• Title/Summary/Keyword: physiological inhibitors

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The Influences of G Proteins, $Ca^{2+}$, and $K^+$ Channels on Electrical Field Stimulation in Cat Esophageal Smooth Muscle

  • Park, Jun-Hong;Kim, Hyun-Sik;Park, Sun-Young;Im, Chae-Uk;Jeong, Ji-Hoon;Kim, In-Kyeom;Sohn, Uy-Dong
    • The Korean Journal of Physiology and Pharmacology
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    • v.13 no.5
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    • pp.393-400
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    • 2009
  • NO released by myenteric neurons controls the off contraction induced by electrical field stimulation (EFS) in distal esophageal smooth muscle, but in the presence of nitric oxide synthase (NOS) inhibitor, L-NAME, contraction by EFS occurs at the same time. The authors investigated the intracellular signaling pathways related with G protein and ionic channel EFS-induced contraction using cat esophageal muscles. EFS-induced contractions were significantly suppressed by tetrodotoxin ($1\;{\mu}M$) and atropine ($1\;{\mu}M$). Furthermore, nimodipine inhibited both on and off contractions by EFS in a concentration dependent meaner. The characteristics of 'on' and 'off contraction and the effects of G-proteins, phospholipase, and $K^+$ channel on EFS-induced contraction in smooth muscle were also investigated. Pertussis toxin (PTX, a $G_i$ inactivator) attenuated both EFS-induced contractions. Cholera toxin (CTX, $G_s$ inactivator) also decreased the amplitudes of EFS-induced off and on contractions. However, phospholipase inhibitors did not affect these contractions. Pinacidil (a $K^+$ channel opener) decreased these contractions, and tetraethylammonium (TEA, ${K^+}_{Ca}$ channel blocker) increased them. These results suggest that EFS-induced on and off contractions can be mediated by the activations Gi or Gs proteins, and that L-type $Ca^{2+}$ channel may be activated by G-protein ${\alpha}$ subunits. Furthermore, ${K^+}_{Ca^-}$ channel involve in the depolarization of esophageal smooth muscle. Further studies are required to characterize the physiological regulation of $Ca^{2+}$ channel and to investigate the effects of other $K^+$ channels on EFS-induced on and off contractions.

Erlotinib Induced Trichomegaly of the Eyelashes

  • Jeon, Sang-Hoon;Ryu, Jeong-Seon;Choi, Gwang-Seong;Kim, Jung-Soo;Kwon, Hea-Yoon;Kim, Min-Su;Nam, Hae-Seong;Cho, Jae-Hwa;Kwak, Seung-Min;Lee, Hong Lyeol;Kim, Hyun-Jung;Hong, Geun-Jeong
    • Tuberculosis and Respiratory Diseases
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    • v.74 no.1
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    • pp.37-40
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    • 2013
  • Epithelial growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) have been widely used for non-small-cell lung cancer patients. Its untoward cutaneous effects are largely well known and developed in many patients treated with EGFR TKIs. However trichomegaly of eyelash is rarely reported. Although trichomegaly is not a drug-limiting side effect, it could be troublesome of continuing the treatment because of cosmetic issue or eyeball irritation by long eyelashes. Therefore clinicians are needed to pay attention to this uncommon effect. We herein describe erlotinib induced trichomegaly of eyelashes in a woman with adenocarcinoma of the lung.

The nervous system of Fibricola seoulensis by acetylcholinesterase histochemistry (Acetylcholinesterase 조직화학법으로 관찰한 Fibricola seoulensis 신경계의 분포)

  • 전은우;김창환
    • Parasites, Hosts and Diseases
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    • v.31 no.4
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    • pp.321-330
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    • 1993
  • F. seoulensis were obtained from artificially infected albino rats at 3, 4, 5, 6, 7 days after infection. The worms and metacercariae were washed in physiological saline solution, and fled with 10% neutral formalin. The acetylcholinesterase (AchE) stained by one histochemistry using acetylthiocholine iodide as substrate. Eserine, ism-OMPA and BW284C51 were used as inhibitors of AchE. The nervous system consists of three pairs longitudinal nerve trunks interconnected with excretory plexus in posterior half, and phinmc and oral sucker in anterior half of metacercariae and adults. The longitudinal nerve trunks are interconnected with transverse commissures and numerous circular commissures. Considerable numbers of circular commissures are interconnected with longitudinal nerve trunks tying on the surface of the worms. At each stage of juvenile worms, AchE and nonspecific cholinesterase activites were observed in the oral sucker, ventral sucker, pharynx and nerve system. Isoxymes of AchE in f seoderuts were separated into the two bands, 69 kDa and 132 kDa. The major band was 69 kDa.

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Status Analysis of Adulterated Herbal Medicine (국내외 위변조 한약 현황 분석)

  • Lee, Soojin
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.34 no.5
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    • pp.215-221
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    • 2020
  • Adulterated herbal medicine is intentionally added with undeclared improper or inferior ingredients which should not be in herbal medicine. The contamination with potentially hazardous substances such as heavy metal, pesticides, fungus, and microorganism sometimes can be regarded as one of adulteration in a broad sense. The problem of adulteration is that adulterated herbal medicine shows poor quality and/or can cause adverse events. Therefore, it is important to control adulteration issues for quality assurance and qualitative improvement of herbal medicines. This study aims to summarize and make a reference how to control adulterated herbal medicine. In this process, this study is to investigate studies about adulterated herbal medicine via searching Korean and foreign electronic databases such as PubMed, NDSL and OASIS. Finally eighteen papers were included to this study and analyzed according to the type of study, the category and efficacy of adulterants, the type of analysis methodologies and possible adverse events of adulterants. Phosphodiesterase type 5 (PDE-5) inhibitors for male sexual enhancement and anorexic, laxative, diuretic agents for weight loss and treating obesity has been used frequently as adulterants. The range of adverse event caused by adulterated herbal medicine were very wide from mild symptoms such as diarrhea, constipation, dizziness and blurred vision to very severe symptoms such as heart failure, hypoglycemia and renal impairment. This study showed the recent trend on the research of adulterated herbal medicine and this will be the ground to develop more detailed systems to control adulterated herbal medicine.

Review on Korean Herbal Medicine Complex Prescriptions and Single Herbal Medicines for Osteoporosis - Focused on Domestic Research Published Since 2013 (골다공증의 한방 복합 처방 및 단일 본초에 대한 국내 연구 고찰 - 2013년 이후 발표된 국내 연구를 중심으로)

  • Lee, Jung Min;Kim, Nam Hoon;Lee, Eun-Jung
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.35 no.3
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    • pp.87-96
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    • 2021
  • The purpose of this study was to investigate the effect of single herbal medicines and Korean herbal medicine complex prescriptions for osteoporosis in Korea. We targeted studies published in domestic journals from January 1, 2013 to April 1, 2021. For domestic databases, RISS, NDSL, OASIS, DBpia, KISS, KISTI, and Korean Traditional Knowledge Portal were used. Words such as "osteoporosis", "herbal medicine", "herbal combination prescription" and "herbal" were combined and searched. A total of 32 studies were selected. Among them, 8 studies were conducted exclusively for animal studies, 18 studies were conducted on cell experiments, and 6 studies were conducted on both animal and cell experiments. There were 18 studies using a single herb and 14 studies using a combination of Herbal medicine. As a result of the investigation of a single herb, it was found that 補陽藥 was most widely used, and it was found that it was mainly used in the herbal combination prescription, mainly for 補陽藥, 補氣藥, and 補陰藥. Studies in animal experiments revealed significant results mainly in bone mineral density, serological indicators, and morphological indicators of bone tissue. In the study of cell experiments, the effects were found in factors related to the differentiation of osteoclasts and inhibitors of inflammation. Through the results of this study, we are able to confirm the effective single herbal medicines and herbal medicine complex prescriptions for the treatment of osteoporosis, and it is expected that they will contribute to clinical treatment.

The Aurora Kinase Inhibitor CYC116 Promotes the Maturation of Cardiomyocytes Derived from Human Pluripotent Stem Cells

  • Sijia, Ji;Wanzhi, Tu;Chenwen, Huang;Ziyang, Chen;Xinyue, Ren;Bingqing, He;Xiaoyan, Ding;Yuelei, Chen;Xin, Xie
    • Molecules and Cells
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    • v.45 no.12
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    • pp.923-934
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    • 2022
  • Human pluripotent stem cell-derived cardiomyocytes (hPSC-CMs) have great potential in applications such as regenerative medicine, cardiac disease modeling, and in vitro drug evaluation. However, hPSC-CMs are immature, which limits their applications. During development, the maturation of CMs is accompanied by a decline in their proliferative capacity. This phenomenon suggests that regulating the cell cycle may facilitate the maturation of hPSC-CMs. Aurora kinases are essential kinases that regulate the cell cycle, the role of which is not well studied in hPSC-CM maturation. Here, we demonstrate that CYC116, an inhibitor of Aurora kinases, significantly promotes the maturation of CMs derived from both human embryonic stem cells (H1 and H9) and iPSCs (induced PSCs) (UC013), resulting in increased expression of genes related to cardiomyocyte function, better organization of the sarcomere, increased sarcomere length, increased number of mitochondria, and enhanced physiological function of the cells. In addition, a number of other Aurora kinase inhibitors have also been found to promote the maturation of hPSC-CMs. Our data suggest that blocking aurora kinase activity and regulating cell cycle progression may promote the maturation of hPSC-CMs.

As a Modulator, Multitasking Roles of SIRT1 in Respiratory Diseases

  • Yunxin Zhou;Fan Zhang;Junying Ding
    • IMMUNE NETWORK
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    • v.22 no.3
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    • pp.21.1-21.21
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    • 2022
  • As far the current severe coronavirus disease 2019 (COVID-19), respiratory disease is still the biggest threat to human health. In addition, infectious respiratory diseases are particularly prominent. In addition to killing and clearing the infection pathogen directly, regulating the immune responses against the pathogens is also an important therapeutic modality. Sirtuins belong to NAD+-dependent class III histone deacetylases. Among 7 types of sirtuins, silent information regulator type-1 (SIRT1) played a multitasking role in modulating a wide range of physiological processes, including oxidative stress, inflammation, cell apoptosis, autophagy, antibacterial and antiviral functions. It showed a critical effect in regulating immune responses by deacetylation modification, especially through high-mobility group box 1 (HMGB1), a core molecule regulating the immune system. SIRT1 was associated with many respiratory diseases, including COVID-19 infection, bacterial pneumonia, tuberculosis, and so on. Here, we reviewed the latest research progress regarding the effects of SIRT1 on immune system in respiratory diseases. First, the structure and catalytic characteristics of SIRT1 were introduced. Next, the roles of SIRT1, and the mechanisms underlying the immune regulatory effect through HMGB1, as well as the specific activators/inhibitors of SIRT1, were elaborated. Finally, the multitasking roles of SIRT1 in several respiratory diseases were discussed separately. Taken together, this review implied that SIRT1 could serve as a promising specific therapeutic target for the treatment of respiratory diseases.

Physiological Activities of Fermented Gastrodia elata Blume Extracts (발효 천마 추출물의 생리 활성)

  • Park, An Na;Ku, Tae Kyu;Kim, Kyung Sun;Lee, Dong Won;Kim, Sang Jin
    • Journal of the Korean Applied Science and Technology
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    • v.32 no.4
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    • pp.702-711
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    • 2015
  • This study was conducted to determine the feasibility of using Gastrodia elata Blume as a cosmetic raw material by investigating the physiological activities of its extracts, varying the concentration, solvent, and fermentation method (non-fermentation and fermentation using lactic acid bacteria and effective microorganisms). Of the extracts in three different solvents-water, EtOH, and 70% EtOH-at four different concentrations (0.725, 1.25, 2.5, and 5 mg/mL), the EtOH extracts demonstrated the highest contents of antioxidants (flavonoids, polyphenols, and DPPH free radical scavengers). The DPPH free radical scavenging activity in the EtOH extracts of EM-fermented Gastrodia elata Blume increased from $27.08{\pm}0.5%$ at 1.25 mg/mL to $35.89{\pm}0.8%$ at 2.5 mg/mL. The tyrosinase inhibitory activity test was performed to measure skin-whitening capacity and revealed the LB-fermented EtOH extracts to be the most efficacious ($39.1{\pm}0.4%$ at 0.725 mg/mL, $62.8{\pm}1.5%$ at 2.5 mg/mL). Viability was found to exceed 85% in RAW 264.7 cells treated with all extracts (water, EtOH, 70% EtOH at 10, 25, $50{\mu}L$, fermented and non-fermented), thus proving that Gastrodia elata Blume extracts do not cause inflammation. When RAW 264.7 cells were stimulated with lipopolysaccharide as positive controls under the same conditions to determine the antioxidant activity in the presence of reactive oxygen species (ROS), EM-fermentation was found to impart excellent antioxidant capacity. This study verified the physiological activities of fermented Gastrodia elata Blume extracts that are best suited for cosmetic ingredients, such as antioxidants, tyrosinase inhibitors and anti-inflammatory agents.

The Physiological Efficacy of Aloe Gel (Aloe Gel의 생리 효과에 대한 고찰 - Gel의 다당류와 미량 성분을 중심으로 -)

  • 서화중
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.24 no.6
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    • pp.1026-1038
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    • 1995
  • Although aloe lost a lot of its previous popularity in modern clinical uses as medicine numerous scientific researches still have claimed the beneficial properties(curing and general tonic effect) of aloe gel. Whereas considerable contradictory reports have helped to confuse the aloe gel issue and continually aroused controversy about aloe gel efficacy. However health food, cosmetic and medicinal products made from aloe gel are widely available in the world market especially in U.S.A. so the growing of Aloe plant and the processing of A. vera gel have become big industries in some countries. In some previous papers the salicylic acid, one of the common trace gel components, was thought to have an analgetic and antinflammatory effect. Large amount of Mg ion in the gel was suggested to act as anesthetic, Mg-lactate as antihistamic, and Aloctin A(a glycoprotein) as wound healer by promoting the cell growth. The carboxypeptidase and bradykinase activity in the gel were proposed to have the pain relieving and antiinflammatory effect. But any of thes etheories concerining the physiological action of the trace gel components has not been demonstrated by modern pharmacology, and failed to be supported by clinical research. It was suggested by some research workers that trace amount of anthraquinone compounds in the gel play an important role to act as false substrate inhibitors for PG and TX production(antiprostanoid effect), by which, they believed, inflammation, burn and frostbite, and infected wound could be healed. This hypothesis has not been substantiated. Butthe suggested antimicrobial action, antidiabetic, and antidotic effect of aloe gel are likely to be attributed to the trace anthraquinone compounds. In a lot of recent experimental reports it has been claimed that aloe gel polysaccharides(acetylglucomannan, acetylmannan, and glycoprotein) have the antimicrobial, antinflammatory, antitumour, and infected wound healing effect by immunoenhancement. It is hoped that these effects will be soon documented in clinical studies, then the controversy on aloe gel beneficial effect will cease. In the 30 days subchronic toxicity test the lowest observed adverse effect level of acemannan(acetylmannan) on dog was 5.0 mg/kg, IP. But the aloe gel is generally agreed to be harmless and non toxic even for the internal use such as health food. In the case of idiosynrasy one must keep the delayed type hypersensitivity reaction of aloe gel in mind. In conclusion it seem to be impossible to simply refuse a lot of evidences made by research workers who have claimed aloe gel's beneficial effects and to deny the fact that there had been long therapeutic histories of Aloe plants.

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In vitro Study of Anti-inflammatory Effects of Salvia Miltiorrhiza Extracts Using Luciferase Reporter Gene Assay (Luciferase Reporter Gene Assay를 이용하는 단삼추물문의 소염 및 진통작용에 대한 in vitro 연구)

  • Lee Han Chang;Yeom Mi Jung;Kim Gun Ho;Han Dong Oh;Zhao Mei Ai;Shim In Sop;Lee Hye Jung;Choi Kang Duk;Hahm Dae Hyun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.18 no.3
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    • pp.740-746
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    • 2004
  • In order to identify the anti-inflammatory and analgesic properties of natural herbal extracts, widely used in the Korean traditional medicine, an in vitro screening system was designed using pGL3, a luciferase reporter vector, and the tumor necrosis factor (TNF)-α and cyclooxygenase (COX)-II as target genes. The promoter regions of each gene was generated by PCR using the human chromosome as template DNA, and inserted into pGL3 vector with Kpnl and Hindlll. The final construct was transfected into human myleomonocytic leukemia cells (U937) that could be differentiated and activated by phorbol 12-myristate 13-acetate (PMA) or lipopolysaccharide (LPS). Using this system, we tested the anti-inflammatory and analgesic effects of several herbal extracts being regarded to have the medicinal effects of diminishing the body heat and complementing Qi. The well-known chemicals of PD98059 and berberine chloride were used as controls of the transcriptional inhibitors of TNF-α and COX-II, respectively. Among them, Salvia miltiorrhiza (Dan-Sam) was found to exhibit the significant medicinal properties of anti-inflammatory and analgesic effects.