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유전자 재조합 인형 과립구 콜로니 자극인자 DA-3030 의 일반약리작용
배은주(Eun Ju Bae),신명수(Myeong Soo Shin),김순회(Soon Hoe Kim),강수형(Soo Hyung Kang),김원배(Won Bae Kim),양중익(Jung Ick Yang) 한국응용약물학회 1994 Biomolecules & Therapeutics(구 응용약물학회지) Vol.2 No.3
Neutropenia is a major dose-limiting factor in cancer chemotherapy diminishing its usefulness and increase patient`s susceptibility to infectious disease. Some recombinant human granulocyte colony stimulating factors(rhG-CSFs) are in use to reduce the risk of this serious side effect. In this study, we examined the pharmacological properties of DA-3030, a rhG-CSF expressed in E. coli. DA-3030 100 and 1000 ㎍/㎏, i. v., had no significant effect on the central nervous, gastrointestinal system in mice and cardiovascular system in rabbits, but it slightly inhibited the spontaneous motility of isolated nonpregnant uterus in rats. It also had no influence on excretion of urinary electrolytes. DA-3030 administered for successive 3 days increased the blood WBC count in zymosan air pouch inflammed rats and in normal rats. These results indicate that DA-3030 has little side effects in animals.
새로운 Anthracycline계 항암제 DA-125의 일반약리작용
김명석,박종완,김영훈,김순회,신명수,김원배,양중익,Kim, Myung-Suk,Park, Jong-Wan,Kim, Young-Hoon,Kim, Soon-Hoe,Shin, Myeong-Soo,Kim, Won-Bae,Yang, Junn-Ick 대한약리학회 1994 대한약리학잡지 Vol.30 No.2
The general pharmacological effects of a new anthracycline anticancer agent, DA-125 $[7-0-(2,\;6-dideoxy-2-fluoro-{\alpha}-L-talopyranosyl)-adriamycinone-14-{\beta}-alaninate{\cdot}HCI]$ were investigated in mice, rats, guinea pigs, rabbits and dogs. Intravenous administration of DA-125 presented no significant effects on the central and peripheral nervous systems of ICR mice except a decrease in the numbers of acetic acid-induced writhing response at a dose of 10 mg/kg. In anesthetized rats and dogs, DA-125 produced a transient depression of blood pressure and an increase in heart rate, but did not affect the peripheral blood flow in the isolated ear vessels of rabbits and the mechanical functions of the isolated hearts of guinea pigs. No significant effects were observed on the gastrointestinal functions and the contractilities of smooth muscle preparations obtained from guinea pig trachea, rabbit ileum, pregnant and non-pregnant uterus and vas deferens of rats. DA-125 Increased the contractility of the isolated ileum of guinea pigs in a dose range of $10^{-6}{\sim}10^{-9}g/ml$, and also increased, but weaker than adriamycin, the vascular permeability in rat skin. DA-125 had no effect on the kallikrein-induced increase in permeability and the permeability of the visceral organs. DA-125 did not adversely affect the liver function and the blood coagulation system, and did not induce hemolysis in vitro. It is concluded from the results that the general pharmachological effects of DA-125 are similar to or weaker than those of adriamycin, and that little adverse effects are anticipated with a therapeutic dose range.
새로운 캅사이신유도체 DA-5018 의 피하주사 및 구소도포시 진통효과
김원배(Won Bae Kim),양중익(Junn Ick Yang),배은주(Eun Ju Bae),신명수(Myeong Soo Shin),손문호(Moon Ho Son),김희기(Hee Kee Kim),공재양(Jae Yang Kong) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.2
The analgesic effects of DA-5018, a new capsaicin derivative, were evaluated in various experimental pain models. Drugs were administered subcutaneously or topically. When drugs were administered subcutaneously, 1) the ED_(50) values of DA-5018, morphine ·HCl, capsaicin and acetaminophen were 0.091-2.0, 0.3-4.3, 1.4-26.5 and 45.4-643 mg/kg, respectively in various pain or inflammatory models including acetic acid writhing, formalin, tail flick, Randall-Selitto, hot plate and croton oil-induced ear edema test, 2) the AD₂ values (the dose for doubling of pain threshold of vehicle control) of DA-5018, capsaicin and ketoprofen were 1.07±0.18, 23.47±4.46 and 2.97±0.43 mg/kg in Freund`s complete adjuvant (FCA)-induced arthritic pain model. And by topical application, 1) neither DA-5018 0.3% cream nor Zostrio-HP (capsaicin 0.075%) were effective in formalin test, 2) although DA-5018 0.3% cream significantly inhibited the croton oil-induced ear edema being better than Zostrix-HP and Kenofen (ketoprofen 3%). 3) Ln FCA model, DA-5018 0.3% cream reversed the decreased pain threshold of arthritic rat from 136.4 g (day 0) to 289.0 g (day 5) and 250.1 g (day 10), which was similar to Zostrix-HP, These results suggest that DA-5018 administered subcutaneously has a potent and broad analgesic spectrum than nonsteroidal antiinflammatory drugs against acute and chronic pain, and by topical application it exerts comparable analgesic and antiinffammatory effects to capsaicin cream.
새로운 캅사이신 유도체 DA-5018 의 급성통증 모델에서의 진통작용
김원배(Won Bae Kim),양중익(Junn Ick Yang),배은주(Eun Ju Bae),신명수(Myeong Soo Shin),김순회(Soon Hoe Kim),손문호(Moon Ho Son),김희기(Hee Kee Kim),박노상(No Sang Park) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.1
Analgesic effect of DA-5018, a new capsaicin derivative, was evaluated in various rat models of experimentally induced acute pain. DA-5018(0.2∼10.0 ㎎/㎏, p.o.) prevented the writhing syndromes induced by acetic acid or phenyl-p-benzoquinone(PBQ). It increased the pain threshold of inflamed paw when tested by the Randall-Selitto method at the dose of 2.0∼20.0 ㎎/㎏ by oral administration. And also it showed antinociceptive activities in tail-pinch(1.0∼20.0 ㎎/㎏, p.o.) and tail-flick test(5.0∼50.0 ㎎/㎏, p.o.). The potency and efficacy of DA-5018 were comparable to morphine·HCl in all the models mentioned above. Acetaminophen exhibited the inhibition of acetic acid-induced writhing syndromes and also analgesic activity in Randall-Selitto test, but it showed the limited efficacy in tail-pinch and tail-flick test. These results mean that DA-5018 has a broader analgesic activity profile than acetaminophen. And we found out that the analgesic activity of DA-5018 was 100 times more potent when administered centrally than administered orally in tail-flick test. These results suggest that DA-5018 has an orally active analgesic activity, and central nervous system may be involved in the action of DA-5018.
Recombinant Human Erythropoietin (DA-3285) 의 효력 및 일반약리작용
김동환(Dong Hwan Kim),안병옥(Byoung Ok Ahn),손문호(Moon Ho Son),신명수(Myeong Soo Shin),이성희(Sung Hee Lee),김원배(Won Bae Kim),양중익(Junn Ick Yang) 한국응용약물학회 1996 Biomolecules & Therapeutics(구 응용약물학회지) Vol.4 No.1
Efficacy and general pharmacology of recombinant human erythropoietin (rHu-EPO), were investigated. Efficacy studies were conducted in normal, cisplatin- and acute hemorrhage-induced anemic rats. Normal and anemic animals were treated intravenously with rHu-EPO for 5 days and the changes in the numbers of red blood cells (RBC), hemoglobin (Hb), hematocrit (Hct) and reticulocytes (Ret) were examined. In normal rats, rHu-EPO significantly increased RBC, Hb, Hct and Ret at doses of 50∼1250 IU/㎏/day. Cisplatin-induced anemic rats showed significant increase of RBC, Hb, Hct and Ret in a dose-dependent manner after administration of rHu-EPO (50∼200 IU/㎏/day). And in acute hemorrhage-induced anemic rats, rHu-EPO(4∼100 IU/㎏/day) accelerated recovery of anemia with significant increase in Ret. These changes disappeared gradually after cessation of the treatment. The general pharmacological effects of rHu-EPO were investigated in mice, rats, guinea-pigs, rabbits and cats. rHu-EPO had no influences on central nervous, cardiovascular, gastrointestinal and blood coagulation system. It also had no influence on the contraction of phrenic nerve-diaphragm preparation. rHu-EPO produced significant increase of urine volume at a dose of 7000 IU/㎏. These results suggest that rHu-EPO might be useful for the therapy of anemia without serious side effect.
유지숙 ( Ryu Ji Sook ),한선경 ( Sun Kyung Han ),신명수 ( Myeong Soo Shin ),이완규 ( Wan Kyu Lee ) 한국가축위생학회 2009 韓國家畜衛生學會誌 Vol.32 No.1
In order to develop probiotic strain for pigs, Lactobacillus spp. (527 isolates), Streptococcus spp. (95 isolates) and Bifidobacterium spp. (25 isolates) were isolated from the feces of 35 pigs. These isolates were tested through in vitro experiment such as acid tolerance at pH 2.0 (Lactobacillus spp. and Streptococcus spp.) or pH 3.0 (Bifidobacterium spp.), bile tolerance in MRS broth containing 0.3% (w/v) Oxgall, heat resistance at 70°C and 80°C for 5 min, antibiotic resistance, antimicrobial activity against pathogenic bacteria and Caco-2 cell adherence assay. Finally ten most superior strain (5 Lactobacillus spp. strain, 3 Bifidobacterium spp. strain and 2 Streptococcus spp. strain) were selected as potential candidate for probiotic use in pig industry. It could be used as an alternative to antibiotics in feed additives.
김원배(Won Bae Kim),양중익(Junn Ick Yang),배은주(Eun Ju Bae),신명수(Myeong Soo Shin),김순회(Soon Hoe Kim),손문호(Moon Ho Son),김희기(Hee Kee Kim),차봉진(Bong Jin Cha) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.1
DA-5018(N-(3-(3,4-dimethylphenyl)propyl)-4-(2-aminoethoxy)-3-methoxyphenylacetamide) is a new capsaicin derivative under development as topical analgesic agent. The general pharmacological properties of DA-5018 on central nervous, cardiovascular, gastrointestinal and other organ systems were studied in experimental animals. DA-5018 cream (0.3%) had no effects on behavior, hexobarbital-induced sleeping time, body temperature, spontaneous activity, blood pressure, heart rate, intestinal charcoal propulsion, urine volume and electrolyte excretion even at a high dose of 2000 mg/kg in rats. In addition, DA-5018 cream had little skin irritation compared to Zostrix-HP (capsaicin, 0.075%) cream in rabbits. In isolated guinea pig tissue studies, DA-5018 increased the contractility of trachea and ileum and also increased sinus rate of atrium in a range of 10^(-8)-10^(-5) M, but its efficacy as a agonist was weak. These results suggest that DA-5018 cream might be used topically without serious side effects.
새로운 캅사이신 유도체 DA-5018 의 국소자극성에 관한 연구
김원배(Won Bae Kim),양중익(Junn Ick Yang),배은주(Eun Ju Bae),신명수(Myeong Soo Shin),김순회(Soon Hoe Kim),손문호(Moon Ho Son),김희기(Hee Kee Kim) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.2
Capsaicin cream has been used to attenuate the pain associated with diabetic neuropathy, rheumatoid arthritis, osteoarthritis and postherpetic neuralgia. But its common side effect, local irritation, limits the use of it and there is still a need for a new analgesic devoid of this side effect. This study was conducted to compare the local irritant effect of DA-5018, a new capsaicin derivative, with that of capsaicin in various animal models and human beings. Capsaicin, applied topically to the mouse ear, produced dose-dependent increase of ear volume and the frequency of ear scratching behavior in mice. Neither ear volume nor scratching behavior was affected by DA-5018. In eye wiping test of rat, DA-5018 was 10 times less irritant than capsaicin. Capsaicin administered intradermally into the rat paw elicited paw lick/lift response with a potency which was three times that of DA-5018. Zostrix-HP (0.075% capsaicin cream), but not DA-5018 0.3% cream, increased ear volume of rat and induced thermal hyperalgesia in normal and carrageenan inflamed paws. Six day-treatment of Zostrix-HP failed to develop tolerance against this thermal hyperalgesia. In human beings, Zostrix-HP produced burning sensation and itching in more than 90% of volunteers involved and its maximum irritant effect was significantly higher than that of DA-5018 cream. These results suggest that local irritation and burning sensation produced by DA-5018 is much less than capsaicin.
신명수,조 현,김창종 중앙대학교 약학연구소 1991 약학 논총 Vol.5 No.-
Hypoglycemic activity of fractions and asarones of Bambusae caulis in Taeniam were studied in normal and streptozotocin-induced hyperglycemic mice. The results were as follows : 1. Asarones were a major principle(0.02%) of essential oil from Bambusae caulis in Taeniam. They were consist of β-(59.16%), γ-(26.03%) and α-asarone(14.81%) 2. The hexane, chloroform, ethyl acetate, butanol and water fractions of Bambusae caulis in Taeniam at the oral dose of 100㎎/㎏ decreased significantly the blood glucose, body weight loss and water cosumption in hyperglycemic mice. Their ethyl acetate, butanol and water fractions at th oral dose of 100㎎/㎏ decreased significantly the blood glucose in normal mice. 3. The mixture of asarones from Bambusae caulis in Taeniam at the oral dose of 20㎎/㎏ decreased significantly the blood glucose in normal mice and hyperglycemic mice. Therefore asarones was one of hypoglycemic principles of Bambusae caulis in Taeniam. 4. Bambusae caulis in Taeniam has the hypoglycemic activity because of improving the degenerative change of β-cell in Langerhan's islet by streptozotocin.