• 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.

• Journal of Oral Medicine and Pain
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• v.32 no.2
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• pp.219-225
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• 2007

This investigation was carried out to evaluate the effect of pain control temporomandibular disorders with clinical application of capsaicin cream. 20 healthy subjects without systemic diseases were measured in current perception threshold and pain tolerance threshold with $Neurometer^{(R)}$ CPT/C (Neurotron, Inc. Baltimore, Maryland, USA) after cold pack, 0.025% capsaicin and 0.075% capsaicin cream application. The obtained results were as follows : 1. The current perception threshold of C-fiber was significantly higher to the baseline on. There were significantly increased in C- fiber current perception threshold of 0.025% capsaicin cream and 0.075% capsaicin cream application comparison to cold pack. 2. There was significantly increased in pain tolerance threshold of cold pack and 0.075% capsaicin application comparison to one of baseline as $A{\beta}$-fiber, There was significantly higher after cold pack and 0.025% capsaicin cream application than baseline as $A{\delta}$-fiber. In C-fiber case, 0.025% capsaicin application's was significantly increased than baseline one. 3.There were significantly higher C-fiber of 0.075% capsaicin application than baseline in visual analogue scale marking pain level of pain tolerance threshold.

• The Korean Journal of Physiology and Pharmacology
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• v.11 no.5
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• pp.215-219
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• 2007

Small and large conductance $Ca^{2+}$-activated $K^+(SK_{Ca}\;and\;BK_{Ca})$ channels are implicated in the modulation of neuronal excitability. We investigated how changes in peripheral $K_{Ca}$ channel activity affect mechanical sensitivity as well as the afferent fiber type responsible for $K_{Ca}$ channel-induced mechanical sensitivity. Blockade of $SK_{Ca}$ and $BK_{Ca}$ channels induced a sustained decrease of mechanical threshold which was significantly attenuated by topical application of capsaicin onto afferent fiber and intraplantar injection of 1-ethyl-2-benzimidazolinone. NS1619 selectively attenuated the decrease of mechanical threshold induced by charybdotoxin, but not by apamin. Spontaneous flinching and paw thickness were not significantly different after $K_{Ca}$ channel blockade. These results suggest that mechanical sensitivity can be modulated by $K_{Ca}$ channels on capsaicin-sensitive afferent fibers.

• Biomolecules & Therapeutics
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• v.5 no.2
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• pp.211-214
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• 1997

In the present study, we investigated the mechanisms of antinociceptive effect and thermoregulatory action of capsaicin in guinea pigs. The administration of capsaicin (5 mg/kg, s.c.) caused a significant decrease in frequency of eye wiping, an indicative of nociceptive threshold. This antinociceptive effect of calsaicin was abolished by co-administration of capsazepine (30 mg/kg, s.c.) with capsaicin, suggesting the involvement of a vanilloid receptor in the antinociceptive action of capsaicin. The administration of capsaicin (1 mg/kg, s.c.) produced a significant decrease in body temperature of guinea pigs. The maximum decrease in body temperature by 2 degrees was shown 1 hour after the treatment, and this decrease was not reversed by coadministration of capsazepine. In conclusion, it is suggested that the mechanism of action of capsaicin-induced thermoregulation involves different pathways from that of capsaicin-induced antinociception.

• Korean journal of food and cookery science
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• v.16 no.6
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• pp.677-680
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• 2000

This study was performed to compare the pungency perception of Koreans with that of Australians by sensory evaluation using capsaicin and capsaicin-containing chilli powder. First, the sensory tests for various concentrations of capsaicin were carried out, and then capsaicin-containing chilli powder was added to water, porridge and noodle, and they were evaluated to find out the threshold concentrations of capsaicin in each medium. In the results, the pungency perception of Australians was higher in low concentrations of capsacin, while Korean perceived the pungency better in high concentrations, and the panels perceived hot taste better in water followed by porridge and noodle. The low concentrations of capsaicin was not easily perceived if it is contained in porridge or noodle.

• The Korean Journal of Physiology and Pharmacology
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• v.4 no.1
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• pp.15-24
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• 2000

Although nociceptive informations are thought to be processed via different neural mechanisms depending on the types of stimuli, sufficient data have not been accumulated yet. We performed a series of experiments to elucidate the possible neural mechanisms as to chemical stimuli such as formalin, capsaicin and ATP. Single unit activity of wide dynamic range (WDR) neurons and high threshold cells were recorded extracellularly from the lumbosacral enlargement of cat spinal cord before and after chemical stimulation to its receptive field (RF). Each chemical substance - formalin $(20{\mu}l,\;4%),$ capsaicin (33 mM) or Mg-ATP (5 mM)- was injected intradermally into the RFs and then the changes in the spontaneous activity, mechanical threshold and responses to the peripheral mechanical stimuli were observed. In many cases, intradermal injection of formalin (5/11) and capsaicin (8/11) resulted in increase of the spontaneous activity with a biphasic pattern, whereas ATP (8/8) only showed initial responses. Time courses of the biphasic pattern, especially the late response, differed between formalin and capsaicin experiments. One hour after injection of each chemical (formalin, capsaicin, or ATP), the responses of the dorsal horn neurons to mechanical stimuli increased at large and the RFs were expended, suggesting development of hypersensitization (formalin 6/10, capsaicin 8/11, and ATP 15/19, respectively). These results are suggested that formalin stimulates peripheral nociceptor, local inflammation and involvement of central sensitization, capsaicin induces central sensitization as well as affects the peripheral C-polymodal nociceptors and neurogenic inflammation, and ATP directly stimulates peripheral nociceptors.

• 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.

• Biomolecules & Therapeutics
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• v.5 no.1
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• pp.94-99
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• 1997

Capsaicin is known to be an analgesic agent, affecting the synthesis, storage, , transport and release of substance p, the principal neurotransmitter of pain from periphery to the central nervous system(CNS). DA-5018, a newly synthesized capsaicin derivative has shown potent analgesic effect comparable to that of morphine in various rat models of experimentally inducted acute pairs. In this study the mechanism of analgesic actlvity of DA-5018 was examined. First, the electrically-evoked contraction of guinea pig trachea was inhibited by DA-5018 and these inhibition was recovered by incubation with capsafepine(3$\muM$), capsaicin receptor antagonist and this result suggested that DA-5018 has affinity on capsaicin receptor. The correlation between the norciceptive threshold and the release of substance P was evaluated. In vivo perfusion of slices of the rat spinal cord with DA-5018(10, 100$\muM$) produced a significant increase of the release of substance P and this increase was less than that of capsaicin(10$\muM$). The norciceptive threshold of rat treated with DA-5018(1 mg/kg, p.o) in tall pinch test increased from 2.9$\pm$0.3 to 23.5 $\pm$6.61. Tail pinch latency increased to a maximun at 15 min after DA-5018 treatment and then declined to control values by 120 min. The capsaicin-evoked release ot substance P from the spinal cord slices of rat treated with DA-5018 reduced from 2.38$\pm$ 0.79 to 0.69$\pm$ 0.26 pg/mg wet weight. This reduction reached to a minium at 15 min after DA-5018 treatment and then recovered to control value by 120 min. These results mean that analgesic activity of DA-5018 is due to release of substance P The effect of DA-5018 cream on electrically-evoked neurogenic inflammation of rat saphenous nerve was compared with capsaicin (zostrix-HP). DA-5018 showed 34% inhibition of the neurogenic extravasation while capsaicin showed significant 67% inhibition. This result indicates that the potency of DA-5018 in the release of substance P is less than that of capsaicin. These results suggest that the release of substance P is partially involved in the mechanism of analgesic action of DA-50l8.

• Biomolecules & Therapeutics
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• v.5 no.2
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• pp.117-124
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• 1997

The analgesic effects of DA-5018, a new caosaucin derivative, were evaluated in various experimental pain models. Drugs were administered subcutaneously or topically. When drugs were administered subcutaneously, 1) the $ED_{50}$ of DA-5018, morphine . HCI, capsaicin and acetaminophen were 0.091-2.0, 0.3-4.3, 1.4-26.5 and 45.4-643 mg/kg, respectively in various pain or inflammatory models including acetic acid writhing, formalin, tail flick, Randall-Selitto, hot plate and crouton oil-induced ear edema test, 2) the AD2 values (the dose for doubling of pain threshold of vehicle control) of DA-5018, capsaicin and ketoprpgin were 1.07 $\pm$ 0. 18, 23.47$\pm$4.46 and 2.97$\pm$0.43 mg/kg in Freund's complete adjuvant (FCA)-induced arthritic pain model. And by topical application, 1) neither DA-5018 0.3% cream nor Zostrix-HP (capsaicin 0.075%) were effective in formalin test, 2) although DA-5018 0.3% cream significantly inhibited the croton oil-induced ear edema being better than Zostrix-HP and Kenofen (ketoprofen 3%). 3) In FCA model, DA-5018 0.3% cream reversed the decreased pain threshold of arthritic rat from 136.4 g (day 0) to 289.0 g (day 5) and 250.1 g (day 10), which was similar to Zostrix-HP. These results suggest that DA-5018 administered subcutaneously has a potent and broad analgesic spectrum than nonsteroidal antiinflammatory drugs against acute and chronic pain, and by topical application it exerts comparable analgesic and antiinglammaatory effects to capsaicin cream.

• Biomolecules & Therapeutics
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• v.5 no.1
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• pp.67-73
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• 1997

Analgesic effect of DA-5018, a new capsaicin derivative, was evaluated in various rat models of experimentally induced acute pain. DA-5018(0.2∼10.0 mg/kg, p.o.) prevented the writhing syndromes induced by acetic acid or phenol-p-benzoquinone(PBQ). It increased the pain threshold of inflamed paw when tested by the Randall-Selitto method at the dose of 2.0∼20.0 mg/kg by oral administration. And also it showed antinociceptive activities in tail-pinch(1.0∼20.0 mg/kg, p.o.) and tail-flick test(5.0∼50.0 mg/kg, p.o.). the potency and efficacy of DA-5018 were comparable to morphine · HCI in all the models mentioned above. Acetaminophen exhibited the inhibition of acetic acid-induced writhing syndromes and also analgesic activity in Randall-Selitto test, but it showed the limited efficacy in tail-pinch and tail-flick test. These results mean that DA-5018 has a broader analgesic activity profile than acetaminophen. And we found out that the analgesic activity of DA-5018 was 100 times more potent when administered centrally than administered orally in tail-flick test. These results suggest that DA-5018 has an orally active analgesic activity, and central nervous system may be involved in the action of DA-5018.