In vivo antiarthritic activity of the ethanol extracts of stem bark and seeds of Calophyllum inophyllum in Freund’s complete adjuvant induced arthritis

Context: Calophyllum inophyllum Linn. (Clusiaceae) (CI) is traditionally used to treat pain, inflammation, eye disorders and rheumatism.

Objective: The present study evaluates the antiarthritic activity of the ethanol extract of the stem bark (ESBCI) and seeds (ESCI) of Calophyllum inophyllum in Freund’s adjuvant induced arthritic Wistar albino rat model.

Materials and methods: ESBCI and ESCI were screened for in vitro anti-inflammatory activity by proteinase inhibition and membrane stabilization assays. Acute oral toxicity studies were conducted according to OECD-425 guidelines. Antiarthritic activity of ESBCI and ESCI at the dose of 250?mg/kg/p.o. was evaluated by Freund’s adjuvant induced arthritic rat model.

Results: ESBCI and ESCI have shown maximum inhibition at 250?μg/mL in proteinase inhibition and haemolysis assays. The LD₅₀ of ESBCI and ESCI was found to be greater than 5000 and 2000?mg/kg/p.o., respectively. In Freund’s adjuvant induced arthritic rat model ESBCI, ESCI and Diclofenac treatment have shown 28.57, 36.36, and 43.51% as maximum reduction in rat paw oedema volume respectively when compared with the arthritic control rats. ESBCI and ESCI treatment at the dose level of 250?mg/kg/p.o. normalized the altered haematological and biochemical parameters of arthritic control rats. Histological and radiological evaluation confirmed the antiarthritic effect of ESBCI and ESCI.

Discussion: ESBCI and ESCI were found to show significant antiarthritic activity evidenced with clinical, biochemical, histological and radiological evaluations.

Conclusion: The present study indicates the antiarthritic activity of ESBCI and ESCI, however its mechanism of action has to be studied in the future.     

Synthesis and antibacterial activity of some imidazole-5-(4H)one derivatives

In the present study, several substituted oxazolones were synthesized by condensation of benzoylglycine with different aldehydes. From such oxazolones, substituted imidazolones were synthesized by condensation with ethylenediamine, urea and 4-N,N-dimethylaminoaniline. All these synthesized compounds produced significant antibacterial activities. Furthermore, compounds containing -CH(2)CH(2)NH(2), -CONH(2) and -C(6)H(4)-N(CH(3))(2) groups as substitutents on the imidazolones were found to be potent antibacterial agents. Thus, among the twelve compounds, 1-(2-aminoethyl)-2-phen yl-4-(4-(dimethylamino)benzylidene)imidazole-5-(4H)one (4d), 1-carboxamido-2-phenyl-4-(4-(dimethylamino)benzylidene)imidazole-5-(4H)one (4e) and 1-(4-(N,N-dimethylamino)phenyl)-2-phenyl-4-(4-(dimethylamino)benzylidene)imidazole-5-(4H)one (4f) were found to have a significant higher antibacterial activity than the other substituted imidazolones. Compound 4e was the most active one in this series.     

Identification of glyburide metabolites formed by hepatic and placental microsomes of humans and baboons

Glyburide (glibenclamide) is a second-generation sulfonylurea used for treatment of type-2 and gestational diabetes mellitus. To date, two glyburide metabolites have been identified in maternal urine: namely, 4-trans-hydroxycyclohexyl glyburide and 3-cis-hydroxycyclohexyl glyburide. The use of glyburide to treat gestational diabetes prompted us to investigate its metabolism by the placenta. The metabolism of glyburide by microsomal preparations from human and baboon placenta was compared with metabolism by their livers. The metabolites formed by the microsomes of the four tissues were identified by high-performance liquid chromatography-mass spectrometry using retention times, ion current (extracted at m/z 510), and selected-ion monitoring. The data obtained revealed the formation of six distinct hydroxylated derivatives of glyburide by each of the four microsomal preparations. However, the amounts of the six metabolites formed by the placentas were a fraction of that formed by the livers. Moreover, the relative quantities of each metabolite formed differed between species as well as between the two tissues. Also, the structure of the unidentified metabolites was determined by comparison with synthesized standards. These metabolites were identified as the 4-cis-hydroxycyclohexyl glyburide, 3-trans-hydroxycyclohexyl glyburide, and 2-trans-hydroxycyclohexyl glyburide. Therefore, one glyburide metabolite remains to be identified, but the data we obtained allowed us to suggest its structure.     

Neighbourhood search feature selection method for content-based mammogram retrieval

Content-based image retrieval plays an increasing role in the clinical process for supporting diagnosis. This paper proposes a neighbourhood search method to select the near-optimal feature subsets for the retrieval of mammograms from the Mammographic Image Analysis Society (MIAS) database. The features based on grey level cooccurrence matrix, Daubechies-4 wavelet, Gabor, Cohen–Daubechies–Feauveau 9/7 wavelet and Zernike moments are extracted from mammograms available in the MIAS database to form the combined or fused feature set for testing various feature selection methods. The performance of feature selection methods is evaluated using precision, storage requirement and retrieval time measures. Using the proposed method, a significant improvement is achieved in mean precision rate and feature dimension. The results show that the proposed method outperforms the state-of-the-art feature selection methods.     

Ethics of transparency in research reports

Transparency in research methods and results is now widely seen as an imperative if the healthcare and research enterprise is to be truly successful. A patient-centred focus in the conduct of clinical care includes its safety, effectiveness, efficiency, equity, and timeliness. Innovative ways are being developed to understand, disseminate, and rapidly apply the best evidence to care delivery. In this article, we demonstrate the use of simple and appropriate statistics in research reports that should help healthcare providers apply knowledge to practice by making it easier for them to understand clinical medicine.