MyMedR

Displaying publications 21 - 29 of 29 in total

Abstract:

Sort:

Fulltext Ezetimibe/simvastatin 10/40 mg versus atorvastatin 40 mg in high cardiovascular risk patients with primary hypercholesterolemia: a randomized, double-blind, active-controlled, multicenter study

Hing Ling PK, Civeira F, Dan AG, Hanson ME, Massaad R, De Tilleghem Cle B, et al.

Lipids Health Dis, 2012;11:18.
PMID: 22293030 DOI: 10.1186/1476-511X-11-18

A considerable number of patients with severely elevated LDL-C do not achieve recommended treatment targets, despite treatment with statins. Adults at high cardiovascular risk with hypercholesterolemia and LDL-C ≥ 2.59 and ≤ 4.14 mmol/L (N = 250), pretreated with atorvastatin 20 mg were randomized to ezetimibe/simvastatin 10/40 mg or atorvastatin 40 mg for 6 weeks. The percent change in LDL-C and other lipids was assessed using a constrained longitudinal data analysis method with terms for treatment, time, time-by-treatment interaction, stratum, and time-by-stratum interaction. Percentage of subjects achieving LDL-C < 1.81 mmol/L, < 2.00 mmol/L, or < 2.59 mmol/L was assessed using a logistic regression model with terms for treatment and stratum. Tolerability was assessed.

Matched MeSH terms: Hypercholesterolemia/drug therapy*
Comparison of the efficacy and level of adherence for morning versus evening versus before bedtime administration of simvastatin in hypercholesterolemic patients

Heng WK, Ng YP, Ooi GS, Habshoh J, Nurazlin J, Nor Azah MN, et al.

Med J Malaysia, 2019 12;74(6):477-482.
PMID: 31929472

BACKGROUND: Simvastatin is usually taken in the evening due to the circadian rhythm of hepatic cholesterol biosynthesis. The degree of reduction of low-density lipoprotein cholesterol (LDL-C) and the level of adherence to different administration time remained unknown in the Malaysian population. This study aims to investigate the effect of simvastatin on the percentage changes of lipid profile and the level of adherence to when simvastatin was instructed to be taken at different timing.
METHODS: Nine primary care health clinics across Malaysia participated in this study. 147 statin-naive subjects were selected through convenient sampling and randomised into one of the three arms (after breakfast, after dinner or before bedtime). Differences on percentage reduction of LDL-C from baseline and level of adherence among the three groups at week-16 were compared. The main outcomes measured in this study were the percentage change of lipid parameters and the percentage of high-adherence (MMAS=8) at week-16.
RESULTS: 59.2% of the patients were male. The mean age of the study population was 53.93± 10.85 years. Most of the patients were Malays (69.4%); followed by Indians (22.4%) and Chinese (8.2%). LDL-C decreased from 4.26 (Standard Deviation, SD1.01) to 2.36 (SD0.69)mmol/L at week-16 for patients taking simvastatin before bedtime; an absolute reduction of 44.95%.The differences of LDL-C percentage reduction between three arms were significantly different (p<0.001). The greatest LDL-C reduction was observed when simvastatin was taken before bedtime and revealed 56.2% patients with high-adherence at week-16.
CONCLUSION: Simvastatin showed superior LDL-reduction and higher level of adherence when being instructed to be taken before bedtime.

Matched MeSH terms: Hypercholesterolemia/drug therapy*
HMG-CoA Reductase as Target for Drug Development

Gunasekaran B, Shukor MY

Methods Mol Biol, 2020;2089:245-250.
PMID: 31773659 DOI: 10.1007/978-1-0716-0163-1_16

The main strategy for lowering blood cholesterol levels is through the inhibition of the NADPH-dependent HMG-CoA reductase (3-hydroxy-3-methyl-glutaryl-CoA reductase). The enzyme catalyses the reduction of HMG-CoA to mevalonate and this process is inhibited by statins that form the bulk of the therapeutic agents to treat high cholesterol since the 1970s. Newer drugs that are safer than statins are constantly being developed. The inhibition of candidate drugs to HMG-CoA reductase remains the mainstay of drug development research. The determination of the enzyme activity is important for the correct assessment of potency of the enzyme as well as determining the inhibition of potential therapeutic agents from the plant and microbial extracts. Also, this chapter covers the use of the popular four-parameter logistics model that can yield accurate estimation of the IC50 values of therapeutic agents and their 95% confidence intervals.

Matched MeSH terms: Hypercholesterolemia/drug therapy
Phaleria macrocarpa (Scheff.) Boerl fruit aqueous extract enhances LDL receptor and PCSK9 expression in vivo and in vitro

Chong SC, Dollah MA, Chong PP, Maha A

J Ethnopharmacol, 2011 Sep 1;137(1):817-27.
PMID: 21763412 DOI: 10.1016/j.jep.2011.06.041

Phaleria macrocarpa (Scheff.) Boerl (Pm) has been shown to reduce cholesterol level in vitro and in vivo experiment.

Matched MeSH terms: Hypercholesterolemia/drug therapy*
Hypocholesterolemic Effects of Kenaf Seed Oil, Macroemulsion, and Nanoemulsion in High-Cholesterol Diet Induced Rats

Cheong AM, Jessica Koh JX, Patrick NO, Tan CP, Nyam KL

J Food Sci, 2018 Mar;83(3):854-863.
PMID: 29412455 DOI: 10.1111/1750-3841.14038

This study aimed to evaluate the effect of kenaf seed oil (KSO), kenaf seed oil-in-water macroemulsion (KSOM), kenaf seed oil-in-water nanoemulsions (KSON), and emulsifier mixtures (EM) on serum lipid profile, liver oxidative status, and histopathological changes in high-cholesterol fed rats. Stability and characteristic of KSOM and KSON were carried out prior to in vivo study. Forty-two Sprague-Dawley rats were divided into 7 groups (6 rats each) and induced hypercholesterolemia by feeding high cholesterol diet (HCD) for 14 days prior to treatments. Different treatments were introduced on day 15 to 29 while supplemented with HCD and removal of HCD during treatment on day 30 to 43, except for HCD group. Body weight and serum lipid profiles were measured at 3 different points: after hypercholesterolemia was induced, on day 29, and at the end of the experiment. Relative liver weight, atherogenic index, coronary risk index, and fecal total bile acids were also determined at the end of experiment. KSON showed significantly higher stability than KSOM and FTIR exhibited good encapsulation of KSO after 1.5 years of storage. Serum total cholesterol, low density lipoprotein cholesterol, lipid peroxidation levels in HCD group without treatment were significantly higher compared to normal control group and all treatment groups. All samples demonstrated hypocholesterolemic effect, but KSON exhibited higher efficiency in cholesterol-lowering properties, weight control and decreased liver fat as confirmed by histopathological evaluation. The overall results revealed that the efficacy of different treatments was in descending order of KSON, KSO, KSOM, and EM.
PRACTICAL APPLICATION: Kenaf seed oil-in-water nanoemulsion (KSON) has the potential to be used as a natural alternative to the synthetic hypocholesterolemic drug in the future. However, larger sample size and clinical trial are needed to confirm on this potential application. In addition, treatment with KSON was suggested to prevent cardiovascular disease and fatty liver.

Matched MeSH terms: Hypercholesterolemia/drug therapy*
Dietary supplementation of defatted kenaf (Hibiscus cannabinus L.) seed meal and its phenolics-saponins rich extract effectively attenuates diet-induced hypercholesterolemia in rats

Chan KW, Ismail M, Mohd Esa N, Imam MU, Ooi J, Khong NMH

Food Funct, 2018 Feb 21;9(2):925-936.
PMID: 29313544 DOI: 10.1039/c7fo01109a

Kenaf is one of the important commercial fiber crops worldwide and defatted kenaf seed meal (DKSM) is a secondary by-product from the kenaf industry. Thus, efforts to turn this low-cost agricultural waste into value-added functional food ingredients will definitely bring advantageous impacts to the community health, environment and economy. The present study was aimed to investigate the cardioprotective properties of DKSM and its phenolics-saponins rich extract (PSRE) in diet-induced hypercholesterolemic rat model. Hypercholesterolemia was induced in Sprague-Dawley rats via atherogenic diet feeding and dietary interventions were conducted by incorporating DKSM (15% and 30%) and equivalent levels of PSRE (2.3% and 4.6%, respectively, equivalent to the total content of phenolics and saponins in DKSM groups) into the atherogenic diets. After 10 weeks of DKSM and PSRE supplementation, the hepatosomatic index, hepatosteatosis, serum lipid profile, Castelli risk indexes as well as hepatic and renal functions of hypercholesterolemic rats were significantly improved (p < 0.05). Besides, the levels of hepatic Hmgcr and serum Pcsk9 were lowered, along with transcriptional upregulations of hepatic Cyp7a1, Abca1, Lcat, ApoA2 and ApoE (p < 0.05). The gene expression of hepatic Ldlr was marginally enhanced by DKSM supplementation (p > 0.05), but superiorly upregulated by PSRE (p < 0.05). The combined results showed that hypercholesterolemia and the atherogenic risk in rats were effectively attenuated by DKSM and PSRE supplementation, possibly via modulations of multiple vital processes in hepatic cholesterol metabolism. Furthermore, phenolics and saponins may be the bioactives conferring DKSM and PSRE with their anti-hypercholesterolemic properties. In conclusion, DKSM and PSRE are prospective cardioprotective functional food ingredients for hypercholesterolemic individuals.

Matched MeSH terms: Hypercholesterolemia/drug therapy*
Fulltext HMG-CoA reductase inhibitory activity and phytocomponent investigation of Basella alba leaf extract as a treatment for hypercholesterolemia

Baskaran G, Salvamani S, Ahmad SA, Shaharuddin NA, Pattiram PD, Shukor MY

Drug Des Devel Ther, 2015;9:509-17.
PMID: 25609924 DOI: 10.2147/DDDT.S75056

The enzyme 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase is the key enzyme of the mevalonate pathway that produces cholesterol. Inhibition of HMG-CoA reductase reduces cholesterol biosynthesis in the liver. Synthetic drugs, statins, are commonly used for the treatment of hypercholesterolemia. Due to the side effects of statins, natural HMG-CoA reductase inhibitors of plant origin are needed. In this study, 25 medicinal plant methanol extracts were screened for anti-HMG-CoA reductase activity. Basella alba leaf extract showed the highest inhibitory effect at about 74%. Thus, B. alba was examined in order to investigate its phytochemical components. Gas chromatography with tandem mass spectrometry and reversed phase high-performance liquid chromatography analysis revealed the presence of phenol 2,6-bis(1,1-dimethylethyl), 1-heptatriacotanol, oleic acid, eicosyl ester, naringin, apigenin, luteolin, ascorbic acid, and α-tocopherol, which have been reported to possess antihypercholesterolemic effects. Further investigation of in vivo models should be performed in order to confirm its potential as an alternative treatment for hypercholesterolemia and related cardiovascular diseases.

Matched MeSH terms: Hypercholesterolemia/drug therapy*
Fulltext Phaleria macrocarpa Boerl. (Thymelaeaceae) leaves increase SR-BI expression and reduce cholesterol levels in rats fed a high cholesterol diet

Andriani Y, Tengku-Muhammad TS, Mohamad H, Saidin J, Syamsumir DF, Chew GS, et al.

Molecules, 2015 Mar 09;20(3):4410-29.
PMID: 25759957 DOI: 10.3390/molecules20034410

In vitro and in vivo studies of the activity of Phaleria macrocarpa Boerl (Thymelaeaceae) leaves against the therapeutic target for hypercholesterolemia were done using the HDL receptor (SR-BI) and hypercholesterolemia-induced Sprague Dawley rats. The in vitro study showed that the active fraction (CF6) obtained from the ethyl acetate extract (EMD) and its component 2',6',4-trihydroxy-4'-methoxybenzophenone increased the SR-BI expression by 95% and 60%, respectively. The in vivo study has proven the effect of EMD at 0.5 g/kgbw dosage in reducing the total cholesterol level by 224.9% and increasing the HDL cholesterol level by 157% compared to the cholesterol group. In the toxicity study, serum glutamate oxalate transaminase (SGOT) and serum glutamate pyruvate transaminase (SGPT) activity were observed to be at normal levels. The liver histology also proved no toxicity and abnormalities in any of the treatment groups, so it can be categorized as non-toxic to the rat liver. The findings taken together show that P. macrocarpa leaves are safe and suitable as an alternative control and prevention treatment for hypercholesterolemia in Sprague Dawley rats.

Matched MeSH terms: Hypercholesterolemia/drug therapy*
Fulltext Changes in the vascular cell adhesion molecule-1, intercellular adhesion molecule-1 and c-reactive protein following administration of aqueous extract of piper sarmentosum on experimental rabbits fed with cholesterol diet

Amran AA, Zakaria Z, Othman F, Das S, Al-Mekhlafi HM, Nordin NA

Lipids Health Dis, 2011 Jan 09;10:2.
PMID: 21214952 DOI: 10.1186/1476-511X-10-2

BACKGROUND: Inflammation process plays an important role in the development of atherosclerosis. Hypercholesterolemia is one of the major risk factors for atherosclerosis. The present study aimed to evaluate the effect of aqueous extract of Piper sarmentosum (P.s) on inflammatory markers like vascular cell adhesion molecule-1 (VCAM-1), intercellular adhesion molecule-1 (ICAM-1), and C-reactive protein (CRP).
METHODS: Forty two male New Zealand white rabbits were divided equally into seven groups; (i) C- control group fed normal rabbit chow (ii) CH- cholesterol diet (1%cholesterol) (iii) X1- 1% cholesterol with water extract of P.s (62.5 mg/kg) (iv) X2- 1% cholesterol with water extract of P.s (125 mg/kg (v) X3- 1% cholesterol with water extract of P.s (250 mg/kg) (vi) X4- 1% cholesterol with water extract of P.s (500 mg/kg) and (vii) SMV group fed with 1% cholesterol supplemented with simvistatin drug (1.2 mg/kg). All animals were treated for 10 weeks. Blood serum was taken for observing the inflammatory markers at the beginning and end of the experiment.
RESULTS: Rabbits fed with 1% cholesterol diet (CH) showed significant increase in the level of VCAM-1, ICAM-1 and CRP compared to the C group. The levels of VCAM-1, ICAM-1 and CRP in the 1% cholesterol group and supplemented with P.s (500 mg/kg) were significantly reduced compared to the cholesterol group. Similar results were also reported with simvistatin group.
CONCLUSION: These results suggest that the supplementation of Piper sarmentosum extract could inhibit inflammatory markers which in turn could prevent atherosclerosis.

Matched MeSH terms: Hypercholesterolemia/drug therapy