Mueller, Klaus and Sellmer, Andreas and Wiegrebe, Wolfgang (1999) Potential antipsoriatic agents: Lapacho compounds as potent inhibitors of HaCaT cell growth. JOURNAL OF NATURAL PRODUCTS, 62 (8). pp. 1134-1136. ISSN 0163-3864, 1520-6025
Full text not available from this repository. (Request a copy)Abstract
A number of lapacho compounds, representing the most common constituents of the inner bark of Tabebuia impetiginosa, together with some synthetic analogues, were evaluated in vitro against the growth of the human keratinocyte cell line HaCaT. With an IC50 value of 0.7 mu M, beta-lapachone (4) displayed activity comparable to that of the antipsoriatic drug anthralin. 2-Acetyl-8-hydroxynaphtho[2,3-b]furan-4,9-dione (7), which was prepared in a four-step synthesis from 2,8-dihydroxy-1,4-naphthoquinone, was the most potent inhibitor among the known lapacho-derived compounds and inhibited cell growth with an IC50 value of 0.35 mu M Furthermore, other active constituents of lapacho inhibited keratinocyte growth, with IC50 values in the range of 0.5-3.0 mu M. However, as already observed with anthralin, treatment of HaCaT cells with these potent lapacho compounds also caused remarkable damage to the plasma membrane. This was documented by leakage of lactate dehydrogenase into the culture medium, which significantly exceeded that of the vehicle control. Because of their potent activity against the growth of human keratinocytes, some lapacho-derived compounds appear to be promising as effective antipsoriatic agents.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | MODULATED REDOX PROPERTIES; PROSTATE-CANCER CELLS; BETA-LAPACHONE; TABEBUIA-AVELLANEDAE; HYDROGEN-PEROXIDE; ANTICANCER AGENTS; FREE-RADICALS; DERIVATIVES; NAPHTHOQUINONES; APOPTOSIS; |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Prof. Wiegrebe |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 11 Jan 2023 13:56 |
| Last Modified: | 11 Jan 2023 13:56 |
| URI: | https://pred.uni-regensburg.de/id/eprint/49093 |
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