TY - JOUR
T1 - Aspergillus species strain m39 produces two naphtho‐γ‐pyrones that reverse drug resistance in human KB cells
AU - Ikeda, Shun‐Ichi ‐I
AU - Sugita, Masanori
AU - Yoshimura, Akihiko
AU - Sumizawa, Tomoyuki
AU - Douzono, Haruhiko
AU - Nagata, Yukihiro
AU - Akiyama, Shin‐Ichi ‐I
PY - 1990/3/15
Y1 - 1990/3/15
N2 - One thousand fungi and Actinomycetes were investigated to see whether they produced compounds that reverse multidrug resistance in KB cells. Only one Aspergillus strain M39 produced agents with resistance‐reversing activity and these compounds were identified to be rubrofusarin B and dianhydro‐aurasperone C. Rubrofusarin B only slightly reversed the resistance of KB‐C2 cells to Adriamycin and daunomycin, partially reversed the resistance to chromomycin A3, and almost completely reversed the resistance to vincristine and mitomycin C. Purified dianhydro‐aurasperone C and rubrofusarin B had similar effects on drug resistance in KB‐8‐5 cells. Dianhydro‐aurasperone C enhanced the accumulation of vinblastine in KB‐8‐5 cells and inhibited the efflux of vinblastine from the cells. Dianhydro‐aurasperone C and rubrofusarin B at 10 μ M completely inhibited 3H‐azidopine photolabelling of P‐glycoprotein. The two products of Aspergillus strain M39 appear to reverse multi‐drug resistance by interacting with P‐glycoprotein and inhibiting its role as an active efflux pump.
AB - One thousand fungi and Actinomycetes were investigated to see whether they produced compounds that reverse multidrug resistance in KB cells. Only one Aspergillus strain M39 produced agents with resistance‐reversing activity and these compounds were identified to be rubrofusarin B and dianhydro‐aurasperone C. Rubrofusarin B only slightly reversed the resistance of KB‐C2 cells to Adriamycin and daunomycin, partially reversed the resistance to chromomycin A3, and almost completely reversed the resistance to vincristine and mitomycin C. Purified dianhydro‐aurasperone C and rubrofusarin B had similar effects on drug resistance in KB‐8‐5 cells. Dianhydro‐aurasperone C enhanced the accumulation of vinblastine in KB‐8‐5 cells and inhibited the efflux of vinblastine from the cells. Dianhydro‐aurasperone C and rubrofusarin B at 10 μ M completely inhibited 3H‐azidopine photolabelling of P‐glycoprotein. The two products of Aspergillus strain M39 appear to reverse multi‐drug resistance by interacting with P‐glycoprotein and inhibiting its role as an active efflux pump.
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U2 - 10.1002/ijc.2910450323
DO - 10.1002/ijc.2910450323
M3 - Article
C2 - 1968438
AN - SCOPUS:0025228907
SN - 0020-7136
VL - 45
SP - 508
EP - 513
JO - International Journal of Cancer
JF - International Journal of Cancer
IS - 3
ER -
