The purpose of the present study was to evaluate the in vivo efficacy of two cinnamic acid synthetic derivatives (allyl 3-[4-hydroxyphenyl]propanoate; HPP304, 1-naphthyl-methyl 3-[4-hydroxyphenyl]propanoate; HPP305) in high-cholesterol fed rats and compare their actions to that of cinnamic acid. Cinnamic acid and its synthetic derivatives were supplemented with a high-cholesterol diet for 42 days at a dose of 0.135 mmol/100g of diet. The supplementation of HPP304 and HPP305 significantly lowered cholesterol and triglyceride levels in the plasma and liver with a simultaneous increase in the HDL-cholesterol concentration, whereas cinnamic acid only lowered the plasma cholesterol concentration. Cinnamic acid lowered hepatic HMG-CoA reductase activity in high-cholesterol fed rats, however, its synthetic derivatives (HPP304 and HPP305) did not affect HMG-CoA reductase activity compared to the control group. Instead, the HPP304 and HPP305 supplements significantly lowered hepatic acyl coenzyme A:cholesterol acyltransferase activity and increased the fecal bile acid. The SOD activity of the erythrocytes and liver was not different between the groups, however, the activities of CAT and GSH-Px, and the level of GSH in the erythrocytes were significantly higher in the HPP304 and HPP305 groups than in the control group. On the other hand, the activities of CAT and GSH-Px, and the level of malondialdehyde in the liver were significantly lower in the HPP304 and HPP305 groups. The antioxidant activities of these cinnamic acid synthetic derivatives were similar to the cinnamic acid in the high-cholesterol fed rats. In addition, HPP304 and HPP305 lowered amniotransferase activity in the plasma. These results suggest that two cinnamic acid synthetic derivatives (HPP304 and HPP305) exert lipid-lowering action and antioxidant properties without hepatotoxicity in high-cholesterol fed rats.
"Several risk factors like hypercholesterolemia and cholesterol-induced oxidative stress enhance the formation of reactive oxygen species (ROS) which leads to the advancement of atherosclerotic lesions in vascular wall  . Studies have reported that elevated lipid level, like total cholesterol (TC), triglyceride (TG), and low density lipoprotein (LDL) cholesterol, and a decrease in high density lipoprotein (HDL) cholesterol are directly associated with hyperlipidemia and atherosclerosis . The cholesterol synthesis is regulated by í µí»½-hydroxy-í µí»½-methylglutaryl- CoA reductase (HMG-CoA reductase) (EC 18.104.22.168), "
[Show abstract][Hide abstract] ABSTRACT: Hypercholesterolemia-induced oxidative stress has been strongly implicated in the pathogenesis of atherosclerosis, which is one of the major causes of mortality worldwide. The current work, for the first time, accounts the antioxidant, genoprotective, antilipoperoxidative, and HMG-CoA reductase (EC 22.214.171.124) inhibitory properties of traditional medicinal plant, Ficus palmata Forsk. Our result showed that among sequentially extracted fractions of Ficus palmata Forsk, FPBA (F. palmata bark aqueous extract) and FPLM (F. palmata leaves methanolic extract) extracts have higher phenolic content and also exhibited significantly more radical scavenging (DPPH and Superoxide) and antioxidant (FRAP) capacity. Moreover, FPBA extract also exhibited significantly higher inhibition of lipid peroxidation assay. Additionally, results showed almost complete and partial protection of oxidatively damaged DNA by these plant extracts when compared to mannitol. Furthermore, our results showed that FPBA extract (IC50 = 9.1 ± 0.61 µg/mL) exhibited noteworthy inhibition of HMG-CoA reductase activity as compared to other extracts, which might suggest its role as cardioprotective agent. In conclusion, results showed that FPBA extract not only possess significant antioxidant and genoprotective property but also is able to attenuate the enzymatic activity of HMG-CoA reductase, which might suggest its role in combating various oxidative stress-related diseases, including atherosclerosis.
BioMed Research International 05/2014; 2014(1):762620. DOI:10.1155/2014/762620 · 3.17 Impact Factor
"CA are antioxidants  that lower platelet reactivity , and hence the prothrombotic state. In animal studies only, CA lowers cholesterol  (a feature shared with HMGA in humans) . The objective of the study was to test the hypothesis that flaxseed would safely combat the seven issues (i.e., reduce hyperglycaemia, dyslipidemia, hypertension, central obesity, inflammation, LDL oxidation, and the prothombotic state) thus potentially offering a means of reducing polypharmacy. "
[Show abstract][Hide abstract] ABSTRACT: Aim. Animal and human study evidence supports the hypothesis that flaxseed lignan complex (FLC) at a dose of 600 mg secoisolariciresinol diglucoside (SDG)/day for three months would combat hyperglycaemia, dyslipidemia, blood pressure, central obesity, prothrombotic state, inflammation, and low density lipoprotein (LDL) oxidation. Methods. Sixteen type 2 diabetic patients completed this double-blind, randomised crossover placebo-controlled study. A univariate repeated measures analysis of covariance (significance P < 0.05) was followed by a mixed linear model effects analysis corrected for multiple comparisons (MCC). Results. Prior to MCC, FLC caused decreased fasting plasma glucose, A1c, inflammation (c-reactive protein (CRP) and interleukin-6 (IL-6)), and increased bleeding time. After correction for multiple comparisons, FLC induced a statistically significant increase in bleeding time and smaller waist circumference gain. No treatment effect occurred in the other variables before or after adjustment. Conclusions. It is concluded that FLC significantly increased bleeding time thus reducing the prothrombotic state, reduced central obesity gain as measured by waist circumference, and did not affect significantly the other dependent variables measured after adjustment for multiple comparisons. These findings, not yet published in human type 2 diabetes, suggest that this FLC dose over at least three months, may, subject to further investigation, reduce polypharmacy.
Journal of nutrition and metabolism 10/2012; 2012(2):585170. DOI:10.1155/2012/585170
[Show abstract][Hide abstract] ABSTRACT: GuiZhiFuLing-Wan (GFW) has been used in China for centuries to improve blood stagnation. In this paper, a HPLC-DAD-MS/MS method was established for the efficient and rapid identification of the chemical constituents in extract of GuiZhiFuLing-Wan. Separation was performed on an Alltima C(18) analytical column by gradient elution with CH(3)CN/H(2)O-CH(3)COOH as mobile phase at a flow rate 1.0ml/min. 27 potentially bioactive compounds including monoterpene glycosides, galloyl glucoses, acetophenones, phenylallyl compounds and triterpenoids were identified or tentatively characterized by online ESI/MS/MS and the comparison with literature data and authentic compounds. After the identification, six different brands of GFW commercial products in various dosage forms were evaluated. The results demonstrated that capsule of GFW was superior to the other two dosage forms, honeyed pill and concentrated pill in administration. The points that should be paid more attention during the manufacturing process of GFW were also analyzed. The method can be the basis for the quality control of this commonly used herbal formula.
Journal of Pharmaceutical and Biomedical Analysis 12/2008; 49(2):267-75. DOI:10.1016/j.jpba.2008.11.012 · 2.98 Impact Factor
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