Inhibitory Activity of Some Plant Methanol Extracts on 3-Hydroxy-3-Methylglutaryl Coenzyme a Reductase

Gholamhoseinian, Ahmad; Shahouzehi, Beydolah; Sharififar, Fariba

doi:10.3923/ijp.2010.705.711

Cited by 37 publications

(29 citation statements)

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“…This type of inhibition depends on special components which bind to enzyme or enzyme‐substrate complex. The presence of HMG‐CoA reductase inhibitor has been reported in various plants such as Heracleum persicum , Camellia sinensis , and Levisticum officinale with 45%, 47%, and 48% of inhibition respectively at 50 µg/mL (Gholamhoseinian et al ., ), which was significantly lower than 84% inhibition (at 20 µg/mL) caused by FVBM extract, indicating its potent hypolipidemic property. Moreover, the FVBM was also found to be non‐cytotoxic, whereas FVLA showed slight toxicity at highest concentrations (data not shown).…”

Section: Resultsmentioning

confidence: 73%

An In Vitro and Molecular Informatics Study to Evaluate the Antioxidative and β‐hydroxy‐β‐methylglutaryl‐CoA Reductase Inhibitory Property of Ficus virens Ait

Iqbal

Khan

Ahmad

et al. 2013

Phytotherapy Research

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The present study is initially intended to evaluate antioxidant and β-hydroxy-β-methylglutaryl-CoA reductase (HMGR) inhibitory property of Ficus virens Ait., first by in vitro analyses followed by a corroboratory molecular informatics study. Our results show that of all the sequentially extracted fraction of F. virens bark and leaves extract, F. virens bark methanol extract exhibits strong radical scavenging, antioxidant and oxidative DNA damage protective activity, which is well correlated with its total phenolic content. In addition, F. virens bark methanol extract, which is non-cytotoxic, significantly and non-covalently inhibit the HMGR activity (IC50 = 3.45 ± 0.45 µg/ml) in comparison with other extracts. The mechanistic aspect of this inhibition activity is authenticated by molecular docking study of bioactive compounds as revealed from gas chromatography-mass spectrometry data, with HMGR. The analysis for the first time indicates that quinic acid (ΔG: -8.11 kcal/mol) and paravastatin (ΔG: -8.22 kcal/mol) exhibit almost same binding energy, while other compounds also showed good binding energy, suggesting that quinic acid alone or in combination with other major bioactive compound is probably responsible for HMGR inhibitory property of the extract and plausibly can be used in in vivo system for the management, prevention, and alleviation of hypercholesterolemia as well as hypercholesterolemia-induced oxidative stress.

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Section: Resultsmentioning

confidence: 73%

An In Vitro and Molecular Informatics Study to Evaluate the Antioxidative and β‐hydroxy‐β‐methylglutaryl‐CoA Reductase Inhibitory Property of Ficus virens Ait

Iqbal

Khan

Ahmad

et al. 2013

Phytotherapy Research

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“…Several mechanisms may be responsible for this therapeutic activity, such as a reduction in high-density lipoprotein cholesterol (HDL-C), destruction of foam cells and macrophages in lymph nodes, and the restoration of the endothelium by neighbouring cells or circulating progenitors [32,37]. The alteration in the lipid profile and the regression of atherosclerotic plaque by the plant extract was supported by results obtained in the invitro HMG-CoA reductase inhibition assay and in-silico evaluation conducted in previous studies [38,39]. The phytoconstituents in the extract were analysed and identified by LCMS, GCMS, and FTIR; which validated the existence of several phytoconstituents identified functional groups that could potentially interact with target enzyme and serve as competitive inhibitors or analogues of substrates [37,38,40].…”

Section: Discussionmentioning

confidence: 76%

Phytoconstituents of an ethanolic pod extract of Prosopis cineraria triggers the inhibition of HMG-CoA reductase and the regression of atherosclerotic plaque in hypercholesterolemic rabbits

et al. 2020

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Background: The HMG-CoA reductase is key enzyme of cholesterol biosynthesis which potentially contributes in management of hypercholesterolemia. The present study was designed to assess the inhibitory effect of phytoconstituents of an ethanolic extract of Prosopis cineraria pods on HMG -CoA reductase and regression potential of atherosclerotic plaque. Methods: Healthy, adult male, albino rabbits in which hypercholesterolemia was induced by supplying the high fat diet and a supplement of cholesterol powder with coconut oil (500 mg/5 ml/Day/kg body weight) for 15 days, were used as a disease model. Phytochemical analysis of an ethanolic extract Prosopis cineraria pods was conducted using LCMS, GCMS and FTIR analysis. Further, in-vitro, in-vivo and in-silico assessments were performed.Results: The in-vitro assessment of HMG -CoA reductase activity indicated a 67.1 and 97.3% inhibition by the extract and a standard drug (Pravastatin), respectively. Additionally, an in-silico evaluation was made using appropriate docking software and results also indicated as significant interactions of the identified compounds with the target enzyme. Treatment of rabbits with the ethanolic extract of P. cineraria pod resulted in significant (P ≤ 0.001) reductions in total cholesterol, LDL cholesterol, VLDL cholesterol, and triglyceride. Accordingly, reductions were occurred in atherosclerotic plaque, intima and media of aortal wall along with lumen volume of the aorta significantly increased (P ≤ 0.001).Conclusion: It can be illustrating that the ethanolic extract of Prosopis cineraria pod contains potent bioactive phytocompounds might be inhibit HMG -CoA reductase and have regression potential of atherosclerotic plaque.

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“…In vitro experiments indicated that especially QI and to some extent RD have inhibitory effect on pancreatic lipase [26] and HMG CoA reductase enzyme [27]. The results of previous [19] and present in vivo studies obviously have confirmed the antilipidemic effect of QI, but RD had no considerable effect.…”

Section: Discussionmentioning

confidence: 61%

Assessment of Safety and Therapeutic Efficacy ofRosa damascenaL. andQuercus infectoriaon Cardiovascular Performance of Normal and Hyperlipidemic Rabbits: Physiologically Based Approach

Joukar

Askarzadeh

Shahouzehi

et al. 2013

Journal of Toxicology

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According to the use of Quercus infectoria (QI) and Rosa damascena L. (RD) for therapeutic purposes and lack of adequate information about their cardiovascular effects, we investigated the cardiovascular indices of rabbits which chronically pretreated with these agents. Animal groups were control group (CTL), RD and QI groups with normal chow plus 1.5 g RD and QI extracts, respectively, in each kg of the diet for 45 days; Hyperlipidemic (H) group received high-fat diet for 45 days; H+RD and H+QI groups received high fat diet plus QI and RD extracts, respectively. Blood pressure was greater in H+RD group than CTL, RD, and H groups. Left ventricular developed pressure and left ventricular systolic pressure increased significantly in H+RD group versus CTL and RD groups (P < 0.05 and P < 0.0001, resp.) and in H+QI groups (P < 0.01 versus QI groups). Left ventricular end diastolic pressure (LVEDP) showed significant reduction in H+QI group versus H group. QI attenuated the values of total cholesterol, LDL, TG, and atherogenic indices of plasma when coadministrated with a high-fat diet. The results suggest the antilipidemic and antiatherogenic effects of QI. In addition, the use of RD along with a high-fat diet may increase the risk of hypertension in rabbits.

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Inhibitory Activity of Some Plant Methanol Extracts on 3-Hydroxy-3-Methylglutaryl Coenzyme a Reductase

Cited by 37 publications

References 0 publications

An In Vitro and Molecular Informatics Study to Evaluate the Antioxidative and β‐hydroxy‐β‐methylglutaryl‐CoA Reductase Inhibitory Property of Ficus virens Ait

An In Vitro and Molecular Informatics Study to Evaluate the Antioxidative and β‐hydroxy‐β‐methylglutaryl‐CoA Reductase Inhibitory Property of Ficus virens Ait

Phytoconstituents of an ethanolic pod extract of Prosopis cineraria triggers the inhibition of HMG-CoA reductase and the regression of atherosclerotic plaque in hypercholesterolemic rabbits

Assessment of Safety and Therapeutic Efficacy ofRosa damascenaL. andQuercus infectoriaon Cardiovascular Performance of Normal and Hyperlipidemic Rabbits: Physiologically Based Approach

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