• Molecules and Cells
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• 제37권3호
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• pp.234-240
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• 2014

Cisplatin is one of the most potent chemotherapy agents. However, its use is limited due to its toxicity in normal tissues, including the kidney and ear. In particular, nephrotoxicity induced by cisplatin is closely associated with oxidative stress and inflammation. Heme oxygenase-1(HO-1), the rate-limiting enzyme in the heme metabolism, has been implicated in a various cellular processes, such as inflammatory injury and anti-oxidant/oxidant homeostasis. Capsaicin is reported to have therapeutic potential in cisplatin-induced renal failures. However, the mechanisms underlying its protective effects on cisplatin-induced nephrotoxicity remain largely unknown. Herein, we demonstrated that administration of capsaicin ameliorates cisplatin-induced renal dysfunction by assessing the levels of serum creatinine and blood urea nitrogen (BUN) as well as tissue histology. In addition, capsaicin treatment attenuates the expression of inflammatory mediators and oxidative stress markers for renal damage. We also found that capsaicin induces HO-1 expression in kidney tissues and HK-2 cells. Notably, the protective effects of capsaicin were completely abrogated by treatment with either the HO inhibitor ZnPP IX or HO-1 knockdown in HK-2 cells. These results suggest that capsaicin has protective effects against cisplatin-induced renal dysfunction through induction of HO-1 as well as inhibition oxidative stress and inflammation.

• 보건의료생명과학 논문지
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• 제9권1호
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• pp.141-146
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• 2021

호신용 스프레이의 자극성 액체에 포함된 capsaicin, dihydrocapsaicin 및 nonivamide의 함량을 기체 크로마토그래피로 정량하는 방법에 대해 연구하였다. Capsaicin과 거의 동등한 수준의 매운맛을 내는 nonivamide는 천연물 내에도 극히 소량 존재하므로 합성된 nonvamide를 합성 캡사이신(Synthetic capsaicinoid) 또는 PAVA(Pelargonic Acid Vanillyl Amide)라고 부르며 식품 향미 재료나 폭동진압용 무능화 작용제로 이용되어왔다. 호신용품이 난립하는 요즘 각종 불법 호신용 스프레이의 품질관리가 제대로 이행되지 않는 사례가 종종 발견되고 있다. 따라서 기체크로마토그래피로 합성 캡사이신이 포함된 제품이 천연 유래인 것처럼 도용되거나 허용농도를 준수하는 지를 판별할 수 있는 간단한 분석방법을 개발하고자 하였다. 마지막으로 분석방법이 확립되면 시판되는 호신용 스프레이 내에 존재하는 자극성 액체의 성분과 함량 조사에 응용하여 보았다.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2001년도 International Symposium on Dietary and Medicinal Antimutgens and Anticarcinogens
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• pp.153-153
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• 2001

Capsaicin, a major pungent ingredient in red hot pepper, has long been used in food additives and drugs. We have previously reported that capsaicin induces apoptosis in Korean stomach cancer cell line, SNU-1. In the present study, the mechanism of capsaicin-induced apoptotic cell death was investigated in SNU-1. Treatment of capsaicin to SNU-1 produced dose-dependent increase of apoptotic cell death and ［Ca2＋］$_{i}$ concentrations.(omitted)d)

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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• pp.147-147
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• 1993

신생쥐의 DRG 배양에서 접종후 1일째 neurite의 형성을 관찰할수 있었고 배양한 세포가 신경세포임을 확인하기 위하여 신경섬유에 대한 항체를 이용한 조직화학적 실험을 실시한 결과 붉게 염색된 세포를 볼 수 있었으므로 이 세포들이 DRG신경세포임을 확인할 수 있었다. 배양한 신경세포중 capsaicin에 대한 감수성을 갖는 신경세포군을 확인하기 위하여 cobalt stain 방법으로 실험한 결과 capsaicin에 대한 감수성율 갖는 신경세포룰 관찰할 수 있었고 비교를 위하여 함께 실험한 resiniferatoxin, KR 25018, 6-paradol, NE-19550, RDL-201등의 capsaicin 유사체들의 경우도 정도는 달리 하였으나 유사한 반응을 보였으므로 일차배양한 신경세포에 대한 작용이 capsaicin의 작용과 같을 가능성을 보여주었다. 진통효과 검정결과 진통효과가 있는 것으로 확인된 capsaicin 구조 유사체들인 resiniferatoxin, 6-paradol, NE-19550, RDL-201, KR-25018모두 농도 의존적인 반응을 보였다. 또한 칼슘 도입을 위해 요구되는 관능기로는 알킬측쇄와 P-위치의 수산기, 3-methoxy기 및 acyl amide 구조가 중요하였다. 알킬측쇄는 NVA의 경우처럼 탄소 8개 정도가 적당했으나 구조적으로 현저히 다른 치환기를 가진 resiniferatoxin이나 KR-25018의 경우에도 유효하였다. Vanillin환의 P-수산기도 필수적이었고 3-methoxy기의 존재시에는 칼슘 도입효과가 강하였다. Acyl amide 결합도 중요하나 필수적은 아니였다.

• 약학회지
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• 제33권4호
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• pp.241-245
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• 1989

A new application of high performance liquid chromatography for the determination of capsaicin and dihydrocapsaicin in cataplasma preparation was investigated. Optimum conditions for a good separation and detection were determined; 0.93 volt, acetonitrile: $H_3PO_4$ sol (pH 2.8), sample size; $7\;{\mu}l$. Recovery rates of capsaicin and dihydrocapsaicin from mixed artificial preparations were 99.9% and 98.4% respectively. Also reproducibility tests showed that the coefficient of variation was 1.59% for capsaicin and 1.14% for dihydrocapsaicin. There was no interference with cataplasma preparation containing thymol, dl-camphor and the commonly encountered excipients or additives such as gelatine, glycerine. This method was rapid, accurate and it gave higher sensitivity than other method.

• 한국식품위생안전성학회지
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• 제4권3호
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• pp.191-198
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• 1989

고속 액체크로마토그래피를 이용하여 고추 중의 주요 신미성분인 Capsaicin 및 Dihydrocapsaicin을 분석하기 위한 최적 조건을 검토하고 고추의 품종, 재배지역 및 건조 방법에 따른 함량의 차이를 비교 검토하였다. 시료중의 Capsaicin 및 Dihydrocapsaicin을 70% ethanol, $60^{\circ}C$에서 1시간 동안 처리함으로써 효과적으로 추출할 수 있었으며 재현성 및 회수율시험 결과 분석데이타의 해석은 피이크의 면적을 기준으로 하는 것이 바람직함을 알수 있었다. 고추의 품종, 재배지역 및 건조 방법에 따라 함량의 차이가 큰 것으로 나타났으며 특히 건조방법에 의한 차이가 더욱 현저하여 태양건조의 경우가 기계건조의 경우에 비하여 capsaicin의 경우는 최고 80%, dihydrocapsaicin의 경우는 최고 60% 정도 높게 나타났다.

• 약학회지
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• 제44권6호
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• pp.499-504
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• 2000

We previously demonstrated that 6-paradol, a compound structurally related to capsaicin, showed to produce prolonged analgesia in experimental animals. The effects of 6-paradol on the release of adenosine were investigated in the rat spinal cord synaptosomes by high performance liquid chromatography. In the presence of $Ca^{++}$, adenosine was released from synaptosomes of rat spinal cord by 6-paradol and capsaicin in a dose dependent manner. Nifedifine, L-type voltage sensitive calcium channel blocker, was found to be ineffective in releasing adenosine by $10\;{\mu}M$ 6-paradol. After exposure to $10\;{\mu}M$ capsazepine, a novel capsaicin selective antagonist, the level of adenosine evoked by $10\;{\mu}M$ 6-paradol was decreased by 75%, and that evoked by $10\;{\mu}M$ capsaicin was blocked completely. These results suggest that the analgesic effect of 6-paradol might be mediated by the vanilloid (capsaicin) sensitive pathway, or the direct binding to the vanilloid receptor.

• Archives of Pharmacal Research
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• 제19권3호
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• pp.246-247
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• 1996

In the previous reports (Park et al., 1991, and 1993), we described the synthesis and analgesic effects of various homovanillic amides as analogs of capsaicin. In the study, we tried to enhance the analgesic actvity of capsaicin by structural modification. Our study has been performed in three directions. First, the amide bond of capsaicin was transposed. Second, a phenyl ring was introduced to replace a double bond of capsaicin. Finally, aminoethylation was performed on 4-hydroxy group of capsaicin to improve oral bioavailability. These studies have led to N-(3-phenylpropyl)homovanillic amide 2 which has high analgesic activity. Our continuing efforts in this area have focused on the introduction of various substituents on the phenyl ring of 2 as well as their pharmacological studies. We report herein the synthesis of homovanillic amide derivatives and their analgesic activity.

• 중환자간호학회지
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• 제14권3호
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• pp.73-86
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• 2021

Purpose : This study aimed to investigate the effects of oropharyngeal sensory stimulation using low-temperature capsaicin on dysphagia, dietary level, aspiration pneumonia, and nutritional status in acute stroke patients with dysphagia admitted to a stroke intensive care unit. Methods : This study used a randomized controlled trial design and 43 participants were randomly assigned to the experimental group (n=21) or control group (n=22). An oropharyngeal sensory stimulation intervention program was constructed based on previous studies. The intervention was provided before meals twice a day for seven days and started with the first meal after hospitalization. In the control group, a solution was made using only bottled water without adding capsaicin solution, and the intervention was provided at the same time, method, and number of times as the experimental group. Results : As a result of the study, dysphagia and dietary level improved in the experimental group that received oropharyngeal sensory stimulation using capsaicin. There were no effects on the nutritional status or aspiration pneumonia. Conclusion : This study provides basic data for the development of an intervention program for patients with dysphagia by presenting a theoretical basis that oropharyngeal sensory stimulation intervention using capsaicin improves dysphagia and dietary levels.

• The Korean Journal of Pain
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• 제35권3호
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• pp.261-270
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• 2022

Background: The rostral ventromedial medulla (RVM) is a critical region for the management of nociception. The RVM is also involved in learning and memory processes due to its relationship with the hippocampus. The purpose of the present study was to investigate the molecular mechanisms behind orexin-A signaling in the RVM and hippocampus's effects on capsaicin-induced pulpal nociception and cognitive impairments in rats. Methods: Capsaicin (100 g) was applied intradentally to male Wistar rats to induce inflammatory pulpal nociception. Orexin-A and an orexin-1 receptor antagonist (SB-334867) were then microinjected into the RVM. Immunoblotting and immunofluorescence staining were used to check the levels of cyclooxygenase-2 (COX-2) and brain-derived neurotrophic factor (BDNF) in the RVM and hippocampus. Results: Interdental capsaicin treatment resulted in nociceptive responses as well as a reduction in spatial learning and memory. Additionally, it resulted in decreased BDNF and increased COX-2 expression levels. Orexin-A administration (50 pmol/1 µL/rat) could reverse such molecular changes. SB-334867 microinjection (80 nM/1 µL/rat) suppressed orexin's effects. Conclusions: Orexin-A signaling in the RVM and hippocampus modulates capsaicin-induced pulpal nociception in male rats by increasing BDNF expression and decreasing COX-2 expression.