• Proceedings of the Korean Society of Toxicology Conference
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• 2003.10b
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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)

• Archives of Pharmacal Research
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• v.27 no.5
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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.

• Proceedings of the Korea Environmental Mutagen Society Conference
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• 2003.10a
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• pp.171-171
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• 2003