A biochemical, theoretical and immunohistochemical study comparing the therapeutic efficacy of curcumin and taurine on T-2 toxin induced hepatotoxicity in rats.

Introduction: Foodborne trichothecene T-2 Toxin, is a highly toxic metabolite produced by Fusarium species contaminating animal and human food, causing multiple organ failure and health hazards. T-2 toxins induce hepatotoxicity via oxidative stress causing hepatocytes cytotoxicity and genotoxicity. In this study, curcumin and taurine were investigated and compared as antioxidants against T-2-provoked hepatotoxicity. Methods: Wistar rats were administrated T-2 toxin sublethal oral dose (0.1 mg/kg) for 2 months, followed by curcumin (80 mg/kg) and taurine (50 mg/kg) for 3 weeks. Biochemical assessment of liver enzymes, lipid profiles, thiobarbituric acid reactive substances (TBARs), AFU, TNF-α, total glutathione, molecular docking, histological and immunohistochemical markers for anti-transforming growth factor-ß1 (TGFß1), double-strand DNA damage (H2AX), regeneration (KI67) and apoptosis (Active caspase3) were done. Results and Discussion: Compared to T-2 toxin, curcumin and taurine treatment significantly ameliorated hepatoxicity as; hemoglobin, hematocrit and glutathione, hepatic glycogen, and KI-67 immune-reactive hepatocytes were significantly increased. Although, liver enzymes, inflammation, fibrosis, TGFß1 immunoexpressing and H2AX and active caspase 3 positive hepatocytes were significantly decreased. Noteworthy, curcumin's therapeutic effect was superior to taurine by histomorphometry parameters. Furthermore, molecular docking of the structural influence of curcumin and taurine on the DNA sequence showed curcumin's higher binding affinity than taurine. Conclusion: Both curcumin and taurine ameliorated T-2 induced hepatotoxicity as strong antioxidative agents with more effectiveness for curcumin.

Correlation between Antioxidant and Anti-Osteoporotic Activities of Shilajit Loaded into Chitosan Nanoparticles and Their Effects on Osteoporosis in Rats.

Various therapies for osteoporosis successfully reduce bone loss and fractures, but they mostly do not contribute to new bone structures and adversely affect patients. Shilajit is a natural mineral substance comprised of multi-components, with proved efficacy to improve immunity, antioxidant activity, and disease resistance. In the present study, various effects of shilajit water extract (SWE) on bone development and its management were determined in experimental glucocorticoid-induced osteoporotic rats. The fabrication of nanochitosan (NCT) and NCT conjugation with SWE were conducted and evaluated as enhanced formulations for treating osteoporosis. NCT and SWE/NCT had mean particle diameters of 196.4 and 248.4 nm, respectively, with high positivity charging and stability. The biochemical and anti-osteoporotic effects of SWE and SWE/NCT conjugates were investigated on different groups of compromised rats. Five groups each including six adult albino female rats were formed and treated for a duration of eight weeks with SWE and SWE/NCT conjugate. Significantly improved serum calcium, phosphorus, osteocalcin, and calcitonin levels but decreased hydrogen peroxide, IL-6, and antioxidant biomarkers were recorded in all SWE- and SWE/NCT-treated groups; the SWE/NCT treatment was most effectual treatment. These results suggest that SWE and SWE/NCT may cause anti-osteoporotic activity by reducing oxidative stress, IL-6, and H2O2 while restoring antioxidant levels. The conjugation of SWE onto NCT is highly recommended for augmenting their activities.

Application of Nanocomposites from Bees Products and Nano-Selenium in Edible Coating for Catfish Fillets Biopreservation.

Bee products, e.g., chitosan and propolis (Pro), have extraordinary importance in many disciplines including food biopreservation. Fish meat is highly susceptible to vast spoilage, especially catfish (Clarias gariepinus) products. The current work involved the extraction of bees' chitosan nanoparticles (BCht), Pro, Pro-mediated SeNPs and their composites, to evaluate them as potential antimicrobial and preservative nano-compounds, for the preservation of catfish fillets and augment their quality. BCht was extracted from bees (Apis mellifera) corpses and had a 151.9 nm mean particle diameter. The Pro was used for biosynthesis of SeNPs, which had 11.2 nm mean diameters. The entire compounds/composites exhibited powerful antibacterial acts against Escherichia coli, Staphylococcus aureus and Salmonella typhimurium, where S aureus had the uppermost resistance. BCht/Pro/SeNPs were the most forceful toward all bacterial strains. The constructed edible coatings (ECs) from produced compounds/composites (BCht, Pro, Pro/SeNPs, Pro/BCht and BCht/Pro/SeNPs) had elevated efficiency for preserving catfish fillets during cold storages for 7 days. The microbiological (total counts, psychrophilic bacteria, yeast and molds), spoilage chemical parameters (TVB-N, TBARS) and sensorial attributes (appearance, odor, color, overall quality) of ECs-treated fillets indicated the nanocomposite's efficiency for protecting the fish from microbial growth, the progress of chemical spoilage indicators and maintaining the sensorial quality of treated stored fillets. The most effective nanocomposite for maintaining the entire fillet's quality was the BCht/Pro/SeNP. The based ECs on BNCt, Pro/SeNPs and their nanocomposites could be endorsed for prospective employment in the biopreservation of various seafoods.

Coconut products alleviate hyperglycaemic, hyperlipidimic and nephropathy indices in streptozotocin-induced diabetic wistar rats.

Type 2 diabetes mellitus (T2DM) is a chronic and one of the most common metabolic diseases affecting large proportion of world population. Diabetes-induced changes in lipid and renal parameters are major risk factors contributing to diabetic complications such as diabetic nephropathy and cardiovascular diseases. Due to adverse effects associated with pharmacological intervention in the T2DM treatment, there is an increased interest in the research focussing on identifying novel plant based therapeutic agents. Here we report the effects of various coconut products on diabetic, lipid and renal parameters in streptozotocin (STZ)-induced diabetic rat model. Diabetic rats demonstrated a significant increase in serum glucose, and glycated haemoglobin levels (HbA1c). Lipid parameters including triglycerides, total cholesterol, low density lipoprotein cholesterol (LDL-cholesterol) and very low density lipoprotein cholesterol (VLDL-cholesterol) were found to be significantly increased, while high density lipoprotein cholesterol (HDL-cholesterol) was significantly declined in diabetic rats. Diabetic rats also displayed increased serum and kidney creatinine, urea, and total protein levels and increased urine glucose, urea, albumin and creatinine levels. Contrastingly, treatment with virgin and filtered coconut oils, coconut water and coconut milk resulted in a significant reversal in the levels of above studied parameters in diabetic rats. Further, these coconut products markedly prevented diabetes induced histopathological changes in kidney tissue. Collectively, the data demonstrate the antidiabetic, hypolipidemic and renal protective properties of various coconut products and underscore the importance of regular consumption of plant based medicinal products in the treatment of T2DM and its complications.

Identification, protein antiglycation, antioxidant, antiproliferative, and molecular docking of novel bioactive peptides produced from hydrolysis of Lens culinaris.

Bioactive peptides produced from natural sources are considered as strategic target for drug discovery. Hyperglycemia caused protein glycation alters the structure of many tissues that impairs their functions and lead complications diseases in human body. This study investigated the bioactive peptides produced from red and brown Lens culinaris that might inhibit protein glycation to prevent diabetic complications. In this study, red and brown Lens culinaris protein hydrolysates were prepared by tryptic digestion, using an enzyme/substrate ratio of 1:20 (g/g), at 37°C, 12 hr then peptide fractions <3 kDa were filtered by using ultrafiltration membranes. Protective ability against protein glycation, DPPH radical scavenging, and anti-proliferative activities (on HepG2, MCF-7, and PC3 cell lines) of peptide fractions were assayed in vitro. Results showed that glycation was inhibited by peptides from 28.1% to 68.3% in different test model. PC3 cell line was more sensitive to the peptides which showed strong anticancer activity with lower IC50 (0.96 mg/ml). Peptide fractions were sequenced by HPLC-MS-MS. Twenty eight novel peptides sequences was identified. In silico study, two peptides could be developed as a potential bioactive peptides exhibited antiglycation, antioxidant, and antiproliferative activities. PRACTICAL APPLICATIONS: Peptides are becoming an emerging source of medications with the development of new technologies. We have selected Lens Culinaris as one of the rich sources of proteins to explore novel bioactive peptides encapsulated in its seeds. Peptides fractions demonstrated protective ability against protein glycation, strong antioxidant potential, and promising antiproliferative activity. We have identified 28 novel peptides and molecular docking study revealed that some peptides showed strong binding potential to insulin receptor and ACE. Thus, these peptides might be used to manage diabetes complication as well as COVID-19 disease due to their interaction with ACE. However, those peptides needs to be further studied as a potential new drug.

Chemoprotective effects of inositol hexaphosphate against cyclophosphamide-induced testicular damage in rats.

Cyclophosphamide (CP) is commonly used as an anticancer agent but has been associated with high toxicity in several animal organs, including the testes. Inositol hexaphosphate (IP6) is a polyphosphorylated carbohydrate that is present in foods with high fibre contents and has a wide range of essential physiological and pathological activities. Thus, we estimated the defensive effects of IP6 against CP-related testicular toxicity in rats. Sperm counts, motilities, viabilities and abnormalities and levels of testosterone, luteinising hormone and follicle-stimulating hormone were evaluated. Testicle specimens were also processed for histological and biochemical analyses, including determinations of malondialdehyde, nitric oxide, total antioxidant capacity, alkaline phosphatase, acid phosphatase, gamma glutamyl transferase, ß-glucuronidase, c-reactive protein, monocyte chemoattractant protein and leukotriene-4 and in comet assays. CP treatments were associated with deleterious histopathological, biochemical and genetic changes in rat testicles, and these were ameliorated by IP6 supplements in drinking water.

Enhanced antimycotic activity of nanoconjugates from fungal chitosan and Saussurea costus extract against resistant pathogenic Candida strains.

Targeting the control of pathogenic Candida spp., especially the fungicides resistant strains from C. albicans and C. glabrata, nanoconjugates from the biopolymer (chitosan) and costus root extract (Saussurea costus) was synthesized and characterized. Chitosan was extracted from the grown mycelia of Aspergillus niger and characterized with high deacetylation degree of 91.2% and moderate molecular weight of 106.8 kDa. Synthesis of nanoconjugates from fungal chitosan/costus extract (NCt/CE) was conducted using ionic gelation technique; the resulted NCt/CE particles were characterized with mean diameter of 48 nm, positive zeta potentiality (+3.28 mV) and high stability. The infra-red spectra of synthesized nanoconjugates indicated their strong biochemical cross-linkage. The antimycotic activities, of the synthesized NCt, CE and their nanocomposite, were evaluated against standard and antibiotic-resistant strains from C. albicans and C. glabrata and revealed that the entire agents had notable antimycotic potentiality against all examined strains; the NCt/CE nanoconjugates had significantly stronger antimicrobial action. The scanning microscope imaging, of exposed resistant strains to NCt/CE, indicated their vigorous structural and morphological alterations and confirmed the antimycotic activity of the nanocomposite. NCt/CE nanoconjugates' synthesis could be exceedingly recommended as a natural, biodegradable and effectual antimycotic agent to control resistant pathogenic yeast strains.

Appliance of fungal chitosan/ceftriaxone nano-composite to strengthen and sustain their antimicrobial potentiality against drug resistant bacteria.

Nano-biopolymers could be employed for the delivery of active compounds to increase their stability, bioavailability, efficacy and sustainability. The bioactive chitosan polymer (Cts) was extracted from grown fungus, Cunninghamella elegans, and used for loading ceftriaxone (CFT) and forming the nano-conjugates using tripolyphosphate (TPP) - ionic crosslinking method. The characterization of synthesized CFT/chitosan nanoparticles (NCT) revealed that they chemically crosslinked and had particles' size mean of 56 nm. The CFT loading capacity onto NCT was 54.37%, while its entrapment efficiency was apparently high (79.43%); the maximum released of CFT was 78% from NCT composite after 90 h from dialysis. The CFT/NCT antibacterial activity was confirmed against 3 strains of Staphylococcus aureus (methicillin resistants), using disc diffusion and scanning images of electron microscope, which elucidate that CFT/NCT nano-composite had a vigorous action toward bacterial cells; most cells were ruptured and exploded after 6 h of exposure and entirely lysed after 9 h. The formulation of CFT/NCT nano-composite is exceedingly recommended for enhancing drug biocidal activity, especially against resistant bacterial strains.

Synthesis and in vitro antitumor activity of novel acylspermidine derivative N-(4-aminobutyl)-N-(3-aminopropyl)-8-hydroxy-dodecanamide (AAHD) against HepG2 cells.

Naturally occurring polyamines like Putrescine, Spermidine, and Spermine are polycations which bind to the DNA, hence stabilizing it and promoting the essential cellular processes. Many synthetic polyamine analogues have been synthesized in the past few years, which have shown cytotoxic effects on different tumours. In the present study, we evaluated the antiproliferative effect of a novel, acylspermidine derivative, (N-(4-aminobutyl)-N-(3-aminopropyl)-8-hydroxy-dodecanamide) (AAHD) on HepG2 cells. Fluorescence staining was performed with nuclear stain (Hoechst 33342) and acridine orange/ethidium bromide double staining. Dose and the time-dependent antiproliferative effect were observed by WST-1 assays, and radical scavenging activity was measured by ROS. Morphological changes such as cell shrinkage & blebbing were analyzed by fluorescent microscopy. It was found that AAHD markedly suppressed the growth of HepG2 cells in a dose- and time-dependent manner. It was also noted that the modulation of ROS levels confirmed the radical scavenging activity. In the near future, AAHD can be a promising drug candidate in chalking out a neoplastic strategy to control the proliferation of tumour cells. This study indicated that AAHD induced anti-proliferative and pro-apoptotic activities on HCC. Since AAHD was active at micromolar concentrations without any adverse effects on the healthy cells (Fibroblasts), it is worthy of further clinical investigations.