Studies on Bioactive Natural Products : Plant-Derived Natural Products and Analogues As Anti-HIV Agents

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概要

• 論文の詳細を見る

• In our search for the plant-derived anti-HIV natural products, various classes of compounds, including tannins, coumarins, triterpenes, lignans, alkaloids, and flavonoids were isolated and identified as possible anti-HIV agents. Among the identified anti-HIV compounds, punicalin, suksdorfin, and betulinic acid were regarded as potential lead or model compounds for development of more potent anti-HIV agents. By chemical modifications, these potential leads yielded 3,3'-dibromo-4,4'-dimethoxy-5,6,5',6'-bis(mcthylenedioxy)-2,2'-bis(methoxycarbonyl)biphenyl,3'4'-di-0-(-)-camphanoyl-(+)-cis-khellactone (DCK), and 3-0-(3',3'-dimethyl)-succinyl-betulinic acid (DSB), which demonstrated very potent anti-HIV activities with EC_<50> values of 0.42, 0.00041, and < 0.00035 μM, respectively, and therapeutic index values of >430, 136719, and > 20000, respectively. These compounds have been selected as candidates for the clinical trial study of anti-AIDS agents.

• 日本生薬学会の論文
• 1999-08-20

著者

• 柏田 良樹

  徳島大学薬学部

• 柏田 良樹

  徳島大院薬

• 柏田 良樹

  徳島大学大学院ヘルスバイオサイエンス研究部(薬学系)

• 柏田 良樹

  Faculty Of Pharmaceutical Sciences Kyushu Unversity

• Kashiwada Y

  Niigata Univ. Pharmacy And Applied Life Sci. Niigata Jpn

• Kashiwada Yoshiki

  Niigata College Of Pharmacy

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