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Author Spotlight: Development and Evaluation of a Compound Acne Rodent Model Using C. acnes and Oleic Acid

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Anticomplement compounds from Polygonum chinense.

Hao-Chuan Zheng¹, Yan Lu², Dao-Feng Chen¹

¹State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China; Department of Pharmacognosy, School of Pharmacy, Fudan University, Shanghai 201203, China.

Bioorganic & Medicinal Chemistry Letters

|April 11, 2018

Summary

This summary is machine-generated.

This study isolated novel compounds from Polygonum chinense, revealing potent anticomplement activity. Phenyldilactones and phenylpropionic tyramines are identified as new anticomplement agents, targeting the complement activation cascade.

Keywords:

Anticomplement Phenyldilactones Phenylpropionic tyramines Polygonum chinense Traditional Chinese medicines

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Area of Science:

Natural Product Chemistry
Immunology
Pharmacology

Background:

Polygonum chinense is a medicinal plant with a history of traditional use.
The complement system plays a crucial role in innate immunity and inflammation.
Identifying novel modulators of the complement system is important for therapeutic development.

Purpose of the Study:

To isolate and characterize new chemical constituents from Polygonum chinense.
To evaluate the anticomplement activity of isolated compounds.
To identify the specific targets of active compounds within the complement activation cascade.

Main Methods:

Isolation and purification of compounds using chromatographic techniques.
Structure elucidation of new compounds via detailed spectral analysis (NMR, MS).
Determination of absolute configurations using Mosher's method, electronic circular dichroism (ECD) data, and ECD calculation.
Assessment of anticomplement activity using CH50 and AP50 assays.

Main Results:

Five new compounds (two phenyldilactones, two coumarins, one N-E-feruloyl tyramine dimer) and 23 known compounds were isolated.
All tested compounds exhibited potent anticomplement activity.
Phenyldilactones and phenylpropionic tyramines were identified as novel anticomplement agents.
Specific targets in the complement activation cascade were identified for compounds 1, 3, 5, and 10.

Conclusions:

Polygonum chinense is a rich source of bioactive natural products.
The identified phenyldilactones and phenylpropionic tyramines represent a new class of anticomplement agents.
Further investigation into these compounds may lead to the development of novel immunomodulatory therapies.