Current Pharmaceutical Biotechnology - Volume 19, Issue 7, 2018

Background: Nanoparticles (NPs) or nanomaterials being used widely in various fields have occupied prime importance in biomedical sciences, owing to their unique size dependent properties which make them superior to bulk materials. One of the major applications of NPs in biomedical field is their therapeutic application including antimicrobial activity. Objective: It is already well known that certain NPs such as silver, zinc oxide, copper, iron etc. bears significant antimicrobial activity as they release metal ions which subsequently generate reactive oxygen species (ROS), consequently demonstrating potential to be a better alternative to antibiotics and other antimicrobial agents. Although some of these NPs have also been found to be effective against multi-drug resistant (MDR) bacteria and correspondingly preventing the biofilm formation. Still resistance can be developed towards these NPs owing to their repeated exposure. Therefore, it becomes pertinent to probe NPs for their better antimicrobial efficacies by using surface functionalization strategies to enable them to interact with some specific cells in order to augment the antimicrobial response. Results: Thus present review focuses on the mode of action of NPs, their toxicity and colloidal stability, shortcomings of antibiotics and other antimicrobial agents towards MDR bacteria, and possible outcomes of NPs functionalized with different agents. Conclusion: In this review we describe functionalized NPs as an alternative for targeting MDR bacteria, their mode of action and future directions that are necessary to move forward with this approach.

Background: Alfalfa and red clover are the most widespread and most important perennial legumes, primarily used as a high-quality feed for livestock. Both alfalfa and red clover, as well as some other plant species from Fabaceae family, are a rich natural source of phytoestrogens, nonsteroidal compounds with an estrogenic activity whose beneficial effects in the prevention and treatment of many diseases are demonstrated in numerous scientific studies. Objectives: Nowadays, various herbal preparations are present on the world market and their use is constantly increasing, as well as the growing demands of consumers for environmentally sound and health-safe production of plant species used as sources of active substances. Because of their widespread distribution, the possibility of organic breeding, and also significant increases in surface area under genetically modified crops in most EU countries, alfalfa and red clover have become more interesting alternative sources of phytoestrogens. The most common phytoestrogens in these forage legumes are genistein, daidzein, glycitein, formononetin, biochanin, coumestrol, kaempferol and apigenin. The content of these substances is significantly influenced by a number of factors including genotype, environment, production technology, plant maturity stage, and individual plant parts. Conclusion: Available evidence suggests that forage legumes represent high promising sources of health-promoting phytoestrogens. Due to numerous favorable features, they can find commercial application in different industries such as pharmaceutical, nutraceutical, cosmetic, and agriculture.

Background: Euryale ferox Salisb. (Makhana) is a rooted macro-hydrophyte, grown as a crop in north Bihar wetlands, India. Makhana refers to yummy pops prepared through mechanical smacking of the baked seeds of E. ferox. New techniques have been evolved to produce pops from seeds at a brisk pace. Objective: It is specially associated with marital rituals possibly in view of its spermatogenic properties. It has a high amino acid index but a low glycemic value. The plant carries medicinal values against cardiovascular and diabetes-related diseases. Makhana pops with a high volume to mass ratio, is developed as a reliable system for drug delivery in the recent times. Results: There is a fair prospect of raising multi-faceted industry based on Makhana culture, harvest, post-harvest safety, preparation of pops and various types of food products therefrom and marketing in areas where water-logging is considered as a curse. It may generate employment and strengthen regional economy propping check on population migration primarily due to non-employment and poverty. Conclusion: Active research is required to harness this macro-hydrophyte along with co-culture of compatible fish varieties and other hydrophytes into a sustainable livelihood and economic prosperity.

Objective: The aim of this study was to evaluate the influence of adalimumab on the expression pattern of genes associated with JAK/STAT signaling pathway in Normal Human Dermal Fibroblast (NHDF) cells stimulated with 8 μg/ml of adalimumab and the identification of miRNAs regulating these genes’ expression. Method: NHDFs were cultured with or without the presence of adalimumab for 2, 8, and 24h. The microarray technology was used to determine expression profile of mRNAs and miRNAs. Results: Out of 22283 ID mRNA, 37 are associated with the JAK/STAT signaling pathway. It can be observed that 18 mRNAs differentiate NHDFs cultures with adalimumab from control. The analysis of miRNAs showed that, among 1105 ID miRNAs, 20 miRNAs are differentiating in cells treated with adalimumab for 2h, 9 miRNAs after 8h, and only 3 miRNAs after 24h. Conclusion: It can be observed that miRNAs play an extremely important role in the regulation of the expression of genes associated with JAK/STAT signaling pathway. The results of this study show the possibility of using changes in mRNAs and miRNAs profile expression, as complementary molecular markers of adalimumab treatment effectiveness.

Background: There are many calcium supplements available in the market, especially those containing calcium in the form of carbonate, which unfortunately is not absorbed by the body to a sufficient degree. Method: Therefore, an attempt was made to prepare new sources of calcium, consuming the chicken eggshells as natural raw materials, which were used in preparation of tablets containing calcium carbonate and calcium citrate as well as tablets with calcium carbonate and calcium bisglycinate. The influence of raw material properties on the pharmaceutical availability of calcium from the obtained tablets was investigated. Results: Based on the obtained calcium release profiles from the prepared tablets, it was found that the optimal source of calcium is a preparation containing calcium from chicken eggshells. It was found that both chicken eggshells and calcium bisglycinate (chelate) may be new, prospective sources of calcium. Calcium citrate prepared using eggshells as starting materials and bisglycinate is completely released within no more than 150 minutes. Conclusion: In turn, calcium carbonate added to calcium bisglycinate statistically significantly prolonges the release of calcium ions to 4 hours.

Background: Skin cancers are the most common malignancy in humans, and the number of cases has increased dramatically in the past few decades. Therefore, it is very important to carry out studies concerning new and safer anticancer natural agents (e.g. perillyl alcohol) and modern drug delivery systems, such as nanoformulations, which increase their bioavailability. Objectives: The aim of this work was to obtain different kinds of topical vehicles formulation and compare their efficiency in the release of perillyl alcohol. The release kinetics was determined by using certain selected mathematical models. Method: Formulations of a hydrogel, O/W nanoemulsion, O/W macroemulsion and nanostructured lipid carrier were developed as carriers for perillyl alcohol – one of the promising anticancer natural agents. The release study of the active agents was carried out using the Spectra/Por Standard Regenerated Cellulose membrane, at temperature T=320C. The concentration of active agents in the receptor solution was analyzed by high performance liquid chromatography. The release kinetics was determined by using selected mathematical models. Results: The results of our release studies have shown that the highest and comparable amount of perillyl alcohol was released from hydrogel (35.72 ± 0.21%), NLC (35.54 ± 1.48%) and nanoemulsion (34.87 ± 4.49%). The release was found to follow Fickian diffusion in the case of hydrogel and macroemulsion, while an anomalous mechanism was observed in the case of nanoformulations. Nevertheless, the obtained nanoformulations, as well as a conventional hydrogel, may be considered potential vehicles in topical delivery of perillyl alcohol.

Background: TGF-β1 gene (TGFB1) is one of the target genes involved in genetic predisposition to autoimmune diseases, particularly Hashimoto's thyroiditis (HT). Objective: In the present study, we attempted to investigate whether -509C/T SNP (rs1800469) in the promoter of TGFB1 is associated with the genetic susceptibility and clinical characteristics of Bulgarian patients with HT. We also analyzed serum TGF-β1 levels in different stages of the disease and its association with the -509C/T polymorphism in the TGFB1 promoter. Methods: The study recruited 121 female out-patients with autoimmune thyroiditis and 250 agematched healthy women (HC). Genotyping of the rs1800469 was performed by restriction fragment length polymorphism (RFLP)-PCR assay. The serum concentrations of latent acid-activated TGF-β1 protein were determined by the quantitative sandwich ELISA method. Results: Upon testing different types of inheritance, a significant risk was found for heterozygotes (CT) with OR=1.640; p=0.05 under the codominant model. The significantly higher risk for developing Hypothyroidism was calculated again for CT-genotype patients with OR=1.789. According to the hormone reference values, a significant association of CT genotype with decreased TSH (75.4%) simultaneously with increased free T4 hormone (94%) levels was also calculated. When patients were stratified by genotype and compared to the same genotype in HC, we observed that the decreased levels in serum TGF-b1 were significant for patients who carried the C-allele in their genotype. Conclusion: We suggest that heterozygous genotype CT is a genetic risk factor for developing more severe HT due to enhanced free T4 serum level at the onset of the disease, before developing the hypothyroid stage.

Background: The plant species Rosmarinus officinalis (RO), Thymus algeriensis (TA) and Thymus capitatus (TC) are widely used in traditional medicine in Tunisia. Their bioactivities have been reported before and particularly referred to their essential oils. The main objective of this work was to assess the phytochemical composition, the antioxidant activity, the antibacterial, antifungal, and cytotoxic potential of these 3 plants. Method: The High Performance Liquid Chromatography (HPLC), chemical tests and spectrophotometric methods were used for screening, quantification of phytochemicals and for antioxidant activities. Extracts were evaluated for antibacterial potential by the microdilution method. Antifungal activities were tested using the Poisoned food method against: Aspergillus niger and Aspergillus flavus. The cytotoxic potential of the plant extracts was checked using HCT 116 cultures. Results: Results revealed that aqueous extracts are not toxic compared to the methanolic extracts. Phenolic compounds were detected and these extracts showed excellent antioxidant activity presenting dose-dependent relationship. For antibacterial potential, all tested strains are more sensitive to Thymus extracts than Rosmarinus extracts. However, for antifungal activities, only Rosmarinus extracts inhibited mycelial growth. HPLC analysis allowed the identification of ten compounds with the abundance of gallic acid. Conclusion: This study showed important bioactivities (antioxidant, antimicrobial, and safety potential) of the plant species RO, TA and TC used in traditional medicine.