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Systematic synthesis of low-molecular weight fucoidan derivatives and their effect on cancer cells
Akihiro Kasai1, Shinsuke Arafuka, Nozomi Koshiba
1Department of Applied Chemistry, Faculty of Science and Technology, Keio University, 3-14-1 Hoyoshi, Kohoku-ku, Yokohama 223-8522, Japan. dtak@applc.keio.ac.jp toshima@applc.keio.ac.jp.
Abstract:
Low-molecular weight type I and II fucoidan derivatives with different sulfation patterns were designed and systematically synthesized from the corresponding common key intermediate and their anti-proliferative activities and apoptosis-inducing activities against human breast cancer (MCF-7) and human cervical epithelioid carcinoma (HeLa) cells were evaluated. Our results demonstrated that one of the type II fucoidan derivatives, 9, effectively reduced the number of viable MCF-7 and HeLa cells in a dose-dependent manner without causing cytotoxicity toward normal WI-38 cells, and that the anti-proliferative activity of 9 was comparable to that of fucoidan 2 isolated from Fucus vesiculosus. Moreover, it was found that both 2 and 9 exhibited similar apoptosis-inducing activities through activation of caspase-8 and -9 on MCF-7 and HeLa cells, respectively.
Insights
Novel fucoidan derivatives show potent anti-cancer effects. Compound 9 effectively reduced proliferation in breast and cervical cancer cells without harming normal cells, indicating therapeutic potential.
Area of Science:
- Marine biotechnology
- Carbohydrate chemistry
- Cancer research
Background:
- Fucoidan, a sulfated polysaccharide from brown algae, exhibits diverse biological activities.
- Investigating fucoidan derivatives offers opportunities for developing novel anti-cancer agents.
- Understanding structure-activity relationships is crucial for optimizing fucoidan's therapeutic potential.
Purpose of the Study:
- To synthesize and evaluate low-molecular weight fucoidan derivatives with varying sulfation patterns.
- To assess the anti-proliferative and apoptosis-inducing activities of these derivatives against human cancer cell lines.
- To compare the efficacy of promising derivatives with naturally occurring fucoidan.
Main Methods:
- Systematic synthesis of type I and II fucoidan derivatives from a common intermediate.
- In vitro evaluation of anti-proliferative activity against MCF-7 (breast) and HeLa (cervical) cancer cells.
- Assessment of cytotoxicity against normal WI-38 cells.
- Apoptosis induction assays, including caspase-8 and caspase-9 activation analysis.
Main Results:
- Fucoidan derivative 9 demonstrated significant dose-dependent anti-proliferative effects on MCF-7 and HeLa cells.
- Derivative 9 exhibited comparable anti-proliferative activity to fucoidan 2 (from Fucus vesiculosus).
- Neither derivative 2 nor 9 showed cytotoxicity towards normal WI-38 cells.
- Both derivatives 2 and 9 effectively induced apoptosis in cancer cells via caspase-8 and -9 activation.
Conclusions:
- Low-molecular weight fucoidan derivatives, particularly type II derivative 9, possess potent anti-cancer properties.
- Derivative 9 is a promising candidate for further investigation as a safe and effective anti-cancer therapeutic.
- The study highlights the potential of chemically modified fucoidans in cancer treatment.
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