Anti-inflammatory potential of 1-O-methyl chrysophanol from Amycolatopsis thermoflava ICTA 103: an exploratory study.

The present study was designed to investigate the anti-inflammatory potential of Amycolatopsis thermoflava producing 1-O-methyl chrysophanol (OMC), a member of the hydroxyanthraquinone family. The anti-inflammatory potential was evaluated initially through in silico analysis against tumor necrosis factor- α and cyclooxygenase-2. The same activity was further confirmed based on the in vitro protein denaturation method as well as in vivo by a carrageenan-induced paw edema model in rats. The OMC compound was isolated, purified, and characterized from the fermentation broth of Amycoloptosis thermoflava. In vitro data revealed that the OMC possesses significant protein denaturation properties with an IC50 of 63.50±2.19 µg/ml higher than the standard drug, with an IC50 value of 71.42±0.715 µg/ml. The percentage of inhibition in paw swelling was observed to be 40.03±5.5 in OMC-treated group, which is comparable to the standard group (52.8±4.7). The histopathological evaluation and immunohistochemistry revealed the anti-inflammatory potential of OMC.

CLInical Profile and Side Effects of chronic use of oral Amiodarone in cardiology outpatients department (CLIPSE-A Study)- A prospective observational study.

Background: Amiodarone belongs to Class-III anti-arrhythmic drugs. It is one of the most effective anti-arrhythmic drugs used to treat or prevent several types of arrhythmias including atrial fibrillation, atrial flutter, ventricular tachycardia, and wide complex tachycardia, but unfortunately carries a high toxicity profile. Also, side effects of amiodarone involving various organs can be life-threatening. Materials & methods: This was an observational study carried out for six months i.e from April to September. The study included patients who are on amiodarone for greater than or equal to six months. The required data was collected in-person from the case sheets, treatment charts, and by interviewing the patients. The data for 67 patients was documented in suitable data collection form for analysis. Results: From our study data, it was noted that amiodarone was used for 3 different indications-atrial fibrillation, atrial flutter, and ventricular tachycardia. Among 67 patients enrolled, 38 had no side-effects. Side-effects data in the rest grouped basing on the organ system affected: 9 patients had renal effects, 6 patients had ophthalmic effects, 4 patients had endocrine effects, and 5 patients had hepatic effects. Conclusion: From our study, it is concluded that amiodarone is a safe and effective anti-arrhythmic drug at lower doses i.e. 200-1100 mg/week. When treated in lower doses of 1400-2800 mg/week, many side effects have been incident. Although these effects are mild and develop only after prolonged usage of the drug, it should be used judiciously.

Design and study of anticaries effect of different medicinal plants against S.mutans glucosyltransferase.

BACKGROUND: The present study was aimed to evaluate the molecular level anticaries effect of different medicinal plants against Streptococcus mutans (S.mutans) glucosyltransferases (gtf). METHODS: A total of six natural sources named as Terminalia chebula (T.chebula), Psidium guajava (P.guajava), Azadirachta indica (A.indica) and Pongamia pinnata (P.pinnata); two essential oils, clove (Syzygium aromaticum) and peppermint oil (Mentha piperita) were selected as test samples. Hydroalcoholic plant extracts and essential oils were examined for their inhibitory potential on gtf isolated from S.mutans. Polyherbal mouth wash was prepared and its effect on gtf activity was compared with commercial chlorhexidine mouth wash (5%w/v). Enzyme kinetic study was carried out in order to explore the molecular mechanism of enzyme action. RESULTS: Out of six natural sources tested, A.indica has shown maximum inhibitory effect of 91.647% on gtf and T.chebula has shown IC50 of 1.091 mg/ml which is significant when compared to standard chlorhexidine. From the final result of kinetic analysis it was found that T.chebula, P.guajava and P.pinnata have show uncompetitive inhibition where as A.indica has shown non-competitive inhibition. Surprisingly, both essential oils have shown allosteric inhibition (sigmoidal response). The polyherbal moutwash has shown significant inhibitory potential on gtf (95.936%) when compared to commercial chlorhexidine mouthwash (p < 0.05). CONCLUSION: All the tested samples have shown considerable gtf inhibitory action. Moreover polyherbal mouth wash has shown promising noncompetitive inhibitory activity against gtf and it could be the future formulation to combat dental caries.

Formulation and evaluation of transdermal drug delivery of topiramate.

BACKGROUND: Transdermal drug delivery system (TDDS) was designed to sustain the release and improve the bioavailability of drug and patient compliance. Among the various types of transdermal patches, matrix dispersion type systems disperse the drug in the solvent along with the polymers and solvent is allowed to evaporate forming a homogeneous drug-polymer matrix. The objective of the present study was to design and formulate TDDS of topiramate (TPM) and to evaluate their extended release in vitro and ex vivo. MATERIALS AND METHODS: In the present study, an attempt has been made to develop a matrix-type transdermal therapeutic system comprising TPM with different ratios of hydrophilic and hydrophobic polymeric combinations using solvent casting technique. RESULTS: The physicochemical compatibility of the drug and the polymers was studied by Fourier transform infrared spectroscopy. The results obtained showed no physical-chemical incompatibility between the drug and the polymers. The patches were further subjected to various physical evaluations along with the ex vivo permeation studies using pig ear skin. CONCLUSIONS: On the basis of results obtained from the physical evaluation and ex vivo studies the patches containing the polymers, that is, Eudragit L 100 and polyvinylpyrrolidone, with oleic acid as the penetration enhancer were considered as the best formulations for the transdermal delivery of TPM.