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  2. 土肥 博史

土肥 博史

ドヒ ヒロフミ  (Hirofumi Dohi)

基本情報

所属
千葉大学 大学院園芸学研究院植物生命科学講座 准教授
学位
博士（工学）(2002年3月 名古屋大学)
研究者番号
10345928
ORCID ID
 https://orcid.org/0000-0001-9087-995X
J-GLOBAL ID
201801004283808215
researchmap会員ID
B000300869

研究キーワード

 5

研究分野

 2

経歴

 14
もっとみる

学歴

 3

委員歴

 1

受賞

 2

主要な論文

 41
  • Siswina, Tessa, Mia Miranti, Dadan Sumiarsa, Eti Apriyanti, Hirofumi Dohi, Dikdik Kurnia
    Molecules 2023年11月22日  査読有り
    <jats:p>Along with the increasing resistance of Candida spp. to some antibiotics, it is necessary to find new antifungal drugs, one of which is from the medicinal plant Red Betel (Piper crocatum). The purpose of this research is to isolate antifungal constituents from P. crocatum and evaluate their activities as ergosterol biosynthesis inhibitors via an in silico study of ADMET and drug-likeness analysis. Two new active compounds 1 and 2 and a known compound 3 were isolated, and their structures were determined using spectroscopic methods, while their bioactivities were evaluated via in vitro and in silico studies, respectively. Antifungal compound 3 was the most active compared to 1 and 2 with zone inhibition values of 14.5, 11.9, and 13.0 mm, respectively, at a concentration of 10% w/v, together with MIC/MFC at 0.31/1.2% w/v. Further in silico study demonstrated that compound 3 had a stronger ΔG than the positive control and compounds 1 and 2 with −11.14, −12.78, −12.00, and −6.89 Kcal/mol against ERG1, ERG2, ERG11, and ERG24, respectively, and also that 3 had the best Ki with 6.8 × 10−3, 4 × 10−4, 1.6 × 10−3, and 8.88 μM. On the other hand, an ADMET analysis of 1–3 met five parameters, while 1 had one violation of Ro5. Based on the research data, the promising antifungal constituents of P. crocatum allow P. crocatum to be proposed as a new antifungal candidate to treat and cure infections due to C. albicans.</jats:p>
  • Hirofumi Dohi, Risa Sakurai, Manami Tamura, Ryota Komai, Yoshihiro Nishida
    Journal of Carbohydrate Chemistry 1-21 2021年3月31日  査読有り筆頭著者責任著者
  • Asako Takahashi, Hirofumi Dohi, Yukari Egashira, Shizuka Hirai
    Phytotherapy research : PTR 34(6) 1358-1366 2020年6月  査読有り
    Osteoporosis is associated with increase in fat tissue in bone marrow in humans. Mesenchymal stem cells in bone marrow are induced to differentiate into osteoblasts rather than adipocytes by the stimulation of peroxisome proliferator-activated receptor (PPAR) γ antagonists. PPARγ antagonists are expected to be useful to prevent osteoporosis by regulating the lineages of mesenchymal stem cells in bone marrow, as well as the prevention of obesity. In this study, we explored natural components suppressing PPARγ transcriptional activity in rosemary. Separation of active fraction of rosemary extract by repeated high performance liquid chromatograph and PPARγ luciferase reporter assay identified erucic acid, one of the monounsaturated fatty acids, as an active component. Twenty-five-micrometer erucic acid significantly decreased PPARγ luciferase activity and enhanced the differentiation of mouse-delivered C3H10T1/2 cells into osteoblasts rather than adipocytes. Furthermore, 25-μM erucic acid significantly decreased the expression of adipocyte marker genes, while accelerating osteoblast marker genes. In conclusion, erucic acid is a novel natural component derived from rosemary regulating mesenchymal stem cell differentiation via suppression of PPARγ transcriptional activity.
  • Hirofumi Dohi, Regis Perion, Maxime Durka, Michael Bosco, Yvain Roue, Francois Moreau, Sylvestre Grizot, Arnaud Ducruix, Sonia Escaich, Stephane P. Vincent
    CHEMISTRY-A EUROPEAN JOURNAL 14(31) 9530-9539 2008年  査読有り筆頭著者
    Heptosides are found in important bacterial glycolipids such as lipopolysaccliaride (LPS). the biosynthesis of which is targeted for the develoopment of novel antibacterial agents. This work describes the synthesis of a fluorinated analogue of ADP-L-glycero-beta-D-manno-heptopyranose, the donor substrate of the heptosyl transferase WaaC, which catalyzes the incorporation of this carbohydrate into LPS. Synthetically, the key step for the preparation of ADP-2F-heptose is the Simultaneous and stercoselective installation of both the fluorine atom at C-2 and the phosphoryl group at C-1 through a selectfluor-mediated (selectfluor= 1-clilol-omettivi-4-fluorodiazonia-bicy[2.2.2]octane bis(triflate)) electrophific addition/nucleophilic substitution involving a heptosylplycal. Therefore, we detail in this article 1) the stereoselective preparation of the key intermediates heptosylglycals, 2) the development of a new fluorophosphorylation procedure allowing an excellent beta-gluco stereoselectivity with "all-equatorial" glycals, 3) the synthesis of the target ADP-2F-heptose, and 4) some comments on the contacts observed between the fluorine atom of the final molecule and the protein in the crystallographic structure of heptosyltransferase WaaC.
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MISC

 4

講演・口頭発表等

 122

担当経験のある科目(授業)

 16
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所属学協会

 5

共同研究・競争的資金等の研究課題

 5

産業財産権

 1
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