anti-AD activity against ACh E and BCh E. In contrast, presence of a sugar moiety and methoxylation markedly reduced the anti-AD activity of the coumarins investigated in this study. With respect to BACE1 inhibition, umbelliferone 6-carboxylic acid, esculetin and daphnetin contained carboxyl or catechol groups, which significantly contributed to their antiAD activities. To further investigate these results, we generated a 3D structure of BACE1 using Autodock 4.2 and simulated binding of umbelliferone 6-carboxylic acid, esculetin and daphnetin. Docking simulations showed that different residues of BACE1 interacted with hydroxyl and carboxylic groups, and the binding energies of umbelliferone 6-carboxylic acid, esculetin and daphnetin were negative(-4.58,-6.25 and-6.37 kcal/mol respectively). Conclusions: Taken together, our results suggest that umbelliferone 6-carboxylic acid, esculetin and daphnetin have anti-AD effects by inhibiting ACh E, BCh E and BACE1, which might be useful against AD.

Management of early-onset sepsis in a teaching hospital: A descriptive retrospective study

Objective: To evaluate the management of early-onset sepsis at Saad Abul-Ella Teaching Hospital, Sudan. Methods: A descriptive retrospective hospital-based study was carried out at the Nursery Department of Saad Abul-Ella Teaching Hospital. All medical records of neonates with suspected or confirmed sepsis during the year 2017 were reviewed to evaluate the management of antibiotics for sepsis using a data collection form. Results: Out of the 205 cases, 82 neonates (40%) were diagnosed as early-onset sepsis, among which the majority was male (68%). All neonates were given cefotaxime plus vancomycin as empirical therapy which was changed to other antibiotics in 23% of the cases. The common risk factors associated with early-onset sepsis wereprolonged rupture of membrane (41.8%), preterm delivery (26.3%) and low birth weight (15.1%). Blood cultures were performed in 168 cases, and 19% had bacterial growth of Staphylococcus aureus which is the most common isolated pathogen. Conclusions: Cefotaxime plus vancomycin are the main empirical antibiotic for sepsis, and Staphylococcus aureus is the most common pathogen associated with early-onset sepsis.

Synthesizing Nanoparticles Using Reactions Occurring in Aerosol Phases

Our ultimate objective is to form nanoparticles by merging oppositely charged nanodroplets containing different constituents of the nanoparticle and construct a desktop apparatus to do this. These nanodroplets will be in oppositely charged aerosols originating from oppositely charged solutions containing the different component of the nanoparticle. In this paper, as the first stage in establishing the feasibility of this concept, we demonstrate that droplets formed from uncharged solutions will merge and the product of such reactions is the same as when their bulk solutions are mixed. We demonstrate that this is the case for three classes of reactions: the chemiluminescent reaction between Luminol and Potassium Ferricyanide, the pH sensitive fluorescence of Umbelliferone and the precipitation of Silver Chromate by reaction of Silver Nitrate with Potassium Chromate. We present arguments that our future goal using oppositely charged droplets is more efficient synthetically and will produce a narrow distribution of nanoparticle sizes.