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Fast dissolving microneedle patch for pronounced systemic delivery of an antihyperlipidemic drug

Ahmad Z, Zafar N, Mahmood A, Sarfraz RM, Latif R, Gad HA

Pharm Dev Technol, 2023 Nov;28(9):896-906.
PMID: 37873604 DOI: 10.1080/10837450.2023.2272863

Fast dissolving microneedles (F-dMN) are quite a novel approach delivering specific drug molecules directly into the bloodstream, bypassing the first-pass effect. The present study reported an F-dMN patch to enhance systemic delivery of simvastatin in a patient-friendly manner. The F-dMN patch was developed using polyvinyl pyrrolidone and polyvinyl alcohol and characterized using light microscopy, SEM, XRD, FTIR, mechanical strength, drug content (%), an ex-vivo penetration study, an ex-vivo drug release study, a skin irritation test, and a pharmacokinetics study. The optimized F-dMN patch exhibited excellent elongation of 35.17%, good tensile strength of 9.68 MPa, an appropriate moisture content of 5.65%, and good penetrability up to 560 µm. Moreover, it showed 93.4% of the drug content within the needles and 81.75% in-vitro release. Histopathological findings and a skin irritation study proved that the F-dMN patch was biocompatible and did not cause any sort of irritation on animal skin. Pharmacokinetic parameters of F-dMN patches were improved (Cmax 6.974 µg/ml, tmax 1 hr and AUC 19. 518 µg.h/ml) as compared to tablet Simva 20 mg solution (Cmax 2.485 µg/ml, tmax 1.4 hr and AUC 11.199 µg.h/ml), thus confirming bioavailability enhancement. Moreover, stability studies confirmed the stability of the developed F-dMN patch, as investigated by axial needle fracture force and drug content.

Matched MeSH terms: Hypolipidemic Agents/pharmacology
A successful pregnancy outcome of homozygous familial hypercholesterolaemia patient on statin therapy

Mohd Kasim NA, Al-Khateeb A, Chua YA, Sanusi AR, Mohd Nawawi H

Malays J Pathol, 2021 Apr;43(1):87-93.
PMID: 33903311

Homozygous familial hypercholesterolaemia (HoFH) is a rare genetic disorder of lipoprotein metabolism mainly due to mutation of the low-density lipoprotein (LDL)-receptor gene (LDLR). It is a life-threatening disease that causes accelerated, multi-vessel atherosclerosis presented in early childhood. Pregnancy in HoFH may pose early coronary morbidity and mortality to both the foetus and mother. The combination of HoFH and pregnancy can be a fatal condition. While statins are very effective in lowering low-density lipoprotein cholesterol (LDL-C) levels, they are generally contraindicated during pregnancy, thus their use during pregnancy is uncommon. On the other hand, lipid apheresis (LA) has turned into an effective treatment to control cholesterol level amid pregnancy. However, the procedure is not widely available in our region. To date, there are scarcely documented case reports of HoFH in pregnancy in which the majority of them underwent LA to keep LDL-C at a low level. We report a rare case of successful pregnancy outcome of HoFH patient treated with lipid-lowering drugs including statin without LA therapy. Apart from that, we also discussed the genetic findings of the proband and all screened family members in which to the best of our knowledge, the first study using the whole-exome sequencing technique to identify the causative gene mutations for familial hypercholesterolaemia among the Malaysian population.

Matched MeSH terms: Hypolipidemic Agents
Formation of Antihyperlipidemic Nano-Ezetimibe from Volatile Microemulsion Template for Enhanced Dissolution Profile

Saleem MA, Yasir Siddique M, Nazar MF, Khan SU, Ahmad A, Khan R, et al.

Langmuir, 2020 07 14;36(27):7908-7915.
PMID: 32551692 DOI: 10.1021/acs.langmuir.0c01016

Nanostructures play an important role in targeting sparingly water-soluble drugs to specific sites. Because of the structural flexibility and stability, the use of template microemulsions (μEs) can produce functional nanopharmaceuticals of different sizes, shapes, and chemical properties. In this article, we report a new volatile oil-in-water (o/w) μE formulation comprising ethyl acetate/ethanol/brij-35/water to obtain the highly water-dispersible nanoparticles of an antihyperlipidemic agent, ezetimibe (EZM-NPs), to enhance its dissolution profile. A pseudoternary phase diagram was delineated in a specified brij-35/ethanol ratio (1:1) to describe the transparent, optically isotropic domain of the as-formulated μE. The water-dilutable μE formulation, comprising an optimum composition of ethyl acetate (18.0%), ethanol (25.0%), brij-35 (25.0%), and water (32.0%), showed a good dissolvability of EZM around 4.8 wt % at pH 5.2. Electron micrographs showed a fine monomodal collection of EZM-loaded μE droplets (∼45 nm) that did not coalesce even after lyophilization, forming small spherical EZM-NPs (∼60 nm). However, the maturity of nanodrug droplets observed through dynamic light scattering suggests the affinity of EZM to the nonpolar microenvironment, which was further supported through peak-to-peak correlation of infrared analysis and fluorescence measurements. Moreover, the release profile of the as-obtained EZM-nanopowder increased significantly >98% in 30 min, which indicates that a reduced drug concentration will be needed for capsules or tablets in the future and can be simply incorporated into the multidosage formulation of EZM.

Matched MeSH terms: Hypolipidemic Agents*
Fulltext Anti-Hypolipidemic and Anti-Oxidative Effects of Hydroalcoholic Extract of Origanum majorana on the Hepatosteatosis Induced with High-Fat Diet in Rats

Pasavei AG, Mohebbati R, Boroumand N, Ghorbani A, Hosseini A, Jamshidi ST, et al.

Malays J Med Sci, 2020 Feb;27(1):57-69.
PMID: 32158345 DOI: 10.21315/mjms2020.27.1.6

Introduction: The aim of the current study is to evaluate the antihyperlipidemic and anti-oxidative effects of hydro-alcoholic extract of marjoram (HAEM) in rats fed with a high-fat diet (HFD).
Methods: In the experimental study, the rats were randomly divided into four groups of five rats in each and fed with high-fat diet for 12 weeks as follows: One group (normal diet group) was fed with a standard diet, one group was fed with HFD, and two groups were fed with HFD and orally fed with 150 and 450 mg/kg/day HAEM. The serum samples and liver tissues were used for measuring the biochemical and oxidative parameters and histopathological studies. HFD induced hepatosteatosis in rats as evidenced by the altered liver enzymes activity, serum lipid profile and oxidative status.
Results: Serum lipid profile (triglyceride, cholesterol and low-density lipoprotein) in rats fed with HFD + HAEM (150 and 450 mg/kg/day) was significantly decreased. Furthermore, the evaluation of oxidative stress showed a reduction of the malondialdehyde (MDA) level and an increase in ferric-reducing anti-oxidant power. Meanwhile, liver enzyme activities declined in response to HAEM.
Conclusion: Using the HAEM could be a future therapeutic agent in treating hepatosteatosis and reducing oxidative damages of HFD in the liver.

Matched MeSH terms: Hypolipidemic Agents
Fulltext Familial hypercholesterolaemia: an updated overall management

Noor Alicezah Mohd Kasim, Chua Yung An, Hapizah Nawawi

Journal of Clinical and Health Sciences, 2020;5(2):19-38.
MyJurnal

Familial hypercholesterolaemia (FH), the commonest and serious but potentially treatable
form of inherited dyslipidaemias, is characterised by severely elevated plasma low-density
lipoprotein-cholesterol (LDL-C) level, which subsequently leads to premature coronary artery
disease (pCAD). Effectiveness of FH early detection and treatment is supported by the
outcome of several international cohort studies. Optimal FH management relies on
prescription of statins either alone or together with other lipid-lowering therapies (LLT).
Intensive lifestyle intervention is required in parallel with LLT, which should be commenced at
diagnosis in adults and childhood. Treatment with high intensity statin should be started as
soon as possible. Combination with ezetimibe and/or bile acid sequestrants is indicated if
target LDL-C is not achieved. For FH patients in the very-high risk category, if their LDL-C
targets are not achieved, despite being on maximally tolerated statin dose and ezetimibe,
proprotein convertase subtilisin/kexin type1 inhibitor (PCSK9i) is recommended. In statin
intolerance, ezetimibe alone, or in combination with PCSK9i may be considered. Clinical
evaluation of response to treatment and safety are recommended to be done about 4-6 weeks
following initiation of treatment. Homozygous FH (HoFH) patients should be treated with
maximally tolerated intensive LLT and, when available, with lipoprotein apheresis. This review
highlights the overall management, and optimal treatment combinations in FH in adults and
children, newer LLT including PCSK9i, microsomal transfer protein inhibitor, allele-specific
oligonucleotide to ApoB100 and PCSK9 mRNA. Family cascade screening and/or screening
of high-risk individuals, is the most cost-effective way of identifying FH cases and initiating
early and adequate LLT.

Matched MeSH terms: Hypolipidemic Agents
Impact of phytosterol supplementation on plasma lipoprotein(a) and free fatty acid (FFA) concentrations: A systematic review and meta-analysis of randomized controlled trials

Fatahi S, Kord-Varkaneh H, Talaei S, Mardali F, Rahmani J, Ghaedi E, et al.

Nutr Metab Cardiovasc Dis, 2019 11;29(11):1168-1175.
PMID: 31582198 DOI: 10.1016/j.numecd.2019.07.011

BACKGROUND AND AIM: Although some earlier studies have indicated the effect of phytosterol (PS) supplementation on serum lipoprotein(a) (Lp(a)) and free fatty acid (FFA) concentration, findings are still conflicting. We aimed to assess the impact of PS supplementation on serum Lp(a) and FFA concentration through a systematic review and meta-analysis of available RCTs.
METHODS AND RESULTS: We performed a systematic search of all available RCTs conducted up to 21 February 2019 in the following databases: PubMed, Scopus, and Cochrane. The choice of fixed- or random-effect model for analysis was determined according to the I2 statistic. Effect sizes were expressed as weighted mean difference (WMD) and 95% confidence interval (CI). Pooling of 12 effect sizes from seven articles revealed a significant reduction of Lp(a) levels following PS supplementation (MD: -0.025 mg/dl, 95% CI: -0.045, -0.004, p = 0.017) without significant heterogeneity among the studies (I2 = 0.0%, p = 0.599). Also, PS supplementation significantly lowered FFA (MD: -0.138 mg/dl, 95% CI: -0.195, -0.081, p = 0.000) without significant heterogeneity among the studies (I2 = 0.0%, p = 0.911). The results for meta-regression and sensitivity analysis were not significant.
CONCLUSION: The meta-analysis suggests that oral PS supplementation could cause a significant reduction in serum Lp(a) and FFA.

Matched MeSH terms: Hypolipidemic Agents/adverse effects; Hypolipidemic Agents/therapeutic use*
Hylocereus polyrhizus peel's high-methoxyl pectin: A potential source of hypolipidemic agent

Zaid RM, Mishra P, Wahid ZA, Sakinah AMM

Int J Biol Macromol, 2019 Aug 01;134:361-367.
PMID: 31059740 DOI: 10.1016/j.ijbiomac.2019.03.143

In the present study, high-methoxyl pectin (HMP) was extracted from Hylocereus polyrhizus peel's using physico-chemical process. In addition, the hypolipidemic activity of HMP was investigated at different concentration and time corresponding to its adsorption ability. FTIR and contact angle analysis were used to determine the sorbent characterization. A high degree of esterification (63.8%) and the contact angle (95.5°) confirmed hydrophobic nature and resulting bad wetting of the HMP extract, respectively. The methoxyl content in the pectin acted as an affinity-precursor of the pectin towards cholesterol due to its increased hydrophobicity. The maximum equilibrium uptake capacity of cholesterol of 370.5mg/g (0.96mmol/g) was observed by HMP. The experimental data showed good fitting for Freundlich isotherm equation and followed pseudo-first-order kinetic model with a correlation coefficient (R2) of 0.89-0.97 due to physisorption mechanism. Intra-particle model confirmed that the cholesterol sorption rate by HMP was significantly influenced by external mass transfer (surface diffusion) and intra-particle diffusion (diffusion control). It was also revealed that the HMP extracted from Hylocereus polyrhizus peels possess a high affinity towards cholesterol, making it an ideal hypolipidemic agent.

Matched MeSH terms: Hypolipidemic Agents/pharmacology*; Hypolipidemic Agents/chemistry*
Guggulsterone, a farnesoid X receptor antagonist lowers plasma trimethylamine-N-oxide levels: An evidence from in vitro and in vivo studies

Gautam A, Paudel YN, Abidin S, Bhandari U

Hum Exp Toxicol, 2019 Mar;38(3):356-370.
PMID: 30526076 DOI: 10.1177/0960327118817862

The current study investigated the role of guggulsterone (GS), a farnesoid X receptor antagonist, in the choline metabolism and its trimethylamine (TMA)/flavin monooxygenases/trimethylamine-N-oxide (TMAO) inhibiting potential in a series of in vitro and in vivo studies as determined by high-performance liquid chromatography (HPLC), mass spectroscopy (MS), and liquid chromatography (LC)-MS techniques. Atherosclerosis (AS) was successfully induced in a group of experimental animals fed with 2% choline diet for 6 weeks. Serum lipid profiles such as total cholesterol, triglycerides, low-density lipoprotein cholesterol, high-density lipoprotein cholesterol, and very low-density lipoprotein cholesterol were measured. Pro-inflammatory cytokines levels, markers for a hepatic injury, and oxidative stress markers were assessed. Interestingly, GS reduced the level of TMA/TMAO in both in vitro and in vivo studies as demonstrated by the peaks obtained from HPLC, MS, and LC-MS. Furthermore, GS exhibited cardioprotective and antihyperlipidemic effects as evidenced by the attenuation of levels of several serum lipid profiles and different atherogenic risk predictor indexes. GS also prevented hepatic injury by successfully restoring the levels of hepatic injury biomarkers to normal. Similarly, GS inhibited the production of pro-inflammatory cytokines levels, as well as GS, enhanced antioxidant capacity, and reduced lipid peroxidation. Histopathological study of aortic sections demonstrated that GS maintained the normal architecture in AS-induced rats. On the basis of results obtained from current investigation, we suggest that GS might have a great therapeutic potential for the treatment of AS.

Matched MeSH terms: Hypolipidemic Agents/pharmacology*
Fulltext Effects of Non-statin Lipid-Modifying Agents on Cardiovascular Morbidity and Mortality Among Statin-Treated Patients: A Systematic Review and Network Meta-Analysis

Chaiyasothi T, Nathisuwan S, Dilokthornsakul P, Vathesatogkit P, Thakkinstian A, Reid C, et al.

Front Pharmacol, 2019;10:547.
PMID: 31191304 DOI: 10.3389/fphar.2019.00547

Background: Currently, there is a lack of information on the comparative efficacy and safety of non-statin lipid-lowering agents (NST) in cardiovascular (CV) disease risk reduction when added to background statin therapy (ST). This study determine the relative treatment effects of NST on fatal and non-fatal CV events among statin-treated patients. Methods: A network meta-analysis based on a systematic review of randomized controlled trials (RCTs) comparing non-statin lipid-modifying agents among statin-treated patients was performed. PubMed, EMBASE, CENTRAL, and Clinicaltrial.gov were searched up to April 10, 2018. The primary outcomes were CV and all-cause mortalities. Secondary CV outcomes were coronary heart disease (CHD) death, non-fatal myocardial infarction (MI), any stroke, and coronary revascularization. Risks of discontinuations were secondary safety outcomes. Results: Sixty-seven RCTs including 259,429 participants with eight interventions were analyzed. No intervention had significant effects on the primary outcomes (CV mortality and all-cause mortality). For secondary endpoints, proprotein convertase subtilisin/kexin type 9 inhibitor (PCSK) plus statin (PCSK/ST) significantly reduced the risk of non-fatal MI (RR 0.82, 95% CI 0.72-0.93, p = 0.003), stroke (RR 0.74, 95% CI 0.65-0.85, p < 0.001), coronary revascularization (RR 0.84, 95% CI 0.75-0.94, p = 0.003) compared to ST. Combinations of ST and all NST except PCSK and ezetimibe showed higher rate of discontinuation due to adverse events compared to ST. Conclusions: None of NST significantly reduced CV or all-cause death when added to ST. PCSKs and to a lesser extent, ezetimibe may help reduce cardiovascular events with acceptable tolerability profile among broad range of patients.

Matched MeSH terms: Hypolipidemic Agents
Therapeutic potential of Artemisia vulgaris: An insight into underlying immunological mechanisms

Soon L, Ng PQ, Chellian J, Madheswaran T, Panneerselvam J, Gupta G, et al.

J Environ Pathol Toxicol Oncol, 2019;38(3):205-216.
PMID: 31679308 DOI: 10.1615/JEnvironPatholToxicolOncol.2019029397

Artemisia vulgaris is a traditional Chinese herb believed to have a wide range of healing properties; it is traditionally used to treat numerous health ailments. The plant is commonly called mugwort or riverside wormwood. The plant is edible, and in addition to its medicinal properties, it is also used as a culinary herb in Asian cooking in the form of a vegetable or in soup. The plant has garnered the attention of researchers in the past few decades, and several research studies have investigated its biological effects, including antioxidant, anti-inflammatory, anticancer, hypolipidemic, and antimicrobial properties. In this review, various studies on these biological effects are discussed along with the tests conducted, compounds involved, and proposed mechanisms of action. This review will be of interest to the researchers working in the field of herbal medicine, pharmacology, medical sciences, and immunology.

Matched MeSH terms: Hypolipidemic Agents/pharmacology
The hypolipidemic effects of Tamarindus indica fruit pulp extract in normal and diet-induced hypercholesterolemic hamsters are associated with altered levels of serum proteins

Lim CY, Junit SM, Aziz AA, Jayapalan JJ, Hashim OH

Electrophoresis, 2018 12;39(23):2965-2973.
PMID: 30280388 DOI: 10.1002/elps.201800258

The hypolipidemic effects of Tamarindus indica fruit pulp extract (Ti-FPE) have been earlier reported but the underlying molecular mechanisms are still uncertain. In this study, hamsters fed with Ti-FPE, both in the absence and presence of high-cholesterol diet, were shown to have significantly reduced levels of serum triglyceride, LDL-C and total cholesterol. The Ti-FPE-fed non-hypercholesterolemic hamsters also showed significant enhanced levels of serum apolipoprotein A1, antithrombin III, transferrin and vitamin D binding protein. In diet-induced hypercholesterolemic hamsters, apolipoprotein A1, antithrombin III and transferrin, which were relatively low in levels, became significantly enhanced when the hamsters were fed with Ti-FPE. These Ti-FPE-fed hypercholesterolemic hamsters also showed significant higher levels of serum vitamin D binding protein. When the different treated groups of hamsters were analyzed for the levels of the four serum proteins by ELISA, similar altered abundance were detected. Ingenuity Pathway Analysis of the Ti-FPE modulated serum proteins singled out "Lipid metabolism, molecular transport, small molecule biochemistry" as the top network. Our results suggest that the hypolipidemic effects of Ti-FPE are associated with alterations of serum proteins that are known to be cardioprotective and involved in the metabolism of lipids. The MS data have been deposited to the ProteomeXchange Consortium with the dataset identifier PXD010232.

Matched MeSH terms: Hypolipidemic Agents/pharmacology*; Hypolipidemic Agents/chemistry
Updates in the management of Dyslipidaemia in the high and very high risk individual for CV risk reduction

Jeyamalar R, Wan Azman WA, Nawawi H, Choo GH, Ng WK, Rosli MA, et al.

Med J Malaysia, 2018 06;73(3):154-162.
PMID: 29962499 MyJurnal

Cardiovascular disease (CVD) has been the main cause of mortality and an important cause of morbidity in Malaysia for several years. To reduce global cardiovascular (CV) risk in the population, primary preventive strategies need to be implemented. Hypercholesterolaemia is one of the major risk factors for CVD. This paper is an expert review on the management of hypercholesterolemia focusing on high and very high risk individuals. In low and Intermediate risk individuals, therapeutic lifestyle changes (TLC) and a healthy lifestyle alone may suffice. In high and very high risk individuals, drug therapy in conjunction with TLC are necessary to achieve the target LDL-C levels which have been shown to slow down progression and sometimes even result in regression of atherosclerotic plaques. Statins are first-line drugs because they have been shown in numerous randomized controlled trials to be effective in reducing CV events and to be safe. In some high risk individuals, despite maximally tolerated statin therapy, target Low Density Lipoprotein Cholesterol (LDL-C) levels are not achieved. These include those with familial hypercholesterolaemia and statin intolerance. This paper discusses non-statin therapies, such as ezetimibe and the newer Proprotein convertase subtilisin/kexin type 9 Inhibitors (PCSK9-i).

Matched MeSH terms: Hypolipidemic Agents/therapeutic use
Prevalence, factors influencing and knowledge about adherence to lipid-lowering therapy among hyperlipidemia patients

Devaraj NK, Mohamed M, Hussein N

Med J Malaysia, 2017 06;72(3):157-164.
PMID: 28733563 MyJurnal

BACKGROUND: Hyperlipidaemia is a significant risk factor for cardiovascular disease. However, adherence to lipidlowering therapy is often unsatisfactory due to a combination of patient factors, therapy, socio-economic and health system-related factors.
AIMS: to identify the prevalence of adherence to lipidlowering therapy, the factors contributing to non-adherence and knowledge regarding hyperlipidaemia and its' treatment among Malaysian patients with hyperlipidemia.
METHODS: A quantitative study using a cross-sectional survey was carried out in an urban primary care clinic in August 2015. Patients on lipid-lowering therapy for ≥ 1 year aged ≥ 18 years were selected using simple random sampling. consenting patients answered a selfadministered questionnaire (in Malay/English) which included socio-demographic profile, hyperlipidaemia profile, adherence to lipid-lowering therapy (using the Morisky Medication Adherence scale-8; score ≥ 6 taken as adherent), reasons leading to non-adherence, knowledge regarding hyperlipidaemia and its' treatment, and use of non-allopathic medicine.
RESULTS: the response rate was 90.7%. the prevalence of adherence to lipid-lowering therapy was 82.4%. "the most common reasons for non-adherence was being worried about side effect of lipid-lowering agent (71.4%), followed by the need to take too many drugs in a day (61.4%) and negative influences by friends, relative and mass media (60%)". Factors associated with non-adherence include male gender, on longer duration of therapy, less frequency of follow-up, less number of follow-up clinics, taking medication at night/random timing and having lower knowledge scores.
CONCLUSION: Overall the prevalence of adherence was high in patients with hyperlipidaemia. Interventions to boost adherence should target those who were identified as nonadherent.

Matched MeSH terms: Hypolipidemic Agents/therapeutic use*
Fulltext Evaluation of medication use in Malaysian predialysis patients

Salman M, Khan AH, Adnan AS, Syed Sulaiman SA, Shehzadi N, Asif N, et al.

Saudi J Kidney Dis Transpl, 2017 5 26;28(3):517-523.
PMID: 28540887 DOI: 10.4103/1319-2442.206451

Chronic kidney disease (CKD) patients suffer from multiple comorbidities and complications as a cause or consequence of kidney disease. Information regarding medication- prescribing patterns in predialysis patients is sparse. We conducted a retrospective study to evaluate the medication prescription patterns among predialysis patients. Medical records (both paper based and computerized) of patients at CKD Resource Centre, Hospital Universiti Sains Malaysia, were reviewed. A total of 615 eligible cases were included in the study. The mean number of medications prescribed per patient was 8.22 ± 2.81, and medication use was correlated to the renal function (stage 3a < stage 3b < stage 4 < stage 5; P <0.001). The top three prescribed medication groups were found to be lipid-lowering agents, calcium channel blockers, and antiplatelet agents. Some medication classes such as nonaluminum/noncalcium phosphate binders, erythropoietin-stimulating agents, and renin-angiotensin-aldosterone system blockers, particularly in advanced stage, were found to be underutilized. In conclusion, predialysis patients are prescribed a large number of medications. Our findings highlight the need for assessing the impact of current medication-prescribing patterns on morbidity and mortality rates in Malaysian predialysis population.

Matched MeSH terms: Hypolipidemic Agents/therapeutic use*
Antioxidative and Inhibitory Effects of the Fruiting Body of Black Lingzhi Mushroom, Amauroderma rugosum (Agaricomycetes), on LDL Oxidation and HMG-CoA Reductase Activity

Seng CK, Abdullah N, Aminudin N

Int J Med Mushrooms, 2017;19(9):797-807.
PMID: 29199554 DOI: 10.1615/IntJMedMushrooms.2017024374

Amauroderma rugosum fruiting bodies possess excellent cardiovascular benefits, including antioxidative, antihyperlipidemic, antihypertensive, antiinflammatory, anti-platelet aggregation, and antithrombotic effects. In this article, we describe our investigations of the in vitro antioxidant activity and in vitro antiatherosclerotic potential through inhibitory effects on low-density lipoprotein (LDL), LDL peroxidation, and 3-hydroxy3-methylglutaryl-coenzyme A (HMG-CoA) reductase catalytic activity using various fruiting body extracts partitioned with an organic solvent. Among 5 extracts/fractions tested, the semipolar ethyl acetate (EA) fraction demonstrated good antioxidant capacity based on total phenolic content, 2,2-diphenyl-1-picrylhydrazyl free radical scavenging, ferrous ion-chelating ability, cupric ion-reducing antioxidant capacity, and lipid peroxidation assays. The EA fraction also showed the strongest inhibitory effect on Cu2+-induced LDL oxidation via thiobarbituric acid reactive substances formation and HMG-CoA reductase activity. Chemical analysis conjointly identified 10 phenolic compounds (4 benzoic acid derivatives, 3 flavonoids, 1 cinnamic acid, 1 hexahydroxydiphenic acid dilactone, and 1 xanthone derivative), some of which play pivotal roles in arresting the physiopathogenesis of atherosclerosis, thereby attenuating the risk of cardiovascular events occurring.

Matched MeSH terms: Hypolipidemic Agents/pharmacology
Caffeoylquinic Acids Rich versus Poor Fractions of Gynura procumbens: Their Comparative Antihyperlipidemic and Antioxidant Potential

Murugesu K, Murugaiyah V, Saghir SAM, Asmawi MZ, Sadikun A

Curr Pharm Biotechnol, 2017;18(14):1132-1140.
PMID: 29564975 DOI: 10.2174/1389201019666180322111800

BACKGROUND: Ethanolic extract of G. procumbens leaves has been previously shown to possess antihyperlipidemic effects.
OBJECTIVE: This study was designed to prepare caffeoylquinic acids rich and poor fractions of the ethanolic extract using resin column technology and compare their antihyperlipidemic and antioxidant potentials.
RESULTS: Among the treatment groups, caffeoylquinic acids rich fraction (F2) and chlorogenic acid (CA, one of the major caffeoylquinic acids) showed potent antihyperlipidemic effects, with significant reductions in total cholesterol (TC), triglycerides (TG), low-density lipoprotein-cholesterol (LDL-C), very low-density lipoprotein-cholesterol (VLDL-C), atherogenic index (AI) and coronary risk index (CRI) (p<0.01 or better) compared to the hyperlipidemic control at the 58 h. The effect was better than that of ethanolic extract. In addition, only F2 significantly increased the high-density lipoproteincholesterol (HDL-C) level (p<0.05). F2 showed better effect than CA alone (60 mg) despite the fact that it only contained 9.81 mg CA/1000 mg dose. The findings suggest that the di-caffeoylquinic acids (86.61 mg/g dose) may also in part be responsible for the potent antihyperlipidemic effect shown by the F2. Likewise, F2 showed the highest antioxidant activity. Thus, simple fractionation of ethanolic extract using the Amberlite XAD-2 resin technique had successfully enriched the caffeoylquinic acids into F2 with improved antihyperlipidemic and antioxidant capacities than that of the ethanolic extract.
CONCLUSION: The resin separation technology may find application in caffeoylquinic acids enrichment of plant extracts for pre-clinical studies. The F2 has potential for development into phytopharmaceuticals as adjunct therapy for management of hyperlipidemia.

Matched MeSH terms: Hypolipidemic Agents/isolation & purification; Hypolipidemic Agents/pharmacology*; Hypolipidemic Agents/therapeutic use
Defining metabolic syndrome and factors associated with metabolic syndrome in a poly-pharmaceutical population

McStea M, McGeechan K, Kamaruzzaman SB, Rajasuriar R, Tan MP

Postgrad Med, 2016 Nov;128(8):797-804.
PMID: 27558757 DOI: 10.1080/00325481.2016.1229103

Metabolic Syndrome (METs) definitions vary and diagnosis takes into account consumption of medications commonly prescribed for conditions defining METs. This paper evaluates the potential differences in population characteristics using two different methods of defining METs, with and without the adjustment of the effects of pharmacotherapy on biochemical and blood pressure (BP) measurements Methods: This was a cross-sectional study utilizing the Malaysian Elders Longitudinal Research (MELoR) cohort comprising urban community-dwellers aged ≥55 years. Participants were interviewed using a structured questionnaire during home visits where medications were reviewed. Health impacts assessed included heart disease, stroke, body mass index (BMI), peptic ulcers, arthritis, and number of medications and comorbidities. Risk factors and health impacts associated with METs were determined by Poisson multivariate regression models using a binary and count dependent variables.

Matched MeSH terms: Hypolipidemic Agents/administration & dosage*
Messages from the Malaysian Diabetes Registries on Diabetes Care in Malaysian public healthcare facilities

Chew BH, Lee PY, Cheong AT, Ismail M, Shariff-Ghazali S, Goh PP

Prim Care Diabetes, 2016 10;10(5):383-6.
PMID: 27459893 DOI: 10.1016/j.pcd.2016.07.003

A persistent and increasing prevalence of diagnosed and undiagnosed diabetes mellitus has recently been reported in the National Health and Morbidity Survey 2015. This commentary recapitulates the relevant and valuable lessons in the Malaysian national diabetes registries to inform the healthcare stakeholders and policy makers on potential areas of clinical practice improvement and future researches. Under performance of the process measures and sub-optimal control of HbA1c, blood pressure and lipids profile were prevalent (<40% achieved treatment targets). Although these had improved slightly from 2009 to 2012, diabetes co-morbidities (hypertension and dyslipidaemia) and complications had also increased. Prevalence of insulin use had doubled, and lipid lowering agent use had increased about 50% in 2012 compared to 2009. We identified six clinical areas for urgent attention and improvement, and three potential areas for future research.

Matched MeSH terms: Hypolipidemic Agents/therapeutic use
Fulltext Hypolipidemic activities of xanthorrhizol purified from centrifugal TLC

Oon SF, Nallappan M, Kassim NK, Shohaimi S, Sa'ariwijaya MS, Tee TT, et al.

Biochem Biophys Res Commun, 2016 09 23;478(3):1403-8.
PMID: 27576204 DOI: 10.1016/j.bbrc.2016.08.136

Hyperlipidemia is defined as the presence of either hypertriglyceridemia or hypercholesterolemia, which could cause atherosclerosis. Although hyperlipidemia can be treated by hypolipidemic drugs, they are limited due to lack of effectiveness and safety. Previous studies demonstrated that xanthorrhizol (XNT) isolated from Curcuma xanthorrhizza Roxb. reduced the levels of free fatty acid and triglyceride in vivo. However, its ability to inhibit cholesterol uptake in HT29 colon cells and adipogenesis in 3T3-L1 cells are yet to be reported. In this study, XNT purified from centrifugal TLC demonstrated 98.3% purity, indicating it could be an alternative purification method. The IC50 values of XNT were 30.81 ± 0.78 μg/mL in HT29 cells and 35.07 ± 0.24 μg/mL in 3T3-L1 adipocytes, respectively. Cholesterol uptake inhibition study using HT29 colon cells showed that XNT (15 μg/mL) significantly inhibited the fluorescent cholesterol analogue NBD uptake by up to 27 ± 3.1% relative to control. On the other hand, higher concentration of XNT (50 μg/mL) significantly suppressed the growth of 3T3-L1 adipocytes (5.9 ± 0.58%) compared to 3T3-L1 preadipocytes (81.31 ± 0.55%). XNT was found to impede adipogenesis of 3T3-L1 adipocytes in a dose-dependent manner from 3.125 to 12.5 μg/mL, where 12.5 μg/mL significantly suppressed 36.13 ± 2.1% of lipid accumulation. We postulate that inhibition of cholesterol uptake, adipogenesis, preadipocyte and adipocyte number may be utilized as treatment modalities to reduce the prevalence of lipidemia. To conclude, XNT could be a potential hypolipidemic agent to improve cardiovascular health in the future.

Matched MeSH terms: Hypolipidemic Agents/isolation & purification*; Hypolipidemic Agents/pharmacology*; Hypolipidemic Agents/chemistry
Effects of Labisia pumila var alata extracts on the lipid profile, serum antioxidant status and abdominal aorta of high-cholesterol diet rats

Dianita R, Jantan I, Jalil J, Amran AZ

Phytomedicine, 2016 Jul 15;23(8):810-7.
PMID: 27288916 DOI: 10.1016/j.phymed.2016.04.004

BACKGROUND: Previous studies on Labisia pumila var. alata (LPva) have showed that it could inhibit low-density lipoprotein (LDL) oxidation and provide protection on myocardial infarction in rats.
HYPOTHESIS/PURPOSE: We hypothesized that LPva extracts can modulate the lipid profiles and serum antioxidant status of hypercholesterolemic rats. In the present study, we investigated the effects of aqueous and 80% ethanol extracts of LPva on atherogenic and serum antioxidant parameters as well as changes in abdominal aorta of high-cholesterol diet rats.
METHODS: The major components of the extracts, gallic acid, flavonoids and alkyl resorcinols were analyzed by using a validated reversed phase HPLC method. The rats were induced to hypercholesterolemic status with daily intake of 2% cholesterol for a duration of 8 weeks. Three different doses (100, 200 and 400mg/kg) of the extracts were administered daily on the 4th week onwards. The rats were then sacrificed and the blood was collected via abdominal aorta and serum was separated by centrifugation for biochemical analysis. Part of the aorta tissues were excised immediately for histopathological examination.
RESULTS: The serum of LPva treated rats showed significant reduction in serum aspartate aminotransferase (AST), alanine aminotransferase (ALT) and lactate dehydrogenase (LDH) levels and the abdominal aorta showed a significant decrease of atheroma lesions in treated rats. Serum lipid profiles of treated rats showed a decrease in total cholesterol, total triglycerides and low-density lipoprotein (LDL) levels as compared to control group. The atherogenic indices in treated rats were significantly improved along with an increasing level of serum high-density lipoprotein (HDL). The extracts also exhibited significant increase of antioxidant enzymes and decrease of MDA as a product of lipid peroxidation.
CONCLUSION: LPva extracts can reduce the risk of dyslipidemia by improving the serum lipid profiles and modulating serum antioxidants.

Matched MeSH terms: Hypolipidemic Agents/pharmacology*

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