Regulation of Intestinal Cholesterol Absorption: A Disease Perspective

Iqbal, Jahangir; Qarni, Ali Al; Hawwari, Abbas

doi:10.4236/abc.2017.71004

Cited by 7 publications

(3 citation statements)

References 98 publications

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“…22 The cross-sectional studies demonstrated that enhanced cholesterol synthesis and reduced cholesterol absorption is a major risk factor for some diseases such as cardiovascular disease, type 2 diabetes and obesity. 23 One of the most important benecial effects of dietary ber (whether SDF or IDF) is to reduce plasma cholesterol levels, as well as the incidence of atherosclerosis. 1,4 As shown in Fig.…”

Section: Oil Holding Capacitymentioning

confidence: 99%

Adsorption activity of coconut (Cocos nucifera L.) cake dietary fibers: effect of acidic treatment, cellulase hydrolysis, particle size and pH

Zheng

et al. 2018

RSC Adv.

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The effects of acidic treatment, cellulase hydrolysis, particle size distribution and pH on the adsorption capacity of defatted coconut cake dietary fibers (DCCDF) were studied. The results demonstrated that cellulase hydrolysis could significantly improve the soluble dietary fiber content, water holding ability and adsorption ability of DCCDF on cholesterol, bile and nitrite ions. Acidic treatment enhanced the oil holding capacity and adsorption ability in cholesterol and nitrite ions. Moreover, the adsorption ability of DFs in cholesterol, nitrite and bile all increased with reduced particle size (250 to 167 mm), and DCCDF demonstrated a higher adsorption capacity at pH 2.0 than at pH 7.0. The change in adsorption capacity of DCCDF might be suitable for application in the food industry as a low-calorie and cholesterol lowering functional ingredient.

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Section: Oil Holding Capacitymentioning

confidence: 99%

Adsorption activity of coconut (Cocos nucifera L.) cake dietary fibers: effect of acidic treatment, cellulase hydrolysis, particle size and pH

Zheng

et al. 2018

RSC Adv.

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“…Disturbed cholesterol homeostasis is explained as towards reduced cholesterol synthesis and increased cholesterol absorption is associated with increased cardiovascular risk. Study showed that patients that has high cholesterol absorption mat not be helpful from treatment with statin, but could increase their cardiovascular risk when place on a drug that decreases endogenous cholesterol synthesis [41].…”

Section: Cholesterol Lowering Medications and Risk Of Cardiovascular/mentioning

confidence: 99%

Association between Cholesterol Homeostasis with Intestinal Proteins, Enzymes and Drugs in Absorption of Cholesterol and its Relationship with Vascular Diseases: A Review

Javaid¹,

Khurshid²,

Munir³

2018

Biochem Pharmacol

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The goal of this review is to discuss many aspects of cholesterol homeostasis in the body in order to presents the standards of cholesterol disposition and its levels, especially when several means might change the features of cholesterol synthesis and absorption and interrupt this equilibrium. With the detection of pathways of cholesterol absorption and the discovery of different compounds that amend cholesterol absorption, there is a series of cholesterol lowering drugs, which may decrease the level of serum cholesterol by altering its absorption. It is recognized that the effects of cholesterol lowering drugs as well as genetics of a person, loss of body weight, enzymes and proteins may increase the cholesterol altering effect, but the impact of these agents on the mechanism of cholesterol homeostasis are poorly understood. The disturbance of cholesterol homeostasis is also related with vascular changes associated with cardiac and kidney problems. Besides using different drugs and other means (plant sterol, enzyme, protein etc.), there is a need to improve the dietary pattern and life style. These may help to improve the cholesterol homeostasis.

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“…Different approaches, which include the regulation of dietary cholesterol absorption, endogenous cholesterol biosynthesis, and plasma LDL levels, have been considered the key in the prevention and management of hypercholesterolemia and its related complications. − Inhibition of cholesterol esterase and cholesterol micellization are the primary targets for the regulation of dietary cholesterol digestion and absorption. However, since de novo cholesterol synthesis is the major source of blood cholesterol, regulation of cholesterol biosynthesis has been considered a crucial step in hypercholesterolemia management.…”

Section: Introductionmentioning

confidence: 99%

Triterpenoids from Protorhus longifolia Exhibit Hypocholesterolemic Potential via Regulation of Cholesterol Biosynthesis and Stimulation of Low-Density Lipoprotein Uptake in HepG2 Cells

Ndlovu,

Serem,

Selepe

et al. 2023

ACS Omega

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The increasing incidence of hypercholesterolemia-related diseases even in the presence of the currently available cholesterol-lowering drugs indicates a need to discover new therapeutic drugs. This study aimed to investigate the hypocholesterolemic potential of two triterpenoids isolated from Protorhus longifolia stem bark. In silico techniques and in vitro enzyme assays were used to evaluate the potential inhibition of cholesterol esterase and HMG-CoA reductase by the triterpenoids (ARM-2 and RA-5). The toxicity, modulation of low-density lipoprotein (LDL) uptake, and associated gene expression were determined in HepG2 hepatocytes. In silico molecular docking revealed that ARM-2 compared with RA-5 has a relatively stronger binding affinity for both enzymes. Both triterpenoids further demonstrated promising in silico drug-likeness properties and favorable ADMET profiles characterized by high intestinal absorption and lack of CYP450 enzyme inhibition. The compounds further showed, to varying degrees of efficacy, inhibition of cholesterol micellization as well as both cholesterol esterase and HMG-CoA reductase activities with IC50 values ranging from 16.4 to 41.1 μM. Moreover, enhanced hepatic cellular LDL uptake and the associated upregulation of the LDL-R and SREBP-2 gene expression were observed in the triterpenoid-treated HepG2 cells. It is evident that the triterpenoids, especially ARM-2, possess hypocholesterolemic properties, and these molecules can serve as leads or structural templates for the development of new hypocholesterolemic drugs.

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Regulation of Intestinal Cholesterol Absorption: A Disease Perspective

Cited by 7 publications

References 98 publications

Adsorption activity of coconut (Cocos nucifera L.) cake dietary fibers: effect of acidic treatment, cellulase hydrolysis, particle size and pH

Adsorption activity of coconut (Cocos nucifera L.) cake dietary fibers: effect of acidic treatment, cellulase hydrolysis, particle size and pH

Association between Cholesterol Homeostasis with Intestinal Proteins, Enzymes and Drugs in Absorption of Cholesterol and its Relationship with Vascular Diseases: A Review

Triterpenoids from Protorhus longifolia Exhibit Hypocholesterolemic Potential via Regulation of Cholesterol Biosynthesis and Stimulation of Low-Density Lipoprotein Uptake in HepG2 Cells

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