In this study, 104 RIL (Recombinant Inbred Pepper Lines: F6) populations which generated by selfing Capsicum annuum (Long pepper) × Capsicum frutescens (PI281420) F6 population were characterized in terms of detailed bioactive properties, major phenolic composition, tocopherol and capsaicinoid profile. Total phenolics, flavonoid and total anthocyanin contents of the red pepper lines were in the range of 7.06-17.15 mg gallic acid equivalent (GAE)/g dw, 1.10-5.46 mg catechin equivalent (CE)/g dw and 7.9-516.6 mg/kg dw extract, respectively. Antiradical activity and antioxidant capacity values also ranged between 18.99 and 49.73% and 6.97-16.47 mg ascorbic acid equivalent (AAE)/kg dw, respectively. Capsaicin and dihydrocapsaicin levels showed a wide variance with the range of 27.9-1405.9 and 12.3-640.4 mg/100 g dw, respectively. Scoville heat unit revealed that the 95% of the peppers were highly pungent. The major tocopherol was alpha tocopherol for the pepper samples with the highest level of 1078.4 µg/g dw. The major phenolics were detected as p-coumaric acid, ferulic acid, myricetin, luteolin and quercetin. Pepper genotypes showed significant differences in terms of the characterized properties and principal component analysis was applied successfully to reveal the similar genotypes.

Transient receptor potential vanilloid 1 (TRPV1)-expressing sensory nerves innervate the pancreatic islets. Sensory neuropeptides, including calcitonin gene-related peptide (CGRP) and substance P (SP), participate in insulin secretion. This study aimed to investigate the role of TRPV1 in glucose-induced insulin secretion.

TRPV1^-/- and wild-type (WT) mice were fed a normal diet for 24 weeks. Glucose tolerance and insulin secretion were measured at the end of the experiments.

TRPV1^-/- mice had greater impairments in glucose tolerance and higher decrease in glucose-induced insulin secretion than WT mice. Capsaicin (a TRPV1 agonist) increased insulin secretion in WT, but not in TRPV1^-/- mice. Glucose-induced insulin secretion was blunted in TRPV1^-/- mice, and was attenuated by AMG9810 (a TRPV1 inhibitor), CGRP_8-37 (a CGRP receptor antagonist), or RP67580 (a NK-1 receptor antagonist) in WT mice. Glucose-induced SP and CGRP release from WT pancreas was higher than that from TRPV1^-/- pancreas.

TRPV1 mediates glucose-induced insulin secretion likely through CGRP and SP release.

In this study, two capsaicin analogues, N-eicosapentaenoyl vanillylamine (EPVA) and N-docosahexaenoyl vanillylamine (DHVA), were enzymatically synthesized from their corresponding n-3 long chain polyunsaturated fatty acids eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), both dietary relevant components. The compounds significantly reduced the production of some lipopolysaccharide (LPS)-induced inflammatory mediators, including nitric oxide (NO), macrophage-inflammatory protein-3α (CCL20) and monocyte chemoattractant protein-1 (MCP-1 or CCL2), by RAW264.7 macrophages. Next to this, only EPVA increased insulin secretion by pancreatic INS-1 832/13 β-cells, while raising intracellular Ca2+ and ATP concentrations. This suggests that the stimulation of insulin release occurs through an increase in the intracellular ATP/ADP ratio in the first phase, while is calcium-mediated in the second phase. Although it is not yet known whether EPVA is endogenously produced, its potential therapeutic value for diabetes treatment merits further investigation.

Quorum sensing controls bacterial pathogenesis and virulence; hence, interrupting this system renders pathogenic bacteria non-virulent, and presents a novel treatment for various bacterial infections. In the search for novel anti-quorum sensing (AQS) compounds, 14 common culinary herbs and spices were screened for potential antipathogenicity activity against Chromobacterium violaceum ATCC 12472. Extracts of Glycyrrhiza glabra (liquorice), Apium graveolens (celery), Capsicum annuum (cayenne pepper) and Syzygium anisatum (aniseed) demonstrated good AQS potential, yielding opaque halo zones ranging from 12⁻19 mm diameter at sub-minimum inhibitory concentrations (0.350⁻4.00 mg/mL). For the same species, the percentage reduction in violacein production ranged from 56.4 to 97.3%. Zones with violacein inhibitory effects were evident in a celery extract analysed using high performance thin layer chromatography-bio-autography. The major active compound was isolated from celery using preparative-high performance liquid chromatography-mass spectrometry and identified using gas chromatography-mass spectrometry (GC-MS) as 3-n-butyl-4,5-dihydrophthalide (sedanenolide). Potent opaque zones of inhibition observed on the HPTLC-bio-autography plate seeded with C. violaceum confirmed that sedanenolide was probably largely responsible for the AQS activity of celery. The bacteriocidal properties of many herbs and spices are reported. This study, however, was focussed on AQS activity, and may serve as initial scientific validation for the anti-infective properties ascribed to several culinary herbs and spices.

Capsaicin, the major active constituent of chilli, is an agonist on transient receptor potential vanilloid channel 1 (TRPV1). TRPV1 is present on many metabolically active tissues, making it a potentially relevant target for metabolic interventions. Insulin resistance and obesity, being the major components of metabolic syndrome, increase the risk for the development of cardiovascular disease, type 2 diabetes, and non-alcoholic fatty liver disease. In vitro and pre-clinical studies have established the effectiveness of low-dose dietary capsaicin in attenuating metabolic disorders. These responses of capsaicin are mediated through activation of TRPV1, which can then modulate processes such as browning of adipocytes, and activation of metabolic modulators including AMP-activated protein kinase (AMPK), peroxisome proliferator-activated receptor α (PPARα), uncoupling protein 1 (UCP1), and glucagon-like peptide 1 (GLP-1). Modulation of these pathways by capsaicin can increase fat oxidation, improve insulin sensitivity, decrease body fat, and improve heart and liver function. Identifying suitable ways of administering capsaicin at an effective dose would warrant its clinical use through the activation of TRPV1. This review highlights the mechanistic options to improve metabolic syndrome with capsaicin.

Blood mononuclear cells consist of T cells and monocyte derived cells. Beside immunity, the blood mononuclear cells belong to the complex tissue control system (TCS), where they exhibit morphostatic function by stimulating proliferation of tissue stem cells followed by cellular differentiation, that is stopped after attaining the proper functional stage, which differs among various tissue types. Therefore, the term immune and morphostatic system (IMS) should be implied. The TCS-mediated morphostasis also consists of vascular pericytes controlled by autonomic innervation, which is regulating the quantity of distinct tissues in vivo. Lack of proper differentiation of tissue cells by TCS causes either tissue underdevelopment, e.g., muscular dystrophy, or degenerative functional failures, e.g., type 1 diabetes and age-associated diseases. With the gradual IMS regression after 35 years of age the gonadal infertility develops, followed by a growing incidence of age-associated diseases and cancers. Without restoring an altered TCS function in a degenerative disease, the implantation of tissue-specific stem cells alone by regenerative medicine can not be successful. Transfused young blood could temporarily restore fertility to enable parenthood. The young blood could also temporarily alleviate aging diseases, and this can be extended by substances inducing IMS regeneration, like the honey bee propolis. The local and/or systemic use of honey bee propolis stopped hair and teeth loss, regressed varicose veins, improved altered hearing, and lowered high blood pressure and sugar levels. Complete regression of stage IV ovarian cancer with liver metastases after a simple elaborated immunotherapy is also reported.

Besides the basic role to flavor and color foods, several health benefits have been attributed to spices. The traditional Cameroonian food "Nkui" is prepared using several spices (Afrostyrax lepidophyllus Mildbr., Capsicum frutescens Linn., Fagara leprieurii Guill. et Perr., Fagara tessmannii Engl., Mondia whitei Hook. F. Skell., Pentadiplandra brazzeana Baill., Solanum gilo Raddi., Tetrapleura tetraptera Taub. and Xylopia parviflora A. Rich. Benthane) that are believed to have a positive impact on the female reproductive physiology. Aiming to determine the potential effect of this food on the female reproductive tract, we evaluated the estrogenic properties of aqueous and ethanol extracts of Nkui using a 3-day uterotrophic assay in ovariectomized (OVX) rats.

OVX female Wistar rats were randomly separated in several groups of five animals each and submitted to a 3-day uterotrophic assay (per os). At the end of treatment, animals were sacrificed and uterus, vagina and mammary gland collected and fixed in 10 % formalin for histological analysis.

These extracts increased the uterine wet weight, the uterine and vaginal epithelial heights, and the lumen and diameter of alveoli in the mammary glands. They also altered the estradiol-induced increase of uterine wet weight. The dichloromethane and methanol fractions of the ethanol extract exhibited estrogenic properties as well by increasing uterine and vaginal endpoints.

These results suggest that the spices of "Nkui" contain estrogenic phytoconstituents and this traditional food may be considered as functional.

The present study aims to evaluate zootechnic parameters and blood sugar in rabbits submitted to diets containing different levels of pepper (Capsicum frutescens).

To this end, 30 rabbits weighing on average 1252±35 g at the beginning of the experiment were subjected to five rations with three repetitions for 56 days: The food R0 (or control) which is floury provender contains 0% of C. frutescens; R5, R10, R15, and R20 provender containing, respectively, 0.5%, 1%, 1.5%, and 2% of C. frutescens fruits' powder. Rabbits consumed on average from 75.47 to 80.97 g dry matter.

Digestibility ranged from 52.39% to 61.01%. The average daily gain and feed consumption index were similar for all diets. Blood glucose was amended by the various servings is 0.98 g/L and 0.88 g/L, respectively, for doses.

It appears from this study that rabbits consumed well diets containing C. frutescens. However, C. frutescens' effect on the growth performances of rabbits is not noticeable. Furthers experiments will be useful to evaluate C. frutescens' mechanism of action on blood sugar.

Obesity is the most prevalent nutritional disease and a growing public health problem worldwide. This disease is a causal component of the metabolic syndrome related with abnormalities, including hyperglycemia, dyslipidemia, hypertension, inflammation, among others. There are anti-obesity drugs, affecting the fundamental processes of the weight regulation; however they have shown serious side effects, which outweigh their beneficial effects. Most recent studies on the treatment of obesity and its complications have focused on the potential role of different plants preparation that can exert a positive effect on the mechanisms involved in this pathology. For instance, anti-obesity effects of green tea and its isolated active principles have been reported in both in vitro (cell cultures) and in vivo (animal models) that possess healthy effects, decreasing adipose tissue through reduction of adipocytes differentiation and proliferation. A positive effect in lipid profile, and lipid and carbohydrates metabolisms were demonstrated as well. In addition, anti-inflammatory and antioxidant activities were studied. However, the consumption of green tea and its products is not that common in Western countries, where other plants with similar bioactivity predominate; nevertheless, the effect extension has not been analyzed in depth, despite of their potential as alternative treatment for obesity. In this review the anti-obesity potential and reported mechanisms of action of diverse plants such as: Camellia sinensis, Hibiscus sabdariffa, Hypericum perforatum, Persea americana, Phaseolus vulgaris, Capsicum annuum, Rosmarinus officinalis, Ilex paraguariensis, Citrus paradisi, Citrus limon, Punica granatum, Aloe vera, Taraxacum officinale and Arachis hypogaea is summarized. We consider the potential of these plants as natural alternative treatments of some metabolic alterations associated with obesity.

Glucose intolerance and cardiovascular complications are major symptoms in patients with diabetes. Many therapies have proven beneficial in treating diabetes in animals by protecting the cardiovascular system and increasing glucose utilization. In this study, we evaluated the effects of caffeic acid phenethyl amide (CAPA) on glucose homeostasis and vascular function in streptozotocin (STZ)-induced type 1 diabetic rats.

Diabetes (blood glucose levels > 350 mg/dL), was induced in Wistar rats by a single intravenous injection of 60 mg/kg STZ. Hypoglycemic effects were then assessed in normal and type 1 diabetic rats. In addition, coronary blood flow in Langendorff-perfused hearts was evaluated in the presence or absence of nitric oxide synthase (NOS) inhibitor. The thoracic aorta was used to measure vascular response to phenylephrine. Finally, the effect of chronic treatment of CAPA and insulin on coronary artery flow and vascular response to phenylephrine were analyzed in diabetic rats.

Oral administration of 0.1 mg/kg CAPA decreased plasma glucose in normal (32.9 ± 2.3% decrease, P < 0.05) and diabetic rats (11.8 ± 5.5% decrease, P < 0.05). In normal and diabetic rat hearts, 1-10 μM CAPA increased coronary flow rate, and this increase was abolished by 10 μM NOS inhibitor. In the thoracic aorta, the concentration/response curve of phenylephrine was right-shifted by administration of 100 μM CAPA. Coronary flow rate was reduced to 7.2 ± 0.2 mL/min at 8 weeks after STZ-induction. However, 4 weeks of treatment with CAPA (3 mg/kg, intraperitoneal, twice daily) started at 4 weeks after STZ induction increased flow rate to 11.2 ± 0.5 mL/min (P < 0.05). In addition, the contractile response induced by 1 μM phenylephrine increased from 6.8 ± 0.6 mN to 11.4 ± 0.4 mN (P < 0.05) and 14.9 ± 1.4 mN (P < 0.05) by insulin (1 IU/kg, intraperitoneal) or CAPA treatment, respectively.

CAPA induced hypoglycemic activity, increased coronary blood flow and vascular response to phenylephrine in type 1 diabetic rats. The increase in coronary blood flow may result from endothelial NOS activation. However, the detailed cellular mechanisms need to be further evaluated.

With increasing lifespan, therapeutic interventions for the treatment of disorders such as type 2 diabetes mellitus are in great demand. Despite billions of dollars invested to reduce the symptoms and complications due to diabetes mellitus, current treatments (e.g., insulin replacements, sensitization) remain inadequate, justifying the search for novel therapeutic approaches or alternative solutions, including dietary supplementation, for the treatment of diabetes mellitus in every age group. The involvement of the vanilloid system in the regulation of metabolism has been identified, and the emerging role of its receptors, the transient receptor potential vanilloid type 1 (TRPV1), in diabetes was recently demonstrated. Indeed, beneficial effects of dietary capsaicin, an agonist of TRPV1 receptors, were identified for improving glucose, insulin and glucagon-like peptide-1 levels. Recent findings regarding TRPV1 receptors in association with whole body metabolism including glucose homeostasis will be reviewed in this article.

The present study was conducted to clarify whether a low or a high, but tolerable, dietary dose of red chilli (RC) can ameliorate the diabetes related complications in a high-fat (HF) diet-fed streptozotocin (STZ)-induced type 2 diabetes model of rats. Five-week-old male Sprague Dawley rats were fed a HF diet for 2 weeks then randomly divided into four groups namely: normal control (NC), diabetic control (DBC), red chilli low (RCL, 0.5%) and red chilli high (RCH, 2.0%) groups. Diabetes was induced by an intraperitoneal (i.p.) injection of STZ (40 mg/kg BW) in all groups except the NC group. After 4 weeks feeding of experimental diets, the fasting blood glucose concentrations in both RC fed groups were not significantly different. The serum insulin concentration was significantly (p < 0.05) increased in the RCH group compared with the DBC and RCL groups. Blood HbA1c, liver weight, liver glycogen and serum lipids were not influenced by the feeding of RC-containing diets. The data of this study suggest that 2% dietary RC is insulinotropic rather than hypoglycemic at least in this experimental condition.

Enzymatic syntheses of N-vanillyl-nonanamide, 1, glycosides with D-glucose, 2, D-galactose, 3, D-mannose, 4, D-ribose, 5, maltose, 6, and lactose, 7, were carried out using amyloglucosidase from Rhizopus and beta-glucosidase from sweet almond. The latter catalysed the syntheses of N-vanillyl-nonanamide glycosides (8-13) and exclusively yielded beta-glycosides with carbohydrates 2, 3, 4, 6 and 7, while amyloglucosidase yielded C1-alpha- and beta-glycosides and 6-O-aryl derivatives (8, 9, 11 and 12).

Capsaicin-sensitive afferent neurons including transient receptor potential vanilloid subfamily 1, TRPV1, and neurohormonal peptides participate in the physiological regulation of pancreatic endocrine. However, the direct effect of capsaicin on insulin secretion remains unknown. Our present study showed that TRPV1 is expressed in islet beta cells as well as in neurons in rat pancreas, and also in rat beta cell lines, RIN and INS1. Capsaicin (10(-11)-10(-9) M) dose-dependently increased insulin secretion from RIN cells, and this effect was inhibited by either a TRPV1 inhibitor capsazepine or EDTA. Systemic capsaicin (10 mg/kg, s.c.) increased plasma insulin level 1 h after the treatment. We demonstrated for the first time that TRPV1 is functionally expressed in rat islet beta cells and plays a role in insulin secretion as a calcium channel. This study may account for the influences of capsaicin on the food intake and energy consumption as well as on the pathophysiological regulation of pancreatic endocrine.