2. Academic Validation
  3. (-)-Neocaryachine, an Antiproliferative Pavine Alkaloid from Cryptocarya laevigata, Induces DNA Double-Strand Breaks

(-)-Neocaryachine, an Antiproliferative Pavine Alkaloid from Cryptocarya laevigata, Induces DNA Double-Strand Breaks

  • J Nat Prod. 2017 Jan 27;80(1):220-224. doi: 10.1021/acs.jnatprod.6b01153.
Yuki Suzuki 1,  Yohei Saito 1,  Masuo Goto 2,  David J Newman 3,  Barry R O'Keefe,  Kuo-Hsiung Lee 2 4 5,  Kyoko Nakagawa-Goto 1 2
Affiliations

Affiliations

  • 1 School of Pharmaceutical Sciences, College of Medical, Pharmaceutical and Health Sciences, Kanazawa University , Kanazawa, 920-1192, Japan.
  • 2 Natural Products Research Laboratories, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill , Chapel Hill, North Carolina 27599-7568, United States.
  • 3 NIH Special Volunteer, Wayne, Pennsylvania 19087, United States.
  • 4 Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill , Chapel Hill, North Carolina 27599-7295, United States.
  • 5 Chinese Medicine Research and Development Center, China Medical University and Hospital , 2 Yuh-Der Road, Taichung, 40447, Taiwan.
PMID: 28099003 DOI: 10.1021/acs.jnatprod.6b01153
Abstract

Twelve benzylisoquinoline Alkaloids, including pavine and phenanthroindolizidine types, were isolated from a MeOH/CH2Cl2 extract of Cryptocarya laevigata (stem bark) through bioactivity-guided fractionation for antitumor effects. Selected compounds were evaluated for antiproliferative activity against five human tumor cell lines, including a multidrug-resistant subline. Since more common 2,3,8,9-tetrasubstituted pavine Alkaloids, such as crychine (3), exhibit very mild or no cytotoxicity, this compound type has not been well investigated for antitumor activity. Thus, this report is the first discovery of a 7-hydroxylated pavine alkaloid, (-)-neocaryachine (1), to demonstrate strong antiproliferative activity, with IC50 values of 0.06 to 0.41 μM against five tested tumor cell lines, including an MDR subline. Further mechanism of action studies revealed that 1 impacts the cellular S-phase by inducing DNA double-strand breaks.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z