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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 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.
김정훈(Jung Hoon Kim),오태영(Tae Young Oh),배은주(Eun Ju Bae),손문호(Moon Ho Son),김순회(Soon Hoe Kim),김원배(Won Bae Kim) 한국응용약물학회 1999 Biomolecules & Therapeutics(구 응용약물학회지) Vol.7 No.3
DA-7101 is a new combined formulation of cefatrizine:clavulanic acid (2:1) under development as oral abtibiotics. The general pharmacological properties of DA-7101 on central nervous, cardiovascular, gastrointestinal and other organ systems were studied by oral administration, in vivo and in vitro. DA-7101 had no marked effects all tests studied such as general behavior, hexobarbital-induced sleeping, spontaneous activity, anticonvulsion, body temperature, acetic acid-induced writhing, rotarod performance, heart rate and blood pressure in cats, isolated ileum movement, intestinal transition, gastric juice secretion and urine volume and elctrolytes in rats. But exceptionally at the highest dose of 900 mg/kg, DA-7101 increased hexobarbital-induced sleeping time, caused a slight hypotension and decreased the secretion of gastric juice. These results suggest that at the estimated clinical dose DA-7101 would not bring about any serious acute adverse effects clinically.
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.
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.
에탄올 - 유발 위점막손상에 대한 애엽추출물 (DA-9601) 의 방어효과 및 기전에 관한 연구
안병옥(Byoung Ok Ahn),김원배(Won Bae Kim),김순회(Soon Hoe Kim),이은방(Eun Bang Lee),오태영(Tae Young Oh),류병권(Byung Kweon Ryu),고준일(Jun Il Ko),손미원(Mi Won Son) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.2
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. DA9601 increased the release of prostaglandin E₂ 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_w-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±6.5 vs 23.0±3.3 mm², p<0.05, mean±SEM), though its exact underlying mechanism remains to be clarified. The present findings demonstrate that DA-9601 exerts gastroprotective 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.
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.
고석태(Suk Tai Ko),유강준(Kang Jun Yu),김순회(Soon Hoe Kim),이은방(Eun Bang Lee),천선아(Seon Ah Cheon),신동숙(Dong Sook Shin),이은심(Eun Shim Lee),김옥경(Ok Kyung Kim),강선영(Seon Young Kang),손문호(Moon Ho Sohn) 한국응용약물학회 1996 Biomolecules & Therapeutics(구 응용약물학회지) Vol.4 No.2
The general pharmacological properties of Artemisia extract powder (DA-9601) produced from Artemisia asiatica leaves were investigated in mice, rats, guinea pigs and rabbits. DA-9601 at the dose of 800 ㎎/㎏ po had no influences on general behaviour, barbital sleeping time and motor coordination of mice. The material at the oral dose of 800 ㎎/㎏ did exhibit neither analgesic action nor hypothermic effect. Anticonvulsant action, muscle relaxant action and the effect on intestinal propulsion were not identified at 800 ㎎/㎏ po. In the isolated ileum and trachea of guinea pig, the material did not show direct effect and inhibitory action of chemically or electrically stimulated contraction at the concentration of 2 x 10^(-5) g/㎖ The sinus rates of atria and contractility of papillary muscle of guinea pig were not influenced by DA-9601 at a dose of 2 x 10^(-5) g/ml. No influences on blood pressure and respiration were observed at 40 ㎎/㎏ iv, in rabbits. However, transient decreases in blood pressure of rabbits were observed as given 120 ㎎/㎏ in iv route with slight respiratory depression, and slight diuretic effect could be found without any changes in Na^+ and K^+ excretion.
새로운 캅사이신 유도체 DA-5018 의 진통활성 기전연구 Opiate 수용체 및 Prostanoid 와의 상관성
손미원(Mi Won Son),손문호(Moon Ho Son),배은주(Eun Ju Bae),김순회(Soon Hoe Kim),김원배(Won Bae Kim),양중익(Junn Ick Yang) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.1
DA-5018, a new capsaicin derivative, showed potent analgesic effect comparable to that of morphine in various experimental acute pain models. In this study, whether the analgesic mechanism of DA-5018 is related to opiate receptors or prostanoids was investigated. The affinity of DA-5018 for opiate receptor was determined by receptor binding assay. The Ki values of DA-5018 for nonspecific and specific μ, k, δ-opiate receptor was 299±8.88, 735±215, 2930±163, 1550±813 nM, respectively and DA-5018 exhibited lower affinity than morphine. DA-5018 (10^(-9)∼3 x 10^(-5) M) inhibited electrically-evoked contractions of the guinea pig ileum and rat vas deferens, and these inhibition was not antagonized by naloxone(10 nM), an opiate receptor antagonist. Antagonism of analgesic effect of DA-5018 by naloxone was examined by tail pinch test. Analgesic action of DA-5018(0.1∼2 mg/kg, s.c.) was not antagonized by naloxone(1 mg/㎍, i.p.). These results indicate that pharmacological action of DA-5018 is not related with opiate receptor. Cyclooxygenase and 5-lipoxygenase activities in rat peritoneal neutrophil treated with A23187 and arachidonic acid were measured by radioimmunoassay. DA-5018 stimulated the cyclooxygenase activity and the concentration showing the two fold increase of activity was 124 μM. DA-5018 slightly inhibited 5-lipoxygenase activity and these results together indicate that analgesic action of DA-5018 is not mediated through inhibition of cyclooxygenase or lipoxygenase. These results suggest that the analgesic effect of DA-5018 is not due to blocking opiate receptor or to inhibiting the synthesis of prostanoids in the arachidonic acid metabolism pathway.