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We purified several hundred mgs of four major theaflavins (theaflavin, theaflavin-3-O-gallate, theaflavin-3'-O-gallate, and theaflavin-3,3'-O-digallate). Among the 25 hTAS2Rs expressed in HEK293T cells, hTAS2R39 and hTAS2R14 were activated by theaflavins. Both hTAS2R39 and hTAS2R14 responded to theaflavin-3'-O-gallate. In addition, hTAS2R39 was activated by theaflavin and theaflavin-3,3'-O-gallate, but not by theaflavin-3-O-gallate. In contrast, hTAS2R14 responded to theaflavin-3-O-gallate.


Toyomi Yamazaki, Miki Sagisaka, Riko Ikeda, Toshiyuki Nakamura, Noriko Matsuda, Takeshi Ishii, Tsutomu Nakayama, Tatsuo Watanabe. The human bitter taste receptor hTAS2R39 is the primary receptor for the bitterness of theaflavins. Bioscience, biotechnology, and biochemistry. 2014;78(10):1753-6

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PMID: 25273142

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