Effects of fangchinoline derivative LYY-32 on biological properties of BLM DNA helicase
- VernacularTitle:汉防己乙素衍生物LYY-32对Bloom综合征解旋酶生物学特性的影响
- Author:
Wang-ming ZHANG
1
;
Qin-ying FENG
;
Xiao-yu SONG
;
Xin-zhong ZHOU
;
Juan LU
;
Wan-qing XIE
;
Zhi-wen LAI
;
Wei-dong PAN
;
Jie-lin LIU
Author Information
- Publication Type:Journal Article
- Keywords: BLM DNA helicase; fangchinoline deriva-tive; binding activity; ATPase activity; unwinding ac-tivity; fluorescence polarization
- From: Chinese Pharmacological Bulletin 2025;41(9):1680-1686
- CountryChina
- Language:Chinese
- Abstract: Aim To investigate the effects of the fangchinoline derivative LYY-32 on the biological prop-erties of the BLM642-1290 DNA helicase,in order to lay a foundation for further research on its antitumor activity.Methods Fluorescence polarization assay,malachite green-phosphate and ammonium molybdate colorime-try,and fluorescein-labeled DNA gel electrophoresis experiments were conducted to study the effects of fangchinoline derivative LYY-32 on the DNA binding activity,ATPase activity,and DNA unwinding activity of BLM642-1290 DNA helicase.The effects of LYY-32 on the DNA unwinding activity of DNA helicase in cells were studied using fluorescent techniques and time-lapse microscopy.Ultraviolet spectral scanning was used to investigate the effects of LYY-32 on the confor-mation of the BLM642-1290 DNA helicase.Results At a concentration of 10 μmol·L-1,the inhibition rate of LYY-32 on BLM642-1290 DNA helicase binding to dsDNA was 53.17％.At a concentration of 5 μmol·L-1,the inhibition rate of LYY-32 on BLM642-1290 DNA helicase binding to ssDNA was 88.49％.The inhibition rate of LYY-32 on the ATPase activity of BLM642-1290 DNA he-licase was 89.3％at a concentration of 50 μmol·L-1.When the concentration of LYY-32 exceeded 5μmol·L-1,its inhibition rate on the DNA unwinding activity of BLM642-1290 DNA helicase was 100％.LYY-32 also significantly inhibited the DNA unwinding ac-tivity of DNA helicase in cells.However,LYY-32 had no effect on the conformation of BLM642-1290 DNA heli-case.Conclusion The DNA binding activity,AT-Pase activity,and DNA unwinding activity of BLM642-1290 DNA helicase could be significantly inhibi-ted by the fangchinoline derivative LYY-32.
