Current Bioactive Compounds - Volume 12, Issue 2, 2016

The aim of the current research work was to formulate, optimize and assess micronized Silver sulfadiazine (mSSD) topical gel containing Aloe vera gel (AV-gel) for the healing effect on second degree burn wounds induced in Albino Wistar rats. Concentration of Carbopol 940, gelling agent, was selected based on observation of optimum spreadability and consistency. Second-degree burn wounds were developed on the posterior part of Albino Wistar rats under anaesthetic condition. The developed wounds were cured by application of mSSD gel once a day (one application every day) for 14 days post wounding, and observation was made until healing. The observation showed a comparison in the rate of wound healing between mSSD gel treated (Group II) and control group (Group I). The mSSD gel treated group showed higher extent of tissue hyperplasia as compared to control group. mSSD topical gel containing AV-gel treated animals showed, 84.96% healing up to 14 days, while control group animals showed 49.48% healing of wounds on 14th day. Inflammation and pus formation were not observed in treated animals, while control group showed evidence of inflammation and pus formation in the first week. In conclusion, prepared mSSD gel containing AV-gel shows potential outcome in the course of treatment of second degree burn wound through reversal of wound retarding process.

The principle of this method was to screen the pharmacological activity of ten prepared polyphyto formulations by using highthroughput screening method for their antihyperlipidemic activity. The study was performed in three stages using single animal, two animals and three animals in a group. The data produced with single animal is compared with the average data shown by two and three experimental animals and further with six animals (one way ANOVA) for the statistical significance and was duly reported. R2 value was determined by Least squares linear regression analysis to interpret as the proportion of the variance in the dependent variable that is predictable from the independent variable. Test formulations were given at 50mg/kg, body weight through p.o. route daily for 14 days in experimental animals induced with hyperlipidemia by injecting Triton X-100 at 100 mg/kg BW i/p and observed for 48 hrs for the development of hyperlipidemia. Two best formulations namely PHF-21 and PHF-26 were selected by highthroughput screening and results repeated in six animals in a group were found to be statically similar.

Formulations were prepared containing Bergenia ligulata, Didymocarpus pedicellata, Dolichos biflorus, Boerhaavia diffusa, Crataeva nurvala and Ocimum sanctum in different ratios and coded as F1, F2 and F3. In vivo urolithiatic activities of the prepared formulations (i.e. F1:20, F1:40, F1:60, F2:20, F2:40, F2:60, F3:20, F3:40 and F3:60) were performed in rats using ethylene glycol induced urolithiasis model. It was observed that in comparison with the standard drug i.e. Cystone (30 mg/kg b wt.) the prepared formulation F3:60 (60 mg/kg b wt.) have shown significant antilithiatic activity.

Secoiridoid glycosides comprise a group of important phyto-components from members of Gentianaceae. They possess significant antipyretic, anti-inflammatory, antidiabetic and hypolipedimic activities. This study is designed for the development of an effective method for extraction of a bioactive secoiridoid glycoside namely swertiamarin, from the whole plant of Enicostema littorale Blume. The conditions for its ultrasound assisted extraction (UAE) were determined using response surface methodology (RSM). RSM consisted of a Box-Behnken design (BBD). The optimal conditions were found to be: extraction with methanol-water (80:20 v/v) with a solid-to-solvent ratio of 1:22.5 w/v at a temperature of 47.8ºC for 81 min. The predicted yield of swertiamarin was 138.10 mg/g. Confirmation experiments under slightly adjusted conditions proved 98.68% validity for the model. UAE was found to be 2.88 fold more efficient than conventional method in extracting swertiamarin from E. littorale. HPTLC densitometric estimation of swertiamarin was used to determine the extraction efficiency of the developed method.

A highly sensitive ultra-high pressure liquid chromatography (UHPLC-MS/MS) method for estimation of paclitaxel in rat plasma has been validated. The chromatographic separation was achieved using isocratic mobile phase, consisting of acetonitrile–2mM ammonium acetate (70:30 v/v; 0.25 mL min-1). Docetaxel was used as an internal standard and tert-butyl methyl ether (TBME) as organic solvent for the liquid-liquid extraction. The mass spectrometer was operated in synapt mass spectrometry mode via positive electrospray ionization using the transitions m/z 854.4 → 286.1for paclitaxel, and m/z 808.3→ 527.2 as a parent ion of docetaxel (IS). The mean extraction-efficiency of QC samples was 90%. The lower limit of quantification (LLOQ) was 1.0 ng/mL. This method covered a linearity range from 1- 5000 ng/ml, with the total run time of 3.0 min. The applicability of UHPLC-MS/MS method was demonstrated and successfully applied for pharmacokinetic profiling of paclitaxel in rat plasma after oral administration.

Over the years, natural products have the dominant status in the discovery of new effective therapeutic agents, but from 1990's, onward pharma-industry showed paradigm shift towards synthetic drugs. However, the strategic shift of the research and development (R) of major pharmaceutical organizations away from synthetic agents that interfere to interact with single targets for therapeutic effect reverse to the discovery of agents that provoke advantageous phenotypic effects, strongly augment the significance of natural products in drug discovery. This mini review encounters the various grounds for the revival of natural products as therapeutic agents.

α-phellandrene antiedematogenic effect (α-Phel) was evaluated in carrageenan, histamine, prostaglandin and substance P induced paw edema and croton oil, TPA and arachidonic acid induced ear edemain mice. Experimental protocols were approved by Ethical Committee for Animal Experimentation (CEEA/UFPI, Protocol Nº 010/2011). α-Phel (100 and 200 mg.kg-1, p.o.) reduced carrageenan and prostaglandina (40.97 % and 61.41 %, respectively) induced paw edema, in doses 50, 100 e 200 mg.kg-1, p.o. reduced histamina induced paw edema formation (31.27 %; 45.14 % e 47.29 %, respectively); on substance P induced paw edema the inhibition occurred when the animal were treated with 200 mg.kg-1 of α-Phel, p.o. (44.05 %).When administered topically, α-Phel (0.2 e 0.4 mg/ear) reduced croton oil (57.34 % e 62.42 %, respectively), TPA (48.29 % e 62.10 %, respectively)and arachidonic acid(0.4 mg/ear) induced ear edema (29.55 %).α-Phelpresents antiedematogenic activity in acute inflammation models.

In this study, anti-inflammatory, wound healing and anti-ulcerogenic properties of chitosan were evaluated ‘in vivo’ using wistar rats and swiss adult mice and the anti-proliferative activity was tested ‘in vitro’. The tested chitosans displayed no anti-proliferative or anti-inflammatory properties. The cytotoxic activity of chitosan was found to be non-existent towards eight tumoral cell lines and no significant differences were found in the ear edema (anti-inflammatory model) induced by croton oil and chitosan groups. However, chitosan showed good anti-ulcerative and wound healing abilities. Low molecular weight (LMW) chitosan effectively reduced ulcerative wounds induced by ethanol, while high molecular weight (HMW) chitosan helped retain the stomachal folds rendering a gastro protective effect. These results suggest that chitosan can potentially be used in the treatment of peptic ulcers. HMW chitosan also potentiated the healing process both in normal and diabetic rats, probably without induction of fibroblast growth but via collagen synthesis.

Heliotropium ellipticum is an herbaceous annual plant; and its resinous exudate is known for various types of therapeutic effects. The recent study was carried out to investigate the presence of flavonoids and their screening for anti-inflammatory and antimicrobial activities. The carrageenan and CFA-induced paw oedema models were adopted for the assessment of anti-inflammatory activity of dichloromethane fraction and isolated flavonoids. The disc diffusion and microdilution methods were used for the determination of antimicrobial activities. Five known flavonoids were isolated and characterized first time from resinous exudate of H. ellipticum. For the in vitro estimation of flavonoids, the callus cultures were established onto MS medium with supplementation of BAP (2.0 mg/l) and NAA (3.0 mg/l). On estimation, it was found that the flavonoids accumulated in higher concentration in intact plant while lower in callus cultures. Observed findings revealed that Chrysin demonstrated maximum inhibition (49.51%) at 4 h with 20 mg/kg dose in carrageenan-induced paw oedema models. The sakuranetin significantly reduced the CFA-induced arthritis (44.72%) with 10.0 mg/kg dose at day 6. The sakuranetin exhibited maximum antimicrobial activity against Bacillus subtilis (IZ=28.09±0.6 mm, MIC=10 μg/ml) and Candida albicans (IZ=22.06±0.6 mm, MIC=25 μg/ml) when antimicrobial activity was tested by disc diffusion and microdilution methods. The isolated flavonoids from this plant species demonstrated significant anti-inflammatory and antimicrobial activities. The isolated flavonoids from H. ellipticum showed the therapeutic efficacy in the treatment of inflammations and infections.