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Title 

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

Authors 

Tae-Hoon KangE I HwangBong Sik YunC S ShinSung Uk Kim

Publisher 

Pharmaceutical Society of Japan

Issue Date 

2008

Citation 

Biological & Pharmaceutical Bulletin, vol. 31, no. 4, pp. 755-759

Keywords 

8,20 dihydroxy 9(11),13 abietadien 12 onechitin synthasechitin synthase 2chitin synthase 3antifungal activitydrug activityminimum inhibitory concentration

Abstract 

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.

ISSN 

0918-6158

Link 

http://dx.doi.org/10.1248/bpb.31.755

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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