• 제목/요약/키워드: Drug lead

검색결과 354건 처리시간 0.028초

Chiral Relevance of Stereoselective Disposition of Proton Pump Inhibitors: Comparision of Lansoprasole to Omeprazole and Pantoprazole

  • Shin, Jae-Gook
    • 대한약학회:학술대회논문집
    • /
    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
    • /
    • pp.169-170
    • /
    • 2002
  • It has been well known for the stereoselectivity in pharmacodynamic effects of many xenobiotics including therapeutic agents, which have lead to the development of enantiomer drugs. Compared to pharmacodynamic stereoselectivity, stereoselective pharmacokinetics of each enantiomer has not been seriously considered in the development of enantiomer drugs although many reports have been demonstrated the stereoselective absorption and metabolism of racemic drug (e.g verapamil). (omitted)

  • PDF

Synthetic Lead Compounds Modulate Activity of Large-conductance $Ca^{2+}$-activated Potassium Channels Expressed in Xenopus Oocytes

  • Ha, Tal-Soo;Kim, Yong-Chul;Park, Chul-Seung
    • 한국생물물리학회:학술대회논문집
    • /
    • 한국생물물리학회 2003년도 정기총회 및 학술발표회
    • /
    • pp.42-42
    • /
    • 2003
  • Large-conductance $Ca^{2+}$-activated potassium channels ($BK_{Ca}$ are a widely distributed and play key roles in various cell functions. In nerve cells, $BK_{Ca}$ channels shorten the duration of action potentials and block $Ca^{2+}$ entry thereby repolarizing excitable cells after excitation. $BK_{Ca}$ channel opening has been postulated to confer neuroprotection during stroke, and has attracted attention as a means for therapeutic intervention in asthma, hypertension, convulsions, and traumatic brain injury. Several natural and synthetic compounds including a steroid hormone, $\beta$-estradiol, have been identified as the activators of $BK_{Ca}$ channels. Based on the structural features of the previously reported activators of $BK_{Ca}$ channels, we designed several lead compounds, synthesized chemically, and tested their functional activity on cloned $BK_{Ca}$ channels. The $\alpha$ subunit of rat $BK_{Ca}$ channel was expressed alone or with different $\beta$ subunits in Xenopus oocytes and the effects of the compounds were tested electrophysiological means. One of the lead compounds affected the activity of the $\alpha$ subunit of $BK_{Ca}$ channel in a $\beta$ subunit-specific manner. While the activity of B $K_{ca}$ channel $\alpha$ subunit was Potentiated, the channel composed of $\alpha$ and $\beta$1 subunits were inhibited by this compound. We are currently investigating the mechanism of the $\beta$ subunit-dependent effects and planning to localize the receptor site of the lead compound.f the lead compound.

  • PDF

식품용 폴리카보네이트 기구류 중 ICP-MS를 이용한 중금속 이행량 조사 (A Study on the Migration of Heavy Metals from Polycarbonate Food Contact Materials Using an Inductively Coupled Plasma Mass Spectrometry (ICP-MS))

  • 박세종;박소라;김미경;최재천
    • 한국포장학회지
    • /
    • 제24권3호
    • /
    • pp.107-112
    • /
    • 2018
  • 납, 카드뮴 및 비소의 폴리카보네이트 기구류에서 식품으로의 이행 수준을 ICP-MS로 조사하였다. 분석법을 확립 및 검증(검량선, 검출한계, 정량한계, 회수율, 정밀성 및 측정불확도)하고 식품모사용매(4% 초산)로 용출시켜 이행량을 분석하였다. 폴리카보네이트 재질 기구인 컵 63종, 용기 62종, 물병 55종, 스푼 9종, 국자 6종 및 집게 5종으로 총 200종의 시료를 $70^{\circ}C$$100^{\circ}C$에서 30분간 용출한 결과, 납, 카드뮴 및 비소가 각각 $ND{\sim}4.67{\mu}g/L$, $ND{\sim}0.49{\mu}g/L$$ND{\sim}2.91{\mu}g/L$수준으로 용출되었다. 또한, 온도에 따른 이행량 차이를 관찰한 결과, $70^{\circ}C$보다는 $100^{\circ}C$에서 용출되는 이행량이 다소 높았다. 결론적으로 현재 국내에 유통 중인 폴리카보네이트 기구류 중 납, 카드뮴 및 비소는 식품용 기구 및 용기 포장 공전에 명시된 용출규격 이하로서 안전하게 관리되고 있는 것으로 판단되었다.

위해평가 및 모니터링 수행을 위한 표본크기 추정연구: 식품 중 중금속 모니터링 데이터를 중심으로 (Sample Size Estimation for Risk Assessment and Monitoring Based on Heavy Metal Monitoring Data from Food Items)

  • 강희승;고아라;정다현;하미라;황명실;홍진환;황인균;윤혜정
    • 한국식품위생안전성학회지
    • /
    • 제30권2호
    • /
    • pp.127-131
    • /
    • 2015
  • 본 연구에서는 기존에 수행된 식품 중금속 모니터링 데이터를 이용하여 위해평가 및 모니터링을 수행할 때 요구되는 표본 수를 추정하고자 하였다. 중금속 3종 (카드뮴, 납 및 수은)과 17개의 식품을 대상으로 2,400개의 모니터링 데이터를 선정하여 연구에 활용하였다. 기존의 연구에서 수행된 모니터링 데이터의 표준편차와 오차범위 및 신뢰구간 값(95, 99% CI)을 활용하여 표본 수 추정공식에 따라 계산하였다. 표본 수 추정 공식에 따라 표본 크기를 추정한 결과, 95% 신뢰구간에서 카드뮴의 경우 계산된 표본의 크기는 최소 8개에서 최대 90개, 납의 경우 최소 7개에서 최대 1,062개, 수은의 경우 최소 11개에서 최대 238개로 각각 추정되었다. 식품 중 중금속 데이터의 표준 편차와 오차범위가 표본 수를 추정하는데 가장 큰 영향을 주는 것으로 나타났다. 본 연구에서는 모니터링 데이터의 특성을 반영하여 표본 크기를 추정하고자 하였으며, 이는 향후 위해평가 및 모니터링 수행 계획을 수립하기 위한 표본 수를 결정하는 기초연구로 활용될 수 있을 것이다.

노인의 건강상태와 복약실태 (A Study on the Status of Health and Medication in the Elderly)

  • 조원순
    • 한국보건간호학회지
    • /
    • 제14권2호
    • /
    • pp.431-445
    • /
    • 2000
  • In general the prevalence of old people is high and frequently have multiple diseases and symtoms requiring treatment. The nature of illness in the elderly has to be faced, and drugs do have an important part in the treatment of that illness. The purpose of this study were to describe health status and medication, and to provide some basic data for elderly's health education, especially for the right medication. Body mass index, self perceived health status, activities of daily living, disease and experience of past operation were surveyed to recognize the 249 elderly's actual health status. The degree of the elderly's understanding the way of medication, experience of side effects, experience of drug combination and incidence of drug adverse reaction along with drug combination were examined for medication. The aged $women(BMI; 10.7\pm13.3\%)$ overweighed the aged $men(BMI; 4.0\pm10.4\%)$. $69.0\%$ of them recognized their health good. Their activities of daily living were diminished following by the age group(p=0.0068) and relationship with self perceived health status were very significant(p=0.0005). They(192 elderly) suffered from multiple disease such as $osteoarthritis(49.5\%)$, $hypertension(32.0\%)$, gastric $disorder(16.1%)$, $diabetes(14.6\%)$, $osteomalacia(10.9\%)$, cardiovascular $disease(9.9\%)$, senile $cataract(5.7\%)$, skin $rash(5.2\%)$, liver $disease(4.2\%)$, kidney $disease(3.6\%)$, spinal cord $problem(3.6\%)$, respiratory $disease(2.1\%)$ $tuberculosis(1.0\%)\;etc(1.0\%).$ $28.3\%$ of them replied that they had an operation for appendictis senile cataract, peptic ulcer, spinal cord problem, pleurisy, hemorrhoid and the rest. Most of $them(87.4\%)$ knew the way very well how to use drugs, and $21.6\%$ of the replied 171 elderly experienced adverse drug reaction. Drug compliance rate were $high(83.6\%)$. In our study 56.9% of the 167 elderly took several medicine together. And $18.9\%$ of the 95 elderly who did drug combination had an experience of drug interaction. One person kept average 5.5 kinds of drugs at home among 243 elderly. They kept $digestives(79.4\%)$, $ointments(68.7\%)$, $vitamins(59.7\%)$, $analgesics(59.7\%)$, cold $medicines(45.3\%)$ antiarthritic $drugs(33.3\%)$, health $foods(27.7\%)$, antihypertensive $drugs(25.1\%)$, anti peptic ulcer $drugs(24.7\%)$, $laxatives(19.8\%)$, $antacids(16.5\%),\;antibiotics(l6.5\%)$, hypoglycemic $agents(10.3\%)$, cardiac $stimulants(7.0\%)$, $diuretics(4.5\%)$, antiarrhythmic $drugs(4.9\%)$, anti anginal $drugs(4.1\%)$, $hypnotics(3.3\%)$, $etc(38.3\%)$. With this result, we ascertain that polypharmacy in the elderly caused by multiple disease is common, which lead to drug interaction. So our task is to educate elderly how to use drugs in order to maximize their efficiency and to minimize their adverse effects.

  • PDF

수산식품 중 말라카이트그린 및 류코말라카이트그린의 분석 (Analysis of malachite green and leuco-malachite green in sea food)

  • 최동미;홍순근;임무혁;정지윤;장문익;박건상;홍무기;우건조
    • 분석과학
    • /
    • 제19권2호
    • /
    • pp.142-148
    • /
    • 2006
  • 고속액체크로마토그라피를 이용하여 어류 중 말라카이트그린 및 류코말라카이트그린의 최적 분석조건을 확립하고 국내유통 수산식품을 분석하였다. 균질화한 시료를 아세토니트릴로 추출하고 디클로로메탄에 분산시켜 농축 후 메탄올에 용해하여 분석하였다. 이동상으로는 아세토니트릴과 아세테이트 완충용액의 혼합용액을 사용하였으며, 검출파장은 620 nm이었다. 류코말라카이트그린을 말라카이트그린과 동시에 분석하기 위하여 산화납(IV) 컬럼을 분석컬럼 뒤에 연결하여 류코말라카이트그린을 말라카이트그린으로 산화하였다. 상관계수($r^2$)는 말라카이트그린이 0.9989, 류코말라카이트그린이 0.9995이었으며, 검출한계는 신호대 잡음비 3 이상에서 말라카이트그린과 류코말라카이트그린의 합으로서 0.005 mg/kg이었다. 회수율은 84~98%(CV는 3~16%)로 만족할 만한 수준이었다. 분석결과 잉어 및 붕어 서료에서 류코말라카이트그린이 검출되었다.

Molecular Mechanism of Dietary Restriction in Neuroprevention and Neurogenesis: Involvement of Neurotrophic Factors

  • Park, Hee-Ra;Park, Mi-Kyung;Kim, Hyung-Sik;Lee, Jae-Won
    • Toxicological Research
    • /
    • 제24권4호
    • /
    • pp.245-251
    • /
    • 2008
  • Dietary restriction (DR) is the most efficacious intervention for retarding the deleterious effects of aging. DR increases longevity, decreases the occurrence and severity of age-related diseases, and retards the physiological decline associated with aging. The beneficial effects of DR have been mostly studied in non-neuronal tissues. However, several studies have showed that DR attenuate neuronal loss after several different insults including exposure to kainate, ischemia, and MPTP. Moreover, administration of the non-metabolizable glucose analog 2-deoxy-D-glucose (2DG) could mimic the neuroprotective effect of DR in rodent, presumably by limiting glucose availability at the cellular level. Based on the studies of chemically induced DR, it has been proposed that the mechanism whereby DR and 2DG protect neurons is largely mediated by stress response proteins such as HSP70 and GRP78 which are increased in neurons of rats and mice fed a DR regimen. In addition, DR, as mild metabolic stress, could lead to the increased activity in neuronal circuits and thus induce expression of neurotrophic factors. Interestingly, such increased neuronal activities also enhance neurogenesis in the brains of adult rodents. In this review, we focus on what is known regarding molecular mechanisms of the protective role of DR in neurodegenerative diseases and aging process. Also, we propose that DR is a mild cellular stress that stimulates production of neurotrophic factors, which are major regulators of neuronal survival, as well as neurogenesis in adult brain.

약물 관련 정보를 이용한 약물 부작용 예측 (Prediction of Drug Side Effects Based on Drug-Related Information)

  • 서수경;이태건;윤영미
    • 한국정보기술학회논문지
    • /
    • 제17권12호
    • /
    • pp.21-28
    • /
    • 2019
  • 약물 부작용이란 질병의 예방, 진단 또는 치료에 사용된 약물로부터 발생한 유해하고 의도하지 않은 현상이다. 이러한 부작용은 환자를 죽음에 이르게 할 수 있으며, 약물 개발 실패의 주요 원인 중 하나이다, 따라서, 다양한 방법들이 부작용을 알아내기 위하여 시도되었다. 본 연구에서는 시스템스 바이올로지 접근법을 기반으로 기존 연구에서 주로 사용되었던 화학적 구조, 생물학적 정보 이외에도 다양한 표현형 정보를 사용하는 것에 주목하였다. 먼저, 5가지 적응증 데이터베이스, 화학적 구조, 타겟 유전자 정보를 수집하고 개별로 유사도를 계산하였다. 테이블은 하나의 약물-부작용에 대하여 앞서 생성된 유사도를 이용하여 생성되었고 다양한 기계학습 기법이 적용되었다. 결과는 AUC(Area Under the ROC Curve)값을 통해 확인하였다. 본 연구의 유의성은 비교 실험을 통하여 확인하였다.

Identification of Selective STAT1 Inhibitors by Computational Approach

  • Veena Jaganivasan;Dona Samuel Karen;Bavya Chandrasekhar
    • 통합자연과학논문집
    • /
    • 제16권3호
    • /
    • pp.81-95
    • /
    • 2023
  • Colorectal cancer is one of the most common types of cancer worldwide, ranking third after lung and breast cancer in terms of global prevalence. With an expected 1.93 million new cases and 935,000 deaths in 2020, it is more prevalent in males than in women. Evidence has shown that during the later stages of colon cancer, STAT1 promotes tumor progression by promoting cell survival and resistance to chemotherapy. Recent studies have shown that inhibiting STAT1 pathway leads to a reduction in tumor cell proliferation and growth, and can also promote apoptosis in colon cancer cells. One of the recent approaches in the field of drug discovery is drug repurposing. In drug repurposing approach we have virtually screened FDA database against STAT1 protein and their interactions have been studied through Molecular docking. Cross docking was performed with the top 10 compounds to be more specific with STAT1 comparing the affinity with STAT2, STAT3, STAT4, STAT5a, STAT5b and STAT6. The drugs that showed higher affinity were subjected to Conceptual - Density functional theory. Besides, the Molecular dynamic simulation was also carried out for the selected leads. We also validated in-vitro against colon cancer cell lines. The results showed mainly Acetyldigitoxin has shown better binding to the target. From this study, we can predict that the drug Acetyldigitoxin has shown noticeable inhibitory efficiency against STAT1, which in turn can also lead to the reduction of tumor cell growth in colon cancer.

해양미생물 추출물의 동종세포반응 (Allogeneic Mixed Lymphocyte Culture) 억제효능 검색 (Screening on Allogeneic Mixed Lymphocyte Culture Inhibitory Activity for the Extracts of Marine-Derived Microorganisms)

  • 윤금자;오근희;이동섭;최홍대;강정숙;손병화
    • 생약학회지
    • /
    • 제42권4호
    • /
    • pp.354-360
    • /
    • 2011
  • In order to screen new allogeneic mixed lymphocyte culture (allo-MLR) inhibitor which is expected to be immunomodulating drug lead, we have investigated allo-MLR inhibitory activity on the marine-derived symbiotic microorganisms (1,895 strains) from the marine algae. The potent inhibitory activities (over 45% inhibition of proliferation at 10 and 2 ${\mu}g/ml$) without cytotoxicity were observed in the extracts of 46 strains. While, the significant stimulating activities (over 100% proliferation at 10 and 2 ${\mu}g/ml$) without cytotoxicity were observed in the extracts of 5 strains. In the second assay using 46 bioactive strains, 14 strains exhibited again significant allo-MLR inhibitory activity. Finally, 11 strains among the 14 strains inhibited proliferation and IFN-${\gamma}$ production of CD4+ T cells during the stimulation with specific antigen in the third assay. On the basis of above results, the marine algae is nice source for isolation of immunomodulating microorganism, and the marine algae-associated microorganism is also nice target for development of the new immunomodulating drug lead.