• Title/Summary/Keyword: Lead compound

Search Result 345, Processing Time 0.022 seconds

Metabolic Engineering of the Brassinosteroid Biosynthetic Pathways (Brassinosteroid의 대사공학)

  • Lee, Mi-Ock;Song, Ki-Hong;Lee, Hyun-Kyung;Jung, Ji-Yoon;Choe, Vit-Nary;Choe, Sung-Hwa
    • Proceedings of the Korean Society of Plant Biotechnology Conference
    • /
    • 2002.04b
    • /
    • pp.69-75
    • /
    • 2002
  • Sterols play two major roles in plants: a bulk component in biological membranes and precursors of plant steroid hormones. Physiological effects of plant steroids, brassinosteroids (BRs), include cell elongation, cell division, stress tolerance, and senescence acceleration. Arabidopsis mutants that carry genetic defects in BR biosynthesis or its signaling display characteristic phenotypes, such as short robust inflorescences, dark-green round leaves, and sterility. Currently there are more than 100 dwarf mutants representing 7 genetic loci in Arabidopsis. Mutants of 6 loci, dwf1/dim1/cbb1, cpd/dwf3, dwf4, dwf5, det2/dwf6, dwf7 are rescued by exogenous application of BRs, whereas bri1/dwf2 shares phenotypes with the above 6 loci but are resistant to BRs. These suggest that the 6 loci are defective in BR biosynthesis, and the one locus is in BR signaling. Biochemical analyses, such as intermediate feeding tests, examining the levels of endogenous BR, and molecular cloning of the genes revealed that dwf7, dwf5, and dwf1 are defective in the three consecutive steps of sterol biosynthesis, from episterol to campesterol via 5-dehydroepisterol. Similarly, det2/dwf6, dwf4, and cpd/dwf3 were Shown to be blocked in $D^4$ reduction, 22a-hydroxylation, and 23 a-hydroxylation, respectively. A signaling mutant bri1/dwf2 carries mutations in a Leucine-rich repeat receptor kinase. Interestingly, the bri1 mutant was shown to accumulate significant amount of BRs, suggesting that signaling and biosynthesis are dynamically coupled in Arabidopsis. Thus it is likely that transgenic plants over-expressing the rate-limiting step enzyme DWF4 as well as blocking its use by BRI1 could dramatically increase the biosynthetic yield of BRs. When applied industrially, BRs will boost new sector of plant biotechnology because of its potential use as a precursor of human steroid hormones, a novel lead compound for cholesterol-lowering effects, and a various application in plant protection.

  • PDF

ORAL HEMORRHAGE CONTROL AS TREATMENT PRIORITY IN A MENTALLY RETARDED PATIENT WITH MULTIPLE TRAUMA (다발성 손상을 가진 정신지체 환자에서 치료 우선순위로 구강출혈의 조절)

  • Oh, Ji-Hyeon;Kim, Ji-Hun;Yoo, Jae-Ha
    • The Journal of Korea Assosiation for Disability and Oral Health
    • /
    • v.12 no.1
    • /
    • pp.20-26
    • /
    • 2016
  • Sympathetic reaction to grotesque facial injuries with oral bleeding can trigger confusion and generate inefficiency among emergency room personnel. Regardless of the extent of the injury, or of the sympathy elicated, the victim must be evaluated and treated as a whole patient with multiple trauma. There must be no confusion as to order of importance in the steps of evaluation : 1. airway 2. hemorrhage 3. shock 4. associated injuries 5. local injury 6. triage of facial injuries. The most dangerous aspect of oral hemorrhage is the possibility of its obstructing the upper airway. Swallowing large amounts of blood will usually cause gastric irritation and lead to vomiting, thus further complicating the management of the patient. Once a clear airway is assured and hemorrhage have been controlled, consideration is given to possible associated injuries before undertaking treatment of the facial injuries themselves. Status of the cardiopulmonary, gastrointestinal and neuromuscular systems all have a bearing on decisions concerning facial injury treatment. In this light, treatment priority becomes exceeding important. On the other hand, the importance of facial injuries should never be minimized, especially in a mentally retarded patient with oral hemorrhage. This is a case report about oral hemorrhage control as treatment priority in a mentally retarded patient.

Effects of Supplementary Vitamin C and E to Moist Pellet Diet on Growth and Body Composition of Juvenile Olive Flounder, Paralichthys olivaceus (습사료에 비타민 C와 E 첨가가 넙치 치어의 성장과 체성분에 미치는 영향)

  • JEONG Gwan Sik;JI Seung Cheol;AHN Chang Bum;SHIN Tae Sun;YOO Jin Hyong
    • Korean Journal of Fisheries and Aquatic Sciences
    • /
    • v.36 no.2
    • /
    • pp.100-106
    • /
    • 2003
  • This study was conducted to investigate the supplementary effects of vitamin C and E to moist pellet on growth and body composition in juvenile olive flounder (Paralichthys olivaceus). Four groups of diet made : moist pellet (MP) diet group was used as the control group where the ratio of raw feed and commercial compound meal is 5:5 $(CP\;30\%,\;CL\;17\%),$ vitamin C added group (VC), vitamin I added group (VE) and vitamin C and I added group (VCE). The supplementary amount of vitamin C and E corresponded to 1000 mg/kg (dry wt.) and 220mg/kg (dry wt.), respectively. Vitamin C was destroyed $50\%$ and vitamin E was destroyed $20\%$ for manufacturing process. After 8 weeks feeding trial, weight gain was $121.9\%$ in MP group, while it ranged from 180.5 to $184.9\%$ in the VC, VE and VCE group. Feed efficiency was $71.\6%$ in MP group, whereas it ranged from 78.7 to $80.6\%$ in the VC, VE and VCE group, weight gain and feed efficiency of fish fed vitamin supplemented diets were significantly higher than control group and no significant difference among the vitamin added groups was observed (p>0.05). There were no significant differences in moisture, crude protein, crude lipid, crude ash, condition factor (CF), hepatosomatic index (HSI), and visceraweight index (VWI) of body composition. Hemoglobin (Hb) was $3.79\%$ in MP group, whereas $4.99\%$ in VC group, $4.55\%$ in VE group and $5.07\%$ in VCE group; Hb was significantly higher in the vitamin added groups than the control group (p<0.05). Vitamin C retention in liver was 18.1, 20.7, 46.6, 54.0 mg/kg in MP, VE, VC and VCE groups, respectively. Vitamin E retention in liver was 25.9, 53.8, 88.2, 124.5 mg/kg in MP, VC, VE and VCE groups, respectively. These results indicate that supplementation of vitamin C and E to moist pellet diet significantly improved growth and feed efficiency of olive flounder, and the mixed addition of vitamin C (1,000 mg/kg dry wt.) and vitamin E (220 mg/kg dry wt.) did not lead to the synergy effect.

In Vitro Antitumor Activity and Nephrotoxicity of the Novel Platinum(II) Coordination Complex Containing Cis-dach/Diphosphine (새로운 Platinum(II)Complex ([Pt(II)(cis-dach)(DPPP)].$(NO_3)_2$의 항암효과 및 신독성)

  • Jung, Jee-Chang;Yim, Sung-Vin;Park, Seung-Joon;Chung, Joo-Ho;Ko, Kye-Chang;Chang, Sung-Goo;Rho, Young-Soo
    • The Korean Journal of Pharmacology
    • /
    • v.32 no.1
    • /
    • pp.93-102
    • /
    • 1996
  • Platinum coordination complexes are currently one of the most compounds used in the treatment of solid tumors. However, its use is limited by severe side effects such as nephrotoxicity. Our platinum-based drug discovery program is aimed at developing drugs capable of diminishing toxicity and broadening the clinical spectrum of activity of cisplatin. We synthesized new Pt(II) complex analogue containing 1,2-diaminocyclohexane (dach) as carrier ligand and 1,3-bis(diphenyl phosphino)propane (DPPP) as a leaving group. Furthermore, nitrate was added to improve the solubility. A new series of PC-1 [Pt(cis-dach) (DPPP)]. $2NO_3_2$ was synthesized and characterized by their elemental analysis and by various spectroscopic techniques [infrared (IR), $^{13}carbon$ nuclear magnetic resonance (NMR)]. PC-1 was demonstrated acceptable antitumor activity aganist SKOV -3, OVCAR-3 human ovarian adenocarcinomacells and significant activity as compared with that of cisplatin. The toxicity of PC-1 was found quite less than that of cisplatin using MTT, $[^3H]thymidine$ uptake and glucose consumption tests in rabbit proximal tubule cells, human kidney cortical cells and human renal cortical tissues. Based on these results, this novel platinum compound represent a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low toxicity.

  • PDF

Metabolic Engineering of the Brassinosteroid Biosynthetic Pathways (Brassinosteroid의 대사공학)

  • Lee, Mi-Ock;Song, Ki-Hong;Lee, Hyun-Kyung;Jung, Ji-Yoon;Choe, Vit-Nary;Choe, Sung-Hwa
    • Journal of Plant Biotechnology
    • /
    • v.29 no.2
    • /
    • pp.139-144
    • /
    • 2002
  • Sterols play two major roles in plants: a bulk component in biological membranes and precursors of plant steroid hormones. Physiological effects of plant steroids, brassinosteroids (BRs), include cell elongation, cell division, stress tolerance, and senescence acceleration. Arabidopsis mutants that carry genetic defects in BR biosynthesis or its signaling display characteristic phenotypes, such as short robust inflorescences, dark-green round leaves, and sterility. Currently there are more than 100 dwarf mutants representing 7 genetic loci in Arabidopsis. Mutants of 6 loci, dwf1/dim1/cbb1, cpd/dwf3, dwf4, dwf5, det2/dwf6, dwf7 are rescued by exogenous application of BRs, whereas bri1/dwf2 shares phenotypes with the above 6 loci but are resistant to BRs. These suggest that the 6 loci are defective in BR biosynthesis, and the one locus is in BR signaling. Biochemical analyses, such as intermediate feeding tests, examining the levels of endogenous BR, and molecular cloning of the genes revealed that dwf7, dwf5, and dwf1 are defective in the three consecutive steps of sterol biosynthesis, from episterol to campesterol via 5-dehydroepisterol. Similarly, det2/dwf6, dwf4, and cpd /dwf3 were shown to be blocked in D$^4$reduction, 22a-hydroxylation, and 23 a-hydroxylation, respectively. A signaling mutant bril/dwf2 carries mutations in a Leucine-rich repeat receptor kinase. Interestingly, the bri1 mutant was shown to accumulate significant amount of BRs, suggesting that signaling and biosynthesis are dynamically coupled in Arabidopsis. Thus it is likely that transgenic plants over-expressing the rate-limiting step enzyme DWF4 as well as blocking its use by BRIl could dramatically increase the biosynthetic yield of BRs. When applied industrially, BRs will boost new sector of plant biotechnology because of its potential use as a precursor of human steroid hormones, a novel lead compound for cholesterol-lowering effects, and a various application in plant protection.

Measurement of Human Cytochrome P450 Enzyme Induction Based on Mesalazine and Mosapride Citrate Treatments Using a Luminescent Assay

  • Kim, Young-Hoon;Bae, Young-Ji;Kim, Hyung Soo;Cha, Hey-Jin;Yun, Jae-Suk;Shin, Ji-Soon;Seong, Won-Keun;Lee, Yong-Moon;Han, Kyoung-Moon
    • Biomolecules & Therapeutics
    • /
    • v.23 no.5
    • /
    • pp.486-492
    • /
    • 2015
  • Drug metabolism mostly occurs in the liver. Cytochrome P450 (CYP) is a drug-metabolizing enzyme that is responsible for many important drug metabolism reactions. Recently, the US FDA and EU EMA have suggested that CYP enzyme induction can be measured by both enzymatic activity and mRNA expression. However, these experiments are time-consuming and their interassay variability can lead to misinterpretations of the results. To resolve these problems and establish a more powerful method to measure CYP induction, we determined CYP induction by using luminescent assay. Luminescent CYP assays link CYP enzyme activity to firefly luciferase luminescence technology. In this study, we measured the induction of CYP isozymes (1A2, 2B6, 2C9, and 3A4) in cryopreserved human hepatocytes (HMC424, 478, and 493) using a luminometer. We then examined the potential induction abilities (unknown so far) of mesalazine, a drug for colitis, and mosapride citrate, which is used as an antispasmodic drug. The results showed that mesalazine promotes CYP2B6 and 3A4 activities, while mosapride citrate promotes CYP1A2, 2B6, and 3A4 activities. Luminescent CYP assays offer rapid and safe advantages over LC-MS/MS and qRT-PCR methods. Furthermore, luminescent CYP assays decrease the interference between the optical properties of the test compound and the CYP substrates. Therefore, luminescent CYP assays are less labor intensive, rapid, and can be used as robust tools for high-throughput CYP screening during early drug discovery.

Applicability for Authenticity of Bronze Artefacts using Scientific Analyses (과학적 분석을 통한 전세품 청동기의 진위판별 적용 가능성 연구)

  • Do, Misol;Chung, Kwang Yong
    • Journal of Conservation Science
    • /
    • v.29 no.4
    • /
    • pp.355-366
    • /
    • 2013
  • Diverse scientific analyses, including microstructure, ICP-AES, SEM-EDS, and P-XRF(Bench Top type and Gun type), were carried out on 6 bronze artefacts which handed from generation to generation. Also, we attempted to study applicability for authenticity of the bronze artefacts using scientific analyses based on the specific element. The results of ICP-AES analysis showed that the bronze were formed from an alloy of Cu, Sn, Pb with trace elements such as Ag, As, Co, Fe, but there were not Zn found. The result of P-XRF are 10~25% lower in Cu and 10~20% higher in Sn than that of ICP-AES. This is because of destannification that the compound of $SnO_2$ are present on the surface. The results of SEM-EDS represented that there is lead segregation. It was difficult to study applicability for authenticity of bronze artefact according to the microstructures and chemical components of the bronze artefacts. Therefore, as bronze artefacts have shown different corrosion materials depending on the buried environment and conserving environment, identifying the authenticity would be possible on the basis of the additional researches on the corrosion and comparative research of ancient art.

Clinical Features, Response to Treatment, Prognosis, and Molecular Characterization in Korean Patients with Inherited Urea Cycle Defects

  • Yoo, Han-Wook;Kim, Gu-Hwan;Seo, Eul-Ju
    • Journal of The Korean Society of Inherited Metabolic disease
    • /
    • v.2 no.1
    • /
    • pp.77-79
    • /
    • 2002
  • The urea cycle, consisting of a series of six enzymatic reactions, plays key roles to prevent the accumulation of toxic nitrogenous compound and synthesize arginine de novo. Five well characterized diseases have been described, resulting from an enzymatic defect in the biosynthesis of one of the normally expressed enzyme. This presentation will focus on two representative diseases; ornithine transcarbamylase(OTC) deficiency and citrullinemia(argininosuccinate synthetase deficiency). OTC deficiency is one of the most common inborn error of urea cycle, which is inherited in X-linked manner. We identified 17 different mutations in 20 unrelated Korean patients with OTC deficiency; L9X, R26P, R26X, T44I, R92X, G100R, R141Q, G195R, M205T, H214Y, D249G, R277W, F281S, 853 del C, R320X, V323M and 10 bp del at nt. 796-805. These mutations occur at well conserved nucleotide sequences across species or CpG hot spot. The L9X and R26X lead to the disruption of leader sequences, required for directing mitochondrial localization of the OTC precursor. Their phenotypes are severe, and neonatal onset. The G100R, R277W and V323M mutations were uniquely identified in patients with late onset OTC deficiency. The other genotypes are associated with neonatal onset. Out of 20 patients with OTC deficiency, only 6 patients are alive; two were liver transplanted, and normal in growth and development at 2, 4 years after transplantation respectively. Citrullinemia is an autosomal recessive disease, caused by the mutations in the argininosuccinate synthetase(ASS) gene. We identified in 3 major mutations in 11 unrelated Korean patients with citrullinemia; G324S, $IVS6^{-2}$ A to G, and 67 bp ins at nt 1125-1126. Among these, the 67 base pair insertion mutation is novel. The allele frequency of each mutation is; G324S(45%), IVS6-2 A to G(32%), and 67 base pair insertion(14%). All patients are diagnosed at neonatal or infantile age. Interestingly, two patients presented with stroke like episode. Out of 11 patients, 5 patients died. Among 6 patients alive, one patient was successfully liver transplanted.

  • PDF

DNA Breakage by Salvianolic acid B in the Presence of Cu (II) (구리이온(II)이 존재할 때 Salvianolic acid B에 의한 DNA 절단)

  • Lee, Pyeongjae;Moon, Cheol;Choi, Yoon Seon;Son, Hyun Kyu
    • Korean Journal of Clinical Laboratory Science
    • /
    • v.50 no.2
    • /
    • pp.205-210
    • /
    • 2018
  • Salvianolic acid B, which is a compound in the Salvia miltiorrhiza, has diverse biological activities, In particular, the antioxidative effects were reported to be involved in the protection of hepatocytes, neurons, and various cell types. On the other hand, some phenolic compounds, such as ferulic acid, which is regarded as an antioxidant, plays a pro-oxidative role in the specific transitional metal environment, which could explain the anticancer effect. This study examined the pro-oxidative effects of salvianolic acid B in the presence of $Cu^{2+}$. Treatment with both salvianolic acid B and $Cu^{2+}$ induced the transition of supercoiled DNA to the open circular or linear form but not in the sole salvianolic acid B or $Cu^{2+}$ treatments. Salvianolic acid B reduced the $Cu^{2+}$ to $Cu^+$ using neocuproine, a $Cu^+$ specific chelator. In addition, catalase, an enzyme that breaks down the $H_2O_2$ to water and molecular oxygen, inhibited the DNA breakage. $H_2O_2$, a reactive oxygen species, has detrimental effects on biological molecules, particularly DNA. Overall, the reduction of $Cu^{2+}$ by salvianolic acid B could lead to the production of $H_2O_2$ followed by DNA breakage. These results suggest that the pro-oxidative effects could be the one of the anti-cancer mechanisms of salvianolic acid B, which remains to be explained.

Effect of Enhancement on Functionality of Germinated Adzuki Bean (Angularis angularis var. nipponensis) with High Hydrostatic Pressure (HHP) Treatment (고압처리에 의한 발아팥의 기능성 향상 효과)

  • Kim, Min Young;Jang, Gwi Yeong;Lee, Yoonjeong;Kim, Kyung Mi;Kang, Tae Su;Lee, Junsoo;Jeong, Heon Sang
    • The Korean Journal of Food And Nutrition
    • /
    • v.31 no.1
    • /
    • pp.135-142
    • /
    • 2018
  • We investigated the influence of germination and high hydrostatic pressure (HHP) treatment conditions on the conversion of functional compounds and antioxidant activity in adzuki bean. The adzuki bean germinated at $25^{\circ}C$ for three- or six-days, and was later subjected to HHP at 0.1, 50, 100, or 150 MPa for 24 h. The highest polyphenol content (5.36 mg gallic acid equivalents (GAE)/g) and flavonoid content (0.91 mg catechin equivalents (CE)/g) were observed after germination for six days and HHP treatment at 100 MPa for 24 h, respectively. The total phenolic acid contents increased with increasing applied pressure from 88.86 to $208.26{\mu}g/g$ (100MPa, 24h). Phenolic acids are divided into two categories; those that exhibit increased content upon HHP treatment, and those that exhibit decreased content. The increasing phenolic acids were gallic acid, chlorogenic acid, (+)-catechin, ${\rho}-coumaric$ acid, ferulic acid, heperidin, salicylic acid, protocatechuic acid, cinnamic acid, naringenin. The total anthocyanin content decreased with increasing applied pressure from 22.42 mg/100 g to 6.28 mg/100 g (150 MPa, 24 h). The highest ABTS radical scavenging activity (8.02 mg eq AA/g) and DPPH radical scavenging activity (1.22 eq Trolox/g) were observed after germination for six days and HHP treatment at 100MPa for 24h, respectively. These results suggested that the combination of HHP and germination can lead to improved functionality in adzuki bean.