Anticomplement compounds from Polygonum chinense

[Display omitted] •Isolation and structure elucidation of five new compounds from Polygonum chinense.•Phenyldilactones and phenylpropionic tyramines were firstly found to show anticomplement activity.•The targets of the bioactive compounds in complement activation cascade were identified. Five new c...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2018-05, Vol.28 (9), p.1495-1500
Main Authors: Zheng, Hao-chuan, Lu, Yan, Chen, Dao-feng
Format: Article
Language:English
Subjects:
Anticomplement
Complement Inactivator Proteins - chemistry
Complement Inactivator Proteins - isolation & purification
Complement Inactivator Proteins - pharmacology
Coumarins - chemistry
Coumarins - isolation & purification
Coumarins - pharmacology
Dose-Response Relationship, Drug
Hemolysis - drug effects
Lactones - chemistry
Lactones - isolation & purification
Lactones - pharmacology
Molecular Structure
Phenyldilactones
Phenylpropionic tyramines
Plants, Medicinal
Polygonum - chemistry
Polygonum chinense
Structure-Activity Relationship
Traditional Chinese medicines
Tyramine - analogs & derivatives
Tyramine - chemistry
Tyramine - pharmacology
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Summary:[Display omitted] •Isolation and structure elucidation of five new compounds from Polygonum chinense.•Phenyldilactones and phenylpropionic tyramines were firstly found to show anticomplement activity.•The targets of the bioactive compounds in complement activation cascade were identified. Five new compounds including two phenyldilactones (1, 2), two coumarins (3, 4) and a dimer of N-E-feruloyl tyramine (5) together with twenty-three known compounds (6–28) were isolated from a medicinal plant Polygonum chinense. The structures of the new compounds were established by detailed spectral analysis. The absolute configurations of 1 and 5 were elucidated by Mosher’s method, Mo2(OAc)4-induced electronic circular dichroism (ECD) data, and ECD calculation. All the compounds were found to show potent anticomplement activity with CH50 and AP50 values ranging from 0.18 to 1.45 mM, and 0.26 to 2.80 mM, respectively. Phenyldilactones and phenylpropionic tyramines were firstly reported as anticomplement agents. The targets of compounds 1, 3, 5 and 10 in complement activation cascade were identified as well.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2018.03.079