• Title/Summary/Keyword: Analogs

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Characteristics of Pinitol as a Functional Food Biomaterial (건강기능성 식품소재로서 pinitol의 특성)

  • Son, Min-Sik;Seo, Myung-Seon;Lee, Sang-Han
    • Journal of Life Science
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    • v.19 no.1
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    • pp.147-151
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    • 2009
  • D-pinitol, another chemical structure of 3-O-methyl-D-chiro-inositol, is an important insulin-sensitizer. The purpose of this review is to examine the characteristics of pinitol and other analogs as functional food biomaterials which were well known to reduce blood glucose levels. Pinitol can be converted to chiro-inositol in normal humans, while diabetic patients can not use the molecule, resulting in exhibiting low level of chiro-inositol in their urine. Recently, it is reported that pinitol can trigger phospholipase C/D, thus the rate of glucose metabolism accelerates to use as fuel for human body. To not only reduce insulin resistance of diabetic patients, but also alleviate the symptoms of diabetes, obesity, and muscle contraction, pinitol and its dietary supplementation is needed.

Permeability Characteristics of Polymerized Vesicles(II) (고분자화된 Vesicles의 투과 특성(II))

  • Bae, Duck-Hwan;Kim, Kong-Soo;Shin, Jae-Sup
    • Applied Chemistry for Engineering
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    • v.3 no.2
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    • pp.335-340
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    • 1992
  • Polymerized vesicles were formed from monomeric surfactants and permeability of polymerized vesicles were compared with that of monomeric analogs. The results showed that crosslinking get the permeability of vesicle decrease. And when the vesicle was polymerized at both inside and outside of vesicle, the vesicle got the lower permeability. Packing structure in the vesicle which is dependent upon the molecular structure of alkyl group in surfactant had an effect on permeability of vesicle.

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CHEMOPREVENTION OF MAMMARY CARCINOGENESIS BY SYNTHETIC ANALOG OF VITAMIN D5.

  • Mehta, Rajendra G.;Hussain, Erum;Moriarty, Robert M.;Mehta, Rajeshwari R.;Das Gupta, Tapas K.
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.10a
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    • pp.52-53
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    • 2001
  • In order for vitamin D to be active, it needs to get metabolized to 1, 25 (OH)$_2$D3. This active metabolite of vitamin D induces epithelial cell differentiation and is antiproliferative. However, at the efficacious concentration, the natural ligand for VDR is hypercalcemic and toxic to cells. Therefore, numerous analogs have been synthesized with the hope of generating a compound that retains vitamin D activity and is non-toxic.(omitted)

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CHEMOPREVENTION OF MAMMARY CARCINOGENESIS BY SYNTHETIC ANALOG OF VITAMIN D5.

  • Mehta, Rajendra G.;Hussain, Erum;Moriarty, Robert M.;Mehta, Rajeshwari R.;DasGupta, Tapas K.
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.10b
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    • pp.9-10
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    • 2001
  • In order for vitamin D to be active, it needs to get metabolized to 1, 25 (OH)$_2$D3. This active metabolite of vitamin D induces epithelial cell differentiation and is antiproliferative. However, at the efficacious concentration, the natural ligand for VDR is hypercalcemic and toxic to cells. Therefore, numerous analogs have been synthesized with the hope of generating a compound that retains vitamin D activity and is non-toxic.(omitted)

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Inhibitory Effect of Ginsenoside-Rp1, a Novel Ginsenoside Derivative, on the Functional Activation of Macrophage-like Cells

  • Park, Tae-Yoon;Cho, Jae-Youl
    • Biomolecules & Therapeutics
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    • v.16 no.4
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    • pp.370-376
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    • 2008
  • Ginsenoside Rp1 (G-Rp1) is a ginseng saponin derivative with chemopreventive and anti-cancer activities. In this study, we examined the regulatory activity of G-Rp1 on the functional activation of macrophages. G-Rp1 remarkably inhibited TNF-$\alpha$ production, LPS-induced cell cytotoxicity, NO production, ROS generation, and phagocytic uptake from lipopolysacchride (LPS)-activated RAW264.7 cells. According to structural feature study using several G-Rp1 analogs, two carbohydrates (glucose-glucose) at R1 position were observedto be highly effective, compared to other structural derivatives. Although the inhibitory activities of G-Rp1 on macrophage functions were not remarkable, several points that G-Rp1 was known to be safe, and that this compound was orally effective, suggest that G-Rp1 may be beneficial in treating macrophage-mediated immunological diseases.

Synthesis of Abscisic Acid Analogs and Their Biological Activity on Growth of Rice Seedling (합성 ABA 유도체의 벼 유묘 생장저해 작용)

  • Lee, Sang-Kap
    • Korean Journal of Environmental Agriculture
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    • v.16 no.3
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    • pp.269-273
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    • 1997
  • This research aims at developing a new plant growth inhibitors related to abscisic acid by means of esterification of (S)-(+)-ABA with p-hydroxy methyl cinnamate and umbelliferone, and testing its biological activity on growth of rice seedlings. The over-all yield of ABA-methyl cinnamate(AC) and ABA-umbelliferone(AC) ester compounds were 83% and 78%, respectively. The growth inhibition activity of these synthetic compounds were shown about 3 to 10 times(AC) and 10 to 30 times(AU) higher than (S)-(+)-ABA.

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Synthesis and Cycloaddition Reactions of N-Aryl-2-furohydrazonyl Chlorides

  • S, Shawali-Ahmad;M, Hassaneen-Hamdi;A, Ibrahim-Hossin
    • Archives of Pharmacal Research
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    • v.13 no.2
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    • pp.126-131
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    • 1990
  • The novel N-phenyl-2-furohydrazonyl chloride 4A and its p-nitro analog 4B have been prepared and identified. The cycloaddition reactions of nitrilimines 5A and 5B, derived by base catalyzed dehydrochlorination of 4A and 4B respectively, to a variety of dipolarophiles were investigated. The results showed that 4A and 4B are usuful precursors for synthesis of differently substituted 3-(2-furyl)-2-pyrazoline derivatives and their pyrazoles and analogs.

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Activity Profiles of Linear, Cyclic Monomer and Cyclic Dimer of Enkephalin

  • Kim, Dong-Hee;Hong, Nam-Joo
    • Bulletin of the Korean Chemical Society
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    • v.33 no.1
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    • pp.261-269
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    • 2012
  • The cyclic dimers of enkephalin were isolated as minor components during the solution synthesis of the corresponding cyclic monomers. The ratio of cyclic dimer to monomer was approximately 1:4 from the percent of yields. In the receptor binding assay of two cyclic dimmers, ($Tyr_2-C[D-Glu-Phe-gPhe]_2$ 6, $Tyr_2-C[D-Asp-Phe-gPhe-rLeu]_2$ 8), both analogs exhibited the high preference for ${\delta}$ receptor compared to monocyclic counterparts. In the nociceptive activity, both showed about 5 times less potent than the cyclic monomers. The repeated synthesis of 14-membered cyclic analog, Tyr-C[D-Glu-Phe-gPhe-D-rLeu] 14, which was known as having three distinct cis-trans isomers, gave rise to apparently different conformational analog arousing only trans isomer. In the receptor binding assay, it showed tremendously high selectivity toward ${\mu}$ receptor $({\delta}/{\mu}=160)$.

Design and Synthesis of New Amides and Thioamides Derived from 3,4-Ethylenedioxythiophene as Potential Anticonvulsants

  • Kulandasamy, Ravi;Adhikari, Airody Vasudeva;Stables, James P.
    • Bulletin of the Korean Chemical Society
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    • v.31 no.11
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    • pp.3318-3326
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    • 2010
  • Five new series of 3,4-ethylenedioxythiophene derivatives carrying important pharamacophores, viz., amide, ester, ether and active secondary aryl moieties have been designed and synthesized through multistep reactions starting from thiodiglycolic ester and diethyl oxalate. They have been characterized by elemental and spectral data. All the target compounds have been screened for their anticonvulsant activity at three different models viz. maximal electroshock (MES), subcutaneous metrazole (scMET), and 6 Hz screen and evaluated for their neurotoxicity in rotorod model. Compound 6a emerged as lead with no neurotoxicity. All the five series of compounds are safe in the toxicity studies at the maximum dose of 300 mg/kg of body weight. Amongst the tested compounds, the ester pharmacophore with thioamide fragment has showed better activity than the other analogs.

Scalarane-type Sesterterpenes from the Philippines Sponge Hyrtios sp.

  • Choi, Jae-Hyeong;Lee, Hyi-Seung;Campos, Wilfredo L.
    • Ocean and Polar Research
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    • v.42 no.1
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    • pp.15-20
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    • 2020
  • The marine sponge Hyrtios sp. collected in the Philippines was extracted and partitioned. The resulting organic layer was purified by C18 reversed-phase column chromatography and HPLC to achieve the separation of nine scalarane-type sesterterpenes, including one new compound with eight known scalarane analogs. The chemical structures of the isolated compounds 1-9 were elucidated by 1D and 2D NMR and MS data analysis. All nine compounds were evaluated for their antibacterial activities against three Gram-positive and three Gram-negative bacteria. The compound 3 exhibited potent antibacterial activities against Bacillus subtilis and Micrococcus luteus. The compounds 7 and 9 displayed considerable activities against Bacillus subtilis and the others had moderate results.