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  1. 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
  2. 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*
  3. Antihyperlipidemic, Antioxidant and Cytotoxic Activities of Methanolic and Aqueous Extracts of Different Parts of Star Fruit
    Saghir SA, Sadikun A, Al-Suede FS, Majid AM, Murugaiyah V
    Curr Pharm Biotechnol, 2016 6 6;17(10):915-25.
    PMID: 27262321 DOI: 10.2174/1389201017666160603013434
    BACKGROUND: Star fruit (Averrhoa carambola) is a well-known plant in Malaysia which bears a great significance in traditional medicine.

    OBJECTIVES: This study aimed to evaluate the antihyperlipidemic effect, antioxidant potential and cytotoxicity of aqueous and methanolic extracts of ripe and unripe fruits, leaves and stem of A. carambola.

    METHODS: Antihyperlipidemic activity was assessed in poloxamer-407 (P-407) induced acute hyperlipidemic rat's model. The antioxidant activity was assessed in vitro using 2, 2'-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radical scavenging, 1-diphenyl-2-dipicrylhydrazyl radical scavenging (DPPH) and ferric reducing antioxidant power (FRAP) assays. In addition, cytotoxicity of A. carambola extracts was assessed using MTS assay on four leukemic cell lines (human colon cancer, human promyeloid leukemia, erythroid leukemia, acute myeloid leukemia) and one normal cell (human umbilical vein endothelial cells).

    RESULTS: Methanolic extract of leaves had the most potent antihyperlipidemic activity in P-407 model, whereby it significantly reduced serum levels of total cholesterol (P<0.01), triglycerides (P<0.01), low-density lipoprotein (P<0.05), verylow- density lipoprotein (P<0.01) and atherogenic index (P<0.01). On the other hand, methanolic extracts of A. carambola stem and leaves showed the strongest antioxidant activity. Total phenolic and flavonoid contents of the extracts exhibited significant correlations with antioxidant but not with antihyperlipidemic activities. All plant parts showed no cytotoxic effect on the selected cancer or normal cell lines.

    CONCLUSION: Antihyperlipidemic activity of different parts of A. carambola is greatly affected by extraction solvents used. Methanolic extract of A. carambola leaves exhibited higher antihyperlipidemic and antioxidant potentials compared to other parts of the plant.
    Matched MeSH terms: Hypolipidemic Agents/pharmacology*
  4. 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
  5. 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*
  6. 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*
  7. 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
  8. Fulltext Anti-Obesity Effects of Melastoma malabathricum var Alba Linn in Rats Fed with a High-Fat Diet
    Karupiah S, Ismail Z
    AAPS PharmSciTech, 2015 Jun;16(3):548-53.
    PMID: 25374344 DOI: 10.1208/s12249-014-0245-1
    Obesity is one of the major public health problems worldwide and it is generally associated with many diseases. Although synthetic drugs are available for the treatment of obesity, herbal remedies may provide safe, natural, and cost-effective alternative to synthetic drugs. One example of such drugs is Melastoma malabathricum var Alba Linn (MM). Although several studies have been reported for the pharmacological activities of MM, there is no report on the anti-obesity effect of MM. The aim of the present study is to evaluate the anti-obesity potential of methanolic extract of MM. The anti-obesity effect of MM on rats fed with a high-fat diet was investigated through determination of the changes in body weight, fat weight, organ weights, and blood biochemicals. The animals in this study were divided into three groups: a normal group with a standard diet (N), a control group fed with high-fat diet (C), and a MM treatment group fed with high-fat (HFD + MM) diet for 8 weeks. There was no significant difference in the amount of food intake between control and HFD + MM treatments. These results also suggest that MM does not induce a dislike for the diet due to its smell or taste. The study shows that MM significantly prevented increases in body weight, cholesterol, LDL, HDL, and total lipids that resulted from the high-fat diet. MM also decreased the epididymal fat (E-fat) and retroperitoneal fat (R-fat) weights and phospholipid concentrations induced by the high-fat diet. On the basis of these findings, it was concluded that MM had anti-obesity effects by suppressing body weight gain and abdominal fat formation.
    Matched MeSH terms: Hypolipidemic Agents/pharmacology*
  9. Effect of extraction solvents and plant parts used on the antihyperlipidemic and antioxidant effects of Garcinia atroviridis: a comparative study
    Al-Mansoub MA, Asmawi MZ, Murugaiyah V
    J Sci Food Agric, 2014 Jun;94(8):1552-8.
    PMID: 24166055 DOI: 10.1002/jsfa.6456
    Garcinia atroviridis is a seasonal fruit plant found in many parts of South East Asia. The fruit rind is used in cooking and traditionally consumed for various reasons, including to lower blood cholesterol. A comparative study was undertaken to investigate the influence of extraction solvents and plant parts used on the lipid-lowering and antioxidant activities of Garcinia atroviridis.
    Matched MeSH terms: Hypolipidemic Agents/pharmacology*
  10. Fulltext Biological activities and phytochemicals of Swietenia macrophylla King
    Moghadamtousi SZ, Goh BH, Chan CK, Shabab T, Kadir HA
    Molecules, 2013 Aug 30;18(9):10465-83.
    PMID: 23999722 DOI: 10.3390/molecules180910465
    Swietenia macrophylla King (Meliaceae) is an endangered and medicinally important plant indigenous to tropical and subtropical regions of the World. S. macrophylla has been widely used in folk medicine to treat various diseases. The review reveals that limonoids and its derivatives are the major constituents of S. macrophylla. There are several data in the literature indicating a great variety of pharmacological activities of S. macrophylla, which exhibits antimicrobial, anti-inflammatory, antioxidant effects, antimutagenic, anticancer, antitumor and antidiabetic activities. Various other activities like anti-nociceptive, hypolipidemic, antidiarrhoeal, anti-infective, antiviral, antimalarial, acaricidal, antifeedant and heavy metal phytoremediation activity have also been reported. In view of the immense medicinal importance of S. macrophylla, this review aimed at compiling all currently available information on its ethnomedicinal uses, phytochemistry and biological activities of S. macrophylla, showing its importance.
    Matched MeSH terms: Hypolipidemic Agents/pharmacology
  11. Alpha lipoic acid possess dual antioxidant and lipid lowering properties in atherosclerotic-induced New Zealand White rabbit
    Zulkhairi A, Zaiton Z, Jamaluddin M, Sharida F, Mohd TH, Hasnah B, et al.
    Biomed Pharmacother, 2008 Dec;62(10):716-22.
    PMID: 18538528 DOI: 10.1016/j.biopha.2006.12.003
    There is accumulating data demonstrated hypercholesterolemia and oxidative stress play an important role in the development of atherosclerosis. In the present study, a protective activity of alpha-lipoic acid; a metabolic antioxidant in hypercholesterolemic-induced animals was investigated. Eighteen adult male New Zealand White (NZW) rabbit were segregated into three groups labelled as group K, AT and ALA (n=6). While group K was fed with normal chow and acted as a control, the rest fed with 100 g/head/day with 1% high cholesterol diet to induce hypercholesterolemia. 4.2 mg/body weight of alpha lipoic acid was supplemented daily to the ALA group. Drinking water was given ad-libitum. The study was designed for 10 weeks. Blood sampling was taken from the ear lobe vein at the beginning of the study, week 5 and week 10 and plasma was prepared for lipid profile estimation and microsomal lipid peroxidation index indicated with malondialdehyde (MDA) formation. Animals were sacrificed at the end of the study and the aortas were excised for intimal lesion analysis. The results showed a significant reduction of lipid peroxidation index indicated with low MDA level (p<0.05) in ALA group compared to that of the AT group. The blood total cholesterol (TCHOL) and low density lipoprotein (LDL) levels were found to be significantly low in ALA group compared to that of the AT group (p<0.05). Histomorphometric intimal lesion analysis of the aorta showing less of atheromatous plaque formation in alpha lipoic acid supplemented group (p<0.05) compared to that of AT group. These findings suggested that apart from its antioxidant activity, alpha lipoic acid may also posses a lipid lowering effect indicated with low plasma TCHOL and LDL levels and reduced the athero-lesion formation in rabbits fed a high cholesterol diet.
    Matched MeSH terms: Hypolipidemic Agents/pharmacology*
  12. 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*
  13. 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*
  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/pharmacology*
  15. 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/pharmacology*
  16. 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
  17. 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
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