Platelet derived growth factor (PDGF)-BB is one of the most potent vascular smooth muscle cell (VSMC) proliferative factors, and abnormal VSMC proliferation by PDGF-BB plays an important role in the development and progression of atherosclerosis. The aim of this study was to assess the effect of YP 12, a newly synthesized obovatol derivative, on the proliferation of PDGF-BB-stimulated rat aortic VSMCs. The anti-proliferative effects of YP 12 on rat aortic VSMCs were examined by direct cell counting and by using [3H] thymidine incorporation assays. It was found that YP 12 potently inhibited the growth of VSMCs. The pre-incubation of YP 12 (1-4 μM)significantly inhibited the proliferation and DNA synthesis of 25 ng/ml PDGF-BB-stimulated rat aortic VSMCs in a concentration-dependent manner. In accordance with these findings, YP 12 revealed blocking of the PDGF-BB-inducible progression through G0/G1 to S phase of the cell cycle in synchronized cells. Whereas, YP 12 did not show any cytotoxicity in rat aortic VSMCs in this experimental condition by WST-1 assay. These results also show that YP 12may have potential as an anti-proliferative agent for the treatment of restenosis and atherosclerosis.

녹차카테킨은 다양한 생리활성을 지닌 것으로 알려지고 있다. 본 실험에서는 사염화탄소와 갈락토사민으로 유발된 간독성에 대한 녹차카테킨의 간기능보호효과가 연구되었다. 녹차카테킨(50 mg/kg와 100 mg/kg)은 사염화탄소(0.5 ml/kg)와 갈락토사민(400 mg/kg)이 투여되기 전 그리고 투여 후 3일동안 흰쥐에 경구투여되었고, 간기능지표로 AST와 ALT를 측정하였다. 녹차카테킨(50 mg/kg)은 사염화탄소 처리된 랫드에서 상승된 혈중 AST와 ALT활성을 전투여군(262±11, 80±19 에서 153±33, 55±25로)과 후투여군(156±40, 105±3에서 106±22, 55±9로)모두 감소시켰다. 또한 갈락토사민으로 유도한 경우에도 AST와 ALT 수치는 전투석군(576±24, 276±68에서 236±13. 115±13로) 후 투여군(233±54, 137±11에서 119±23, 44±17로)에서 모두 유의성있게 감소된 결과를 나타내었다 또한 간 조직학적 검사에서도 사염화탄소와 갈락토사민으로 유도된 간경변을 유의성있게 억제하였다. 이상의 결과로 볼 때 녹차카테킨은 간독성에 의한 병변을 예방 및 치료할 수 있는 신약후보물질로서의 가능성을 시사한다.

The purpose of this study was to elucidate the effects of green tea catechins (GTC) on the lipid peroxidation and superoxide dismutase (SOD). GTC showed the high SOD activity, while significantly inhibited the peroxide value of linoleic acid (93%) and lipid petoacidation (84%) from rat liver microsomal fraction induced by Fe^(2+)/ascorbate system. The effects of GTC on the SOD and catalase activities, and lipid peroxidation after oral administration were investigated. GTC (50 mg/kg) significantly increased SOD (62%) and catalase activities (75%), while significantly inhibited the lipid peroxidation (52%) of rat liver microsome in a dose-dependent manner. These results suggest that GTC has the antioxidative effect which is related to the prevention of aging and cancer.

6-(4-Iodophenyl)amino-7-chloro-5,8-quinolinedione (RCK9) was evaluated for antifungal activities. The MIC values of RCK9 were determined against A. flavus, C. albicans, C. neoformans and F. oxysporium. The RCK9 showed generally potent antifungal activities against the tested fungi. Acute oral toxicity studies of RCK9 were carried out in ICR mice of both sexes. These acute oral toxicities of RCK9 were low and LDSO values were over 2,850 mg/kg in ICR mice. The genotoxicities of RCK9 had been evaluated. RCK9 was negative in Ames test with Salmonella typhimurium and chromosomal aberration test in CHL cells. The clastogenicity was tested on the RCK9 with in vivo mouse micronucleus assay. RCK9 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. The results indicate that RCK9 has no genotoxic potential under these experimental conditions.

6-[(N-3,4-Dibromophenyl)amino]-7-chloro-5,8-quinolinedione(RCK13) was tested for antifungal activities. The MIC values were determined by the two-fold dilution method. The therapeutic potential of RCK13 had been assessed in comparison with ketoconazole and fluconazole against systemic infections with Candida albicans in normal mice. RCK13 had ED_(50), 0.80±0.21 mg/kg but ketoconazole had ED_(50), 8.00±0.73 mg/kg respectively. And administered RCK13 at the ED_(50) for 14 days improved survival rates as well as ketoconazole. Acute oral toaicity studies of RCK13 were carried out in ICR mice of both sexes. These acute oral toxicities of RCK13 were low and LD_(50) values were over 2,850 mg/kg in ICR mice. The genotoxicities of RCK 13 had been evaluated. RCK13 was negative in Ames test with Salmonella ryphimurium and chromosomal aberration test in CHL cells. The clastogenicity was tested on the RCK13 with in vivo mouse micronucleus assay. RCK13 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. These results indicate that RCK13 has no genotoxic potential under these experimental conditions.

The objective of this study is to investigate the direct effects of green tea catechins(GTC) on vascular smooth muscle tension and ^(46)Ca^(2+) uptake in rat aorta. The methods used in this study are isometric tension measurements using physiograph, Lanthanum method for ^(46)Cac^(2+) (2 uCi/ml) uptake measurement in rat aorta. GTC modified tension induced by 40 mM KCl or 1 uM norepinephrine in rat aorta. Low concentrations of GTC($lt;0.5 mg/m increased tension by 40 mM KCl or 1 tM norepinephrine, individually. However, high concentrations of GTC($gt; 0.5 mg/ml) inhibited tension by 40 mM KCl or 1 uM norepinephrine, individually. GTC increased ^(45)Ca uptake induced by 40 mM KCl in a dose-dependent manner. From these results, GTC has the dual actions in vascular smooth muscle in vitro. Low concentrations of GTC augments tension by K or norepinephrine. However, high concentrations of GTC inhibits tension by K or norpeinephrine. GTC may have Ca^(2+) channel activation action, which may result in unphysiological vasodilation by Ca^(2+) overload in vascular smooth muscle.

Green tea catechins(GTC) were studied for its inhibitory effect on human platelet aggregation in vitro, for its antithrombotic effect in mice in vivo, and for bleeding and clotting time in rats. The catechins were isolated and purified from green tea, which were composed of (-)-epigallocatechin gallate, (-)-epigallocatechin, (-)-epicatechin gallate and (-)-epicatechin. GTC produced a potent inhibition of human platelet aggregation in a dose-dependent manner against the stimulants such as ADP, collagen, epinephrine and ristocetin in vitro. GTC also prevented death due to the formation of pulmonary thrombosis by platelet aggregates in mice in a dose-dependent manner in vivo. GTC increased the bleeding time, whole blood clotting time and plasma clotting time in rats, too. These results suggest that GTC is a promising antithrombotic agent.

The genotoxicity of combinations of four p-oxybenzoic acids (methyl paraben, ethyl paraben, isopropyl paraben, butyl paraben) and benzoic acid had been evaluated. The in vitro Ames test using Salmonella typhimurium (TA 98, TA 100, TA 1535, TA 1537) and the in uiuo micronucleus assay using mouse peripheral blood were performed. Methyl paraben plus benzoic acid, ethyl paraben plus benzoic acid, and ethyl paraben plus butyl paraben slightly increased the frequency of micronucleated reticulocytes in the high doses, but were negative in Ames test with Salmonella typhimurzum with and without rat liver microsomal activation. The other combinations tested were negative in Ames test and did not show any clastogenic effect in micronucleus test. These results suggest that genotoxicity can produced by the combinations of p-oxybenzoic acid.

In order to study the effects of Aloe vera Linne treatment on the clinical chemistry in patients with liver disease, seven patients were administered orally with 800-1, 600 mg of Aloe vern Linne four times a day for six months. The high levels of serum AST, ALT, ALP, γ-GTP and total bilirubin in patients were significantly reduced by administration of Aloe vem L.. The reduced serum albumin/globulin value was increased by Aloe vera L. treatment. But other blood parameters of clinical chemistry values were not affected by Aloe very L. treatment. These data suggest that Aloe very L. can be effective in treatment of the patients with liver disease.

In order to study the effects of Aloe vera treatment on blood glucose level and clinical chemistry in diabetic patients, eight diabetic patients were administered orally with 800 mg of Aloe vera three times a day for three months. The high levels of blood and urine glucose in diabetic patients were significantly reduced by administration of Aloe vera. The increased plasma triglyceride concentration was also significantly reduced by Aloe vera treatment. A little amount of urine bilirubin, hematuria, nitrite, urobilinogen, protein and ketone bodies were detected before treatment, but not detected after Aloe vera treatment. But other blood parameters of clinical chemistry values were not affected by Aloe vera treatment. These data suggest that Aloe vera can be effective in the treatment of the diabetic patients,