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  1. 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
  2. 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
  3. Fulltext The statin studies: from targeting hypercholesterolaemia to targeting the high-risk patient
    Ong HT
    QJM, 2005 Aug;98(8):599-614.
    PMID: 16006501
    The landmark HMG-CoA reductase inhibitor (statin) studies have practical lessons for clinicans. The 4S trial established the importance of treating the hypercholesterolaemic patient with cardiovascular heart disease. Next, WOSCOPS showed the benefit of treating healthy, high-risk hypercholesterolaemic men. CARE, a secondary prevention trial, showed the benefit of treating patients with cholesterol levels within normal limits. This was confirmed by the LIPID trial, another secondary prevention study, which enrolled patients with cholesterol levels 155-271 mg/dl (4-7 mmol/l). The importance of treating patients with established ischaemic heart disease, and those at high risk of developing heart disease, regardless of cholesterol level, was being realized. In the MIRACL trial, hypocholesterolaemic therapy was useful in the setting of an acute coronary syndrome, while the AVERT study showed that aggressive statin therapy is as good as angioplasty in reducing ischaemic events in patients with stable angina. By showing the value of fluvastatin after percutaneous intervention, LIPS confirmed that benefit is a class action of the statins. The HPS randomized over 20 000 patients, and showed beyond doubt the value of statins in reducing cardiovascular events in the high-risk patient. Although PROSPER showed benefit in treating the elderly patients above 70 years, statin therapy in this trial was associated with an increase in cancer incidence. The comparative statin trials, PROVE-IT, REVERSAL, Phase Z of the A to Z, ALLIANCE and TNT, all showed that high-dose statins will better reduce cardiovascular events in the high-risk patient, although the adverse effects of therapy will also be increased. ALLHAT-LLT, ASCOT-LLA and CARDS showed that for statin therapy to demonstrate a significant benefit, hypertensive or diabetic patients must be at sufficiently high risk of cardiovascular events. The emphasis is now on the risk level for developing cardiovascular events, and treatment should target the high-risk group and not the lipid level of the patient. No therapy is free of adverse effect. Treatment of those most at risk will bring the most benefit; treatment of those not at high risk of cardiovascular disease may expose patients who would not benefit much from therapy to its adverse effects.
    Matched MeSH terms: Hypolipidemic Agents/administration & dosage; Hypolipidemic Agents/therapeutic use*
  4. The influence of fenofibrate on lipid profile, endothelial dysfunction, and inflammatory markers in type 2 diabetes mellitus patients with typical and mixed dyslipidemia
    Ghani RA, Bin Yaakob I, Wahab NA, Zainudin S, Mustafa N, Sukor N, et al.
    J Clin Lipidol, 2013 Sep-Oct;7(5):446-53.
    PMID: 24079286 DOI: 10.1016/j.jacl.2013.04.004
    BACKGROUND: Type 2 diabetes is associated with early development of endothelial dysfunction. Patients present with typical dyslipidemia (predominantly high levels of triglycerides [TG] and low levels of high-density lipoprotein cholesterol [HDL-C]) or mixed hypercholesterolemia (high levels of low-density lipoprotein cholesterol [LDL-C] and TG with low HDL-C). Normal levels include LDL-C < 100 mg/dL, TG < 135 mg/dL, and HDL-C > 40 mg/dL for men and >50 mg/dL for women.
    OBJECTIVE: To determine the effects of 8 weeks' administration of fenofibrate on inflammatory markers, metabolic parameters, and endothelial dysfunction.
    METHODS: We administered micronized fenofibrate (Laboratories Fourneir S.A Dijon, France) daily for 8 weeks to 40 dyslipidemic, type 2 diabetes patients with equal numbers in each arm of the typical or mixed dyslipidemia groups. Noninvasive endothelial function assessments were performed and serum inflammatory markers obtained before and after treatment.
    RESULTS: The typical group demonstrated significantly greater TG reduction and HDL-C increment, ie, 56% vs, 21.3% (P < .005) and 21% vs. 7.6% (P = .001), respectively, compared with the mixed group. There was greater LDL-C reduction within the mixed group compared with the typical group 21.0% vs. 2.2% (P < .05). Endothelial dysfunction was present in both groups at baseline. After treatment, the typical group demonstrated significant improvement in resting brachial diameter (3.9 mm [interquartile range {IQR} 3.3-4.7] to 4.2 mm [IQR 3.4-4.8], P = .001) compared with no change within the mixed group (3.6 mm [IQR 3.1-5.4] to 3.7 mm [IQR 3.1-5.3], P = .26). Flow-mediated diameter improved significantly in both groups. The mixed group had significantly greater levels of hs-CRP at baseline but no changes throughout the study. The mixed group demonstrated an increase in vascular adhesion molecule-1 from 706 ng/mL (IQR 566-1195) to 845 ng/mL (637-1653; P = .01), a reduction of tumor necrosis factor-α from 7.0 pg/mL (IQR 1.0-43.5) to 2.5 pg/mL (IQR 1.5-13.5; P = .04) throughout the study.
    CONCLUSIONS: We effectively compared 8 weeks of fenofibrate therapy in type 2 diabetics with contrasting lipid abnormalities. The typical dyslipidemia group showed significantly greater lipid improvements compared with the mixed dyslipidemia group. Both groups had improvements in endothelial functions that were independent of the lipid levels. We concluded that fibrate therapy in type 2 diabetics is beneficial, especially those with typical dyslipidemia and extends beyond its lipid lowering properties.
    KEYWORDS: Endothelial dysfunction; Fenofibrate; High-density lipoprotein cholesterol; Low density lipoprotein; Noninvasive endothelial function assessments; Triglyceride; Vascular cell adhesion molecule-1; hsCRP
    Matched MeSH terms: Hypolipidemic Agents/pharmacology*; Hypolipidemic Agents/therapeutic use
  5. 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
  6. Sargassum polycystum reduces hyperglycaemia, dyslipidaemia and oxidative stress via increasing insulin sensitivity in a rat model of type 2 diabetes
    Motshakeri M, Ebrahimi M, Goh YM, Matanjun P, Mohamed S
    J Sci Food Agric, 2013 May;93(7):1772-8.
    PMID: 23208488 DOI: 10.1002/jsfa.5971
    BACKGROUND: Sargassum polycystum, a brown seaweed, contains various nutrients and bioactive compounds that have antioxidant and healing properties. The research hypothesises that antioxidants and pigments in dietary S. polycystum extracts can improve insulin sensitivity, blood sugar levels and blood lipid levels in a rat model of type 2 diabetes. The diabetes was induced by a high-sugar, high-fat diet for 16 weeks to enhance insulin resistance, followed by a low-dose intraperitoneal injection of streptozotocin (35 mg kg(-1) body weight). The doses of S. polycystum tested on diabetic rats were 150 and 300 mg kg(-1) body weight for the ethanolic extract or 150 and 300 mg kg(-1) for the water extract. Normal rats, untreated diabetic and metformin-treated diabetic rats (n = 6) were used as control.

    RESULTS: Both doses of the alcohol extract of S. polycystum and the 300 mg kg(-1) water extract, significantly reduced blood glucose and glycosylated haemoglobin (HbA1C ) levels. Serum total cholesterol, triglyceride levels and plasma atherogenic index were significantly decreased after 22 days treatment in all seaweed groups. Unlike metformin, S. polycystum did not significantly change plasma insulin in the rats, but increased the response to insulin.

    CONCLUSION: The consumption of either ethanolic or water extracts of S. polycystum dose dependently reduced dyslipidaemia in type 2 diabetic rats. S. polycystum is a potential insulin sensitiser, for a comestible complementary therapy in the management of type 2 diabetes which can help reduce atherogenic risk.

    Matched MeSH terms: Hypolipidemic Agents/pharmacology; Hypolipidemic Agents/therapeutic use*
  7. Fulltext Rhabdomyolysis and acute renal failure following a switchover of therapy between two fibric acid derivatives
    Kamaliah MD, Sanjay LD
    Singapore Med J, 2001 Aug;42(8):368-72.
    PMID: 11764054
    Drug induced myopathy has been reported with the use of fibric acid derivatives, hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors and nicotinic acid. Over the last three decades, hypolipemiants like fibric acid derivatives and statins have been increasingly recognised as causes of rhabdomyolysis and acute renal failure especially during combination therapy and in the presence of underlying renal impairment. We report two cases of bezafibrate-induced rhabdomyolysis in patients with underlying coronary artery disease and pre-existing renal impairment. Both patients developed rhabdomyolysis leading to acute renal failure soon after their hyperlipidaemia treatment was changed from gemfibrozil to bezafibrate. There were no intercurrent illnesses or co-administration of other lipid lowering drugs in both patients. Even though both drugs belong to the same fibric acid derivatives group, these patients developed the complication only after a switchover of therapy.
    Matched MeSH terms: Hypolipidemic Agents/adverse effects*
  8. 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*
  9. Fulltext Poor glycemic control in younger women attending Malaysian public primary care clinics: findings from adults diabetes control and management registry
    Cheong AT, Lee PY, Sazlina SG, Mohamad Adam B, Chew BH, Mastura I, et al.
    BMC Fam Pract, 2013;14:188.
    PMID: 24325794 DOI: 10.1186/1471-2296-14-188
    BACKGROUND: Women of reproductive age are a group of particular concern as diabetes may affect their pregnancy outcome as well as long-term morbidity and mortality. This study aimed to compare the clinical profiles and glycemic control of reproductive and non-reproductive age women with type 2 diabetes (T2D) in primary care settings, and to determine the associated factors of poor glycemic control in the reproductive age group women.
    METHODS: This was a cross-sectional study using cases reported by public primary care clinics to the Adult Diabetes Control and Management registry from 1st January to 31st December 2009. All Malaysian women aged 18 years old and above and diagnosed with T2D for at least 1 year were included in the analysis. The target for glycemic control (HbA1c < 6.5%) is in accordance to the recommended national guidelines. Both univariate and multivariate approaches of logistic regression were applied to determine whether reproductive age women have an association with poor glycemic control.
    RESULTS: Data from a total of 30,427 women were analyzed and 21.8% (6,622) were of reproductive age. There were 12.5% of reproductive age women and 18.0% of non-reproductive age women that achieved glycemic control. Reproductive age group women were associated with poorer glycemic control (OR = 1.5, 95% CI = 1.2-1.8). The risk factors associated with poor glycemic control in the reproductive age women were being of Malay and Indian race, longer duration of diabetes, patients on anti-diabetic agents, and those who had not achieved the target total cholesterol and triglycerides.
    CONCLUSION: Women with T2D have poor glycemic control, but being of reproductive age was associated with even poorer control. Health care providers need to pay more attention to this group of patients especially for those with risk factors. More aggressive therapeutic strategies to improve their cardiometabolic control and pregnancy outcome are warranted.
    Matched MeSH terms: Hypolipidemic Agents/therapeutic use
  10. Pharmaceutical, cosmeceutical, and traditional applications of marine carbohydrates
    Ahmed AB, Adel M, Karimi P, Peidayesh M
    Adv. Food Nutr. Res., 2014;73:197-220.
    PMID: 25300548 DOI: 10.1016/B978-0-12-800268-1.00010-X
    Marine carbohydrates are most important organic molecules made by photosynthetic organisms. It is very essential for humankind: the role in being an energy source for the organism and they are considered as an important dissolve organic compound (DOC) in marine environment's sediments. Carbohydrates found in different marine environments in different concentrations. Polysaccharides of carbohydrates play an important role in various fields such as pharmaceutical, food production, cosmeceutical, and so on. Marine organisms are good resources of nutrients, and they are rich carbohydrate in sulfated polysaccharide. Seaweeds (marine microalgae) are used in different pharmaceutical industries, especially in pharmaceutical compound production. Seaweeds have a significant amount of sulfated polysaccharides, which are used in cosmeceutical industry, besides based on the biological applications. Since then, traditional people, cosmetics products, and pharmaceutical applications consider many types of seaweed as an important organism used in food process. Sulfated polysaccharides containing seaweed have potential uses in the blood coagulation system, antiviral activity, antioxidant activity, anticancer activity, immunomodulating activity, antilipidepic activity, etc. Some species of marine organisms are rich in polysaccharides such as sulfated galactans. Various polysaccharides such as agar and alginates, which are extracted from marine organisms, have several applications in food production and cosmeceutical industries. Due to their high health benefits, compound-derived extracts of marine polysaccharides have various applications and traditional people were using them since long time ago. In the future, much attention is supposed to be paid to unraveling the structural, compositional, and sequential properties of marine carbohydrate as well.
    Matched MeSH terms: Hypolipidemic Agents
  11. 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
  12. Lipid-lowering treatment in hypercholesterolaemic patients: the CEPHEUS Pan-Asian survey
    Park JE, Chiang CE, Munawar M, Pham GK, Sukonthasarn A, Aquino AR, et al.
    Eur J Prev Cardiol, 2012 Aug;19(4):781-94.
    PMID: 21450606 DOI: 10.1177/1741826710397100
    BACKGROUND: Treatment of hypercholesterolaemia in Asia is rarely evaluated on a large scale, and data on treatment outcome are scarce. The Pan-Asian CEPHEUS study aimed to assess low-density lipoprotein cholesterol (LDL-C) goal attainment among patients on lipid-lowering therapy.
    METHODS: This survey was conducted in eight Asian countries. Hypercholesterolaemic patients aged ≥18 years who had been on lipid-lowering treatment for ≥3 months (stable medication for ≥6 weeks) were recruited, and lipid concentrations were measured. Demographic and other clinically relevant information were collected, and the cardiovascular risk of each patient was determined. Definitions and criteria set by the updated 2004 National Cholesterol Education Program guidelines were applied.
    RESULTS: In this survey, 501 physicians enrolled 8064 patients, of whom 7281 were included in the final analysis. The mean age was 61.0 years, 44.4% were female, and 85.1% were on statin monotherapy. LDL-C goal attainment was reported in 49.1% of patients overall, including 51.2% of primary and 48.7% of secondary prevention patients, and 36.6% of patients with familial hypercholesterolaemia. The LDL-C goal was attained in 75.4% of moderate risk, 55.4% of high risk, and only 34.9% of very high-risk patients. Goal attainment was directly related to age and inversely related to cardiovascular risk and baseline LDL-C.
    CONCLUSION: A large proportion of Asian hypercholesterolaemic patients on lipid-lowering drugs are not at recommended LDL-C levels and remain at risk for cardiovascular disease. Given the proven efficacy of lipid-lowering drugs in the reduction of LDL-C, there is room for further optimization of treatments to maximize benefits and improve outcomes.
    Matched MeSH terms: Hypolipidemic Agents/therapeutic use*
  13. 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*
  14. 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
  15. 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*
  16. Hibiscus sabdariffa linn. (roselle) protects against nicotine-induced heart damage in rats
    Satirah Zainalabidin, Siti Nor Farhanah Sh Nor Shabidin, Siti Balkis Budin
    Sains Malaysiana, 2016;45:207-214.
    Nicotine has been identified as one of the causal factor for oxidative stress, hypertension and hyperlipidemia. Roselle has been widely studied for its potential as an antioxidant, antihyperlipidemic and antihypertensive. However, no studies have been done to investigate if roselle could diminish the oxidative stress caused by nicotine which could further lead to cardiac damages. Thus, this study was aimed to investigate the effect of roselle extract (HSE) on blood pressure, serum lipid profile, oxidative stress marker levels and histological changes to the heart in nicotine-treated rats. A total of 21 Sprague-Dawley rats were randomly divided into 3 groups (n=7 per group): Control group received normal saline (0.5 mL/day, i.p); nicotine group received 0.6 mg/kg/BW nicotine (i.p); and treated group received 100 mg/kg/b.w HSE through oral force feeding followed with 0.6 mg/kg/b.w nicotine (i.p) for 21 consecutive days. The results showed that HSE significantly (p>0.05) reduced the heart rate but no effect to the blood pressure. For lipid profile study, HSE increased the high-density lipoprotein concentration significantly (p<0.05) in rats given with nicotine, without any significant changes in total cholesterol, triglyceride and low-density lipoprotein (LDL) concentration. Besides, HSE treatment was also found to reverse malondialdehyde (MDA) level, superoxide dimustase (SOD) enzyme activity and protein concentration significantly (p<0.05) in nicotine-treated rats. In summary, these results indicated that HSE is an effective antioxidant against oxidative damage in heart caused by nicotine, but not as antihyperlipidemic and antihypertensive agent in this rat model.
    Matched MeSH terms: Hypolipidemic Agents
  17. 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*
  18. Fulltext Glycyrrhizic acid improved lipoprotein lipase expression, insulin sensitivity, serum lipid and lipid deposition in high-fat diet-induced obese rats
    Eu CH, Lim WY, Ton SH, bin Abdul Kadir K
    Lipids Health Dis, 2010;9:81.
    PMID: 20670429 DOI: 10.1186/1476-511X-9-81
    The metabolic syndrome, known also as the insulin resistance syndrome, refers to the clustering of several risk factors for atherosclerotic cardiovascular disease. Dyslipidaemia is a hallmark of the syndrome and is associated with a whole body reduction in the activity of lipoprotein lipase (LPL), an enzyme under the regulation of the class of nuclear receptors known as peroxisome proliferator-activated receptor (PPAR). Glycyrrhizic acid (GA), a triterpenoid saponin, is the primary bioactive constituent of the roots of the shrub Glycyrrhiza glabra. Studies have indicated that triterpenoids could act as PPAR agonists and GA is therefore postulated to restore LPL expression in the insulin resistant state.
    Matched MeSH terms: Hypolipidemic Agents/pharmacology; Hypolipidemic Agents/therapeutic use*
  19. 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*
  20. 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
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