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Screening of promising chemotherapeutic candidates from plants extracts
Junei Kinjo1, Daisuke Nakano2, Toshihiro Fujioka2
1Faculty of Pharmaceutical Sciences, Fukuoka University, 8-19-1 Nanakuma, Jonan-ku, Fukuoka, 814-0180, Japan. kinjojun@fukuoka-u.ac.jp.
Abstract:
Over the course of our studies investigating anti-proliferative properties of compounds originating from plants against human gastric adenocarcinoma (MK-1), human uterine carcinoma (HeLa), murine melanoma (B16F10), and two human T cell lymphotropic virus type 1 (HTLV-1)-infected T-cell lines (MT-1 and MT-2), we have screened 582 extracted samples obtained from a variety of parts from 370 plants. A few extracts showed anti-proliferative activity against all cell lines, but upon further investigation, toxicity toward selected cell lines was recognized. After activity-guided fractionation, isolation of the active principles was achieved. Structure-activity relationship studies identified the components and functionalities responsible for the specific selectivity against each cancer cell line. The effect of polyacetylenes against MK-1 cells was more potent than against HeLa and B16F10 cells. The compound having a 3,4-dihydroxyphenethyl group also showed an anti-proliferative effect against B16F10 cells. Some 6-methoxyflavone derivatives and 8-hydroxy furanocoumarins were good inhibitors of HeLa cell growth. The 17 compounds whose EC50 values were less than 1 nM did not show specific cellular selectivity. Because the cytotoxic effect of 24, 25-dihydrowithanolide D toward control cells was observed at a concentration about 100 times higher than those for the cancer cell lines, withanolide was identified as the most promising chemotherapeutic candidate in our experiments.
Insights
Researchers screened 582 plant extracts for anti-cancer properties. Withanolide emerged as a promising chemotherapeutic candidate due to its selective cytotoxicity against cancer cell lines.
Area of Science:
- Natural Product Chemistry
- Pharmacology
- Cancer Biology
Background:
- Investigating plant-derived compounds for anti-proliferative effects against various cancer cell lines.
- Screening of 582 extracts from 370 plants to identify potential anti-cancer agents.
Purpose of the Study:
- To identify and characterize plant-derived compounds with selective anti-proliferative activity against human gastric adenocarcinoma (MK-1), human uterine carcinoma (HeLa), and murine melanoma (B16F10) cells.
- To determine the structure-activity relationships of identified compounds.
- To evaluate the chemotherapeutic potential of promising candidates.
Main Methods:
- Activity-guided fractionation and isolation of active compounds from plant extracts.
- Structure-activity relationship (SAR) studies to identify key structural features responsible for activity and selectivity.
- Cytotoxicity assays to determine EC50 values and selectivity against cancer cell lines and control cells.
Main Results:
- Several plant extracts exhibited anti-proliferative activity, though some showed general toxicity.
- Specific compounds like polyacetylenes, a 3,4-dihydroxyphenethyl derivative, 6-methoxyflavone derivatives, and 8-hydroxy furanocoumarins demonstrated selective activity against MK-1, B16F10, and HeLa cells, respectively.
- 24, 25-dihydrowithanolide D showed significant selective cytotoxicity, with a 100-fold higher effective concentration against control cells compared to cancer cells.
Conclusions:
- Withanolide compounds, particularly 24, 25-dihydrowithanolide D, represent promising candidates for further development as selective chemotherapeutic agents.
- Understanding SAR is crucial for optimizing anti-cancer drug design and minimizing off-target effects.
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