Abstract
The anti-Candida potentials of 12 Korean medicinal plants were explored: methanol extracts from Coptis rhizoma and Phellodendron amurense caused significant inhibition of growth of Candida albicans, Candida glabrata, Candida krusei and Candida parapsilosis. The predominant active components of the extracts were the protoberberines berberine and palmatine; the most potent inhibition of growth was exhibited by berberine on C. krusei (MIC < 4 mg/L) and palmatine on C. parapsilosis (MIC 16 mg/L). Both berberine and palmatine inhibited the in-vivo rate of incorporation of L-[methyl/14C]methionine into C-24 of ergosterol in C. albicans (50% inhibition concentration (IC50 values), 25 μM and 300 μM, respectively); this result suggests that sterol 24-methyl transferase (24-SMT) is one of the cellular targets for the antifungal activity of the protoberberines. In-vitro 24-SMT activity in microsomes from the yeast growth form of C. albicans was inhibited by both berberine (inhibition constant (K(i)) 232 μM) and palmatine (K(i) 257 μM) in a non-competitive manner; inhibition of 24-SMT was more marked for the mycelial form than for the yeast growth form of this organism. Palmatine inhibited chitin synthase from both the yeast and mycelial growth phases of C. albicans in a non-competitive manner (K(i) 780 μM). The effects of protoberberines, extracted from established medicinal plants, on both sterol and cell wall biosyntheses in pathogenic fungi indicate that the potential of these compounds, or their semi-synthetic derivatives, as a novel class of antifungal agents should be investigated more fully.
| Original language | English |
|---|---|
| Pages (from-to) | 667-674 |
| Number of pages | 8 |
| Journal | Journal of Antimicrobial Chemotherapy |
| Volume | 43 |
| Issue number | 5 |
| DOIs | |
| Publication status | Published - 1999 Jan 1 |
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All Science Journal Classification (ASJC) codes
- Pharmacology
- Microbiology (medical)
- Pharmacology (medical)
- Infectious Diseases
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Differential inhibitory effects of protoberberines on sterol and chitin biosyntheses in Candida albicans. / Park, Kang Sik; Kang, Kap Chul; Kim, Jai Hyun; Adams, David J.; Johng, Tae Neung; Paik, Young Ki.
In: Journal of Antimicrobial Chemotherapy, Vol. 43, No. 5, 01.01.1999, p. 667-674.Research output: Contribution to journal › Article
TY - JOUR
T1 - Differential inhibitory effects of protoberberines on sterol and chitin biosyntheses in Candida albicans
AU - Park, Kang Sik
AU - Kang, Kap Chul
AU - Kim, Jai Hyun
AU - Adams, David J.
AU - Johng, Tae Neung
AU - Paik, Young Ki
PY - 1999/1/1
Y1 - 1999/1/1
N2 - The anti-Candida potentials of 12 Korean medicinal plants were explored: methanol extracts from Coptis rhizoma and Phellodendron amurense caused significant inhibition of growth of Candida albicans, Candida glabrata, Candida krusei and Candida parapsilosis. The predominant active components of the extracts were the protoberberines berberine and palmatine; the most potent inhibition of growth was exhibited by berberine on C. krusei (MIC < 4 mg/L) and palmatine on C. parapsilosis (MIC 16 mg/L). Both berberine and palmatine inhibited the in-vivo rate of incorporation of L-[methyl/14C]methionine into C-24 of ergosterol in C. albicans (50% inhibition concentration (IC50 values), 25 μM and 300 μM, respectively); this result suggests that sterol 24-methyl transferase (24-SMT) is one of the cellular targets for the antifungal activity of the protoberberines. In-vitro 24-SMT activity in microsomes from the yeast growth form of C. albicans was inhibited by both berberine (inhibition constant (K(i)) 232 μM) and palmatine (K(i) 257 μM) in a non-competitive manner; inhibition of 24-SMT was more marked for the mycelial form than for the yeast growth form of this organism. Palmatine inhibited chitin synthase from both the yeast and mycelial growth phases of C. albicans in a non-competitive manner (K(i) 780 μM). The effects of protoberberines, extracted from established medicinal plants, on both sterol and cell wall biosyntheses in pathogenic fungi indicate that the potential of these compounds, or their semi-synthetic derivatives, as a novel class of antifungal agents should be investigated more fully.
AB - The anti-Candida potentials of 12 Korean medicinal plants were explored: methanol extracts from Coptis rhizoma and Phellodendron amurense caused significant inhibition of growth of Candida albicans, Candida glabrata, Candida krusei and Candida parapsilosis. The predominant active components of the extracts were the protoberberines berberine and palmatine; the most potent inhibition of growth was exhibited by berberine on C. krusei (MIC < 4 mg/L) and palmatine on C. parapsilosis (MIC 16 mg/L). Both berberine and palmatine inhibited the in-vivo rate of incorporation of L-[methyl/14C]methionine into C-24 of ergosterol in C. albicans (50% inhibition concentration (IC50 values), 25 μM and 300 μM, respectively); this result suggests that sterol 24-methyl transferase (24-SMT) is one of the cellular targets for the antifungal activity of the protoberberines. In-vitro 24-SMT activity in microsomes from the yeast growth form of C. albicans was inhibited by both berberine (inhibition constant (K(i)) 232 μM) and palmatine (K(i) 257 μM) in a non-competitive manner; inhibition of 24-SMT was more marked for the mycelial form than for the yeast growth form of this organism. Palmatine inhibited chitin synthase from both the yeast and mycelial growth phases of C. albicans in a non-competitive manner (K(i) 780 μM). The effects of protoberberines, extracted from established medicinal plants, on both sterol and cell wall biosyntheses in pathogenic fungi indicate that the potential of these compounds, or their semi-synthetic derivatives, as a novel class of antifungal agents should be investigated more fully.
UR - http://www.scopus.com/inward/record.url?scp=0032953701&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0032953701&partnerID=8YFLogxK
U2 - 10.1093/jac/43.5.667
DO - 10.1093/jac/43.5.667
M3 - Article
C2 - 10382888
AN - SCOPUS:0032953701
VL - 43
SP - 667
EP - 674
JO - Journal of Antimicrobial Chemotherapy
JF - Journal of Antimicrobial Chemotherapy
SN - 0305-7453
IS - 5
ER -