A dual-function fluorescence 'turn-on' probe that allows Zn (II) bioimaging and quantification of water in the organic solvent.

Herein, a Eugenol-derived fluorescence 'turn-on' probe FLHE was synthesized by condensing 2-((3-(trifluoromethyl)phenyl)amino)benzohydrazide with 5-allyl-2-hydroxy-3-methoxybenzaldehyde. FLHE demonstrated very low fluorescence in the studied organic solvents of varying polarities. However, upon titration with Zn2+ in HEPES buffer (pH = 7.4, 50% ACN, v/v), FLHE showed 40-fold higher fluorescence signals indicating the formation of the FLHE-Zn2+ complex. The fluorescence turn-on phenomenon upon FLHE-Zn2+ complex formation results from a chelation-enhanced fluorescence (CHEF) effect. The FLHE-Zn2+ complexation demonstrated a stokes shift of 156 nm (λex = 350 nm, λem = 506 nm) and an about 33-fold increase in the quantum yield (FLHE, Φ = 0.007; FLHE-Zn2+ complex, Φ = 0.23). The binding constant (Ka) determined by the Benesi-Hildebrand plot for interaction between FLHE and Zn2+ was 5.33 × 103 M-1. FLHE demonstrated a LOD of 31.8 nM for detecting Zn2+ in the environmental samples without interference from other cations and anions. FLHE-based paper strip (FLHE-PS) assay was developed to quantify the Zn2+ ions in water and the water content of organic solvent. FLHE-PS allows the detection of Zn2+ in aqueous solutions with a LOD of 63.2 nM and quantifying water in acetonitrile with a LOD of 0.14%. These results indicate that the FLHE has high applicability for detecting Zn2+ in living cells and environmental samples and detecting the presence of water in the organic solvents.

Designing a TiO2-MoO3-BMIMBr nanocomposite by a solvohydrothermal method using an ionic liquid aqueous mixture: an ultra high sensitive acetaminophen sensor.

This study shows a simplistic, efficient procedure to synthesize TiO2-MoO3-BMIMBr nanocomposites. Powder X-ray diffraction, scanning electron microscopy, energy-dispersive X-ray spectroscopy, and X-ray photoelectron spectroscopy have all been used to completely analyse the materials. The detection of acetaminophen (AC) has been examined at a modified glassy carbon electrode with TiO2-MoO3-BMIMBr nanocomposites. Moreover, the electrochemical behavior of the nanocomposite modified electrode has been studied by cyclic voltammetry (CV), differential pulse voltammetry (DPV), chronoamperometry and electrochemical impedance spectroscopy (EIS). The linear response of AC was observed in the range 8.26-124.03 nM. The sensitivity and detection limits (S/N = 3) were found to be 1.16 µA L mol-1 cm-2 and 11.54 nM by CV and 24 µA L mol-1 cm-2 and 8.16 nM by DPV respectively.

Development and Evaluation of Naproxen Sodium Gel Using Piper cubeba for Enhanced Transdermal Drug Delivery and Therapeutic Facilitation.

BACKGROUND: The absorption of drug through skin avoids many side effects of oral route like gastric irritation, nausea, systemic toxicity etc and thus improves patient compliance. Naproxen sodium (NPRS) is one of the potent NSAID agents. OBJECTIVE: The present study was aimed to develop and evaluate the gel formulation containing NPRS for transdermal drug delivery reducing the side effects and improving patient compliance. The patents on topical delivery of NSAIDS (US 9012402 B1, US 9072659 B2, US 20150258196 A1) and patents indicating use of herbal penetration enhancers (US 20100273746A1, WO 2005009510 A2, US 6004969 A) helped in selecting the drug, excipients. METHOD: Current protocol employs various extracts of Piper cubeba fruit to evaluate its role in absorption of NPRS. Various batches containing 1% NPRS and varying concentrations of synthetic permeation enhancers or the extracts were formulated in carbopol gel. Gel was evaluated for parameters like organoleptic parameters, pH, viscosity and spreadability. An ex-vivo percutaneous absorption of NPRS from gel was investigated and compared with best performing synthetic enhancer, transcutol P (TP). RESULT: The batch containing 2% n-hexane extract (NHE) of Piper cubeba showed higher permeation than TP and Chloroform (CE), Methanolic (ME) and aqueous (AE) extracts as well. It showed improved % cumulative release (85.09%) and flux (278.61µg/cm2.h), as compared to TP and other extracts. Histopathology indicated the formulation safer as compared to that with synthetic enhancer. CONCLUSION: It suggests P. cubeba as effective and safer tool for transdermal delivery and acts as therapeutic facilitator for naproxen. GC-MS analysis indicates lignans & terpenes in NHE to which this permeation enhancement activity may be attributed.

Synthesis, characterization and evaluation of the suppression of insulin resistance in Type-II diabetes mellitus animals by treatment with metal complex.

The present study is characterized toward thespesone isolation from Thespesia populnea (Malvaceae). Subsequently it was modified and characterized to study its effect on diabetes related symptoms. The complex is administered to diabetes induced mice with the doses of 5, 10 and 20 mg/kg, p.o. and the effect of complex on the level of body weight, lipid profile and blood glucose was studied after 22 days. The results have indicated that diabetic mice show a significant (p < 0.01) decrease in the level of serum triglyceride, plasma glucose and increase in body weight. Hence the present investigation reveals that newly synthesized complex is useful in the management of Type-II diabetes mellitus because of its ability to reduce insulin resistance.

The isolation, Characterization and Preclinical Studies of Metal Complex of Thespesia populnea for the Potential Peroxisome Proliferator-activated Receptors-γ Agonist Activity.

BACKGROUND: Diabetes mellitus is an international public health problem since ancient days. The condition is predominantly more severe in developing countries like India where, life is more sedentary due to the even changing lifestyles in this fast-paced global scenario. Thespesia populnea is widely used in the ayurvedic system of medicine for treatment of diabetes mellitus in India for years. The aim of this work is to explore the anti-diabetic activity of the isolated compound. MATERIALS AND METHODS: The sesquiterpene isolated from hexane fraction of bark of T. populnea modified synthetically then identified by using analytical techniques such as electron paramagnetic resonance spectra for confirmation and the anti-diabetic activity was evaluated by anti-hyperglycemic, hypoglycemic potential. RESULT: In the present work, we have studied the anti-hyperglycemic and hypoglycemic activity of the vanadium complex in glucose loaded and normal animals were shown significantly decreased in plasma blood glucose level. The results derived from preclinical studies confirm the potential of new sesquiterpene. CONCLUSION: The findings could provide evidence regarding the anti-diabetic potential of T. populnea by lowering blood glucose level. SUMMARY: Thespesia populnea is widely used in the ayurvedic system of medicine for treatment of diabetes in India. Present study aimed to explore the anti diabetic potential of isolated compound. Isolation of sesquiterpene from hexane fraction of bark of Thespesia populnea and modified synthetically then authenticated by using analytical techniques such as electron paramagnetic resonance spectra for confirmation. The modified complex was further assessed for its anti diabetic property in glucose loaded rats. Vanadium complex demonstrated significant reduction in plasma blood glucose level in glucose loaded animals. The results derived from preclinical studies confirm the potential of new sesquiterpene. The present findings conclude that anti diabetic potential of Thespesia populnea could be due to lowering blood glucose level by acting on PPAR-γ receptor.

Strychnos potatorum: Phytochemical and pharmacological review.

In traditional system of medicine, the seeds of Strychnos potatorum Linn. (family: Loganiaceae) are used in the treatment of gonorrhea, leukorrhea leukeorrhea, gastropathy, bronchitis, chronic diarrhea, dysentery, renal and vesicle calculi, diabetes, conjunctivitis, scleritis, ulcers and other eye disease. An attempt has been made to highlight this medicinal seeds through phytochemical and pharmacological study. The present review deals with the phytochemical and pharmacological screening of therapeutic importance from Strychnos potatorum L., an important medicinal plant. This study includes the collective information of different medicinal uses of Strychnos potatorum. The generated data has provided the basis for its wide use as the therapeutant both in the traditional and folk medicines.

Quantitative estimation of diacerein in bulk and in capsule formulation using hydrotropic solubilizing agents by UV-spectrophotometry and the first order derivative using the area under curve method.

PURPOSE: This study was designed to develop and validate two simple, rapid, and economical UV-spectrophotometric and the first-order derivative methods using the area under curve method for estimation of diacerein in bulk and in capsule formulation. MATERIALS AND METHODS: In this study, hydrotrophic solution of 8 M urea and 0.5 M potassium citrate were employed as the solubilizing agent to solubilize a poorly water-soluble drug, diacerein. In the UV-spectrophotometry method, two wavelengths 252.0 nm and 266.2 nm and in the first-order derivative spectrophotometric methods two wavelengths 259.4 nm and 274.2 nm in 8 M urea and two wavelengths 247.8 nm and 267.4 nm in the UV-spectrophotometry method and in the first-order derivative spectrophotometric methods two wavelengths 259.2 nm and 274.2 nm in 0.5 M potassium citrate were selected for determination of areas. RESULTS: Hydrotrophic agents used did not interfere in spectrophotometric analysis of diacerein. Diacerein followed linearity in the concentration range of 2-12 µg/mL with a coefficient correlation of 0.999 for both methods. CONCLUSION: The amount of drugs estimated by both proposed methods are in good accord with label claim. The % RSD value in recovery, precision, and ruggedness studies are found to be less than 2 indicate that the method is accurate, precise, and rugged.

Design and development of a stable polyherbal formulation based on the results of compatibility studies.

INTRODUCTION: Ayurvedic and herbal medicinal products contain a combination of botanicals; each of these contains a number of chemical compounds that may give the anticipated activity in combination. Therefore, it is very important to analyze and evaluate the compatibility of various active constituents and markers from different medicinal plants for their possible chemical interactions with various excipients at different storage conditions during the development of a stable polyherbal formulation. OBJECTIVE: To study chemical stability of kalmegh (Andrographis paniculata) and kutki (Picrorhiza kurroa) extract for their active markers andrographolide, kutkoside and picroside-I and to develop stable polyherbal formulation based on the incompatibility studies. MATERIALS AND METHODS: The compatibility study was carried out on individual ethanolic extracts of these two plants along with the commonly used excipients in the ratio of 1:1 at 40 ± 2°C and 75 ± 5% relative humidity and at a refrigeration temperature of 5 ± 1°C for initial, 7-, 15- and 30-day intervals. The analysis was carried out using the validated reverse phase-high-performance liquid chromatography methods. A stable tablet dosage form was developed based on the results of these studies. RESULT: The study suggested that the active markers of kutki (kutkoside and picroside-I) were found to be degraded in the presence of the kalmegh extract. However, the active marker of the kalmegh extract (andrographolide) was found to be stable. Both the extracts showed excellent compatibility with all the excipients used in making this formulation. No significant decrease in the kutkoside and picroside-I content from the formulation was observed. CONCLUSION: By separate granulation process the exposure of both the extracts can be minimized thus avoiding the degradation of active markers.

Rapid microwave-assisted extraction and HPTLC-photodensitometric method for the quality assessment of Boerhaavia diffusa L.

A rapid and cost-effective method for the extraction of rotenoids in Boerhaavia diffusa L., based on the use of microwave-assisted extraction (MAE), is proposed. The conventional reflux, soxhlet, and maceration extraction methods were also conducted to validate the reliability of the new method. Under the optimized conditions, two rotenoids (boeravinone B and E) were extracted and quantified by HPTLC. The yield of boeravinone B and E achieved by MAE was 0.15 and 0.32% (w/w), respectively. The result showed that MAE-HPTLC is a simple, rapid, and solvent-sparing method for the extraction and quantitation of boeravinone B and E from B. diffusa L.