• 제목/요약/키워드: Asiatic acid derivatives

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Structure-Activity Relationship Study of Asiatic Acid Derivatives for New Wound Healing Agent

  • Jeong, Byeong-Seon
    • Archives of Pharmacal Research
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    • 제29권7호
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    • pp.556-562
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    • 2006
  • Ten semi-synthetic derivatives of asiatic acid were prepared and their wound healing effects were evaluated by employing a tensile strength assay and a wound area assay. Among them, ethoxymethyl 2-oxo-3,23-isopropylidene-asiatate (12) showed the strongest and the fastest wound healing activity. Furthermore, it left the smallest scar after healing.

Structure-Related Cytotoxicity and Anti-Hepatofibric Effect of Asiatic Acid Derivatives in Rat Hepatic Stellate Cell-Line, HSC-T6

  • Dong, Mi-Sook;Jung, Seung-Hyun;Kim, Hyun-Jung;Kim, Jeong-Ran;Zhao, Long-Suan;Lee, Eung-Seok;Lee, Eun-Joo;Yi, Jung-Bum;Lee, Nam-Kyu;Cho, Yong-Baik;Kwak, Wie-Jong;Park, Young-In
    • Archives of Pharmacal Research
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    • 제27권5호
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    • pp.512-517
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    • 2004
  • The structural relationship of 16 asiatic acid (AA) derivatives, including AA and asiaticoside (AS) to cytotoxicity and anti-hepatofibrotic activity in HSC-T6 cells, were investigated. Cytotoxicities of AA derivatives varied from 5.5 $\mu$M to over 2000 $\mu$M of $IC_{50}$/ depending on AA functional group modifications. Substituting the hydroxyl group at the C(2) to N≡C and substituting bulky groups for dihydroxyl groups at (3), (23) of the A-ring increased the cytotoxicity, but keto group at C(11) and benzoyl ester at C(2) were greatly reduced it. Modification of the carboxylic acid group at C28 also reduced the cytotoxicity. The collagen synthesis determined by hydroxyproline content in the cells was inhibited from a maximum of 48% (Zlx-i-85 and 87) to 15% (AS) by AA derivatives. The anti-hepatofibrotic effect of these compounds might be due to the reduced expression of prolyl 4-hydroxylase $\alpha$ and $\beta$ subunits and TIMP2. However, the inhibition of collagen by asiaticoside derivatives did not show any structural-activity relationship.

Structure-Activity Relationship Study of Asiatic Acid Derivatives for New Wound Healing Agent

  • Jew, Sang-Sup;Lim, Doo-Yeon;Park, Sun-Young;Suh, Sung-Ki;Nam, Tae-Kyu;Kim, So-Yeon;Kim, Dong-Sun;Cha, Kyung-Hoe;Park, Eun-Hee;Son, Dong-Whan;Kim, Sang-Gun;Park, Hyeung-Geun
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.340.1-340.1
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    • 2002
  • Centella asiatica is an herbal plant used on different continents by diverse ancient cultures and tribal groups. Historically. the extract has been used as a wound healing agent, The extract has three different triterpenoid ingredients: asiaticoside. asiatic acid, and madecassic acid. It has been reported that its wound healing activity is associated with the modulation of collagen synthesis in the skin dermis. The wound healing property of the extract has led to its commercial introduction under the trade name, Madecrlssol. As part of our program toward the development of new wound healing agents. structere activity relationship (SAR) studies have been performed by modifying asiatic acid. In this communication. the SAR study of esiatic acid for the development of an efficient woind healing agent is reported.

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Structure-Related Cytotoxicity and Anti-Heaptofibric Effect of Asiaticoside Derivatives in Rat Hepatic Stellate Cell Line, Hsc-T6

  • Kim, Jeong-Ran;Jung, Seung-Hyun;Lee, Eung-Seok;Lee, Eun-Joo;Yi, Jung-Bum;Lee, Namkyu;Cho, Yong-Baik;Kwak, Wie-Jong;Park, Young-In
    • 한국독성학회:학술대회논문집
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    • 한국독성학회 2003년도 추계학술대회
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    • pp.171-171
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    • 2003
  • Asiaticoside, a biologically active triterpenoid present in Centella asicatica, has been known to exert a variety of biological effect such as wound-healing, hepatoprotective, anti-inflammatory. In this study, we observed the effect of asiatic acid asiaticoside and its 16 derivatives on the cytotoxicity and the content of hydroxyproline in rat hepatic stellate cell line, HSC-T6 cell as a preliminary study for screening the anti-hepatofibrotic effect.(omitted)

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