Piperine potentiates the hypocholesterolemic effect of curcumin in rats fed on a high fat diet

Tu, Y S; Sun, Dongmei; Zeng, Xiaohui; Yao, Nan; Huang, Xuejun; Huang, Dane; Yuxing, Chen

doi:10.3892/etm.2014.1717

Cited by 36 publications

(24 citation statements)

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“…Cognitive measures were not included in their study design. Statistically significant results were shown for a number of these markers including increased catalase, nitric oxide and antioxidant status, with lowered Curcumin Inhibits BACE1 up-regulation (68)(69)(70)(71) Lowers cholesterol levels (91)(92)(93)(94)(95)(96)(97) Enhances A phagocytosis by microglia/macrophages (22,(87)(88)(89) Anti-inflammatory Antioxidant Inhibits acetylcholinesterase activities (124,126) Neuroprotection Cognition Promotes neuroplasticity and cell growth (108) Binds A (40)(41) Anti-amyloidogenic…”

Section: Effects Of Curcumin On Human Cognitionmentioning

confidence: 99%

Examining the potential clinical value of curcumin in the prevention and diagnosis of Alzheimer’s disease

et al. 2015

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Curcumin derived from turmeric is well documented for its anti-carcinogenic, antioxidant and anti-inflammatory properties. Recent studies show that curcumin also possesses neuroprotective and cognitive-enhancing properties that may help delay or prevent neurodegenerative diseases, including Alzheimer’s disease (AD). Currently, clinical diagnosis of AD is onerous, and it is primarily based on the exclusion of other causes of dementia. In addition, phase III clinical trials of potential treatments have mostly failed, leaving disease-modifying interventions elusive. AD can be characterised neuropathologically by the deposition of extracellular β amyloid (Aβ) plaques and intracellular accumulation of tau-containing neurofibrillary tangles. Disruptions in Aβ metabolism/clearance contribute to AD pathogenesis. In vitro studies have shown that Aβ metabolism is altered by curcumin, and animal studies report that curcumin may influence brain function and the development of dementia, because of its antioxidant and anti-inflammatory properties, as well as its ability to influence Aβ metabolism. However, clinical studies of curcumin have revealed limited effects to date, most likely because of curcumin’s relatively low solubility and bioavailability, and because of selection of cohorts with diagnosed AD, in whom there is already major neuropathology. However, the fresh approach of targeting early AD pathology (by treating healthy, pre-clinical and mild cognitive impairment-stage cohorts) combined with new curcumin formulations that increase bioavailability is renewing optimism concerning curcumin-based therapy. The aim of this paper is to review the current evidence supporting an association between curcumin and modulation of AD pathology, including in vitro and in vivo studies. We also review the use of curcumin in emerging retinal imaging technology, as a fluorochrome for AD diagnostics.

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Section: Effects Of Curcumin On Human Cognitionmentioning

confidence: 99%

Examining the potential clinical value of curcumin in the prevention and diagnosis of Alzheimer’s disease

et al. 2015

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“…Given the broad use of black pepper as spice all over the world, piperine, its most distinct constituent has also already gained significant research attention in the context of cardiovascular disease and a number of in vivo studies suggest that it has antiatherosclerotic activity . While macrophage ChE enhancement is one possible way for a small molecule to exert an antiatherosclerotic effect, the ChE‐inducing potential of piperine has not been studied so far.…”

Section: Discussionmentioning

confidence: 99%

“…The present study shows for the first time that piperine increases ChE from human THP-1-derived macrophages and inhibits the degradation of the ChE transporter ABCA1, likely by reducing its calpain-mediated degradation. Given the broad use of black pepper as spice all over the world, piperine, its most distinct constituent has also already gained significant research attention in the context of cardiovascular disease and a number of in vivo studies suggest that it has antiatherosclerotic activity [21][22][23][24]37]. While macrophage ChE enhancement is one possible way for a small molecule to exert an antiatherosclerotic effect, the ChE-inducing potential of piperine has not been studied so far.…”

Section: Discussionmentioning

confidence: 99%

“…Recent research also shows that piperine exhibits beneficial cardiovascular effects in vivo. In rats fed on a high-fat diet enriched with cholesterol and other lipids, elevated plasma levels of HDL and apo A1, and decreased plasma levels of total cholesterol, triglyceride, and LDL cholesterol (LDL cholesterol) were observed in animals supplied with piperine-supplemented food [20][21][22][23]. Another study found that rats fed with high carbo-hydrate, high-fat diet supplemented with piperine displayed normalized blood pressure and improved aortic reactivity [24].…”

Section: Introductionmentioning

confidence: 99%

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Piperine inhibits ABCA1 degradation and promotes cholesterol efflux from THP‐1‐derived macrophages

Wang

Palme

Rotter

et al. 2016

Molecular Nutrition Food Res

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ScopeIncreased macrophage cholesterol efflux (ChE) is considered to have anti-atherosclerotic effect counteracting cardiovascular disease. The principle pungent ingredient of the fruits of Piper nigrum, piperine, is identified in this study as a ChE inducer in THP-1-derived macrophages, and mechanisms underlying this effect are explored.Methods and resultsWithout affecting cell viability, piperine concentration-dependently enhances ChE in THP-1-derived macrophages from 25 to 100 μM. The expression level of the key cholesterol transporter protein ATP-binding cassette transporter A1 (ABCA1) is significantly upregulated by piperine, as revealed by western blot analyses. However, two other ChE-mediating transporter proteins, ATP-binding cassette transporter G1 (ABCG1) and scavenger receptor class B member 1 (SR-B1), remain unaffected. Piperine exerts no influence on ABCA1 mRNA levels, but significantly inhibits the degradation of ABCA1, as evident by an increased half-life of the protein in the presence of cycloheximide. Furthermore, it is found that piperine likely interferes with the calpain-mediated ABCA1 degradation pathway and exhibits significant inhibition of calpain activity.ConclusionOur findings suggest that piperine promotes ChE in THP-1-derived macrophages by upregulation of ABCA1, which might be mediated by inhibition of calpain activity. This novel bioactivity makes the dietary constituent piperine a good candidate to be further explored for therapeutic or preventive applications in the context of atherosclerosis.

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“…It exists extensively in nature, particularly in the Piperaceae plants (Venkatasamy et al, 2004). The pharmacological effects of piperine and its derivatives are extensive, including oxidation resistance, immunoregulation, antineoplastic, and drug metabolism promotion activities, among others (Tu et al, 2014). They can be used to treat central nervous system diseases and have received increasing attention in studies in recent years (Mao et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

Effect of GBOT on blood lipid and blood glucose metabolism in rats with atherosclerosis

2015

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ABSTRACT. We observed the variation in in vivo blood lipid and blood glucose metabolism in rats with atherosclerosis after 5-(3,4-dihydroxyphenyl)-1-piperidin-1-yl-penta-2,4-dien-1-one (GBOT) administration. Wistar rats aged 10 weeks received a high-fat diet to establish the atherosclerosis model. Metabolic indices related to blood lipid and blood glucose were measured before modeling and at 4 and 8 weeks after modeling. Liver fat levels in rats were measured at 8 weeks to analyze the relationship between liver fat and blood lipid levels. We examined the mechanism of blood lipid reduction. The levels of serum triglycerides, total cholesterol, and very-low-density lipoprotein cholesterol in rats in the control group were significantly decreased (P < 0.05) compared with those in the 4-week control group at 4 weeks and decreased significantly and continuously until the 8th week (P < 0.05). Compared with the 8-week control group, the blood glucose level in rats in the 8-week experimental group decreased significantly (P < 0.05), and the level of insulin sensitivity index decreased significantly (P < 0.05). Compared with the control group, triglyceride and total cholesterol levels per unit mass in rat liver tissue in the 8-week experimental group decreased significantly (P < 0.05). Western blotting indicated that GBOT significantly increased the expression of lecithin-cholesterol acyltransferase, low-density lipoprotein receptor, and cholesterol 7 alpha-hydroxylase proteins. GBOT can significantly decrease the levels of blood lipid and blood glucose in rat models of atherosclerosis, and its mechanism may be associated with the promotion of expression of lecithin-cholesterol acyltransferase, low-density lipoprotein receptor, and cholesterol 7 alpha-hydroxylase proteins.

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Piperine potentiates the hypocholesterolemic effect of curcumin in rats fed on a high fat diet

Cited by 36 publications

References 38 publications

Examining the potential clinical value of curcumin in the prevention and diagnosis of Alzheimer’s disease

Examining the potential clinical value of curcumin in the prevention and diagnosis of Alzheimer’s disease

Piperine inhibits ABCA1 degradation and promotes cholesterol efflux from THP‐1‐derived macrophages

Effect of GBOT on blood lipid and blood glucose metabolism in rats with atherosclerosis

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