• 제목/요약/키워드: 2-a]pyrimidine

검색결과 167건 처리시간 0.019초

생쥐 小腸에서의 Pyrimidine Deoxyribonucleoside 代謝와 CdR-aminohydrolase의 熱抵抗性 (Metabolism of Pyrimidine Deoxyribonucleosides and Heat-resistivity of CdR-aminohydrolase in the Mouse Small Intestine)

  • Kang, Man-Sik;Rhee, Juong-Gile;Cho, Joong-Myung
    • 한국동물학회지
    • /
    • 제17권3호
    • /
    • pp.107-116
    • /
    • 1974
  • 생쥐 小腸의 deoxycytidine-2-$^14 C$ (CdR-2-$^14 C$)와 deoxyuridine-2-$^14 C$ (UdR-2-$^14 C$)의 代謝를 관계酵素의 熱處理에 대한 영향과 관련해서 in vitro에서 고찰하였다. CdR-2-$^14 C$는 CdR-aminohydrolase의 作用에 의해서 먼저 nucleoside level에 급속히 deamination된 후, nucleosidase의 作用에 의해 uracil로 分解된다. 생쥐 小腸에서는 nucleosidase 가 CdR과 CR에는 親和力이 없기 때문에 이들 cytosine nucleoside의 N-pentose 結合을 分解하지 못하는 것으로 보인다. CdR-aminohydrolase는 $80^\\circ C$ 높은 不活性化溫度를 나타냈으며, 이에 반해서 nucleosidase는 $60^\\circ C$에서 不活性化가 되었다. 品種이 다른 생쥐의 여러 組織에 있는 CdR-aminohydrolase는 모두 $80^\\circ C$에서 不活性化됨이 관찰되었으나, 토끼 組織에서는 $80^\\circ C$에서도 不活性化가 일어나지 않는 점으로 미루어 不活性化溫度에는 "屬"特異性이 있는 것으로 짐작된다. 哺乳類의 分化된 組織에서 CdR-aminohydrolase 가 出現하는 生物學的 意味는 주로 分解過程과 有關한 것으로 생각된다. 것으로 생각된다.

  • PDF

세균 게놈 유래성 PyrR Orthologue의 기능 분석 (Characterization and Functional Study of PyrR Orthologues from Genome Sequences of Bacteria)

  • 김사열;조현수;설경조;박승환
    • 한국미생물·생명공학회지
    • /
    • 제31권2호
    • /
    • pp.103-110
    • /
    • 2003
  • 그람 양성세균에서 PyrR단백질에 의하여 피리미딘의 생합성이 조절된다는 발견을 바탕으로 하여, Synechocystis sp.PCC6803과 Haemophilus influenzae의 PyrR orthologue 유전자를 Bacillus subtilis에서 형질전환 시켜 피리미딘 생합성의 조절 유무를 조사하였다. Synechocystis sp.PCC6803과 H. influenzae의 PyrR orthologue유전자를 pUC19과 T-vector에 클로닝 한후 pKH1, pKH2, pHPSK1, pHPSK2으로 각각 명명하였다. 이것을 다시 Escherichia. coli와 B. subtiius용 shuttle vector인 pHPS9에 클로닝 하여 pKH3, pKH4, pHPSK3, pHPSK4로 각각 명명하였다. B. subtilis DB104Δ PyrR에 pKH3, pKH4, pHPSK3, pHPSK4을 형질전환후 ATCase 활성을 측정결과 pHPSK3을 가진 균주만 피리미딘에 의한 조절작용이 일어난다는 사실을 통하여, H. influenzae의 PyrR orthologue 유전자의 선도 부분에 조절에 관여하는 미지의 부분이 있음을 예측할 수 있었다. 서로 다른 유래의 PyrR orthologue단백질을 정제하기 위하여 pET14b에 클로닝후 pKH5, pHPSK5으로 각각 명명하였다. SDS-PAGE로 분석한 결과 각각 약 18 kDa과 21 kDa의 분자량을 나타내었다. 정제된 PyrR orthologue 단백질의 UPRTase 활성을 측정한 결과 H. infuenzae의 PyrR orthologue 단백질은 UPRTase 활성을 나타내었으며 다양한 pH에서 측정한 결과 pH 5에서 가장 높은 활성을 나타내었다. 반면에, Synechocystis sp. PCC6803의 PyrR orhologue 단백질은 UPRTase 활성을 나타내지 않았다. 여러 가지 균주의 PyrR 아미노산 서열을 비교한 계통수 분석은 PyrR 단백질의 조절기작과 어느 정도 연관됨을 시사해 주었다.

Control and Mechanism of Tumor Promotion in UV-Carcinogenesis

  • Ueda, Masato;Budiyanto, Arief;Ashida, Masashi;Bito, Toshinori;Ichihashi, Masamitsu
    • Journal of Photoscience
    • /
    • 제9권2호
    • /
    • pp.221-224
    • /
    • 2002
  • Carcinogenesis can be theoretically divided to intiation step and promotion step. Intiation associates with genetic alterations including p53 tumor suppressor gene and ras oncogene. Promotion involves in clonal expansion of of an initiated cell by epigenetic mechanism, mainly through signal transduction and gene expression. Ultraviolet light (UV) acts as both initiator and promoter. Initiation is closely related with DNA damage induced by UV, including cyclobutane pyrimidine dimers, (6-4) photoproducts and 8-hydroxy-2'-deoxyguanosine. Cyclobutane pyrimidine dimers and (6-4) photoproducts are directly induced by UV, while 8-hydroxy-2'-deoxyguanosine is induced indirectly by the reactive oxygen species. Because initiation is an irreversal genetic event, while promotion is a reversal and epigenetic event, to know the molecular mechanisms of tumor promotion in UV-carcinogenesis is crucial to develop preventive medicine and suppress UV-carcinogenesis. Because ROS is also involved in signal transduction of the cell, anti-oxidant could be the good candidate of anti-promoting agent. Here, we describe the suppressive effect of UV-carcinogenesis by various anti-oxidant including olive oil. In addition, we discuss about the mechanism of UVB-induced expression of cyclooxygenase-2, which might be a representative molecule involved in promotion of UV-carcinogenesis.

  • PDF

Synthesis and Biological Activities of New Substituted Indoles

  • Hishmat, Orchidee H.;Nakkady, Sally S.;El Shabrawy, Osama A.;Mahmoud, Sawsan S.
    • Archives of Pharmacal Research
    • /
    • 제15권1호
    • /
    • pp.104-108
    • /
    • 1992
  • 2, 3-Diphenyl-6-formyl-5-methoxyindole reacts with ethyl cyano acetate to yield the arylidene derivative which forms with urea and thiourea the corresponding pyrimidine derivatives. The arylidene derivatives react with hydrazines and with active methylenes to form the respective pyrazole derivatives and the $\alpha, \;\beta$-disubstituted acrylonitriles. Seven new compounds were tested for their effects on the arterial blood pressure of rats and analgesic activity.

  • PDF

Differences in the Amino Acid Sequences of CPD Photolyases of UV-sensitive and UV-resistant Rice Cultivars

  • Teranishi, Mika;Hidema, Jun;Fujino, Takana;Hirouchi, Tokuhisa;Yamamoto, Kazuo;Kumagai, Tadashi
    • Journal of Photoscience
    • /
    • 제9권2호
    • /
    • pp.329-331
    • /
    • 2002
  • There is a difference in the inhibitory effects to supplemental UVB (wavelengths 280 to 320 nm) among Japanese rice (Oryza sativa L.), the cultivar Norin I is less resistant while the cultivar Sasanishiki is resistant. UVB induces photodamage in DNA. Cyclobutane pyrimidine dimer (CPD) is a major UV-induced DNA lesion. Photorepair, which is mediated by photolyase, is the major pathway in plants for repairing CPD. We have analyzed CPD induction and repair in Sasanishiki and its close relative Norin I using alkaline agarose gel electrophoresis. Norin I is deficient in CPD photoreactivation and excision, thus UV sensitivity correlates with deficient dimer repair [I]. The photorepair deficiency in Norin I results from a functionally altered photolyase with a photoflash analysis [2]. In this paper, we examined the UVB-sensitivity of several other UV-sensitive and -resistant cultivars and found that the CPD photolyase activity was deficient in UV-sensitive ones. It was also evident that there was a variation in the deduced amino acid sequences of CPD photolyases of the UV-sensitive and -resistant cultivars, whereas each deduced amino acid sequence of the UV-sensitive cultivars and of the UV-resistant ones was the same. These results suggest that the difference in the CPD photolyases of UV-sensitive and -resistant rice might be due to the structural alteration of CPD photolyase.

  • PDF

자외선에 의한 세포손상에 대한 말채나무잎의 보호효과 (The Protective Effects of Cornus walteri Wanger Leaves against UV Induced Cellular Damage in Human Fibroblast)

  • 박현철;정택규;윤경섭
    • 대한화장품학회지
    • /
    • 제41권1호
    • /
    • pp.1-7
    • /
    • 2015
  • 말채나무는 한국의 민간요법으로 사용되던 약재이다. 자외선은 피부의 광손상을 일으키는 것으로 알려져 있다. 본 연구에서는 자외선에 의한 손상된 세포를 회복시키기 위해서 효소처리 된 말채나무잎추출물(CWE)을 사용하였다. 섬유아세포에 UVB를 조사한 후, CWE를 처리하여 세포의 회복을 조사하였다. UVB를 조사한 섬유아세포에는 caspase-3 활성, phospho-p53, ${\gamma}H2AX$, cyclobutane pyrimidine dimers (CPDs) formation, 그리고 DNA fragmentation이 증가하게 된다. 그러나 CWE를 UVB가 조사된 섬유아세포에 12 h 처리하였을 때 caspase-3 활성, phospho-p53, ${\gamma}H2AX$, CPDs formation, 그리고 DNA fragmentation이 감소하였다. 또한 CWE은 인체첩포시험을 통해 인체피부에 자극을 유발하지 않음을 확인하였다. 이러한 결과를 종합할 때 CWE는 자외선에 대한 광보호 효과가 있는 원료로서 가능성을 가지고 있다고 판단된다.

Synthesis, Reactions and Antimicrobial Activity of 2-Amino-4-(8-quinolinol-5-yl)-1-(p-tolyl)-pyrrole-3-carbonitrile

  • Abdel-Mohsen, Shawkat A.
    • Bulletin of the Korean Chemical Society
    • /
    • 제26권5호
    • /
    • pp.719-728
    • /
    • 2005
  • A novel 2-amino-4-(8-quinolinol-5-yl)-1- (p-tolyl)-pyrrole-3-cabonitrile (2) was obtained by the reaction of 2-[2-bromo-1-(8-hydroxyquinolin-5-yl)-ethylidene]-malononitrile (1) with p-toluidene. The new synthon compound (2) could be annelated to the corresponding pyrrolo[2,3-d]pyrimidines (4, 6, 7, 26-28), triazolo[1,5-c]pyrrolo[3,2-e]pyrimidines (10, 29, 30), pyrrolo[2,3-c]pyrazoles (11-15), pyrrolo[1,2-a]pyrrolo[3,2-e] pyrimidine (17) and imidazo[1,2-c]pyrrolo[3,2-e]pyrimidines (18-25) via the reaction with some reagents such as acetic anhydride, formamide, triethyl orthoformate, hydrazine hydrate, hydroxylamine, ethylenediamine, carbon disulfide and phosphorus oxychloride. Chemical and spectroscopic evidences for the structures of these compounds are presented. The antifungal and antibacterial activity of the newly synthesized comounds were evaluated.

Synthesis and Biological Evaluation of 9-[2-Fluoro-4-hydroxy-3-hydroxymethyl-2-butenyl]adenine and its Related Compounds as Open-chain Analogues of Neplanocin A

  • Choi, Myung-Hee;Kim, Hee-Doo
    • Archives of Pharmacal Research
    • /
    • 제20권5호
    • /
    • pp.501-506
    • /
    • 1997
  • Novel 9-[2-fluoro-4-hydroxy-3-hydroxymethyl-2-butenyl]adenine and its related compounds were designed and synthesized as open-chain analogues of neplanocin A. Alkylation of adenine or pyrimidine bases with the mesylate 4 was chosen as a simple approach to the synthesis of 2-fluoro-2-butenylated nucleosides. Mesylate 4 was prepared from dihydroxyacetone dimer via four steps in 58% overall yield. The synthesized compounds were evaluated their antiviral activity against HSV, HIV and Polio viruses.

  • PDF

인산감수성(燐酸感受性)이 다른 대두품종간(大豆品種間) 유기산(有機酸) 및 당(糖)에 대(對)한 질소원(窒素源)의 영향(影響) (Effects of Nitrogen Sources on Sugars and Organic Acids of Soybean Cultivars Different in Phosphorus Sensitivity)

  • 박훈;찰스 에이 스뚜디
    • 한국토양비료학회지
    • /
    • 제10권2호
    • /
    • pp.85-92
    • /
    • 1977
  • 인산감수성(燐酸感受性)이 다른 9개대두재배종(個大豆栽培種) Lee, Hill, Harosoy, Clark-63, Chippewa 및 R56-49을 서로 다른 질소원(窒素源)으로 수경재배(水耕栽培)하여 엽중유리당(葉中遊離糖)과 유기산(有機酸)을 gas chronatograph로 조사(調査)하여 미동정(未同定)의 X, Y peak와 Sucrose peak가 주(主) peak로 나타났다. X 화합물(化合物)은 NO3-N 급여(給與)경우 흔적으로 나타난데 반하여 NH4-N나 urea 급여(給與)경우에 다량(多量)나타났다. Y 화합물(化合物)을 Urea 급여(給與)경우 감소하는 경향이었다. Sucrose는 NH4-N 급여(給與)에서 흔적으로 나타나고 Urea에서 NO3-N에서보다 높았다. X 화합물(化合物)은 erythrose에서 유래(由來)한 4 탄소(炭素) 산성당(酸性糖)이거나 Purine이나 Pyrimidine에서 유래(由來)한 환상화합물(環狀化合物)로 Y 화합물(化合物)은 glycolysis path에서 유래(由來)한 6 탄당(炭糖)으로 추정(推定)되었다. Y/X 치(値)는 인산감수성(燐酸感受性)의 좋은 지표(指標)가 되므로(역관계(逆關係)) 이 두 화합물(化合物)은 ammonia 독작용(毒作用) 및 인산감수성(燐酸感受性) 기작(機作)에 관여(關與)하는 요인화합물(要因化合物)로 보였다.

  • PDF

Photoprotection by Topical DNA Repair Enzymes

  • Yarosh, Daniel B.
    • Journal of Photoscience
    • /
    • 제9권2호
    • /
    • pp.186-189
    • /
    • 2002
  • Many of the adverse effects of solar UV exposure appear to be directly attributable to damage to epidermal DNA. In particular, cyclobutane pyrimidine dimers (CPD) may initiate mutagenic changes as well as induce signal transduction responses that lead to a loss of skin immune surveillance and micro-destruction of skin structure. Our approach is to reverse the DNA damage using prokaryotic DNA repair enzymes delivered into skin using specially engineered liposomes. T4 endonuclease V encapsulated in liposomes (T4N5 liposome lotion) enhanced DNA repair by shifting repair of CPD from the nucleotide excision to the base excision repair pathway. Following topical application to humans, increased repair limited UV-induction of cytokines, many of which are immunosuppressive. In a recent clinical study, topical treatment of UV-irradiated human skin with T4N5 liposome lotion reduced the suppression of the nickel sulfate contact hypersensitivity response. Similarly, the photoreactivating enzyme enhances repair by directly reversing CPDs after absorbing activating light. Here also treatment of UV-irradiated human skin with photoreactivating enzyme in liposomes and photoreactivating light restored the response to the contact allergen nickel sulfate. These findings confirm in humans the observation in mice that UV induced suppression of contact hypersensitivity is caused in part by CPDs. We have tested the ability of T4N5 liposome lotion to prevent UV-induced skin cancer in patients with xeroderma pigmentosum (XP), who have an elevated incidence of skin cancer resulting from a genetic defect in DNA repair. Daily use of the lotion for one year in a group of 20 XP patients reduced the average number of actinic keratoses by 68% and basal cell cancers by 30% compared to 9 patients in the placebo control group. Delivery of DNA repair enzymes to skin is a promising new approach to photoprotection.

  • PDF