Anti-Obesity Potential of Ponciri Fructus: Effects of Extracts,Fractions and Compounds on Adipogenesis in 3T3-L1 Preadipocytes

Background: Ponciri Fructus, a crude drug consisting of the dried immature fruits of Poncirus trifoliata (L.) Raf., is a popular folk medicine used for the treatment of allergy and gastrointestinal disorders in Korea and China. In this study, the anti-adipogenic activity of extracts and isolated compounds were evaluated using 3T3-L1 preadipocytes. Methods: Dried immature fruits were extracted and fractionated into n-hexane, ethyl acetate (EtOAc), n-butanol and water-soluble fractions. The ethanol extract and fractions were tested for anti-adipogenic activity in the 3T3-L1 cell line. The active fractions (n-hexane and EtOAc fractions) were further subjected to chromatographic techniques to isolate and identify active compounds. Furthermore, the isolated compounds were evaluated for their anti-adipogenic activity. Results: Altogether, seven compounds, including two flavonoids, one phytosteroid and four coumarin derivatives, were isolated. Ethanol extract, n-hexane fraction, EtOAc fraction and three isolated compounds (phellopterin, oxypeucedanin and poncirin) showed significant anti-adipogenic activity as observed by reduced lipid deposition in differentiated 3T3-L1 cells. Further, oxypeucedanin downregulated the key adipogenic markers, such as peroxisome proliferator-activated receptors proteins γ (PPAR-γ), sterol response element binding proteins-1 (SREBP-1), CCAAT/enhancer binding proteins-α (C/EBP-α), adipocyte-specific lipid binding proteins (FABP-4), adipocyte fatty acid binding proteins (aP2), lipoprotein lipase (LPL) and leptin. Conclusion: This study indicated that the ethanol extract, hexane fraction and ethyl acetate fraction of P. trifoliata fruits possess strong anti-adipogenic activity, containing the active compounds such as phellopterin, oxypeucedanin and poncirin. Further research is recommended to explore their efficacy and safety in animal and clinical models.     

1, 3-azaphospholo[5, 1-b]thiazolines and benzothiazoles

The title compounds 3 and 7 are novel heterocyclic systems incorporating two-coordinate phosphorus. They are obtained in reasonable to good yields from the condensation of suitable 2-ethyl-3-alkylthiazolinium and -benzothiazolium bromides 2 and 6 with phosphorus trichloride in the presence of triethylamine in an aprotic solvent. Intermediate dichlorophosphino-substituted N-ylides can be observed or isolated in some cases. From a 2-methyl-3-alkylthiazolinium bromide ( 2a ), a 1-(dichlorophosphino) substituted 1, 3-azaphospholo[5,1-b]thiazoline ( 4 ) was obtained. The chemical shift of the two-coordinate phosphorus in 1,3-azaphosphole derivatives clearly reflects the influence of the heterocyclic system annulated to its 1,5-bond and of the substituents in its 2-and 4-positions.     

Structure-mechanics statistical learning uncovers mechanical relay in proteins

A protein''s adaptive response to its substrates is one of the key questions driving molecular physics and physical chemistry. This work employs the recently developed structure-mechanics statistical learning method to establish a mechanical perspective. Specifically, by mapping all-atom molecular dynamics simulations onto the spring parameters of a backbone-side-chain elastic network model, the chemical moiety specific force constants (or mechanical rigidity) are used to assemble the rigidity graph, which is the matrix of inter-residue coupling strength. Using the S1A protease and the PDZ3 signaling domain as examples, chains of spatially contiguous residues are found to exhibit prominent changes in their mechanical rigidity upon substrate binding or dissociation. Such a mechanical-relay picture thus provides a mechanistic underpinning for conformational changes, long-range communication, and inter-domain allostery in both proteins, where the responsive mechanical hotspots are mostly residues having important biological functions or significant mutation sensitivity.

Protein residues exhibit specific routes of mechanical relay as the adaptive responses to substrate binding or dissociation. On such physically contiguous connections, residues experience prominent changes in their coupling strengths.     

Field dependence of hole mobility in TPD-doped polystyrene

Field and temperature dependence of hole mobility in N,N^′-diphenyl-N,N^′-bis(3-methylphenyl)-(1,1′-biphenyl)-4,4′-diamine (TPD) doped in polystyrene (PS) is studied using the transient photoconductivity technique. We observe both the positive and negative field dependence of mobility with increasing field and temperature. The field and temperature at which negative field dependence begins is low compared with earlier reports on similar systems (with 20 wt% dopant concentration). Results are discussed on the basis of the Gaussian disorder model (GDM), which predicts that the interplay of both the energetic and positional disorder of dopant molecules in the sample decides the slope of the logμ versus E^1/2 plot. The observed mobility dependence is rationalized on the basis of low energetic disorder in the sample. The reason for low energetic disorder is purely due to the film morphology of the sample. Even for a dopant concentration of 20 wt%, we observe clustering and chaining of TPD molecules, which may provide low energetic and positional disorder.     

Cosmological Models with Variable <Emphasis Type="Italic">G</Emphasis> in <Emphasis Type="Italic">C</Emphasis>-Field Cosmology

Cosmological models with variable G in C-field cosmology for barotropic fluid distribution in FRW space-time are investigated. To get the deterministic model of the universe, we have assumed that G=R ⁿ where R is the scale factor and n the constant. To obtain the results in terms of cosmic time t, we have assumed n=−1. We find that for n=−1, Creation field (C) and spatial volume increase with time, G and ρ (matter density) decreases with time, the model represent accelerating universe. Thus inflationary scenario exists in the model. The model is also free from horizon. The results so obtained match with the astronomical observations.     

Topological charge quantization via path integration: An application of the Kustaanheimo-Stiefel transformation

Editorial note: The complete text of this paper, dedicated to Professor Asim O. Barut, will appear in the August 1993 issue ofFoundations of Physics.     

Investigation of energy and exergy performance on a small-scale refrigeration system with PCMs inserted between coil and wall of the evaporator cabin

Journal of Thermal Analysis and Calorimetry - Domestic refrigerators have become an indispensable part of the modern life. Since they are connected to the electric mains and operate throughout the...     

Practicing Reform‐Based Science Curriculum in an Urban Classroom: A Hispanic Elementary School Teacher's Thinking and Decisions

This study explores the thinking and decisions of Vera (pseudonym), a Hispanic elementary teacher, while she enacted a reform‐based science curriculum in an urban school in the southern United States. Vera's thinking, decisions, experiences, and practices were documented over a 2‐year period. Using the data collected from semistructured interviews, participant observations and classroom documents, a rich and complex case study of Vera is developed in this paper. This case study describes how Vera makes curricular choices from reform‐based science curricula such as the LiFE curriculum; how she enacts those choices to empower poor urban minority students; how Vera believes that preparing students for the high‐stakes test is empowering because it ensures continued schooling for students; how, for Vera, teaching connected science using students' lived experiences is a risky act; and how she uses negotiation in her science teaching.     

Metabolite assignment of ultrafiltered synovial fluid extracted from knee joints of reactive arthritis patients using high resolution NMR spectroscopy

Currently, there are no reliable biomarkers available that can aid early differential diagnosis of reactive arthritis (ReA) from other inflammatory joint diseases. Metabolic profiling of synovial fluid (SF)—obtained from joints affected in ReA—holds great promise in this regard and will further aid monitoring treatment and improving our understanding about disease mechanism. As a first step in this direction, we report here the metabolite specific assignment of ¹H and ¹³C resonances detected in the NMR spectra of SF samples extracted from human patients with established ReA. The metabolite characterization has been carried out on both normal and ultrafiltered (deproteinized) SF samples of eight ReA patients (n = 8) using high-resolution (800 MHz) ¹H and ¹H─¹³C NMR spectroscopy methods such as one-dimensional ¹H CPMG and two-dimensional J-resolved¹H NMR and homonuclear ¹H─¹H TOCSY and heteronuclear¹H─¹³C HSQC correlation spectra. Compared with normal SF samples, several distinctive ¹H NMR signals were identified and assigned to metabolites in the ¹H NMR spectra of ultrafiltered SF samples. Overall, we assigned 53 metabolites in normal filtered SF and 64 metabolites in filtered pooled SF sample compared with nonfiltered SF samples for which only 48 metabolites (including lipid/membrane metabolites as well) have been identified. The established NMR characterization of SF metabolites will serve to guide future metabolomics studies aiming to identify/evaluate the SF-based metabolic biomarkers of diagnostic/prognostic potential or seeking biochemical insights into disease mechanisms in a clinical perspective.