Effect of flaxseed supplementation and exercise training on lipid profile, oxidative stress and inflammation in rats with myocardial ischemia.

BACKGROUND: Flaxseed has recently gained attention in the area of cardiovascular disease primarily because of its rich contents of α-linolenic acid (ALA), lignans, and fiber. Although the benefits of exercise on any single risk factor are unquestionable, the effect of exercise on overall cardiovascular risk, when combined with other lifestyle modifications such as proper nutrition, can be dramatic.This study was carried out to evaluate the protective role of flaxseed and exercise on cardiac markers, lipids profile and inflammatory markers in isoproterenol (ISO)-induced myocardial ischemia in rats. METHODS: The research was conducted on 40 male albino rats, divided into 4 groups (n=10): group I served as control, group II has acute myocardial ischemia induced by isoproterenol, groups III and IV have acute myocardial ischemia induced by isoproterenol pretreated with flaxseed supplementation orally for 6 weeks, additionally group IV practiced muscular exercise through swimming. RESULTS: Alterations of lipid profile, cardiac and inflammatory markers (Il-1ß, PTX 3 and TNF- α) were observed in myocardial ischemia group. Flaxseed supplementation combined with exercise training showed significant increase of HDL and PON 1, on the other hand cardiac troponin, Il- 1ß and TNF- α levels significantly decreased as compared to myocardial ischemic group. Receiver Operating Characteristics (ROC) analysis of cTnI, PTX 3, Il-1ß and TNF- α revealed a satisfactory level of sensitivity and specificity. CONCLUSION: Regular exercise enhances the improvement in plasma lipoprotein levels and cardiovascular protection that results from flaxseed supplementation by mitigating the pathophysiology of atherosclerosis. Elevation of HDL, the antioxidant PON 1 and the cardioprotective marker PTX 3 emphasizes the protective effects of flaxseed and muscular exercise mutually against the harmful effects of acute myocardial ischemia.

Synthesis of some novel benzoxazole derivatives as anticancer, anti-HIV-1 and antimicrobial agents.

In an effort to establish new candidates with improved antineoplastic, anti-HIV-1 and antimicrobial activities we report here the synthesis and in vitro biological evaluation of various series of 2-substituted benzoxazoles: 2-[(Arylhydrazono, arylidene, cycloalkylidene and N-substituted thiocarbamoyl)cyanomethyl]-benzoxazoles(2-4 and 7, respectively); 2-[(4- or 5-oxothiazoliden-2-yliden)benzoxazoles (5 and 6) and 2-(4-amino-3-substituted-2-thioxo-2,3-dihydrothiazol-5-yl)benzoxazoles (8), together with the synthesis of some substituted 3H-pyrido[2,1-b]benzoxazoles (9-11). The absolute configuration of compound 3b was determined by X-ray crystallography. The results of the in vitro anticancer screening revealed that some of the tested compounds exhibited broad spectrum antitumor activity. The most active compounds are 2a, 3b, 8a and 8d, their GI50 MG-MID values: 37.7, 19.1, 20.0 and 15.8 microM; TGI MG-MID values: 75.9, 53.7, 53.7, and 58.9 microM; and LC50 MG-MID values: 97.7, 93.3, 89.1 and 93.3 microM, respectively. The in vitro microbiological data showed that compound 7c was the most active against Staphylococcus aureus (minimal inhibitory concentration (MIC)<12.5 microg ml(-1). While compounds 5, 8a, and 8d were the most active against Bacillus subtilis (MIC values<12.5 microg ml(-1)). On the other hand, compounds 5 and 7c were the most active against Escherichia coli (MIC<25 microg ml(-1)), their activity is about half the activity of ampicillin and streptomycin . In addition, compound 4b and 7c were the most active against Pseudomonas aeruginosa (MIC<25, 50 microg ml(-1)). Compound 4b was two times as active as ampicillin and streptomycin while compound 7c was active as both. The results of antimycotic activity indicated that, Compound 7c showed mild activity against Candida albicans when compared with clotrimazole (MIC<100 microg ml(-1)). In vitro HIV-1 testing revealed that compound 7a displayed moderate anti-HIV-1 activity (maximum % cell protection, 36.6 at 2 x 10(-5) microM).

Polysubstituted pyrazoles, part 5. Synthesis of new 1-(4-chlorophenyl)-4-hydroxy-1H-pyrazole-3-carboxylic acid hydrazide analogs and some derived ring systems. A novel class of potential antitumor and anti-HCV agents.

A novel series of 1-(4-chlorophenyl)-4-hydroxy-1H-pyrazole-3-carboxylic acid hydrazide analogs and some derived 4-substituted-1,2,4-triazolin-3-thiones, 2-substituted-1,3,4-thiadiazole and 2-substituted-1,3,4-oxadiazoles has been synthesized. Ten of the newly synthesized compounds were selected by the National Cancer Institute (NCI)-in vitro-disease oriented antitumor screening to be evaluated for their antitumor activity. Seven compounds, namely 7a-c, 9, 11, 13 and 14, exhibited potential and broad spectrum antitumor activity against most of the tested subpanel tumour cell lines (GI50<100 microM). Compounds 14 (GI50, TGI, and LC50 MG-MID values of 0.08, 15.8 and 64.6 microM, respectively) and 11 (GI50, TGI, and LC50 MG-MID values of 0.20, 11.7 and 87.1 microM, respectively) proved to be the most active members in this study with potential activity against all the tested subpanel tumour cell lines and particular effectiveness on the leukaemia subpanel at both the GI50 (0.03 and 0.09 microM, respectively) and the TGI levels (35.2 and 28.1 microM, respectively). Moreover, compound 14 exhibited a super sensitivity profile towards about 26 different cancer cell lines with GI50 values lying in the nanomolar concentration range (GI50 values<0.01 microM). In addition, compounds 2-5, 6a-d, 7a, 8-11, 12a, 13, 14 were investigated for their in vitro effect on the replication of hepatitis-C virus (HCV) in HepG2 hepatocellular carcinoma cell line infected with the virus using the reverse transcription-polymerase chain reaction (RT-PCR) technique. The results revealed that compounds 2 and 5 were capable of inhibiting the replication of both the HCV RNA (+) and (-) strands at 10-100 microg mL(-1) concentration range.