The Experts below are selected from a list of 66 Experts worldwide ranked by ideXlab platform
Seung Wook Ham - One of the best experts on this subject based on the ideXlab platform.
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a novel Organogermanium protected atopic dermatitis induced by oxazolone
ChemInform, 2010Co-Authors: Doo Hyeon Lim, Junga Seo, Kyungmin Lim, Seung Wook HamAbstract:A novel Organogermanium Compound (IV) with ascorbic acid as hydrophilic moiety is synthesized and the anti-inflammatory and barrier protecting effects are investigated for chronic oxazolone-induced murine atopic dermatitis.
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a novel Organogermanium protected atopic dermatitis induced by oxazolone
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Doo Hyeon Lim, Junga Seo, Kyungmin Lim, Seung Wook HamAbstract:Atopic dermatitis (AD) is a chronic inflammatory disease of the skin that is often associated with other atopic diseases, such as asthma and allergic rhinitis. Although topical steroids have widely been prescribed for patients with AD, skin abnormalities are frequently observed after prolonged steroid treatment. In this study, a novel water-soluble Organogermanium Compound (Ge-Vit) was prepared because Organogermanium is a known INF-γ inducer. The Ge-Vit treatment decreased the basal TEWL and IgE production and attenuated the disruption of the skin barrier function in a murine model of chronic contact dermatitis. The histological examination further supported the anti-AD activities. These results suggested that Ge-Vit can be a useful drug candidate for treating atopic dermatitis.
Takashi Nakamura - One of the best experts on this subject based on the ideXlab platform.
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Quantitative assessment of the interactions between the Organogermanium Compound and saccharides using an NMR reporter molecule.
Carbohydrate research, 2020Co-Authors: Yasuhiro Shimada, Takashi Nakamura, Katsuyuki Sato, Mika Masaki, Yoshihiko TokujiAbstract:Abstract Poly-trans-[(2-carboxyethyl)germasesquioxane], Ge-132, is a water-soluble Organogermanium Compound reported to have physiological effects such as immunostimulatory and antiviral effects. The hydrolysate of Ge-132, 3-(trihydroxygermyl)propanoic acid (THGP), can interact with diols; therefore, it likely can interact with diol-containing sugars in sugar chains, glycoproteins, and glycolipids, which have important physiological functions. In this study, we quantitatively assessed the ability of THGP to interact with saccharides using nuclear magnetic resonance (NMR) spectroscopy and THGP derivatives. THGP was complexed by binding its trihydroxy group with saccharides in aqueous solutions via the cis-diol group rather than the trans-diol group. The spectra of THGP and monosaccharides indicated that THGP has a higher affinity for ketose than aldose. Moreover, the complexation ability between THGP and saccharides was influenced by the number of cis-diol groups on the saccharide structure. Thus, interactions of THGP with important biological sugars might be involved in the physiological functions of Ge-132.
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The Organogermanium Compound THGP Suppresses Melanin Synthesis via Complex Formation with L-DOPA on Mushroom Tyrosinase and in B16 4A5 Melanoma Cells.
International journal of molecular sciences, 2019Co-Authors: Junya Azumi, Tomoya Takeda, Yasuhiro Shimada, Hisashi Aso, Takashi NakamuraAbstract:The Organogermanium Compound 3-(trihydroxygermyl)propanoic acid (THGP) has various biological activities. We previously reported that THGP forms a complex with cis-diol structures. L-3,4-Dihydroxyphenylalanine (L-DOPA), a precursor of melanin, contains a cis-diol structure in its catechol skeleton, and excessive melanin production causes skin darkening and staining. Thus, the cosmetic field is investigating substances that suppress melanin production. In this study, we investigated whether THGP inhibits melanin synthesis via the formation of a complex with L-DOPA using mushroom tyrosinase and B16 4A5 melanoma cells. The ability of THGP to interact with L-DOPA was analyzed by 1H-NMR, and the influence of THGP and/or kojic acid on melanin synthesis was investigated. We also examined the effect of THGP on cytotoxicity, tyrosinase activity, and gene expression and found that THGP interacted with L-DOPA, a precursor of melanin with a cis-diol structure. The results also showed that THGP inhibited melanin synthesis, exerted a synergistic effect with kojic acid, and did not affect tyrosinase activity or gene expression. These results suggest that THGP is a useful substrate that functions as an inhibitor of melanogenesis and that its effect is enhanced by combination with kojic acid.
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Organogermanium Compound, Ge-132, forms complexes with adrenaline, ATP and other physiological cis-diol Compounds
Future medicinal chemistry, 2015Co-Authors: Takashi Nakamura, Yasuhiro Shimada, Tomoya Takeda, Katsuyuki Sato, Mitsuo Akiba, Haruhiko FukayaAbstract:Background: In mammals, adrenaline and ATP are life-essential vicinal diol and cis-diol functional groups. Here, we show that interactions between a safe Organogermanium Compound and these cis-diol Compounds have the potential to regulate physiological functions. In addition, we represent a possible new druggable target for controlling the action of cis-diol Compounds. Results: We analyzed a single crystal structure of Organogermanium 3-(trihydroxygermyl)propanoic acid (THGPA), a hydrolysate of safe Ge-132, in complex with catecholamine (adrenaline and noradrenaline), and evaluated the affinity between several cis-diol Compounds and THGPA by NMR. An in vitro study using normal human epidermal keratinocytes was performed to investigate the inhibition of cis-diol Compound-stimulated receptors by THGPA. At high concentration, THGPA inhibited the calcium influx caused by adrenaline and ATP. Conclusion: This study demonstrates that THGPA can modify cis-diol-mediated cell-to-cell signaling.
Yasuhiro Shimada - One of the best experts on this subject based on the ideXlab platform.
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Quantitative assessment of the interactions between the Organogermanium Compound and saccharides using an NMR reporter molecule.
Carbohydrate research, 2020Co-Authors: Yasuhiro Shimada, Takashi Nakamura, Katsuyuki Sato, Mika Masaki, Yoshihiko TokujiAbstract:Abstract Poly-trans-[(2-carboxyethyl)germasesquioxane], Ge-132, is a water-soluble Organogermanium Compound reported to have physiological effects such as immunostimulatory and antiviral effects. The hydrolysate of Ge-132, 3-(trihydroxygermyl)propanoic acid (THGP), can interact with diols; therefore, it likely can interact with diol-containing sugars in sugar chains, glycoproteins, and glycolipids, which have important physiological functions. In this study, we quantitatively assessed the ability of THGP to interact with saccharides using nuclear magnetic resonance (NMR) spectroscopy and THGP derivatives. THGP was complexed by binding its trihydroxy group with saccharides in aqueous solutions via the cis-diol group rather than the trans-diol group. The spectra of THGP and monosaccharides indicated that THGP has a higher affinity for ketose than aldose. Moreover, the complexation ability between THGP and saccharides was influenced by the number of cis-diol groups on the saccharide structure. Thus, interactions of THGP with important biological sugars might be involved in the physiological functions of Ge-132.
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The Organogermanium Compound THGP Suppresses Melanin Synthesis via Complex Formation with L-DOPA on Mushroom Tyrosinase and in B16 4A5 Melanoma Cells.
International journal of molecular sciences, 2019Co-Authors: Junya Azumi, Tomoya Takeda, Yasuhiro Shimada, Hisashi Aso, Takashi NakamuraAbstract:The Organogermanium Compound 3-(trihydroxygermyl)propanoic acid (THGP) has various biological activities. We previously reported that THGP forms a complex with cis-diol structures. L-3,4-Dihydroxyphenylalanine (L-DOPA), a precursor of melanin, contains a cis-diol structure in its catechol skeleton, and excessive melanin production causes skin darkening and staining. Thus, the cosmetic field is investigating substances that suppress melanin production. In this study, we investigated whether THGP inhibits melanin synthesis via the formation of a complex with L-DOPA using mushroom tyrosinase and B16 4A5 melanoma cells. The ability of THGP to interact with L-DOPA was analyzed by 1H-NMR, and the influence of THGP and/or kojic acid on melanin synthesis was investigated. We also examined the effect of THGP on cytotoxicity, tyrosinase activity, and gene expression and found that THGP interacted with L-DOPA, a precursor of melanin with a cis-diol structure. The results also showed that THGP inhibited melanin synthesis, exerted a synergistic effect with kojic acid, and did not affect tyrosinase activity or gene expression. These results suggest that THGP is a useful substrate that functions as an inhibitor of melanogenesis and that its effect is enhanced by combination with kojic acid.
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The Organogermanium Compound Ge-132 Interacts with Nucleic Acid Components and Inhibits the Catalysis of Adenosine Substrate by Adenosine Deaminase
Biological Trace Element Research, 2018Co-Authors: Yasuhiro Shimada, Tomoya Takeda, Katsuyuki Sato, Yoshihiko TokujiAbstract:Poly- trans -[(2-carboxyethyl)germasesquioxane] (Ge-132) is a water-soluble Organogermanium Compound that exerts various physiological effects, including anti-inflammatory activity and pain relief. In water, Ge-132 is hydrolyzed to 3-(trihydroxygermyl)propanoic acid (THGP), which in turn is capable of interacting with cis -diol Compounds through its trihydroxy group, indicating that this Compound could also interact with diol-containing nucleic acid constituents. In this study, we evaluated the ability of THGP to interact with nucleosides or nucleotides via nuclear magnetic resonance (NMR) analysis. In addition, we evaluated the effect of added THGP on the enzymatic activity of adenosine deaminase (ADA) when using adenosine or 2′-deoxyadenosine as a substrate. In solution, THGP indeed formed complexes with nucleotides or nucleosides through their cis -diol group. Moreover, the ability of THGP to form complexes with nucleotides was influenced by the number of phosphate groups present on the ribose moiety. Notably, THGP also inhibited the catalysis of adenosine by ADA in a concentration-dependent manner. Thus, interactions between THGP and important biological nucleic acid constituents might be implicated in the physiological effects of Ge-132.
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Organogermanium Compound, Ge-132, forms complexes with adrenaline, ATP and other physiological cis-diol Compounds
Future medicinal chemistry, 2015Co-Authors: Takashi Nakamura, Yasuhiro Shimada, Tomoya Takeda, Katsuyuki Sato, Mitsuo Akiba, Haruhiko FukayaAbstract:Background: In mammals, adrenaline and ATP are life-essential vicinal diol and cis-diol functional groups. Here, we show that interactions between a safe Organogermanium Compound and these cis-diol Compounds have the potential to regulate physiological functions. In addition, we represent a possible new druggable target for controlling the action of cis-diol Compounds. Results: We analyzed a single crystal structure of Organogermanium 3-(trihydroxygermyl)propanoic acid (THGPA), a hydrolysate of safe Ge-132, in complex with catecholamine (adrenaline and noradrenaline), and evaluated the affinity between several cis-diol Compounds and THGPA by NMR. An in vitro study using normal human epidermal keratinocytes was performed to investigate the inhibition of cis-diol Compound-stimulated receptors by THGPA. At high concentration, THGPA inhibited the calcium influx caused by adrenaline and ATP. Conclusion: This study demonstrates that THGPA can modify cis-diol-mediated cell-to-cell signaling.
Doo Hyeon Lim - One of the best experts on this subject based on the ideXlab platform.
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a novel Organogermanium protected atopic dermatitis induced by oxazolone
ChemInform, 2010Co-Authors: Doo Hyeon Lim, Junga Seo, Kyungmin Lim, Seung Wook HamAbstract:A novel Organogermanium Compound (IV) with ascorbic acid as hydrophilic moiety is synthesized and the anti-inflammatory and barrier protecting effects are investigated for chronic oxazolone-induced murine atopic dermatitis.
-
a novel Organogermanium protected atopic dermatitis induced by oxazolone
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Doo Hyeon Lim, Junga Seo, Kyungmin Lim, Seung Wook HamAbstract:Atopic dermatitis (AD) is a chronic inflammatory disease of the skin that is often associated with other atopic diseases, such as asthma and allergic rhinitis. Although topical steroids have widely been prescribed for patients with AD, skin abnormalities are frequently observed after prolonged steroid treatment. In this study, a novel water-soluble Organogermanium Compound (Ge-Vit) was prepared because Organogermanium is a known INF-γ inducer. The Ge-Vit treatment decreased the basal TEWL and IgE production and attenuated the disruption of the skin barrier function in a murine model of chronic contact dermatitis. The histological examination further supported the anti-AD activities. These results suggested that Ge-Vit can be a useful drug candidate for treating atopic dermatitis.
Kyungmin Lim - One of the best experts on this subject based on the ideXlab platform.
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a novel Organogermanium protected atopic dermatitis induced by oxazolone
ChemInform, 2010Co-Authors: Doo Hyeon Lim, Junga Seo, Kyungmin Lim, Seung Wook HamAbstract:A novel Organogermanium Compound (IV) with ascorbic acid as hydrophilic moiety is synthesized and the anti-inflammatory and barrier protecting effects are investigated for chronic oxazolone-induced murine atopic dermatitis.
-
a novel Organogermanium protected atopic dermatitis induced by oxazolone
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Doo Hyeon Lim, Junga Seo, Kyungmin Lim, Seung Wook HamAbstract:Atopic dermatitis (AD) is a chronic inflammatory disease of the skin that is often associated with other atopic diseases, such as asthma and allergic rhinitis. Although topical steroids have widely been prescribed for patients with AD, skin abnormalities are frequently observed after prolonged steroid treatment. In this study, a novel water-soluble Organogermanium Compound (Ge-Vit) was prepared because Organogermanium is a known INF-γ inducer. The Ge-Vit treatment decreased the basal TEWL and IgE production and attenuated the disruption of the skin barrier function in a murine model of chronic contact dermatitis. The histological examination further supported the anti-AD activities. These results suggested that Ge-Vit can be a useful drug candidate for treating atopic dermatitis.