scholarly journals Radiological Pharmacology Drugs: Therapeutic Potential of Melatonin

2020 ◽  
pp. 35-39
Author(s):  
N. Kolotilov
Keyword(s):  
Pain Sensitivity ◽  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Reproductive Function ◽  
Calcium Content ◽  
Off Label ◽  
Dose Dependent ◽  
Label Strategy ◽  
Neuroendocrine Functions ◽  
Basic Medical

The purpose of the article is to draw attention to Melatonin as a means of radiological pharmacology within the framework of drugs’ reprofiling [13] and the “off-label” strategy (application for medical purposes does not correspond to the instructions for the basic medical use of the drug). Melatonin has, to varying degrees, a dose-dependent antistressor, sedative, hypnogenic, neuroprotective, geroprotective (a general consistent pattern for all geroprotectors – earlier initiation of drug use provides a greater effect), antidepressant, antioxidant, antitumor, antiapoptotic (in normal cells), proapoptotic (in cancer cells), oncostatic, antimetastatic, immunomodulatory, radioprotective, radiosensitizing, anti-infectious, analgesic, hepatoprotective geroprotective, antihypertensive, anti-inflammatory, moderate contraceptive (for women) action. Melatonin regulates neuroendocrine functions, respiratory rate, reproductive function, osteogenic differentiation of mesenchymal stem cells, formation and protection of bones; modulates the activity of bone-forming osteoblasts and bone-resorbing osteoclasts; reduces pain sensitivity; affects the intracellular calcium content. The antioxidant properties of Melatonin are closely related to its antitumor effect. Studies have demonstrated that melatonin has a self-sufficient oncostatic effect in cancer of the breast, ovaries, endometrium, pancreas, prostate, lungs; melanoma, hepatocellular carcinoma, colorectal cancer, glioblastoma, and leiomyosarcoma. Key words: pineal gland, melatonin, radioprotector, radiological pharmacology.

Estimation of total phenolics and flavonoidal contents as well as in vitro antioxidant potential of Apium leptophyllum Pers.

2013 ◽  
Vol 59 (3) ◽  
pp. 37-50 ◽  
Author(s):  
Bhusan Sahoo Himanshu ◽  
Subrat Kumar Bhattamisra ◽  
Uttam Kumar Biswas ◽  
Rakesh Sagar
Keyword(s):  
Nitric Oxide ◽  
Methanolic Extract ◽  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
The Body ◽  
Total Phenolic ◽  
Dependent Manner ◽  
Pharmaceutical Industries ◽  
Dose Dependent

Abstract At present, major causes of diseases is oxidative stress affecting both metabolic and physiological functions of the body. That is why there is a great need for investigation of nutritious food supplements for counteracting these oxidative stresses. Therefore, the aim of study was to evaluate the therapeutic potential of Apium leptophyllum Pers. fruits by estimating total phenolic as well as flavonoidal contents and antioxidant values. The collected fruits were extracted separately using different solvents like methanol, ethanol and water. Total phenolic and flavonoid contents were measured from the respective extracts and correlated with their antioxidant values. The antioxidant properties of various fruit extracts (12.5, 25, 50, 100 and 150 μg/ml) were evaluated by DPPH, hydroxyl, nitric oxide and superoxide scavenging assay and compared with ascorbic acid as a standard. All the extracts of A. leptophyllum were found to be dose dependent inhibition against these free radicals. Among all these extracts, the methanolic one was found better in the scavenging activity and followed dose-dependent manner against DPPH, hydroxyl radical, nitric oxide, superoxide anions with minimum IC50 values of 97.9, 89.02, 135.37, 127.73 μg/ml, respectively, and also observed more significant (p<0.01) as compared with standard Furthermore, total phenolic and flavonoidal contents were found highest in methanolic extract. The results obtained in this study clearly indicate that the methanolic extract of A. leptophyllum may be used as a new potential source of natural nutritional supplement in food or pharmaceutical industries due to rich source of phenolic, flavonoidal contents as well as antioxidant property

Anticoagulant Activity of Hirulog™, a Direct Thrombin Inhibitor, in Humans

1993 ◽  
Vol 69 (02) ◽  
pp. 157-163 ◽  
Author(s):  
Irving Fox ◽  
Adrian Dawson ◽  
Peter Loynds ◽  
Jane Eisner ◽  
Kathleen Findlen ◽  
...  
Keyword(s):  
Rational Design ◽  
Therapeutic Potential ◽  
Anticoagulant Activity ◽  
Subcutaneous Administration ◽  
Direct Thrombin Inhibitor ◽  
Controlled Study ◽  
Thrombin Inhibitor ◽  
Thrombin Time ◽  
Thrombotic Disease ◽  
Dose Dependent

SummaryHirulog™ (BG8967) is a direct thrombin inhibitor built by rational design using the protein hirudin as a model (Maraganore et al. [1990]; Biochemistry 29: 7095–101). In order to evaluate the therapeutic potential for hirulog in the management of thrombotic disease, the tolerability and anticoagulant activity of the agent were examined in a study of human volunteers.In a randomized, placebo-controlled study (n = 54), the intravenous infusion of hirulog over 15 min showed a rapid, dose-dependent prolongation of activated partial thromboplastin time (APTT), prothrombin time (PT), and thrombin time (TT). There was a corresponding dose-dependent increase in plasma hirulog levels. The peptide was rapidly cleared with a half-life of 36 min and a total body clearance rate for the peptide of 0.43 1 kg−1 h−1. Similar activity was observed following subcutaneous injection but with sustained pharmacodynamic and pharmacokinetic behavior. There was a significant correlation between pharmacokinetic and pharmacodynamic variables for both intravenous (r = 0.8, p <0.001) and subcutaneous administration (r = 0.7, p = 0.002).To evaluate the possible interactions of aspirin on the tolerability and anticoagulant activity of intravenous hirulog, a cross-over design was employed in eight subjects. Aspirin administration did not modify the peptide’s activity. At the administered dose of 0.6 mg kg−1 h−1 for 2 h, hirulog infusion prolonged APTT from 230 to 260% baseline. The infusion of hirulog in subjects who had received aspirin was not associated with any significant changes in the template bleeding time.The final phase of the study examined the activity and tolerability of hirulog in ten subjects during prolonged intravenous infusions for up to 24 h. The peptide (0.3 mg kg−1 h−1) exhibited sustained anticoagulant activity with no evidence for a cumulative effect. During hirulog infusion, APTT was prolonged from 210 to 250% baseline.In all phases of the study, hirulog administration was generally well-tolerated.Our observations show that hirulog is an active antithrombin agent with excellent tolerability in humans. As a direct thrombin inhibitor, hirulog provides a novel approach for the management of thrombotic disease.

Evaluation of diuretic and antioxidant properties in aqueous bark and fruit extracts of pine

2020 ◽  
Vol 17 ◽  
Author(s):  
Hadi Shariati ◽  
Mohammad Hassanpour ◽  
Gholamreza Sharifzadeh ◽  
Asghar Zarban ◽  
Saeed Samarghandian ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Phenolic Content ◽  
Antioxidant Properties ◽  
Pine Bark ◽  
Male Rats ◽  
Total Phenolic ◽  
Dependent Manner ◽  
Aqueous Extracts ◽  
Antioxidant Power ◽  
Dose Dependent

Objective: The present study has been carried out to evaluate the diuretic and antioxidant properties of pine herb in an animal model. Materials and Methods: 45 adult male rats were randomly divided into nine groups including: groups I (the negative control), groups II (positive control, furosemide 10 mg/kg), groups III to VIII (treatment groups received 100, 200, 400 mg/kg of the aqueous extracts of bark and fruit) and group IX received the combination of aqueous extract of bark (100 mg/kg) and the fruit (100 mg/kg). The urine output, glomerular filtration rate (GFR), electrolytes, urea, and creatinine levels were evaluated . Furthermore, the phenolic content and antioxidant activity of both extracts were also assessed using 2, 2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP) and Folin–Ciocalteu methods. Results: The aqueous extracts of the pine bark and fruit increased the urinary output in a dose-dependent manner. The combination of the two extracts compared to the other extracts alone significantly increased the serum potassium level. This study also showed each extract increase creatinine clearance in a dose-dependent manner (p<0.01 and p<0.05). The increase of GFR in the combination group was not significant. The current data showed a significant increase in the total phenolic content in pine bark extract in compared with the fruit extract. Conclusion: The pine bark and fruit can be useful in the prevention and treatment of kidney stones due to the high antioxidant activity.

β-1, 3-Glucan attenuated chronic unpredictable mild stress induced cognitive impairment in rodents via normalizing corticosterone levels

2020 ◽  
Vol 20 ◽  
Author(s):  
Saniya Hashim Khan ◽  
Sheraz Khan ◽  
Inamullah Khan ◽  
Narmeen Hashim
Keyword(s):  
Water Maze ◽  
Memory Impairment ◽  
Glucocorticoid Receptors ◽  
Therapeutic Potential ◽  
Mild Stress ◽  
Chronic Unpredictable Mild Stress ◽  
Neuroprotective Effects ◽  
Injurious Effect ◽  
Naturally Occurring ◽  
Dose Dependent

Background: Chronic stress elevates the cortisol beyond normal levels, which affects cognition including learning & memory. This injurious effect is primarily mediated via over excitation of metabotropic glucocorticoid receptors (mGR). Methods: The present study was aimed appraise the neuroprotective effects of naturally occurring molecule β-1,3-glucan by interfering with stress-cortisol-mGR axis. Our data of virtual screening (in silico) exhibited the promising interactions of βglucan with the mGR. Therefore, the study was extended to evaluate its efficacy (2.5, 5 and 10 mg/kg/ i.p) in an animal model of chronic unpredictable mild stress (CUMS, 28 days) induced memory impairment. Results: Results of the current study revealed the β-glucan provided dose dependent protection against deleterious effects of stress on learning and memory associated parameters observed in Morris water maze (MWM) task. At higher tested doses, it has also significantly antagonized the stress induced weight loss and corticosterone elevation. Conclusion: From these findings, it can be deduced that the β-glucan possesses therapeutic potential against stress induced memory impairment, and this effect can be attributed to its normalizing effect on corticosterone levels.

Structurally Related Edaravone Analogues: Synthesis, Antiradical, Antioxidant, and Copper-Chelating Properties

2020 ◽  
Vol 18 (10) ◽  
pp. 779-790 ◽  
Author(s):  
Alexandre LeBlanc ◽  
Miroslava Cuperlovic-Culf ◽  
Pier Jr. Morin ◽  
Mohamed Touaibia
Keyword(s):  
Oxidative Stress ◽  
Amyotrophic Lateral Sclerosis ◽  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Therapeutic Options ◽  
Partial Charge ◽  
Associated Diseases ◽  
Significant Interest ◽  
Lateral Sclerosis

Background:: The current therapeutic options available to patients diagnosed with Amyotrophic Lateral Sclerosis (ALS) are limited and edaravone is a compound that has gained significant interest for its therapeutic potential in this condition. Objectives: : The current work was thus undertaken to synthesize and characterize a series of edaravone analogues. Methods: A total of 17 analogues were synthesized and characterized for their antioxidant properties, radical scavenging potential and copper-chelating capabilities. Results: Radical scavenging and copper-chelating properties were notably observed for edaravone. Analogues bearing hydrogen in position 1 and a phenyl at position 3 and a phenyl in both positions of pyrazol-5 (4H)-one displayed substantial radical scavenging, antioxidants and copper-chelating properties. High accessibility of electronegative groups combined with higher electronegativity and partial charge of the carbonyl moiety in edaravone might explain the observed difference in the activity of edaravone relative to the closely related analogues 6 and 7 bearing hydrogen at position 1 and a phenyl at position 3 (6) and a phenyl in both positions (7). Conclusion: Overall, this study reveals a subset of edaravone analogues with interesting properties. Further investigation of these compounds is foreseen in relevant models of oxidative stress-associated diseases in order to assess their therapeutic potential in such conditions.

scholarly journals Flavonoids from the Genus Euphorbia: Isolation, Structure, Pharmacological Activities and Structure–Activity Relationships

2021 ◽  
Vol 14 (5) ◽  
pp. 428
Author(s):  
Douglas Kemboi Magozwi ◽  
Mmabatho Dinala ◽  
Nthabiseng Mokwana ◽  
Xavier Siwe-Noundou ◽  
Rui W. M. Krause ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Structure Activity Relationship ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Skeletal Structure ◽  
Activity Relationship ◽  
Hydroxyl Groups ◽  
Structure Activity ◽  
Review Reports

Plants of the genus Euphorbia are widely distributed across temperate, tropical and subtropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure–activity relationship of Euphorbia flavonoids for the period covering 2000–2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells. Of the investigated species, over 80 different types of flavonoids have been isolated to date. Most of the isolated flavonoids were flavonols and comprised simple O-substitution patterns, C-methylation and prenylation. Others had a glycoside, glycosidic linkages and a carbohydrate attached at either C-3 or C-7, and were designated as d-glucose, l-rhamnose or glucorhamnose. The structure–activity relationship studies showed that methylation of the hydroxyl groups on C-3 or C-7 reduces the activities while glycosylation loses the activity and that the parent skeletal structure is essential in retaining the activity. These constituents can therefore offer potential alternative scaffolds towards development of new Euphorbia-based therapeutic agents.

scholarly journals Biological Properties and Prospects for the Application of Eugenol—A Review

2021 ◽  
Vol 22 (7) ◽  
pp. 3671
Author(s):  
Magdalena Ulanowska ◽  
Beata Olas
Keyword(s):  
Body Weight ◽  
Aromatic Compound ◽  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Biological Properties ◽  
Clove Oil ◽  
Current State ◽  
Potential Component ◽  
Anti Inflammatory ◽  
High Concentrations

Eugenol is a phenolic aromatic compound obtained mainly from clove oil. Due to its known antibacterial, antiviral, antifungal, anticancer, anti-inflammatory and antioxidant properties, it has long been used in various areas, such as cosmetology, medicine, and pharmacology. However, high concentrations can be toxic. A dose of 2.5 mg/kg body weight is regarded as safe. This paper reviews the current state of knowledge regarding the activities and application of eugenol and its derivatives and recent research of these compounds. This review is based on information concerning eugenol characteristics and recent research from articles in PubMed. Eugenol remains of great interest to researchers, since its multidirectional action allows it to be a potential component of drugs and other products with therapeutic potential against a range of diseases.

scholarly journals In Vitro Evaluation of the Anti-Inflammatory Effect of KMUP-1 and in Vivo Analysis of Its Therapeutic Potential in Osteoarthritis

Biomedicines ◽  
2021 ◽  
Vol 9 (6) ◽  
pp. 615
Author(s):  
Shang-En Huang ◽  
Erna Sulistyowati ◽  
Yu-Ying Chao ◽  
Bin-Nan Wu ◽  
Zen-Kong Dai ◽  
...  
Keyword(s):  
Articular Cartilage ◽  
Inflammatory Responses ◽  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Serum Levels ◽  
Gene Expressions ◽  
Tnf Α ◽  
Anti Inflammatory

Osteoarthritis is a degenerative arthropathy that is mainly characterized by dysregulation of inflammatory responses. KMUP-1, a derived chemical synthetic of xanthine, has been shown to have anti-inflammatory and antioxidant properties. Here, we aimed to investigate the in vitro anti-inflammatory and in vivo anti-osteoarthritis effects of KMUP-1. Protein and gene expressions of inflammation markers were determined by ELISA, Western blotting and microarray, respectively. RAW264.7 mouse macrophages were cultured and pretreated with KMUP-1 (1, 5, 10 μM). The productions of TNF-α, IL-6, MMP-2 and MMP- 9 were reduced by KMUP-1 pretreatment in LPS-induced inflammation of RAW264.7 cells. The expressions of iNOS, TNF-α, COX-2, MMP-2 and MMP-9 were also inhibited by KMUP-1 pretreatment. The gene expression levels of TNF and COX families were also downregulated. In addition, KMUP-1 suppressed the activations of ERK, JNK and p38 as well as phosphorylation of IκBα/NF-κB signaling pathways. Furthermore, SIRT1 inhibitor attenuated the inhibitory effect of KMUP-1 in LPS-induced NF-κB activation. In vivo study showed that KMUP-1 reduced mechanical hyperalgesia in monoiodoacetic acid (MIA)-induced rats OA. Additionally, KMUP-1 pretreatment reduced the serum levels of TNF-α and IL-6 in MIA-injected rats. Moreover, macroscopic and histological observation showed that KMUP-1 reduced articular cartilage erosion in rats. Our results demonstrated that KMUP-1 inhibited the inflammatory responses and restored SIRT1 in vitro, alleviated joint-related pain and cartilage destruction in vivo. Taken together, KMUP-1 has the potential to improve MIA-induced articular cartilage degradation by inhibiting the levels and expression of inflammatory mediators suggesting that KMUP-1 might be a potential therapeutic agent for OA.

Abstract 619: Alpha Keto Acids Decompose Peroxides and Prevents Oxidation of Lipoproteins

2016 ◽  
Vol 36 (suppl_1) ◽  
Author(s):  
Chandrakala Aluganti Narasimhulu ◽  
Kathryn Young Burge ◽  
Yu Yuan ◽  
Sampath Parthasarathy
Keyword(s):  
Therapeutic Potential ◽  
Lipid Peroxides ◽  
Enzymatic Oxidation ◽  
Raw 264.7 Cells ◽  
Dependent Manner ◽  
Gene Expressions ◽  
Dual Effect ◽  
Keto Acids ◽  
Hydroperoxyoctadecadienoic Acid ◽  
Dose Dependent

Background: Alpha keto acids are unstable and decompose rapidly. In this study, we tested the ability of alpha keto acids to reduce peroxides and inhibit oxidation of lipoproteins. Methods: Keto salicylic acid (KSA) and Keto Octanoicacid (KoA) were synthesized and their ability to reduce hydrogen peroxides as well as lipid peroxides (LOOH) was measured using 13-hydroperoxyoctadecadienoic acid (13-HPODE). Lipoproteins (LDL and HDL) were isolated from human plasma and oxidation of liporproteins was performed using copper and MPO in the presence or absence of the keto compounds. RAW 264.7 cells and HUVECS were incubated with LPS and mm-LDL respectively either in the presence or absence of the keto compounds. RNA was isolated from treated cells and real time PCR was performed to analyze IL-1α, IL-6, MCP-1 and VCAM1 gene expressions. Reactive oxygen species were evaluated using DCF fluorescence in presence and absence of the keto compounds. Results: KSA reduced both H2O2 and 13-HPODE whereas KoA is able to reduce the former but not the latter. Both compounds inhibited the lipoprotein oxidation in a dose dependent manner and were able to reduce ROS production by H2O2. KSA is able to inhibit both LPS as well as mm-LDL induced inflammation. However, KoA showed a dual effect as it induced inflammatory markers in the presence of LPS, but inhibited the mm-LDL-induced inflammatory gene expressions. Conclusion: The results of our studies suggest that these keto compounds a) inhibit both enzymatic and non enzymatic oxidation of lipoproteins; b) reduce peroxides and ROS and c) have inhibitory and inducing effect on inflammatory cytokine/gene production in presence of mm-LDL and LPS respectively. Based on these results, we predict that these keto compounds could have therapeutic potential in reducing CVD/atherosclerosis-associated inflammation.

scholarly journals Assessment of the Anti-apoptotic Effects of Peganum harmala Leaf Extract on Type 2 Diabetes in the Kidney of Male Wistar Rats

2020 ◽  
Vol 8 (2) ◽  
pp. 74-82
Author(s):  
Forough Kajbaf ◽  
Shahrbanoo Oryan ◽  
Ramesh Ahmadi ◽  
Akram Eidi
Keyword(s):  
Wistar Rats ◽  
Leaf Extract ◽  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Diabetic Control ◽  
Albumin Level ◽  
Lower Percentage ◽  
Peganum Harmala ◽  
Diabetic Kidney ◽  
Male Wistar Rats

Background: Growing evidence has shown that the apoptosis of cells plays an important role in the advancement of the Diabetic nephropathy (DN). Objectives: This study attempted to discover the therapeutic potential of Peganum harmala leaf extract in the apoptosis of diabetic kidney disease. Methods: In the present experimental research, 32 male Wistar rats were studied, and diabetes was induced by streptozotocin (STZ) (65 mg/kg). The animals were randomly divided into four groups (n=8, in each group) as follows: control, diabetic, control+leaf extract, diabetic+leaf extract. For our purposes, the methanolic extract of P. harmala leaves (150 mg/kg) was given by gavage for 28 days. Flow cytometry and real-time polymerase chain reaction (PCR) analyses were utilized to determine the percentages of apoptotic cells. Also, histological alterations and blood biochemical parameters were evaluated. Results: The P. harmala leaf extract has a high amount of flavonoids (25.84%), a lower percentage of alkaloids (0.14%), and some antioxidant properties. Serum urea (P<0.001) and apoptosis (P<0.05) significantly elevated in diabetic rats relative to the control ones. The mean of fasting blood creatinine, urea, and albumin level was not significantly changed in diabetic+leaf extract rats as compared to the diabetic ones. Histopathological results also displayed that diabetic complications in the kidney could not be improved following treatment by the leaf extract of P. harmala. In addition, the leaf extract could not significantly reduce the apoptosis and caspase-3 expression compared to diabetics in renal cells. Conclusion: Based on our findings, the leaf extract of P. harmala is unable to inhibit apoptosis in the diabetic kidney model.

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