• 제목/요약/키워드: anti-ulcer

검색결과 172건 처리시간 0.024초

High Throughput Screening for Natural Products to Find Biologically Active Compounds : Natural Products versus Combinatorial Chemistry

  • Sankawa, Ushio
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1997년도 추계학술대회
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    • pp.47-50
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    • 1997
  • Drug development began with the finding of biologically active compounds which are obtained by chemical synthesis or from natural sources. The advent of Combinatorial Chemistry is recognized as a strategy which has a potential to change the methodology of research and development(R&D) of new drugs. Drug development has been carried out with diverse strategies. In the past several decades a variety of new methodology have been introduced in R&D. Random screening of accumulated synthetic samples which had been synthesized for development of other drugs led to the discovery of new drugs. The typical examples are anti-asthma drug trimethoquinol and calcium antagonist diltiazem. (herbesser). In particular the latter drug has been used as a calcium antagonist worldwide, however it was first synthesized to find new tranquilizer and this is the reason why diltiazem has benzodiazepam skeleton. The random screening contributed in the finding of new drugs were carried out with whole animal test and it is a standard methodology in R&D of new drugs. Aspirin is the first synthetic non-steroidal antiinflammatory drug(NSAID) and has been used for more than one hundred years. It is the first example of drug developed from natural product. Salicin is the main constituent of willow bark which had been used in Europe for a long time to treat arthritis and aspirin was developed from salicin. Most of NSAID used clinically were developed from the structure of aspirin, however it took 70 years to clarify why aspirin exhibits its antiinflammatory, analgesic and antipyretic activities. The target of aspirin is cyclooxygenase(COX)which is the first enzyme involved in arachidonate cascade leading to the production of prostaglandins(PG) and thromboxan(TX). Side effect of aspirin causing ulcer in stomach is rather serious problem, since aspirin is so popular drug easily obtained in drug store(OTP). This problem is now going to be solved by a new finding on COX, which have two different types, one is constitutionally expressed COX 1 in almost all organs and the other is inducible COX 2. COX 2 is the responsible enzyme in inflammation etc and now the search of COX 2 specific inhibitors is the target of R&D of next generation NSAID.

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한방 변증과 양방 협진에 의한 전신성 홍반성 낭창(Systemic Lupus Erythematosus) 치료 1예 (One Case of Systemic Lupus Erythematosus treated by Integrated Therapy of Western Medicine with Oriental Differential Diagnosis of Symptoms and Signs)

  • 정대영;백동기;황상일;신선호;김동웅;한명아
    • 대한한방내과학회지
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    • 제23권2호
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    • pp.306-312
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    • 2002
  • Systemic Lupus Erythematosus(SLE) is a autoimmune disease characterized by combined symtoms of malar rash, discoid rash, neuropsychiatric disorder, renal disorder, hematologic disorder, photosensitivity immunologic disorder, oral ulcer, anti-nuclear antibody, arthritis, pleuritis and pericarditis, etc. Multiple genetic or environmental causes are supposed to facilitate antiboby production to autoantigen such as ds-DNA, histone, phospholipid, red blood cell, platelet, etc. And defective complementary system fail to remove autoantigen-antibody complex, which deposit in multiple organs and result in inflammatory damages. SLE does not correctly correspond to any specific category of oriental medicine. But, accoring to previous reports, it can be controlled by herb medications used differently patients-to-patients. So we are to report this one SLE case being successfully controlled by classic corticosteroids with herb medications based on oriental diffrential diagnosis of symptoms and signs.

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에탄올-유발 위점막손상에 대한 애엽추출물 (DA-9601)의 방어효과 및 기전에 관한 연구 (Studies on Protective Effect of DA-9601\ulcorner an Artimisiae Herba Extract, against Ethanol-induced Gastric Mucosal Damage and its Mechanism)

  • 오태영;안병옥;고준일;류병권;손미원;김순희;김원배;이은방
    • Biomolecules & Therapeutics
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    • 제5권2호
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    • pp.202-210
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    • 1997
  • Protective effect of DA-9601, an extract of Artemisia Herb, against ethanol-induced gastric mucosal injury was evaluated in rats. In the prophylactic study, DA-9601 exhibited total protection (99.4%) against absolute ethanol-induced gastropathy, And the protective effect of DA-9601 lasted up to 2 hours, which was longer than those of other contemporary mucoprotectants. In the treatment study, DA-9601 significantly facilitated the healing of 70% ethanol-induced mucosal damage, which was superior to cetraxate, a commonly used anti-ulcer drug. The mechanisms of mucoprotection of DA-9601 were also assessed. DA-9601 increased the release of prostaglandin E$_2$ from murine neutrophils in a dose-dependent manner in vitro. The cytoprotective effect of DA-9601 against ethanol-induced mucosal damage was significantly diminished by the concommitant injection of N$\omega$-nitro-L-arginine methyl ester (L-NAME, 5 mg/kg, i.v.), a non-specific nitric oxide (NO) synthase inhibitor, while it was not affected by preinjection of indomethacin (5 mg/kg, s.c.), a prostaglandins-depletor. And it was found that DA-9601 significantly enhanced adaptive cytoprotective action of 10% ethanol against absolute ethanol (56.9$\pm$6.5 vs 23.0$\pm$3.3 mm$^2$, p<0.05, mean$\pm$SEM), though its exact underlying mechanism remains to be clarified. The present fin[lings demonstrate that DA-9601 exerts gastroprotecticv actions for the stomach against ethanol through several different underlying mechanisms, in which prostanglandins and NO are involved. In conclusion, the results obtained suggest that DA-9601 can be useful both in prevention and treatment of ethanol-induced gastric damage.

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정기천향탕(正氣天香湯) 및 가미정기천향탕(加味正氣天香湯)의 효능(效能)에 대한 실험적(實驗的) 연구(硏究) (Experimental Study on the Effect of Jeongkicheonhyangtang and Kamijeongkicheonhyangtang)

  • 박찬기;권정남;김형균
    • 한국한의학연구원논문집
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    • 제3권1호
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    • pp.241-260
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    • 1997
  • Effect of Jeongkicheonhyangtang and Kamijeongkicheonhyangtang have been experimentally studied. The results have been obtained as follows : 1. It is proved that analgecic effect on sample I group and sample II group are clearly decreased than control group. Thus, the statistically significant decrease is p<0.005. 2. It is proved that anti-inflammatory effect on sample I group and sample II group are decreased compare to control group. Thus, the statistically significant decrease of sample I group is p<0.05 in 30 and 60-minute, p<0.01 in 90-minute, and p<0.005 in 120 and 180-minute. And those of sample ll group is p<0.05 in 30 and 60-minute and p<0.005 in 90, 120 and 180-minute. 3. It is proved that appearance of gastric ulcer is decreased compare to the control group and the statistically significant decrease is p<0.05. 4. It is proved that plasma epinephrine contents of sample I and II group are clearly decreased compare to the Control Group and the statistically significant decrease is p<0.005. 5. It is proved that plasma norepinephrine contents of sample I group is drastically decreased compare to the control group and the statistically significant decrease is p<0.005. 6. It is proved that plasma dopamine contents of sample I and II group are decreased than the contort group and statistically significant decrease of the sample I group is p<0.005, and those of the sample II group is p<0.05. As the above mentioned results of experiment, It is belived that Jeongklcheonhyang and Kamijeongkicheonhyang have effect for stress.

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흉선암종과 동반된 전신홍반루푸스의 1예 (A Case of Concurrent Thymic Carcinoma with Systemic Lupus Erythematosus)

  • 이영주;최상태;김세현;정경수;윤설희;정수진;이승우;김주항
    • Tuberculosis and Respiratory Diseases
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    • 제62권1호
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    • pp.67-70
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    • 2007
  • 흉선암종은 드문 종격동의 악성 종양으로서 흉선상피세포에서 기원하지만 흉선종과는 조직학적 특징이 다르다. 흉선종이 자가면역질환을 종종 동반하는데 반해 흉선암종에서 자가면역질환이 동반되는 예는 드물다. 국내에서는 흉선암종과 자가면역질환이 동반된 예가 보고된 적이 없는데 저자들은 전신 근육통을 주소로 내원한 49세 남자 환자가 전신홍반루프스와 흉선암종을 동시에 진단받고 항암치료를 시작한 1예를 경험하였기에 문헌 고찰과 함께 보고하는 바이다.

Toxicological Evaluation of Phytochemical Characterized Aqueous Extract of Wild Dried Lentinus squarrosulus (Mont.) Mushroom in Rats

  • Ugbogu, Eziuche Amadike;Akubugwo, Iroha Emmanuel;Ude, Victor Chibueze;Gilbert, James;Ekeanyanwu, Blessing
    • Toxicological Research
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    • 제35권2호
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    • pp.181-190
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    • 2019
  • Lentinus squarrosulus (Mont.) is an edible wild mushroom with tough fruiting body that belongs to the family Polyporaceae. It is used in ethnomedicine for the treatment of ulcer, anaemia, cough and fever. Recent studies have demonstrated its anticancer, anti-diabetic and antioxidant properties. However, little or no information is available regarding the bioactive components and toxicological study of wild dried L. squarrosulus. Therefore, this study investigated the bioactive components of aqueous extract of boiled wild dried L. squarrosulus and its toxicological effects in rats. The extract of L. squarrosulus was subjected to GC-MS analysis. The acute toxicity test was performed by oral administration of a single dose of up to 5,000 mg/kg extract of L. squarrosulus. In subacute study, the rats were orally administered extract of L. squarrosulus at the doses of 500, 1,000 and 1,500 mg/kg body weight daily for 14 days. The haematological, lipid profile, liver and kidney function parameters were determined and the histopathology of the liver and kidney were examined. The GC-MS analysis revealed the presence of bioactive compounds; 1-tetradecene, fumaric acid, monochloride, 6-ethyloct-3-yl ester, 9-eicosene, phytol, octahydropyrrolo[1,2-a]pyrazine and 3-trifluoroacetoxypentadecane. In acute toxicity study, neither death nor toxicity sign was recorded. In the sub-acute toxicity study, significant differences (p < 0.05) were observed on creatinine, aspartate aminotransferase, alanine aminotransferase, total cholesterol, triglycerides and high-density lipoprotein cholesterol. Whilst no significant differences (p > 0.05) were observed on packed cell volume, heamoglobin, red blood cell, white blood cell and alkaline phosphatase, in all the tested doses. No histopathological alterations were recorded. Our findings revealed that aqueous extract of L. squarrosulus may have antimicrobial, antinocieptive and antioxidant properties based on the result of GC-MS analysis. Results of the toxicity test showed no deleterious effect at the tested doses, suggesting that L. squarrosulus is safe for consumption at the tested doses.

식욕부진을 주소로 내원한 노인 환자 증례 2례 - 복약력 확인 및 감염 관리의 중요성 (Two Case Reports of Elderly Patients with Anorexia: the Importance of Confirming Medication and a Potential Infectious Disease)

  • 주성희;안소연;허소영;장은경;김영철;이장훈
    • 대한한방내과학회지
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    • 제40권3호
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    • pp.491-498
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    • 2019
  • Objectives: This study aimed to put clinical emphasis on the importance of considering medical precautions, such as drug history and a possible infection, when treating elderly patients. Methods: We closely observed two elderly female patients aged 79 and 76 who had been hospitalized for the treatment of anorexia at the Department of Hepato-Hemopoietic System, Kyung Hee University Korean Medicine Hospital in April 2018 for 5 and 9 days, respectively. Results: Through an elaborate medical investigation including a detailed inquiry and laboratory examinations, modifying some drugs and treating a urinary tract infection were preferentially needed to treat these two patients. In the first case, her overall symptoms, including anorexia, were improved after taking Dansambohyeol-tang combined with three types of antacids adjusted by holding 10 drugs in total, including nonsteroidal anti-inflammatory drugs that mainly causing chronic gastric ulcer. In the second case, the urinary tract infection was detected by blood test and urine analysis during the hospitalization period. After taking Geummogpaljeong-san and antibiotics for the treatment of the infection, the chief complaints including anorexia and the negative reaction to nitrite in the urinary analysis were improved. Conclusion: Considering the clinical precautions, including medications and infection possibility, is important especially when treating elderly patients.

건강보험 급여 한약제제와 양방 처방의약품의 병용투여 현황 (Concurrent Use of Korean Herbal Medicines and Western Chemical Medicines: Evidence from HIRA-NPS)

  • 이혜재;윤난희;박소현;신승원;박민정
    • 대한예방한의학회지
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    • 제25권2호
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    • pp.1-11
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    • 2021
  • Objective : The purpose of this study is to analyze Korean patients' characteristics, who were concurrently treated with both Korean herbal medicines and Western chemical medicines using nation-wide database. Method : Using the patients sample data (HIRA-NPS 2018) provided by Health Insurance Review and Assessment Service, a group of patients who co-administered Korean herbal and Western medicines was selected, and their basic characteristics, diagnosis, and prescribed chemical medicines were analyzed. Results : Out of the 1,481,921 sample population, 17,629 patients (1.2%) were selected as a concurrent medication group. Compared to the whole sample, the concurrent medication group was composed of more women (65.8% vs. 51.1%), the more elderly people (65 or older years old) (44.5% vs. 14.6%), and the higher prevalence of chronic diseases (49.1% vs. 22.2%). The most frequent diagnosis treated with Western medicines was mental and behavioral disorders, musculoskeletal and circulatory disorders. Frequently used drugs among concurrent medication group were anti-anxiety drugs, gastric ulcer treatment drugs, and senile diseases treatment drugs. Conclusion : The evidence reported in this study is expected to provide herb-drug interaction researchers with important reference to set the priorities of research topics in the future.

Reduced risk of gastrointestinal bleeding associated with eupatilin in aspirin plus acid suppressant users: nationwide population-based study

  • Hyun Seok Lee;Ji Hyung Nam;Dong Jun Oh;Yeo Rae Moon;Yun Jeong Lim
    • The Korean journal of internal medicine
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    • 제39권2호
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    • pp.261-271
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    • 2024
  • Background/Aims: Mucoprotective agents, such as eupatilin, are often prescribed to prevent gastrointestinal (GI) bleeding in addition to an acid suppressant despite the absence of a large-scale study. We evaluated the additional effect of eupatilin on the prevention of GI bleeding in both the upper and lower GI tract in concomitant aspirin and acid suppressant users using the nationwide database of national claims data from the Korean National Health Insurance Service (NHIS). Methods: An aspirin cohort was constructed using the NHIS claims data from 2013 to 2020. Patients who manifested with hematemesis, melena, or hematochezia were considered to have GI bleeding. A Cox proportional hazards regression model was used to determine the risk factors for GI bleeding associated with the concomitant use of GI drugs and other covariates among aspirin users. Results: Overall, a total of 432,208 aspirin users were included. The concurrent use of an acid suppressant and eupatilin (hazard ratio [HR] = 0.85, p = 0.016, vs. acid suppressant only) was a statistically significant preventive factor for GI bleeding. Moreover, a more than 3-month duration (HR = 0.88, p = 0.030) of acid suppressant and eupatilin prescription (vs. acid suppressant only) was a statistically significant preventive factor for GI bleeding. Conclusions: Eupatilin administration for ≥ 3 months showed additional preventive effect on GI bleeding in concomitant aspirin and acid suppressant users. Thus, cotreatment with eupatilin with a duration of 3 months or longer is recommended for reducing GI bleeding among aspirin plus acid suppressant users.

교맥의 RBL-2H3 비만세포 탈과립과 cytokine 생산 억제 효과 (Inhibitory effect of Fagopyrum esculentum on degranulation and production of cytokine in RBL-2H3 cells)

  • 강경화;이승연
    • 한방안이비인후피부과학회지
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    • 제25권3호
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    • pp.1-12
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    • 2012
  • Objectives : Fagopyrum esculentum(FE) has been used for removal of inflammation of internal organs and treatment of sore and ulcer by heat toxin in Korean herbal medicines. In this study, To investigated the protective effect of FE on allergic response, we determined whether FE inhibits allergic response. Methods : The effect of FE was analyzed by ELISA, RT-PCR and Western blot in RBL-2H3 cells. We investigated cell viability, ${\beta}$-hexosaminidase, as a marker of degranulation, cytokne, and intracellular ROS and MAPK and NF-${\kappa}B$ signaling. Results : We found that FE suppressed ${\beta}$-hexosaminidase release, the production of IL-4 and TNF-${\alpha}$ and intracellular ROS level in RBL-2H3 by the anti-DNP IgE plus DNP-HSA stimulation. FE also significantly inhibited cytokine mRNA expressions, such as IL-$1{\beta}$, IL-2, IL-3, IL-4, IL-5, IL-6, IL-13, TNF-${\alpha}$ and GM-CSF in RBL-2H3. In addition, PF suppressed the phospholyation of ERK1/2, JNK1/2, p38 and $I{\kappa}B{\alpha}$ and NF-${\kappa}B$ signal transduction pathway. Conclusions : Our results indicate that FE protects against allergic response and exerts an anti-inflammatory effect through the inhibition of degranulation and production of cytokines and ROS via the suppression MAPK and NF-${\kappa}B$ of signal transduction. Abbrevations : FE, Fagopyrum esculentum; RBL-2H3, rat basophilic leukemia cell line; ROS, reactive oxygen species; MAPK, Mitogen-activated protein kinase; $NF{\kappa}B$, nuclear factor ${\kappa}B$; $TNF{\alpha}$, Tumor necrosis factor alpha; GM-CSF, Granulocyte macrophage colony-stimulating factor; ERK, extracellular-signal-regulated kinase; JNK, c-Jun NH2-terminal kinase; p38, p38 MAP kinase; $I{\kappa}B{\alpha}$, inhibitory-kappa B alpha.