• Title/Summary/Keyword: analgesic activity

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Effect of the Changes in Arterial Carbon Dioxide Pressure on the Neuronal Activities of Rostral Ventrolateral Medulla in the Cat (고양이에서 동맥혈 탄산가스 분압의 변동이 연수의 통각정보 처리과정에 미치는 영향)

  • Lee, Young-Tak;Kim, Chong-Whan;Kim, Jun
    • Journal of Chest Surgery
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    • v.29 no.5
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    • pp.477-486
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    • 1996
  • Endogenous analgesic systems are known to be activated by peripheral noxious stimulation as well as arterial carbon dioxide elevation. In the present study, neuronal Activities in the rostral ventrolateral med- ulla were identified and classified in according to their rhythmic activities, and their responses to noxious peripheral nerve stimulations before and after elevating the arterial carbon dioxide partial pressure were investigated Using extracellular recording technic, a total of 53 spontaneously active neurons were recorded from the rostral ventrolateral medulla in u-chloralose anesthetized cats. These were classified as cardiovascular (28), respiratory (16), both cardiovascular and respiratory (2) and noncardiovascular - nonrespiratory (7). - Among the 28 cardiovascular neurons eleven showed increased activities during arterial hypercapnia, thirteen showed decreased responses, and four showed no change. Nine respiratory neurons showed increased responses to arterial hypercapnia, six showed decreased responses and one showed no change. neither of the cardiovascular and respiratory neurons showed significant change in its activity during ar- terial hypercapnia, however, four of the noncardiovascular - nonrespiratory neurons exhibited decreased their activities in response to arterial hypercapnia while two exhibited increased activities. Arterial hypercapnia increased the responses of cardiovascular neurons to peripheral nerve stimulation with C-inteniity, while not changing the responses to Ak_stimulation significantly . From the above results it was conclllded that during arterial hypercapnia, some cardiovascular neurons and respiratory neurons have increased activities as well as increased reponses to C-Hber stimulation.

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Potential Seizurogenic Effect of Tramadol in a Dog with Necrotizing Meningoencephalitis (괴사성 뇌척수막염을 가진 진돗개에서 Tramadol에 의한 잠재적 경련발생 증례)

  • Kim, Se-Hun;Heo, Su-Young;Lee, Ki-Chang;Lee, Hae-Beom;Kim, Nam-Soo;Kim, Min-Su
    • Journal of Veterinary Clinics
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    • v.28 no.3
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    • pp.323-327
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    • 2011
  • A Jindo dog (8-month-old, intact male) was referred for hind limb lameness on the right side. The dog was diagnosed with a simple femoral fracture by radiological examination. After surgical fixation of the femoral fracture, tramadol: a narcotic-like synthetic analgesic was intravenously administrated for post-operative analgesia. After injection of the tramadol, generalized tonic clonic seizure was immediately occurred in the dog. Seventeen hours later, the dog died despite intensive care. We suspected that tramadol might induce the seizurogenic effect resulted in death. A necropsy was performed to examine the cause of the death. In consequence, the dog was diagnosed as necrotizing meningoencephalitis (NME) based on histopathological examination. We would be concerned that tramadol may be related to seizure activity in the NME patient. From this case, it is known that although tramadol has been proven to be a safe and effective agent for the control of pain in veterinary medicine, it would be carefully used to patient with history of neurological diseases including meningoencephalitis, hydrocephalus, and encephalopathy.

Enhanced Skin Permeation of a New Capsaicin Derivative (DA-5018) from a Binary Vehicle System Composed of Isopropyl-myristate and Ethoxydiglycol

  • Cha, Bong-Jin;Lee, Eung-Doo;Kim, Won-Bae;Chung, Suk-Jae;Lee, Min-Hwa;Shim, Chang-Koo
    • Archives of Pharmacal Research
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    • v.24 no.3
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    • pp.224-228
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    • 2001
  • DA-5018, a recently synthesized capsaicin analog, appears to possess potent analgesic activity when administered topically. The objective of this study is to test the feasibility of the topical administration of this compound. Specifically, our goal was to identify vehicle system that permit a reasonable transdermal permeation of the compound in mice. Among the vehicles examined, isopropyl myristate (IPM) showed the largest in vitro permeability across the intact skin (83.6 ${\pm}$ 5.42${\mu}$l/$\textrm{cm}^2$/h ). However, due to the limited solubility of DA-5018 in IPM (0.53 mg/ml), the maximal flux from the IPM medium remained at only 44.3 ${\pm}2.87{\mu}$g/$\textrm{cm}^2$/hr. In order to increase the flux, addition of better solvents for DA-5018 was attempted, under the assumption that flux is the result of both solubility and permeability. Ethoxydiglycol (EG) and oleic acid (OA) were selected as examples of food solvents. The addition of IC or OA to IPM at a 1:1 volume ratio resulted in a comparable increase in the solubility of the compound (i.e., to 61.1 and 50.2 mg/ml for EG and OA, respectively). However, the addition of EG at a 1:1 volume ratio, for example, increased the flux 6.3 fold (i.e., $279{\mu}$g/$\textrm{cm}^2$/hr), while OA, at a 1:1 volume ratio, decreased the flux 5 fold (i.e., $9.26{\mu}$g/$\textrm{cm}^2$//hr). The mechanism of this discrepancy between EG and OA was investigated by measuring the permeabilty of DA-5018 across the stratum corneum-removed skin of the mouse, under the hypothesis that the viable skin layer may serve as a barrier for the permeation of lipophilic substances such as DA 5018. The permeability of DA-5018, from the medium of EG or OA, across the viable skin differed greatly for EG ($0.41{\mu}$l/$\textrm{cm}^2$/hr) and OA ($0.086{\mu}$l/$\textrm{cm}^2$/hr), suggesting that a higher permeability across the viable skin layer is needed for the second solvents. The maximum flux across the intact skin was achieved for DA-5018 when EG was added to IPM at a 1:1 volume ratio. Thus, the use of a binary system appears to be the best approach for realizing the transdermal delivery of DA-5018 at a reasonable rate.

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Depressor Responses to Intravenously Administered Artemisia asiatica Nakai Juice in Cats (애엽(艾葉) (Artemisia asiatica Nakai)의 혈압강하작용(血壓降下作用))

  • Kim, Yun-Ho;Shin, Hong-Kee;Kim, Kee-Soon
    • The Korean Journal of Physiology
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    • v.15 no.2
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    • pp.91-96
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    • 1981
  • The wormwood is one of the plants which occur widely throughout the world. Though the precise data on the entire chemical composition of mugwort leaves are not available, the major principles which have been found so far include inulin, alkaloid, thujon, sesquiterpene and several vitamins. Santonin, a parasiticide, is one of the glucosides extracted from the limited species of wormwood. It has long been known in herb medicine that the plants of this family has not only strong hemostatic, analgesic and parasiticidal actions but also therapeutic effects for diarrhea, stomachache and asthma. In recent pharmaceutical botany the wormwood is introduced to have antipyretic and astringent actions also. The mugwort(Artemisia asiatica Nakai) is the most common species of wormwood that occurs in Korea. The usage of this edible leaves of mugwort is rather various. It is used not only for wormwood bath but also as forage, moxa and medicinal agents. Recently Kim et al reported from their study on the effect of mugwort on the motility of isolated intestine of rabbits that tonus and motility were markedly enhanced by mugwort but this effect of mugwort on intestinal motility was almost completely blocked by atropine suggesting that activity of mugwort was exerted through its cholinergic effect. It was the findings of Kim et al that prompted the authors to do the present experiment. The present study was undertaken to investigate effects of mugwort(Artemisia asiatica Nakai) juice on the respiration and blood pressure in cats. And also studied was the mechanism of depressor action of Artemisia asiatica Nakai Juice (AAJ). The results obtained are as follows; 1) It was observed that mean arterial blood pressure and heart rate were decreased markedly by AAJ. Following administration of 0.15 ml/kg and 0.3 ml/kg AAJ into cats the maximum depressor responses observed were $77.5{\pm}2.2\;mmHg$ and $94.0{\pm}3.7\;mmHg$ respectively. 2) Depressor responses to AAJ were blocked markedly by atropine whereas the responses were not affected by propranolol and dibenamine. Therefore it is strongly inferred that depressor action of AAJ results mainly from its cholinergic effect. This inference was further substantiated by the fact that heart rate change which invariably accompanies depressor responses to AAJ was almost completely abolished by atropinization. 3) After administration of AAJ into cats frequency of respiration was markedly increased while depth of respiration decreased during first 2-3 seconds.

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Pharmacological Effect of Decursin, Decursinol Angelate, and Decursinol Derived from Angelica gigas Nakai (참당귀(Angelica gigas Nakai) 유래 decursin, decursinol 그리고 decursinol angelate의 약리 효과)

  • Kang, Jae Seon
    • Journal of Life Science
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    • v.31 no.12
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    • pp.1128-1141
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    • 2021
  • 'Angelica' is one of the most traditionally consumed medicinal herbs around Northeast Asia including Korea for treatments of various diseases or health care purposes like hematopoiesis, blood circulation for women, sedative, analgesic, and a tonic medicine etc. Angelica gigas Nakai, a Korean native species of Angelica, is clearly different from the others in containing a high concentration of active ingredients like pyranocoumarines including decursin, decursinol, and decursinol angelate. These compounds have various kinds of positive effects such as anti-tumor activity including the precaution of neutropenia occurred during anticancer drug administration, improvements of metabolic disorders, menstrual irregularity, impairment of renal function, respiration improvement, cognition-enhancement, anti-inflammatory effect, anti-oxidative effect, enhancing fertility and so forth. Thus it implies incredible potentialities in future development for foods and drugs. However, certain purity-related qualities and/or overdose in food products can cause side effects like toxicities; therefore, their safety profiles should also be considered. This review focuses on the positive and negative effects of three pyranocoumarines in Angelica gigas Nakai and some possibilities and considerations for future food and drug products development.

Protective Effect of Betula Platyphylla on Ultraviolet B-irradiated HaCaT Keratinocytes (화피(樺皮) 에탄올 추출물의 Ultraviolet B로 자극한 피부 각질 세포 보호 작용)

  • Hag Soon Choi;Hyun Joo Kim;Hark Song Lee;Seung Won Paik;Ji Eun Kim;Yung Sun Song
    • The Journal of Korean Medicine
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    • v.44 no.2
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    • pp.119-131
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    • 2023
  • Objectives: Betula Platyphylla(BP) has been used as a analgesic, anti-microbial, anti-oxidant drug in Eastern Asia. However, it is still unknown whether BP ethanol extract could exhibit the inhibitory activities against ultraviolet B(UVB)-induced skin injury on human keratinocytes, HaCaT cells. This study was aimed to investigate the protective activity of BP ethanol extract on UVB-irradiated skin injury in HaCaT cells. Methods: The skin injury model of HaCaT cells was established under UVB stimulation. HaCaT keratinocyte cells were pre-treated with BP ethanol extract for 1 h, and then stimulated with UVB. Then, the cells were harvested to measure the cell viability, production of reactive oxygen species(ROS), pro-inflammatory cytokines such as interleukin(IL) 1-beta, IL-6, and tumor necrosis factor(TNF)-𝛼, hyaluronidase, type 1 collagen, matrix metalloproteinase(MMP)s. In addition, we examined the mitogen activated protein kinases(MAPKs) and inhibitory kappa B alpha(I𝜅;-B𝛼) as inhibitory mechanisms of BP ethanol extract. Results: The treatment of BP ethanol extract inhibited the UVBinduced cell death and ROS production in HaCaT cells. BP ethanol extract treatment inhibited the UVB-induced increase of IL-1beta, IL-6, and TNF-𝛼. BP ethanol extract treatment inhibited the increase of hyaluronidase, MMP and decrease of collagen. BP ethanol extract treatment inhibited the activation of MAPKs and the degradation of I𝜅-B𝛼. Conclusions: Our result suggest that treatment of BP ethanol extract could inhibit the UVB-induced skin injury via deactivation of MAPKs and nuclear factor kappa B(NF-𝜅B) in HaCaT cells. This study could suggest that BP ethanol extract could be a beneficial agent to prevent skin damage or inflammation.

Xylazole inhibits NO-cGMP pathway in fetal rat nerve cells

  • Wang, Xinyu;Wu, Yue;Liu, Lin;Bai, Hui;Zhang, Zhiheng;Zhao, Mingchao;Ma, Tianwen;Song, Xiaopeng;Jia, Lina;Lv, Liangyu;Yu, Yue;Xu, Xinyu;Chen, Hong;Gao, Li
    • Journal of Veterinary Science
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    • v.23 no.1
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    • pp.16.1-16.13
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    • 2022
  • Background: Xylazole (Xyl) is a veterinary anesthetic that is structurally and functionally similar to xylazine. However, the effects of Xyl in vitro remain unknown. Objectives: This study aimed to investigate the anesthetic mechanism of Xyl using fetal rat nerve cells treated with Xyl. Methods: Fetal rat nerve cells cultured for seven days were treated with 10, 20, 30, and 40 ㎍/ mL Xyl for 0, 5, 10, 15, 20, 25, 30, 45, 60, 90, and 120 min. Variations of amino acid neurotransmitters (AANTs), Nitric oxide-Cyclic GMP (NO-cGMP) signaling pathway, and ATPase were evaluated. Results: Xyl decreased the levels of cGMP and NO in nerve cells. Furthermore, Xyl affected the AANT content and Na+-K+-ATPase and Ca2+-Mg2+-ATPase activity in nerve cells. These findings suggested that Xyl inhibited the NO-cGMP signaling pathway in nerve cells in vitro. Conclusions: This study provided new evidence that the anesthetic and analgesic effects of Xyl are related to the inhibition of the NO-cGMP signaling pathway.

Ulmus macrocarpa Hance Water Extract Improved Splenocytes Survival and NK Cell Cytotoxicity (왕느릅나무 추출물에 의한 비장세포 생존률 및 NK cell 세포독성 증가)

  • Lee, Sung Do;Kim, Deok Won;Lee, Inhwan;Lee, Jong-Hwan;Hyun, Sook Kyung;Kang, Kyung-Hwa;Hwang, HyeJin;Kim, CheolMin;Kim, Byoung Woo;Chung, Kyung Tae
    • Journal of Life Science
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    • v.26 no.1
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    • pp.109-116
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    • 2016
  • Ulmi cortex is the elm bark or root bark of Ulmus macrocarpa Hance and has been used as an ingredient of traditional medicine for anti-inflammatory, analgesic, anti-cancer and wound healing on both the East and the West. This study investigated whether the Ulmus macrocarpa Hance Water extract (UMWE) has the in vivo and in vitro immune activating effect. Animals were orally administrated for 14 days as follows: no treat group with distilled water, cyclophosphamide (CY) group with 120 mg/kg of CY, UMWE 100+CY group with 100 mg/kg of UMWE and 120 mg/kg of CY, UMWE 200+CY group with 200 mg/kg of UMWE and 120 mg/kg of CY, UMWE 100 group with 100 mg/kg of UMWE and UMWE 200 group with 200 mg/kg of UMWE. The immunosuppressive drug CY was intraperitoneally injected to induce immune suppression. Spleen indices showed small changes in CY injected groups but splenocyte indices showed greater decrease in the same groups. However, UMWE appeared to relieve CY’s immunosuppression. UMWE also delayed in vitro splenocyte death increasing its longevity. These data obtained by MTT assay and 7-amino-actinomycin D which stains preferentially dead than live cells. UMWE alone did not show cytotoxicity based on its apoptototic effect on splenocytes in vitro and in vivo. Splenic NK cell activity was maintained by UMWE under the presence of CY in vitro. The data indicated that UMWE protects splenocytes from the immunosuppressive drug CY under in vitro and in vivo conditions.

Effects of Ginseng and Its Saponins on Experimental Amnesia in Mice and on Cell Cultures of Neurons (인삼 및 인삼 사포닌이 쥐의 건망증 및 신경세포배양에 미치는 영향)

  • Saito Hiroshi;Nishiyama Nobuyoshi;Iwai Akihiko;Kawajiri Shinichi;Himi Toshiyuki;Sakai Toshimi;Fukunaka Chizu
    • Proceedings of the Ginseng society Conference
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    • 1988.08a
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    • pp.92-98
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    • 1988
  • The present study was performed to find the effects of ginseng and its saponins. which is written in Chung Yao Ta Tsu Tien as anti-amnesia in its chief indication. on experimental amnesia in mice. In the step through test. ginsenoside $Rb_1\;(GRb_1)\;and\;GRg_1$ facilitated the registration of memory and antagonized the electroconvulsive shock (ECS)-induced inhibition of the retention of memory. Moreover. $GRg_1$ antagonized the EtOH-induced inhibition of the retrieval of memory. In the step down test. $GRb_1\;GRb_2\;and\;GRg_1$ antagonized the ECS-induced inhibition of the retention of memory. Moreover. $GRg_1$ antagonized the EtOH-induced inhibition of the retrieval of memory and facilitated the acquisition of short term memory. In the shuttle hox and lever press tests. they have no effects on acquisition and retrieval of memory. except $GRb_1\;GRb_1$ depressed the retrieval of conditioned avoidance response in the shuttle box test. After the end of four tests. the effects of these orally administered drugs on sedative. analgesic. antipyretic and anticonvulsant actions. and on spontaneous and exploratory movements were tested in doses of less than 500mg/kg. but they had none of these effects. Present study may indicate that $GRg_1$ had effects on the retrieval of memory and on the acquisition process of learning response. The recent research on the role of NGF for the survival. regeneration and regulation of brain in adult animals. indicated the importance of NGF on dementia and amnesia. During our research on the specificity of the neurite out growth induced by NGF. we found that the effect of NGF was potentiated by $GRb_1$ in organ cultures of chick embryonic dorsal root ganglia. Then. the effect of $GRb_1$ on neuronal cell survivalin cell culture system was studied. $GRb_1$ potentiated the NGF-mediated increase of neurofilaments in cell cultures of chick embryonic sensory and sympathetic neurons. NGF with $GRb_1$ also showed a tendency to increase the number of surviving neurons of rat embryonic cerebral cortex. NGF increased choline acetyl transferase activity in cell cultures of rat embryonic septum area neurons. but $GRb_1$ did not potentiate NGF activity in cell cultures of rat embryonic septum area neurons. Present study may indicate that $GRb_1$ plays an important role for the survival or regeneration of neurons in the brain.

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