Antitumor activity of flavones with special references to skullcapflavon Ⅱ = Skullcapflavon Ⅱ 를 주로한 후라본류의 항암 작용

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On screening various oriental herbs which have long been used as medicines to treat some cancer-like diseases we have found in our laboratory that the root extracts of $\mbox{\underline{Scutellaria}}$ $\mbox{\underline{baicalensis}}$ have strong inhibitory effect on mouse leukemia L1210 cells. The present investigation was planed to isolate and identify the cytotoxic principle. Furthermore, The substance and its analogues were synthesized to search a pharmacophoric moiety and obtain enough amount for the quantitative animal tests. The work for clarifying the cytotoxic mechanism was also carried out. To isolate the cytotoxic principle the ether extract of the roots was chromatographed on silica gel and the fractions obtained were tested on the L1210 cells. By repeated chromatography and crystallization the cytotoxic substance was isolated, and its structure was identified as skullcapflavon II (5,2``-dihydroxy-6,7,8,6``-tetramethoxyflavone) based on the chemical and spectral data obtained. The majority of other flavones isolated from $\mbox{\underline{S.}}$ $\mbox{\underline{baicalensis}}$ showed no significant inhibition on L1210 growth. From the modification of A-ring of baicalein, 5,8-dihydroxy-6,7-dimethoxyflavone (III) was found as a moderate cytotoxic flavone ($ED_50=7.5μg/ml$), but any obivious role of A-ring for the activity was not observed except that the fully oxidized A-ring was essential for the cytotoxic flavones. To observe the relation between the activity and the substitutions in B-ring of a flavone, skullcapflavon II and its analogues were synthesized by Baker-Venkataraman rearrangement, partial debenzylation and methylation. By this method skullcapflavon II was obtained from 2,6-dibenzyloxybenzoyl chloride and 2,6-dihydroxy-3,4,5-trimethoxyacetophenone with 33% yield and other analogues with comparable yields. Among the synthesized flavones, 5,2``,6``-trihydroxy-6,7,8-trimethoxyflavone (XVII) and skullcapflavon II (I) showed the strong cytotoxi...
Pack, Moo-Young박무영
한국과학기술원 : 생물공학과,
Issue Date
60888/325007 / 000795077

학위논문(박사) - 한국과학기술원 : 생물공학과, 1985.8, [ x, 122 p. ]

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