Synthesis, characterization, and antibacterial activity of novel bis(indolyl)methanes sourced from biorenewable furfurals using gluconic acid aqueous solution (GAAS) as a sustainable catalyst.

Bis(indolyl)methanes (BIMs) are important heterocycle-containing molecular scaffolds that show remarkable biological and pharmacological activities. This work reports the synthesis of novel BIMs using carbohydrate-derived 5-substituted-2-furaldehydes as renewable reactants. Structural diversity was introduced in the BIMs as substituents in the indole and furaldehyde moieties. Various commonly encountered biorenewable carboxylic acids were screened as catalysts for the acid-catalyzed transformation under organic solvent-free conditions. All the novel BIMs were characterized by spectroscopic techniques (FTIR, 1H-NMR, 13C-NMR) and elemental analysis. The reaction was optimized on the reaction temperature, duration, catalyst type, and catalyst loading. The gluconic acid aqueous solution (GAAS) showed the best catalytic activity for the transformation, affording satisfactory isolated yields (68-96%) of the targeted BIMs under optimized conditions. The GAAS catalyst was conveniently recovered from the reaction mixture and reused for four consecutive cycles without catastrophic loss in either mass or activity. Moreover, the antibacterial activities of the novel BIMs were studied on Gram-positive and Gram-negative bacterial strains, such as Enterococcus faecalis and Pseudomonas syringae.

Efficient Synthesis of Novel Biginelli and Hantzsch Products Sourced from Biorenewable Furfurals Using Gluconic Acid Aqueous Solution as the Green Organocatalyst.

The Biginelli reaction provides 3,4-dihydropyrimidin-2(1H)-ones (DHPMs), whereas the Hantzsch reaction leads to 1,4-dihydropyridines (DHPs) by the one-pot, multicomponent, and operationally simple transformations starting from readily available starting materials. DHPMs and DHPs are well-established heterocyclic moieties in the synthetic organic chemistry literature and have pronounced pharmacological activities. This work reports the synthesis of novel DHPMs and DHPs from carbohydrate-derived 5-substituted-2-furaldehydes by employing gluconic acid aqueous solution (GAAS) as an efficient, inexpensive, and eco-friendly catalyst. The use of urea (or thiourea) as the reagent led to DHPMs, whereas ammonium acetate produced DHPs, selectively, keeping the other two starting materials (i.e., furfurals and ethyl acetoacetate) and the reaction parameters unaltered. Using the general synthetic protocol under optimized reaction conditions (60 °C, 3-6 h, 25 mol % GAAS cat.), all the DHPM and DHP derivatives were obtained in good to excellent isolated yields.

Isolation and Characterization of Antibacterial Compound from a Mangrove-Endophytic Fungus, Penicillium chrysogenum MTCC 5108.

Microorganisms, especially endophytic fungi that reside in the tissue of living mangrove plants, seem to play a major role in meeting the general demand for new biologically active substances. During the course of screening for biologically active secondary metabolites from marine microorganisms, an antibiotic compound containing an indole and a diketopiperazine moiety was isolated from the culture medium of Penicillium chrysogenum, (MTCC 5108), an endophytic fungus on the mangrove plant Porteresia coarctata (Roxb.). The cell free culture medium of P. chrysogenum showed significant activity against Vibrio cholerae, (MCM B-322), a pathogen causing cholera in humans. Bioassay guided chemical characterization of the crude extract led to the isolation of a secondary metabolite possessing a molecular formula C19H21O2N3. Its antibacterial activity was comparable with standard antibiotic, streptomycin. This compound (1) was found to be (3,1'-didehydro-3[2″(3'″,3'″-dimethyl-prop-2-enyl)-3″-indolylmethylene]-6-methyl pipera-zine-2,5-dione) on the basis of mass spectrometry, infrared spectroscopy and one and two-dimensional nuclear magnetic resonance analysis.

Active pharmaceutical ingredient (api) from an estuarine fungus, Microdochium nivale (Fr.).

Various marine habitats sustain variety of bio-sources of ecological and biotech potentials. Pharmaceutical potential compound Cyclosporine A was reported from marine fungus Microdochium nivale associated with Porteresia coarctata, a marine salt marsh grass from mangrove environment distributed along the Central West Coast (CWC) of India. This study involves association of M. nivale with P. coarctata plant, fermentation conditions, purification of Cyclosporine A, chemical characterization etc. Its antifungal inhibition and MIC (Minimum inhibitory concentration) against Aspergillus strains (A. niger, A. japonicus, A. fresenii), yeasts and dermatophytes (Candida sp., Cryptococcus neoformans, Trichophyton mentagrophytes, T. tonsurans, T. violaceum, Microsporium gypsum and Fusarium sp.) were evaluated. However, the MIC against A. japonicus, C. neoformans, Candida sp. and T. tonsurans were confirmed to be as low as 12.5-25 mg disc(-1). The antifungal properties of Cyclosporine A against Aspergillus species, yeast and dermatophytes revealed that CyclosporineAwould be a potential compound for life threatening diseases caused by above fungi in both human and animals. Furthermore, we have reported herewith another source of Cyclosporin Aderived from filamentous fungus, M. nivale. occurring in marine environment.

Intraoperative consultation and smear cytology in the diagnosis of brain tumours.

BACKGROUND: Intraoperative smear cytology provides a rapid and reliable intraoperative diagnosis and guidance to the neurosurgeon during surgical resection and lesion targeting. It also helps the surgeon to monitor and modify the approach at surgery. OBJECTIVES: 1) To assess the utility of intraoperative smear cytology and correlate with the final histopathological diagnosis. 2) To describe the cytomorphological features of common brain tumours in smear preparation. MATERIALS AND METHODS: The material for this study was obtained from 100 consecutive biopsies of central nervous system neoplasms sent for intraoperative consultation. Smears were prepared from the biopsy samples sent in isotonic saline for immediate processing. The smears were stained by the rapid Haematoxylin and Eosin method. The cytomorphological features were noted and correlated with paraffin section findings. RESULTS: Of the total 100 cases, 86 showed accuracy when compared with histopathological diagnosis. This was comparable with other studies. Of the remaining, two cases were frank errors, 12 cases showed partial correlation, with five cases showed incomplete typing of the cell type and seven, discrepancy in grading of tumours. The error percentage was 14%. Correlation with clinical details and radiological findings were helpful in improving the accuracy rate. CONCLUSIONS: Smear technique is a fairly accurate, relatively safe, rapid, simple, easily reproducible and cost effective tool to diagnose brain tumours. Smear cytology is of great value in intraoperative consultation of central nervous system pathology.

Tandem mass spectrometry of kahalalides: identification of two new cyclic depsipeptides, kahalalide R and S from Elysia grandifolia.

Spectra obtained using electrospray ionization mass spectrometry (ESI-MS) of the mollusk Elysia grandifolia showed a cluster of molecular ion peaks centered at a molecular mass of 1478 Da (kahalalide F, an anticancer agent). Two new molecules, kahalalide R (m/z 1464) and S (m/z 1492) were characterized using tandem mass spectrometry. The mass differences of 14 Da suggest that they are homologous molecules. In addition, previously identified kahalalide D and kahalalide G are also reported. However, the ESI-MS of the mollusk's algal diet Bryopsis plumosa showed the presence of only kahalalide F. The amino acid sequences of kahalalide R and S are proposed using collision-induced dissociation (CID) experiments of singly and doubly charged molecular ions and by comparison with the amino acid sequence of kahalalide F. The pathway is presented for the loss of amino acid residues in kahalalide F. It is observed that there is sequential loss of amino acids in the linear peptide chain, but in the cyclic part the ring opens at the amide bond rather than at the lactone linkage, and the loss of amino acid residues is not sequential. The CID experiment of the alkali-metal-cationized molecular ions shows that the sodium and potassium ions coordinate to the amide nitrogen/oxygen in the linear peptide chain of the molecule and not to the lactone oxygen of the lactone. In the case of kahalalide D, CID of the protonated peptide opens the depsipeptide ring to form a linear peptide with acylium ion, and fragment ion signals indicate losses of amino acids in sequential order. In this study, tandem mass spectrometry has provided the detailed information required to fully characterize the new peptides.

Pure lipoma of the uterus: a rare case report.

Pure fatty tumors of the uterus are exceedingly rare. The more common lipomatous tumor is lipoleiomyoma with varying amounts of two components. Most are post-operative chance findings following hysterectomy for leiomyoma. Computed Tomography and Magnetic Resonance Imaging can assist in pre-operative diagnosis. A 60 year old post-menopausal woman presented with a mass per abdomen. Ultrasound revealed fibroid uterus with lipomatous areas. The hysterectomy specimen showed a pure intramural lipoma of the uterus. As clinical symptoms and signs of uterine lipoma are indistinguishable from uterine leiomyoma, various imaging techniques can aid in pre-operative diagnosis. The diagnosis of pure lipoma of the uterus should only be made when any smooth muscle if present is confined to the periphery of the tumor.

Superolateral dislocation of the intact mandibular condyle: report of a rare case with a review.

Dislocation of the temporomandibular joint, which represents 3% of all dislocated joints reported in the body, occurs when the mandibular condyle is displaced anteriorly beyond the articular eminence. Although anterior dislocation of the mandibular condyle is well documented in the literature, superior, lateral, and posterior dislocation of the condyle is rare. Only a few reports documenting superolateral dislocation with anterior mandible fractures have been published in the past. However such dislocations without any associated fractures are even rarer. This report documents a case of superolateral dislocation of an intact mandible in a 48-year-old woman following a traumatic incident. This paper also reviews previously documented case reports and focuses on the causative mechanism, dynamics, and management of such dislocations.

Epidermoid Cyst of Tongue.

Epidermoid cyst occurring within the tongue is rare. A 5 year old male child was brought to OPD with a tongue mass which was gradually increasing in size. There was associated difficulty in speech and mastication as the swelling increased in size. Intraoral examination revealed moderately tender,fluctuant and enlarged tongue. A diagnosis of dermoid cyst was made and the patient was booked for surgery. Excision of the cyst was done under general anaesthesia. Post-operative histopathology was done. The histopathological findings confirm the diagnosis of an epidermoid cyst, characterized by the presence of: (I) a cyst cavity lined by stratified squamous epithelium with keratinization on the surface; and (II) connective tissue with a mild inflammation. The proposed treatment was considered successful as the case was solved and there was no recurrence.

Maxillary Calcifying Epithelial Odontogenic Tumour.

The calcifying epithelial odontogenic tumor is a benign, locally invasive, slow-growing neoplasm occurring as intraosseous (94%) and extraosseous (6%) variants and with a frequency of 1-2%. Extraosseous variant is diagnosed slightly earlier than the intraosseous type. The intraosseous CEOT shows a maxilla:mandible site ratio of 1:2 and are mainly located in the premolar/molar region. Histologically, the CEOT is characterized by the occurrence of sheets, nests and masses of polyhedral, eosinophilic epithelial cells which may show cellular abnormalities including giant cell formation and nuclear pleomorphism. Some cells increase in size and produce a homogeneous, eosinophilic, 'amyloid-like' substance which may become calcified and which may be liberated as the cells break down. Enucleation with a margin of macroscopically normal tissue is the recommended treatment for CEOT involving the mandible. Maxillary CEOT are treated more aggressively, as they tend to grow more rapidly and do not usually remain well confined.

Tandem mass spectrometric approach for determining the structure of molecular species of ceramide in the marine sponge Haliclona cribricutis.

Ceramides are important intracellular second messengers that play a role in the regulation of cell growth, differentiation and programmed cell death. Analysis of these second messengers requires sensitive and specific analytical method to detect individual ceramide species and to differentiate between them. Eight molecular species of ceramide were identified from the marine sponge Haliclona cribricutis using electrospray ionization tandem mass spectrometry (ESI-MS/MS). From this marine sponge N-hencicosanoyl (N21:0) to N-hexasanoyl (N26:0) Octadecasphing-4 (E)-enine have been reported for the first time. The ESI-MS spectra gave several strong protonated molecular ion [M+H](+) with the corresponding bis (2-ethyl hexyl) phthalate adduct [M+H+DHEP](+). The collision induced dissociation (CID) on ceramides at m/z 622.7337, 636.7645, 650.7789, 664.7925 and 678.8130 conducted at low-collision energy produced well characteristic product ions at m/z 252.31, 264.32, 278.33, 282.33 and 296 .35 for d18:1 sphingosine regardless of the length of the fatty chain. The MS/MS of the Phthalate adduct [M+H+DHEP](+) at m/z 1013.1820, 1027.1971, 1041.2176, 1055.2394 and 1069.2573 also yielded characterizing product ions for sphingosine and confirmed the molecular ion at m/z 391 for bis (2-ethyl hexyl) phthalate. The major ions in the [M+H](+) and [M+H+DHEP](+) were due to neutral loss of [M+H-H(2)O](+) and [M+H(H(2)O)(2)](+).

Bioactivity of marine organisms: Part VII--Effect of seaweed extract on central nervous system.

Alcohol extracts of marine algae (Rhodophyceae, Phaeophyceae and Chlorophyceae) were screened for their effect on central nervous system. Of 69 species investigated 8 appeared biologically active, 6 being CNS stimulant and two depressant, sites and dates of collection are given.

Sterculic oil, a natural inhibitor of SCD1, improves the metabolic state of obese OLETF rats.

OBJECTIVE: Abnormal lipid metabolism and excess accumulation of lipid in non-adipose tissues are defining characteristics of obesity and its comorbidities. Expression and/or activity of stearoyl-CoA desaturase-1 (SCD1), a major regulator of lipid metabolism, is increased with obesity and the reduction/ablation of this enzyme is associated with an improved metabolic profile. Sterculic oil (SO), obtained from the seeds of the Sterculia feotida tree, contains a high concentration of cyclopropenoic fatty acids which are known inhibitors of SCD1. The purpose of this study was to determine the effects of SO supplementation on the development of obesity and insulin resistance in hyperphagic, obese Otsuka Long-Evans Tokushima Fatty (OLETF) rats. DESIGN & METHODS: Rats received either an AIN-93G diet (control) or an AIN-93G diet containing 0.5% SO for 10 weeks. RESULTS: SO did not alter body weight or body composition. Importantly, the desaturase indices, a proxy for the activity of SCD1, were reduced in the liver and adipose tissue of SO supplemented animals. This reduction in SCD1 activity was associated with a reduction in fasting blood glucose concentrations and improved glucose tolerance. In addition, SO reduced intra-abdominal fat mass and adipocyte size and resulted in a ∼3-fold increase in GLUT1 gene expression in intra-abdominal fat. Liver triglyceride content and lipogenic gene expression were reduced by SO. Consistent with an improved metabolic phenotype, SO also improved plasma cholesterol, LDL-cholesterol, and triglyceride concentrations. CONCLUSION: Overall, our data demonstrate an improved metabolic phenotype with SO supplementation and suggest further studies are required to better understand the therapeutic potential of SO.

Mastoid infection caused by entomophthorales: a rare fungal disease.

OBJECTIVE: To report an unusual case of fungal mastoiditis caused by entomophthorales in an immunocompetent patient, and its management. METHOD: Case report with a review of the literature. CASE REPORT: A 13-year-old girl presented to us with a mastoid abscess. Entomophthoromycotic infection of the mastoid was diagnosed on histopathological examination, and subsequently treated with surgical debridement and amphotericin B injection. CONCLUSION: This is the first reported case of mastoid abscess secondary to entomophthoromycosis. Early detection and treatment contributed to this patient's good outcome.

Endoscopic adenoidectomy with microdebrider.

To describe endoscopic power assisted adenoidectomy and review the experience with the procedure demonstrating its safety and efficacy. Prospective study of 44 patients aged between 7 to 15 years undergoing power assisted adenoidectomy between Jan 2004 and July 2006. Tertiary care private teaching hospital. Forty four consecutive children with adenoid hypertrophy undergoing power assisted adenoidectomy. Therapeutic endoscopic adenoidectomy using microdebrider. Operative time, blood loss, complications, completeness and depth of removal, surgeon's satisfaction and recovery period. The average operative time was 12 min (range: 8-16 min) and average blood loss was 30 ml (range: 24-42 ml). Complete resection was possible under vision with few complications. The surgeon satisfaction was high and post-operative recovery good. Power assisted adenoidectomy is quick, precise and safe. There is good visualization during resection thus improving precision and ensuring complete removal of adenoid tissue.