Mitigating efficacy of piperine in the physiological derangements of high fat diet induced obesity in Sprague Dawley rats

Parim, Brahmanaidu; Nemani, Harishankar; Meriga, Balaji; Mehar, Santosh Kumar; Potana, Sailaja; Ramgopalrao, Sajjalaguddam

doi:10.1016/j.cbi.2014.07.008

Cited by 73 publications

(53 citation statements)

References 42 publications

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“…The orlistat PL-IC 50 value obtained in this current study is comparable to the other reported PL-IC 50 values [20]. These significant anti-lipase effects of sage may be solidly related to the effect of the major compounds identified in the crude extract [8,20] acting additively or synergistically in optimal ratio [22]. Hydrocarbons, sterols, triterpenes, fatty acids, phenolic acids, and flavonoids have been identified in S. triloba.…”

Section: Discussionsupporting

confidence: 81%

Antilipolytic and hypotriglyceridemic effects of dietary <i>Salvia triloba</i> Lf (Lamiaceae) in experimental rats

Arabiyat¹,

Al-Rabi'ee²,

Zalloum³

et al. 2016

Trop. J. Pharm Res

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Purpose: Pancreatic triacylglycerol lipase (PL) is a noteworthy pharmacological target for the management of dyslipidemia, and diabetes and obesity. This study was aimed to evaluate the modulatory effects of Salvia triloba L.f. (Lamiaceae) leaves methanol extract (ME) on a high fat diet (HFD)-induced hypertriglyceridemia in rats, with complementary in vitro evaluation of sage PL-inhibitory potential. Methods: Pre-induction of HFD hypertriglyceridemia sage leaves ME (750 mg/kg) was orally supplemented (via gastric intubation) to overnight fasting rats (n = 5). Potential plant modulation of PL was also quantified in vitro by a colorimetric assay (n = 3

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Section: Discussionsupporting

confidence: 81%

Antilipolytic and hypotriglyceridemic effects of dietary <i>Salvia triloba</i> Lf (Lamiaceae) in experimental rats

Arabiyat¹,

Al-Rabi'ee²,

Zalloum³

et al. 2016

Trop. J. Pharm Res

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“…A number of targets have been identified, but none have been shown to be causative (31,33,(38)(39)(40). Our data show that piperine enhances thermogenesis of resting muscle via a perturbation of the SRX/DRX ratio, thus providing a mechanism.…”

Section: Discussionmentioning

confidence: 72%

“…All animals gained fat mass, but those also receiving piperine gained less than the controls. The difference in fat mass gain varied between 20 and 70% in different studies (31)(32)(33)(34)(35). Changes in lean mass were small, ∼10%.…”

Section: Discussionmentioning

confidence: 94%

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Piperine’s mitigation of obesity and diabetes can be explained by its up-regulation of the metabolic rate of resting muscle

Nogara

Naber

Pate

et al. 2016

Proc. Natl. Acad. Sci. U.S.A.

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We identify a target for treating obesity and type 2 diabetes, the consumption of calories by an increase in the metabolic rate of resting skeletal muscle. The metabolic rate of skeletal muscle can be increased by shifting myosin heads from the super-relaxed state (SRX), with a low ATPase activity, to a disordered relaxed state (DRX), with a higher ATPase activity. The shift of myosin heads was detected by a change in fluorescent intensity of a probe attached to the myosin regulatory light chain in skinned skeletal fibers, allowing us to perform a highthroughput screen of 2,128 compounds. The screen identified one compound, which destabilized the super-relaxed state, piperine (the main alkaloid component of black pepper). Destabilization of the SRX by piperine was confirmed by single-nucleotide turnover measurements. The effect was only observed in fast twitch skeletal fibers and not in slow twitch fibers or cardiac tissues. Piperine increased ATPase activity of skinned relaxed fibers by 66 ± 15%. The K d was ∼2 μM. Piperine had little effect on the mechanics of either fully active or resting muscle fibers. Previous work has shown that piperine can mitigate both obesity and type 2 diabetes in rodent models of these conditions. We propose that the increase in resting muscle metabolism contributes to these positive effects. The results described here show that up-regulation of resting muscle metabolism could treat obesity and type 2 diabetes and that piperine would provide a useful lead compound for the development of these therapies.myosin | fluorescence | skeletal muscle | super-relaxed state | obesity A n epidemic of obesity and type 2 diabetes is currently affecting a large fraction of the world population (1, 2). This is primarily due to an overconsumption of food coupled with a reduction in physical activity. A natural antidote to both obesity and type 2 diabetes is to choose a healthy lifestyle, including a low-calorie diet and increased physical activity. However, many do not choose this option, and for some advanced patients, increased physical activity is not possible. The response to overfeeding in humans is diverse: some store the excess calories almost entirely, whereas others metabolize most of them (3). The variation is strongly dependent on both lifestyle and genetics. As strenuous activity was limited in some of these protocols, the diversity of weight gain was attributed to light activities, such as fidgeting (3, 4). Alternatively, the diversity may be due to variation in the metabolic rate of resting muscle and to how this responds to activity (5).A pharmacological approach to combating obesity has been of limited value, of the order of 5-10% weight loss when combined with lifestyle changes (for review, see refs. 6 and 7). Therapies for type 2 diabetes produce little effect, with the exception of metformin (for review, see ref. 8). Lifestyle changes, including better diets and increased activity levels, have a larger effect than pharmaceuticals. Here we suggest a target for combating obesity and...

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“…Some of these supplements, including Ephedra sinica, Paullinia cupana, Plantago psyllium, and Pausinystalia yohimbe, have harmful effects, whereas Garcinia cambogia and Ilex paraguariensis are considered relatively safe and merit further investigation [Pittler et al, 2005]. of potential compounds in the treatment of obesity [Bulló et al, 2007;Lim et al, 2013;BrahmaNaidu et al, 2014]. Thus, the aim of the present study was to evaluate the time-dependent effects of S. marianum on HFD-related metabolic disorders and weight increase.…”

Section: Introductionmentioning

confidence: 99%

Effects of Silybum marianum Extract on High-Fat Diet Induced Metabolic Disorders in Rats

Sayın¹,

Büyükbaş²,

Başaralı³

et al. 2016

Pol. J. Food Nutr. Sci.

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Mitigating efficacy of piperine in the physiological derangements of high fat diet induced obesity in Sprague Dawley rats

Cited by 73 publications

References 42 publications

Antilipolytic and hypotriglyceridemic effects of dietary <i>Salvia triloba</i> Lf (Lamiaceae) in experimental rats

Antilipolytic and hypotriglyceridemic effects of dietary <i>Salvia triloba</i> Lf (Lamiaceae) in experimental rats

Piperine’s mitigation of obesity and diabetes can be explained by its up-regulation of the metabolic rate of resting muscle

Effects of Silybum marianum Extract on High-Fat Diet Induced Metabolic Disorders in Rats

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