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Journal ArticleDOI

Characterization, Modes of Synthesis, and Pleiotropic Effects of Hypocholesterolemic Compounds – A Review

TL;DR: Major natural sources as well as synthetic and biological routes of synthesis of these compounds are reviewed in a concise manner and various HMG-CoA analogues including statins have been reviewed specifically.
Abstract: Studies on the various cholesterol-lowering agents is one of the important areas in clinical research. Identifica- tion and characterization of potential molecules from various sources have been carried out in the past and their relation- ship with the enzymes which are involved in the cholesterol cascade is gaining interest. In this review, we have high- lighted various inhibitors involved in the cholesterol cascade as well as cholesterol-lowering agents, viz., tocotrienol, flavonoids, phytosterols, phytostanols, statins, DADS, and synthetic compounds. The mechanism of action and characteri- zation of these hypocholesterolemic compounds are discussed in this communication. Major natural sources as well as synthetic and biological routes of synthesis of these compounds are reviewed in a concise manner. Especially, various HMG-CoA analogues including statins have been reviewed specifically. In this respect, researchers have identified 2,3- oxidosqualene cyclase-lanosterol synthase (lanosterol syn- thase, oxidosqualene-lanosterol cyclase, lanosterol synthase, 2,3-oxidosqualene-lanosterol cyclase, human lanosterol syn- thase (EC 5.4.99.7)) having a molecular weight of 83 kDa, catalyzing the highly selective cyclization reaction from the substrate 2,3-oxidosqualene (squalene 2,3-epoxide, squalene 2,3-oxide, (S)-squalene-2,3-epoxide, 2,3-epoxisqualene, oxidosqualene) into lanosterol, as an appropriate step for the inhibition of cholesterol biosynthesis (3). Oxidosqualene cyclase inhibitors (OSCI) arrest the downstream of 2,3- oxidosqualene which helps to stimulate epoxysterols to

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Journal ArticleDOI
TL;DR: In this article, the authors investigated the possible mechanisms for the use of phenolic extracts from grapefruit peels in the management/prevention of cardiovascular complications and found that the phenolic contents of the extracts were investigated using HPLC-DAD.

39 citations

Journal ArticleDOI
TL;DR: The phenolic compounds and volatile compounds which have been linked with the biological activities of the peels have been characterized and the bioactive compounds of citrus peels and the mechanisms for the biological Activities are looked at.
Abstract: Citrus peels, which are an environmental menace in many developing countries have been in use in folk medicine for the management of some degenerative conditions, though there was limited information on the mechanism of such medicinal properties. These medicinal properties also promote the peels as functional foods; since they are generally regarded as safe and are consumed in some countries in forms of candies, wines, infusions and additives. Studies on the mechanisms for the antioxidant, anti-diabetic, cardioprotective, neuroprotective and anticancer activities of the peels have established the intereaction with some key enzymes relevant to the management of such diseases. The phenolic compounds and volatile compounds which have been linked with the biological activities of the peels have been characterized. This review looks at the bioactive compounds of citrus peels and the mechanisms for the biological activities of the peels.

23 citations


Cites background from "Characterization, Modes of Synthesi..."

  • ...The inhibition of HMG-CoA reductase by phenolic compounds is both competitive with HMG-CoA and non-competitive with NADPH (Sung et al. 2004a, b; Seenivasan et al. 2011)....

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Journal ArticleDOI
TL;DR: In this article, the authors characterized the soluble free and bound phenolic compounds from shaddock peels and investigated their effect on 3-hydroxy-methyl-3-glutaryl coenzyme A reductase (HMG-CoA) and glutathione-linked enzymes in colon (Caco-2) cells.

10 citations

Journal ArticleDOI
TL;DR: The estimation of Lovastatin produced by Monascus purpureus and pure lovastatin was attempted by UV-visible spectrophotometer as well as HPLC, and HPLC analysis consistently gave reliable results for the estimation of lovastsatin under all the experimental conditions studied.
Abstract: Development of a novel method for the quantification of lovastatin is an interesting problem in the analytical field. In the literature, many reports use spectrophotometric method for the quantification of lovastatin. However, the analysis of fermentation broth containing lovastatin appears to be inaccurate using spectrophotometric method. Hence, the estimation of lovastatin produced by Monascus purpureus and pure lovastatin was attempted by UV-visible spectrophotometer as well as HPLC. It was observed that the analogues and/or intermediates of lovastatin synthesized in the fermentation broth and the products of fermentation caused superimposition effect on the absorption spectrum. Phosphate is a medium constituent for the production of lovastatin by the organism which contributed significantly to the superimposition of absorption spectrum. On the other hand, HPLC analysis consistently gave reliable results for the estimation of lovastatin under all the experimental conditions studied.

10 citations

Journal ArticleDOI
TL;DR: Predicted specific substrate utilization and product excretion rates have been correlated well with the experimental observations, which validate the proposed metabolic pathway developed from metabolic footprinting data.

8 citations

References
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1 citations


"Characterization, Modes of Synthesi..." refers background in this paper

  • ...Among this group, few flavonoids have shown hypocholesterolemic activity in addition to anti-cancer, metal-chelating and prooxidant activities [32, 33, 36]....

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  • ...Stigmasterol, a derivative of sitosterol is poorly absorbed than sitosterol in the intestines [36]....

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