Chitin synthase 2 inhibitory activity of 0-methyl pisiferic acid and 8,20-dihydroxy-9(11),13-abietadien-12-one, isolated from Chamaecyparis pisifera = 화백으로부터 분리한 0-methyl pisiferic acid와 8,20-dihydroxy-9(11),13-abietadien-12-one 화합물의 키틴
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- Chitin synthase 2 inhibitory activity of 0-methyl pisiferic acid and 8,20-dihydroxy-9(11),13-abietadien-12-one, isolated from Chamaecyparis pisifera = 화백으로부터 분리한 0-methyl pisiferic acid와 8,20-dihydroxy-9(11),13-abietadien-12-one 화합물의 키틴
- Tae-Hoon Kang; E I Hwang; Bong Sik Yun; C S Shin; Sung Uk Kim
- Bibliographic Citation
- Biological & Pharmaceutical Bulletin, vol. 31, no. 4, pp. 755-759
- Publication Year
- In the course of search for potent chitin synthase inhibitors from plant extracts, the chitin synthase 2 inhibitors, O-methyl pisiferic acid and 8,20-dihydroxy-9(11),13-abietadien-12-one which have diterpene skeleton, were isolated from the leaves of Chamaecyparis pisifera. These compounds inhibited chitin synthase 2 of Saccharomyces cerevisiae with the IC50 values of 5.8 and 226.4 μM, respectively. Especially, O-methyl pisiferic acid showed 15.3-fold stronger inhibitory activity than polyoxin D (IC50=88.6 μM), a well-known chitin synthase inhibitor. These compounds exhibited weaker inhibitory activities against chitin synthase 1 than chitin synthase 2, whereas it showed no inhibitory activity for chitin synthase 3. The compound exhibited mixed competitive inhibition with respect to UDP-N-acetyl-D-glucosamine as substrate (Ki=5 μM). These results indicated that O-methyl pisiferic acid is a specific inhibitor of chitin synthase 2. The compound also inhibited chitin synthase 1 of Candida albicans, which represents analogues to chitin synthase 2 of S. cerevisiae, with an IC50 of 75.6 μM, which represents 1.8-fold weaker activity than that of polyoxin D. Although O-methyl pisiferic acid has been reported for antibacterial and insecticidal activities, the present study is the first report on its inhibitory activity against chitin synthase 2.
- Antifungal activity; Chamaecyparis pisifera; Chitin synthase inhibitor; O-methyl pisiferic acid
- Pharmaceutical Soc Japan
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- 1. Journal Articles > Journal Articles
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