지원사업
학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
커뮤니티
연구자들이 자신의 연구와 전문성을 널리 알리고, 새로운 협력의 기회를 만들 수 있는 네트워킹 공간이에요.
논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 저널정보
- 대한약학회 Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 제26권 제8호
- 발행연도
- 2003.1
- 수록면
- 631 - 637 (7page)
이용수
초록· 키워드
오류제보하기
Chloroquine has been used for many decades in the prophylaxis and treatment of malaria. It is metabolized in humans through the N-dealkylation pathway, to desethylchloroquine (DCQ) and bisdesethylchloroquine (BDCQ), by cytochrome P450 (CYP). However, until recently, no data are available on the metabolic pathway of chloroquine. Therefore, the metabolic pathway of chloroquine was evaluated using human liver microsomes and cDNA-expressed CYPs. Chloroquine is mainly metabolized to DCQ, and its Eadie-Hofstee plots were biphasic, indicating the involvement of multiple enzymes, with apparent $K_m and V_{max}$ values of 0.21 mM and 1.02 nmol/min/mg protein 3.43 mM and 10.47 nmol/min/mg protein for high and low affinity components, respectively. Of the cDNA-expressing CYPs examined, CYP1A2, 2C8, 2C19, 2D6 and 3A4/5 exhibited significant DCQ formation. A study using chemical inhibitors showed only quercetin (a CYP2C8 inhibitor) and ketoconazole (a CYP3A4/5 inhibitor) inhibited the DCQ formation. In addition, the DCQ formation significantly correlated with the CYP3A4/5-catalyzed midazolam 1-hydroxylation (r=0.868) and CYP2C8-catalyzed paclitaxel 6$\alpha$-hydroxylation (r = 0.900). In conclusion, the results of the present study demonstrated that CYP2C8 and CYP3A4/5 are the major enzymes responsible for the chloroquine N-deethylation to DCQ in human liver microsomes.
목차
등록된 정보가 없습니다.
참고문헌 (0)
참고문헌 신청함께 읽어보면 좋을 논문
논문 유사도에 따라 DBpia 가 추천하는 논문입니다. 함께 보면 좋을 연관 논문을 확인해보세요!
-
한약재의 Cytochrome P450 결합관련 안전성에 관한 연구
대한한방내과학회지
2013 .01
-
Effects of Korean traditional herbal formula for common cold on the activities of human CYP450 isozymes
대한한의학회지
2014 .06
-
Effects of CYP1A2$^*$1C and CYP1A2$^*$1F Genotypes on the Activity and Inducibility of CYP1A2 Determined by Urinary Caffeine Metabolite Ratio in Koreans
Molecular & cellular toxicology
2007 .01
-
CYP2E15B, CYP2E16, CYP2E17B, CYP2E12, and CYP2E13 Allele Frequencies in Iranian Populations
Asian Pacific journal of cancer prevention : APJCP
2012 .01
-
Expression of CYP2A6, CYP2D6 and CYP4A11 Polymorphisms in COS7 Mammalian Cell Line
Toxicological Research
2011 .03
-
Roles of CYP2C9 and its variants (CYP2C9*2 and CYP2C9*3) in the metabolism of 6-methoxy-2-napthylacetic acid, an active metabolite of the prodrug nabumetone
Journal of Pharmaceutical Investigation
2020 .01
-
CYP2E1과 CYP2C19 유전자 다형성이 위암 발생 감수성에 미치는 영향
Annals of Surgical Treatment and Research
2007 .08
-
Simultaneous determination of seven major human cytochrome P450 activities using LC/MS/MS
대한약학회 학술대회
2002 .01
-
암브록솔과 세티리진의 Cytochrome P450 저해 활성 평가
약학회지
2013 .01
-
한국인 정신분열병 환자의 지연성 운동장애와 $CYP2D6^*4$ 및 $CYP2D6^*10$ 다형성들의 연합에 대한 고찰
생물정신의학
2000 .01
-
약물대사효소 CYP2C19, CYP2D6의 다형성과 사상체질의 관련성 연구
대한한의학회지
2007 .03
-
Analysis of CYP17, CYP19 and CYP1A1 Gene Polymorphisms in Iranian Women with Breast Cancer
Asian Pacific journal of cancer prevention : APJCP
2016 .01
-
Relationship between CYP17 and CYP11${\alpha}$, and PCOS in Korean Population
대한생식의학회 학술대회
2003 .01
-
RNA Expression of Cytochrome P450 in Mexican Women with Breast Cancer
Asian Pacific journal of cancer prevention : APJCP
2012 .01
-
Xylene에 의한 CYP2B1/2의 유도와 대사에 있어서 toluene의 영향
한국산업보건학회지
2009 .01
-
Effects of Hydroxyl Group Numbers on the B-Ring of 5,7-Dihydroxyflavones on the Differential Inhibition of Human CYP 1A and CYP1B1 Enzymes
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
2005 .01
-
Association of CYP2C19*2 and *3 Genetic Variants with Essential Hypertension in Koreans
Yonsei Medical Journal
2012 .01
-
In Vitro Metabolism of a New Neuroprotective Agent, KR-31543 in the Human Liver Microsomes : Identification of Human Cytochrome P450
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
2004 .01
-
Preferential Induction of CYP1A1 over CYP1B1 in Human Breast Cancer MCF-7 Cells after Exposure to Berberine
Asian Pacific journal of cancer prevention : APJCP
2014 .01
-
CYP2C19 Polymorphism in Korean Patients on Warfarin Therapy
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
2007 .01
이 논문의 저자 정보
최근 본 자료
댓글(0)
0