Juber Akhtar

Eupalitin induces apoptosis in prostate carcinoma cells through ROS generation and increase of caspase-3 activity.

Prostate cancer is the second most common malignancy in the human reproductive system. Eupalitin is one of the O‐methylated flavonol‐exhibited enhanced cancer chemopreventive agents. The current study highlights the structural determination of eupalitin and aims to explore the antitumor activity of eupalitin in human prostate cancer cell (PC3) and its underlying mechanism. Eupalitin structure was determined by using FTIR, 1H NMR, and 13C NMR. PC3 cells were treated with increasing concentrations of eupalitin, followed by analysis of the cell viability with an MTT assay. The results demonstrated that eupalitin markedly inhibited the proliferation of PC3 cells in a concentration‐dependent manner. The results from fluorescent microscopic analysis of nuclear condensation and intracellular ROS generation determined that eupalitin significantly induced ROS level lead to nuclear apoptosis. Cell cycle analysis revealed that eupalitin‐induced cell cycle progression as a percentage of cells in G0/G1 phase decreased whereas S phase increased. Caspase‐3 immunofluorescence analysis confirms the efficacy of eupalitin‐inducing apoptotic pathway and cell death. Thus, our study is helpful in understanding the mechanism underlying these effects in prostate cancer and it may provide novel molecular targets for prostate cancer therapy.

Nanoemulsion: for improved oral delivery of repaglinide

Abstract Repaglinide (RPG) is a fast-acting prandial glucose regulator. It acts by stimulating insulin release from pancreatic β-cells. Recurrent dosing of RPG before each meal is burdensome remedy. Hence the plan of the present study was to evaluate nanoemulsion as a hopeful carrier for RPG for persistent hypoglycemic effect. The drug was incorporated into oil phase of nanoemulsion to give improved biopharmaceutical properties as compared to the lipid-based systems. Pseudo ternary phase diagrams were prepared by aqueous titration method. Formulations were selected at a difference of 5% w/w of oil from the o/w nanoemulsion region of phase diagrams. The optimized nanoemulsion formulation constituted sefsol-218 (5% v/v) as an oil phase, 30% v/v of Tween-80 and transcutol as a surfactant and co-surfactant to restrain nanodroplet size and low viscosity and distilled water (65%). In vitro dissolution studies showed higher drug release (98.22%), finest droplet size (76.23 nm), slightest polydispersity value (0.183), least viscosity (21.45 cps) and immeasurable dilution capability from the nanoemulsion as compared with existing oral tablet formulation. The optimized RPG nanoemulsion formulation showed better hypoglycemic effect in comparison to tablet formulation in experimental diabetic rats. No significant variations were also observed in the optimized formulation when subjected to accelerated stability study at different temperature and relative humidity over a period of 3 months.

Algal bioactive compounds in the cosmeceutical industry: a review

Abstract: The term cosmeceutical is derived from a combination of ‘cosmetic’ and ‘pharmaceutical’, and indicates that active ingredients are present in a specific cosmetic product. These cosmeceuticals or cosmetic products have ingredients with medical or drug-like benefits. They are formulated to increase positive physiological effects at the cellular level in addition to enhancing the skins appearance. Cosmeceutical applications using algae are rapidly growing because of increasing demands from customers. The basic premise is that novel bioactive substances from natural sources are safer and equally or more efficacious than artificial substances. These compounds should have highly effective and stable properties for therapeutic use with low potential toxicity. Recently, marine organisms have been demonstrated as rich sources of structurally diverse, biologically active compounds with extensive cosmeceutical potential. Numerous compounds have been isolated from marine organisms, and these compounds have various purported cosmeceutical activities including antioxidant, anti-inflammatory, antiallergenic, antiaging and antiwrinkling effects, and ultraviolet protection. This review is focused on algal natural products and their potential for development of cosmeceuticals from novel and potent phytochemical compounds.

Silymarin nanoemulsion against human hepatocellular carcinoma: development and optimization

Abstract Objective: Nanoemulsion of silymarin was developed and optimized. Materials and methods: Nanoemulsion was made by aqueous titration method. Sefsol 218 (5.8% v/v), Kolliphor RH40 and polyethylene glycol 400 (Smix; 2:1; 28.99% v/v) were used as oil phase, surfactant and co-surfactant while distilled water (65.22% v/v) acted as an aqueous phase. Nanoemulsion was characterized on the basis of particle size, viscosity, electrical conductivity and refractive index. Further, in vitro release, in vivo pharmacokinetic study, stability study and cancer cell line studies were also performed. Results and discussion: The optimized formulation (NE9) with mean particle size of 21.24 nm showed a minimum viscosity of 9.59 cps, maximum drug release (97.75%) in 24 h. The NE9 formulation also showed higher AUC (p < .01) and Cmax (p < .01) and shorter Tmax (p < .05) compared with conventional and standard suspensions of silymarin. The stability study also showed considerably stable formulations at refrigerator temperature as compared with room temperature (p > .05). The cancer cell line studies also confirmed that silymarin nanoemulsion reduced the cell viability and increased ROS intensity and chromatin condensation (p < .05). Conclusion: Our results concluded that nanoemulsion may be an efficient carrier for oral delivery of silymarin against human hepatocellular carcinoma without damaging normal cells.

Evaluation of anticancer activity of Cordia dichotoma leaves against a human prostate carcinoma cell line, PC3

Mechanisms of antioxidant and apoptosis induction may be involved in the management of cancer by medicinal plants. Aim of the study was designed to evaluate anticancer activity of the methanolic extract of Cordia dichotoma leaves (MECD) against a human prostate carcinoma cell line, PC3. Flavonoid content was determined by colorimetric principle and antioxidant activity by various in vitro assays. MTT, DCFH-DA and DAPI staining assays were performed for the evaluation of cytotoxicity, analysis of induction of apoptosis and intracellular reactive oxygen species (ROS) activity level by MECD against human prostate carcinoma cell line, PC3. Flavonoid content was found to be 160 mg QE/g extract. IC50 values for MECD treatment in various assays based on scavenging of 2,2-diphenyl-1-picrylhydrazyl, 2,2-azinobis(3-ethylenebenzothiazoline-6-sulfonic acid), nitric oxide, peroxy radical, superoxide anion, hydroxy radical were found to be 315.5, 38, 476, 523, 197, 82 μg/ml respectively. MECD exposure to PC3 cells significantly increased the cell death (p < 0.001, IC50 = 74.5 μg/ml), nuclear condensation, apoptosis (p < 0.001) and induced production of ROS (p < 0.001) initiating apoptotic cascade in a dose dependent manner. This study confirms that MECD possesses antioxidant property and can prevent carcinogenesis by reducing oxidative stress. MECD possesses anticancer activity and lead to PC3 cell death via induction of apoptosis mediated through excessive ROS generation. Flavonoids in MECD may be responsible for these activities due to dual antioxidant and pro-oxidant properties.

Gold Nanoparticles Conjugated Levofloxacin: For Improved Antibacterial Activity Over Levofloxacin Alone

BACKGROUND Levofloxacin is a potent antibiotic with severe side effects due to its high doses. Bacterial resistance may be due to frequent use of antibiotics. Biogenic gold nanoparticles conjugated levofloxacin (Au-HSA-LvN-NPs) were developed by Human Serum Albumin (HSA) and nitrate reductasemediated pathways. METHODS Au-HSA-LvN-NPs (size = 27.2 ± 1 nm) were readily generated with high emulsion stability zeta potential (-13.3 mV). The developed nanoparticles were also characterized by UVvisible spectroscopy, Transmission Electron Microscopy and Dynamic Light Scattering techniques. RESULTS The optimized nanoparticles were found efficient against both Gram-positive bacteria and Gramnegative bacteria specifically S. aureus (MIC-0.373 µg/ml), E. coli (MIC-0.149 µg/ml) and P. aeruginosa (MIC-0.346 µg/ml) respectively. CONCLUSION The efficiency of bioconjugated levofloxacin got improved by 1.94 times, 2.89 times and 1.46 times against S. aureus, E. coli and P. aeruginosa respectively, in comparison to pure levofloxacin.

Protection of hepatotoxicity using Spondias pinnata by prevention of ethanol-induced oxidative stress, DNA-damage and altered biochemical markers in Wistar rats

Background Traditional systems of medicine use herbal drugs for hepatoprotection. Thus, the study was designed to evaluate the hepatoprotective and antioxidant effects of Spondias pinnata bark extracts against ethanol-induced liver injury in Wistar rats. Methods Group I animals were treated with 1 mL/kg 0.3% carboxymethyl cellulose and Group II with 12 mL/kg 50% ethanol for 8 consecutive days. Groups III–VII animals were first treated with 400 mg/kg petroleum ether extract, chloroform extract, acetone extract (AE), ethanol extract (EE), and 100 mg/kg silymarin, and then 12 mL/kg 50% ethanol orally after 2 hours pretreatment each day for 8 consecutive days. Six hours after the last dose, blood was withdrawn. The hepatoprotective activity was assessed by several biochemical and antioxidant parameters. It was accomplished by the histopathology and DNA fragmentation study of liver tissues. Results Treatment with S. pinnata extracts, mainly AE and EE significantly (p < 0.05–0.01) and dose-dependently prevented the ethanol-induced increase in serum levels of aspartate aminotransferase, alanine aminotransferase, alkaline phosphatase, lactate dehydrogenase, cholesterol, bilirubin, and malondialdehyde, and decrease in reduced glutathione, catalase, superoxide dismutase, and albumin. They also attenuated the ethanol-induced DNA damage. Hepatoprotective potential of the extract was less than that of standard drug silymarin. Results of the study were well supported by the histopathological observations. Conclusion S. pinnata extracts AE and EE possess a potent hepatoprotective effect against ethanol-induced liver injury in Wistar rats, and protect them from hepatotoxicity by prevention of ethanol-induced oxidative stress, DNA-damage and altered biochemical markers.

An insight of pharmacognostic study and phytopharmacology of Aquilaria agallocha

Aquilaria agallocha, an important medicinal plant is one of the most widely growing species of the family Thymelaeaceae. It is a precious plant on the earth because of its spacious medicinal properties. The present review provides significant information regarding its phytochemical investigations, pharmacological activities and medicinal properties as a folk medicine to treat several diseases like inflammation, arthritis, vomiting, cardiac disorders, cough, asthma, leprosy, anorexia, headache and gout. The plant has been reported to possess several pharmacological activities such as antinociceptive, antimicrobial, laxative, anti-oxidant, sedative, antihyperglycaemic, thrombolytic, antidiabetic, ulcer protective, anticancerous, antidiarrhoeal, hepatoprotective and CNS activities. Every portion of the plant has beneficial properties that can serve the mankind. The entire plant can be extensively studied for further future prospectives.

A new linoleiyl arabinopyranoside from the bark of Bauhinia racemosa Lam and a new flavonoidal glycoside from the leaves of Cordia dichotoma Linn

Abstract Phytochemical investigation is very valuable for the ethnomedicinally important plants Bauhinia racemosa Lam (BR) and Cordia dichotoma Linn (CD) used for the cure of variety of ailments. This study was thus designed for phytochemical investigation of BR bark and CD leaves. Phytoconstituents were isolated from the methanolic extracts of the plants by column chromatography using silica gel as stationary phase. The structures had been established on the basis of their physicochemical and spectral data, i.e. IR, 1H NMR, 13C NMR and MS. Elution of the columns with different solvents furnished six compounds (1–6) from the methanolic extract of BR bark and three compounds (7–9) from the methanolic extract of CD leaves which were structurally elucidated. The present phytochemical investigation reported several new compounds useful in increasing the existing knowledge of phytoconstituents from BR bark and CD leaves which is very valuable, as these drugs are used in the Indian traditional systems of medicine.

Nanomulsion as a Carrier for Efficient Delivery of Metformin

Metformin (MTF) improves hyperglycemia primarily by suppressing glucose production by the liver. The objective of our investigation was to evaluate nanoemulsion as a promising carrier for MTF for sustained hypoglycemic effect. The drug was incorporated into oil phase of nanoemulsion, which finally improved biopharmaceutical properties achieved when compared with lipid based systems. Pseudo ternary phase diagrams were prepared by aqueous titration method. Formulations were selected at a difference of 5% v/v of oil from the o/w nanoemulsion region of phase diagrams, and then thermodynamic stability and dispersibility tests were performed. The composition of optimized formulation was hydrogenated castor oil (5% v/v), 30% v/v of surfactant (tween 80), co-surfactant (transcutol) and distilled water (65% v/v) as an aqueous phase. The preparation showed maximum drug release (98.70%), optimal globule size (92.25 nm), lowest polydispersity value (0.172), lesser viscosity (22.124 cps) and infinite dilution capability. The antidiabetic activity of optimized MTF nanoemulsion formulation evaluated by blood glucose estimation showed significant hypoglycemic effect which was comparable to that observed with conventional marketed formulation in experimental diabetic rats. Optimized formulation was subjected to stability studies at different temperature and relative humidity and was found to be stable. No significant variations were observed in the formulation over a period of 3 months at accelerated storage conditions.