Cardiovascular & Hematological Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Cardiovascular & Hematological Agents) - Volume 17, Issue 1, 2019

Objectives: We performed a systematic review and meta-analysis to explore the risk of an aortic aneurysm or aortic dissection following fluoroquinolone administration. Methods: PubMed, Cochrane library, ClinicalTrials.gov, Embase and Google Scholar were systematically reviewed for controlled studies including adult patients exposed to fluoroquinolones with a primary outcome of aortic aneurysm or aortic dissection. Results: The meta-analysis was conducted by pooling the effect estimates of four controlled observational studies (one case-control, one case-crossover and two cohort studies). Fluoroquinolone administration more than doubled the risk to develop aortic aneurysm or aortic dissection within 60 days following fluoroquinolone exposure (adjusted Relative Risk [RR] (95% confidence interval [CI]) = 2.14 (1.93 - 2.36); I2 = 15.8%). The quality of the finding was rated as moderate. The risk increase for aortic aneurysm alone was found to be significant (adjusted RR (95% CI) = 2.23 (2.01 - 2.45); I2 = 0%) while the risk increase for aortic dissection alone was not found to be significant (adjusted RR = 1.88 (0.11 - 3.65); I2 = 74%). In subgroup analysis, the risk increase for aortic aneurysm or aortic dissection appeared to be higher in females compared to males (RR = 1.87 (1.24 - 2.51); I2 = 0% versus RR = 1.58 (1.25 - 1.92); I2 = 0%, respectively) and higher in older patients compared to younger patients (RR = 1.72 (1.37 - 2.07); I2 = 0% versus RR = 1.47 (0.91 - 2.04); I2 = 0%, respectively). Subgroup analysis of two studies which measured the duration-response analysis found that as the duration of fluoroquinolone therapy increased from 3 to 14 days to greater than 14 days, there was an increased risk of aortic aneurysm or dissection. Conclusion: The findings of this meta-analysis confirm the positive association between fluoroquinolones and the development of aortic aneurysm or dissection. The data tend to show that this association may be majorly driven by aortic aneurysm. Additionally, some risk factors appear to prevail including prolonged fluoroquinolone treatment and older age.

Artificial blood is an innovative concept of transfusion medicine where specifically designed compounds perform the task of transport and delivery of oxygen in the body to replace this function of allogenic human blood transfusion. Several molecules have been developed in the past few decades to achieve this objective and continous refinements are being continuously made in the quest of the ideal blood substitute. Currently, available technology manufactures artificial blood from haemoglobin obtained from outdated human/bovine blood (Haemoglobin Based Oxygen Carriers) or utilizing Perfluorocarbons. These synthetic blood substitutes are advantageous in that they do not require compatibility testing, are free from blood borne infections, have prolonged shelf life and do not require refrigeration. Artificial blood is projected to have a significant impact on the development of medical care in the future. It can complement the current blood products for transfusion and create a stable supply of safe and effective products. It is likely to reduce the requirements of blood transfusions drastically especially in settings of trauma and surgery thereby reducing the reliance on banked donated blood.

Chrysin is one of the flavonoids fruits, vegetables, and plant especially found in honey, it has been indicated that its cardiovascular protective effect is due to its antioxidative effects and antiinflammatory activities. Chrysin exerts an antioxidant effect by enhancing the antioxidant system, suppressing pro-oxidant enzymes, scavenging free radicals and chelating redox active transitionmetal ions. Chrysin decreases lipid synthesis and also increases its metabolism, thereby ameliorating blood lipid profile. Chrysin modulates vascular function by increasing the bioavailability of endothelial nitric oxide. Chrysin inhibits the development of atherosclerosis by decreasing vascular inflammation. The anti-inflammatory effects of chrysin may relate to its inhibitory effect on the nuclear transcriptional factor-kB signaling pathway. It also prevents vascular smooth muscle cells proliferation and thrombogenesis. Altogether, chrysin may be effective as a natural agent for the prevention and treatment of cardiovascular diseases; however, several clinical trial studies should be done to confirm its protective effects on humans.

Background and Objective: Warionia saharae Benth and Coss, is a medicinal plant used for its anti-diabetic properties in Morocco. This study was designed to examine the effect of the Flavonoid- Enriched Extract (FEE) obtained from Warionia saharae (W. saharae) on glucose and lipid metabolism in normal and streptozotocin (STZ)-induced diabetic rats. Methods: Acute (6 h) and sub-chronic (15 days) oral administration of FEE (10 mg/kg) was used to assess the glucose and lipid-lowering activity in normal and diabetic rats. Furthermore, glucose test tolerance, liver histopathological examination and in vitro antioxidant activity of FEE were carried out in this study. Results: Results indicated that FEE was able to exert antihyperglycemic activity. Additionally, FEE improved histopathological status of liver and pancreas in diabetic rats and possessed antioxidant activity. Conclusion: In conclusion, the present investigation revealed that FEE had potent antidiabetic effect in diabetic rats.

Objectives: Gliclazide (GL) is widely used to reduce hyperglycemia in diabetic patients. The aim of this study was to investigate the protective effect of GL against chromosome damage induced by ionizing radiation in human blood lymphocytes. Methods: In this experimental study, peripheral blood samples were collected from human volunteers and treated with GL at various concentrations (5, 25, 50 or 100 μM) for three hours. Then samples were irradiated to X-ray (1.5 Gy). Blood samples were cultured with mitogenic stimulation. The frequencies of micronuclei in cytokinesis-blocked binucleated lymphocytes were determined in the different samples. The antioxidant activities of GL were assayed by two different methods as 1,1- diphenyl-2-picryl hydrazyl radical (DPPH) free radical scavenging and reducing antioxidant power assays. Results: GL significantly reduced the percentage of micronuclei in lymphocytes which were irradiated. The maximum radioprotection in the reduction of percentage of micronuclei in lymphocytes was observed at 100 μM of GL with 52% efficacy. GL exhibited excellent free radical scavenging activity and reducing power at concentration dependent activities. The IC50 values of GL were lower than ascorbic acid. Higher potencies were observed in the antioxidant activities for GL than ascorbic acid in both methods. Conclusion: This data exhibits that GL is a powerful radioprotective agent that could protect healthy cells against the chromosome damage induced by ionizing radiation through antioxidant activity. The radioprotective effect is new indication of GL for patients' protection against side effect induced by ionizing radiation.

Objective: The evaluation of the hypolipidemic and antioxidant activities of the aerial parts aqueous extract of Corrigiola telephiifolia (APAE of C. telephiifolia) in normal and streptozotocin (STZ)-induced diabetic rats. Methods: The effects of oral administration of APAE of C. telephiifolia (5 mg/kg) on the lipid profile as well as the in vitro antioxidant activity of this aqueous extract have been determined. Results: APAE of C. telephiifolia (5 mg/kg) reduced significantly (p<0.001) the plasma total cholesterol levels in diabetic rats. In contrast, no significant increase in plasma triglyceride levels in normal and in STZ-induced diabetic rats was observed. On the other hand, APAE of C. telephiifolia showed an antioxidant activity. Conclusion: The APAE of C. telephiifolia exhibits an antioxidant, cholesterol and body weightlowering activities in diabetic rats.

Background: Dietary high fat possibly causes oxidative stress. Also, it alters the pathophysiology of metabolically active myocardial tissues and vascular architecture. Emblica officinalis contains a potential antioxidant that counteracts oxidative stress and possibly maintains vascular integrity. Objectives: To assess the effect of ethanolic extract of Emblica officinalis (EEO) on High Fat Diet (HFD) induced changes in vascular chemistry and histopathology of the cardiovascular system in male albino rats. Materials and Methods: Ethanolic extract of Emblica Officinalis (EEO) was prepared and phytochemical analysis was done. Rats were divided into four groups, having six rats in each group as follows: group 1- Control (20% fat); group 2 (20% fat+ EEO 100 mg/kg/b w); group 3 (30% fat) and group 4 (30% fat + EEO 100 mg/kg/b w). Dietary and EEO supplementation was continued for 21 days. Gravimetric and oxidative stress markers like MDA, NO, antioxidants like Vitamin C and E, and molecular marker (NOS3) were evaluated. Histopathological analysis was done on the myocardium and elastic artery along with measurement of coronary arterial wall thickness and lumen diameter. One way ANOVA was done for analysis of data. Results: High fat diet showed a significant increase in MDA, decrease of NO with unaltered NOS3 protein in rats fed with high fat diet, which indicate possible alteration of vascular pathophysiology. Supplementation of EEO showed an ameliorating effect on high fat diet induced oxidative stress. These results were further corroborated with findings of a histopathological study on the myocardium, elastic artery and coronary arterial architecture. Conclusion: Ethanolic extract of Emblica officinalis (EEO) indicates its cardioprotective efficacy against rats fed with high fat diet.

Introduction: Argania Spinosa L. (Sapotaceae) is an endemic species from south-western Morocco. This plant has many traditional uses including its use in the treatment of diabetes. Objective: The objective of the study was to evaluate the antidiabetic activity of Argania Spinosa Leaf Aqueous Extract (A.S.L.A.E). Methods: The antidiabetic effect of A.S.L.A.E was evaluated in both normal and streptozotocin (STZ)-induced diabetic rats treated at a dose of 20 mg/kg body weight for 15 days. The histopathological changes in the liver were evaluated. In addition, the antioxidant activity of this extract was also studied. Results: Single oral administration of A.S.L.A.E (20 mg/kg) showed no significant change in blood glucose levels in both normal and STZ induced diabetic rats after 6 hours of administration. Furthermore, in normal rats, repeated oral administration of A.S.L.A.E reduced blood glucose levels. Moreover, blood glucose levels decreased in STZ diabetic rats after fifteen days of treatment. According to the oral glucose tolerance test, the A.S.L.A.E (20 mg/kg) was shown to prevent significantly the increase in blood glucose levels in normal treated rats. Moreover, A.S.L.A.E showed antioxidant activity. Conclusion: The results show that Argania spinosa leaf aqueous extract possesses significant antihyperglycemic activity.