Biochemical Estimations Research Articles

Coconut (Cocos nucifera L.) inflorescence sap-derived sugar restores the glucose and lipid homeostasis in streptozotocin-induced diabetic Wistar rat model

Introduction and Aim: Coconut palm sugar (CPS) is a functional food comprising unique phytonutrients such as polyphenolics, minerals, inulin, etc., and has a low glycemic index (GI). Based on its distinctive biochemical composition, it was hypothesized that CPS would provide a glucose homeostatic effect. We investigated the effects of CPS oral administration in Wistar rats with streptozotocin-induced diabetes. Materials and Methods: Diabetic Wistar rats were administered with different doses of CPS (200,400 and 800 mg/Kg body weight) and standard gliclazide (5 mg/Kg b.w.) for 28 days. Biochemical estimations for fasting blood glucose, lipid profile and antioxidant status were performed. Results: Treatment with CPS significantly (P 0.001) decreased the plasma glucose levels at 120 min after glucose load. Serum blood glucose, hepatic enzymes (alanine transaminase (ALT), aspartate transaminase (AST), alkaline phosphatase (AP)), total cholesterol (TC), total triglycerides (TG), and low-density lipoprotein (LDL) levels were also decreased. However, levels of total serum protein and high-density lipoprotein (HDL) increased in a significant manner. Pancreatic enzymatic antioxidant levels were restored, and lipid peroxidation was decreased by CPS. Conclusion: CPS showed quite a few health benefits in diabetic rats by bringing back the glucose and lipid homeostasis to normal and yielded favorable outcomes in case of oxidative stress.

Effect of standardized Eucalyptus globulus leaf extract on brain oxidative stress and aberrant neurochemistry of fructose-streptozotocin-induced diabetic rats.

The neuro-pharmacological effect of Eucalyptus globulus ethanol leaf extract in fructose-streptozotocin-induced diabetic rats was evaluated in this study. The phytochemical analysis of the extract was carried out using HPLC-DAD. Diabetes was induced in rats with 10% fructose in drinking water and a single intraperitoneal injection of 40 mg/kg streptozotocin (STZ). Diabetic animals were orally treated with 100-400 mg/kg of the extract for 21 days with glibenclamide as the reference drug. Blood and brain tissue were processed for the determination of serum electrolyte levels, hematological indices, and biochemical estimations. Ergosterol, pinitol, catechin, quercetin, robinetinidol, and other polyphenols were identified in the extract. Diabetic animals showed decreased serum potassium and sodium ion levels and decreased hematocrit, hemoglobin, red blood cells, white blood cells and lymphocytes but increased neutrophils. The brains of animals in the untreated diabetic group with increased blood glucose level showed oxidative stress (increased level of MDA and myeloperoxidase but decreased level of reduced glutathione and superoxide dismutase) and disturbed neurochemistry (increased level of acetylcholinesterase and monoamine oxidase but decreased level of Na+K+ATPase, tyrosine hydroxylase and dopamine). Administration of the Eucalyptus globulus leaf extract remarkably ameliorated the observed hyperglycemia, electrolyte, and hematological imbalances in animals. In addition, the administration of the extract attenuated the brain redox imbalance, and neurochemical disturbances in the rats. These results show that Eucalyptus globulus leaves contain antioxidant and neurotransmitter modulating phytochemicals with the potential to be developed as therapeutic agents for the management of diabetic cerebrovascular problems and related complications.

Thymoquinone Ameliorates Carfilzomib-Induced Renal Impairment by Modulating Oxidative Stress Markers, Inflammatory/Apoptotic Mediators, and Augmenting Nrf2 in Rats.

Chemotherapy-induced kidney damage is an emerging problem that restricts cancer treatment effectiveness. The proteasome inhibitor carfilzomib (CFZ) is primarily used to treat multiple myeloma and has been associated with severe renal injury in humans. CFZ-induced nephrotoxicity remains an unmet medical need, and there is an urgent need to find and develop a nephroprotective and antioxidant therapy for this condition. Thymoquinone (TQ) is a bioactive compound that has been isolated from Nigella sativa seeds. It has a wide range of pharmacological properties. Therefore, this experimental design aimed to study the effectiveness of TQ against CFZ-induced renal toxicity in rats. The first group of rats was a normal control (CNT); the second group received CFZ (4 mg/kg b.w.); the third and fourth groups received TQ (10 and 20 mg/kg b.w.) 2 h before receiving CFZ; the fifth group received only TQ (20 mg/kg b.w.). This experiment was conducted for 16 days, and at the end of the experiment, blood samples and kidney tissue were collected for biochemical assays. The results indicated that administration of CFZ significantly enhanced serum marker levels such as BUN, creatinine, and uric acid in the CFZ group. Similarly, it was also noticed that CFZ administration induced oxidative stress by reducing antioxidants (GSH) and antioxidant enzymes (CAT and SOD) and increasing lipid peroxidation. CFZ treatment also enhanced the expression of IL-1β, IL-6, and TNF-α production. Moreover, CFZ increased caspase-3 concentrations and reduced Nrf2 expression in the CFZ-administered group. However, treatment with 10 and 20 mg/kg TQ significantly decreased serum markers and increased antioxidant enzymes. TQ treatment considerably reduced IL-1β, IL-6, TNF-α, and caspase-3 concentrations. Overall, this biochemical estimation was also supported by histopathological outcomes. This study revealed that TQ administration significantly mitigated the negative effects of CFZ treatment on Nrf2 expression. Thus, it indicates that TQ may have utility as a potential drug to prevent CFZ-induced nephrotoxicity in the future.

Protective Effect of Galantamine against Doxorubicin-Induced Neurotoxicity.

Doxorubicin (DOX) causes cognitive impairment (chemobrain) in patients with cancer. While DOX damages the cholinergic system, few studies have focused on the protective effects of cholinergic function on chemobrain. The acetylcholinesterase inhibitor galantamine (GAL) demonstrates neuroprotective properties. We investigated the mechanisms associated with DOX-induced cognitive impairments and the potential protective role of GAL in preventing chemobrain. Female Wistar rats were divided into control, DOX, GAL, and DOX + GAL groups. The rats in the DOX group were administered DOX (5 mg/kg intraperitoneally twice weekly for two weeks), while those in the GAL group were orally administered GAL (2.5 mg/kg) via oral gavage once daily for 15 days. The combination group (DOX + GAL) received GAL (once daily) and DOX (two times per week) concurrently. The body weights and survival rates were monitored daily. The animals were subjected to behavioral tests to assess the memory function followed by the biochemical estimation of inflammatory markers, including tumor necrosis factor-α (TNF-α), interleukine-1β (IL-1β), and interleukine-6 (IL-6) in rat brain tissue and RT-qPCR. DOX caused a reduction in the body weight and survival rate, which was alleviated by GAL concomitant treatment with DOX (DOX + GAL). These groups had reduced body weights and survival rates. DOX-treated animals exhibited an impairment of short-term spatial working memory, manifested as a behavioral alteration in the Y-maze test, the novel object recognition (NOR) test, and the elevated plus-maze (EPM) test. Concurrent treatment with GAL (DOX + GAL) showed improved memory function, as evidenced by an increase in the number of entries and time spent in the novel arm, the time spent exploring the novel object, and the transfer latency in the Y-maze, NOR test, and EPM test, respectively. These findings were also supported by biochemical observations showing the reversal of DOX-induced changes in IL-1β, IL-6, and TNF-α, as well as their relative expression of mRNA in brain tissue following concurrent GAL treatment. GAL appeared to be a neuroprotective agent against neuroinflammation caused by DOX by reducing inflammatory markers in the brain.

Estimation of Uric Acid Level for the Assessment of the Severity of Diseases with Clinically Diagnosed Sepsis

Background and Aim: The incidences of sepsis and septic shock depend on how acute organ dysfunction and infection are defined as well as on which data sources are studied. Hence this study was conducted to bring out the correlation between hyperuricemia in clinically diagnosed sepsis patients and morbidity and mortality. Material and Methods: Total of 150 patients was included in the study. For the uric acid estimation of the included patients; blood samples were taken from the patient. For the biochemical estimation of the uric acid level the collaboration was done with the department of biochemistry, medical college and hospital. Results: Among the 150 study participants, 64 patients had elevated uric acid levels which constitutes about 42.7%, whereas 86 patients constituting 57.3% had normal uric acid levels. It can be inferred that among the study population, patients had type 2 diabetes mellitus as the most common comorbidity at 40%. The most prevalent comorbidities among the patients with hyperuricemia were diabetesmellitus type 2 and type 1, decompensated liver disease and cerebrovascular accident. Patients without any comorbidities about 36% of the study population also developed sepsis. Conclusion: This study demonstrates that Serum Uric acid may be potentially used as a marker of severity of illness as well as predictor of mortality and morbidity in patients with clinically diagnosed sepsis in the IMCU. This study recommends further studies on a large basis to confirm the observations.

Effect of Europinidin against Alcohol-Induced Liver Damage in Rats by Inhibiting the TNF-α/TGF-β/IFN-γ/NF-kB/Caspase-3 Signaling Pathway.

The effect of europinidin on alcoholic liver damage in rats was examined in this research. A total of 24 Wistar rats were grouped in the same way into four groups: normal control (normal), ethanol control (EtOH), europinidin low dose (10 mg/kg), and europinidin higher dose (20 mg/kg). The test group rats were orally treated with europinidin-10 and europinidin-20 for 4 weeks, whereas 5 mL/kg distilled water was administered to control rats. In addition, 1 h after the last dose of the above-mentioned oral treatment, 5 mL/kg (i.p.) EtOH was injected to induce liver injury. After 5 h of EtOH treatment, samples of blood were withdrawn for biochemical estimations. Administration of europinidin at both doses restored all of the estimated serum, i.e., liver function tests (ALT, AST, ALP), biochemical test (Creatinine, albumin, BUN, direct bilirubin, and LDH), lipid assessment (TC and TG), endogenous antioxidants (GSH-Px, SOD, and CAT), malondialdehyde (MDA), nitric oxide (NO), cytokines (TGF-β, TNF-α, IL-1β, IL-6, IFN-γ, and IL-12), caspase-3, and nuclear factor kappa B (NF-κB) associated with the EtOH group. The results of the investigation showed that europinidin had favorable effects in rats given EtOH and may have hepatoprotective potential property.

Design, synthesis and pharmacological evaluation of disubstituted 1,3,4 thiadiazoles derivatives for the treatment of cognitive dysfunction

Acetylcholinesterase has emerged as a promising target for the development of potential treatments for cognitive decline. The deleterious effect of oxidative stress on the learning and memory paradigms of an individual has also been well documented. As a result, the current study shows the design, synthesis, and pharmacological evaluation of 2, 5 disubstituted 1,3,4 thiadiazole derivatives. Twenty-seven molecules were designed and the molecular docking study performed to predict the binding mode of the designed compounds also suggested that these compounds bind appreciably to the amino acids present in the active site of the recombinant human acetylcholinesterase (rhAChE). Based on docking analysis, Five novel hybrids (8,14, 22, 24 and 27) have been synthesized by employing suitable synthetic procedures and characterized by various spectral and elemental techniques. Further, these synthesized compounds were studied the pharmacokinetic study and evaluated against behavioral alterations using step-down passive avoidance and escape learning protocol at a dose of 0.5 mg/kg with reference to the standard, donepezil. All the synthesized compounds were evaluated for their in vitro acetylcholinesterase (AChE) inhibition at five different concentrations using mice brain homogenate as the source of the enzyme. Biochemical estimation of markers of oxidative stress has also been carried out to assess the role of synthesized molecules on the oxidative damage induced by ascorbic acid. Compounds 14 and 22 demonstrated significant acetylcholinesterase inhibition activity. These compounds also decreased ascorbic acid-induced oxidative stress, thus serving as promising leads for the amelioration of oxidative stress-induced cognitive decline. The findings suggested that these compounds could be investigated further as AChE and oxidative stress inhibitors for the treatment of cognitive dysfunction.

DNA-Based Molecular Markers and Antioxidant Properties to Study Genetic Diversity and Relationship Assessment in Blueberries

Blueberries (Vaccinium L. spp.) are an economically and medicinally important plant. Their antioxidant properties are well-known for their medicinal value in negating the harmful effects of free radicals. It is very important to develop genotypes that are high in health-promoting factors and economic value to meet present world needs. Estimation of genetic diversity using molecular markers, antioxidant properties, and their association can reveal genotypes with important characteristics and help in berry improvement programs. Wild blueberries are a better source of antioxidant metabolites compared to cultivated ones. Extensive variations are present in molecular and biochemical contents among wild clones and cultivars. The current review provides detailed and updated information on the economic and medicinal importance of blueberries, the application of molecular markers, and biochemical estimation in berry improvement and conservation, filling the gap in the literature.

Intranasal cerium oxide nanoparticles improves locomotor activity and reduces oxidative stress and neuroinflammation in haloperidol-induced parkinsonism in rats.

Introduction: Cerium oxide nanoparticles (CONPs) have been investigated for their therapeutic potential in Parkinson's disease (PD) due to their potent and regenerative antioxidant activity. In the present study, CONPs were used to ameliorate the oxidative stress caused by free radicals in haloperidol-induced PD in rats following intranasal administration. Method: The antioxidant potential of the CONPs was evaluated in vitro using ferric reducing antioxidant power (FRAP) assay. The penetration and local toxicity of the CONPs was evaluated ex-vivo using goat nasal mucosa. The acute local toxicity of intranasal CONPs was also studied in rat. Gamma scintigraphy was used to assess the targeted brain delivery of CONPs. Acute toxicity studies were performed in rats to demonstrate safety of intranasal CONPs. Further, open field test, pole test, biochemical estimations and brain histopathology was performed to evaluate efficacy of intranasal CONPs in haloperidol-induced PD rat model. Results: The FRAP assay revealed highest antioxidant activity of prepared CONPs at a concentration of 25μg/mL. Confocal microscopy showed deep and homogenous distribution of CONPs in the goat nasal mucus layers. No signs of irritation or injury were seen in goat nasal membrane when treated with optimized CONPs. Scintigraphy studies in rats showed targeted brain delivery of intranasal CONPs and acute toxicity study demonstrated safety. The results of open field and pole test showed highly significant (p < 0.001) improvement in locomotor activity of rats treated with intranasal CONPs compared to untreated rats. Further, brain histopathology of treatment group rats showed reduced neurodegeneration with presence of more live cells. The amount of thiobarbituric acid reactive substances (TBARS) was reduced significantly, whereas the levels of catalase (CAT), superoxide dismutase (SOD), and GSH were increased significantly, while amounts of interleukin-6 (IL-6) and tumour necrosis factor-alpha (TNF-α) showed significant reduction after intranasal administration of CONPs. Also, the intranasal CONPs, significantly high (p < 0.001) dopamine concentration (13.93 ± 0.85ng/mg protein) as compared to haloperidol-induced control rats (5.76 ± 0.70ng/mg protein). Conclusion: The overall results concluded that the intranasal CONPs could be safe and effective therapeutics for the management of PD.

Therapeutic Potential of Metformin-preconditioned Mesenchymal Stem Cells for Pancreatic Regeneration.

Diabetes occurs due to insulin deficiency or less insulin. To manage this condition, insulin administration as well as increased insulin sensitivity is required, but exogeneous insulin cannot replace the sensitive and gentle regulation of blood glucose levels same as β cells of healthy individuals. By considering the ability of regeneration and differentiation of stem cells, the current study planned to evaluate the effect of metformin preconditioned buccal fat pad (BFP) derived mesenchymal stem cells (MSCs) on streptozotocin (STZ) induced diabetes mellitus in Wistar rats. The disease condition was established by using a diabetes-inducing agent STZ in Wistar rats. Then, the animals were grouped into disease control, blank, and test groups. Only the test group received the metformin-preconditioned cells. The total study period for this experiment was 33 days. During this period, the animals were monitored for blood glucose level, body weight, and food-water intake twice a week. At the end of 33 days, the biochemical estimations for serum insulin level and pancreatic insulin level were performed. Also, histopathology of the pancreas, liver and skeletal muscle was performed. The test groups showed a decline in the blood glucose level and an increase in the serum pancreatic insulin level as compared to the disease group. No significant change in food and water intake was observed within the three groups, while body weight was significantly reduced in the test group when compared with the blank group, but the life span was increased when compared with the disease group. In the present study, we concluded that metformin preconditioned buccal fat pad-derived mesenchymal stem cells have the ability to regenerate damaged pancreatic β cells and have antidiabetic activity, and this therapy is a better choice for future research.

Cornu aspersum mucin attenuates indomethacin-induced gastric ulcers in mice via alleviating oxidative stress and inflammation

In the past three decades, a significant progress has been made in the prevention and treatment of gastric ulcers. The incidence of the disease has decreased, but gastric ulcer is still a medical problem. Currently, the available drugs for gastric ulcer treatment have many side effects; therefore, searching for new and safe therapeutic agents is mandatory. The present study aims to investigate the gastroprotective potential of Cornu aspersum (C. aspersum) mucin against gastric ulcers, and the mechanisms related to oxidative stress and inflammation. C. aspersum mucin was collected from 50 snails. The characteristics of C. aspersum mucin (chemical and microbiological) were evaluated. Mice were pretreated with famotidine and C. aspersum mucin (7.5 and 15 ml/kg b.w.) for 5 days, and then gastric ulcers were induced by indomethacin. Macroscopic examination, biochemical estimations, and Quantitative real-time PCR were carried out. Also, histopathological and immunohistopathological examinations were evaluated. We found that the high dose of the mucin significantly decreased the gastric mucosal malondialdehyde (MDA) and nitric oxide (NO) contents as well as interleukin 1β (IL-1β) and nuclear factor kappa β (NF-ҡB) expression, and inducible nitric oxide synthase (iNOS) immunostaining. It also increased the gastric mucosal GSH and catalase contents as well as hemoxygenase-1 (HO-1) and nuclear factor-erythroid 2-related factor 2 (Nrf2) expressions with regressions in gastric mucosal lesions. In conclusion, C. aspersum mucin could be a potential therapeutic candidate to protect against gastric ulceration.

Osajin from Maclura pomifera alleviates sepsis-induced liver injury in rats: biochemical, histopathological and immunohistochemical estimation

This paper aimed to examine the impact of flavonoid osajin (OSJ) on liver damage induced by sepsis. A total of 30 male rats were divided into 5 groups (Sham, sepsis, OSJ 150, OSJ 300 and reference). During sepsis, elevated lipid peroxidation (LPO) level and catalase activity (CAT) and decreased glutathione (GSH) level and superoxide dismutase (SOD) activity were observed in hepatic tissues of sepsis group in comparison with Sham group. A strong interleukin-33 and caspase-3 expressions were detected in hepatic tissues of sepsis group. On the contrary, OSJ administration to OSJ 300 group showed a significant decrease (P < 0.001) in LPO level (176±2.926) and significant increase (P < 0.001) in GSH level (10.586±0.083) and SOD activity (29.152±0.094) in comparison with sepsis group (185.777±1.735, 8.246±0.124, 24.307±0.379 respectively). In addition, the consumption of OSJ reduced expressions of interleukin-33 and caspase-3 and improved histopathological integrity. In conclusions, OSJ has hepatoprotective effect against sepsis-induced liver injury.

Assessment of Anti-Hepatotoxic Effect of Bahuinia tomentosa Linn against Paracetamol induced Hepatocellular Damage In Albino Mice

In today’s modern world the chemical induced hepatotoxicity is one huge threat to human life, even the drugs which have easy accessibility and availability are also produces side effects, when they are used irrationally, so the need for antidote from herbal industry is a common factor. Bauhinia tomentosa Linn belongs to fabaceae, considered as one such potential agent which constitutes wide range of chemical compounds which has therapeutic as well as antidote effect. In this study Bahuinia tomentosa Linn was extracted with ethyl alcohol and the prepared ethanolic extract was evaluated for its hepato protective effect against Acetaminophen induced hepato toxicity in albino mice. The biochemical estimation, histo pathological studies are served as index for the assessment of hepatoprotective activity. Modification in body and liver weight, proteins, levels of biomarkers, antioxidant enzymes along with histopatological variations of extract treated groups were compared with standard hepatoprotective drug silymarin. Marked hepatoprotective activity was noticed in extract treated groups in dose dependent manner. The study results revealed the antihepatato toxic effect of Bauhinia tomentosa Linn and recommended as an excellent natural source of drug in the treatment of acetaminophen induced hepatotoxicity.

Hypoglycaemic, Hypolipidaemic and Antioxidant Properties of Celastrus paniculatus Seed Extract in STZ-induced Diabetic Rats

Background: Celastrus paniculatus is a herb used in the Ayurvedic system of medicine that has been reported to show multiple pharmacological properties. In this study, we explored the antioxidative, hypolipidaemic and hypoglycaemic potential of C. paniculatus methanolic seed extract (CPMSE) in high-fat diet (HFD)/streptozotocin (STZ)-induced type 2 diabetes mellitus (T2DM) rats.Materials and methods: Seeds of C. paniculatus were extracted in methanol using Soxhlet extraction method. A total of 36 rats were induced with STZ and HFD and treated with glibenclamide or various concentrations of CPMSE. Upon treatment, blood samples were collected and kidney and liver samples were homogenised. Serum biochemical estimation was performed using several diagnostic kits. Protein was estimated by bicinchoninic acid (BCA) method. Oxidative stress was assessed by measuring malondialdehyde level and superoxide dismutase (SOD), catalase (CAT) and glutathione-S-transferase (GST) activity.Results: CPMSE caused improvements in glucose homeostasis, lipid profile, liver function and oxidative stress parameters in a dose-dependent manner. CPMSE significantly decreased the levels of fasting blood glucose and glycated haemoglobin as well as increased insulin level and total protein content. There was an increase in total cholesterol (TC), low density lipoprotein-cholesterol (LDL-C), triglycerides (TG) levels and reduction in high density lipoprotein-cholesterol (HDL-C) level. There was a decrease in serum levels of serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT) and alkaline phosphatase (ALP). CPMSE decreased LPO and increased CAT, SOD and GST activity.Conclusion: CPMSE has hypoglycaemic, hypolipidaemic and antioxidant properties by reducing the oxidative stress.Keywords: diabetes mellitus, Celastrus paniculatus, antioxidant, phytochemicals, phytonutrients, streptozotocin, high-fat diet

Morus alba fruit diet ameliorates cognitive deficit in mouse model of streptozotocin-induced memory impairment.

Mounting evidence shows that dietary intake of fruits with polyphenols is beneficial to improve impaired memory functions. This study explored the preventive as well as therapeutic effects of diet enriched with Morus alba fruits extract (DEMA) in streptozotocin (STZ) induced mouse model of memory impairment. The study consisted of two facets: one aspect consisted of pretreatment of animals with DEMA for two weeks followed by STZ (i.c.v) intervention and the second phase involved induction of dementia with STZ (i.c.v) followed by treatment with DEMA for 14days. Cognitive functions of animals were measured by Morris Water Maze test and to delineate the associated mechanism of action, brain biochemical estimations (acetyl-cholinesterase activity, myeloperoxidase activity, thiobarbituric acid reactive species, superoxide dismutase activity, reduced glutathione and nitrite/nitrate) and histopathological studies (haematoxylin and eosin staining) were performed. Pre- and post- treatment with DEMA significantly prevented and attenuated, respectively, the detrimental effects of STZ on mice brain. The results demonstrated that dietary modification, by incorporation of M. alba fruits, reduces the incidence and aids in treatment of memory disorder in mice by reducing central cholinergic activity, decreasing oxidative stress and preventing neurodegeneration.

Assessment of Dose Dependent Toxicity of Meloxicam in Gallus Domesticus

The main objective of the study was to investigate long term use of meloxicam on avian species especially on Gallus domesticus. Animals were divided into 4 groups each having 5 animals. Group I was control and was fed normal diet (maize, grains and millet). Group II was treated with low dose of meloxicam for 15 days. Group III was treated with low dose of meloxicam for 30 days. Group IV was treated with low dose of meloxicam for 60 days. The effect was studied specially on hepatic and renal functions. Meloxicam was given at low dose (0.1 mg/kg body weight) to treatment groups for 15, 30 and 60 days. For biochemical estimation blood and serum were collected by sacrificing animals. Tissues of vital organs were fixed for histological examination. Long term administration of meloxicam cause variation in liver and kidney functioning. No significant change was observed in organ weight of treated groups as compared with control. No significant changes were observed in treated groups as compared to control in hematological parameters, biochemical parameters and lipid profile except SGOT, SGPT and alkaline phosphate in these parameters significant increase was observed. Significant changes were also observed in antioxidant analysis of treated groups as significant increase was observed in LPO and significant decrease in FRAP concentration was observed which signifies the results of histological changes especially in kidney and liver. Changes in histology of treated groups showed effect on kidney and liver as reduction (shrinkage) in glomerulus size and changes in histoarchitecture of central vein in liver of treated group was observed as compared to control group other histological examinations were normal. From results this can be concluded that long term low dose treatment of meloxicam has altered the histoarchitecture of liver and kidney of Gallus domesticus.

Characterization of leaf surface phenotypes based on light interaction

BackgroundLeaf surface phenotypes can indicate plant health and relate to a plant’s adaptations to environmental stresses. Identifying these phenotypes using non-invasive techniques can assist in high-throughput phenotyping and can improve decision making in plant breeding. Identification of these surface phenotypes can also assist in stress identification. Incorporating surface phenotypes into leaf optical modelling can lead to improved biochemical parameter retrieval and species identification.ResultsIn this paper, leaf surface phenotypes are characterized for 349 leaf samples based on polarized light reflectance measured at Brewster’s Angle, and microscopic observation. Four main leaf surface phenotypes (glossy wax, glaucous wax, high trichome density, and glabrous) were identified for the leaf samples. The microscopic and visual observations of the phenotypes were used as ground truth for comparison with the spectral classification. In addition to surface classification, the microscope images were used to assess cell size, shape, and cell cap aspect ratios; these surface attributes were not found to correlate significantly with spectral measurements obtained in this study. Using a quadratic discriminant analysis function, a series of 10,000 classifications were run with the data randomly split between training and testing datasets, with 150 and 199 samples, respectively. The average correct classification rate was 72.9% with a worst-case classification of 60.3%.ConclusionsLeaf surface phenotypes were successfully correlated with spectral measurements that can be obtained remotely. Remote identification of these surface phenotypes will improve leaf optical modelling and biochemical parameter estimations. Phenotyping of leaf surfaces can inform plant breeding decisions and assist with plant health monitoring.

Synthesis, in-Silico studies and biological evaluation of pyrimidine based thiazolidinedione derivatives as potential anti-diabetic agent

Despite the advancements in the management of Diabetes mellitus, the design and synthesis of drug molecule which ameliorates the hyperglycemia and associated secondary complications in diabetic patients, still remains a challenge. Herein, we report the synthesis, characterization and anti-diabetic evaluation of pyrimidine-thiazolidinedione derivatives. The synthesized compounds were characterized by 1H NMR, 13C NMR, FTIR and Mass Spectroscopic analytical techniques. The in-silico ADME studies depicted that the compounds were within the permissible limits of the Lipinski’s rule of five. The compounds 6e and 6m showing the best results in OGTT were evaluated for in-vivo anti-diabetic evaluation in STZ induced diabetic rats. Administration of 6e and 6m for four weeks decreased the blood glucose levels significantly. Compound 6e (4.5 mg/kg p.o.) was the most potent compound of the series. It reduced the level of blood glucose to 145.2 ± 1.35 compared to the standard Pioglitazone (150.2 ± 1.06). Moreover, the 6e and 6m treated group did not show increase in bodyweight. The biochemical estimations showed that the levels of ALT, ASP, ALP, urea, creatinine, blood urea nitrogen, total protein and LDH restored to normal in 6e and 6m treated groups as compared to STZ control group. The histopathological studies supported the results obtained in biochemical estimations. Both the compounds did not show any toxicity. Moreover, the histopathological studies of pancreas, liver, heart and kidney revealed that the structural integrity of these tissues restored to almost normal in 6e and 6m treated groups as compared to STZ control group. Based upon these findings it can be concluded that the pyrimidine-based thiazolidinedione derivatives represent novel anti-diabetic agents with least side effects.

Development and Evaluation of Some Molecular Hybrids of N-(1-Benzylpiperidin-4-yl)-2-((5-phenyl-1,3,4-oxadiazol-2-yl)thio) as Multifunctional Agents to Combat Alzheimer's Disease.

A series of some novel compounds (SD-1-17) were designed following a molecular hybridization approach, synthesized, and biologically tested for hAChE, hBChE, hBACE-1, and Aβ aggregation inhibition potential to improve cognition and memory functions associated with Alzheimer's disease. Compounds SD-4 and SD-6 have shown multifunctional inhibitory profiles against hAChE, hBChE, and hBACE-1 enzymes in vitro. Compounds SD-4 and SD-6 have also shown anti-Aβ aggregation potential in self- and acetylcholinesterase (AChE)-induced thioflavin T assay. Both compounds have shown a significant propidium iodide (PI) displacement from the cholinesterase-peripheral active site (ChE-PAS) region with excellent blood-brain barrier (BBB) permeability and devoid of neurotoxic liabilities. Compound SD-6 ameliorates cognition and memory functions in scopolamine- and Aβ-induced behavioral rat models of Alzheimer's disease (AD). Ex vivo biochemical estimation revealed a significant decrease in malonaldehyde (MDA) and AChE levels, while a substantial increase of superoxide dismutase (SOD), catalase, glutathione (GSH), and ACh levels is seen in the hippocampal brain homogenates. The histopathological examination of brain slices also revealed no sign of neuronal or any tissue damage in the SD-6-treated experimental animals. The in silico molecular docking results of compounds SD-4 and SD-6 showed their binding with hChE-catalytic anionic site (CAS), PAS, and the catalytic dyad residues of the hBACE-1 enzymes. A 100 ns molecular dynamic simulation study of both compounds with ChE and hBACE-1 enzymes also confirmed the ligand-protein complex's stability, while quikprop analysis suggested drug-like properties of the compounds.

Engineering of Lurasidone Hydrochloride Loaded Niosomes for Enhancing the Antipsychotic Potential for Nasal Administration

Background: Drugs having high first-pass metabolism or that are susceptible to enzymatic degradation can be administered through the nasal route to avoid their degradation. Lurasidone exhibits less toxicity and side effects as compared to its sister drugs like risperidone, ziprasidone, clozapine, etc. Objectives: The present study aimed to develop Lurasidone loaded niosomes for nasal delivery. Methods: Lurasidone niosomes were developed by adapting the ether injection method and optimized using a central composite design. In vitro and in vivo studies were conducted using optimized formulation. Results: The findings showed that the optimized formulation exhibited a particle size of 159.02 ± 0.58 nm and an entrapment efficiency of 91.6 ± 1.6%. The findings from the nasal histopathological analysis revealed that the optimized formulation was non-irritant and non-toxic for nasal mucosa. The findings from in vitro studies revealed 94.61 ± 0.27% of drug release from optimized formulation F7 throughout 24 hrs. The findings of in vivo (Albino Wistar rats) studies demonstrated that various pharmacokinetic parameters (Cmax, Tmax, AUC(0-24), T1/2, Vd and Cl) and pharmcodynamic parameters (conditioned avoidance response, biochemical estimation using oxidative markers such as superoxide dismutase, malondialdehyde and glutathione) were significantly improved compared to marketed tablets (Lurasid® 40 mg) and pure drug suspension. Optimized formulation F-7 exhibited 4.9 times more bioavailability than that of pure drug suspension following intranasal administration. Conclusion: These findings indicate that nasal niosomal formulation of Lurasidone HCl is a promising nanoplatform for enhancing the overall performance of Lurasidone. These results could open new avenues into the future of nanomedicine.