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2-Acetylaminofluorene의 투여량에 따른 쥐간의 Monooxygenase에 관한 쇠기름 및 콩기름의 영향
김현덕,김현아,한성림,김경민,장경자,최혜미,Kim, Hyeon-Duck,Kim, Hyeon-A,Han, Sung-Nim,Kim, Kyung-Min,Jang, Kyung-Ja,Choi, Hay-Mie 생화학분자생물학회 1993 한국생화학회지 Vol.26 No.1
이유된 Sprague Dawley종 숫쥐를 식이 지방의 종류에 따라 쇠기름군과 콩기름군으로 나누고, 식이지방은 실험식이의 15% 수준으로 하여 8주 동안 사육하였으며 9주째 체중 kg당 25mg과 100mg의 2-AAF를 각각 3일간 연속 복강주사로 투여하고 다음날 희생시켰다. 간 microsome으로부터 cytochrome P-450, cytochrome bs 함량, NADPH-cytochrome P-450 reductase 활성도, lipid peroxide 함량을 측정 비교하였다. 25mg AAF를 투여했을 때 cytochrome P-450 lipid peroxide 함량은 콩기름군이 쇠기름군보다 유의적 (p<0.05)으로 높았고, 100mg AAF를 투여 했을 때는 cytochrome P-450 함량은 감소했지만 cytochrome $b_5$ 함량은 증가하였다. NADPH-cytochrome P-450 reductase 활성도는 식이지방의 종류에 따라서는 차이가 없었으나 두 식이군 모두 2-AAF 투여량이 증가함에 따라 상승되었다. 이 결과로부터 식이지방의 불포화도가 높을수록 cytochrome P-450의 유도도 뿐아니라 100mg 2-AAF에 의한 손상도 촉진되는 것으로 보여지며, 지질과산화물과는 크게 연관성을 나타내지 않았다. Weanling Sprague Dawley male rats were fed the diet containing 15% beef tallow and soybean oil for 8 weeks. At 9th week, 2-AAF was injected everyday for 3 days by intraperitoneally at the levels of 25 mg and 100 mg/㎏ body weight and sacrificed next day. Cytochrome P-450 and cytochrome $b_5$ contents, NADPH-cytochrome P-450 reductase activity, lipid peroxide values were determined from isolated microsome. Cytochrome P-450 contents and lipid peroxide values were significantly higher in soybean oil group than beef tallow group by 25 mg 2-AAF injection, and cytochrome P-450 contents decreased but cytochrome $b_5$ contents increased in soybean oil group by 100 mg 2-AAF injection. NADPH-cytochrome P-450 reductase activities were not significantly different between dietary groups, but were elevated by 2-AAF injection and positively correlated to the levels of 2-AAF in each dietary group. These results suggest that soybean oil is more susceptible to the damage as well as induction of cytochrome P-450 by 2-AAF, and that lipid peroxide is not positively correlated to the cytochrome P-450 contents.
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2 - Acetylaminofluorene 의 투여량에 따른 쥐간의 Monooxygenase 에 관한 쇠기름 및 콩기름의 영향
김현덕,김현아,한성림,김경민,장경자,최혜미 ( Hyeon Duck Kim,Hyeon A Kim,Sung Nim Han,Kyung Min Kim,Kyung Ja Jang,Hay Mie Choi ) 생화학분자생물학회 1993 BMB Reports Vol.26 No.1
Weanling Sprague Dawley male rats were fed the diet containing 15% beef tallow and soybean oil for 8 weeks. At 9th week, 2-AAF was injected everyday for 3 days by intraperitoneally at the levels of 25 ㎎ and 100 ㎎/㎏ body weight and sacrificed next day. Cytochrome P-450 and cytochrome b_5 contents, NADPH-cytochrome P-450 reductase activity, lipid peroxide values were determined from isolated microsome. Cytochrome P-450 contents and lipid peroxide values were significantly higher in soybean oil group than beef tallow group by 25 ㎎ 2-AAF injection, and cytochrome P-450 contents decreased but cytochrome b_5 contents increased in soybean oil group by 100 ㎎ 2-AAF injection. NADPH-cytochrome P-450 reductase activities were not significantly different between dietary groups, but were elevated by 2-AAF injection and positively correlated to the levels of 2-AAF in each dietary group. These results suggest that soybean oil is more susceptible to the damage as well as induction of cytochrome P-450 by 2-AAF, and that lipid peroxide is not positively correlated to the cytochrome P-450 contents.
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Efficient synthesis of mibefradil analogues: an insight into <i>in vitro</i> stability
Lee, Ji Eun,Kwon, Tae Hui,Gu, Su Jin,Lee, Duck-Hyung,Kim, B. Moon,Lee, Jae Yeol,Lee, Jae Kyun,Seo, Seon Hee,Pae, Ae Nim,Keum, Gyochang,Cho, Yong Seo,Min, Sun-Joon The Royal Society of Chemistry 2014 Organic & Biomolecular Chemistry Vol.12 No.30
<P>This article describes the synthesis and biological evaluation of a chemical library of mibefradil analogues to investigate the effect of structural modification on <I>in vitro</I> stability. The construction of the dihydrobenzopyran structure in mibefradil derivatives <B>2</B> was achieved through two efficient approaches based on a diastereoselective intermolecular Reformatsky reaction and an intramolecular carbonyl–ene cyclization. In particular, the second strategy through the intramolecular carbonyl–ene reaction led to the formation of a key intermediate <B>3</B> in a short and highly stereoselective way, which has allowed for practical and convenient preparation of analogues <B>2</B>. Using this protocol, we could obtain 22 new mibefradil analogues <B>2</B>, which were biologically tested for <I>in vitro</I> efficacies against T-type calcium channels and metabolic stabilities. Among the synthesized compounds, we found that analogue <B>2aa</B> containing a dihydrobenzopyran ring and a secondary amine linker showed high % remaining activities of the tested CYP enzymes retaining the excellent T-type calcium channel blocking activity. These findings indicated that the structural modification of <B>1</B> was effective for improving <I>in vitro</I> stability, <I>i.e.</I>, reducing CYP inhibition and metabolic degradation.</P> <P>Graphic Abstract</P><P>New mibefradil analogues were synthesized by a diastereoselective intramolecular carbonyl–ene reaction as a key transformation. The structural modification of mibefradil significantly reduced CYP inhibition and microsomal degradation. <IMG SRC='http://pubs.rsc.org/services/images/RSCpubs.ePlatform.Service.FreeContent.ImageService.svc/ImageService/image/GA?id=c4ob00504j'> </P>
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가미귀비탕(加味歸脾湯)이 백서(白鼠)의 배란(排卵)에 미치는 영향(影響)
최창민,홍기철,김덕님,김송백,유심근,Choe Chang-Min,Hong Gi-Chul,Kim Duck-Nim,Kim Song-Baeg,Yoo Sim-Keun 대한한의학방제학회 2003 大韓韓醫學方劑學會誌 Vol.11 No.2
Gamiguibitang(GMGBT) is used in amenorrhea and female infertility caused by ovulation disorder. An attempt was made to evaluate the influences of GMGBT on the serum concentrations of FSH, LH, estradiol(E2) and progesterone, the histological and optical changes of ovary of rats. The results of the study were as follows: 1. Blood FSH level significantly increased in experimental group controlled by four times quantity as compared with control group. 2. Blood LH level increased in experimental group controlled by four times quantity as compared with control group, which showed no efficacy. 3. Blood E2 level increased in experimental group controlled by four times quantity as compared with control group, which showed no efficacy. 4. Blood progesterone level significantly decreased in experimental group controlled by double quantity as compared with control group. 5. In optically observations of ovary, weight of ovary significantly increased in experimental group controlled by double quantity as compared with control group 6. In histological observations of ovary, ovulation significantly increased in experimental group controlled by both double and four times quantity as compared with control group. According to these results, it can be concluded that GMGBT influences the pituitary gland and ovary to increase the ovulation of rats.
ScienceON
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