Management of postburn perioral contracture using a customized static commissural splint and intralesional injections of triamcinolone.

A perioral facial burn is usually accompanied by a reduction in size of the oral orifice because of the contraction of the healing wound. Perioral contracture leads to microstomia, restricting nutrition, speech, and jaw movements and impairing the esthetic appearance of the face. It is imperative to introduce splints as early as possible to prevent the postburn sequelae. A delay in splinting allows postburn contractures. Overcoming these contractures to regain the size of the stoma requires restructuring of the hypertrophic scar using mechanical force and the biomodification of the tissues. This article describes the treatment of microstomia and the hypertrophic scarring of the perioral tissue using a novel static commissural splint with customizable components in conjunction with intralesional injections of triamcinolone. Within 6 months, the splint together with the steroid injections had helped increase the vertical opening of the mouth by 15 mm and the intercommissural distance by 16 mm.

Histamine H3 Receptor Agonist Imetit Attenuated Isoproterenol Induced Renin Angiotensin System and Sympathetic Nervous System Overactivity in Myocardial Infarction of Rats.

BACKGROUND: Myocardial infarction is an alarming health issue, needs great attention. The present study investigated the role of histamine-H3 receptor (H3R) agonist imetit in relationship to sympathetic and renin angiotensin system in Wistar rats. MATERIALS AND METHODS: Subcutaneous injection of isoproterenol (85 mg/kg) on last 2 consecutive days in per se group and 7 days treatment of different groups at 24 h interval induced myocardial infarction in Wistar rats. H3R agonist imetit (10 mg/kg), H3R antagonist thioperamide (5 mg/kg), losartan (10 mg/kg) were administered orally to evaluate imetit's cardioprotective potential effect by measuring plasma cardiac antioxidant markers, angiotensin II, norepinephrine levels and histopathological analysis. RESULTS: Isoproterenol significantly elevated the angiotensin II and norepinephrine levels in rat plasma. This study revealed that pre-treatment with imetit similar to losartan attenuated norepinephrine and angiotensin II levels whereas thioperamide showed its antagonistic effect by diminishing imetit's effects. Furthermore, its protective effect was confirmed by restoration of cardiac antioxidant markers and histopathological improvement of myocardium integrity. CONCLUSION: This study confirm imetit's cardioprotective potential and also reveals renin angiotensin system, sympathetic system and H3R correlation in isoproterenol induced toxicity in rats. However, molecular studies must be warranted to prove the role of H3R in myocardial infarction.

Reduced estradiol synthesis by letrozole, an aromatase inhibitor, is protective against development of pentylenetetrazole-induced kindling in mice.

Neurosteroids, such as testosterone and their metabolites, are known to modulate neuronal excitability. The enzymes regulating the metabolism of these neurosteroids, thus, may be targeted as a noval strategy for the development of new antiepileptic drugs. The present work targeted two such enzymes i,e aromatase and 5α-reductase in order to explore the potential of letrozole (an aromatase inhibitor) on pentylenetetrazole (PTZ)-induced kindling in mice and the ability of finasteride (a 5α-reductase inhibitor) to modulate any such effects. PTZ (30 mg/kg, i.p.), when administered once every two days (for a total of 24 doses) induced kindling in Swiss albino mice. Letrozole (1 mg/kg, p.o.), administered prior to PTZ, significantly reduced the % incidence of kindling, delayed mean onset time of seizures and reduced seizure severity score. Letrozole reduced the levels of plasma 17ß-estradiol after induction of kindling. The concurrent administration of finasteride and letrozole produced effects similar to letrozole on PTZ-kindling and on estradiol levels. This implies that the ability of letrozole to redirect the synthesis of dihydrotestosterone (DHT) and 5α-androstanediol from testosterone doesn't appear to play a significant role in the protective effects of letrozole against PTZ kindling. Letrozole, however, increased the levels of 5α-DHT in mice plasma. The aromatase inhibitors, thus, may be exploited for inhibiting the synthesis of proconvulsant (17ß-estradiol) and/or redirecting the synthesis of anticonvulsant (DHT and 5α-androstanediol) neurosteroids.

Assessment of antibacterial activity of smaller chain tripeptides and tetrapeptides.

Our objective is to investigate the smaller chain tripeptides and tetrapeptides with the efforts mainly directed towards the identification of compounds presenting a high bactericidal activity. In this connection, 5 peptides, Met-Arg-Tyr (MRY), Met-Val-Tyr (MVY), Met-Ile-Cys-Tyr (MICY), Phe-Trp-Lys-Tyr (FWKY) and Met-Trp-Lys-Tyr (MWKY) were synthesized by solid phase peptide synthesis. The column eluted pure synthesized compounds were tested for in-vitro antibacterial disc diffusion assay using 2 g positive S. aureus, B.subtilis and 1 g negative E.coli bacterial strains at different concentrations predicted by pH and inhibitory concentration findings. 2 of the tetrapeptides, Phe-Trp-Lys-Tyr (FWKY) and Met-Trp-Lys-Tyr (MWKY) were found to be highly efficient against all the gram positive and microbial strains tested. Maximum activity was observed at a concentration of 300 µg/ml (499.17 µM) for the tetrapeptide Phe-Trp-Lys-Tyr (FWKY) against B. subtilis and at a concentration of 450 µg/ml (748.75 µM) against E. coli with the corresponding zonal inhibition diameter readings (17 mm; 16 mm). The tetrapeptide Met-Trp-Lys-Tyr (MWKY) was found to have high potency against S. aureus at a concentration of 450 µg/ml (769.23 µM) with the corresponding zonal inhibition diameter as 13 mm. The experimental results are analysed statistically by t-test at 5% and 1% level of significance. Our tetrapeptides have shown antibacterial action against both gram positive and gram negative strains and are considered safer as par with commercial antibiotics available today. Further clinical studies will make sure to position our potent small chain tetrapeptides in the arsenal of new broad spectrum anti-gram positive and anti-gram negative agent.

Antimicrobial glycopeptides: synthesis and antibacterial activity of N-linked and O-linked smaller chain glycopeptides.

Our objective is to synthesize the smaller chain N-linked and O-linked glycopeptides using sugars belong to mono, di and polysaccharides, with the efforts mainly directed towards the identification of antibacterial compounds. 7 glycopeptides, viz., Arg-Asn-Mannose, Arg-Asn-Lactose, His-Asn-Mannose, His-Asn-Lactose (N-glycopeptides), Arg-Ser-Lactose, Arg-Thr-Lactose, Arg-Thr-Starch (O-glycopeptides) were prepared by dicyclohexyl carbodimide (DCC) coupling for amino acids using microwave oven (50W power; 15 min) and activated and coupled with respective sugar moieties using microwave oven at 120 W for 20-25 min. The column eluted compounds were tested for disc diffusion assay using 3 gram positive S. aureus, B. subtilis, S. caprae and 3 gram negative E. coli, P. aeruginosa and S. sonnei strains at different concentrations predicted by pH and inhibitory concentrations. One of the test glycopeptide, His-Asn-Lactose was found to be very effective against all the microbial strains tested and 3 other Test Compounds, viz., His-Asn-Mannose, Arg-Thr-Lactose and Arg-Thr-Starch are also proved to be effective against 2 gram positive and 2 gram negative strains tested. Maximum activity was observed at a concentration of 450 µg/ml (747.51 µM) for the N-glycopeptide His-Asn-Lactose with the corresponding zonal inhibition diameters (15 mm; 19 mm; 14 mm; 18 mm; 16 mm; 17 mm) against S. aureus, B. subtilis, S. caprae, E. coli, P. aeruginosa, S. sonnei. This is the first evidence based report that our N-glycopeptide, His-Asn-Lactose tested, has shown antibacterial action against both gram positive and gram negative strains. Further in vivo testing and clinical studies will make sure to position our potent small chain N-glycopeptide in the arsenal of new broad spectrum anti-gram positive and negative agent.

Alginate immobilization of Escherichia coli MTCC 1652 whole cells for bioconversion of glycyrrhizinic acid and into 18-beta glycyrrhetinic acid.

Microbial biotransformation of Glycyrrhizinic acid (GL) into 18-beta Glycyrrhetinic Acid (GA) was achieved using Escherichia coli MTCC 1652 whole cell. The E. coli whole cell was immobilized by entrapment method within calcium alginate beads using cell suspension of equal volume with sodium alginate 8%. The pH of solution, reaction volume and % of GL were optimized during the immobilization procedure and optimum pH 6.5, reaction volume of 4 mL and at 3% GL concentration for 12 h of incubation time showed highest concentration of GA (72.649 microg mL(-1)) with 76% bioconversion of GL to GA. Under optimized condition the immobilized cell produces 58.663 microg per mL of GA in licorice root extract containing 95.118 microg of GL per mL of the extract with 61% conversion at 12 h.

Lacidipine encapsulated gastroretentive microspheres prepared by chemical denaturation for pylorospasm.

The purpose of this research work was to formulate and systematically evaluate in vitro performance of mucoadhesive microspheres of lacidipine for treatment of pylorospasm. Lacidipine microspheres containing chitosan were prepared by chemical denaturation using glutaraldehyde as a cross-linking agent. The microspheres were evaluated for physical characteristics such as particle size, particle shape and surface morphology by scanning electron microscopy, drug entrapment efficiency and in vitro mucoadhesion. Results of preliminary trials indicated that the polymer concentration, cross-linking agent and stirring speed had a noticeable effect on size and surface morphology. A central composite design was employed to study the effect of independent variables, polymer concentration (X(1)), volume of glutaraldehyde (X(2)), stirring speed (X(3)) and cross-linking time (X(4)) on dependent variables, drug entrapment efficiency and percentage mucoadhesion. The entrapment efficiency varied from 14-40.82% depending upon the polymer concentration, volume of cross-linker and stirring speed. All batches of microspheres exhibited good mucoadhesive property (73-83%) in the in vitro wash-off test. It was observed that polymer concentration and glutaraldehyde volume had a more significant effect on the dependent variables. Maximum entrapment (36.53%) and mucoadhesion (81.33%) was predicted at 3.5% chitosan, 3 ml glutaraldehyde, 3000 rpm stirring speed and 75 min cross-linking time under optimized process condition. The selected formulation showed controlled release for more than 6 h. The release followed Higuchi kinetics via a Fickian diffusion.