• Title/Summary/Keyword: $1{\alpha}-(OH)D_3$

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The search and development for antitumor compounds from the marine algae (해조류 유래의 항종양성 물질의 탐색과 개발)

  • 손병화
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.211-211
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    • 1994
  • 항종양성 화합물의 개발을 지향한 해양생물 유래의 생물활성 물질의 화학적 연구의 일환으로써 다양한 종류의 생물활성 (즉, 항균작용, 혈중콜레스테롤 저하작용)등을 나타내며, 구입수가 용이한 홍조 꼬시래기 (Gracilaria verrucosa) 및 갈조 지충이 (Sargassum thunbergii)의 아세톤 및 메탄올 엑스를 EtOAc 및 n-BuOH로 분획한후 각 분획을 SiO$_2$ column, TSK gel(Toyo pearl HW-40F), $\mu$-Bondapak column 및 HPLC등으로 분리 정제하여, 새로운 glyceroglycolipid(GV-5, -6, ST-6) 및 glycerylglycoside(GV-12)를 얻었다. 이렇게 분리된 화합물의 물리화학적 성질, 화학반응 및 분광학적 data를 종합 검토한 결과 GV-5, -6, -12, 및 ST-6은 각각 1,2-diacyl-3-0-($\alpha$-D-galactopyranosyl) glycerol (acyl : palmitate-oleate-arachidonate 4: 1 : 9) (1), 1,2-diacyl -3-0-〔$\alpha$-D-galactopyranosyl -(1 "$\longrightarrow$6')-0-$\beta$-D-galactopyranosyl〕 glycerol (acyl : palmitate-oleate-arachidonate(5:1:4)(3), 2-0-($\alpha$-D-galactopyranosyl) glycerol (5), 및 sodium salt of 1-acyl-3-0-(6'-sulfo-$\alpha$-D-quinovopyranosyl) glycerol(acyl:palmitate-oleate 96:4)(8) 이라는 것이 판명되었다. 그리고 GV-5 및 -6은 마우스 백혈병세포 (L1210)에 대한 세포독성 ($IC_{50}$/ of GV-5, and -6:8.0$\mu\textrm{g}$/ml and 10.8$\mu\textrm{g}$/ml )외에, 사람의 상피암세포에 대한 성장억제효과 [growth inhibitor(%) in 20$\mu\textrm{g}$/m1 :GV-5(39.9%), GV-6(16.7%)를 나타내었으며, 한편, GV-5, GV-6, -12 및 ST-6은 각각 쥐의 F9 기형암종 세포의 분화유도 활성을 나타내어 항종양제로의 개발에 많은 흥미가 기대된다.기대된다.

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Effectiveness of Once-weekly Compared with Thrice-weekly Subcutaneous Epoetin Alpha for the Treatment of Chemotherapy-induced Anemia (항암치료로 인한 빈혈의 치료에서 Epoetin Alpha 주일회요법과 주삼회요법의 약효 비교 연구)

  • Lee, Yoon-Duck;Kim, Kyung-Im;Kim, Young-Ju;Shin, Wan-Gyoon;Oh, Jung-Mi
    • Korean Journal of Clinical Pharmacy
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    • v.19 no.2
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    • pp.146-152
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    • 2009
  • Purpose : 본 연구의 목적은 항암치료로 인한 빈혈환자의 치료에서 epoetin alpha (rHuEPO) 피하주사 시, 주일회 요법과 주삼회요법의 헤모글로빈(hemoglobin, Hb) 상승 효과를 비교하는 것이다. Methods : 본 연구는 1999년 3월부터 2005년 3월까지 국립암센터에서 항암치료로 인한 빈혈로 epoetin alpha를 투여 받은 환자를 대상으로 의무기록의 자료를 후향적으로 수집하여 분석하였다. 연구에 포함된 환자는 rHuEPO 10,000 IU 주삼회투여군(n = 127)과 20,000 IU 주일회투여군(n = 81)으로 구분되었으며, 이들은 필요에 따라 경구용 철분보조제를 섭취하였다. Epoetin alpha 치료 시작 후 최대 8주까지 2주 간격으로 Hb 수치변화를 분석하였다. Results : 치료 시작 시점의 rHuEPO 10,000 IU 주삼회투여군과 20,000 IU 주일회투여군의 평균 Hb수치는 유사하였 다 (9.4 g/dL vs. 9.7 g/dL). Epoetin alpha 치료 후 8주까지 두 그룹간의 헤모글로빈 수치의 상승 정도에는 유의한 차이가 없었다 ($1.57{\pm}1.39$ g/dL vs. $1.68{\pm}1.35$ g/dL, p=0.59). 또한 경구용 철분보조제 투여여부, cisplatin 포함 항암제 투여여부 및 성별에 따른 군의 분류에 있어서도 rHuEPO 10,000 IU 주삼회투여군과 20,000 IU 주일회투여군의 평균 Hb 상승수치는 유의한 차이를 보이지 않았다. Conclusion : 한국인에서 항암치료로 인한 빈혈의 치료 시에 rHuEPO 20,000 IU 주일회투여 용법은 10,000 IU 주 삼회투여 용법과 유사한 Hb 상승효과를 가진다.

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A Study on the Synthesis of High-Purity ${\alpha}-Al_2O_3$ Ultra-Fine Powders by Wet Chemical Method (습식 합성법에 의한 고순도 ${\alpha}-Al_2O_3$ 미세분말의 합성 연구)

  • Jin-Ho Choy;Jong-Seok Yoo;Yang-Su Han;Joon Kim;Hyeon-Kook Lee;Hyuk-Nyun Kim
    • Journal of the Korean Chemical Society
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    • v.35 no.3
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    • pp.275-279
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    • 1991
  • Ultra-fine alumina, ${\alpha}-Al_2O_3$, with ${\phi}$ = 0.1∼0.5 ${\mu}$m was obtained from pure ammonium aluminum sulfate(alum) as the thermal decomposition product. Pure alum(> 99.7%) could be prepared by the precepitation and the successive recrystallization in an acidic aqueous solution at pH = 1.5∼2.5, which was theoretically predicted by only considering the concentrations of hydroxide and carbonate for aluminum and sodium in the solution, and also experimentally confirmed as the optimum precepitation condition for alum without forming any impurities like aluminum hydroxide or sodium one.

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Sesquiterpenes from Syneilesis palmata and Their Cytotoxicity Against Human Cancer Cell Lines In Vitro

  • Lee Kyu Ha;Cho Sang Un;Lee Kang Ro
    • Archives of Pharmacal Research
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    • v.28 no.3
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    • pp.280-284
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    • 2005
  • The chromatographic separation of the MeOH extract from the aerial parts of Syneilesis palmata led to the isolation of a new sesquiterpene glycoside 4, together with four known compounds. Their structures were characterized to be 4$\beta$,5$\beta$-epoxy-caryophill-8,(15)-ene (1), 3$\beta$­hydroxy-gultin-5-ene (2), 4$\alpha$,5$\beta$-dihydroxy-caryophill-8,(15)-ene (3), (-)-oplopan-4-one-10-$\alpha$-O­$\beta$-D-glucose (4) and 3-hexenyl-1-O-$\beta$-D-glucopyranose (5), based on spectroscopic and chemical methods. Compound 2 showed moderate cytotoxicity against five human tumor cell lines in vitro with its EDso values ranging from 5.90-1 0.83 $\mu$g/mL.

EFFECT OF TUMOR NECROSIS FACTOR-α ON THE BONE METABOLISM (Tumor Necrosis Factor-α가 골대사에 미치는 영향)

  • Kim, Sang-Sub;Lee, Su-Jong
    • Restorative Dentistry and Endodontics
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    • v.24 no.1
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    • pp.187-199
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    • 1999
  • Bone remodeling is characterized by the continuing processes of osteoblast-mediated bone formation and osteoclast-mediated bone resorption. Bone metabolism is tightly regulated at the local level by networks of hormones, cytokines, and other factors. In pathological conditions of bone remodeling, including osteoporosis and periodontal diseases, inflammatory cytokines and local mediators are responsible for enhancement of osteoclast resorption and inhibition of repair at the sites of bone resorption. TNF-${\alpha}$ is a pleiotropic hormone with actions on the differentiation, growth, and functional activities of normal and malignant cells from numerous tissues. TNF-${\alpha}$ has been proposed as a local mediator of the control of bone turnover in situations of chronic inflammation, and it has been assumed that the local source of TNF-${\alpha}$ is the monocyte in the adjacent bone marrow or the local circulation. TNF-${\alpha}$ is a potent inducer of bone resorption. TNF-${\alpha}$ is known to induce the activation of apoptotic signaling pathway, which leads to the apoptosis of bone cells. We demonstrated that treatment of murine osteoblastic MC3T3E1 cells with TNF-${\alpha}$ decreases proliferation as well as alkaline phosphatase (ALP) activity in a dose depenent manner. In addition, TNF-${\alpha}$ increases osteoclast-like cell formation in $1{\alpha}$, 25(OH)2D3 or PGE2-treated bone marrow cell culture. When cells were cultured in TNF-${\alpha}$ free ${\alpha}$-MEM, this inhibitory effect of ALP activity was reversible up to 10 ng/ml TNF-${\alpha}$, in contrast, at the 20 ng/ml TNF-${\alpha}$, irreversible. In this concentration, TNF-${\alpha}$ may induce apoptosis in MC3T3E1 cells. In this study, TNF-${\alpha}$ induces apoptosis resulting in chromosomal DNA fragmentation, preceded by JNK/SAPKs and caspase-3 activation. Our present results show that JNK/SAPKs and caspase-3 are activated by TNF-${\alpha}$, suggesting that the JNK/SAPKs and caspase-3 participate in the bone resorption, associated with apoptosis.

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Isolation of Anti-oxidant from Domestic Crataegus pinnatifida Bunge Leaves (국산 산사나무 잎으로부터 항산화 활성성분의 분리)

  • Kang, In-Ho;Cha, Ja-Hyun;Han, Jeong-Hun;Lee, Seong-Wan;Kim, Hon-Jin;Kwon, Suck-Hyung;Ham, In-Hye;Hwang, Bo-Sik;Whang, Wan-Kyunn
    • Korean Journal of Pharmacognosy
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    • v.36 no.2 s.141
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    • pp.121-128
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    • 2005
  • In order to find the antioxidative compounds, fractionation of the MeOH extract of the leaves of Crataegus pinnatifida guided by DPPH scavenging test furnished seven phenolic compounds, $quercetin-3-O-{\alpha}-L-rhamnopyranosyl(1{\rightarrow}6)-{\beta}-D-glucopyranoside$ (1), myricetin-3-O-rhamnose (2), $quercetin-3-O-{\alpha}-L-rhamnopyranosyl-(1{\rightarrow}6)-{\beta}-D-galctopyranoside$ (3), $quercetin-3-O-{\beta}-D-galactopyranoside$ (4), quercetin (5), $apigenin-8-C-{\beta}-L-rhamnopyranosyl-(1{\rightarrow}6)-{\beta}-D-glucopyranoside$ (2'-O-rhamnosylvitexin) (6) and (-)-epicatechin (7). All of isolated compounds showed the significant antioxidative effect on DPPH free radical scavenging test and TBARS assay.

Chemical Constituents of the Leaves of Weigela subsesillis (병꽃나무 잎의 성분)

  • Won, Hee-Mok;Kwon, Yong-Soo;Lee, Jin-Hoon;Kim, Chang-Min
    • Korean Journal of Pharmacognosy
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    • v.35 no.1 s.136
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    • pp.1-5
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    • 2004
  • Eight compounds were isolated from the n-BuOH soluble fraction of the leaves of Weigela subsesillis. On the basis of spectral data, they wεre identified as $kaempferol-O-3-{\alpha}-L-(3-O-acetyl)\;rhamnopyranosyl-7-O-{\alpha}-L-rhamnopyranoside$ (1), sutchuenoside A (2), kaempferitrin (3), astragalin (4), kaempferol 7-O-rhamnoside (5), scopolin (6), farxin (7), kaempferol 3-O-{\alpha}-L-rhamnosyl-7-O-{\beta}-D-glucoside (8), respectively.

Steroids from the Cold Water Starfish Ctenodiscus crispatus with Cytotoxic and Apoptotic Effects on Human Hepatocellular Carcinoma and Glioblastoma Cells

  • Quang, Tran Hong;Lee, Dong-Sung;Han, Se Jong;Kim, Il Chan;Yim, Joung Han;Kim, Youn-Chul;Oh, Hyuncheol
    • Bulletin of the Korean Chemical Society
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    • v.35 no.8
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    • pp.2335-2341
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    • 2014
  • Chemical investigation on the methanol extract of the starfish Ctenodiscus crispatus resulted in the isolation of five steroids, (22E,$24{\zeta}$)-26,27-bisnor-24-methyl-$5{\alpha}$-cholest-22-en-$3{\beta}$,5,$6{\beta}$,$15{\alpha}$,25-pentol 25-O-sulfate (1), (22E,24R,25R)-24-methyl-$5{\alpha}$-cholest-22-en-$3{\beta}$,5,$6{\beta}$,$15{\alpha}$,25,26-hexol 26-O-sulfate (2), (28R)-24-ethyl-$5{\alpha}$-cholesta-$3{\beta}$,5,$6{\beta}$,8,$15{\alpha}$,28,29-heptaol-24-sulfate (3), (25S)-$5{\alpha}$-cholestane-$3{\beta}$,5,$6{\beta}$,$15{\alpha}$,$16{\beta}$,26-hexaol (4), and ${\Delta}7$-sitosterol (5). Their structures were identified by extensive spectroscopic analyses, including 1D, 2D NMR and MS and chemical methods. Compound 4 showed cytotoxicity against human hepatoma HepG2 and glioblastoma U87MG cells via inhibition of cell growth and induction of apoptosis. Induction of apoptosis by 4 was demonstrated by cell death, DNA fragmentation, increased Bax/Bcl-2 protein ratio and the activation of caspase-3, caspase-9 and poly (ADP-ribose) polymerase (PARP).

Phytochemical Constituents of Salsola komarovii and Their Effects on NGF Induction

  • Cho, Hyeon Kyung;Suh, Won Se;Kim, Ki Hyun;Kim, Sun Yeou;Lee, Kang Ro
    • Natural Product Sciences
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    • v.20 no.2
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    • pp.95-101
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    • 2014
  • Five lignan glycosides, seven megastigmane glycosides, and seven phenolic compounds were isolated by repeated column chromatography from the MeOH extract of Salsola komarovii. Their structures were determined to be lariciresinol-9-O-${\beta}$-$\small{D}$-glucopyranoside (1), alangilignoside C (2), conicaoside (3), (+)-lyoniresinol 9'-O-${\beta}$-$\small{D}$-glucopyranoside (4), (8S,8'R,7'R)-9'-[(${\beta}$-glucopyranosyl)oxy]lyoniresinol (5), blumenyl B ${\beta}$-$\small{D}$-glucopyranoside (6), blumenyl A ${\beta}$-$\small{D}$-glucopyranoside (7), staphylionoside D (8), icariside $B_2$ (9), (6R,9S)-3-oxo-${\alpha}$-ionol ${\beta}$-$\small{D}$-glucopyranoside (10), 3-oxo-${\alpha}$-ionol 9-O-${\beta}$-$\small{D}$-apiofuranosyl-($1{\rightarrow}6$)-${\beta}$-$\small{D}$-glucopyranoside (11), blumenol B 9-O-${\beta}$-$\small{D}$-apiofuranosyl-($1{\rightarrow}6$)-${\beta}$-$\small{D}$-glucopyranoside (12), benzyl 6-O-${\beta}$-$\small{D}$-apiofuranosyl-${\beta}$-$\small{D}$-glucopyranoside (13), canthoside C (14), tachioside (15), isotachioside (16), biophenol 2 (17), 2-(3,4-dihydroxy)-phenyl-ethyl-${\beta}$-$\small{D}$-glucopyranoside (18), and cuneataside C (19) by spectroscopic methods. All the isolated compounds 1 - 19 were reported from this source for the first time. Compounds 2, 3 and 6 upregulated NGF secretion to $118.8{\pm}3.6%$, $128.2{\pm}9.3%$ and $111.1{\pm}7.1%$ without significant cell toxicity.

Ergosterol peroxides from the fruit body of Sparassis crispa (꽃송이버섯(Sparassis crispa) 자실체로부터 ergosteol peroxide의 분리 및 동정)

  • Lee, Yeong-Geun;Thi, Nhan Nguyen;Kim, Hyoung-Geun;Lee, Dae Young;Lee, Seung-Eun;Kim, Geum-Soog;Baek, Nam-In
    • Journal of Applied Biological Chemistry
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    • v.59 no.4
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    • pp.313-316
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    • 2016
  • Sparassis crispa fruits were extracted in 80 % MeOH, and the concentrated extract was partitioned into EtOAc, n-butyl alcohol, and water fractions. The repeated octadecyl $SiO_2$ and silica gel ($SiO_2$) column chromatographies for the EtOAc and nbutyl alcohol fractions led to isolation of two ergosterol peroxides. There chemical structures were determined as ($3{\beta}$,$5{\alpha}$,$8{\alpha}$,22E)-5,8-Epidioxyergosta-6,22-dien-3-ol (ergosterol peroxide) (1) and 3-O-${\beta}$-D-glucopyranosyl ergosterol peroxide (2) based on spectroscopic data analyses including nuclear magnetic resonance, infrared spectrometry, and mass spectrometry (MS). Compounds 1 and 2 were for the first time isolated from S. crispa in this study.