• Journal of Veterinary Clinics
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• v.23 no.2
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• pp.144-148
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• 2006

Apoptotic death of articular chondrocytes has been implicated in the pathogenesis of osteoarthritis. Tartrate resistant acid phosphatase (TRAP) has been used for several years as a marker enzyme of bone-resorbing osteoclasts. This study investigated the activity of TRAP in media of apoptotic cell death-induced canine chondrocyte. We exposed canine chondrocyte to capsaicin and the results showed that capsaicin induced cell death in a dose dependent manner. And we measured TRAP activity in media of chondrocyte death induced by capsaicin treatment and the results capsaicin significantly increased the activity of TRAP in media for dose dependent. We also investigated whether the combination treatment with capsaicin and TRAIL enhance apoptotic cell death in canine chondrocyte. We exposed canine chondrocyte to capsaicin for 24 hrs at the indicated dose, and then treated with recombinant TRAIL protein for 24 hrs. TRAIL alone did not induce cell death after 24 hours, but the combined treatment of both induced more cell death compared with capsaicin alone in a dose dependent manner. Also, the combination treatment with capsaicin and TRAIL increased the activity of TRAP in culture media. These results suggest that TRAP can flow out into extracellular after chondrocyte damage, and TRAP may be a successful biomarker for detection of joint disease such as osteoarthritis.

• Restorative Dentistry and Endodontics
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• v.17 no.1
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• pp.10-21
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• 1992

The purpose of this study was to investigate the analgesic effect of eugenol, capsaicin and demethoxy-NE. Young adult cats, weighing 2.0 to 3.0kg, were used. Each animal was anesthetized (${\alpha}$-chloralose 60mg per kg body weight) and divided into four groups; control, eugenol, capsaicin and demethoxy-NE group. The anterior digastric muscles were exposed and a pair of electrodes was inserted to record the electromyograms. To expose the pulp, each canine teeth was prepared with a low speed bur under cooling and used for recording anterior digastric muscular EMGs evoked by noxious stimulation of dental pulp. To observe effects on jaw opening reflex, inferior alveolar nerve of both sides were exposed for drug application and wire electrodes were inserted in anterior digstric muscle for recording the EMGs. To observe effects on action potential, saphenous nerves of both sides were exposed and three tissue pools were made from surrounding tissue. The most distal pool was used for applying stimulation, the most proximal one for recording of action potential, and the other one for drug application. One side of inferior alveolar nerve and saphenous nerve were used for eugenol, capsaicin, or demethoxy-NE application, the other side of nerve for control experiments(only vehicle application). Anterior digastric muscular EMGs evoked by noxious stimulation of dental pulp were recorded before drug application, immediate after drug application, at 60 and 120 minutes, and 5 days after drug application. Action potentials were recorded before drug application, immediate after 30 minutes drug application, at 30, 60 and 120 minutes after drug had been washed out. The results were as follows; 1. Eugenol had a continuous blocking effect on the anterior digastric muscular EMGs evoked by noxious pulp stimulation and after 5 days, showed completely blocking effect. 2. After 5 days, demethoxy-NE applied to dental pulp had a considerable blocking effect on the jaw opening retlex evoked by noxious stimulation but capsaicin had no significant effect. 3. After 5 days, eugenol group showed the strongest blocking effect among the all experimental groups on the jaw opening reflex evoked by noxious stimulation of dental pulp and capsaicin group showed the weakest blocking effect. 4. Eugenol had a completely blocking effect on the action potential conductivity of peripheral nerve. Capsaicin and demethoxy-NE had the blocking effect on the action potential conductivity of ${\alpha}$-and C-nerve fibers. 5. Capsaicin, demethoxy-NE and eugenol applied to inferior alveolar nerve surppressed the jaw opening reflex evoked by noxious stimulation of dental pulp.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.235-235
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• 1996

1. 초산 writhing법에서 DA-5018, morphine, capsaicin 및 acetaminophen의 E $D_{50}$ 은 각각 0.1, 0.3, 1.4 및 45.4 mg/kg이었으며, formalin법에서 DA-5018과 morphine의 E $D_{50}$은 0.17과 4.3 mg/kg이었다. Randall-Selitto법에서 DA-5018, morphine, capsaicin 및 acetaminophen의 E $D_{50}$은 0.66, 3.9, 4.2 및 643 mg/kg이었다. Tail flick법에서 DA-5018, morphine 및 capsaicin의 E $D_{50}$ 은 2.0, 2.6 및 14.2 mg/kg이었고 hot plate법에서 DA-5018과 capsaicin의 E $D_{50}$은 1.7 및 26.5mg/kg이었다. 그러나 열자극에 의한 동통모델에서 acetaminophen은 진통효과가 없었다. 2. Streptozotocin유발 당뇨랫드에 DA-5018 0.2, 0.5 및 1.0mg/kg 또는 capsaicin 10 mg/kg 투여시 1, 3, 7 일째에서 각각 유의성있는 동통역치의 증가를 나타내었으나 ketoprofen(10 mg/kg) 및 desipramin(10 mg/kg) 투여시는 동통역치의 유의성있는 증가가 나타내지 않았다. 관절염 동통모델에서 DA-5018, ketoprofen 및 capsaicin을 투여한 후 7일째에 동통역치를 2배 증가시키는 용량은 각각 0.66, 3.76 및 17.38 mg/kg이었다. 3. 이상의 결과로부터 DA-5018은 morphine 및 capsaicin에 비해 동등 이상의 효력을 갖고 있으며, 비스테로이드성 진통제보다 효능이 우수함을 확인하였다.

• The Korean Journal of Pain
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• v.31 no.3
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• pp.174-182
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• 2018

Background: The trigeminal nucleus caudalis (Vc) is a primary central site for trigeminal transmitting. Noxious stimulation of the trigeminal nociceptors alters the central synaptic releases and neural expression of some inflammatory and trophic agents. Orexin-A and the orexin 1 receptor (OX1R) are expressed in pain pathways including trigeminal pain transmission. However, the the mechanism(s) underling orexin-A effects on trigeminal pain modulation have not been fully clarified. Methods: Trigeminal pain was induced by subcutaneous injection of capsaicin in the upper lip in rats. The effect of trigeminal pain on cyclooxygenase-2 (COX-2) and brain-derived neurotrophic factor (BDNF) expression in the Vc of animals was determined by immunofluorescence. Subsequently, OX1R agonist (orexin-A) and antagonist (SB-334867-A) was administrated in the Vc to investigate the possible roles of the Vc OX1R on changes in COX-2 and BDNF levels following pain induction. Results: The data indicated an increase in COX-2 and decrease in BDNF immuno-reactivity in the Vc of capsaicin, and capsaicin- pretreated with SB-334867-A (80 nM), groups of rat. However, the effect of capsaicin on COX-2 and BDNF expressions was reversed by a Vc microinjection of orexin-A (100 pM). Conclusions: Overall, the present data reveals that orexin-A can attenuate capsaicin-induced trigeminal pain through the modulation of pain effects on COX-2 and BDNF expressions in the Vc of rats.

• Journal of the Korean Society of Food Science and Nutrition
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• v.41 no.6
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• pp.870-874
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• 2012

The objective of this study was to determine the content of capsaicinoids in different commercial pepper powders and pepper-containing products in the Korean market. The two major capsaicinoids in the samples, capsaicin and dihydrocapsaicin, were analyzed using reversed-phase HPLC. The levels of capsaicin and dihydrocapsaicin in pepper powders and pepper-containing products ranged from 0.21 to 78.24 and 0.20 to 38.82 mg/100 g sample, respectively. Pepper powders contained generally higher amounts of capsaicin and dihydrocapsaicin than pepper- containing products. In addition, the analytical method validation parameters including accuracy, precision, and specificity were provided to ensure the validity of the extraction procedure for capsaicinoid analysis. Overall recovery from pepper powder and pepper paste was close to 100% (n=3). The results of validation parameters indicated that the present method was reliable and reproducible for the HPLC analyses of capsaicin and dihydrocapsaicin in commercial pepper products.

• Journal of Pharmacopuncture
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• v.23 no.4
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• pp.237-246
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• 2020

Objectives: Capsaicin-containing (CP) pharmacopuncture was developed to treat neuropathic pain. This study was conducted to assess the toxicity of CP extract for pharmacopuncture, using a micronucleus test. Methods: First, a dose range finding study was conducted. Then an in vivo micronucleus test was performed to determine the induction of micronuclei in mouse bone marrow cells after intramuscular administration of CP twice with a 24-hour interval to 8-week-old ICR mice. A high dose of 0.2 mL/animal was selected, and this was sequentially diluted by applying a geometric ratio of 2 to produce two lower dose levels (0.1 and 0.05 mL/animal). In addition, negative and positive control groups were set up, and an HPLC analysis was conducted to confirm the capsaicin content of CP. Results: The incidence of micro-nucleated polychromatic erythrocytes in polychromatic erythrocytes in the CP-treated group was similar to that in the negative-control group, while that in the positive-control group was significantly greater. In addition, the ratio of polychromatic erythrocytes to total erythrocytes in the CP treatment group and the positive control group was not significantly different from the negative control group. In the HPLC analysis, capsaicin in the CP was identified through a comparison with the retention time of the capsaicin standard of 27 min. Conclusion: CP did not show any indication of any potential to induce micronuclei formation in bone marrow cells of ICR mice under the conditions of this study. Further toxicity studies are necessary to ensure the safety of the use of CP in clinical practice.

• The Korean Journal of Physiology
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• v.26 no.2
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• pp.143-150
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• 1992

The purpose of this study is to obtain the effective concentration of capsaicin to relieve pain with no change in the number of C-fibers and its effective duration for pain relief. Capsaicin has been used extremely as a experimental tool and as topical medications for acute or chronic tissue injuries and partial nerve injury is the main cause of causalgiform pain disorders in humans. Here, the left sciatic nerve was ligated unilaterally at the high level of the thigh to prepare an animal model of this pain condition. The rat developed guarding behavior of the ipsilateral hind paw within a few hours after the operation and this behavior was maintained for several months thereafter, suggesting the possibility of spontaneous pain. These animals were divided into two groups(4-week & 8-week) and each group was subdivided into five groups by different concentration (0.05, 0.1, 0.5, 1.0 & 2.0%). Each capsaicin concentration was treated locally on the spinal cord-side of the ligated nerve and the foot withdrawal latency was measured. Thereafter, the dorsal roots of L5 were removed from both sides immediately after in tracardial perfusion for the counting of C-fibers by the histological procedure. There were no significant differences in the foot-withdrawal latency and the number of C-fibers between the left side treated with 0.05% capsaicin and the right side treated with the vehicle. However, latencies of the left sides treated with 0.1, 0.5, and 1.0% capsaicin increased significantly throughout 4-6 weeks with almost no change in the number of C-fibers, and the latencies showed the trends to approach slowly to those of the conditions after operation. The latency of subgroup treated with 2.0% increased by approximate 10% more than that of the right side throughout 8 weeks, and the number of C-fibers decreased by about 30% or more These results suggest that the elevated latency with capsaicin(0.1-1.0%) treatment is due to the inhibition of impulse transmission throughout the primary afferent fiber and the data from 2.0% are due to partial destruction of C-fibers. Therefore, capsaicin concentrations from 0.1% to 1.0% are probably very effective for the treatment of causalgiform pain with almost no destruction of C-fibers.

• Journal of Life Science
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• v.14 no.4
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• pp.541-546
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• 2004

The antioxidative activities of capsaicin (Cap, 0.02 and 0.04%) on the lipid peroxidation of tissues in male Sprague Dawley rats fed diets with or without orotic acid (1.0%, w/w) were studied in vivo system by measuring thiobarbituric acid reactive substances (TBARS) concentrations. Body weight gain, food intakes, food efficiency ratio and the relative tissues weights of brain, kidney, spleen, heart, and testis were not significantly different among dietary groups. Relative weights of liver were higher in the OA group than that in the other groups. TBARS concentrations in liver were significantly higher in the OA or 0.04% Cap groups than in the normal group, while this raise was not observed 0.02% Cap group. A significant increase in TBARS concentrations was found in the liver of the OA +0.04% Cap group compared with the OA or the 0.04% Cap groups. Nonheme iron concentrations were significantly higher in the liver of the OA, 0.04% Cap, OA+0.02% Cap, OA+0.04% Cap groups than that in the normal group. TBARS concentrations in kidney were lower in the 0.02% or 0.04% Cap groups than that in the normal group, but this concentrations were higher in either the OA, OA+0.02% Cap or OA+0.04% Cap groups than that in the normal group. Meanwhile, TBARS concentrations of brain, spleen, heart and testis were not significantly different among groups. The present study suggested that the lipid peroxidation was increased in the rats liver fed diet with erotic acid, and the simultaneous supplementation of capsaicin further enhanced.

• Journal of Nutrition and Health
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• v.34 no.7
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• pp.748-753
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• 2001

This study is to investigate the effects of capsaicin with high-fat diet on tissue glycogen contents in exercise-trained rats. Forty male Sprague-Dawley rats were offered a high-fat diet for 2 wks in individual cages and were exercise-trained by a animal treadmill running throughout the experimental period. After 2 wks of the prefeeding with high-fat diet, the rats were divided into two group: high-fat diet group(CON)and high-fat diet + capsaicin(0.014%) group(CAP). The rats were killed by decapitation at 10 hr(rest), 1 hr and 2 hr after treadmill running(27m/min, 6$^{\circ}$). Body weight and epididymal adipose tissure weight were significantly lower in CAP than in CON, but soleus muscle weight was not different between the two groups. Glycogen contents in liver, soleus and gastrocnemius white muscles were significantly lower in CAP than in CON at rest, 1 hr and 2 hr (p<0.05). However, glycogen content in gastrocnemius red muscle was significantly higher in CAP compared with CON at 2 hr after the exercise(p<0.05). These results indicate that capsaicin intake with high-fat diet would decrease glycogen contents in liver and muscle, however, this effect on glycogen metabolism could be changed by muscle type.

• The Korean Journal of Physiology and Pharmacology
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• v.13 no.6
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• pp.425-429
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• 2009

Intracranial headaches, including migraines, are mediated by nociceptive activation of the trigeminal nucleus caudalis (TNC), but the precise mechanisms are poorly understood. We previously demonstrated that selective blockage of spinal sigma-1 receptors (Sig-1R) produces a prominent antinociceptive effect in several types of pain models. This study evaluates whether the Sig-1R antagonist (BD1047) has an antinociceptive effect on capsaicin (a potent C-fiber activator) induced headache models in rats. Intracisternal infusion of capsaicin evoked pain behavior (face grooming), which was significantly attenuated by BD1047 pretreatment. BD1047 consistently reduced capsaicin-induced Fos-like immunoreactivity (Fos-LI), a neuronal activator, in the TNC in a dose-dependent manner. Moreover, capsaicininduced phosphorylation of N-methyl-D-aspartate receptor subunit 1 was reversed by BD1047 pretreatment in the TNC. These results indicate that the Sig-1R antagonist has an inhibitory effect on nociceptive activation of the TNC in the capsaicin-induced headache animal model.