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Sunday, 27 October 2013

Phytochemicals in Foods - 11 Health Benefits of Piperine

Piperine is a phytochemical alkaloid in the class of organosulfur compound, found abundantly in white and black pepper, long pepper, etc.

Health Benefits
1. Anti bacterial activities
In the valuation of novel synthetic analogues of piperine as inhibitors of multidrug efflux pump NorA of Staphylococcus aureus, showed that
a newly identified class of compounds derived from a natural amide, piperine, is more potent than the parent molecule in potentiating the activity of ciprofloxacin through the inhibition of the NorA efflux pump. These molecules may prove useful in augmenting the antibacterial activities of fluoroquinolones in a clinical setting, according to "Novel structural analogues of piperine as inhibitors of the NorA efflux pump of Staphylococcus aureus" by Ashwani Kumar, Inshad Ali Khan, Surrinder Koul, Jawahir Lal Koul, Subhash Chandra Taneja, Intzar Ali, Furqan Ali, Sandeep Sharma, Zahid Mehmood Mirza, Manoj Kumar, Pyare Lal Sangwan, Pankaj Gupta, Niranjan Thota and Ghulam Nabi Qazi(1)

2. Anti-inflammatory Effect
In the investigation of investigate the anti-inflammatory effect of piperine against adjuvant-induced arthritis in rats, an experimental model for rheumatoid arthritis and compared it with that of the non-steroidal anti-inflammatory drug indomethacin, found that Histopathological analysis of joints also revealed that synovial hyperplasia and mononuclear infiltration observed in arthritic rats were alleviated by piperine. Thus, the present study clearly indicated that piperine possesses promising anti-inflammatory effect against adjuvant-induced arthritis by suppressing inflammation and cartilage destruction, according to "Anti-inflammatory Effect of Piperine in Adjuvant-Induced Arthritic Rats-a Biochemical Approach" by Murunikkara V, Pragasam SJ, Kodandaraman G, Sabina EP, Rasool M.(2)

3. Murine breast cancer
In the investigation of the effects of piperine, a major pungent alkaloid present in Piper nigrum and Piper longum, on the tumor growth and metastasis of mouse 4T1 mammary carcinoma in vitro and in vivo, and elucidation of the underlying mechanisms, showed that Treatment of 4T1 cells with piperine (70-280 μmol/L) dose-dependently induced apoptosis of 4T1 cells, accompanying activation of caspase 3. The cells treated with piperine (140 and 280 μmol/L) significantly increased the percentage of cells in G(2)/M phase with a reduction in the expression of cyclin B1. Piperine (140 and 280 μmol/L) significantly decreased the expression of MMP-9 and MMP-13, and inhibited 4T1 cell migration in vitro. Injection of piperine (2.5 and 5 mg/kg) dose-dependently suppressed the primary 4T1 tumor growth and injection of piperine (5 mg/kg) significantly inhibited the lung metastasis, according to "Piperine suppresses tumor growth and metastasis in vitro and in vivo in a 4T1 murine breast cancer model" by Lai LH, Fu QH, Liu Y, Jiang K, Guo QM, Chen QY, Yan B, Wang QQ, Shen JG.(3)

4. Cytotoxicity
In the investigation of the protective effect of piperine treatment on corticosterone-induced neurotoxicity in cultured rat pheochromocytoma (PC12) cells, showed that piperine co-treatment revealed a differential effect on the cytotoxicity of corticosterone and had its maximum inhibitory effect at 1 μM. Piperine (1 μM) co-treatment also significantly decreased intracellular reactive oxygen species level, and enhanced superoxide dismutase activity and total glutathione level in corticosterone-treated PC12 cells. In addition, piperine (1 μM) co-treatment was found to reverse the decreased brain-derived neurotrophic factor (BDNF) mRNA level caused by corticosterone in PC12 cells, according to "Protective Effects of Piperine Against Corticosterone-Induced Neurotoxicity in PC12 Cells" by Mao QQ, Huang Z, Ip SP, Xian YF, Che CT.(4)

5. Human metabolic syndrome
In the examination of the dietary supplementation with piperine, the active principle of black pepper, to high carbohydrate, high fat (HCHF) diet-fed rats as a model of human metabolic syndrome. Rats were fed with either HCHF diet (carbohydrate, 52%; fat, 24%; 25% fructose in drinking water) or cornstarch (CS) diet for a total of 16 weeks. Diets of the treatment groups (CS + piperine and HCHF + piperine) were supplemented with piperine for the last 8 weeks of this protocol, found that After 16 weeks, rats fed with HCHF diet developed hypertension, elevated oxidative stress and inflammation-induced cardiac changes (infiltration of inflammatory cells in heart, increase in count and degranulation of mast cells in heart, cardiac fibrosis and increase in ventricular stiffness), reduced responsiveness of aortic rings, impaired glucose tolerance, abdominal obesity together with liver fibrosis, fat deposition and increased plasma liver enzymes. Supplementation with piperine (375 mg/kg food; approximately 30 mg/kg/day) in HCHF-fed rats normalized blood pressure, improved glucose tolerance and reactivity of aortic rings, reduced plasma parameters of oxidative stress and inflammation, attenuated cardiac and hepatic inflammatory cell infiltration and fibrosis and improved liver function, according to "Piperine Attenuates Cardiovascular, Liver and Metabolic Changes in High Carbohydrate, High Fat-Fed Rats" by Diwan V, Poudyal H, Brown L.(5)

6. Hypertension
In the study of the effects of curcuma and black pepper compounds on increased blood pressure and remodeling of aorta in the rat model of experimental NO-deficient hypertension, showed that administration of piperine or curcumin, less their combination, is able to partially prevent the increase of blood pressure caused by chronic L-NAME administration. The spices modify the remodeling of the wall of the aorta induced by hypertension. Our results show that independent administration of curcumin is more effective in preventing negative changes in blood vessel morphology accompanying hypertensive disease, according to"Spice up the hypertension diet - curcumin and piperine prevent remodeling of aorta in experimental L-NAME induced hypertension" by Hlavačková L, Janegová A, Uličná O, Janega P, Cerná A, Babál P.(6)

7. Synergistic effects
in the evaluation of the effects of curcumin alone and with adjuvant piperine against benzo(a)pyrene (BaP) induced oxidative stress in lungs of male Swiss albino mice, showed that BaP treatment alone did not alter significantly the GST activity. Pretreatment with curcumin increased the GST activity in BaP treated group, which was enhanced further upon synergistic treatment with piperine and curcumin. Therefore, combined administration of curcumin and piperine shall prove to be more effective in attenuating BaP induced toxicity, according to "Synergistic effects of piperine and curcumin in modulating benzo(a)pyrene induced redox imbalance in mice lungs" by Sehgal A, Kumar M, Jain M, Dhawan DK.(7)

8. Antimicrobial, antileishmanial and cytotoxic compounds
in the evaluation of the petroleum ether and chloroform extracts of the root of Piper chaba showed antimicrobial, antileishmanial and cytotoxic activities, led to the isolation of Bornyl piperate (1), piperlonguminine (2) and piperine (3), showed that the isolated compounds (1 and 2) showed potent antifungal activity when compared with standard drug Nystatin, and significant cytotoxic activity with the IC(50) values of 0.76 and 0.83 µg mL(-1), respectively. These compounds were also found to have weak antibacterial and antileishmanial activities. This is the first report about the antileishmanial activity of Piper isolates, according to "Antimicrobial, antileishmanial and cytotoxic compounds from Piper chaba" by
Naz T, Mosaddik A, Rahman MM, Muhammad I, Haque ME, Cho SK.(8)

9. Antigenotoxic effects
In the investigation of the antigenotoxic effects of curcumin and piperine separately and in combination against benzo(a)pyrene (BaP) induced DNA damage in lungs and livers of mice, found thatPretreatments of curcumin and curcumin plus piperine before administration of single dose of BaP significantly decreased the levels of 8-oxo-dG content and % DNA in the comet tail in both the tissues. Moreover, the genoprotective potential of curcumin plus piperine was significantly higher as compared to curcumin alone against BaP induced DNA damage, according to "Combined effects of curcumin and piperine in ameliorating benzo(a)pyrene induced DNA damage" by Sehgal A, Kumar M, Jain M, Dhawan DK.(9)

10. Multidrug resistant cancer cells
Over-expression of P-gp, MRP1 and BCRP in tumor cells is one of the important mechanisms leading to multidrug resistance (MDR), which impairs the efficacy of chemotherapy. P-gp, MRP1 and BCRP are ABC (ATP-Binding Cassette) transporters, piperine can potentiate the cytotoxicity of anti-cancer drugs in resistant sublines, such as MCF-7/DOX and A-549/DDP, which were derived from MCF-7 and A-549 cell lines. At a concentration of 50 μM piperine could reverse the resistance to doxorubicin 32.16 and 14.14 folds, respectively. It also re-sensitized cells to mitoxantrone 6.98 folds. In addition, long-term treatment of cells by piperine inhibits transcription of the corresponding ABC transporter genes, according to "Piperine, a piperidine alkaloid from Piper nigrum re-sensitizes P-gp, MRP1 and BCRP dependent multidrug resistant cancer cells" by Li S, Lei Y, Jia Y, Li N, Wink M, Ma Y.(10)

11. Cytosolic isoforms hCA I and II
In the examination of Caffeine and piperine extracted for inhibition of the human (h) cytosolic isoforms hCA I and II, indicated that The IC(50) values of caffeine against hCA I was of 55 mM, whereas that of piperine of 60 mM. The IC(50) values of caffeine and piperine against hCA II were of 2 mM. Although these are quite weak inhibitors they may constitute leads for developing tighter binding compounds, according to "Carbonic anhydrase I and II inhibition with natural products: caffeine and piperine" by Sethi KK, Sahoo SK, Pichikala JN, Suresh P.(11)

12. Etc.
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Sources
(1) http://jac.oxfordjournals.org/content/61/6/1270.full
(2) http://www.ncbi.nlm.nih.gov/pubmed/22389056
(3) http://www.ncbi.nlm.nih.gov/pubmed/22388073
(4) http://www.ncbi.nlm.nih.gov/pubmed/22205277
(5) http://www.ncbi.nlm.nih.gov/pubmed/22038304
(6) http://www.ncbi.nlm.nih.gov/pubmed/22005253
(7) http://www.ncbi.nlm.nih.gov/pubmed/21859361
(8) http://www.ncbi.nlm.nih.gov/pubmed/21834629
(9) http://www.ncbi.nlm.nih.gov/pubmed/21827816
(10) http://www.ncbi.nlm.nih.gov/pubmed/21802927
(11) http://www.ncbi.nlm.nih.gov/pubmed/21612376