Capsaicin may have important potential for promoting vascular and metabolic health

Open Heart - Tập 2 Số 1 - Trang e000262 - 2015
Mark F. McCarty1, James J. DiNicolantonio2, James H. O’Keefe2
1Catalytic Longevity , Encinitas, California , USA.
2Mid America Heart Institute, St. Luke's Hospital, Kansas City, Missouri, USA

Tóm tắt

Capsaicin, the phytochemical responsible for the spiciness of peppers, has the potential to modulate metabolism via activation of transient receptor potential vanilloid 1 (TRPV1) receptors, which are found not only on nociceptive sensory neurons, but also in a range of other tissues. TRPV1 activation induces calcium influx, and in certain tissues this is associated with increased activation or expression of key proteins such as endothelial nitric oxide synthase (eNOS), uncoupling protein 2 (UCP2), KLF2, PPARdelta, PPARgamma, and LXRα. The calcium influx triggered by TRPV1 activation in endothelial cells mimics the impact of shear stress in this regard, activating and increasing the expression of eNOS—but also increasing expression of cox-2, thrombomodulin, and nrf2-responsive antioxidant enzymes, while decreasing expression of proinflammatory proteins. Hence, dietary capsaicin has favourably impacted endothelium-dependent vasodilation in rodents. TRPV1-mediated induction of LXRα in foam cells promotes cholesterol export, antagonising plaque formation. Capsaicin-mediated activation of TRPV1-expressing neurons in the gastrointestinal tract promotes sympathetically mediated stimulation of brown fat, raising metabolic rate. The increased expression of UCP2 induced by TRPV1 activation exerts a protective antioxidant effect on the liver in non-alcoholic fatty liver disease, and on vascular endothelium in the context of hyperglycaemia. In rodent studies, capsaicin-rich diets have shown favourable effects on atherosclerosis, metabolic syndrome, diabetes, obesity, non-alcoholic fatty liver, cardiac hypertrophy, hypertension and stroke risk. Clinically, ingestion of capsaicin—or its less stable non-pungent analogue capsiate—has been shown to boost metabolic rate modestly. Topical application of capsaicin via patch was found to increase exercise time to ischaemic threshold in patients with angina. Further clinical studies with capsaicin administered in food, capsules, or via patch, are needed to establish protocols that are tolerable for most patients, and to evaluate the potential of capsaicin for promoting vascular and metabolic health.

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Tài liệu tham khảo

10.1016/j.jdiacomp.2012.11.006

10.1124/pr.113.008268

10.1007/s00424-010-0902-5

10.1016/S0028-3908(03)00100-X

10.1016/0041-008X(84)90121-2

10.1016/j.jconrel.2014.09.027

Chaiyasit, 2009, Pharmacokinetic and the effect of capsaicin in Capsicum frutescens on decreasing plasma glucose level, J Med Assoc Thai, 92, 108

10.1097/00001756-199511270-00016

10.1016/S0024-3205(01)01027-X

Vyklicky, 2008, Calcium-dependent desensitization of vanilloid receptor TRPV1: a mechanism possibly involved in analgesia induced by topical application of capsaicin, Physiol Res, 57, S59, 10.33549/physiolres.931478

10.1213/ane.0b013e318162cfa3

10.1097/AJP.0b013e318158ed9e

10.3109/15360288.2010.547561

10.2174/138161208783330754

10.1371/journal.pone.0078184

10.1016/S0008-6363(99)00094-2

10.1073/pnas.1003833107

10.1161/ATVBAHA.109.193540

10.1182/blood-2009-05-224824

10.1172/JCI24787

10.1084/jem.20031132

10.1161/01.RES.0000159707.05637.a1

10.1182/blood-2006-07-036020

10.1161/ATVBAHA.108.165811

10.1097/00005344-200310000-00009

10.1093/cvr/cvr104

10.1016/j.cmet.2010.05.015

10.1161/STROKEAHA.111.618306

10.1093/cvr/cvr245

Zhao, 2013, Activation of TRPV1 prevents OxLDL-induced lipid accumulation and TNF-alpha-induced inflammation in macrophages: role of liver X receptor alpha, Mediators Inflamm, 2013, 925171, 10.1155/2013/925171

10.1097/01.fjc.0000137161.76616.85

10.1007/s00424-011-0921-x

10.1161/HYPERTENSIONAHA.114.03105

10.1152/ajpheart.01191.2007

10.1038/22761

10.1111/j.1476-5381.2011.01645.x

10.1016/j.ijcard.2008.12.080

10.1016/j.ijcard.2010.02.034

10.1186/1475-2840-12-69

10.1007/s00424-012-1078-y

Gao, 2014, TRPV1 activation attenuates high-salt diet-induced cardiac hypertrophy and fibrosis through PPAR-delta upregulation, PPAR Res, 2014, 491963, 10.1155/2014/491963

10.1016/j.cardiores.2004.11.011

Negre-Salvayre, 1997, A role for uncoupling protein-2 as a regulator of mitochondrial hydrogen peroxide generation, FASEB J, 11, 809, 10.1096/fasebj.11.10.9271366

10.1038/415096a

10.1179/135100007X162158

10.1002/dmrr.613

10.1016/j.diabres.2007.01.031

10.1161/CIRCRESAHA.111.262170

10.2337/db07-1292

10.1016/j.mam.2007.09.014

10.1136/gut.2007.147496

10.1007/s00424-013-1274-4

10.1016/j.mehy.2004.01.040

10.1016/j.febslet.2007.07.082

10.1089/jmf.2010.1367

10.1002/oby.20246

10.1186/s12933-015-0183-6

10.2337/db11-1503

10.1271/bbb.90555

10.1152/japplphysiol.00128.2010

10.1093/chemse/bjr100

10.1016/j.appet.2013.11.005

10.3945/ajcn.111.018606

10.1097/MOL.0b013e32835a4f40

10.1177/1091581809359427

10.3945/ajcn.2008.26561

10.1097/MCO.0b013e3283653ee1

10.1080/1040-830491379236

Mozsik, 2014, Capsaicin as new orally applicable gastroprotective and therapeutic drug alone or in combination with nonsteroidal anti-inflammatory drugs in healthy human subjects and in patients, Prog Drug Res, 68, 209

10.1556/APhysiol.101.2014.4.4

10.1007/s12029-014-9610-2

10.1177/0192623312444471

10.3748/wjg.v11.i21.3175

10.1016/0278-6915(94)90127-9

10.1007/978-3-642-38007-5_6

10.1128/IAI.01271-12

10.1079/BJN2003938

Peppin, 2011, Tolerability of NGX-4010, a capsaicin 8% patch for peripheral neuropathic pain, J Pain Res, 4, 385, 10.2147/JPR.S22954

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Open Heart

Tập 2 Số 1

e000262

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