• 제목/요약/키워드: Anti-inflammatory drug

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Development of Drug Candidate for the Treatment of Lymphedema Using Natural Product and its Derivatives from Rhus verniciflua Strokes (옻나무(Rhus verniciflua Strokes) 주요 단일성분과 그 유도체를 이용한 다중기전 림프부종 치료제 후보물질 개발)

  • Sukchan Lee;Jin-Mo Ku
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2022.09a
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    • pp.20-20
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    • 2022
  • Herein, we demonstrate that butein (1) can prevent swelling in a murine lymphedema model by suppressing tumor necrosis factor α (TNF-α) production. Butein derivatives were synthesized and evaluated to identify compounds with in vitro anti-inflammatory activity. Among them, 20 µM of compounds 7j, 7m, and 14a showed 50% suppression of TNF-α production in mouse peritoneal macrophages after lipopolysaccharide stimulation. Compound 14a, exhibited the strongest potency with an in vitro IC50 of 14.6 µM and suppressed limb volume by 70% in a murine lymphedema model. The prodrug strategy enabled a six-fold increase in kinetic solubility of compound 1 and five-fold higher levels of active metabolite in the blood for compound 14a via oral administration in the pharmacokinetics study. We suggest that the compound 14a could be developed as a potential therapeutic agent targeting anti-inflammatory activity to alleviate lymphedema progression.

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Anti-asthmatic Effects of Samjajihwang-tang in OVA-induced Mice (삼자지황탕(三子地黃湯)의 생쥐 모델에 대한 항천식 효과)

  • Kim, Woon-Kil;Park, Yang-Chun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.23 no.2
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    • pp.343-350
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    • 2009
  • This study aimed to evaluate the anti-asthmatic effects of Samjajihwang-tang (SJT) using OVA-induced asthmatic mice model. Asthmatic mice model was conducted by repeated challenge of OVA using C57BL/6 mice. Each group was treated with distilled water, SJT (400 mg/kg and 200 mg/kg) extract or cyclosporin A (10 mg/kg) for the later 8 weeks, Penh (plethysmography and enhanced pause), immune cells subpopulation, eotaxin, IL-5, TNF-${\alpha}$, Anti-OVA-lgE in BALF (bronchoalveolar lavage), and lung tissue was analyzed, No cytotoxicity of SJT was shown on hFCs (human fibroblast cells). Administration of SJT significantly decreased Penh levels comparing to control group. SJT treatment significantly ameliorated the increase of total cells number and eosinophil including of immune cell subpopulation of $CD3^+/CD69^+$, $CCR3^+$, $B220^+/CD22^+$, $B220^+/CD45^+$, and $B220^+/lgE^+$ cells in BALF comparing to control group. Eotaxin, IL-5, TNF-${\alpha}$, and Anti-OVA-lgE level in BALF were significantly decreased by SJT treatment too. Histopathological finding verified the improvement of infiltration of inflammatory cells and collagen tissue in the SJT groups comparing to control group. These results strongly suggest that SJT would be a effective candidate for herbal-originated anti-asthmatic drug. However, this drug should be further studied for characterization of the accurate action and underlying mechanisms using variant disease model in the future.

Tolfenamic Acid Suppresses Inflammatory Stimuli-Mediated Activation of NF-κB Signaling

  • Shao, Hong Jun;Lou, Zhiyuan;Jeong, Jin Boo;Kim, Kui Jin;Lee, Jihye;Lee, Seong-Ho
    • Biomolecules & Therapeutics
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    • v.23 no.1
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    • pp.39-44
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    • 2015
  • Tolfenamic acid (TA) is a traditional non-steroid anti-inflammatory drug (NSAID) and has been broadly used for the treatment of migraines. Nuclear factor kappa B (NF-${\kappa}B$) is a sequence-specific transcription factor and plays a key role in the development and progression of inflammation and cancer. We performed the current study to investigate the underlying mechanisms by which TA suppresses inflammation focusing on NF-${\kappa}B$ pathway in TNF-${\alpha}$ stimulated human normal and cancer cell lines and lipopolysaccharide (LPS)-stimulated mouse macrophages. Different types of human cells (HCT116, HT-29 and HEK293) and mouse macrophages (RAW264.7) were pre-treated with different concentrations of TA and then exposed to inflammatory stimuli such as TNF-${\alpha}$ and LPS. Transcriptional activity of NF-${\kappa}B$, $l{\kappa}B-{\alpha}$-degradation, p65 translocation and mitogen-activated protein kinase (MAPK) activations were measured using luciferase assay and Western blots. Pre-treatment of TA repressed TNF-${\alpha}$- or LPS-stimulated NF-${\kappa}B$ transactivation in a dose-dependent manner. TA treatment reduced degradation of $l{\kappa}B-{\alpha}$ and subsequent translocation of p65 into nucleus. TA significantly down-regulated the phosphorylation of c-Jun N-terminal kinase (JNK). However, TA had no effect on NF-${\kappa}B$ signaling and JNK phosphorylation in HT-29 human colorectal cancer cells. TA possesses anti-inflammatory activities through suppression of JNK/NF-${\kappa}B$ pathway in different types of cells.

Effect of Artemisiae Capillaris Herba on Anti-inflammatory Properties in RAW264.7 Cell Line

  • Kang Seong Yeob;Kim Sung Hoon;Kim Su Myung;Namgoong Uk;Kim Dong Hee
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.18 no.6
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    • pp.1832-1842
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    • 2004
  • The present study was performed to examine the possible anti-inflammatory effects of a herbal drug ASCH in RAW264.7 cell line. Inflammation was induced by LPS toxin treatment to RAW264.7 macrophage cell line. Increases in cytokine production such as IL-1β, IL-6. and IL-18, COX-2, NOS-Ⅱ (iNOS), and TNF-alpha were observed at mRNA level in the LPS-treated RAW264.7 cells. Measurement of IL-6, nitric oxide and the reactive oxygen species (ROS) showed increased production of these inflammation mediators. Treatment of ASCH effectively decreased IL-1β protein in a dose-dependent manner, and IL-6 and IL-18 were reduced at 100㎍/㎖ of ASCH concentration. NO production was also decreased by ASCH treatment. A slight inhibition for TNF-alpha in terms of protein, but not mRNA level was obtained by 100㎍/㎖ of ASCH treatment. ASCH treatment to normal RAW264.7 cells did not produce any cytotoxicity, indicting that the action of ASCH was selective to inflammatory cells. Thus, the present data suggest that ASCH may act as an important regulator to alleviate the inflammatory symptoms.

3,4,5-Trihydroxycinnamic Acid Inhibits LPS-Induced iNOS Expression by Suppressing NF-${\kappa}B$ Activation in BV2 Microglial Cells

  • Lee, Jae-Won;Bae, Chang-Jun;Choi, Yong-Jun;Kim, Song-In;Kim, Nam-Ho;Lee, Hee-Jae;Kim, Sung-Soo;Kwon, Yong-Soo;Chun, Wan-Joo
    • The Korean Journal of Physiology and Pharmacology
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    • v.16 no.2
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    • pp.107-112
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    • 2012
  • Although various derivatives of caffeic acid have been reported to possess a wide variety of biological activities such as neuronal protection against excitotoxicity and anti-inflammatory property, the biological activity of 3,4,5-trihydroxycinnamic acid (THC), a derivative of hydroxycinnamic acids, has not been clearly examined. The objective of the present study is to evaluate the anti-inflammatory effects of THC on lipopolysaccharide (LPS)-stimulated BV2 microglial cells. THC significantly suppressed LPS-induced excessive production of nitric oxide (NO) and expression of iNOS, which is responsible for the production of iNOS. THC also suppressed LPS-induced overproduction of pro-inflammatory cytokines such as IL-$1{\beta}$and TNF-${\alpha}$ in BV2 microgilal cells. Furthermore, THC significantly suppressed LPS-induced degradation of $I{\kappa}B$, which retains NF-${\kappa}B$ in the cytoplasm. Therefore, THC attenuated nuclear translocation of NF-${\kappa}B$, a major pro-inflammatory transcription factor. Taken together, the present study for the first time demonstrates that THC exhibits antiinflammatory activity through the suppression of NF-${\kappa}B$ transcriptional activation in LPS-stimulated BV2 microglial cells.

Articular Cartilage Protective Effects of Kangwhaldoche-tang(Qianghuodaozhi-tang) Aqueous Extracts on the Adjuvant-induced Rat Rheumatoid Arthritis (강활도체탕(羌活導滯湯) 물 추출물의 Adjuvant 유발 류마티스 관절염 랫트에 대한 관절연골 보호효과)

  • Kwon, O-Gon;An, Hee-Duk
    • Journal of Korean Medicine Rehabilitation
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    • v.23 no.2
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    • pp.49-61
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    • 2013
  • Objectives : This study was conducted to determine whether or not Kangwhaldoche-tang(Qianghuodaozhi-tang) (KDT) aqueous extracts can protect articular cartilage losses on the Freund's complete adjuvant(FCA)-induced rat rheumatoid arthritis. Methods : 520, 260 or 130 mg/kg of KDT were orally administered once a day for 14 days from 14 days after FCA treatments, and 15 mg/kg of dexamethasone was intraperitoneally administered as reference drug in this experiment. Changes on the body weight, knee circumferences, gross arthritis score, inflammatory tissue prostaglandin(PG) $E_2$ levels were monitored with cartilage collagen components and glucosaminoglycans(GAGs) compositions - chondroitin sulphate, heparin sulphate and hyaluronic acid in the present study. Results : As results of FCA treatment, classic rheumatoid arthritis featuring dramatic decreases of the body weights, cartilage collagen and GAGs contents with increases of the knee circumferences, gross arthritis scores and inflammatory tissue $PGE_2$ levels, were demonstrated in the present study. However, these changes from FCA - induced rheumatoid arthritis were clearly inhibited by treatment of dexamethasone and all three different dosages of KDT. Although overall anti-inflammatory effects of KDT 520 mg/kg were lowered than those of dexamethasone 15 mg/kg treated rats, KDT 520 mg/kg showed more favorable preserve effects on the cartilage GAGs and KDT 260 mg/kg treated rats showed similar preserve effects as compared with dexamethasone 15 mg/kg in this experiment. Conclusions : The present results supported that over 75 mg/kg of KDT showed favorable anti-arthritic effects on the FCA-induced arthritis mediated by suppression of $PGE_2$, representative inflammatory mediator, and may help improve rheumatoid arthritis.

Review about using Herbal medicine on steroid tapering and steroid overuse in Skin disease (피부과 영역에서 steroid 테이퍼링 및 남용 완화를 위한 한약 사용에 대한 고찰)

  • Han, Chang-Yi;Kim, Jun-Dong;Kang, Dong-Won;Kim, Kyu-Seok;Kim, Yoon-Bum
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.33 no.3
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    • pp.115-124
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    • 2020
  • Objectives : The purpose of this study is to investigate the effect and side effects of steroids on dermatitis and skin barrier through lipid metabolism. And to propose using Herbal medicine to suppress Steroid rebound and prevent side effects. Methods : We reviewed recent studies about the relationship between dermatitis, skin lipid, steroid, and herbal medicine through Google scholar. Results : In various inflammatory skin diseases, the corticosteroid is selected as the primary drug due to its strong anti-inflammatory and immunosuppressive effect. However, long-term use of steroids has a variety of side effects, especially lipid metabolism disruption, which aggravates skin barrier damage underlying various skin diseases and is more susceptible to inflammatory reactions. Conclusions : Herbal medicine is used as a comprehensive approach, and it can be used to reduce the frequency of steroid exposure by protecting against barrier damage by controlling anti-inflammatory, antioxidant, and systemic/sebaceous lipid metabolism and stratum corneum protein differentiation.

The Effects of Protecting Liver and Improving Liver Function on Cabbage Extract (양배추 추출물의 간보호 및 간기능 개선 효과)

  • Kim, Hyun Kyoung
    • The Journal of the Convergence on Culture Technology
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    • v.5 no.2
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    • pp.389-395
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    • 2019
  • This study investigated the pharmaceutical extraction and the functional health food extraction, which have a beneficial effect on the human body and which can be used safely for a long period of time without adverse side effects and also have excellent effects of protecting liver and improving liver function. As the results, the cabbage extract does not show cytotoxicity, and thus can be used safely. In an experiment performed on an animal model with liver injury induced by a drug (APAP), it could be seen that the cabbage extract exhibited the effects of protecting liver and improving liver function by effectively reducing AST and ALT which are liver injury markers, indicating that the cabbage extract is effective as a pharmaceutical extraction for preventing or treating liver disease. In particular, the cabbage extract was effective in treating inflammation of the liver by reducing the expression of the inflammatory mediators iNOS and COX-2 and the proinflammatory cytokine $IL-1{\beta}$, which are involved in acute inflammatory reactions accompanying liver injury. In the results, an extract of cabbage heat-treated at a temperature of 100 to $150^{\circ}C$ had a better liver function-improving effect or anti-inflammatory effect than an extract of raw cabbage.

The Anti-inflammatory Effects of Heat-treated Broccoli Extract (열처리된 브로콜리 추출물의 항염증 효과)

  • Kim, Hyun Kyoung
    • The Journal of the Convergence on Culture Technology
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    • v.5 no.2
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    • pp.397-404
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    • 2019
  • This study was carried out to investigate the heat-treated broccoli extraction which have a beneficial effect on the human body and which can be used safely for a long period of time without adverse side effects and also have excellent effects of protecting liver and improving liver function. The heat-treated broccoli extract does not show cytotoxicity, and thus can be used safely. In an experiment performed on an animal model with liver injury induced by a drug (APAP), it could be seen that the heat-treated cabbage extract exhibited the effects of protecting liver and improving liver function by effectively reducing AST and ALT which are liver injury markers, indicating that the heat-treated brocoli extract is effective as a pharmaceutical extraction for preventing or treating liver disease. In particular, the heat-treated broccoli extract was effective in treating inflammation of the liver by reducing the expression of the inflammatory mediators iNOS and COX-2 and the proinflammatory cytokine $IL-1{\beta}$, which are involved in acute inflammatory reactions accompanying liver injury.

Acupotomy for Scapulohumeral Periarthritis

  • Guo, Chang Qing;Ma, Shi Ning;Fu, Xin Yi;Wang, Quan Gui;Lee, Mira
    • Journal of Acupuncture Research
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    • v.37 no.4
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    • pp.254-258
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    • 2020
  • Background: Scapulohumeral periarthritis causes pain and stiffness, and limits movement but it is a treatable condition. This was a clinical study of acupotomy treatment for scapulohumeral periarthritis. Methods: There were 80 patients randomly assigned to the traditional Chinese Medicine group (acupotomy) and the Western medicine group (naproxen), with 40 cases in each group. All patients had adjunct physiotherapy exercises for 14 days. Patients received acupotomy treatment 3 times for 14 days (Day 0, 7 and 14) or naproxen (0.22 g capsule; a non-steroidal anti-inflammatory drug) 3 times a day, for 14 days. The visual analogue scale (VAS) scores, range of motion (ROM) values, and the Melle scale, together with the therapeutic standard of diseases and syndromes in traditional Chinese Medicine were used for diagnosis and evaluation. Results: There were significant differences in the VAS scores, ROM, Melle scores, cure rate and total effective rate in the group which took naproxen and the acupotomy group, before and after treatment (p < 0.01). There were significant differences in the changes in VAS, ROM and Melle scores between the 2 groups (p < 0.01), and the acupotomy group was better than the naproxen group. Conclusion: Traditional Chinese Medicine and Western medicine can improve functional activity and reduce the level of pain experienced by patients suffering from scapulohumeral periarthritis. However, improvement of functional activity of the shoulder joint following acupotomy treatment was more obvious than the use of a non-steroidal anti-inflammatory drug, and the cure rate, and total effective rate of acupotomy was better.