| For medical practitioners and the general public - Cholesterol Journal Article Catalog. |
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| Hypocholesterolaemic effects of an ethanol precipitate of Kabosu juice in stroke-prone spontaneously hypertensive rats fed a cholesterol-free diet Ogawa, H. and S. Mochizuki (2003), Clin Exp Pharmacol Physiol 30(8): 532-6. Abstract: 1. We have previously identified strong inhibitory effects of Kabosu (Citrus sphaerocarpa Hort.) juice precipitate (KJP) on cholesterol elevation in stroke-prone spontaneously hypertensive rats (SHRSP) fed a cholesterol diet. In the present study, to elucidate the hypocholesterolaemic mechanism, we examined the effect of dietary KJP on lipid metabolism by using SHRSP fed a cholesterol-free diet. 2. Compositions of the experimental diet containing 10% KJP powder were adjusted to those of the control diet. Seven-week-old male SHRSP were fed control or experimental diet for 2 weeks with free access to the diet and water. 3. Serum levels of cholesterol, phospholipid and triglyceride of the KJP group were significantly reduced, which was due to decreases in the very low-density lipoprotein (VLDL), low-density lipoprotein (LDL) and high-density lipoprotein (HDL) fractions. 4. Serum concentrations of apolipoproteins A-I and E (apoA-I and E) of the KJP group were significantly lower than those of the control group, whereas no significant differences were observed in serum apoB and apoA-IV between the two groups. 5. In liver, there were no significant differences in the contents of lipids or relative liver weight between the two groups. The activity of microsomal cholesterol 7alpha-hydroxylase of the KJP group tended to increase, whereas that of microsomal acyl-coenzyme A: cholesterol acyltransferase was significantly reduced, compared with the control group. 6. These results indicate that dietary KJP produces reductions of serum lipid levels, which are due to reductions in VLDL, apoE HDL and apoA-I HDL, and may promote catabolism and excretion of hepatic cholesterol in SHRSP fed a cholesterol-free diet. |
| Hypocholesterolemic action and prevention of cholesterol absorption via the gut by F-1394, a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, in cholesterol diet-fed rats Kusunoki, J., K. Aragane, et al. (1995), Jpn J Pharmacol 69(1): 53-60. Abstract: In the present study, we investigated the hypocholesterolemic effect of F-1394 ((1s,2s)-2-3-(2,2-dimethylpropyl)-3-nonylureidoaminocycloh exane-1-yl 3-N-(2,2,5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino propionate), a potent and selective inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), and the effect on cholesterol absorption via the gut in rats fed a 1% cholesterol diet. Single administration of F-1394 to the cholesterol diet-fed rats at the doses of 3-30 mg/kg, p.o. decreased the serum cholesterol levels by 16-54% 3 hr after the administration. The ACAT activity in the small intestinal mucosa of the rats given orally F-1394 (30 mg/kg) was significantly inhibited 3 hr after the administration. The hypocholesterolemic action of F-1394 had a faster onset than that of DL-melinamide or CL-277,083. The study by the dual isotope ratio method showed that F-1394 (30 mg/kg, p.o.) significantly suppressed the dietary cholesterol absorption. Furthermore, in the determination of cholesterol absorption by using 14C-cholesterol as the oral tracer, the administration of F-1394 (30 mg/kg, p.o.) 1 or 2 hr before or immediately after the application of the oral tracer significantly prevented the appearance of the radioactivity in the circulation by around 90%. These results indicate that oral administration of F-1394 inhibits the ACAT activity in the small intestinal mucosa and subsequently contributes much to the prevention of cholesterol absorption via the gut, resulting in the decrease in serum cholesterol levels in the cholesterol diet-fed rats. Furthermore, the effect of F-1394 appears immediately after its administration in contrast to that of DL-melinamide or CL-277,082. |
| Hypocholesterolemic action of beta-cyclodextrin and its effects on cholesterol metabolism in pigs fed a cholesterol-enriched diet Ferezou, J., M. Riottot, et al. (1997), J Lipid Res 38(1): 86-100. Abstract: To examine the effects of beta-cyclodextrin (BCD), a non-absorbable carbohydrate, on lipid metabolism, growing pigs were fed a 0.3% cholesterol-enriched diet for 4 weeks or this diet containing 5% or 10% BCD. Pigs fed a basal diet without added cholesterol or BCD were used as controls. The cholesterol-rich diet induced hypercholesterolemia (1.75 vs. 0.84 g/l plasma) due to increased LDL concentration, delayed the plasma clearance of vitamin A, enhanced liver cholesterol storage, lowered the hepatic activities of LDL-receptors (by 47%) and HMG-CoA reductase (by 62%), stimulated cholesterol 7alpha-hydroxylase (x3), and accelerated the fecal output of neutral sterols (x4). Addition of BCD to the cholesterol-rich diet prevented the elevation of plasma cholesterol due to dietary cholesterol excess. Moreover, BCD produced a dose-dependent effect in reducing liver cholesterol storage, stimulating hepatic cholesterogenesis, increasing the proportion of primary bile acids in bile and in feces, and the fecal loss of neutral sterols and bile acids. Pigs receiving 10% BCD thus differed markedly from controls, especially for HMG-CoA reductase and cholesterol 7alpha-hydroxylase hepatic activities (x5), and fecal output of total bile acids (x3) and hyocholic acid (x20), and their overall cholesterol synthesis was higher (+50%), despite the abundant dietary cholesterol. Owing to the property of BCD to bind cholesterol and bile acids in vitro, these results suggest that this resistant carbohydrate accelerates body cholesterol turnover by reducing cholesterol absorption, increasing cholesterol and bile acid synthesis, and altering the action of the intestinal microflora. |
| Hypocholesterolemic actions of atorvastatin are associated with alterations on hepatic cholesterol metabolism and lipoprotein composition in the guinea pig Conde, K., M. Vergara-Jimenez, et al. (1996), J Lipid Res 37(11): 2372-82. Abstract: Guinea pigs were fed 15% (w/W) fat, high in lauric and myristic acids, a diet known to produce hypercholesterolemia in these animals. The diet was given alone or in combination with four doses of atorvastatin equivalent to 1, 3, 10, and 20 mg/kg per day. Atorvastatin reduced plasma LDL cholesterol concentrations by 46, 50, 53, and 70%, respectively (P < 0.001). Plasma apoB concentrations were reduced by atorvastatin (P < 0.001) and compositional changes occurred in VLDL and LDL with reductions of the relative proportion of cholesteryl ester and increases in triacylglycerol. A reduction in hepatic cholesteryl ester (66%) was observed only with the highest atorvastatin dose (20 mg/kg per day) while microsomal cholesterol was reduced by 30% with 3-20 mg/kg per day. Hepatic ACAT activity was down-regulated and apoB/E receptor number was increased by atorvastatin. In contrast, HMG-CoA reductase activity and cholesterol 7 alpha-hydroxylase were not affected by the drug. VLDL apoB secretion rates were decreased by atorvastatin treatment 59 and 76% with 3 and 20 mg/kg per day, respectively. Nascent VLDL particles were larger after drug treatment, showing an increased number in triacylglycerol molecules. These results support the hypothesis that the plasma LDL lowering induced by atorvastatin is due to a decreased secretion of apoB in combination with an increase of hepatic apoB/E receptors. |
| Hypocholesterolemic activity of a novel inhibitor of cholesterol absorption, SCH 48461 Salisbury, B. G., H. R. Davis, et al. (1995), Atherosclerosis 115(1): 45-63. Abstract: The amount of cholesterol that circulates in the plasma as lipoproteins can be affected by the balance of cholesterol metabolism within and between the intestines and liver. In the present report, we describe a novel hypocholesterolemic agent and document its pharmacological effects in animal models of hypercholesterolemia. The oral administration of (3R,4S)-1,4-bis-(4-methoxyphenyl)-3-(3-phenylpropyl)-2-azetidinone (SCH 48461) reduced plasma cholesterol concentrations in cholesterol-fed hamsters, rats and rhesus monkeys with ED50s of 1, 2 and 0.2 mg/kg per day, respectively, SCH 48461 was also highly effective in reducing hepatic cholesteryl ester accumulation in cholesterol-fed hamsters and rats after 7 days of treatment. In one 3 week study, rhesus monkeys were fed a 0.25% cholesterol/22% saturated fat diet with or without SCH 48461. At the end of the 3 week period the control group's VLDL + LDL-cholesterol increased to 180 Mg/dl from a baseline of approximately 65 mg/dl while plasma apolipoprotein B levels had doubled. Animals treated daily with 1 mg/kg SCH 48461 maintained their baseline levels of VLDL + LDL-cholesterol, HDL-cholesterol, and plasma apolipoproteins B and A-I. After 3 weeks the diets of the two groups were switched. Within 1 week SCH 48461 (1 mg/kg per day) rapidly reversed the elevated VLDL + LDL-cholesterol levels of the previous control group to near baseline values. SCH 48461 exerted its hypocholesterolemic effect through the inhibition of cholesterol absorption. A dose of 10 mg/kg per day inhibited cholesterol absorption in cholesterol-fed hamsters by 68% while a similar reduction was achieved in chow-fed monkeys with 3 mg/kg per day. This latter dose inhibited cholesterol absorption in cholesterol-fed monkeys by 95%. Treatment of cholesterol-fed monkeys with 10 mg/kg per day SCH 48461 significantly increased fecal neutral sterol excretion (52 vs. 32 mg/kg) but had no effect on acidic sterol excretion. Using a 2-h absorption model in cholesterol-fed hamsters, SCH 48461 caused a 46% inhibition of unesterified 14Ccholesterol accumulation in the intestinal wall and a 90% inhibition of cholesteryl ester formation at a dose of 10 mg/kg. Similar data were observed when the plasma radioactivity was assessed, indicating inhibition of both free (61%) and esterified (85%) cholesterol appearance. In contrast, CI-976, a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, did not affect the uptake of free cholesterol into the intestines while inhibiting cholesterol esterification (98% inhibition).(ABSTRACT TRUNCATED AT 400 WORDS) |
| Hypocholesterolemic activity of beta-sitosterol in cholesterol fed sea quail Day, C. E. (1991), Artery 18(3): 125-32. Abstract: Male SEA quail were fed a 0.5% cholesterol supplemented diet, to which was added 0%, 1%, and 2% beta-sitosterol, for a period of seven days. Dietarily administered beta-sitosterol reduced total serum cholesterol levels by 62% and 72% at the 1% and 2% treatment doses, respectively. This hypocholesterolemic activity of sitosterol in cholesterol fed SEA quail was anticipated on the basis of the numerous earlier studies demonstrating similar activity in cholesterol fed chickens. Beta-sitosterol was tested in SEA quail to experimentally confirm its expected serum cholesterol lowering effects and to expand further the utility of the SEA quail model in cholesterol and atherosclerosis research. |
| Hypocholesterolemic activity of nut shell extract of Semecarpus anacardium (Bhilawa) in cholesterol fed rabbits Sharma, A., R. Mathur, et al. (1995), Indian J Exp Biol 33(6): 444-8. Abstract: Administration of S. anacardium nut shell extract to cholesterol fed rabbits resulted in a significant reduction in serum cholesterol (-73.3%) and serum LDL-Chol. (-80%). The extract feeding also prevented the accumulation of cholesterol/triglycerides in liver, heart muscle and aorta and caused a regression of plaques (75.3-83.5%). These results indicate that S. anacardium is hypocholesterolemic in action and prevents cholesterol induced atheroma. Possible mechanism of action is discussed. |
| Hypocholesterolemic effect of indigestible fraction of Chlorella regularis in cholesterol-fed rats Shibata, S., K. Oda, et al. (2001), J Nutr Sci Vitaminol (Tokyo) 47(6): 373-7. Abstract: The effects of Chlorella regularis powder (CP) and Chlorella regularis indigestible fraction (CIF) on serum and liver lipid concentrations and on fecal steroid excretion were estimated in rats fed diets containing 5 g/kg cholesterol and 2.5 g/kg sodium cholate. The ingestion of 12.7% CP or 5.3% CIF did not influence food intake or growth. CP and CIF decreased the levels of serum cholesterol, but had no effect on the levels of serum triacylglycerol and phospholipid. Liver cholesterol contents were lower in the CP and CIF groups than in the control group, but CP and CIF did not affect liver triacylglycerol content. CP and CIF increased the total amount of fecal neutral steroids excreted, but did not modify the total bile acid excretion. However, the soluble bile acid concentrations of reconstituted fecal water in the rats fed CP and CIF diets were lower than the control value. Moreover, CP and CIF had a high bile acid binding capacity in vitro. These results indicated that CIF had a hypocholesterolemic effect and enhanced fecal neutral steroid excretion while decreasing the soluble fecal bile acid concentration. |
| Hypocholesterolemic effect of Lactobacillus gasseri SBT0270 in rats fed a cholesterol-enriched diet Usman and A. Hosono (2001), J Dairy Res 68(4): 617-24. Abstract: The effects of administration of Lactobacillus gasseri SBT0270 on serum lipids and bile acids, faecal bile acids and microflora were estimated in hypercholesterolemic rats. An effective dose of strain SBT0270 to exert its hypocholesterolemic effect was 10(9) viable cells/d. The dose of 10(9) cells/d did not affect the faecal coliform counts, but the number of faecal lactobacilli in rats fed this dose was significantly higher than that in the control group observed at the end of feeding period. Hypocholesterolemic effect of Lb. gasseri SBT0270 was attributed to its ability to suppress the reabsorption of bile acids into the enterohepatic circulation and to enhance the excretion of acidic steroids in faeces of hypercholesterolemic rats. |
| Hypocholesterolemic effect of lycopene and beta-carotene is related to suppression of cholesterol synthesis and augmentation of LDL receptor activity in macrophages Fuhrman, B., A. Elis, et al. (1997), Biochem Biophys Res Commun 233(3): 658-62. Abstract: Beta-Carotene and lycopene are derived from plants, and they share similar initial synthetic pathway with cholesterol, which is synthesized in animal but not in plant cells. Thus, we sought to analyze the effect of carotenoids on macrophage cholesterol metabolism, in comparison to the effect of LDL cholesterol and of the cholesterol synthesis inhibitor, fluvastatin. In J-774 A. 1 macrophage cell line, the cellular cholesterol synthesis from 3H-acetate, but not from 14C mevalonate, was suppressed by 63% any by 73% following cell incubation with beta-carotene or lycopene (10 microM) respectively, in comparison to a 90% and 91% inhibition by LDL (100 micrograms of cholesterol), or by fluvastatin (10 micrograms/ml) respectively. However, unlike LDL derived cholesterol, which also suppresses macrophage LDL receptor activity, lycopene and beta-carotene augmented the activity of the macrophage LDL receptor, similarly to the effect of fluvasfatin. In agreement with these in vitro observations, dietary supplementation of tomato's lycopene (60 mg/day) to 6 males for a 3 months period resulted in a significant 14% reduction in their plasma LDL cholesterol concentrations. We thus conclude that dietary supplementation of carotenoids may act as moderate hypocholesterolemic agents, secondary to their inhibitory effect on macrophage 3-hydroxy-3-methyl glutaryl coenzyme A (HMGCoA) reductase, the rate limiting enzyme in cholesterol synthesis. |
| Hypocholesterolemic effect of naringin associated with hepatic cholesterol regulating enzyme changes in rats Shin, Y. W., S. H. Bok, et al. (1999), Int J Vitam Nutr Res 69(5): 341-7. Abstract: The effects of the citrus bioflavonoid naringin were tested by using it as a supplement in a high-cholesterol diet. Male rats were fed for 42 days with a 1% (wt/wt) high cholesterol diet either with or without naringin-supplementation (0.1%, wt/wt) to study the effect on plasma lipid levels, hepatic lipid contents, hepatic enzyme activity, and the excretion of fecal neutral sterols. Naringin did not significantly alter the levels of plasma triglycerides, however, the levels of plasma cholesterol (3.80 +/- 0.31 mmol/L vs. 2.61 +/- 0.30 mmol/L, mean +/- SE; p < 0.05) and hepatic cholesterol (70.3 +/- 4.3 mg/g vs. 54.3 +/- 3.8 mg/g, mean +/- SD; p < 0.05) were significantly lowered compared to those of the control. HMG-CoA reductase (2487.0 +/- 210.0 pmole/min/mg vs. 1879.0 +/- 236.0 pmole/min/mg, mean +/- SE; p < 0.05) and ACAT (806.0 +/- 105.0 pmole/min/mg vs. 643.0 +/- 80.0 pmole/min/mg, mean +/- SE; p < 0.05) activities were both substantially lower in the naringin-supplemented group than in the control. The naringin supplementation markedly decreased the excretion of fecal neutral sterols (204.7 +/- 28.5 mg/day) compared to the control (521.9 +/- 53.9 mg/day). The combination of the inhibited HMG-CoA reductase (-24.4%) and ACAT (-20.2%) activities as a result of naringin supplementation could account for the decrease of fecal neutral sterols. |
| Hypocholesterolemic effect of pravastatin is associated with increased content of antioxidant vitamin-E in cholesterol fractions Blaha, V., Z. Zadak, et al. (1998), Acta Medica (Hradec Kralove) 41(2): 87-90. Abstract: Metabolic studies support the findings that antioxidants inhibit atherosclerosis. Treatment with vitamin E reduced both the susceptibility of low density lipoprotein cholesterol (LDL-C) to in vivo lipid peroxidation and atherosclerosis and smooth muscle proliferation. Thus the aim of present study was to examine metabolic consequences of reduced plasma LDL-C during hypolipidemic therapy and the distribution of antioxidant vitamin E. A group of 10 patients (4 men, 6 women, age 35-65y) with familial hypercholesterolaemia was treated using pravastatin (Lipostat Bristol Myers Squibb, 40 mg daily at 6:00 PM). Blood samples were examined before treatment, after 4 and 8 weeks of therapy. After ultracentrifugation, samples were analyzed for lipoprotein fractions and the content of vitamin E and cholesterol. Pravastatin reduced both total cholesterol (9.85 +/- 0.74 vs. 6.81 +/- 0.51 mmol/1; p < 0.01), LDL-C (6.42 +/- 0.45 vs. 4.51 +/- 0.45 mmol/l; p < 0.01), light LDL1-C (4.56 +/- 0.50 vs. 3.11 +/- 0.34 mmol/l; p < 0.05) and dense LDL2-C (1.86 +/- 0.27 vs. 1.42 +/- 0.17 mmol/l; ns). Serum vitamin E was reduced during hypolipidemic therapy in the fraction of total, LDL1, LDL2, and VLDL-cholesterol. However, the ratio of serum vitamin E/total serum cholesterol (4.57 +/- 0.32 vs. 5.12 +/- 0.37 mmol/l/mmol/l; p < 0.05) and ratio of LDL2-C vitamin E/LDL2-C (3.92 +/- 0.07 vs. 4.64 +/- 0.37 mmol/l/mmol/l; p = 0.08) increased in comparison to pre-treatment values. We conclude that pravastatin therapy may possess anti-atherogenic properties which involve not only its hypocholesterolemic effect, but also its favorable effects on the distribution of LDL subclasses and the content of antioxidant vitamin E in atherogenic lipoproteins. |
| Hypocholesterolemic effect of ursodeoxycholylcysteic acid in hamsters fed a high cholesterol diet Shimizu, H., M. Yoshii, et al. (1992), J Pharmacobiodyn 15(10): 573-80. Abstract: We studied the effect of feeding ursodeoxycholylcysteic acid, the cysteic acid conjugated analog of ursodeoxycholyltaurine, on serum and liver cholesterol levels and on intestinal absorption of cholesterol and bile salts in hamsters. Addition of ursodeoxycholylcysteic acid to the cholesterol-enriched diet reduced the elevation of serum and liver cholesterol levels caused by feeding cholesterol. However, supplementation with ursodeoxycholylcysteic acid to the standard diet did not show any significant change in serum and liver cholesterol levels. Administration of ursodeoxycholylcysteic acid caused a decrease in dietary cholesterol absorption but did not interfere with the ileal transport of endogenous bile salts. Hence the hypocholesterolemic activity of dietary ursodeoxycholylcysteic acid is thought to be the effect on intestinal absorption of cholesterol but not to be the interruption of the enterohepatic circulation of bile salts. |
| Hypocholesterolemic effect of vitamin E on cholesterol-fed rabbit Phonpanichrasamee, C., P. Komaratat, et al. (1990), Int J Vitam Nutr Res 60(3): 240-4. Abstract: Serum cholesterol level increased sharply in rabbits fed an atherosclerosis-promoting diet containing 0.25% or 0.5% cholesterol. Oral supplementation with 2100 IU of vitamin E per week manifested a hypocholesterolemic effect only after four weeks, with 50% reduction attained on the 8th week. Changes in low density and very low density lipoprotein cholesterol levels paralleled those in the serum. Liver total cholesterol level and the ratio of free to ester forms were not different between vitamin E-supplemented and nonsupplemented rabbits, whereas a 4-5 fold increase in hepatic cholesterol-7 alpha-hydroxylase activity, elevation of bile salt concentration and improvement in bile lithogenic index were observed in the vitamin E-supplemented groups. |
| Hypocholesterolemic effects of a flavonoid-rich extract of Hypericum perforatum L. in rats fed a cholesterol-rich diet Zou, Y., Y. Lu, et al. (2005), J Agric Food Chem 53(7): 2462-6. Abstract: In a previous study, a flavonoid-rich extract of Hypericum perforatum L. (FEHP) was prepared and its antioxidant activity was determined by a series of models in vitro. In this study, the hypocholesterolemic effects of FEHP in rats fed a cholesterol-rich diet were tested. Forty Wistar rats fed a standard laboratory diet or a cholesterol-rich diet for 16 weeks were used. The serum lipid levels, as well as malondialdehyde (MDA) and activity of superoxide dismutase (SOD) and catalase (CAT) in serum and liver, were examined. Cholesterol-rich diet induced hypercholesterolemia was manifested in the elevation of serum lipid levels such as total cholesterol (TC), total triglycerides (TG), and low density lipoprotein cholesterol (LDL-C). Administration of middle-dose (75 mg/kg of BW/day) and high-dose (150 mg/kg of BW/day) FEHP significantly lowered the serum levels of TC, TG, and LDL-C, while increasing the serum level of high density lipoprotein cholesterol (HDL-C). Also, the content of MDA in serum and liver decreased significantly after oral administration of FEHP compared with those of rats fed a cholesterol-rich diet. In addition, FEHP increased the activity of SOD in serum and liver, but the activity of CAT was significantly elevated only in liver. These results suggested that the hypocholesterolemic effects of FEHP might be due to its abilities to lower serum TC, TG, and LDL-C levels as well as to slow the lipid peroxidation process and to enhance the antioxidant enzyme activity. |
| Hypocholesterolemic properties of plant indoles. Inhibition of acyl-CoA:cholesterol acyltransferase activity and reduction of serum LDL/VLDL cholesterol levels by glucobrassicin derivatives Dunn, S. E. and G. A. LeBlanc (1994), Biochem Pharmacol 47(2): 359-64. Abstract: Studies were undertaken to investigate the effects of the plant compound indole-3-carbinol (I3C) and its acid condensation products, which are generated in the stomach following ingestion of I3C, on cholesterol homeostasis in mice. Individual acid condensation products were synthesized and purified by HPLC. In vitro experiments revealed that several of the acid condensation products effectively inhibited the enzyme acyl-CoA:cholesterol acyltransferase (ACAT), which is responsible for the conversion of free cholesterol to the cholesteryl ester, at micromolar concentrations. Since the inhibition of ACAT in vivo should reduce serum cholesterol levels, I3C was administered to mice, and the effects on serum cholesterol levels were evaluated. Total serum cholesterol levels were elevated by 29% in mice provided a 3% cholesterol-supplemented diet, but this elevation was attenuated significantly (P < or = 0.05) by approximately 50% when I3C (100 mg/kg/day) was added to this diet. This effect of I3C was entirely on low density lipoprotein (LDL)/very low density lipoprotein (VLDL) cholesterol, which was lowered significantly (P < or = 0.05) by approximately 30%. In summary, I3C lowered serum LDL/VLDL cholesterol levels in mice, and this effect was likely mediated by the inhibition of ACAT by some of the acid condensation products of I3C. These results provide a possible mechanism by which I3C-rich vegetables lower serum cholesterol levels. |
| Hypo-fibrinolysis in patients with hypertension and elevated cholesterol Jansson, J. H., B. Johansson, et al. (1991), J Intern Med 229(4): 309-16. Abstract: To test the hypothesis that increased blood pressure and hyperlipidaemia result in changes in the fibrinolytic system, 84 subjects with both hypertension and elevated serum cholesterol levels (the high risk group) were compared with 55 controls matched with respect to age, sex and body mass index (BMI). Plasminogen activator inhibitor (PAI-1), and tissue plasminogen activator (tPA) antigen and activity were measured before and after venous occlusion. In the high risk group, tPA activity was significantly lower both before and after venous occlusion and PAI-1 levels were significantly higher. In a multivariate analysis the triglyceride levels, diastolic blood pressure and cholesterol levels were independently associated with the PAI-1 levels. Diastolic blood pressure was independently and inversely associated with resting tPA activity. We conclude that patients with hypertension and hyperlipidaemia have a reduced activity of the fibrinolytic system, an effect which is unrelated to differences in age, sex, smoking or BMI. |
| Hypolipidaemic effect of fruit juice of Emblica officinalis in cholesterol-fed rabbits Mathur, R., A. Sharma, et al. (1996), J Ethnopharmacol 50(2): 61-8. Abstract: The lipid lowering and antiatherosclerotic effects of Emblica officinalis (Amla) fresh juice were evaluated in cholesterol-fed rabbits (rendered hyperlipidaemic by atherogenic diet and cholesterol feeding). E. officinalis fresh juice was administered at a dose of 5 ml/kg body weight per rabbit per day for 60 days. Serum cholesterol, TG, phospholipid and LDL levels were lowered by 82%, 66%, 77% and 90%, respectively. Similarly, the tissue lipid levels showed a significant reduction following E. officinalis juice administration. Aortic plaques were regressed. E. officinalis juice treated rabbits excreted more cholesterol and phospholipids, suggesting that the mode of absorption was affected. E. officinalis juice is an effective hypolipidaemic agent and can be used as a pharmaceutical tool in hyperlipidaemic subjects. |
| Hypolipidemic action of F-1394, an acyl-CoA: cholesterol acyltransferase (ACAT) inhibitor, in high-fat diet fed beagle dogs Kusunoki, J., K. Aragane, et al. (1997), Yakugaku Zasshi 117(4): 233-41. Abstract: In the present study, we investigated the hypolipidemic effect of F-1394, a potent and selective inhibitor of acyl-CoA: cholesterol acyltransferase (ACAT), in dogs fed with a high-fat diet consisting of regular foods, 5% cholesterol and 16% fat. The serum cholesterol levels in dogs reached the steady-state 1 week after the start of feeding of a high-fat diet and were about 2-fold greater than those in normolipidemic dogs. Graded administration of the doses of F-1394 (1-30 mg/kg/d) to the dogs fed with a high-fat diet prevented the elevation of serum cholesterol levels. In the hyperlipidemic dogs fed with a high-fat diet for 14 d before the start of the administration of F-1394, the oral administration of F-1394 at a dose of 1, 3 or 10 mg/kg/d for 21 d reduced the serum cholesterol levels in a dose-dependent manner. The estimated ID50 value was 7.2 +/- 0.3 mg/kg/d p. o. (12.1 +/- 0.5 mol/kg/d p. o.). F-1394 did not affect the body weight and no diarrhea was observed by the administration of F-1394. F-1394 at a dose of 10 mg/kg/d or more also significantly inhibited the increase of serum triglyceride levels 3 h after the feeding of high-fat diet. These results suggest that F-1394 inhibits the ACAT activity in the canine small intestine and, subsequently, the inhibition of ACAT activity contributes much to the prevention of cholesterol absorption via the gut, resulting in a decrease in serum cholesterol levels in the dogs fed with high-fat diet. Furthermore, F-1394 may also have an inhibitory effect on the triglyceride absorption via the gut, and the therapeutical use for postprandial hypertriglyceridemia is expected. |
| Hypolipidemic and anti-atherogenic effects of long-term Cholestin (Monascus purpureus-fermented rice, red yeast rice) in cholesterol fed rabbits Wei, W., C. Li, et al. (2003), J Nutr Biochem 14(6): 314-8. Abstract: Long-term effects of Cholestin (Monascus purpureus rice; red yeast rice) on serum lipids and severity of atherosclerosis were examined in rabbits fed for 200 days on a semi-purified diet containing 0.25% cholesterol. Serum total cholesterol was 25 and 40% lower, respectively, in rabbits fed 0.4 or 1.35 g/kg/day of Cholestin (Monascus purpureus rice; red yeast rice) compared to controls. This treatment also lowered serum LDL cholesterol. This 200-day treatment significantly reduced serum triglycerides and atherosclerotic index (ratio of non-HDL-cholesterol to HDL-cholesterol). Although similar reductions of total, LDL-cholesterol and triglycerides were observed, a parallel group of rabbits fed lovastatin (0.0024 g/kg/day) failed to reduce the index significantly. Apolipoprotein A(1) was increased and apolipoprotein B was reduced in all treatment groups. Severity of atherosclerosis was reduced significantly in all treatment groups. The sudanophilic area of involvement was 80.6% in controls, and reduced significantly; to 30.1% on the low dose of Cholestin (Monascus purpureus rice; red yeast rice), and 17.2% on the high dose. Lovastatin reduced severity of lesions by 89% (sudanophilia) and 84% (visual). Visual grading of lesion severity showed reduction by 38% and 68%. |