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Keywords = pungent pepper

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18 pages, 2745 KiB  
Article
Obesity-Induced MASLD Is Reversed by Capsaicin via Hepatic TRPV1 Activation
by Padmamalini Baskaran, Ryan Christensen, Kimberley D. Bruce and Robert H. Eckel
Curr. Issues Mol. Biol. 2025, 47(8), 618; https://doi.org/10.3390/cimb47080618 - 4 Aug 2025
Abstract
Background and Objectives: Metabolic dysfunction-associated steatotic liver disease (MASLD) is a progressive liver disorder associated with metabolic risk factors such as obesity, type 2 diabetes, and cardiovascular disease. If left untreated, the accumulation of excess hepatic fat can lead to inflammation, fibrosis, cirrhosis, [...] Read more.
Background and Objectives: Metabolic dysfunction-associated steatotic liver disease (MASLD) is a progressive liver disorder associated with metabolic risk factors such as obesity, type 2 diabetes, and cardiovascular disease. If left untreated, the accumulation of excess hepatic fat can lead to inflammation, fibrosis, cirrhosis, hepatocellular carcinoma, and ultimately liver failure. Capsaicin (CAP), the primary pungent compound in chili peppers, has previously been shown to prevent weight gain in high-fat diet (HFD)-induced obesity models. In this study, we investigated the potential of dietary CAP to prevent HFD-induced MASLD. Methods: C57BL/6 mice were fed an HFD (60% kcal from fat) with or without 0.01% CAP supplementation for 26 weeks. We evaluated CAP’s effects on hepatic fat accumulation, inflammation, and mitochondrial function to determine its role in preventing MASLD. Results: CAP acts as a potent and selective agonist of the transient receptor potential vanilloid 1 (TRPV1) channel. We confirmed TRPV1 expression in the liver and demonstrated that CAP activates hepatic TRPV1, thereby preventing steatosis, improving insulin sensitivity, reducing inflammation, and enhancing fatty acid oxidation. These beneficial effects were observed in wild-type but not in TRPV1 knockout mice. Mechanistically, CAP-induced TRPV1 activation promotes calcium influx and activates AMPK, which leads to SIRT1-dependent upregulation of PPARα and PGC-1α, enhancing mitochondrial biogenesis and lipid metabolism. Conclusions: Our findings suggest that dietary CAP prevents MASLD through TRPV1 activation. TRPV1 signaling represents a promising therapeutic target for the prevention and management of MASLD in individuals with metabolic disorders. Full article
(This article belongs to the Special Issue Mechanisms and Pathophysiology of Obesity)
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29 pages, 1977 KiB  
Review
Capsaicin as a Microbiome Modulator: Metabolic Interactions and Implications for Host Health
by Iván Artemio Corral-Guerrero, Angela Elena Martínez-Medina, Litzy Yazmin Alvarado-Mata, Ana Cristina Figueroa Chávez, Roberto Muñoz-García, Miriam Paulina Luévanos-Escareño, Jazel Doménica Sosa-Martínez, María José Castro-Alonso, Padma Nimmakayala, Umesh K. Reddy and Nagamani Balagurusamy
Metabolites 2025, 15(6), 372; https://doi.org/10.3390/metabo15060372 - 5 Jun 2025
Viewed by 3057
Abstract
Background/Objectives: Capsaicin is the principal pungent compound in chili peppers and is increasingly recognized as a multifunctional phytochemical with systemic effects beyond its sensory properties. It has been linked to metabolic regulation, neuroprotection, inflammation control, and cancer modulation. This review aims to provide [...] Read more.
Background/Objectives: Capsaicin is the principal pungent compound in chili peppers and is increasingly recognized as a multifunctional phytochemical with systemic effects beyond its sensory properties. It has been linked to metabolic regulation, neuroprotection, inflammation control, and cancer modulation. This review aims to provide an integrative synthesis of capsaicin’s metabolism, its interaction with the gut microbiome, and its physiological implications across organ systems. Methods: We conducted a critical literature review of recent in vivo and in vitro studies exploring capsaicin’s metabolic fate, biotransformation by host enzymes and gut microbes, tissue distribution, and molecular pathways. The literature was analyzed thematically to cover gastrointestinal absorption, hepatic metabolism, microbiota interactions, and systemic cellular responses. Results: Capsaicin undergoes extensive hepatic metabolism, producing hydroxylated and dehydrogenated metabolites that differ in transient receptor potential vanilloid type 1 (TRPV1) receptor affinity and tissue-specific bioactivity. It crosses the blood–brain barrier, alters neurotransmitter levels, and accumulates in brain regions involved in cognition. In addition to its systemic effects, capsaicin appears to undergo microbial transformation and influences gut microbial composition, favoring short-chain fatty acid producers and suppressing pro-inflammatory taxa. These changes contribute to anti-obesity, anti-inflammatory, and potentially anticancer effects. Dose-dependent adverse outcomes, such as epithelial damage or tumor promotion, have also been observed. Conclusions: Capsaicin represents a diet-derived bioactive molecule whose systemic impact is shaped by dynamic interactions between host metabolism and the gut microbiota. Clarifying its biotransformation pathways and context-specific effects is essential for its safe and effective use in metabolic and neurological health strategies. Full article
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16 pages, 3006 KiB  
Article
Genetic and Seasonal Factors Influence Pungent Pepper Capsaicinoid and Vitamin C Content
by Ingrid Melinda Gyalai, Lajos Helyes, Hussein G. Daood, Flórián Kovács, Adrienn Szarvas and Ferenc Lantos
Horticulturae 2025, 11(3), 286; https://doi.org/10.3390/horticulturae11030286 - 6 Mar 2025
Cited by 3 | Viewed by 1291
Abstract
Pungent red peppers and chilis are healthy foods and crucial ingredients of modern diets due to their content of bioactive phytochemicals such as carotenoids, tocopherols, capsaicinoids, polyphenols, and vitamin C. The production of pungent peppers with outstanding nutritional properties is influenced by genetic [...] Read more.
Pungent red peppers and chilis are healthy foods and crucial ingredients of modern diets due to their content of bioactive phytochemicals such as carotenoids, tocopherols, capsaicinoids, polyphenols, and vitamin C. The production of pungent peppers with outstanding nutritional properties is influenced by genetic factors and their interaction with the environments where they are cultivated. This study was conducted to investigate the effects of genotype and climate conditions on the response of capsaicinoids and vitamin C. The extracts of pungent materials and vitamin C were separated and qualitatively determined by HPLC alone or hyphenated with mass spectroscopy. Four genotypes were selected and cultivated under traditional agricultural practices in southern Hungary. The yield properties and the contents of capsaicinoids and vitamin C were significantly influenced by genetic factors and, to a high extent, by the interaction between genotype × environment. The highest yield of 2.86 ± 0.59 kg/m2 was recorded for the CS variety. The yield was significantly decreased under high precipitation and low air temperature. The highest concentration of capsaicin of 1586–1734 µg/g dwt was found in the BHJ variety. The lowest level of 514 µg/g dwt of capsaicin was determined in the CS variety, in which the content significantly increased to 772 µg/g dwt with the increase in rainfall and decrease in air temperature in the warmer season of 2022. In most cultivars examined, capsaicin content negatively responded to the change of the climate toward higher precipitation and lower temperature except for SZ178, in which the concentration of capsaicinoids stayed insignificantly varied. The amount of vitamin C ranged between 570 and 135 µg/g dwt, with the highest content being in the BHJ and the lowest in the REK variety. In most varieties except the REK, vitamin C positively responded to a high and negatively to the reduced levels of precipitation. In conclusion, the phytochemical components of hot peppers respond differently to climatic factors—such as high rainfall, elevated air temperature, and intense sunlight—depending on the genotype’s ability to adapt to environmental changes. Full article
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16 pages, 2295 KiB  
Review
The Influence of Different Factors on the Metabolism of Capsaicinoids in Pepper (Capsicum annuum L.)
by Yuanling Yang, Chengan Gao, Qingjing Ye, Chenxu Liu, Hongjian Wan, Meiying Ruan, Guozhi Zhou, Rongqing Wang, Zhimiao Li, Ming Diao and Yuan Cheng
Plants 2024, 13(20), 2887; https://doi.org/10.3390/plants13202887 - 15 Oct 2024
Cited by 13 | Viewed by 3474
Abstract
Pepper is a globally cultivated vegetable known for its distinct pungent flavor, which is derived from the presence of capsaicinoids, a class of unique secondary metabolites that accumulate specifically in pepper fruits. Since the accumulation of capsaicinoids is influenced by various factors, it [...] Read more.
Pepper is a globally cultivated vegetable known for its distinct pungent flavor, which is derived from the presence of capsaicinoids, a class of unique secondary metabolites that accumulate specifically in pepper fruits. Since the accumulation of capsaicinoids is influenced by various factors, it is imperative to comprehend the metabolic regulatory mechanisms governing capsaicinoids production. This review offers a thorough examination of the factors that govern the metabolism of capsaicinoids in pepper fruit, with a specific focus on three primary facets: (1) the impact of genotype and developmental stage on capsaicinoids metabolism, (2) the influence of environmental factors on capsaicinoids metabolism, and (3) exogenous substances like methyl jasmonate, chlorophenoxyacetic acid, gibberellic acid, and salicylic acid regulate capsaicinoid metabolism. The findings of this study are expected to enhance comprehension of capsaicinoids metabolism and aid in the improvement of breeding and cultivation practices for high-quality pepper in the future. Full article
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49 pages, 2460 KiB  
Review
Capsaicin: Emerging Pharmacological and Therapeutic Insights
by Elena Madalina Petran, Argyrios Periferakis, Lamprini Troumpata, Aristodemos-Theodoros Periferakis, Andreea-Elena Scheau, Ioana Anca Badarau, Konstantinos Periferakis, Ana Caruntu, Ilinca Savulescu-Fiedler, Romina-Marina Sima, Daniela Calina, Carolina Constantin, Monica Neagu, Constantin Caruntu and Cristian Scheau
Curr. Issues Mol. Biol. 2024, 46(8), 7895-7943; https://doi.org/10.3390/cimb46080468 - 24 Jul 2024
Cited by 18 | Viewed by 10259
Abstract
Capsaicin, the most prominent pungent compound of chilli peppers, has been used in traditional medicine systems for centuries; it already has a number of established clinical and industrial applications. Capsaicin is known to act through the TRPV1 receptor, which exists in various tissues; [...] Read more.
Capsaicin, the most prominent pungent compound of chilli peppers, has been used in traditional medicine systems for centuries; it already has a number of established clinical and industrial applications. Capsaicin is known to act through the TRPV1 receptor, which exists in various tissues; capsaicin is hepatically metabolised, having a half-life correlated with the method of application. Research on various applications of capsaicin in different formulations is still ongoing. Thus, local capsaicin applications have a pronounced anti-inflammatory effect, while systemic applications have a multitude of different effects because their increased lipophilic character ensures their augmented bioavailability. Furthermore, various teams have documented capsaicin’s anti-cancer effects, proven both in vivo and in vitro designs. A notable constraint in the therapeutic effects of capsaicin is its increased toxicity, especially in sensitive tissues. Regarding the traditional applications of capsaicin, apart from all the effects recorded as medicinal effects, the application of capsaicin in acupuncture points has been demonstrated to be effective and the combination of acupuncture and capsaicin warrants further research. Finally, capsaicin has demonstrated antimicrobial effects, which can supplement its anti-inflammatory and anti-carcinogenic actions. Full article
(This article belongs to the Special Issue Latest Review Papers in Molecular Biology 2024)
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19 pages, 3557 KiB  
Article
Agronomic and Functional Quality Traits in Various Underutilized Hot Pepper Landraces
by Marwa Chouikhi, Imen Tlili, Imen Henane, Sándor Takács, Hussein Daood, Zoltàn Pék, Lajos Helyes, Anna Montefusco, Monica De Caroli, Gian Pietro Di Sansebastiano, Muhammad Azam, Mohammed Wasim Siddiqui, Riadh Ilahy, Marcello Salvatore Lenucci and Thouraya R’him
Horticulturae 2024, 10(7), 710; https://doi.org/10.3390/horticulturae10070710 - 4 Jul 2024
Viewed by 1596
Abstract
Landraces are considered a crucial component of biodiversity conservation, serving as a reservoir of genetic diversity. Consequently, the collection, cultivation, and detailed characterization of such landraces constitute an inherent aspect of the world’s natural resource heritage. This effort holds promise for the development [...] Read more.
Landraces are considered a crucial component of biodiversity conservation, serving as a reservoir of genetic diversity. Consequently, the collection, cultivation, and detailed characterization of such landraces constitute an inherent aspect of the world’s natural resource heritage. This effort holds promise for the development of elite varieties capable of thriving amidst continuous global climate fluctuations. In this context, we conducted a comprehensive assessment of the main agronomic attributes, physico-chemical properties, and functional quality traits of the major hot pepper landraces adapted to diverse climatic conditions in Tunisia. These landraces include ‘Dhirat’, ‘Semmane’, ‘Beldi’, ‘Nabeul’, ‘Jerid’, ‘Mahdia’, ‘Cayenne’, ‘Kairouan’, and ‘Baklouti’. Most of the pepper landraces exhibited satisfactory yields, ranging from 1163.25 to 1841.67 g plant−1 in ‘Jerid’ and ‘Kairouan’, respectively, indicating robust productivity, especially under prevailing climatic changes and high temperatures during both growing cycles. The levels of antioxidants comprising capsaicinoids, carotenoids, phenolics, and tocopherols, as well as radical scavenging activity, emerged as key discriminating factors among pungent pepper landraces. Irrespective of genotype, capsaicin and dihydrocapsaicin constituted the major capsaicinoids, accounting for 44–91% of the total capsaicinoids content. Total capsaicinoids ranged from 1.81 µg g−1 fw to 193.71 µg g−1 fw, with ‘Baklouti’ and ‘Jerid’ identified as the most pungent landraces. Total carotenoids ranged from 45.94 µg g−1 fw to 174.52 µg g−1 fw, with ‘Semmane’ and ‘Jerid’ exhibiting the highest levels. Considerable variation was observed in β-carotene content, spanning from 3% to 24% of the total carotenoids. α-Tocopherol content ranged from 19.03 µg g−1 fw in ‘Kairouan’ to 30.93 µg g−1 fw in ‘Beldi’, exerting a notable influence on the overall tocopherol content. Conversely, the β- and γ-tocopherol isomers were detected at very low concentrations. The total vitamin C content ranged from 132 mg 100g−1 fw in ‘Mahdia’ to 200 mg 100 g−1 fw in ‘Nabeul’, indicating relatively low genetic variability. However, large variability was detected in total phenolics content, ranging from 168.58 mg GAE kg−1 fw in ‘Beldi’ to 302.98 mg GAE kg−1 fw in ‘Cayenne’. Landraces such as ‘Dhirat’, ‘Nabeul’, ‘Semmane’, ‘Kairouan’, ‘Cayenne’, and ‘Mahdia’ appear suitable for both fresh consumption and processing, owing to their favorable average fruit weight, soluble solids content, and bioactive content. Among the pepper landraces tested, ‘Cayenne’ achieved the highest value of radical scavenging activity in both hydrophilic and lipophilic fractions (RSAHF and RSALF), with variations ranging from 59% to 120% for RSAHF and from 4% to 63% for RSALF. This study aims to preserve and enhance the value of local genetic resources and contribute to identify desirable traits for incorporation into breeding programs to develop high-quality, high-yielding landraces and elite lines. Full article
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17 pages, 1964 KiB  
Review
Are We Ready to Recommend Capsaicin for Disorders Other Than Neuropathic Pain?
by Janayne L. Silva, Elandia A. Santos and Jacqueline I. Alvarez-Leite
Nutrients 2023, 15(20), 4469; https://doi.org/10.3390/nu15204469 - 21 Oct 2023
Cited by 8 | Viewed by 6423
Abstract
Capsaicin, a lipophilic, volatile compound, is responsible for the pungent properties of chili peppers. In recent years, a significant increase in investigations into its properties has allowed the production of new formulations and the development of tools with biotechnological, diagnostic, and potential therapeutic [...] Read more.
Capsaicin, a lipophilic, volatile compound, is responsible for the pungent properties of chili peppers. In recent years, a significant increase in investigations into its properties has allowed the production of new formulations and the development of tools with biotechnological, diagnostic, and potential therapeutic applications. Most of these studies show beneficial effects, improving antioxidant and anti-inflammatory status, inducing thermogenesis, and reducing white adipose tissue. Other mechanisms, including reducing food intake and improving intestinal dysbiosis, are also described. In this way, the possible clinical application of such compound is expanding every year. This opinion article aims to provide a synthesis of recent findings regarding the mechanisms by which capsaicin participates in the control of non-communicable diseases such as obesity, diabetes, and dyslipidemia. Full article
(This article belongs to the Special Issue The Action of Bioactive Compounds on Human Health or Disease)
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11 pages, 1704 KiB  
Article
Stability of Hydroxy-α-Sanshool in Medium-Chain Triglyceride Oil and Corresponding Oil/Water Emulsions
by Takahiko Mitani, Yasuko Yawata, Nami Yamamoto, Mitsunori Nishide, Hidefumi Sakamoto and Shin-ichi Kayano
Foods 2023, 12(19), 3589; https://doi.org/10.3390/foods12193589 - 27 Sep 2023
Viewed by 2074
Abstract
The pungent component of sansho (Japanese pepper, Zanthoxylum pipritum) is sanshool, which is easily oxidized and decomposed. We have previously reported several sanshool stabilizers, such as α-tocopherol (α-Toc). Sansho pericarp powder treated with middle-chain triglycerides (MCTs) can be used to obtain extracts [...] Read more.
The pungent component of sansho (Japanese pepper, Zanthoxylum pipritum) is sanshool, which is easily oxidized and decomposed. We have previously reported several sanshool stabilizers, such as α-tocopherol (α-Toc). Sansho pericarp powder treated with middle-chain triglycerides (MCTs) can be used to obtain extracts containing hydroxy-α-sanshool (HαS). Although HαS is stabilized when α-Toc is added to the MCT extracts, the loss of HαS is accelerated when it is mixed with a powder such as lactose. The separation of α-Toc from sanshools was thought to inevitably lead to their oxidation. Therefore, using sansho pericarp MCT extracts with or without α-Toc, oil/water (o/w) emulsions were prepared by adding a surfactant, glycerin, and water to these extracts. In both emulsions, HαS was stable in accelerated tests at 50 °C. However, when lactose powder was added to the emulsions and an accelerated test was performed, HαS in the emulsion containing α-Toc was stable, but HαS in the emulsion without α-Toc was unstable. These results highlight the importance of maintaining the close proximity of HαS and α-Toc in the emulsion. The stabilization of sanshools using emulsion technology can facilitate the production of various processed beverages, foods, cosmetics, and pharmaceuticals containing Japanese pepper. Full article
(This article belongs to the Section Food Engineering and Technology)
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12 pages, 4022 KiB  
Article
Integrated Processes Turning Pepper Sauce Waste into Valuable By-Products
by Jicheng Shu, Yongqin Yin and Zhijun Liu
Foods 2023, 12(1), 67; https://doi.org/10.3390/foods12010067 - 23 Dec 2022
Cited by 4 | Viewed by 3334
Abstract
Background: Safe and efficient disposal of millions of tons of pepper sauce waste (PSW) can be a challenge to pepper sauce manufacturers that are concerned about creating environmental hazards from the processing (e.g., preservative salt and vinegar) and intrinsic (e.g., the pungent capsaicins) [...] Read more.
Background: Safe and efficient disposal of millions of tons of pepper sauce waste (PSW) can be a challenge to pepper sauce manufacturers that are concerned about creating environmental hazards from the processing (e.g., preservative salt and vinegar) and intrinsic (e.g., the pungent capsaicins) ingredients. It will be immensely beneficial to process these waste materials before they go to disposal. This work presents integrated approaches for a complete utilization of waste materials by removing and recovering valuable by-products and/or ingredients while succeeding to minimal to zero hazards. Methods: Laboratory- and pilot-scale extraction processes were used to demonstrate the recovery of intrinsic compounds from PSW to pungent pepper oil. Flash chromatography was then applied to isolate the pungent capsaicins out of the pepper oil, thus generating a no-heat pepper oil. Results: By processing the waste materials, a number of valuable by-products with various yield percentages were produced. They included (1) hot red pepper oil (RPO, 8.0% v/w), (2) no-heat pepper residue (NHPR, 25.3% w/w), (3) no-heat red pepper oil (NHRPO, 4.0% v/w), (4) capsaicinoids (0.8% w/w), and (5) capsaicin (0.4% w/w). The optimum processing conditions for products 1, 2, and 3 include extracting the waste materials with 95% ethanol twice, each lasting three hours. The optimal isolation conditions of flash column chromatography to obtain products 4 and 5 include the use of the pre-packed chromatography column 130 g Redisep C18, preparing the sample concentration to 100 mg/mL, eluting with aqueous ethanol, and detecting capsaicins at a wavelength of 228 nm. Conclusions: An integrated approach is offered for the complete utilization of PSW. It not only turns organic food waste into numerous new commodities but also significantly reduces the volume and degree of potential environmental hazard to the disposal sites. Full article
(This article belongs to the Special Issue Renewable Resources from Food Waste and Food Co-products)
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23 pages, 3149 KiB  
Article
Structural Studies of Piperine Inclusion Complexes in Native and Derivative β-Cyclodextrins
by Elias Christoforides, Athena Andreou, Andreas Papaioannou and Kostas Bethanis
Biomolecules 2022, 12(12), 1762; https://doi.org/10.3390/biom12121762 - 26 Nov 2022
Cited by 15 | Viewed by 3632
Abstract
Piperine (PN), the primary pungent alkaloid in black pepper shows several biological activities such as antioxidant, antimicrobial and anti-cancerogenic effects. Similar to other alkaloids, PN is characterized by poor water solubility. One way to improve its solubility and thus its biological activities is [...] Read more.
Piperine (PN), the primary pungent alkaloid in black pepper shows several biological activities such as antioxidant, antimicrobial and anti-cancerogenic effects. Similar to other alkaloids, PN is characterized by poor water solubility. One way to improve its solubility and thus its biological activities is by forming inclusion complexes with suitable cyclodextrins. In this work PN inclusion complexes in native β-cyclodextrin (β-CD), its methylated (randomly methylated (RM-β-CD), heptakis-(2,6-di-O-methyl)-β-CD (DM-β-CD) and heptakis-(2,3,6-tri-O-methyl)-β-CD (TM-β-CD)) and 2-hydroxypropylated (HP-β-CD) derivatives are investigated using physicochemical methods, such as phase solubility study and X-ray crystallography complemented by theoretical (molecular dynamics simulations) studies. The determination of the crystal structure of the PN inclusion complexes in β-CD, DM-β-CD and TM-β-CD, reveals the formation of 1:2 guest:host inclusion complexes in the crystalline state. The guest PN molecule threads the hydrophobic cavities of the hosts which are arranged as couples in a tail-to-tail mode in the case of PN/β-CD and in a head-to-tail mode in the cases of PN/DM-β-CD and PN/TM-β-CD. MD studies based on the crystallographically determined structures and docked models show the stability of the examined complexes in an aqueous environment whereas the binding affinity of PN for the host molecules is calculated by the MM/GBSA method. Finally, phase-solubility studies of PN with β-CD, RM-β-CD and HP-β-CD are presented, indicating a Bs-type for the PN/β-CD complex and an AL-type for the PN/RM-β-CD and PN/HP-β-CD complexes with 1:1 guest:host stoichiometry. Full article
(This article belongs to the Special Issue Perspectives of Cyclodextrins II)
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14 pages, 2295 KiB  
Article
Capsaicin Ameliorates High-Fat Diet-Induced Atherosclerosis in ApoE−/− Mice via Remodeling Gut Microbiota
by Zijian Dai, Siqi Li, Yantong Meng, Qingyu Zhao, Yiyun Zhang, Zhuoma Suonan, Yuge Sun, Qun Shen, Xiaojun Liao and Yong Xue
Nutrients 2022, 14(20), 4334; https://doi.org/10.3390/nu14204334 - 17 Oct 2022
Cited by 31 | Viewed by 3817
Abstract
Capsaicin is a pungent alkaloid abundantly present in peppers with outstanding biological activities, including the anti-atherosclerosis effect. Previous studies revealed that gut microbiota played an important role in the beneficial effects of capsaicin, but whether it is essential for the anti-atherosclerosis effect of [...] Read more.
Capsaicin is a pungent alkaloid abundantly present in peppers with outstanding biological activities, including the anti-atherosclerosis effect. Previous studies revealed that gut microbiota played an important role in the beneficial effects of capsaicin, but whether it is essential for the anti-atherosclerosis effect of capsaicin is unclear. This study evaluated the anti-atherosclerosis effect of capsaicin in ApoE−/− mice and further explored the role of depleting gut microbiota in the improvement of atherosclerosis. The results showed that capsaicin administration could prevent the development of atherosclerosis and improve serum lipids and inflammation, while antibiotic intervention abolished the alleviation of atherosclerosis by capsaicin. In addition, capsaicin administration could significantly increase the abundance of Turicibacter, Odoribacter, and Ileibacterium in feces, and decrease the abundance of deoxycholic acid, cholic acid, hypoxanthine, and stercobilin in cecal content. Our study provides evidence that gut microbiota plays a critical role in the anti-atherosclerosis effect of capsaicin. Full article
(This article belongs to the Special Issue Phytochemicals Effect in Chronic Metabolic Diseases)
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16 pages, 2070 KiB  
Article
Capsaicin Inhibits Multiple Voltage-Gated Ion Channels in Rabbit Ventricular Cardiomyocytes in TRPV1-Independent Manner
by Dmytro Isaev, Keun-Hang Susan Yang, Waheed Shabbir, Frank Christopher Howarth and Murat Oz
Pharmaceuticals 2022, 15(10), 1187; https://doi.org/10.3390/ph15101187 - 26 Sep 2022
Cited by 7 | Viewed by 2482
Abstract
Capsaicin is a naturally occurring alkaloid derived from chili pepper which is responsible for its hot, pungent taste. It exerts multiple pharmacological actions, including pain-relieving, anti-cancer, anti-inflammatory, anti-obesity, and antioxidant effects. Previous studies have shown that capsaicin significantly affects the contractility and automaticity [...] Read more.
Capsaicin is a naturally occurring alkaloid derived from chili pepper which is responsible for its hot, pungent taste. It exerts multiple pharmacological actions, including pain-relieving, anti-cancer, anti-inflammatory, anti-obesity, and antioxidant effects. Previous studies have shown that capsaicin significantly affects the contractility and automaticity of the heart and alters cardiovascular functions. In this study, the effects of capsaicin were investigated on voltage-gated ion currents in rabbit ventricular myocytes. Capsaicin inhibited rapidly activated (IKr) and slowly activated (IKs) K+ currents and transient outward (Ito) K+ current with IC50 values of 3.4 µM,14.7 µM, and 9.6 µM, respectively. In addition, capsaicin, at higher concentrations, suppressed voltage-gated Na+ and Ca2+ currents and inward rectifier IK1 current with IC50 values of 42.7 µM, 34.9 µM, and 38.8 µM, respectively. Capsaicin inhibitions of INa, IL-Ca, IKr, IKs, Ito, and IK1 were not reversed in the presence of capsazepine (3 µM), a TRPV1 antagonist. The inhibitory effects of capsaicin on these currents developed gradually, reaching steady-state levels within 3 to 6 min, and the recoveries were usually incomplete during washout. In concentration-inhibition curves, apparent Hill coefficients higher than unity suggested multiple interaction sites of capsaicin on these channels. Collectively, these findings indicate that capsaicin affects cardiac electrophysiology by acting on a diverse range of ion channels and suggest that caution should be exercised when capsaicin is administered to carriers of cardiac channelopathies or to individuals with arrhythmia-prone conditions, such as ischemic heart diseases. Full article
(This article belongs to the Section Natural Products)
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17 pages, 2209 KiB  
Article
Peppers in Diet: Genome-Wide Transcriptome and Metabolome Changes in Drosophila melanogaster
by Carlos Lopez-Ortiz, Mary Edwards, Purushothaman Natarajan, Armando Pacheco-Valenciana, Padma Nimmakayala, Donald A. Adjeroh, Cristian Sirbu and Umesh K. Reddy
Int. J. Mol. Sci. 2022, 23(17), 9924; https://doi.org/10.3390/ijms23179924 - 1 Sep 2022
Cited by 7 | Viewed by 3451
Abstract
The habanero pepper (Capsicum chinense) is an increasingly important spice and vegetable crop worldwide because of its high capsaicin content and pungent flavor. Diets supplemented with the phytochemicals found in habanero peppers might cause shifts in an organism’s metabolism and gene [...] Read more.
The habanero pepper (Capsicum chinense) is an increasingly important spice and vegetable crop worldwide because of its high capsaicin content and pungent flavor. Diets supplemented with the phytochemicals found in habanero peppers might cause shifts in an organism’s metabolism and gene expression. Thus, understanding how these interactions occur can reveal the potential health effects associated with such changes. We performed transcriptomic and metabolomic analyses of Drosophila melanogaster adult flies reared on a habanero pepper diet. We found 539 genes/59 metabolites that were differentially expressed/accumulated in flies fed a pepper versus control diet. Transcriptome results indicated that olfactory sensitivity and behavioral responses to the pepper diet were mediated by olfactory and nutrient-related genes including gustatory receptors (Gr63a, Gr66a, and Gr89a), odorant receptors (Or23a, Or59a, Or82a, and Orco), and odorant-binding proteins (Obp28a, Obp83a, Obp83b, Obp93a, and Obp99a). Metabolome analysis revealed that campesterol, sitosterol, and sucrose were highly upregulated and azelaic acid, ethyl phosphoric acid, and citric acid were the major metabolites downregulated in response to the habanero pepper diet. Further investigation by integration analysis between transcriptome and metabolome data at gene pathway levels revealed six unique enriched pathways, including phenylalanine metabolism; insect hormone biosynthesis; pyrimidine metabolism; glyoxylate, and dicarboxylate metabolism; glycine, serine, threonine metabolism; and glycerolipid metabolism. In view of the transcriptome and metabolome findings, our comprehensive analysis of the response to a pepper diet in Drosophila have implications for exploring the molecular mechanism of pepper consumption. Full article
(This article belongs to the Special Issue Role of Drosophila in Human Disease Research 3.0)
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14 pages, 2694 KiB  
Article
Pepper Alkaloid Piperine Increases Radiation Sensitivity of Cancer Cells from Glioblastoma and Hypopharynx In Vitro
by Sascha Diehl, Guido Hildebrandt and Katrin Manda
Int. J. Mol. Sci. 2022, 23(15), 8548; https://doi.org/10.3390/ijms23158548 - 1 Aug 2022
Cited by 7 | Viewed by 2333
Abstract
In our study, our aim was to examine the cytotoxic and radio-sensitizing effect of the alkaloid piperine, a major pungent of black pepper, on two different human epithelial tumor cell lines in vitro. The growth of the human cell lines T98G (glioblastoma) and [...] Read more.
In our study, our aim was to examine the cytotoxic and radio-sensitizing effect of the alkaloid piperine, a major pungent of black pepper, on two different human epithelial tumor cell lines in vitro. The growth of the human cell lines T98G (glioblastoma) and FaDu (hypopharyngeal carcinoma) was examined under the influence of piperine in different concentrations. In addition, after combined treatment with ionizing radiation, long-term survival was investigated with a colony formation assay. The proliferation was analyzed using the BrdU-assay, while the DNA repair capacity was examined via the γH2AX assay. Piperine reduced the growth of both cell lines in a concentration-dependent manner as well as a time-dependent one. After combined treatment with piperine and ionizing radiation, an inhibition of clonogenic survival could be proven. A reduced proliferation capacity and an additive effect on DNA damage 24 h after irradiation are possible causal mechanisms, which were also demonstrated for both cell lines. Based on the results presented in this study, piperine was shown to have cytotoxic antitumor activity and a radio-sensitizing effect in micromolar concentrations in the human tumor cells that were tested. Based on these results piperine represents a potential therapeutic option in radio-oncological treatment. Full article
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17 pages, 2298 KiB  
Review
Capsaicin for Weight Control: “Exercise in a Pill” (or Just Another Fad)?
by Arpad Szallasi
Pharmaceuticals 2022, 15(7), 851; https://doi.org/10.3390/ph15070851 - 11 Jul 2022
Cited by 21 | Viewed by 16513
Abstract
Medical management of obesity represents a large unmet clinical need. Animal experiments suggest a therapeutic potential for dietary capsaicin, the pungent ingredient in hot chili peppers, to lose weight. This is an attractive theory since capsaicin has been a culinary staple for thousands [...] Read more.
Medical management of obesity represents a large unmet clinical need. Animal experiments suggest a therapeutic potential for dietary capsaicin, the pungent ingredient in hot chili peppers, to lose weight. This is an attractive theory since capsaicin has been a culinary staple for thousands of years and is generally deemed safe when consumed in hedonically acceptable, restaurant-like doses. This review critically evaluates the available experimental and clinical evidence for and against capsaicin as a weight control agent and comes to the conclusion that capsaicin is not a magic “exercise in a pill”, although there is emerging evidence that it may help restore a healthy gut microbiota. Full article
(This article belongs to the Special Issue Adipose Tissue as a Therapy and Therapeutic Target for Human Diseases)
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