• Title, Summary, Keyword: Capsaicin

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Capsaicin induced apoptosis and the enhanced anticancer effect of anticancer drugs in cancer cells (종양세포에서의 capsaicin에 의한 apoptosis 유도와 항암제의 항암효과의 증가)

  • Kim, Sun Young;Lee, You Jin;Park, Eun Hye;Yi, Ho Keun;Jo, Dae Sun;Kim, Jung Soo;Hwang, Pyoung Han
    • Clinical and Experimental Pediatrics
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    • v.51 no.3
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    • pp.307-314
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    • 2008
  • Purpose : Capsaicin, the major pungent ingredient in red pepper, has long been used in spices and food additives. It has been recently shown to induce apoptosis in several cell lines through a not well known mechanism. The aim of this study was to investigate the apoptosis-inducing effect of capsaicin on gastric cancer cells, and to provide valuable information concerning the application of capsaicin for therapeutic purposes. Methods : Cultured SNU-668 cells were treated with capsaicin. We analyzed cell survival by trypan blue and crystal violet analysis, cell cytotoxicity by MTT assay, apoptosis by nuclear condensation and DNA fragmentation, bcl-2 and bax mRNA expression by RT-PCR, and the expression of apoptosis related proteins by Western immunoblot analysis. In order to assess whether the growth inhibitory effect of anticancer drugs is enhanced by capsaicin, we investigated the effects of cell cytotoxicity and the expression of apoptosis related proteins of etoposide and adriamycin treated with capsaicin in cells. Results : Capsaicin inhibited growth of SNU-668 cells in a dose-dependent manner. This inhibitory effect of capsaicin on cell growth was mainly due to the induction of apoptosis as evidenced by DNA fragmentation, nuclear condensation and the expression of apoptosis related proteins. Furthermore, capsaicin prominently reduced the ratio of anti-apoptotic Bcl-2 to pro-apoptotic Bax and consequently increased caspase-3 activity. The cells treated with capsaicin were more sensitive to death induced by etoposide and adriamycin than the cells without capsaicin. Conclusion : These results demonstrate that capsaicin efficiently induced apoptosis in SNU-668 cells through a caspase-3-dependent mechanism and sensitizes cancer cells to anticancer drugs toward apoptotic cell death, which may contribute to its anticancer effect and chemosensitizer function against gastric cancer.

A study on the comparison of antioxidant effects between hot pepper extract and capsaicin (고추와 Capsaicin의 항산화 효능 비교)

  • Gang, Hyeon-Min;Park, Hee-Soo;Rhim, Tae-Jin;Kwon, Ki-Rok
    • Journal of Pharmacopuncture
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    • v.11 no.1
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    • pp.109-118
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    • 2008
  • Objective : The objective of this study was to compare the antioxidant effects of hot pepper extract and capsaicin. Methods : In vitro, antioxidant activities were examined by DPPH radical scavenging activity, total antioxidant capacity(TAC), oxygen radical scavenging capacity(ORAC), inhibition of induced lipid peroxidation using liver mitochonria and total phenolic contents. Results : 1. DPPH free radical scavenging activities at the concentrations of both 1 and $10mg/m{\ell}$ were 1.2 to 1.9 times higher in capsaicin than in hot pepper extract. The concentration of capsaicin required for 50% radical scavenging was lower than that of hot pepper extract(3.9 vs $5.9mg/m{\ell}$), indicating that capsaicin had higher DPPH radical scavenging activity than hot pepper extract. 2. Total antioxidant capacities of capsaicin at the concentrations of 0.1 and 1mg/ml(13.8 and 41.3 nmol Trolox equivalent) were not significantly different from those at the concentrations of 1 and $10mg/m{\ell}$(11.4 and 41.2nmol Trolox equivalent), indicating that capsaicin showed 10 times higher ABTS radical scavenging activity compared to hot pepper extract. 3. ORAC of capsaicin at the concentrations of 1, 5, 10 and 100 mg/ml were 0.04, 0.17, 0.29 and 1.74nmol gallic acid equivalent, respectively. On the other hand, ORAC of hot pepper extract at the concentrations of 1, 5, 10 and $100{\mu}g/m{\ell}$ were 0.15, 0.44, 0.75 and 2.49nmol gallic acid equivalent, respectively, indicating that capsaicin showed higher peroxyl radical scavenging activity than hot pepper extract. 4. Inhibition of lipid peroxidation caused by hot pepper extract at the concentrations of 1 and $10mg/m{\ell}$ were 12.2 and 61.4%, respectively. Inhibition of lipid peroxidation caused by capsaicin at the concentrations of 1 and $10mg/m{\ell}l$ were 64.0 and 96.8%, respectively. Thus capsaicin showed 10 times stronger effect in inhibiton of lipid peroxidation than hot pepper extract. 5. Total phenolic contents of hot pepper extract at the concentrations of 0.1 and $1mg/m{\ell}$ were 1.4 and 20.8nmol gallic acid equivalent, respectively. Total phenolic contents of capsaicin at the concentrations of 0.1 and $1mg/m{\ell}$ were 6.1 and 55.4 nmol gallic acid equivalent, respectively, indicating that capsaicin had 2.7 to 4.3 times higher total phenolic contents than hot pepper extract. Conclusions : In summary, the results of this study demonstrate significant antioxidant activity of hot pepper extract, although the activity was lowered compared to capsaicin, suggesting that hot pepper extract play a role in prevention of oxidative-related diseases.

Effect of Enteral Capsaicin on the Lymphatic Absorption of Cholesterol and Fats in Rats (흰쥐 모델에서 Capsaicin이 소장 콜레스테롤 및 중성지방 흡수율에 미치는 영향)

  • Seo, Yun-Jung;Kim, Ju-yeoun;Noh, Sang-K.
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.12
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    • pp.1712-1717
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    • 2009
  • Capsaicin has been shown to affect lipid metabolism. However, it is currently not known whether capsaicin would lower the intestinal absorption of cholesterol. Thus, this study was conducted to investigate the effect of intraduodenally infused capsaicin on the lymphatic absorption of cholesterol and lipids in rats. Male Sprague-Dawley rats weighing 300-350 g were starved for 16 hr and the mesenteric lymph duct was cannulated. Each rat was infused at 3.0 mL/hr for 8 hr via the duodenal catheter with a lipid emulsion, which contained 33.3 kBq [$^{14}C$]-cholesterol, 20.7 μmol cholesterol, 452 μmol triolein, 3.1 μmol $\alpha$-tocopherol, and 396.0 μmol Na-taurocholate without (control) or with 5.0 mg capsaicin in 24 mL PBS buffer (pH 6.4). Simultaneously, lymph was collected hourly for 8 hr. There was no significant difference in lymph flow between the groups. However, the lymphatic absorption of 14C-cholesterol for 8 hr was significantly lower in rats infused with capsaicin than in those infused with no capsaicin. Also, the output of oleic acid for 8 hr was significantly decreased by capsaicin. However, the intestinal absorption of $\alpha$-tocopherol did not differ between the groups. The results indicate that the luminal infusion of capsaicin inhibits the intestinal absorption of cholesterol and lipids in rats.

Effect of Capsaicin on Delayed Rectifier $K^+$ Current in Adult Rat Dorsal Root Ganglion Neurons

  • Hahn, Jung-Hyun;Chung, Sung-Kwon;Bang, Hyo-Weon
    • The Korean Journal of Physiology and Pharmacology
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    • v.4 no.1
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    • pp.9-14
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    • 2000
  • $K^+$ currents play multiple roles in the excitability of dorsal root ganglion (DRG) neurons. Influences on these currents change the shape of the action potential, its firing threshold and the resting membrane potential. In this study, whole cell configuration of patch clamp technique had been applied to record the blocking effect of capsaicin, a lipophilic alkaloid, on the delayed rectifier $K^+$ current in cultured small diameter DRG neurons of adult rat. Capsaicin reduced the amplitude of $K^+$ current in dose dependent manner, and the concentration-dependence curve was well described by the Hill equation with $K_D$ value of $19.1{\mu}M.$ The blocking effect of capsaicin was reversible. Capsaicin $(10 {\mu}M)$ shifted the steady-state inactivation curve in the hyperpolarizing direction by about 15 mV and increased the rate of inactivation. The voltage dependence of activation was not affected by capsaicin. These multiple effects of capsaicin may suggest that capsaicin bind to the region of $K^+$ channel, participating in inactivation process.

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Effects of Capsaicin on the Liver Toxicity of Ethanol in Mice (Mouse에 있어서 Ethanol의 간독성에 미치는 Capsaicin의 영향)

  • 안영근;김정훈;이선원;김성오
    • Environmental Analysis Health and Toxicology
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    • v.3 no.1_2
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    • pp.21-31
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    • 1988
  • The effect of capsaicin on the toxicity of ethanol in mice were studied. Capsaicin was administered i.p. every other day for 4 weeks and 5% ethanol was provided ad libitum by tap water for 4 weeks. The administration of capsaicin 3.0 mg/kg showed the increase of body weight gain, ratio of liver wt./body wt., s-GPT. s-triglyceride and s-cholesterol, and showed the decrease of BUN as compared to control group. Capsaicin administered 3.0 mg/kg showed severe moth eaten appearance. eosinophilic necrosis and cholangitis in mouse liver The administration of 5% ethanol showed the decrease of body weight gain, ratios of liver, kidney and spleen wt./body wt., s-tryglyceride and s-cholestrol. Ethanol administered 5% solution showed little fatty change, moth eaten appearance, Kupffer cell proliferation, spotty necrosis and nuclear regeneration. The administration of capsaicin and ethanol together decreased the influence of ethanol on body weight gain, ratios of liver, kidney and spleen wt./body wt., s-triglyceride and s-cholesterol, and showed the less severe moth eaten appearance, eosinophilic necrosis and cholangitis. It might be concluded that the administration of capsaicin and ethanol together decreased the toxicity caused by capsaicin or ethanol respectively.

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Capsaicinoids-induced Neurotoxic Desensitization in Guinea Pig: Antinociception and Loss of Substance P-like Immunoreactivity from Peripheral Sensory Nerve Endings in Bronchi

  • Jung, Yi-Sook;Lee, Buyean;Shin, Hwa-Sup;Kong, Jae-Yang;Park, No-Sang;Cho, Tai-Soon
    • Biomolecules & Therapeutics
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    • v.3 no.4
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    • pp.256-259
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    • 1995
  • Antinociceptive and desensitizing effects of systemically administered capsaicinoids (capsaicin and KR25018) were investigated in guinea pig. Nociceptive sensitivity to chemical stimulus was examined to test sensory function, and the content of substance P-like immunorractivity (SP-LI) in bronchi was determined as a peripheral marker of capsaicin-sensitive primary afferent neurons. Guinea pigs were pretreated s.c. with several doses of capsaicin (1,2.5,5, 10 mg/kg) or KR25018 (1, 2.5, 5, 10 mg/kg) one week prior to the experiments. Frequency of eye wiping was significantly decreased by capsaicin and KR25018 in a pretreatment dosedependent manner. In capsaicin- or KR25018-pretreated guinea pigs, there was a significant loss of SP-LI in bronchial tissue extracts. In summary, a newly synthesized capsaicin analogue H725018 exhibited antinociceptive effect against chemical stimulus in guinea pig, with comparable potency to capsaicin. This desensitizing activity of capsaicin or KR25018 might be related to the loss of SP-LI in peripheral afferent nerves.

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Capsaicin-Induced Apoptosis of H-Ras-Transformed Human Breast Epithelial Cells is Rac-Dependent via ROS Generation

  • Kim, Seon-Hoe;Moon, Aree
    • Archives of Pharmacal Research
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    • v.27 no.8
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    • pp.845-849
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    • 2004
  • Many studies have focused on the anticarcinogenic, antimutagenic or chemopreventive activi-ties of capsaicin (trans-8-methyl-N-vanillyl-6-nonenamide) which is a major pungent ingredient in red pepper. We have previously shown that capsaicin selectively induces apoptosis in H-ras-transformed MCF10A human breast epithelial cells but not in their normal cell counter-parts (Int. J. Cancer, 103, 475-482,2003). In this study, we investigated the possible roles of reactive oxygen species (ROS) and Rac1 in capsaicin-induced apoptosis of H-ras MCF10A cells. Selective induction of ROS generation by capsaicin treatment was observed only in H-ras MCF10A cells. Pretreatment of H-ras MCF10A cells with an antioxidant N-acetylcysteine(NAC) significantly reversed capsaicin-induced growth inhibition, suggesting that ROS may mediate the apoptosis of H-ras-transformed cells induced by capsaicin. Rac1 was prominently activated by H-ras in MCF10A cells. Based on the studies using a wild type Rac1 and a domi-nant negative Rac1 constructs, we propose that Rac1 activity is critical for inhibitory effect of capsaicin on growth of H-ras-transformed MCF10A cells possibly through ROS generation.

Relationship between Red Pepper Intake, Capsaicin Threshold, Nutrient Intake, and Anthropometric Measurements in Young Korean Women (젊은 한국여성에서 붉은고추의 섭취량, 캡사이신 역치, 영양소 섭취량 및 신체계측치간의 관련성)

  • Kim Seok-Young;Park Gyeong-Min
    • Journal of Nutrition and Health
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    • v.38 no.1
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    • pp.76-81
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    • 2005
  • The effects of the amount of red pepper intake per a day on the capsaicin threshold, nutrient intake, and anthropo-metric measurements were investigated in 100 female students of university. Three 24-hour recalls were performed to estimate usual nutrient and red pepper intake of free-living participants. The solutions containing capsaicin at concentration of 0.05, 0.1, 0.2, 0.3, 0.4, 0.5ppm used for the evaluation of hot-taste detection threshold. Subjects were asked to recognize the burning sensation after tasting l0ml of each test solution in ascending order of capsaicin concentrations. Mean intake of red pepper was 4.6 g/d and the capsaicin threshold was 0.27 ppm. The detection threshold for capsaicin was correlated with the amount of pepper intake per a day. Red pepper intake was correlated with energy, protein, lipid, carbohydrate, Iron, vitamin A, vitamin B$_2$ niacin, and vitamin E intakes. However, it was not correlated with intake of calcium, vitamin B$_1$ or vitamin C. The red pepper intake was negatively correlated with fat mass and waist girth and the capsaicin threshold was also negatively correlated with pulse. In conclusion, red pepper intake was associated with nutrient intake and capsaicin threshold whereas it was negatively correlated with fat mass and waist girth.

Induction of Apoptosis by Eugenol and Capsaicin in Human Gastric Cancer AGS Cells - Elucidating the Role of p53

  • Sarkar, Arnab;Bhattacharjee, Shamee;Mandal, Deba Prasad
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.15
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    • pp.6753-6759
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    • 2015
  • Background: Loss of function of the p53 gene is implicated in defective apoptotic responses of tumors to chemotherapy. Although the pro-apoptotic roles of eugenol and capsaicin have been amply reported, their dependence on p53 for apoptosis induction in gastric cancer cells is not well elucidated. The aim of the study was to elucidate the role of p53 in the induction of apoptosis by eugenol and capsaicin in a human gastric cancer cell line, AGS. Materials and Methods: AGS cells were incubated with or without various concentrations of capsaicin and eugenol for 12 hrs, in the presence and absence of p53 siRNA. Cell cycling, annexin V and expression of apoptosis related proteins Bax, Bcl-2 ratio, p21, cyt c-caspase-9 association, caspase-3 and caspase-8 were studied. Results: In the presence of p53, capsaicin was a more potent pro-apoptotic agent than eugenol. However, silencing of p53 significantly abrogated apoptosis induced by capsaicin but not that by eugenol. Western blot analysis of pro-apoptotic markers revealed that as opposed to capsaicin, eugenol could induce caspase-8 and caspase-3 even in the absence of p53. Conclusions: Unlike capsaicin, eugenol could induce apoptosis both in presence and absence of functional p53. Agents which can induce apoptosis irrespective of the cellular p53 status have immense scope for development as potential anticancer agents.

Capsaicin Intake Estimated by Urinary Metabolites as Biomarkers (뇨중 대사체 정량에 의한 capsaicinoid의 생화학적 섭취지표 개발 연구)

  • Choo, Yeon-Soo;Kwon, Hoon-Jeong
    • Korean Journal of Food Science and Technology
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    • v.33 no.6
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    • pp.784-788
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    • 2001
  • Reliable data on the exposure of capsaicin, which evokes hot sensation in hot red pepper, are important prerequisites for studying biological functions of capsaicin in human body since its roles are controversial according to animal and epidemiological studies. To get accurate data, the use of urinary biomarkers was considered as a measure of internal exposure of capsaicin. After 2-day-capsaicin depletion five to six women in their 20's were instructed to eat 60 or 80 g/day hot red pepper soybean paste as a capsaicin source with meal which did not contain capsaicinoid, and to collect their urine separately. HPLC conditions were set to detect capsaicinoid and urinary metabolites at the same time. Most of capsaicinoid were excreted in the form of 4-hydroxy-3-methoxybenzoic acid in three subjects at the highest dose. This result suggests the oxidation of the 4-hydroxy3-methoxybenzaldehyde, the hydrolysis product of capsaicin, is the major metabolic pathway in the human body, whereas the reduction of the aldehyde is the major route in rats. However, neither any metabolite nor the parent compound was ever shown in two of the subjects reflecting large individual differences of capsaicin absorption and/or biotransformation.

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