Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Structure–Activity Relationship of Anti-malarial Allylpyrocatechol Isolated from Piper betle
Satoru TamuraAkihito MiyoshiTomikazu KawanoToshihiro HoriiSawako ItagakiNobutoshi Murakami
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2020 Volume 68 Issue 8 Pages 784-790

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Abstract

Malaria disease remains a serious worldwide health problem. In South-East Asia, one of the malaria infection “hot-spots,” medicinal plants such as Piper betle have traditionally been used for the treatment of malaria, and allylpyrocatechol (1), a constituent of P. betle, has been shown to exhibit anti-malarial activities. In this study, we verified that 1 showed in vivo anti-malarial activity through not only intraperitoneal (i.p.) but also peroral (p.o.) administration. Additionally, some analogs of 1 were synthesized and the structure–activity relationship was analyzed to disclose the crucial sub-structures for the potent activity.

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