Inhibitory effect of novel diallyldisulfide analogs on HMG-CoA reductase expression in hypercholesterolemic rats: CREB as a potential upstream target

Kumar, Santosh; Sharma, Meenakshi; Tiwari, Manisha

doi:10.1016/j.lfs.2009.05.020

Cited by 64 publications

(44 citation statements)

References 36 publications

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“…Garlic-derived compounds such as DADS and DATS can attenuate the deleterious effects of oxidized LDL on nitric oxide production (Lei et al 2010) and attenuate myocardial ischemia/reperfusion in mice (Predmore et al 2010). DADS is also known to inhibit 3-hydroxy-3-methylglutaryl-CoA and thus may be a potential antihyperlipidemic agent (Rai et al 2009). It is also reported that oral administration of raw garlic homogenate in diabetic rats increased insulin sensitivity and reduced metabolic complications along with oxidative stress (Padiya et al 2011).…”

Section: Garlic-derived Sulfur-containing Compoundsmentioning

confidence: 99%

Medicinal Chemistry: Insights into the Development of Novel H2S Donors

Zhao

Pacheco

Xian

2015

Handbook of Experimental Pharmacology

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Hydrogen sulfide (H2S) was traditionally considered as a toxic gas. However, recent studies have demonstrated H2S is an endogenously generated gaseous signaling molecule (gasotransmitter) with importance on par with that of two other well-known endogenous gasotransmitters, nitric oxide (NO) and carbon monoxide (CO). Although H2S's exact mechanisms of action are still under investigation, the production of endogenous H2S and the exogenous administration of H2S have been demonstrated to elicit a wide range of physiological responses including modulation of blood pressure and protection of ischemia reperfusion injury, exertion of anti-inflammatory effects, and reduction of metabolic rate. These results strongly suggest that modulation of H2S levels could have potential therapeutic values. In this regard, synthetic H2S-releasing agents (i.e., H2S donors) are not only important research tools, but also potential therapeutic agents. This chapter summarizes the knowledge of currently available H2S donors. Their preparation, H2S releasing mechanisms, and biological applications are discussed.

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Section: Garlic-derived Sulfur-containing Compoundsmentioning

confidence: 99%

Medicinal Chemistry: Insights into the Development of Novel H2S Donors

Zhao

Pacheco

Xian

2015

Handbook of Experimental Pharmacology

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“…Their analogues inhibit the cholesterol cascade ( Table 1). These compounds inhibit the activation of sterol regulatory element binding protein-2 (SREBP-2) and cAMP response element-binding proteins (CREB), which are responsible for the expression of some enzymes involved in the cholesterol cascade especially HMG-CoA reductase [2]. …”

Section: Characterization and Mechanisms Of Hypocholesterolemic Compomentioning

confidence: 99%

“…Diallyl disul-fide has antiatherosclerotic and antioxidant properties. Their analogues have the specific property of hypochloesterolemia helping to reduce the LDL-cholesterol and serum cholesterol levels by inhibiting transcriptional activators [2].…”

Section: Pleiotropic Effects Of Different Hypo-cholesterolemic Drugsmentioning

confidence: 99%

“…Body also exhibits its own natural regulation mechanisms to control cholesterol synthesis. One of the short-term regulations of the cholesterol biosynthesis cascade is done by the phosphorylation of the glycoprotein, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (EC 1.1.1.34) using AMP-dependent protein kinase [1,2].…”

Section: Introductionmentioning

confidence: 99%

“…Some fungi produce group 1 statins as secondary metabolites. A few organisms have been employed for biotransformation studies to improve the efficiency of fermentation-derived statin compounds [2,15,16]. Differences in structure and binding characteristics partly contribute to differences in the inhibition efficiency of statins.…”

Section: Introductionmentioning

confidence: 99%

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

Seenivasan¹,

Panda

Théodore³

2011

TOEIJ

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Studies on the various cholesterol-lowering agents is one of the important areas in clinical research. Identification and characterization of potential molecules from various sources have been carried out in the past and their relationship with the enzymes which are involved in the cholesterol cascade is gaining interest. In this review, we have highlighted 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 characterization 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.

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Design, Synthesis and Anti‐Cancer Activities of Benzyl Analogues of Garlic‐Derived Diallyl Disulfide (DADS) and the Corresponding Diselenides

et al. 2017

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The anti‐cancer activity of garlic mainly arises due to the presence of various organosulfur compounds including diallyl sulfide (DAS), diallyl disulfide (DADS) and diallyl trisulfide (DATS). Herewith, we report a number of 4‐substituted benzyl analogs of DADS and their selenium counterparts for a detailed structure‐activity relationship towards their anti‐proliferative activities in human breast cancer cell lines. Disulfide having 4‐cyano group exhibited highest activity among all disulfides. In contrast, all diselenides exhibited very good anti‐proliferative activities than DADS. Furthermore, unlike disulfides, diselenides were more selective towards cancer cells over normal cells. Some active compounds were further tested for their activities in some organ specific cell lines such as HepG2, PC‐3 and HCT‐116 to understand their efficacy. Elevated level of intracellular reactive oxygen species (ROS) by most of the benzyl diselenides reveals a possible mode of their action. Therefore, this study indicates that the anti‐proliferative activity of DADS can be significantly enhanced upon suitable structural modifications.

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Inhibitory effect of novel diallyldisulfide analogs on HMG-CoA reductase expression in hypercholesterolemic rats: CREB as a potential upstream target

Cited by 64 publications

References 36 publications

Medicinal Chemistry: Insights into the Development of Novel H2S Donors

Medicinal Chemistry: Insights into the Development of Novel H2S Donors

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

Design, Synthesis and Anti‐Cancer Activities of Benzyl Analogues of Garlic‐Derived Diallyl Disulfide (DADS) and the Corresponding Diselenides

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