INHIBITORS FROM MELIA DUBIA AGAINST SDIA MEDIATED QUORUM SENSING OF UROPATHOGENIC E. COLI

Objective: To investigate the potentiality of Meliadubiastem extracts for quorum sensing (SdiA-selective) inhibitory activity against uropathogenic Escherichia coli (UPEC).Methods: The antimicrobial (cell-density) and anti-virulent (swarming motility, protein, protease, hemolysis, hemagglutination, hydrophobicity and biofilm inhibition) properties of the Meliadubia stem extracts were performed.Results: The biofilm, hemolysis, swarming motility were inhibited by 45.71%, 12.97 % and 33.33% respectively when the media were supplemented with 30 mg/ml of ethanolic extract. The GC-MS spectrum of ethanolic extract showed an array of 49 structurally unrelated compounds with the natural ligand, AHL. Their interaction with the quorum regulator, SdiA, was predicted by Glide module of Schrödinger suite and the ligands C 7, C 20, C 28 showed appreciable activity with the following G-Score 11.4, 10.7, 9.9 respectively. In vitro and in silico molecular docking analysis data showed fairly good correlation, suggesting that the ethanolic extract has the potential to attenuate the quorum sensing of UPEC. Further investigation is desired to study the antagonistic effect of the above ligand by in vitro and in vivo strategies.Conclusion: The quorum quenching activity of Meliadubia stem was proven from the overall analysis and its effect towards the inhibition of biofilm and virulence factors were analyzed.Â

QUALITY BY DESIGN-BASED OPTIMIZATION AND VALIDATION OF NEW REVERSE PHASE-HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY METHOD FOR SIMULTANEOUS ESTIMATION OF LEVOFLOXACIN HEMIHYDRATE AND AMBROXOL HYDROCHLORIDE IN BULK AND ITS PHARMACEUTICAL DOSAGE FORM

ABSTRACTObjective: Innovative application of quality by design (QbD) technique for simultaneous estimation of levofloxacin and ambroxol hydrochloride (HCL)in bulk and its pharmaceutical dosage form using reverse phase-high-performance liquid chromatography (RP-HPLC) method.Method: A method has been developed for the separation of levofloxacin and ambroxol HCL using RP-HPLC on C18 column (250 4.6 mm, 5 ml) withultraviolet detection at 306 nm. Experimental designs were applied for multivariate optimization of the experimental conditions of RP-HPLC method.Three independent factors: Acetonitrile content in the mobile phase composition, buffer pH, and flow rate were used to design mathematical models.Here, central composite design (CCD) experimental design was used to study the response surface technique and to study in depth the effects ofthese independent factors. Derringer's desirability function was applied to simultaneously optimize the retention time of last eluting peak (ambroxolhydrochloride) and resolution between levofloxacin and ambroxol hydrochloride.Result and Discussion: The predicted optimum assay condition consisted of acetonitrile, potassium dihydrogen phosphate buffer (pH 5.00;potassium dihydrogen phosphate), and methanol in a proportion of 20:70:10% v/v, respectively, as the mobile phase at a flow rate of 1.2 ml/minute.Using this optimum condition, baseline separation of both drugs with good resolution and a run time of <5 minutes were achieved. The optimizedassay condition was validated according to the ICH guidelines to confirm specificity, linearity, accuracy, and precision.Keywords: Levofloxacin, Ambroxol hydrochloride, Experimental design, Response surface methodology, Derringer's desirability, Quality by designapproach

SYNTHETIC ROUTES AND NATURAL SOURCES OF 2-PYRIDONE DERIVATIVES AND THEIR PHARMACOLOGICAL ACTIVITY

Objective: 2-pyridone is a well-known heterocyclic ring having significant biological and medical application. The molecular structures and various activities of 2-pyridone derivatives as well as their syntheses and natural occurrence are analyzed and reviewed, and their reactivity toward various nucleophiles is discussed. Methods: 2-pyridone derivatives, first naturally obtained and described as early as before the 19th century, have been attracting increasing attention in view of their high reactivity as building blocks for the preparation of compounds of various classes due to their selective transformations with different reagents. Much information describing the natural occurrence, synthesis and the significant biological activity of 2-pyridone compounds are scattered throughout the literature. There are short chapters dealing with the synthesis and activity of 2-pyridone derivatives. Results: After compiling the above material, the abundance of certain heterocyclic ring and nature of typical chemical transformations applied in current drug synthesis. It is likely this results from the abundance of these heterocycles in natural products such as alkaloids and various synthetic derivatives revealing different biological activity. This might suggest a classical approach to drug design where substrate analogs gain inspiration from existing natural ligands. Conclusions: The data considered in this review clearly demonstrate the high synthetic potential of 2-pyridone derivatives. Many biologically active heterocyclic compounds have been obtained based on this heterocyclic ring. This suggests that 2-pyridone can be used in the design of novel highly effective pharmaceuticals with a broad spectrum of bioresponses

Evaluation of herbal ointment containing ethanol extract of Plecranthus amboinicus root for the management of psoriasis

Plant, Plecranthus amboinicus (Lour.) Spreng, belonging to the family Lamiaceae, commonly known as ‘Karpuravalli’ in Tamil language is widely used in folk medicine to treat conditions like cold, asthma, constipation, headache, cough, fever and skin diseases. The present study aimed to evaluate antipsoriatic effect of the ethanol extract of Plecranthus amboinicus root. Ointment containing ethanolic extract of Plecranthus amboinicus root was prepared and evaluated for antipsoriatic activity using complete Freund's adjuvant (CFA) and formaldehyde induced animal model. Psoriasis is induced by applying mixture of 0.1 mL of prepared CFA and formaldehyde mixture (1:10 ratio) topically for 7 days on the dorsum surface of the skin of Swiss albino mice. Antipsoriatic effect of 0.5% and 1.0% (w/w) ointments containing ethanolic extract of Plecranthus amboinicus root was evaluated in terms of Psoriasis severity index (PSI) by the phenotypic features (redness, scales and erythema) and histological features (epidermal thickness). The result showed that there was a significant increase in the orthokeratinocyte layer and a significant reduction in the epidermal layer of skin in the in vivo mice model with a progressive reduction (p**<0.01) in the severity of psoriatic lesions (redness, erythema, and scales) from day 7 to 21st day and significant (p*<0.05) decreased epidermal thickness and increased orthokeratotic regions in animals treated with 0.5% and 1.0% (w/w) ointments of Plecranthus amboinicus root. The present investigations revealed that Plecranthus amboinicus root possess potent antipsoriatic activity, confirming their traditional use in skin disorders

Evaluation of herbal ointment containing ethanol extract of Plecranthus amboinicus root for the management of psoriasis

553-559Plant, Plecranthus amboinicus (Lour.) Spreng, belonging to the family Lamiaceae, commonly known as ‘Karpuravalli’ in Tamil language is widely used in folk medicine to treat conditions like cold, asthma, constipation, headache, cough, fever and skin diseases. The present study aimed to evaluate antipsoriatic effect of the ethanol extract of Plecranthus amboinicus root. Ointment containing ethanolic extract of Plecranthus amboinicus root was prepared and evaluated for antipsoriatic activity using complete Freund's adjuvant (CFA) and formaldehyde induced animal model. Psoriasis is induced by applying mixture of 0.1 mL of prepared CFA and formaldehyde mixture (1:10 ratio) topically for 7 days on the dorsum surface of the skin of Swiss albino mice. Antipsoriatic effect of 0.5% and 1.0% (w/w) ointments containing ethanolic extract of Plecranthus amboinicus root was evaluated in terms of Psoriasis severity index (PSI) by the phenotypic features (redness, scales and erythema) and histological features (epidermal thickness). The result showed that there was a significant increase in the orthokeratinocyte layer and a significant reduction in the epidermal layer of skin in the in vivo mice model with a progressive reduction (p**st day and significant (p*Plecranthus amboinicus root. The present investigations revealed that Plecranthus amboinicus root possess potent antipsoriatic activity, confirming their traditional use in skin disorders

Novel drug delivery system

This investigation aims to evaluate the Anti tumour potential of the petroleum ether extract of Abrus precatorius Linn (PEEAP) on Ehrlich Ascitis Carcinoma (EAC) tumour model. Tumour was induced in mice by intraperitoneal injection of EAC cells (1 ×10 6 cells/mouse). PEEAP was administered to the experimental animals at the dose levels of 250,500 and 1000 mg/kg per day after 24 hrs of tumour inoculation. The anti tumour effect of PEEAP was evaluated by assessing and body weight, survival time, haematological parameters. Oral administration of PEEAP increased the survival time of the EAC bearing mice. The PEEAP brought back the alter levels of the haematological parameters in a dose dependent manner in EAC bearing mice. The results were comparable to that of the result obtained from the animals treated with the standard drug 5-flurouracil (20mg/kg.b.w). Thus present study revealed that PEEAP possessed significant anti tumour activity. This article can be downloaded from www.ijpbs.ne

Quantification and comparison of neurosurgical approaches in the preclinical setting: literature review

There is a growing awareness of the need for evidence-based surgery and of the issues that are specific to research in surgery. Well-conducted anatomical studies can represent the first, preclinical step for evidence-based surgical innovation and evaluation. In the last two decades, various reports have quantified and compared neurosurgical approaches in the anatomy laboratory using different methods and technology. The aim of this study was to critically review these papers. A PubMed and Scopus search was performed to select articles that quantified and compared different neurosurgical approaches in the preclinical setting. The basic characteristics that anatomically define a surgical approach were defined. Each study was analyzed for measured features and quantification method and technique. Ninety-nine papers, published from 1990 to 2013, were included in this review. A heterogeneous use of terms to define the features of a surgical approach was evident. Different methods to study these features have been reported; they are generally based on quantification of distances, angles, and areas. Measuring tools have evolved from the simple ruler to frameless stereotactic devices. The reported methods have each specific advantages and limits; a common limitation is the lack of 3D visualization and surgical volume quantification. There is a need for a uniform nomenclature in anatomical studies. Frameless stereotactic devices provide a powerful tool for anatomical studies. Volume quantification and 3D visualization of the surgical approach is not provided with most available methods

ABNORMAL UTERINE BLEEDING IN REPRODUCTIVE WOMEN: DIAGNOSIS, MANAGEMENT AND TREATMENT

Abnormal Uterine Bleeding (AUB) is a common cause for concern among reproductive women and their families, as well as a frequent cause of visits to the Emergency Department and/or health care provider. In the pilot study which was conducted in 50 patients, observed that majority of patients were admitted due to menorrhagia and most of them were peri-menopausal women. Fibroid uterus is the most common cause in the study population, other than cyst and adenomyosis. Among the 50 patients, 54% were managed with drugs, 32% with surgery & drugs and the remaining with surgery alone. Among the drugs used, tranexamicacid is an effective therapy for the management of aub. The adolescents were treated with oral progestins. Anemia which was assessed in 20% and was corrected with folic acid supplements, iron sucrose and blood transfusions if required. Hysterectomy was done in majority of patients with cyst and fibroid excisions.Key words: AUB, Menorrhagia, fibroid uterus, tranexamic acid, progestins, anemia, hysterectom